Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
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name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Potency)		 # tested GPCRs
(Potency)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
11583188 138752 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Activity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assayActivity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assay
ChEMBL 448 4 0 5 3.3 COc1ccccc1N1CCN(Cc2cn3cc(I)ccc3n2)CC1 10.1021/jm060166w
CHEMBL379125 138752 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Activity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assayActivity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assay
ChEMBL 448 4 0 5 3.3 COc1ccccc1N1CCN(Cc2cn3cc(I)ccc3n2)CC1 10.1021/jm060166w
44400674 124669 0 None 1 2 Human 9.3 pEC50 = 9.3 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL None None None None 10.1021/jm050170s
CHEMBL364516 124669 0 None 1 2 Human 9.3 pEC50 = 9.3 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL None None None None 10.1021/jm050170s
17449900 139012 12 None -2 3 Human 9.2 pEC50 = 9.2 Functional
Intrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 348 5 0 5 3.2 COc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2006.02.075
CHEMBL379602 139012 12 None -2 3 Human 9.2 pEC50 = 9.2 Functional
Intrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 348 5 0 5 3.2 COc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2006.02.075
16094675 81745 1 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 315 4 1 4 3.3 Cc1cccc(NC(=O)CN2CCC(c3nccs3)CC2)c1 10.1021/jm060662k
CHEMBL216922 81745 1 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 315 4 1 4 3.3 Cc1cccc(NC(=O)CN2CCC(c3nccs3)CC2)c1 10.1021/jm060662k
10359019 82912 5 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 326 4 1 2 4.0 Cc1cccc(NC(=O)CN2CCC(c3ccccc3F)CC2)c1 10.1021/jm060662k
CHEMBL219129 82912 5 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 326 4 1 2 4.0 Cc1cccc(NC(=O)CN2CCC(c3ccccc3F)CC2)c1 10.1021/jm060662k
10088259 101443 3 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 334 4 1 4 2.4 Cc1ccc(C(=O)NCN2CCN(c3ccccc3C#N)CC2)cc1 10.1021/jm970021c
CHEMBL300956 101443 3 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 334 4 1 4 2.4 Cc1ccc(C(=O)NCN2CCN(c3ccccc3C#N)CC2)cc1 10.1021/jm970021c
44400585 68313 0 None 2 2 Human 8.9 pEC50 = 8.9 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL None None None None 10.1021/jm050170s
CHEMBL191962 68313 0 None 2 2 Human 8.9 pEC50 = 8.9 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL None None None None 10.1021/jm050170s
2 3210 19 None -2 7 Human 8.9 pEC50 = 8.9 Functional
Activity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assayActivity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm060166w
54562 3210 19 None -2 7 Human 8.9 pEC50 = 8.9 Functional
Activity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assayActivity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm060166w
CHEMBL240773 3210 19 None -2 7 Human 8.9 pEC50 = 8.9 Functional
Activity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assayActivity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm060166w
11725531 53769 1 None - 1 Human 8.8 pEC50 = 8.8 Functional
Tested for the effective concentration against human D4.2 receptor in CHO 10001 cells established in mitogenesis assayTested for the effective concentration against human D4.2 receptor in CHO 10001 cells established in mitogenesis assay
ChEMBL 351 3 0 5 3.2 N#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
CHEMBL160626 53769 1 None - 1 Human 8.8 pEC50 = 8.8 Functional
Tested for the effective concentration against human D4.2 receptor in CHO 10001 cells established in mitogenesis assayTested for the effective concentration against human D4.2 receptor in CHO 10001 cells established in mitogenesis assay
ChEMBL 351 3 0 5 3.2 N#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
6469918 79481 13 None - 1 Human 8.7 pEC50 = 8.7 Functional
Activity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assayActivity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assay
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1 10.1021/jm060166w
CHEMBL212370 79481 13 None - 1 Human 8.7 pEC50 = 8.7 Functional
Activity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assayActivity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assay
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1 10.1021/jm060166w
681 1437 65 None -7 12 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
940 1437 65 None -7 12 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
947 1437 65 None -7 12 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
CHEMBL59 1437 65 None -7 12 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
DB00988 1437 65 None -7 12 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
155559617 174312 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assayAgonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4563944 174312 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assayAgonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
44400585 68313 0 None 2 2 Human 8.7 pEC50 = 8.7 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL None None None None 10.1021/jm050170s
CHEMBL191962 68313 0 None 2 2 Human 8.7 pEC50 = 8.7 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL None None None None 10.1021/jm050170s
10378194 196088 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 265 3 1 2 2.3 C#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1 10.1016/s0960-894x(02)00316-5
CHEMBL57176 196088 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 265 3 1 2 2.3 C#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1 10.1016/s0960-894x(02)00316-5
681 1437 65 None -7 12 Human 8.0 pEC50 = 8 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm0604979
940 1437 65 None -7 12 Human 8.0 pEC50 = 8 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm0604979
947 1437 65 None -7 12 Human 8.0 pEC50 = 8 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm0604979
CHEMBL59 1437 65 None -7 12 Human 8.0 pEC50 = 8 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm0604979
DB00988 1437 65 None -7 12 Human 8.0 pEC50 = 8 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm0604979
10383724 82998 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 357 5 1 4 2.9 CSc1cccc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
CHEMBL219570 82998 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 357 5 1 4 2.9 CSc1cccc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
16094681 82934 0 None -1 2 Rat 7.0 pEC50 = 7 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 343 4 1 3 2.6 Cc1cc(F)ccc1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
CHEMBL219261 82934 0 None -1 2 Rat 7.0 pEC50 = 7 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 343 4 1 3 2.6 Cc1cc(F)ccc1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
16094684 136077 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 347 4 1 3 2.4 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1ccc(F)cc1F 10.1021/jm060662k
CHEMBL373964 136077 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 347 4 1 3 2.4 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1ccc(F)cc1F 10.1021/jm060662k
10065188 101133 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 329 4 1 3 2.9 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccccc1 10.1021/jm970021c
CHEMBL298763 101133 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 329 4 1 3 2.9 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccccc1 10.1021/jm970021c
155568867 175580 0 None -3 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 297 4 1 5 1.2 O=C(CN1CCN(c2ccccn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
CHEMBL4592753 175580 0 None -3 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 297 4 1 5 1.2 O=C(CN1CCN(c2ccccn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
11221906 79501 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(C)c(C)c1 10.1021/jm060279f
CHEMBL212444 79501 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(C)c(C)c1 10.1021/jm060279f
155536720 171621 0 None 37 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 359 4 1 3 3.9 Cc1cccc(NC(=O)CN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4473652 171621 0 None 37 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 359 4 1 3 3.9 Cc1cccc(NC(=O)CN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/acs.jmedchem.9b00231
11849262 79707 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 337 7 0 4 3.6 CCO/N=C(\CCN1CCN(c2ccccc2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL213246 79707 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 337 7 0 4 3.6 CCO/N=C(\CCN1CCN(c2ccccc2)CC1)c1ccccc1 10.1021/jm060279f
2 3210 19 None -2 7 Human 8.0 pEC50 = 8.0 Functional
Intrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmcl.2006.02.075
54562 3210 19 None -2 7 Human 8.0 pEC50 = 8.0 Functional
Intrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmcl.2006.02.075
CHEMBL240773 3210 19 None -2 7 Human 8.0 pEC50 = 8.0 Functional
Intrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmcl.2006.02.075
11849223 79437 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 344 5 1 5 3.1 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(Cl)c1 10.1021/jm060279f
CHEMBL212189 79437 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 344 5 1 5 3.1 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(Cl)c1 10.1021/jm060279f
25142456 81994 2 None -3 2 Human 7.0 pEC50 = 7.0 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)C1c3ccccc3CNC1CO2 10.1021/jm0604979
CHEMBL217299 81994 2 None -3 2 Human 7.0 pEC50 = 7.0 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)C1c3ccccc3CNC1CO2 10.1021/jm0604979
44418745 82997 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 337 5 1 3 3.8 CCc1cccc(C)c1NC(=O)CN1CCC(c2ccccn2)CC1 10.1021/jm060662k
CHEMBL219567 82997 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 337 5 1 3 3.8 CCc1cccc(C)c1NC(=O)CN1CCC(c2ccccn2)CC1 10.1021/jm060662k
11325818 79378 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 358 6 0 5 3.3 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(Cl)c1 10.1021/jm060279f
CHEMBL211930 79378 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 358 6 0 5 3.3 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(Cl)c1 10.1021/jm060279f
10428669 83052 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 361 4 1 3 3.0 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1ccc2ccccc2c1 10.1021/jm060662k
CHEMBL220015 83052 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 361 4 1 3 3.0 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1ccc2ccccc2c1 10.1021/jm060662k
9835713 18300 1 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 292 3 1 3 3.3 c1ccc(C2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm060662k
CHEMBL127226 18300 1 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 292 3 1 3 3.3 c1ccc(C2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm060662k
10404144 203591 19 None - 1 Human 7.9 pEC50 = 7.9 Functional
Tested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assayTested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assay
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(01)00814-9
CHEMBL7927 203591 19 None - 1 Human 7.9 pEC50 = 7.9 Functional
Tested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assayTested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assay
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(01)00814-9
10361512 54154 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Tested for the effective concentration against human D4.2 receptor in CHO 10001 cells established in mitogenesis assayTested for the effective concentration against human D4.2 receptor in CHO 10001 cells established in mitogenesis assay
ChEMBL 365 3 0 5 3.5 Cc1nn2c(C#N)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
CHEMBL160932 54154 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Tested for the effective concentration against human D4.2 receptor in CHO 10001 cells established in mitogenesis assayTested for the effective concentration against human D4.2 receptor in CHO 10001 cells established in mitogenesis assay
ChEMBL 365 3 0 5 3.5 Cc1nn2c(C#N)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
168285560 192316 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Partial agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assayPartial agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assay
ChEMBL 350 5 0 4 2.6 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccn2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5196873 192316 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Partial agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assayPartial agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assay
ChEMBL 350 5 0 4 2.6 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccn2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222201 192316 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Partial agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assayPartial agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assay
ChEMBL 350 5 0 4 2.6 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccn2)CC1 10.1021/acs.jmedchem.2c00840
5025739 168630 40 None 1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm060662k
CHEMBL440687 168630 40 None 1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm060662k
44414898 138377 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 341 6 1 7 1.0 CO/N=C(/c1cccnc1)C(O)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
CHEMBL378302 138377 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 341 6 1 7 1.0 CO/N=C(/c1cccnc1)C(O)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
10316440 141134 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 359 4 1 3 3.1 Cc1ccc(Cl)cc1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
CHEMBL385417 141134 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 359 4 1 3 3.1 Cc1ccc(Cl)cc1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
16094706 141377 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 346 4 1 4 1.9 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1cnccc1Cl 10.1021/jm060662k
CHEMBL386917 141377 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 346 4 1 4 1.9 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1cnccc1Cl 10.1021/jm060662k
10382581 100828 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2cccc(C)c2)CC1 10.1021/jm970021c
CHEMBL296506 100828 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2cccc(C)c2)CC1 10.1021/jm970021c
44400626 70059 0 None -2 2 Human 7.9 pEC50 = 7.9 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL None None None None 10.1021/jm050170s
CHEMBL194555 70059 0 None -2 2 Human 7.9 pEC50 = 7.9 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL None None None None 10.1021/jm050170s
11849638 79604 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 335 5 1 6 2.3 N#Cc1cccc(/C(CCN2CCN(c3ccccn3)CC2)=N/O)c1 10.1021/jm060279f
CHEMBL212847 79604 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 335 5 1 6 2.3 N#Cc1cccc(/C(CCN2CCN(c3ccccn3)CC2)=N/O)c1 10.1021/jm060279f
11772242 165734 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 342 6 0 5 2.8 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL427048 165734 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 342 6 0 5 2.8 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
9861462 82921 0 None -5 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 309 3 2 5 2.0 Oc1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm060662k
CHEMBL219179 82921 0 None -5 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 309 3 2 5 2.0 Oc1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm060662k
5025739 168630 40 None -1 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm060662k
CHEMBL440687 168630 40 None -1 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm060662k
16094682 83066 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 370 5 1 5 2.4 Cc1ccc([N+](=O)[O-])cc1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
CHEMBL220139 83066 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 370 5 1 5 2.4 Cc1ccc([N+](=O)[O-])cc1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
11280225 80684 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 372 6 0 5 3.6 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)c(C)c1 10.1021/jm060279f
CHEMBL215569 80684 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 372 6 0 5 3.6 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)c(C)c1 10.1021/jm060279f
10430781 82865 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 395 5 1 4 3.0 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cccc(OC(F)(F)F)c1 10.1021/jm060662k
CHEMBL218852 82865 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 395 5 1 4 3.0 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cccc(OC(F)(F)F)c1 10.1021/jm060662k
11849734 79742 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 363 7 0 6 2.9 CCO/N=C(\CCN1CCN(c2ncccc2C#N)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL213398 79742 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 363 7 0 6 2.9 CCO/N=C(\CCN1CCN(c2ncccc2C#N)CC1)c1ccccc1 10.1021/jm060279f
10425450 199 23 None 125 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/jm060662k
3301 199 23 None 125 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/jm060662k
CHEMBL375596 199 23 None 125 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/jm060662k
44400519 132608 0 None -2 2 Human 7.9 pEC50 = 7.9 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL None None None None 10.1021/jm050170s
CHEMBL370297 132608 0 None -2 2 Human 7.9 pEC50 = 7.9 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL None None None None 10.1021/jm050170s
681 1437 65 None -7 12 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
940 1437 65 None -7 12 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
947 1437 65 None -7 12 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
CHEMBL59 1437 65 None -7 12 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
DB00988 1437 65 None -7 12 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
16094672 82856 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 397 4 1 3 4.9 O=C(CN1CCC(c2ccccn2)CC1)Nc1c(Cl)cc(Cl)cc1Cl 10.1021/jm060662k
CHEMBL218797 82856 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 397 4 1 3 4.9 O=C(CN1CCC(c2ccccn2)CC1)Nc1c(Cl)cc(Cl)cc1Cl 10.1021/jm060662k
11451703 138489 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 376 6 0 5 3.4 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(F)c(Cl)c1 10.1021/jm060279f
CHEMBL378576 138489 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 376 6 0 5 3.4 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(F)c(Cl)c1 10.1021/jm060279f
10642239 186077 1 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1021/jm970021c
CHEMBL48819 186077 1 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1021/jm970021c
119570 3110 90 None -11 7 Human 7.8 pEC50 = 7.8 Functional
Effective concentration required for agonistic activity against human D4.2 receptorEffective concentration required for agonistic activity against human D4.2 receptor
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
2233 3110 90 None -11 7 Human 7.8 pEC50 = 7.8 Functional
Effective concentration required for agonistic activity against human D4.2 receptorEffective concentration required for agonistic activity against human D4.2 receptor
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
953 3110 90 None -11 7 Human 7.8 pEC50 = 7.8 Functional
Effective concentration required for agonistic activity against human D4.2 receptorEffective concentration required for agonistic activity against human D4.2 receptor
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
CHEMBL301265 3110 90 None -11 7 Human 7.8 pEC50 = 7.8 Functional
Effective concentration required for agonistic activity against human D4.2 receptorEffective concentration required for agonistic activity against human D4.2 receptor
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
DB00413 3110 90 None -11 7 Human 7.8 pEC50 = 7.8 Functional
Effective concentration required for agonistic activity against human D4.2 receptorEffective concentration required for agonistic activity against human D4.2 receptor
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
16094666 81315 2 None 251 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL216393 81315 2 None 251 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/acs.jmedchem.9b00231
10022369 83075 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 375 5 1 4 2.5 COc1cc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)ccc1Cl 10.1021/jm060662k
CHEMBL220192 83075 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 375 5 1 4 2.5 COc1cc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)ccc1Cl 10.1021/jm060662k
10665101 101055 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 343 4 1 3 3.2 Cc1cccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)c1 10.1021/jm970021c
CHEMBL298166 101055 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 343 4 1 3 3.2 Cc1cccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)c1 10.1021/jm970021c
10404144 203591 19 None - 1 Human 7.8 pEC50 = 7.8 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(02)00316-5
CHEMBL7927 203591 19 None - 1 Human 7.8 pEC50 = 7.8 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(02)00316-5
168268756 192162 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assay
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5171439 192162 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assay
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5221187 192162 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assay
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
16094678 82972 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 329 4 1 3 2.3 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cccc(F)c1 10.1021/jm060662k
CHEMBL219417 82972 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 329 4 1 3 2.3 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cccc(F)c1 10.1021/jm060662k
10045314 165430 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 379 4 1 3 3.4 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cc(Cl)cc(Cl)c1 10.1021/jm060662k
CHEMBL425288 165430 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 379 4 1 3 3.4 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cc(Cl)cc(Cl)c1 10.1021/jm060662k
11175610 137597 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 7 0 5 3.4 CC(C)O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL376639 137597 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 7 0 5 3.4 CC(C)O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
6603820 95330 13 None -1 7 Human 7.8 pEC50 = 7.8 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm0604979
CHEMBL25856 95330 13 None -1 7 Human 7.8 pEC50 = 7.8 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm0604979
3645619 2985 13 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm970021c
975 2985 13 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm970021c
CHEMBL45244 2985 13 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm970021c
1353 1880 85 None -7 27 Human 7.8 pEC50 = 7.8 Functional
Agonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assayAgonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(03)00587-0
3559 1880 85 None -7 27 Human 7.8 pEC50 = 7.8 Functional
Agonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assayAgonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(03)00587-0
86 1880 85 None -7 27 Human 7.8 pEC50 = 7.8 Functional
Agonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assayAgonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(03)00587-0
CHEMBL54 1880 85 None -7 27 Human 7.8 pEC50 = 7.8 Functional
Agonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assayAgonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(03)00587-0
DB00502 1880 85 None -7 27 Human 7.8 pEC50 = 7.8 Functional
Agonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assayAgonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(03)00587-0
11849636 79436 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 328 5 1 5 2.6 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(F)c1 10.1021/jm060279f
CHEMBL212188 79436 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 328 5 1 5 2.6 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(F)c1 10.1021/jm060279f
11849225 79769 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 346 5 1 5 2.8 O/N=C(/CCN1CCN(c2ccccn2)CC1)c1cc(F)cc(F)c1 10.1021/jm060279f
CHEMBL213518 79769 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 346 5 1 5 2.8 O/N=C(/CCN1CCN(c2ccccn2)CC1)c1cc(F)cc(F)c1 10.1021/jm060279f
16094666 81315 2 None 251 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/jm060662k
CHEMBL216393 81315 2 None 251 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/jm060662k
16094705 82951 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 429 5 1 4 3.4 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1ccc(OC(F)(F)F)c(Cl)c1 10.1021/jm060662k
CHEMBL219340 82951 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 429 5 1 4 3.4 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1ccc(OC(F)(F)F)c(Cl)c1 10.1021/jm060662k
11325645 138148 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cc(C)cc(C)c1 10.1021/jm060279f
CHEMBL377794 138148 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cc(C)cc(C)c1 10.1021/jm060279f
44415054 80717 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 335 5 1 6 2.3 N#Cc1cccnc1N1CCN(CC/C(=N\O)c2ccccc2)CC1 10.1021/jm060279f
CHEMBL215670 80717 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 335 5 1 6 2.3 N#Cc1cccnc1N1CCN(CC/C(=N\O)c2ccccc2)CC1 10.1021/jm060279f
9997550 136076 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 343 4 1 3 2.6 Cc1cc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)ccc1F 10.1021/jm060662k
CHEMBL373963 136076 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 343 4 1 3 2.6 Cc1cc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)ccc1F 10.1021/jm060662k
10339711 82994 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 379 4 1 3 3.4 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cccc(Cl)c1Cl 10.1021/jm060662k
CHEMBL219564 82994 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 379 4 1 3 3.4 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cccc(Cl)c1Cl 10.1021/jm060662k
11849777 138103 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 402 6 0 5 3.4 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Br)cc1 10.1021/jm060279f
CHEMBL377585 138103 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 402 6 0 5 3.4 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Br)cc1 10.1021/jm060279f
2 3210 19 None -2 7 Human 7.7 pEC50 = 7.7 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm050170s
54562 3210 19 None -2 7 Human 7.7 pEC50 = 7.7 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm050170s
CHEMBL240773 3210 19 None -2 7 Human 7.7 pEC50 = 7.7 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm050170s
135407844 79674 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 340 5 2 6 2.5 Cc1ccc(O)c(/C(CCN2CCN(c3ccccn3)CC2)=N/O)c1 10.1021/jm060279f
CHEMBL213106 79674 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 340 5 2 6 2.5 Cc1ccc(O)c(/C(CCN2CCN(c3ccccn3)CC2)=N/O)c1 10.1021/jm060279f
11849639 79947 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 346 5 1 5 2.8 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1cc(F)cc(F)c1 10.1021/jm060279f
CHEMBL214343 79947 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 346 5 1 5 2.8 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1cc(F)cc(F)c1 10.1021/jm060279f
11849816 77725 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 357 6 0 4 4.4 CO/N=C(\CCN1CCC(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL210101 77725 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 357 6 0 4 4.4 CO/N=C(\CCN1CCC(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
11849822 79699 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 388 7 0 6 2.9 CO/N=C(\c1ccc(Cl)cc1)C(CN1CCN(c2ccccn2)CC1)OC 10.1021/jm060279f
CHEMBL213208 79699 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 388 7 0 6 2.9 CO/N=C(\c1ccc(Cl)cc1)C(CN1CCN(c2ccccn2)CC1)OC 10.1021/jm060279f
2 3210 19 None -2 7 Human 8.7 pEC50 = 8.7 Functional
Tested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assayTested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(01)00814-9
54562 3210 19 None -2 7 Human 8.7 pEC50 = 8.7 Functional
Tested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assayTested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(01)00814-9
CHEMBL240773 3210 19 None -2 7 Human 8.7 pEC50 = 8.7 Functional
Tested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assayTested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(01)00814-9
2 3210 19 None -2 7 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assayAgonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b01085
54562 3210 19 None -2 7 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assayAgonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b01085
CHEMBL240773 3210 19 None -2 7 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assayAgonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b01085
681 1437 65 None -7 12 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
940 1437 65 None -7 12 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
947 1437 65 None -7 12 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
CHEMBL59 1437 65 None -7 12 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
DB00988 1437 65 None -7 12 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
2 3210 19 None -2 7 Human 8.7 pEC50 = 8.7 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(02)00316-5
54562 3210 19 None -2 7 Human 8.7 pEC50 = 8.7 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(02)00316-5
CHEMBL240773 3210 19 None -2 7 Human 8.7 pEC50 = 8.7 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(02)00316-5
11849637 79463 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 324 5 1 5 2.8 Cc1cccc(/C(CCN2CCN(c3ccccn3)CC2)=N/O)c1 10.1021/jm060279f
CHEMBL212298 79463 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 324 5 1 5 2.8 Cc1cccc(/C(CCN2CCN(c3ccccn3)CC2)=N/O)c1 10.1021/jm060279f
9861462 82921 0 None 5 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 309 3 2 5 2.0 Oc1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm060662k
CHEMBL219179 82921 0 None 5 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 309 3 2 5 2.0 Oc1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm060662k
681 1437 65 None -1 12 Rat 8.6 pEC50 = 8.6 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
940 1437 65 None -1 12 Rat 8.6 pEC50 = 8.6 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
947 1437 65 None -1 12 Rat 8.6 pEC50 = 8.6 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
CHEMBL59 1437 65 None -1 12 Rat 8.6 pEC50 = 8.6 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
DB00988 1437 65 None -1 12 Rat 8.6 pEC50 = 8.6 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
44400674 124669 0 None 1 2 Human 8.6 pEC50 = 8.6 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL None None None None 10.1021/jm050170s
CHEMBL364516 124669 0 None 1 2 Human 8.6 pEC50 = 8.6 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL None None None None 10.1021/jm050170s
6469918 79481 13 None - 1 Human 8.6 pEC50 = 8.6 Functional
Activity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS bindingActivity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS binding
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1 10.1021/jm060166w
CHEMBL212370 79481 13 None - 1 Human 8.6 pEC50 = 8.6 Functional
Activity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS bindingActivity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS binding
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1 10.1021/jm060166w
2 3210 19 None -2 7 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acsmedchemlett.9b00050
54562 3210 19 None -2 7 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acsmedchemlett.9b00050
CHEMBL240773 3210 19 None -2 7 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acsmedchemlett.9b00050
10425450 199 23 None 125 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
3301 199 23 None 125 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
CHEMBL375596 199 23 None 125 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
11439072 168393 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 335 5 1 6 2.3 N#Cc1cccnc1N1CCN(CC/C(=N/O)c2ccccc2)CC1 10.1021/jm060279f
CHEMBL438961 168393 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 335 5 1 6 2.3 N#Cc1cccnc1N1CCN(CC/C(=N/O)c2ccccc2)CC1 10.1021/jm060279f
11849635 79969 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 324 5 1 5 2.8 Cc1ccccc1/C(CCN1CCN(c2ccccn2)CC1)=N\O 10.1021/jm060279f
CHEMBL214440 79969 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 324 5 1 5 2.8 Cc1ccccc1/C(CCN1CCN(c2ccccn2)CC1)=N\O 10.1021/jm060279f
681 1437 65 None -7 12 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
940 1437 65 None -7 12 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
947 1437 65 None -7 12 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
CHEMBL59 1437 65 None -7 12 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
DB00988 1437 65 None -7 12 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
11849182 79459 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 417 9 1 7 2.7 CO/N=C(/c1ccc(Cl)cc1)C(CNOC)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
CHEMBL212288 79459 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 417 9 1 7 2.7 CO/N=C(/c1ccc(Cl)cc1)C(CNOC)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
16094698 137343 4 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 338 5 1 3 3.6 COc1ccccc1C1CCN(CNC(=O)c2cccc(C)c2)CC1 10.1021/jm060662k
CHEMBL376092 137343 4 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 338 5 1 3 3.6 COc1ccccc1C1CCN(CNC(=O)c2cccc(C)c2)CC1 10.1021/jm060662k
44417647 81749 0 None 52 3 Human 7.7 pEC50 = 7.7 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 311 2 2 4 3.2 CCCN1Cc2ccccc2C2c3cc(O)c(O)cc3OCC21 10.1021/jm0604979
CHEMBL1203924 81749 0 None 52 3 Human 7.7 pEC50 = 7.7 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 311 2 2 4 3.2 CCCN1Cc2ccccc2C2c3cc(O)c(O)cc3OCC21 10.1021/jm0604979
CHEMBL216945 81749 0 None 52 3 Human 7.7 pEC50 = 7.7 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 311 2 2 4 3.2 CCCN1Cc2ccccc2C2c3cc(O)c(O)cc3OCC21 10.1021/jm0604979
11301354 141116 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 310 5 1 5 2.5 O/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL385350 141116 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 310 5 1 5 2.5 O/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
10617381 189094 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 343 4 1 3 3.2 Cc1ccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)cc1 10.1021/jm970021c
CHEMBL51536 189094 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 343 4 1 3 3.2 Cc1ccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)cc1 10.1021/jm970021c
44400553 70435 0 None -2 2 Human 7.7 pEC50 = 7.7 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL None None None None 10.1021/jm050170s
CHEMBL195083 70435 0 None -2 2 Human 7.7 pEC50 = 7.7 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL None None None None 10.1021/jm050170s
11849821 168734 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 374 6 1 6 2.3 CO/N=C(/c1ccc(Cl)cc1)C(O)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
CHEMBL441529 168734 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 374 6 1 6 2.3 CO/N=C(/c1ccc(Cl)cc1)C(O)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
44400553 70435 0 None -2 2 Human 7.6 pEC50 = 7.6 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL None None None None 10.1021/jm050170s
CHEMBL195083 70435 0 None -2 2 Human 7.6 pEC50 = 7.6 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL None None None None 10.1021/jm050170s
2 3210 19 None -2 7 Human 7.6 pEC50 = 7.6 Functional
Intrinsic activity against dopamine D4 receptor expressed in CHO cells by GTPgammaS assayIntrinsic activity against dopamine D4 receptor expressed in CHO cells by GTPgammaS assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmcl.2006.02.075
54562 3210 19 None -2 7 Human 7.6 pEC50 = 7.6 Functional
Intrinsic activity against dopamine D4 receptor expressed in CHO cells by GTPgammaS assayIntrinsic activity against dopamine D4 receptor expressed in CHO cells by GTPgammaS assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmcl.2006.02.075
CHEMBL240773 3210 19 None -2 7 Human 7.6 pEC50 = 7.6 Functional
Intrinsic activity against dopamine D4 receptor expressed in CHO cells by GTPgammaS assayIntrinsic activity against dopamine D4 receptor expressed in CHO cells by GTPgammaS assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmcl.2006.02.075
24878061 140879 0 None 4 2 Human 6.6 pEC50 = 6.6 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)[C@@H]1c3ccccc3CN[C@H]1CO2 10.1021/jm0604979
CHEMBL384046 140879 0 None 4 2 Human 6.6 pEC50 = 6.6 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)[C@@H]1c3ccccc3CN[C@H]1CO2 10.1021/jm0604979
11849633 80166 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 344 5 1 5 3.1 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1Cl 10.1021/jm060279f
CHEMBL214954 80166 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 344 5 1 5 3.1 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1Cl 10.1021/jm060279f
9883554 164802 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 320 4 1 4 2.1 N#Cc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1021/jm970021c
CHEMBL423659 164802 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 320 4 1 4 2.1 N#Cc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1021/jm970021c
11163137 141205 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 324 6 0 5 2.6 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL385826 141205 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 324 6 0 5 2.6 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
16094671 82964 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 357 4 1 3 4.2 Cc1cc(Cl)cc(C)c1NC(=O)CN1CCC(c2ccccn2)CC1 10.1021/jm060662k
CHEMBL219392 82964 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 357 4 1 3 4.2 Cc1cc(Cl)cc(C)c1NC(=O)CN1CCC(c2ccccn2)CC1 10.1021/jm060662k
10338536 81722 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 359 4 1 3 2.8 Cc1cc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)ccc1Cl 10.1021/jm060662k
CHEMBL216721 81722 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 359 4 1 3 2.8 Cc1cc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)ccc1Cl 10.1021/jm060662k
11269392 77656 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 392 6 0 5 4.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)cc1Cl 10.1021/jm060279f
CHEMBL209759 77656 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 392 6 0 5 4.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)cc1Cl 10.1021/jm060279f
11849634 141091 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 344 5 1 5 3.1 O/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccccc1Cl 10.1021/jm060279f
CHEMBL385230 141091 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 344 5 1 5 3.1 O/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccccc1Cl 10.1021/jm060279f
11849265 139010 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 7 0 5 3.3 CCO/N=C(\CCN1CCN(c2ncccc2C)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL379597 139010 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 7 0 5 3.3 CCO/N=C(\CCN1CCN(c2ncccc2C)CC1)c1ccccc1 10.1021/jm060279f
11738945 79537 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 328 5 0 5 2.4 CO/N=C(/CN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL212595 79537 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 328 5 0 5 2.4 CO/N=C(/CN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
2653640 65887 12 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5
ChEMBL 339 5 1 4 2.8 COc1ccccc1N1CCN(CC(=O)Nc2cccc(C)c2)CC1 10.1016/j.bmcl.2004.07.068
CHEMBL184486 65887 12 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5
ChEMBL 339 5 1 4 2.8 COc1ccccc1N1CCN(CC(=O)Nc2cccc(C)c2)CC1 10.1016/j.bmcl.2004.07.068
11849263 160390 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 367 8 0 5 3.6 CCO/N=C(\CCN1CCN(c2cccc(OC)c2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL411545 160390 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 367 8 0 5 3.6 CCO/N=C(\CCN1CCN(c2cccc(OC)c2)CC1)c1ccccc1 10.1021/jm060279f
681 1437 65 None -7 12 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
940 1437 65 None -7 12 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
947 1437 65 None -7 12 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
CHEMBL59 1437 65 None -7 12 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
DB00988 1437 65 None -7 12 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
3303 2213 41 None 1 5 Human 7.6 pEC50 = 7.6 Functional
Tested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assayTested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00814-9
5311200 2213 41 None 1 5 Human 7.6 pEC50 = 7.6 Functional
Tested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assayTested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00814-9
CHEMBL267014 2213 41 None 1 5 Human 7.6 pEC50 = 7.6 Functional
Tested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assayTested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00814-9
11849776 79362 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 349 6 0 6 2.5 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(C#N)c1 10.1021/jm060279f
CHEMBL211836 79362 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 349 6 0 6 2.5 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(C#N)c1 10.1021/jm060279f
11739255 79608 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 6 0 5 3.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(C)c1 10.1021/jm060279f
CHEMBL212861 79608 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 6 0 5 3.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(C)c1 10.1021/jm060279f
10042205 136423 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 329 4 1 3 2.3 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1ccccc1F 10.1021/jm060662k
CHEMBL374326 136423 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 329 4 1 3 2.3 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1ccccc1F 10.1021/jm060662k
11256262 79591 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 7 0 5 3.0 CCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL212782 79591 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 7 0 5 3.0 CCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
45361874 169454 2 None 58 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 324 5 1 4 2.4 CCc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4442548 169454 2 None 58 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 324 5 1 4 2.4 CCc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
11474734 79515 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 388 7 0 6 2.9 CO/N=C(/c1ccc(Cl)cc1)C(CN1CCN(c2ccccn2)CC1)OC 10.1021/jm060279f
CHEMBL212490 79515 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 388 7 0 6 2.9 CO/N=C(/c1ccc(Cl)cc1)C(CN1CCN(c2ccccn2)CC1)OC 10.1021/jm060279f
16094685 83218 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 317 4 1 3 1.9 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)NC1CCCCC1 10.1021/jm060662k
CHEMBL220469 83218 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 317 4 1 3 1.9 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)NC1CCCCC1 10.1021/jm060662k
11292299 79360 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 392 6 0 5 4.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)cc1Cl 10.1021/jm060279f
CHEMBL211829 79360 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 392 6 0 5 4.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)cc1Cl 10.1021/jm060279f
6469693 79545 17 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assayActivity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assay
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cn3ccccc3n2)CC1 10.1021/jm060166w
CHEMBL212631 79545 17 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assayActivity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assay
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cn3ccccc3n2)CC1 10.1021/jm060166w
10593191 188519 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2ccc(C)cc2)CC1 10.1021/jm970021c
CHEMBL51023 188519 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2ccc(C)cc2)CC1 10.1021/jm970021c
6466372 169495 12 None 58 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 311 4 1 5 1.5 Cc1cccc(NC(=O)CN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4443054 169495 12 None 58 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 311 4 1 5 1.5 Cc1cccc(NC(=O)CN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
4797946 169856 8 None 81 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 310 4 1 4 2.2 Cc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4448320 169856 8 None 81 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 310 4 1 4 2.2 Cc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
16094704 81744 1 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 325 4 2 4 2.9 Cc1cccc(NC(=O)CN2CCC(c3ccc(O)cn3)CC2)c1 10.1021/jm060662k
CHEMBL216921 81744 1 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 325 4 2 4 2.9 Cc1cccc(NC(=O)CN2CCC(c3ccc(O)cn3)CC2)c1 10.1021/jm060662k
11849224 79623 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 328 5 1 5 2.6 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL212902 79623 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 328 5 1 5 2.6 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
10616050 186064 3 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 325 5 1 4 2.2 COc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1021/jm970021c
CHEMBL48807 186064 3 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 325 5 1 4 2.2 COc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1021/jm970021c
2 3210 19 None -2 7 Human 7.5 pEC50 = 7.5 Functional
Agonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesisAgonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(01)00484-x
54562 3210 19 None -2 7 Human 7.5 pEC50 = 7.5 Functional
Agonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesisAgonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(01)00484-x
CHEMBL240773 3210 19 None -2 7 Human 7.5 pEC50 = 7.5 Functional
Agonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesisAgonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(01)00484-x
10247720 12943 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesisAgonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesis
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL1190042 12943 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesisAgonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesis
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL540039 12943 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesisAgonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesis
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
10018402 81721 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 312 4 1 4 1.3 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1ccccn1 10.1021/jm060662k
CHEMBL216719 81721 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 312 4 1 4 1.3 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1ccccn1 10.1021/jm060662k
11324794 137731 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 324 6 0 5 2.6 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL377050 137731 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 324 6 0 5 2.6 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
16094677 82923 0 None 1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 325 4 1 3 2.4 Cc1cccc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
CHEMBL219185 82923 0 None 1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 325 4 1 3 2.4 Cc1cccc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
11198974 79600 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 8 0 5 3.4 CCCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL212831 79600 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 8 0 5 3.4 CCCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
11849299 78985 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 430 9 0 6 3.9 CO/N=C(/c1ccc(Cl)cc1)C(COC(C)C)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
CHEMBL211360 78985 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 430 9 0 6 3.9 CO/N=C(/c1ccc(Cl)cc1)C(COC(C)C)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
10405923 82990 3 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 355 6 1 4 2.3 CCOc1cccc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
CHEMBL219551 82990 3 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 355 6 1 4 2.3 CCOc1cccc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
11849229 137646 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 349 7 0 6 2.5 N#CCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL376955 137646 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 349 7 0 6 2.5 N#CCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
11370781 79461 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 325 6 0 6 2.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccnc1 10.1021/jm060279f
CHEMBL212291 79461 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 325 6 0 6 2.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccnc1 10.1021/jm060279f
11849820 77600 0 None 10 2 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 356 7 0 5 3.2 CO/N=C(/CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL209645 77600 0 None 10 2 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 356 7 0 5 3.2 CO/N=C(/CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
11849267 79462 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 372 6 0 5 3.7 CO/N=C(\CCN1CCN(c2ccccn2)CC1C)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL212292 79462 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 372 6 0 5 3.7 CO/N=C(\CCN1CCN(c2ccccn2)CC1C)c1ccc(Cl)cc1 10.1021/jm060279f
11849730 79539 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 367 8 0 5 3.6 CCO/N=C(\CCN1CCN(c2ccccc2OC)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL212607 79539 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 367 8 0 5 3.6 CCO/N=C(\CCN1CCN(c2ccccc2OC)CC1)c1ccccc1 10.1021/jm060279f
11849180 79398 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 354 6 1 6 2.4 COC(CN1CCN(c2ccccn2)CC1)/C(=N\O)c1cccc(C)c1 10.1021/jm060279f
CHEMBL212028 79398 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 354 6 1 6 2.4 COC(CN1CCN(c2ccccn2)CC1)/C(=N\O)c1cccc(C)c1 10.1021/jm060279f
16094668 82913 3 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 322 4 1 2 4.1 Cc1cccc(NC(=O)CN2CCC(c3ccccc3C)CC2)c1 10.1021/jm060662k
CHEMBL219130 82913 3 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 322 4 1 2 4.1 Cc1cccc(NC(=O)CN2CCC(c3ccccc3C)CC2)c1 10.1021/jm060662k
10405922 82995 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 355 5 1 4 2.5 COc1cccc(C)c1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
CHEMBL219565 82995 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 355 5 1 4 2.5 COc1cccc(C)c1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
11849780 79773 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 392 6 0 5 4.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm060279f
CHEMBL213558 79773 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 392 6 0 5 4.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm060279f
16094683 137347 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 393 4 1 3 3.8 Cc1ccc(Cl)c(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1Cl 10.1021/jm060662k
CHEMBL376196 137347 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 393 4 1 3 3.8 Cc1ccc(Cl)c(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1Cl 10.1021/jm060662k
10042826 165586 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 339 4 1 3 2.8 Cc1cccc(C)c1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
CHEMBL426167 165586 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 339 4 1 3 2.8 Cc1cccc(C)c1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
44415055 80729 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 381 9 0 5 4.0 CCO/N=C(\CCN1CCN(c2cccc(OCC)c2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL215704 80729 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 381 9 0 5 4.0 CCO/N=C(\CCN1CCN(c2cccc(OCC)c2)CC1)c1ccccc1 10.1021/jm060279f
155530763 171003 0 None -2 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 323 5 1 3 3.6 Cc1cccc(NC(=O)CCN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4464861 171003 0 None -2 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 323 5 1 3 3.6 Cc1cccc(NC(=O)CCN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
44400519 132608 0 None -2 2 Human 7.5 pEC50 = 7.5 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL None None None None 10.1021/jm050170s
CHEMBL370297 132608 0 None -2 2 Human 7.5 pEC50 = 7.5 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL None None None None 10.1021/jm050170s
11849684 79805 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 350 8 0 5 3.2 C=CCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL213700 79805 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 350 8 0 5 3.2 C=CCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
16094674 141135 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 334 4 1 4 3.1 Cc1cccc(NC(=O)CN2CCC(c3cccc(C#N)n3)CC2)c1 10.1021/jm060662k
CHEMBL385418 141135 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 334 4 1 4 3.1 Cc1cccc(NC(=O)CN2CCC(c3cccc(C#N)n3)CC2)c1 10.1021/jm060662k
16094708 165520 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 387 5 1 3 3.8 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cccc(-c2ccccc2)c1 10.1021/jm060662k
CHEMBL425793 165520 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 387 5 1 3 3.8 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cccc(-c2ccccc2)c1 10.1021/jm060662k
11164276 79342 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 360 6 0 5 2.9 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cc(F)cc(F)c1 10.1021/jm060279f
CHEMBL211732 79342 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 360 6 0 5 2.9 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cc(F)cc(F)c1 10.1021/jm060279f
11199162 79449 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 358 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL212235 79449 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 358 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
10404935 82996 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 339 4 1 3 2.5 Cc1ccc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)cc1C 10.1021/jm060662k
CHEMBL219566 82996 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 339 4 1 3 2.5 Cc1ccc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)cc1C 10.1021/jm060662k
11849228 95969 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 366 9 0 5 3.8 CCCCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL261957 95969 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 366 9 0 5 3.8 CCCCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
11151081 79385 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 311 5 1 6 1.9 O/N=C(\CCN1CCN(c2ncccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL211972 79385 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 311 5 1 6 1.9 O/N=C(\CCN1CCN(c2ncccn2)CC1)c1ccccc1 10.1021/jm060279f
11849222 80807 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 324 5 1 5 2.8 Cc1ccccc1/C(CCN1CCN(c2ccccn2)CC1)=N/O 10.1021/jm060279f
CHEMBL215849 80807 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 324 5 1 5 2.8 Cc1ccccc1/C(CCN1CCN(c2ccccn2)CC1)=N/O 10.1021/jm060279f
228 441 26 None -1 8 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
33 441 26 None -1 8 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
6005 441 26 None -1 8 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
CHEMBL53 441 26 None -1 8 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
DB00714 441 26 None -1 8 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
11185987 79938 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 310 5 1 5 2.5 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL214314 79938 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 310 5 1 5 2.5 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
6469693 79545 17 None - 1 Human 8.4 pEC50 = 8.4 Functional
Activity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS bindingActivity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS binding
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cn3ccccc3n2)CC1 10.1021/jm060166w
CHEMBL212631 79545 17 None - 1 Human 8.4 pEC50 = 8.4 Functional
Activity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS bindingActivity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS binding
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cn3ccccc3n2)CC1 10.1021/jm060166w
11849179 80733 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 340 5 2 6 1.8 Cc1cccc(/C(=N/O)C(O)CN2CCN(c3ccccn3)CC2)c1 10.1021/jm060279f
CHEMBL215723 80733 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 340 5 2 6 1.8 Cc1cccc(/C(=N/O)C(O)CN2CCN(c3ccccn3)CC2)c1 10.1021/jm060279f
44418748 169891 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 339 5 1 4 3.2 COc1cccc(C)c1NC(=O)CN1CCC(c2ccccn2)CC1 10.1021/jm060662k
CHEMBL444881 169891 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 339 5 1 4 3.2 COc1cccc(C)c1NC(=O)CN1CCC(c2ccccn2)CC1 10.1021/jm060662k
11450607 79762 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 6 0 5 3.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccccc1C 10.1021/jm060279f
CHEMBL213486 79762 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 6 0 5 3.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccccc1C 10.1021/jm060279f
155552185 173489 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assayAgonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4544086 173489 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assayAgonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
11849819 79836 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 356 7 0 5 3.2 CO/N=C(\CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL213828 79836 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 356 7 0 5 3.2 CO/N=C(\CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
11371795 79410 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 358 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1Cl 10.1021/jm060279f
CHEMBL212073 79410 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 358 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1Cl 10.1021/jm060279f
10472323 82846 4 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 338 5 1 3 3.8 COc1ccccc1C1CCN(CC(=O)Nc2cccc(C)c2)CC1 10.1021/jm060662k
CHEMBL218761 82846 4 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 338 5 1 3 3.8 COc1ccccc1C1CCN(CC(=O)Nc2cccc(C)c2)CC1 10.1021/jm060662k
11849817 138401 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 314 4 1 5 2.2 O/N=C(\CN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL378427 138401 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 314 4 1 5 2.2 O/N=C(\CN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
11771801 79619 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 328 5 0 5 2.4 CO/N=C(\CN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL212891 79619 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 328 5 0 5 2.4 CO/N=C(\CN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
10084583 104299 3 None -151 3 Human 6.4 pEC50 = 6.4 Functional
Effective concentration required for agonistic activity against human D4.2 receptorEffective concentration required for agonistic activity against human D4.2 receptor
ChEMBL 271 5 0 3 3.3 CCCN(CCC)[C@H]1CCc2nn3ccccc3c2C1 10.1016/s0960-894x(02)00390-6
CHEMBL310867 104299 3 None -151 3 Human 6.4 pEC50 = 6.4 Functional
Effective concentration required for agonistic activity against human D4.2 receptorEffective concentration required for agonistic activity against human D4.2 receptor
ChEMBL 271 5 0 3 3.3 CCCN(CCC)[C@H]1CCc2nn3ccccc3c2C1 10.1016/s0960-894x(02)00390-6
11849775 165643 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 342 6 0 5 2.8 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(F)c1 10.1021/jm060279f
CHEMBL426510 165643 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 342 6 0 5 2.8 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(F)c1 10.1021/jm060279f
11849823 79195 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 340 5 2 6 1.8 Cc1cccc(/C(=N\O)C(O)CN2CCN(c3ccccn3)CC2)c1 10.1021/jm060279f
CHEMBL211463 79195 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 340 5 2 6 1.8 Cc1cccc(/C(=N\O)C(O)CN2CCN(c3ccccn3)CC2)c1 10.1021/jm060279f
11151919 79776 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 7 0 5 3.0 CCO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL213572 79776 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 7 0 5 3.0 CCO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
10385089 141198 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 379 4 1 3 3.2 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1cc(Cl)cc(Cl)c1 10.1021/jm060662k
CHEMBL385781 141198 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 379 4 1 3 3.2 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1cc(Cl)cc(Cl)c1 10.1021/jm060662k
11849681 79391 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 5 1 5 3.1 Cc1cc(C)cc(/C(CCN2CCN(c3ccccn3)CC2)=N/O)c1 10.1021/jm060279f
CHEMBL211985 79391 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 5 1 5 3.1 Cc1cc(C)cc(/C(CCN2CCN(c3ccccn3)CC2)=N/O)c1 10.1021/jm060279f
11849181 79650 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 372 6 0 5 3.5 CO/N=C(/c1ccc(Cl)cc1)C(C)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
CHEMBL213004 79650 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 372 6 0 5 3.5 CO/N=C(/c1ccc(Cl)cc1)C(C)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
11211058 79924 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 374 6 1 6 2.3 CO/N=C(\c1ccc(Cl)cc1)C(O)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
CHEMBL214247 79924 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 374 6 1 6 2.3 CO/N=C(\c1ccc(Cl)cc1)C(O)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
11187957 139000 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 373 6 0 4 3.6 CO/N=C(/CCN1CCC(c2cccc[n+]2[O-])CC1)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL379546 139000 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 373 6 0 4 3.6 CO/N=C(/CCN1CCC(c2cccc[n+]2[O-])CC1)c1ccc(Cl)cc1 10.1021/jm060279f
11849778 80730 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 360 6 0 5 2.9 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cc(F)cc(F)c1 10.1021/jm060279f
CHEMBL215705 80730 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 360 6 0 5 2.9 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cc(F)cc(F)c1 10.1021/jm060279f
16094709 82922 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 397 4 1 3 3.3 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1ccc(F)cc1C(F)(F)F 10.1021/jm060662k
CHEMBL219181 82922 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 397 4 1 3 3.3 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1ccc(F)cc1C(F)(F)F 10.1021/jm060662k
11473427 140975 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 344 5 1 5 3.1 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL384529 140975 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 344 5 1 5 3.1 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
11849184 79622 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 364 5 0 5 3.2 CCO/N=C1/c2ccccc2CCC1CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
CHEMBL212901 79622 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 364 5 0 5 3.2 CCO/N=C1/c2ccccc2CCC1CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
11849729 141370 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 362 7 0 5 3.5 CCO/N=C(\CCN1CCN(c2ccccc2C#N)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL386867 141370 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 362 7 0 5 3.5 CCO/N=C(\CCN1CCN(c2ccccc2C#N)CC1)c1ccccc1 10.1021/jm060279f
11325334 79641 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 342 6 0 5 2.8 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL212969 79641 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 342 6 0 5 2.8 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
2 3210 19 None -2 7 Human 7.3 pEC50 = 7.3 Functional
Activity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS bindingActivity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS binding
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm060166w
54562 3210 19 None -2 7 Human 7.3 pEC50 = 7.3 Functional
Activity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS bindingActivity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS binding
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm060166w
CHEMBL240773 3210 19 None -2 7 Human 7.3 pEC50 = 7.3 Functional
Activity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS bindingActivity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS binding
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm060166w
2 3210 19 None -2 7 Human 7.3 pEC50 = 7.3 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm050170s
54562 3210 19 None -2 7 Human 7.3 pEC50 = 7.3 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm050170s
CHEMBL240773 3210 19 None -2 7 Human 7.3 pEC50 = 7.3 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm050170s
3038495 700 30 None -91 7 Human 7.3 pEC50 = 7.3 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm050170s
7625 700 30 None -91 7 Human 7.3 pEC50 = 7.3 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm050170s
CHEMBL25236 700 30 None -91 7 Human 7.3 pEC50 = 7.3 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm050170s
11849688 79527 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 316 5 1 6 2.5 O/N=C(\CCN1CCN(c2nccs2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL212545 79527 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 316 5 1 6 2.5 O/N=C(\CCN1CCN(c2nccs2)CC1)c1ccccc1 10.1021/jm060279f
2 3210 19 None -2 7 Human 8.3 pEC50 = 8.3 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0604979
54562 3210 19 None -2 7 Human 8.3 pEC50 = 8.3 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0604979
CHEMBL240773 3210 19 None -2 7 Human 8.3 pEC50 = 8.3 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0604979
9975465 187068 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1021/jm970021c
CHEMBL49502 187068 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1021/jm970021c
228 441 26 None 1 8 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
33 441 26 None 1 8 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
6005 441 26 None 1 8 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
CHEMBL53 441 26 None 1 8 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
DB00714 441 26 None 1 8 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
44301054 194474 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 266 3 1 3 2.2 N#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1 10.1016/s0960-894x(02)00316-5
CHEMBL56118 194474 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 266 3 1 3 2.2 N#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1 10.1016/s0960-894x(02)00316-5
11983282 138414 0 None -2 3 Human 8.3 pEC50 = 8.3 Functional
Intrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 315 4 0 3 4.2 C1=C(c2ccccc2)CCN(Cc2cnn(-c3ccccc3)c2)C1 10.1016/j.bmcl.2006.02.075
CHEMBL378455 138414 0 None -2 3 Human 8.3 pEC50 = 8.3 Functional
Intrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 315 4 0 3 4.2 C1=C(c2ccccc2)CCN(Cc2cnn(-c3ccccc3)c2)C1 10.1016/j.bmcl.2006.02.075
10088811 82924 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 343 4 1 3 2.3 Cc1cc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)ccc1F 10.1021/jm060662k
CHEMBL219186 82924 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 343 4 1 3 2.3 Cc1cc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)ccc1F 10.1021/jm060662k
168285556 192315 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assay
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5196870 192315 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assay
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222200 192315 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assay
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
10064956 135863 5 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 326 4 1 2 4.0 Cc1cccc(NC(=O)CN2CCC(c3cccc(F)c3)CC2)c1 10.1021/jm060662k
CHEMBL373516 135863 5 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 326 4 1 2 4.0 Cc1cccc(NC(=O)CN2CCC(c3cccc(F)c3)CC2)c1 10.1021/jm060662k
10020098 82927 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 339 4 1 3 2.8 Cc1cc(C)cc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
CHEMBL219210 82927 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 339 4 1 3 2.8 Cc1cc(C)cc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
10335627 82974 3 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 311 4 1 3 1.9 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1ccccc1 10.1021/jm060662k
CHEMBL219426 82974 3 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 311 4 1 3 1.9 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1ccccc1 10.1021/jm060662k
11849298 79324 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 354 6 1 6 2.4 COC(CN1CCN(c2ccccn2)CC1)/C(=N/O)c1cccc(C)c1 10.1021/jm060279f
CHEMBL211623 79324 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 354 6 1 6 2.4 COC(CN1CCN(c2ccccn2)CC1)/C(=N/O)c1cccc(C)c1 10.1021/jm060279f
155513053 169131 0 None 23 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 323 5 1 3 3.5 CCc1cccc(NC(=O)CN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4437912 169131 0 None 23 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 323 5 1 3 3.5 CCc1cccc(NC(=O)CN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
16094697 136704 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 308 3 1 3 2.6 [O-][n+]1ccccc1C1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm060662k
CHEMBL375120 136704 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 308 3 1 3 2.6 [O-][n+]1ccccc1C1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm060662k
11200205 138382 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 392 6 0 5 4.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm060279f
CHEMBL378324 138382 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 392 6 0 5 4.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm060279f
16094679 82864 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 369 6 1 4 2.9 CC(C)Oc1cccc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
CHEMBL218851 82864 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 369 6 1 4 2.9 CC(C)Oc1cccc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
11314352 79450 1 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 358 6 0 5 3.3 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL212236 79450 1 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 358 6 0 5 3.3 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
109030515 175412 1 None 14 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 325 5 1 5 1.9 Cc1cccc(NC(=O)CCN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4588808 175412 1 None 14 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 325 5 1 5 1.9 Cc1cccc(NC(=O)CCN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
16094677 82923 0 None -1 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 325 4 1 3 2.4 Cc1cccc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
CHEMBL219185 82923 0 None -1 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 325 4 1 3 2.4 Cc1cccc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
11849774 79460 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 358 6 0 5 3.3 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccccc1Cl 10.1021/jm060279f
CHEMBL212290 79460 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 358 6 0 5 3.3 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccccc1Cl 10.1021/jm060279f
11849269 79142 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 342 6 1 5 3.0 O/N=C(/CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL211415 79142 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 342 6 1 5 3.0 O/N=C(/CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
71452737 78681 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 399 8 0 5 4.2 CO/N=C(\CCN1CCN(c2ccccc2OC(C)C)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL2113243 78681 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 399 8 0 5 4.2 CO/N=C(\CCN1CCN(c2ccccc2OC(C)C)CC1)c1ccc(F)cc1 10.1021/jm060279f
44300865 200310 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 317 4 1 2 4.0 c1ccc(-c2c[nH]c(CN3CCN(c4ccccc4)CC3)c2)cc1 10.1016/s0960-894x(02)00316-5
CHEMBL60815 200310 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 317 4 1 2 4.0 c1ccc(-c2c[nH]c(CN3CCN(c4ccccc4)CC3)c2)cc1 10.1016/s0960-894x(02)00316-5
16094681 82934 0 None 1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 343 4 1 3 2.6 Cc1cc(F)ccc1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
CHEMBL219261 82934 0 None 1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 343 4 1 3 2.6 Cc1cc(F)ccc1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
44418747 82965 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 343 4 1 3 3.9 Cc1cccc(Cl)c1NC(=O)CN1CCC(c2ccccn2)CC1 10.1021/jm060662k
CHEMBL219394 82965 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 343 4 1 3 3.9 Cc1cccc(Cl)c1NC(=O)CN1CCC(c2ccccn2)CC1 10.1021/jm060662k
5311189 203133 4 None -2 4 Human 7.2 pEC50 = 7.2 Functional
Effective concentration required for agonistic activity against human D4.2 receptorEffective concentration required for agonistic activity against human D4.2 receptor
ChEMBL 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 10.1016/s0960-894x(02)00390-6
CHEMBL7549 203133 4 None -2 4 Human 7.2 pEC50 = 7.2 Functional
Effective concentration required for agonistic activity against human D4.2 receptorEffective concentration required for agonistic activity against human D4.2 receptor
ChEMBL 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 10.1016/s0960-894x(02)00390-6
11336814 79691 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 342 6 0 5 2.8 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(F)c1 10.1021/jm060279f
CHEMBL213164 79691 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 342 6 0 5 2.8 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(F)c1 10.1021/jm060279f
71456253 78682 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 399 8 0 5 4.2 CO/N=C(/CCN1CCN(c2ccccc2OC(C)C)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL2113244 78682 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 399 8 0 5 4.2 CO/N=C(/CCN1CCN(c2ccccc2OC(C)C)CC1)c1ccc(F)cc1 10.1021/jm060279f
11739823 79361 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 357 6 0 4 4.4 CO/N=C(\CCN1CCCC(c2ccccn2)C1)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL211831 79361 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 357 6 0 4 4.4 CO/N=C(\CCN1CCCC(c2ccccn2)C1)c1ccc(Cl)cc1 10.1021/jm060279f
11151920 79624 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 6 0 5 3.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(C)c1 10.1021/jm060279f
CHEMBL212903 79624 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 6 0 5 3.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(C)c1 10.1021/jm060279f
109030343 170293 1 None 1 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 324 5 1 4 2.5 Cc1cccc(NC(=O)CCN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4454068 170293 1 None 1 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 324 5 1 4 2.5 Cc1cccc(NC(=O)CCN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
11849735 137704 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 339 7 0 6 2.4 CCO/N=C(\CCN1CCN(c2ncccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL377023 137704 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 339 7 0 6 2.4 CCO/N=C(\CCN1CCN(c2ncccn2)CC1)c1ccccc1 10.1021/jm060279f
10066168 161300 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 345 4 1 3 2.8 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cccc(Cl)c1 10.1021/jm060662k
CHEMBL414706 161300 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 345 4 1 3 2.8 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cccc(Cl)c1 10.1021/jm060662k
10428816 82935 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 363 4 1 3 2.7 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1ccc(F)c(Cl)c1 10.1021/jm060662k
CHEMBL219263 82935 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 363 4 1 3 2.7 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1ccc(F)c(Cl)c1 10.1021/jm060662k
11256583 168221 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 349 6 0 6 2.5 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(C#N)c1 10.1021/jm060279f
CHEMBL437493 168221 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 349 6 0 6 2.5 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(C#N)c1 10.1021/jm060279f
10024158 82928 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 403 4 1 3 3.2 Cc1cc(Br)ccc1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
CHEMBL219211 82928 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 403 4 1 3 3.2 Cc1cc(Br)ccc1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
10404821 168115 4 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 337 5 1 3 2.5 C=Cc1cccc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
CHEMBL436527 168115 4 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 337 5 1 3 2.5 C=Cc1cccc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
10383571 82845 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 355 5 1 4 2.2 COc1cccc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)c1C 10.1021/jm060662k
CHEMBL218757 82845 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 355 5 1 4 2.2 COc1cccc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)c1C 10.1021/jm060662k
11849687 79596 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 311 5 1 6 1.9 O/N=C(/CCN1CCN(c2ncccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL212804 79596 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 311 5 1 6 1.9 O/N=C(/CCN1CCN(c2ncccn2)CC1)c1ccccc1 10.1021/jm060279f
11724450 123330 4 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL184158 123330 4 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL362542 123330 4 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.bmcl.2004.07.068
44400626 70059 0 None -2 2 Human 8.1 pEC50 = 8.1 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL None None None None 10.1021/jm050170s
CHEMBL194555 70059 0 None -2 2 Human 8.1 pEC50 = 8.1 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL None None None None 10.1021/jm050170s
16094670 83042 5 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 324 4 2 3 3.5 Cc1cccc(NC(=O)CN2CCC(c3ccc(O)cc3)CC2)c1 10.1021/jm060662k
CHEMBL219966 83042 5 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 324 4 2 3 3.5 Cc1cccc(NC(=O)CN2CCC(c3ccc(O)cc3)CC2)c1 10.1021/jm060662k
11772112 168251 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 6 0 5 3.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1C 10.1021/jm060279f
CHEMBL437687 168251 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 6 0 5 3.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1C 10.1021/jm060279f
11849779 79485 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 6 0 5 3.3 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cc(C)cc(C)c1 10.1021/jm060279f
CHEMBL212393 79485 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 6 0 5 3.3 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cc(C)cc(C)c1 10.1021/jm060279f
16094707 96278 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 379 4 1 3 3.2 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cccc(C(F)(F)F)c1 10.1021/jm060662k
CHEMBL264286 96278 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 379 4 1 3 3.2 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cccc(C(F)(F)F)c1 10.1021/jm060662k
16094667 81430 5 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 333 4 1 3 3.7 Cc1cccc(NC(=O)CN2CCC(c3ccccc3C#N)CC2)c1 10.1021/jm060662k
CHEMBL216450 81430 5 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 333 4 1 3 3.7 Cc1cccc(NC(=O)CN2CCC(c3ccccc3C#N)CC2)c1 10.1021/jm060662k
16094700 169156 4 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 324 4 2 3 3.5 Cc1cccc(NC(=O)CN2CCC(c3cccc(O)c3)CC2)c1 10.1021/jm060662k
CHEMBL443838 169156 4 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 324 4 2 3 3.5 Cc1cccc(NC(=O)CN2CCC(c3cccc(O)c3)CC2)c1 10.1021/jm060662k
3645619 2985 13 None -1 2 Human 8.1 pEC50 = 8.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm060279f
975 2985 13 None -1 2 Human 8.1 pEC50 = 8.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm060279f
CHEMBL45244 2985 13 None -1 2 Human 8.1 pEC50 = 8.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm060279f
3645619 2985 13 None -1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm060662k
975 2985 13 None -1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm060662k
CHEMBL45244 2985 13 None -1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm060662k
10737474 100883 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 363 4 1 3 3.5 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccc(Cl)cc1 10.1021/jm970021c
CHEMBL296953 100883 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 363 4 1 3 3.5 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccc(Cl)cc1 10.1021/jm970021c
10473658 186610 3 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1021/jm970021c
CHEMBL49231 186610 3 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1021/jm970021c
168285560 192316 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Partial agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assayPartial agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assay
ChEMBL 350 5 0 4 2.6 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccn2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5196873 192316 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Partial agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assayPartial agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assay
ChEMBL 350 5 0 4 2.6 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccn2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222201 192316 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Partial agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assayPartial agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assay
ChEMBL 350 5 0 4 2.6 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccn2)CC1 10.1021/acs.jmedchem.2c00840
155515982 169443 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assayAgonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assay
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4442460 169443 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assayAgonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assay
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
11849682 79909 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 346 5 1 5 2.8 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1F 10.1021/jm060279f
CHEMBL214190 79909 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 346 5 1 5 2.8 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1F 10.1021/jm060279f
11849736 137887 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 344 7 0 6 3.1 CCO/N=C(\CCN1CCN(c2nccs2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL377388 137887 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 344 7 0 6 3.1 CCO/N=C(\CCN1CCN(c2nccs2)CC1)c1ccccc1 10.1021/jm060279f
11774041 79610 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 402 6 0 5 3.4 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(Br)cc1 10.1021/jm060279f
CHEMBL212872 79610 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 402 6 0 5 3.4 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(Br)cc1 10.1021/jm060279f
11394708 79672 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 373 6 0 4 3.6 CO/N=C(\CCN1CCC(c2cccc[n+]2[O-])CC1)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL213097 79672 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 373 6 0 4 3.6 CO/N=C(\CCN1CCC(c2cccc[n+]2[O-])CC1)c1ccc(Cl)cc1 10.1021/jm060279f
10359645 141004 4 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 336 4 1 4 1.8 N#Cc1cccc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
CHEMBL384690 141004 4 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 336 4 1 4 1.8 N#Cc1cccc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
10385883 81159 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 393 4 1 3 3.2 Cc1ccc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)cc1C(F)(F)F 10.1021/jm060662k
CHEMBL216215 81159 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 393 4 1 3 3.2 Cc1ccc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)cc1C(F)(F)F 10.1021/jm060662k
10314506 168111 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 329 4 1 3 2.3 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1ccc(F)cc1 10.1021/jm060662k
CHEMBL436491 168111 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 329 4 1 3 2.3 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1ccc(F)cc1 10.1021/jm060662k
11772767 79592 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 358 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(Cl)c1 10.1021/jm060279f
CHEMBL212784 79592 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 358 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(Cl)c1 10.1021/jm060279f
16094676 230 17 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 325 4 1 3 2.2 Cc1cccc(c1)C(=O)NCN1CCC(CC1)c1cccc[n+]1[O-] 10.1021/jm060662k
8439 230 17 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 325 4 1 3 2.2 Cc1cccc(c1)C(=O)NCN1CCC(CC1)c1cccc[n+]1[O-] 10.1021/jm060662k
CHEMBL219182 230 17 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 325 4 1 3 2.2 Cc1cccc(c1)C(=O)NCN1CCC(CC1)c1cccc[n+]1[O-] 10.1021/jm060662k
16094699 81733 4 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 309 4 1 3 3.0 Cc1cccc(C(=O)NCN2CCC(c3ccccn3)CC2)c1 10.1021/jm060662k
CHEMBL216794 81733 4 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 309 4 1 3 3.0 Cc1cccc(C(=O)NCN2CCC(c3ccccn3)CC2)c1 10.1021/jm060662k
9859861 167517 1 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assayAgonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assay
ChEMBL 218 0 1 2 3.2 Cc1sc(C)c2c1CCCc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
CHEMBL432579 167517 1 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assayAgonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assay
ChEMBL 218 0 1 2 3.2 Cc1sc(C)c2c1CCCc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
10314824 35153 1 None - 1 Human 8.0 pEC50 = 8.0 Functional
Effective dose was measured by the stimulation of mitogenesis at dopamine D4.2 receptorEffective dose was measured by the stimulation of mitogenesis at dopamine D4.2 receptor
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(F)cc4)CC3)cc2c1 10.1021/jm0009989
CHEMBL143761 35153 1 None - 1 Human 8.0 pEC50 = 8.0 Functional
Effective dose was measured by the stimulation of mitogenesis at dopamine D4.2 receptorEffective dose was measured by the stimulation of mitogenesis at dopamine D4.2 receptor
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(F)cc4)CC3)cc2c1 10.1021/jm0009989
11849818 77564 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 342 6 1 5 3.0 O/N=C(\CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL209447 77564 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 342 6 1 5 3.0 O/N=C(\CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
11983282 138414 0 None -2 3 Human 8.0 pEC50 = 8.0 Functional
Intrinsic activity against dopamine D4 receptor expressed in CHO cells by GTPgammaS assayIntrinsic activity against dopamine D4 receptor expressed in CHO cells by GTPgammaS assay
ChEMBL 315 4 0 3 4.2 C1=C(c2ccccc2)CCN(Cc2cnn(-c3ccccc3)c2)C1 10.1016/j.bmcl.2006.02.075
CHEMBL378455 138414 0 None -2 3 Human 8.0 pEC50 = 8.0 Functional
Intrinsic activity against dopamine D4 receptor expressed in CHO cells by GTPgammaS assayIntrinsic activity against dopamine D4 receptor expressed in CHO cells by GTPgammaS assay
ChEMBL 315 4 0 3 4.2 C1=C(c2ccccc2)CCN(Cc2cnn(-c3ccccc3)c2)C1 10.1016/j.bmcl.2006.02.075
16094665 83056 5 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 315 4 1 4 3.0 Cc1cccc(C(=O)NCN2CCC(c3nccs3)CC2)c1 10.1021/jm060662k
CHEMBL220083 83056 5 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 315 4 1 4 3.0 Cc1cccc(C(=O)NCN2CCC(c3nccs3)CC2)c1 10.1021/jm060662k
10449865 82857 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 339 4 1 3 2.5 Cc1cc(C)cc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
CHEMBL218798 82857 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 339 4 1 3 2.5 Cc1cc(C)cc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
11416883 80718 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 6 0 5 3.3 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(C)c(C)c1 10.1021/jm060279f
CHEMBL215678 80718 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 6 0 5 3.3 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(C)c(C)c1 10.1021/jm060279f
16094676 230 17 None -1 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 325 4 1 3 2.2 Cc1cccc(c1)C(=O)NCN1CCC(CC1)c1cccc[n+]1[O-] 10.1021/jm060662k
8439 230 17 None -1 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 325 4 1 3 2.2 Cc1cccc(c1)C(=O)NCN1CCC(CC1)c1cccc[n+]1[O-] 10.1021/jm060662k
CHEMBL219182 230 17 None -1 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 325 4 1 3 2.2 Cc1cccc(c1)C(=O)NCN1CCC(CC1)c1cccc[n+]1[O-] 10.1021/jm060662k
15981509 141426 1 None -3 2 Human 7.0 pEC50 = 7.0 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CO2 10.1021/jm0604979
CHEMBL387250 141426 1 None -3 2 Human 7.0 pEC50 = 7.0 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CO2 10.1021/jm0604979
11222637 79373 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 376 6 0 5 3.4 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(F)c(Cl)c1 10.1021/jm060279f
CHEMBL211902 79373 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 376 6 0 5 3.4 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(F)c(Cl)c1 10.1021/jm060279f
16094680 82962 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 339 5 1 3 2.7 CCc1cccc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
CHEMBL219389 82962 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 339 5 1 3 2.7 CCc1cccc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
44393797 66028 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5
ChEMBL 412 4 1 4 3.4 Cc1cc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)ccc1Br 10.1016/j.bmcl.2004.07.068
CHEMBL185149 66028 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5
ChEMBL 412 4 1 4 3.4 Cc1cc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)ccc1Br 10.1016/j.bmcl.2004.07.068
11849266 80657 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 372 6 0 5 3.6 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)c(C)c1 10.1021/jm060279f
CHEMBL215450 80657 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 372 6 0 5 3.6 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)c(C)c1 10.1021/jm060279f
11849781 79911 0 None - 1 Human 7.0 pEC50 = 7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 372 6 0 5 3.7 CO/N=C(/CCN1CCN(c2ccccn2)CC1C)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL214197 79911 0 None - 1 Human 7.0 pEC50 = 7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 372 6 0 5 3.7 CO/N=C(/CCN1CCN(c2ccccn2)CC1C)c1ccc(Cl)cc1 10.1021/jm060279f
9995904 31004 2 None - 0 Human 8.8 pED50 = 8.8 Functional
Effective dose was measured by the stimulation of mitogenesis at dopamine D4.2 receptorEffective dose was measured by the stimulation of mitogenesis at dopamine D4.2 receptor
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4)CC3)cc2c1 10.1021/jm0009989
CHEMBL140099 31004 2 None - 0 Human 8.8 pED50 = 8.8 Functional
Effective dose was measured by the stimulation of mitogenesis at dopamine D4.2 receptorEffective dose was measured by the stimulation of mitogenesis at dopamine D4.2 receptor
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4)CC3)cc2c1 10.1021/jm0009989
71458071 79090 0 None - 0 Human 8.1 pED50 = 8.1 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 266 3 1 3 2.2 N#Cc1cc(CN2CCN(c3ccccc3)CC2)c[nH]1 10.1016/s0960-894x(02)00316-5
CHEMBL2113718 79090 0 None - 0 Human 8.1 pED50 = 8.1 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 266 3 1 3 2.2 N#Cc1cc(CN2CCN(c3ccccc3)CC2)c[nH]1 10.1016/s0960-894x(02)00316-5
9926143 113027 1 None - 1 Human 8.9 pIC50 = 8.9 Functional
Compound was tested for the inhibition of [3H]thymidine uptake in CHO p-5 cells transfected with human Dopamine receptor D4.2Compound was tested for the inhibition of [3H]thymidine uptake in CHO p-5 cells transfected with human Dopamine receptor D4.2
ChEMBL 294 6 2 4 3.0 O=c1ccc2ccc(CNCCNc3ccccc3)cc2o1 10.1021/jm990266k
CHEMBL332154 113027 1 None - 1 Human 8.9 pIC50 = 8.9 Functional
Compound was tested for the inhibition of [3H]thymidine uptake in CHO p-5 cells transfected with human Dopamine receptor D4.2Compound was tested for the inhibition of [3H]thymidine uptake in CHO p-5 cells transfected with human Dopamine receptor D4.2
ChEMBL 294 6 2 4 3.0 O=c1ccc2ccc(CNCCNc3ccccc3)cc2o1 10.1021/jm990266k
168285556 192315 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5196870 192315 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222200 192315 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
168277064 192236 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 379 6 0 4 3.2 COc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5178868 192236 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 379 6 0 4 3.2 COc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5221670 192236 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 379 6 0 4 3.2 COc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
168268756 192162 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5171439 192162 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5221187 192162 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
168268756 192162 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5171439 192162 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5221187 192162 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
45361874 169454 2 None 58 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 324 5 1 4 2.4 CCc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4442548 169454 2 None 58 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 324 5 1 4 2.4 CCc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
3303 2213 41 None 1 5 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.2c00840
5311200 2213 41 None 1 5 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.2c00840
CHEMBL267014 2213 41 None 1 5 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.2c00840
10021193 66031 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Inhibitory concentration required to reverse the dopamine inhibition of forskolin-stimulated adenyl cyclase activity in CHO cells stably expressing hD4 receptorInhibitory concentration required to reverse the dopamine inhibition of forskolin-stimulated adenyl cyclase activity in CHO cells stably expressing hD4 receptor
ChEMBL 356 5 1 2 4.4 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL185156 66031 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Inhibitory concentration required to reverse the dopamine inhibition of forskolin-stimulated adenyl cyclase activity in CHO cells stably expressing hD4 receptorInhibitory concentration required to reverse the dopamine inhibition of forskolin-stimulated adenyl cyclase activity in CHO cells stably expressing hD4 receptor
ChEMBL 356 5 1 2 4.4 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2004.07.045
3303 2213 41 None 1 5 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.2c00840
5311200 2213 41 None 1 5 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.2c00840
CHEMBL267014 2213 41 None 1 5 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.2c00840
109030343 170293 1 None 1 3 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 324 5 1 4 2.5 Cc1cccc(NC(=O)CCN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4454068 170293 1 None 1 3 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 324 5 1 4 2.5 Cc1cccc(NC(=O)CCN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
135398737 944 89 None -44 36 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant at D4 receptor assessed as inhibition of dopamine-induced cAMP accumulationAntagonist activity at human recombinant at D4 receptor assessed as inhibition of dopamine-induced cAMP accumulation
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401895u
38 944 89 None -44 36 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant at D4 receptor assessed as inhibition of dopamine-induced cAMP accumulationAntagonist activity at human recombinant at D4 receptor assessed as inhibition of dopamine-induced cAMP accumulation
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401895u
722 944 89 None -44 36 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant at D4 receptor assessed as inhibition of dopamine-induced cAMP accumulationAntagonist activity at human recombinant at D4 receptor assessed as inhibition of dopamine-induced cAMP accumulation
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401895u
CHEMBL42 944 89 None -44 36 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant at D4 receptor assessed as inhibition of dopamine-induced cAMP accumulationAntagonist activity at human recombinant at D4 receptor assessed as inhibition of dopamine-induced cAMP accumulation
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401895u
DB00363 944 89 None -44 36 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant at D4 receptor assessed as inhibition of dopamine-induced cAMP accumulationAntagonist activity at human recombinant at D4 receptor assessed as inhibition of dopamine-induced cAMP accumulation
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401895u
155513053 169131 0 None 23 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 323 5 1 3 3.5 CCc1cccc(NC(=O)CN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4437912 169131 0 None 23 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 323 5 1 3 3.5 CCc1cccc(NC(=O)CN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
3303 2213 41 None 1 5 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.2c00840
5311200 2213 41 None 1 5 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.2c00840
CHEMBL267014 2213 41 None 1 5 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.2c00840
16094666 81315 2 None 251 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL216393 81315 2 None 251 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/acs.jmedchem.9b00231
109030515 175412 1 None 14 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 325 5 1 5 1.9 Cc1cccc(NC(=O)CCN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4588808 175412 1 None 14 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 325 5 1 5 1.9 Cc1cccc(NC(=O)CCN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
168285556 192315 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5196870 192315 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222200 192315 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
155536720 171621 0 None 37 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 359 4 1 3 3.9 Cc1cccc(NC(=O)CN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4473652 171621 0 None 37 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 359 4 1 3 3.9 Cc1cccc(NC(=O)CN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/acs.jmedchem.9b00231
168277064 192236 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 379 6 0 4 3.2 COc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5178868 192236 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 379 6 0 4 3.2 COc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5221670 192236 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 379 6 0 4 3.2 COc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
155536815 171641 0 None 13 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 322 4 1 2 4.1 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)cc1 10.1021/acs.jmedchem.9b00231
CHEMBL4473792 171641 0 None 13 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 322 4 1 2 4.1 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)cc1 10.1021/acs.jmedchem.9b00231
168268756 192162 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5171439 192162 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5221187 192162 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
168285556 192315 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5196870 192315 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222200 192315 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
168277064 192236 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 379 6 0 4 3.2 COc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5178868 192236 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 379 6 0 4 3.2 COc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5221670 192236 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 379 6 0 4 3.2 COc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
155568411 175506 0 None 2 2 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 331 4 1 5 1.9 O=C(CN1CCN(c2ccc(Cl)cn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
CHEMBL4591118 175506 0 None 2 2 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 331 4 1 5 1.9 O=C(CN1CCN(c2ccc(Cl)cn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
155562395 175375 0 None 169 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 323 4 1 3 3.5 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)nc1 10.1021/acs.jmedchem.9b00231
CHEMBL4587925 175375 0 None 169 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 323 4 1 3 3.5 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)nc1 10.1021/acs.jmedchem.9b00231
6466372 169495 12 None 58 3 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 311 4 1 5 1.5 Cc1cccc(NC(=O)CN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4443054 169495 12 None 58 3 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 311 4 1 5 1.5 Cc1cccc(NC(=O)CN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
155563301 174678 0 None 10 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 344 4 1 4 2.8 Cc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4572245 174678 0 None 10 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 344 4 1 4 2.8 Cc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
9907332 16219 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Compound was tested for the inhibition of [3H]thymidine uptake in CHO p-5 cells transfected with human Dopamine receptor D4.2Compound was tested for the inhibition of [3H]thymidine uptake in CHO p-5 cells transfected with human Dopamine receptor D4.2
ChEMBL 368 3 0 4 4.1 Cc1ccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)cc1Cl 10.1021/jm990266k
CHEMBL123031 16219 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Compound was tested for the inhibition of [3H]thymidine uptake in CHO p-5 cells transfected with human Dopamine receptor D4.2Compound was tested for the inhibition of [3H]thymidine uptake in CHO p-5 cells transfected with human Dopamine receptor D4.2
ChEMBL 368 3 0 4 4.1 Cc1ccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)cc1Cl 10.1021/jm990266k
155530763 171003 0 None -2 3 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 323 5 1 3 3.6 Cc1cccc(NC(=O)CCN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4464861 171003 0 None -2 3 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 323 5 1 3 3.6 Cc1cccc(NC(=O)CCN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
168285560 192316 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 350 5 0 4 2.6 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccn2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5196873 192316 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 350 5 0 4 2.6 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccn2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222201 192316 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 350 5 0 4 2.6 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccn2)CC1 10.1021/acs.jmedchem.2c00840
10425450 199 23 None 125 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
3301 199 23 None 125 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
CHEMBL375596 199 23 None 125 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
155511803 169038 0 None 1 2 Human 4.2 pIC50 = 4.2 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 342 4 1 2 4.5 Cc1cccc(NC(=O)CN2CCC(c3ccc(Cl)cc3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4436479 169038 0 None 1 2 Human 4.2 pIC50 = 4.2 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 342 4 1 2 4.5 Cc1cccc(NC(=O)CN2CCC(c3ccc(Cl)cc3)CC2)c1 10.1021/acs.jmedchem.9b00231
155516494 169554 0 None 6 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 358 5 1 4 3.1 CCc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4443848 169554 0 None 6 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 358 5 1 4 3.1 CCc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
4797946 169856 8 None 81 3 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 310 4 1 4 2.2 Cc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4448320 169856 8 None 81 3 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 310 4 1 4 2.2 Cc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
155568867 175580 0 None -3 3 Human 4.1 pIC50 = 4.1 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 297 4 1 5 1.2 O=C(CN1CCN(c2ccccn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
CHEMBL4592753 175580 0 None -3 3 Human 4.1 pIC50 = 4.1 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 297 4 1 5 1.2 O=C(CN1CCN(c2ccccn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
9948546 16148 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Compound was tested for the inhibition of [3H]thymidine uptake in CHO p-5 cells transfected with human Dopamine receptor D4.2Compound was tested for the inhibition of [3H]thymidine uptake in CHO p-5 cells transfected with human Dopamine receptor D4.2
ChEMBL 308 6 2 4 3.3 Cc1ccc(NCCNCc2ccc3ccc(=O)oc3c2)cc1 10.1021/jm990266k
CHEMBL122754 16148 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Compound was tested for the inhibition of [3H]thymidine uptake in CHO p-5 cells transfected with human Dopamine receptor D4.2Compound was tested for the inhibition of [3H]thymidine uptake in CHO p-5 cells transfected with human Dopamine receptor D4.2
ChEMBL 308 6 2 4 3.3 Cc1ccc(NCCNCc2ccc3ccc(=O)oc3c2)cc1 10.1021/jm990266k
24815434 198014 0 None - 2 Human 7.0 pKi = 7 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 305 3 0 3 4.0 Cn1c(CN2CCC(c3ccccc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL593196 198014 0 None - 2 Human 7.0 pKi = 7 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 305 3 0 3 4.0 Cn1c(CN2CCC(c3ccccc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
46225337 198294 0 None - 1 Human 6.0 pKi = 6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 375 3 0 5 3.3 Cn1c(CN2CCN(c3ccc(C(F)(F)F)cn3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL595151 198294 0 None - 1 Human 6.0 pKi = 6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 375 3 0 5 3.3 Cn1c(CN2CCN(c3ccc(C(F)(F)F)cn3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
24815976 198077 0 None - 2 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 373 3 0 3 5.0 Cn1c(CN2CCC(c3ccc(C(F)(F)F)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL593745 198077 0 None - 2 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 373 3 0 3 5.0 Cn1c(CN2CCC(c3ccc(C(F)(F)F)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
798232 198451 9 None - 1 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 340 3 0 4 3.5 Cn1c(CN2CCN(c3ccc(Cl)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL596271 198451 9 None - 1 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 340 3 0 4 3.5 Cn1c(CN2CCN(c3ccc(Cl)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
10615684 17857 0 None 9 2 Human 7.9 pKi = 7.9 Functional
Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cellsAntagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cells
ChEMBL 320 4 0 2 4.2 Cc1ccc(N2CCN(C[C@@H]3C[C@H]3c3ccccc3)CC2)c(C)c1 10.1021/jm990562x
CHEMBL1202208 17857 0 None 9 2 Human 7.9 pKi = 7.9 Functional
Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cellsAntagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cells
ChEMBL 320 4 0 2 4.2 Cc1ccc(N2CCN(C[C@@H]3C[C@H]3c3ccccc3)CC2)c(C)c1 10.1021/jm990562x
CHEMBL126493 17857 0 None 9 2 Human 7.9 pKi = 7.9 Functional
Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cellsAntagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cells
ChEMBL 320 4 0 2 4.2 Cc1ccc(N2CCN(C[C@@H]3C[C@H]3c3ccccc3)CC2)c(C)c1 10.1021/jm990562x
44517726 194348 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at dopamine D4 receptorAntagonist activity at dopamine D4 receptor
ChEMBL 341 4 0 2 3.6 O=C1N(CCN2Cc3ccccc3C2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2009.06.043
CHEMBL560177 194348 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at dopamine D4 receptorAntagonist activity at dopamine D4 receptor
ChEMBL 341 4 0 2 3.6 O=C1N(CCN2Cc3ccccc3C2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2009.06.043
46225583 198490 0 None - 1 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 362 3 0 5 4.6 Cn1c(CN2CCC(c3nsc4ccccc34)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL596527 198490 0 None - 1 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 362 3 0 5 4.6 Cn1c(CN2CCC(c3nsc4ccccc34)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
1353 1880 85 None -7 27 Human 8.7 pKi = 8.7 Functional
Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cellsAntagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm990562x
3559 1880 85 None -7 27 Human 8.7 pKi = 8.7 Functional
Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cellsAntagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm990562x
86 1880 85 None -7 27 Human 8.7 pKi = 8.7 Functional
Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cellsAntagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm990562x
CHEMBL54 1880 85 None -7 27 Human 8.7 pKi = 8.7 Functional
Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cellsAntagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm990562x
DB00502 1880 85 None -7 27 Human 8.7 pKi = 8.7 Functional
Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cellsAntagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm990562x
9820304 101599 0 None 10 2 Human 7.6 pKi = 7.6 Functional
Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cellsAntagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cells
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(Cl)c1 10.1021/jm990562x
CHEMBL1204116 101599 0 None 10 2 Human 7.6 pKi = 7.6 Functional
Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cellsAntagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cells
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(Cl)c1 10.1021/jm990562x
CHEMBL302075 101599 0 None 10 2 Human 7.6 pKi = 7.6 Functional
Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cellsAntagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cells
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(Cl)c1 10.1021/jm990562x
46225334 198363 0 None - 1 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 358 3 0 4 3.7 Cn1c(CN2CCN(c3ccc(Cl)cc3F)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL595607 198363 0 None - 1 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 358 3 0 4 3.7 Cn1c(CN2CCN(c3ccc(Cl)cc3F)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
24815883 199777 0 None - 1 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 373 3 0 3 5.0 Cn1c(CN2CCC(c3cccc(C(F)(F)F)c3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL604993 199777 0 None - 1 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 373 3 0 3 5.0 Cn1c(CN2CCC(c3cccc(C(F)(F)F)c3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
46225581 200302 0 None - 1 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 339 3 0 3 4.6 Cn1c(CN2CCC(c3cccc(Cl)c3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL608103 200302 0 None - 1 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 339 3 0 3 4.6 Cn1c(CN2CCC(c3cccc(Cl)c3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
46190878 1842 3 None - 1 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 342 3 0 6 2.3 Clc1cnc(nc1)N1CCN(CC1)Cc1nc2c(n1C)cccc2 10.1016/j.bmcl.2009.11.032
6253 1842 3 None - 1 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 342 3 0 6 2.3 Clc1cnc(nc1)N1CCN(CC1)Cc1nc2c(n1C)cccc2 10.1016/j.bmcl.2009.11.032
CHEMBL595759 1842 3 None - 1 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 342 3 0 6 2.3 Clc1cnc(nc1)N1CCN(CC1)Cc1nc2c(n1C)cccc2 10.1016/j.bmcl.2009.11.032
46225584 197993 0 None - 1 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 408 3 0 4 5.0 Cn1c(CN2CCC(c3ncc(C(F)(F)F)cc3Cl)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL593056 197993 0 None - 1 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 408 3 0 4 5.0 Cn1c(CN2CCC(c3ncc(C(F)(F)F)cc3Cl)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
10157556 119730 0 None - 0 Human 8.5 pKi = 8.5 Functional
D4 receptor functional activity was measured inhibition of quinpirole stimulated [35S]GTP-gamma-S binding from cell membranes.D4 receptor functional activity was measured inhibition of quinpirole stimulated [35S]GTP-gamma-S binding from cell membranes.
ChEMBL 395 3 0 3 3.4 O=C1C(N2CCN(Cc3ccc(Cl)cc3)CC2)CCc2cccc3c2N1CC3 10.1016/s0960-894x(02)01056-9
CHEMBL352207 119730 0 None - 0 Human 8.5 pKi = 8.5 Functional
D4 receptor functional activity was measured inhibition of quinpirole stimulated [35S]GTP-gamma-S binding from cell membranes.D4 receptor functional activity was measured inhibition of quinpirole stimulated [35S]GTP-gamma-S binding from cell membranes.
ChEMBL 395 3 0 3 3.4 O=C1C(N2CCN(Cc3ccc(Cl)cc3)CC2)CCc2cccc3c2N1CC3 10.1016/s0960-894x(02)01056-9
3691783 4696 1 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at dopamine D4 receptorAntagonist activity at dopamine D4 receptor
ChEMBL 318 4 1 3 3.4 c1ccc(-c2nc(CN3CCN(c4ccccc4)CC3)c[nH]2)cc1 10.1016/j.bmc.2010.01.040
CHEMBL103871 4696 1 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at dopamine D4 receptorAntagonist activity at dopamine D4 receptor
ChEMBL 318 4 1 3 3.4 c1ccc(-c2nc(CN3CCN(c4ccccc4)CC3)c[nH]2)cc1 10.1016/j.bmc.2010.01.040
46225335 198364 0 None - 1 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 374 3 0 4 3.9 Cn1c(CN2CCN(c3ccc(C(F)(F)F)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL595608 198364 0 None - 1 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 374 3 0 4 3.9 Cn1c(CN2CCN(c3ccc(C(F)(F)F)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
24849462 198076 0 None - 1 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 339 3 0 3 4.6 Cn1c(CN2CCC(c3ccc(Cl)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL593744 198076 0 None - 1 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 339 3 0 3 4.6 Cn1c(CN2CCC(c3ccc(Cl)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
46190877 1841 3 None - 1 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 409 3 0 5 4.0 Clc1cc(cnc1N1CCN(CC1)Cc1nc2c(n1C)cccc2)C(F)(F)F 10.1016/j.bmcl.2009.11.032
6252 1841 3 None - 1 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 409 3 0 5 4.0 Clc1cc(cnc1N1CCN(CC1)Cc1nc2c(n1C)cccc2)C(F)(F)F 10.1016/j.bmcl.2009.11.032
CHEMBL605836 1841 3 None - 1 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 409 3 0 5 4.0 Clc1cc(cnc1N1CCN(CC1)Cc1nc2c(n1C)cccc2)C(F)(F)F 10.1016/j.bmcl.2009.11.032
46225320 199498 0 None - 1 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 374 3 0 4 3.9 Cn1c(CN2CCN(c3ccccc3C(F)(F)F)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL603443 199498 0 None - 1 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 374 3 0 4 3.9 Cn1c(CN2CCN(c3ccccc3C(F)(F)F)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
9799123 5543 0 None 61 2 Human 8.2 pKi = 8.2 Functional
Dopamine D4 receptor functional activity was assessed via inhibition of quinpirole stimulated [35S]GTP-gamma-S binding from cell membranes.Dopamine D4 receptor functional activity was assessed via inhibition of quinpirole stimulated [35S]GTP-gamma-S binding from cell membranes.
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
CHEMBL107742 5543 0 None 61 2 Human 8.2 pKi = 8.2 Functional
Dopamine D4 receptor functional activity was assessed via inhibition of quinpirole stimulated [35S]GTP-gamma-S binding from cell membranes.Dopamine D4 receptor functional activity was assessed via inhibition of quinpirole stimulated [35S]GTP-gamma-S binding from cell membranes.
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
46225582 199930 0 None - 1 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 362 3 0 5 4.6 Cn1c(CN2CCC(c3nc4ccccc4s3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL605831 199930 0 None - 1 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 362 3 0 5 4.6 Cn1c(CN2CCC(c3nc4ccccc4s3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
46225336 198365 0 None - 1 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 363 3 0 6 3.5 Cn1c(CN2CCN(c3nc4ccccc4s3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL595609 198365 0 None - 1 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 363 3 0 6 3.5 Cn1c(CN2CCN(c3nc4ccccc4s3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
9952003 5288 0 None - 0 Human 6.0 pKi = 6.0 Functional
Dopamine Receptor D4 functional activity was assessed via inhibition of quinpirole stimulated [35S]GTP-gamma-S binding from cell membranes.Dopamine Receptor D4 functional activity was assessed via inhibition of quinpirole stimulated [35S]GTP-gamma-S binding from cell membranes.
ChEMBL 383 4 0 3 3.4 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL106916 5288 0 None - 0 Human 6.0 pKi = 6.0 Functional
Dopamine Receptor D4 functional activity was assessed via inhibition of quinpirole stimulated [35S]GTP-gamma-S binding from cell membranes.Dopamine Receptor D4 functional activity was assessed via inhibition of quinpirole stimulated [35S]GTP-gamma-S binding from cell membranes.
ChEMBL 383 4 0 3 3.4 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
681 1437 65 None -1 12 Rat 8.1 pEC50 = 8.1 Functional
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1437 65 None -1 12 Rat 8.1 pEC50 = 8.1 Functional
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1437 65 None -1 12 Rat 8.1 pEC50 = 8.1 Functional
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1437 65 None -1 12 Rat 8.1 pEC50 = 8.1 Functional
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1437 65 None -1 12 Rat 8.1 pEC50 = 8.1 Functional
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
228 441 26 None 1 8 Rat 8.1 pEC50 = 8.1 Functional
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
33 441 26 None 1 8 Rat 8.1 pEC50 = 8.1 Functional
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
6005 441 26 None 1 8 Rat 8.1 pEC50 = 8.1 Functional
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
CHEMBL53 441 26 None 1 8 Rat 8.1 pEC50 = 8.1 Functional
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
DB00714 441 26 None 1 8 Rat 8.1 pEC50 = 8.1 Functional
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
30699 215969 0 None -1 14 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 423 7 2 8 0.5 CC(=O)OCC1=C(N2[C@H](SC1)[C@H](NC(=O)CSC1=CC=NC=C1)C2=O)C(O)=O None
4223 3929 88 None -588 15 Rat 8.3 pIC50 = 8.3 Functional
Inhibition of rat dopamine D4 receptorInhibition of rat dopamine D4 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
6918314 3929 88 None -588 15 Rat 8.3 pIC50 = 8.3 Functional
Inhibition of rat dopamine D4 receptorInhibition of rat dopamine D4 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
7427 3929 88 None -588 15 Rat 8.3 pIC50 = 8.3 Functional
Inhibition of rat dopamine D4 receptorInhibition of rat dopamine D4 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
CHEMBL439849 3929 88 None -588 15 Rat 8.3 pIC50 = 8.3 Functional
Inhibition of rat dopamine D4 receptorInhibition of rat dopamine D4 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
DB06684 3929 88 None -588 15 Rat 8.3 pIC50 = 8.3 Functional
Inhibition of rat dopamine D4 receptorInhibition of rat dopamine D4 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
10263487 3020 0 None -19 2 Human 5.4 pIC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 235 3 1 4 1.8 CCCN1C[C@H](OC[C@@H]1C)c1ccc(nc1)N 22470105
7683 3020 0 None -19 2 Human 5.4 pIC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 235 3 1 4 1.8 CCCN1C[C@H](OC[C@@H]1C)c1ccc(nc1)N 22470105


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Ligands Receptor Assay information Chemical information
Sel. page Common
name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Affinity)		 # tested GPCRs
(Affinity)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
14925759 157494 6 None 18 13 Human 9.8 pEC50 = 9.8 Binding
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assay
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4085780 157494 6 None 18 13 Human 9.8 pEC50 = 9.8 Binding
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assay
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
9945233 203383 1 None - 1 Human 9.0 pEC50 = 9 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm0305669
CHEMBL77563 203383 1 None - 1 Human 9.0 pEC50 = 9 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm0305669
228 441 26 None - 24 Rat 8.8 pEC50 = 8.8 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
33 441 26 None - 24 Rat 8.8 pEC50 = 8.8 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
6005 441 26 None - 24 Rat 8.8 pEC50 = 8.8 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
CHEMBL53 441 26 None - 24 Rat 8.8 pEC50 = 8.8 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
DB00714 441 26 None - 24 Rat 8.8 pEC50 = 8.8 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
9857248 203394 6 None - 1 Human 8.0 pEC50 = 8 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 292 3 1 3 2.9 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)cc1 10.1021/jm0305669
CHEMBL77708 203394 6 None - 1 Human 8.0 pEC50 = 8 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 292 3 1 3 2.9 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)cc1 10.1021/jm0305669
10268039 17832 0 None - 0 Human 7.0 pEC50 = 7 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 321 4 1 3 4.0 COc1ccccc1C1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
CHEMBL126361 17832 0 None - 0 Human 7.0 pEC50 = 7 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 321 4 1 3 4.0 COc1ccccc1C1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
44315403 203760 0 None - 1 Human 5.0 pEC50 = 5 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 327 3 1 4 2.9 Clc1ccccc1N1CCN(Cc2nc3ccc[nH]c-3n2)CC1 10.1021/jm0305669
CHEMBL80469 203760 0 None - 1 Human 5.0 pEC50 = 5 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 327 3 1 4 2.9 Clc1ccccc1N1CCN(Cc2nc3ccc[nH]c-3n2)CC1 10.1021/jm0305669
164612037 184795 0 None -1 20 Human 7.0 pEC50 = 7.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
CHEMBL4860528 184795 0 None -1 20 Human 7.0 pEC50 = 7.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
11392147 17904 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human D4.4 receptor using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human D4.4 receptor using FLIPR assay
ChEMBL 290 3 1 3 3.2 C1=C(c2ccccn2)CCN(Cc2nc3ccccc3[nH]2)C1 10.1021/jm030505a
CHEMBL126754 17904 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human D4.4 receptor using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human D4.4 receptor using FLIPR assay
ChEMBL 290 3 1 3 3.2 C1=C(c2ccccn2)CCN(Cc2nc3ccccc3[nH]2)C1 10.1021/jm030505a
681 1437 65 None -2 38 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b00265
940 1437 65 None -2 38 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b00265
947 1437 65 None -2 38 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b00265
CHEMBL59 1437 65 None -2 38 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b00265
DB00988 1437 65 None -2 38 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b00265
5025739 168630 40 None 30 2 Human 7.9 pEC50 = 7.9 Binding
D4 efficacy was measured using recombinant human Dopamine receptor D4 expressed in HEK293 cellsD4 efficacy was measured using recombinant human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm0305669
CHEMBL440687 168630 40 None 30 2 Human 7.9 pEC50 = 7.9 Binding
D4 efficacy was measured using recombinant human Dopamine receptor D4 expressed in HEK293 cellsD4 efficacy was measured using recombinant human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm0305669
4826074 103627 6 None - 1 Human 7.9 pEC50 = 7.9 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 322 4 1 4 2.9 COc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
CHEMBL309372 103627 6 None - 1 Human 7.9 pEC50 = 7.9 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 322 4 1 4 2.9 COc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
5025739 168630 40 None 30 2 Human 7.9 pEC50 = 7.9 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm030505a
CHEMBL440687 168630 40 None 30 2 Human 7.9 pEC50 = 7.9 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm030505a
9836662 97701 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 318 3 1 5 2.2 N#Cc1cccnc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
CHEMBL273772 97701 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 318 3 1 5 2.2 N#Cc1cccnc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
45361874 169454 2 None 48 3 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 324 5 1 4 2.4 CCc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4442548 169454 2 None 48 3 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 324 5 1 4 2.4 CCc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
11474209 116871 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 371 4 1 6 1.7 CS(=O)(=O)c1cccnc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
CHEMBL339791 116871 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 371 4 1 6 1.7 CS(=O)(=O)c1cccnc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
9835713 18300 1 None - 0 Human 7.9 pEC50 = 7.9 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 292 3 1 3 3.3 c1ccc(C2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm030505a
CHEMBL127226 18300 1 None - 0 Human 7.9 pEC50 = 7.9 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 292 3 1 3 3.3 c1ccc(C2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm030505a
5025739 168630 40 None - 2 Rat 7.8 pEC50 = 7.8 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm030505a
CHEMBL440687 168630 40 None - 2 Rat 7.8 pEC50 = 7.8 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm030505a
9858141 117126 1 None - 0 Human 7.8 pEC50 = 7.8 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 317 3 1 4 2.8 N#Cc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
CHEMBL340099 117126 1 None - 0 Human 7.8 pEC50 = 7.8 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 317 3 1 4 2.8 N#Cc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
9901273 17861 3 None - 0 Human 7.8 pEC50 = 7.8 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 310 3 1 3 3.0 Fc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
CHEMBL126510 17861 3 None - 0 Human 7.8 pEC50 = 7.8 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 310 3 1 3 3.0 Fc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
119570 3110 90 None -10 40 Human 7.8 pEC50 = 7.8 Binding
Effective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
2233 3110 90 None -10 40 Human 7.8 pEC50 = 7.8 Binding
Effective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
953 3110 90 None -10 40 Human 7.8 pEC50 = 7.8 Binding
Effective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
CHEMBL301265 3110 90 None -10 40 Human 7.8 pEC50 = 7.8 Binding
Effective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
DB00413 3110 90 None -10 40 Human 7.8 pEC50 = 7.8 Binding
Effective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
10336538 1595 44 None -3 8 Human 6.8 pEC50 = 6.8 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm0305669
974 1595 44 None -3 8 Human 6.8 pEC50 = 6.8 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm0305669
CHEMBL310843 1595 44 None -3 8 Human 6.8 pEC50 = 6.8 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm0305669
681 1437 65 None -2 38 Human 8.7 pEC50 = 8.7 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
940 1437 65 None -2 38 Human 8.7 pEC50 = 8.7 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
947 1437 65 None -2 38 Human 8.7 pEC50 = 8.7 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
CHEMBL59 1437 65 None -2 38 Human 8.7 pEC50 = 8.7 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
DB00988 1437 65 None -2 38 Human 8.7 pEC50 = 8.7 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
681 1437 65 None -7 38 Rat 8.6 pEC50 = 8.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
940 1437 65 None -7 38 Rat 8.6 pEC50 = 8.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
947 1437 65 None -7 38 Rat 8.6 pEC50 = 8.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
CHEMBL59 1437 65 None -7 38 Rat 8.6 pEC50 = 8.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
DB00988 1437 65 None -7 38 Rat 8.6 pEC50 = 8.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
681 1437 65 None -7 38 Rat 8.6 pEC50 = 8.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
940 1437 65 None -7 38 Rat 8.6 pEC50 = 8.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
947 1437 65 None -7 38 Rat 8.6 pEC50 = 8.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
CHEMBL59 1437 65 None -7 38 Rat 8.6 pEC50 = 8.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
DB00988 1437 65 None -7 38 Rat 8.6 pEC50 = 8.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
973 1154 33 None 9 6 Rat 7.7 pEC50 = 7.7 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm030505a
9796720 1154 33 None 9 6 Rat 7.7 pEC50 = 7.7 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm030505a
CHEMBL77395 1154 33 None 9 6 Rat 7.7 pEC50 = 7.7 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm030505a
3303 2213 41 None 1 15 Human 5.7 pEC50 = 5.7 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm0305669
5311200 2213 41 None 1 15 Human 5.7 pEC50 = 5.7 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm0305669
CHEMBL267014 2213 41 None 1 15 Human 5.7 pEC50 = 5.7 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm0305669
168294767 192417 0 None -1 20 Human 5.7 pEC50 = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5207281 192417 0 None -1 20 Human 5.7 pEC50 = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222802 192417 0 None -1 20 Human 5.7 pEC50 = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
9838927 18632 11 None - 0 Human 6.6 pEC50 = 6.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human D4.4 receptor using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human D4.4 receptor using FLIPR assay
ChEMBL 289 3 1 2 3.9 C1=C(c2ccccc2)CCN(Cc2nc3ccccc3[nH]2)C1 10.1021/jm030505a
CHEMBL127930 18632 11 None - 0 Human 6.6 pEC50 = 6.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human D4.4 receptor using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human D4.4 receptor using FLIPR assay
ChEMBL 289 3 1 2 3.9 C1=C(c2ccccc2)CCN(Cc2nc3ccccc3[nH]2)C1 10.1021/jm030505a
11255258 18645 4 None - 0 Human 7.6 pEC50 = 7.6 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 307 4 1 4 2.3 c1ccc(N2CCN(CCc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm030505a
CHEMBL128040 18645 4 None - 0 Human 7.6 pEC50 = 7.6 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 307 4 1 4 2.3 c1ccc(N2CCN(CCc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm030505a
5025739 168630 40 None - 2 Rat 7.6 pEC50 = 7.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm030505a
CHEMBL440687 168630 40 None - 2 Rat 7.6 pEC50 = 7.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm030505a
9966489 17892 1 None - 0 Human 7.6 pEC50 = 7.6 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 311 3 1 4 2.4 Fc1cccnc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
CHEMBL126687 17892 1 None - 0 Human 7.6 pEC50 = 7.6 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 311 3 1 4 2.4 Fc1cccnc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
16094666 81315 2 None 52 3 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL216393 81315 2 None 52 3 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/acs.jmedchem.9b00231
9945714 18532 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 336 5 1 4 3.3 CCOc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
CHEMBL127752 18532 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 336 5 1 4 3.3 CCOc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
155515982 169443 0 None 6 17 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assayAgonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assay
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4442460 169443 0 None 6 17 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assayAgonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assay
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
155568867 175580 0 None - 1 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 297 4 1 5 1.2 O=C(CN1CCN(c2ccccn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
CHEMBL4592753 175580 0 None - 1 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 297 4 1 5 1.2 O=C(CN1CCN(c2ccccn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
6466372 169495 12 None 93 3 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 311 4 1 5 1.5 Cc1cccc(NC(=O)CN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4443054 169495 12 None 93 3 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 311 4 1 5 1.5 Cc1cccc(NC(=O)CN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
9945753 16689 5 None - 0 Human 8.4 pEC50 = 8.4 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 337 4 1 5 2.8 O=[N+]([O-])c1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
CHEMBL124927 16689 5 None - 0 Human 8.4 pEC50 = 8.4 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 337 4 1 5 2.8 O=[N+]([O-])c1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
9857248 203394 6 None - 1 Human 7.5 pEC50 = 7.5 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 292 3 1 3 2.9 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)cc1 10.1021/jm030505a
CHEMBL77708 203394 6 None - 1 Human 7.5 pEC50 = 7.5 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 292 3 1 3 2.9 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)cc1 10.1021/jm030505a
973 1154 33 None -9 6 Human 7.5 pEC50 = 7.5 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm0305669
9796720 1154 33 None -9 6 Human 7.5 pEC50 = 7.5 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm0305669
CHEMBL77395 1154 33 None -9 6 Human 7.5 pEC50 = 7.5 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm0305669
973 1154 33 None -9 6 Human 7.5 pEC50 = 7.5 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm030505a
9796720 1154 33 None -9 6 Human 7.5 pEC50 = 7.5 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm030505a
CHEMBL77395 1154 33 None -9 6 Human 7.5 pEC50 = 7.5 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm030505a
155559617 174312 0 None 9 3 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assayAgonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4563944 174312 0 None 9 3 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assayAgonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
137646281 157264 0 None -1659 17 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assayAgonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 423 8 0 7 3.8 COc1ccccc1N1CCN(CCCSc2nnc(-c3ccccc3)n2C)CC1 10.1021/acs.jmedchem.9b00412
CHEMBL4083252 157264 0 None -1659 17 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assayAgonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 423 8 0 7 3.8 COc1ccccc1N1CCN(CCCSc2nnc(-c3ccccc3)n2C)CC1 10.1021/acs.jmedchem.9b00412
973 1154 33 None 9 6 Rat 7.4 pEC50 = 7.4 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm030505a
9796720 1154 33 None 9 6 Rat 7.4 pEC50 = 7.4 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm030505a
CHEMBL77395 1154 33 None 9 6 Rat 7.4 pEC50 = 7.4 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm030505a
9879627 16875 1 None - 0 Human 7.4 pEC50 = 7.4 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 307 3 1 4 2.6 Cc1cccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)n1 10.1021/jm030505a
CHEMBL125464 16875 1 None - 0 Human 7.4 pEC50 = 7.4 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 307 3 1 4 2.6 Cc1cccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)n1 10.1021/jm030505a
4797946 169856 8 None 165 3 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 310 4 1 4 2.2 Cc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4448320 169856 8 None 165 3 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 310 4 1 4 2.2 Cc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
72901200 119272 21 None 154 4 Human 8.4 pEC50 = 8.4 Binding
Affinity On-target Cellular interaction (Split luciferase based cAMP receptor assay (HEK293T cells)) EUB0000539a DRD4Affinity On-target Cellular interaction (Split luciferase based cAMP receptor assay (HEK293T cells)) EUB0000539a DRD4
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 nan
CHEMBL3480577 119272 21 None 154 4 Human 8.4 pEC50 = 8.4 Binding
Affinity On-target Cellular interaction (Split luciferase based cAMP receptor assay (HEK293T cells)) EUB0000539a DRD4Affinity On-target Cellular interaction (Split luciferase based cAMP receptor assay (HEK293T cells)) EUB0000539a DRD4
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 nan
228 441 26 None -1 24 Human 8.4 pEC50 = 8.4 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
33 441 26 None -1 24 Human 8.4 pEC50 = 8.4 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
6005 441 26 None -1 24 Human 8.4 pEC50 = 8.4 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
CHEMBL53 441 26 None -1 24 Human 8.4 pEC50 = 8.4 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
DB00714 441 26 None -1 24 Human 8.4 pEC50 = 8.4 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
10225902 17894 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 449 3 1 4 3.8 Brc1cc(Br)c2[nH]c(CN3CCN(c4ccccn4)CC3)nc2c1 10.1021/jm030505a
CHEMBL126698 17894 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 449 3 1 4 3.8 Brc1cc(Br)c2[nH]c(CN3CCN(c4ccccn4)CC3)nc2c1 10.1021/jm030505a
10014924 106787 0 None -16 5 Human 5.4 pEC50 = 5.4 Binding
Effective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1 10.1021/jm049269+
CHEMBL316983 106787 0 None -16 5 Human 5.4 pEC50 = 5.4 Binding
Effective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1 10.1021/jm049269+
9922161 17874 5 None - 0 Human 7.4 pEC50 = 7.4 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 294 3 1 5 1.7 c1cnc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm030505a
CHEMBL126595 17874 5 None - 0 Human 7.4 pEC50 = 7.4 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 294 3 1 5 1.7 c1cnc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm030505a
10425450 199 23 None -1 4 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
3301 199 23 None -1 4 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
CHEMBL375596 199 23 None -1 4 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
228 441 26 None - 24 Rat 8.3 pEC50 = 8.3 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
33 441 26 None - 24 Rat 8.3 pEC50 = 8.3 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
6005 441 26 None - 24 Rat 8.3 pEC50 = 8.3 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
CHEMBL53 441 26 None - 24 Rat 8.3 pEC50 = 8.3 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
DB00714 441 26 None - 24 Rat 8.3 pEC50 = 8.3 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
4826074 103627 6 None - 1 Human 8.3 pEC50 = 8.3 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 322 4 1 4 2.9 COc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm0305669
CHEMBL309372 103627 6 None - 1 Human 8.3 pEC50 = 8.3 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 322 4 1 4 2.9 COc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm0305669
44381216 119826 0 None 8511 4 Human 7.3 pEC50 = 7.3 Binding
Effective concentration for [3H]thymidine uptake in growing CHO cells stably expressing the dopamine D4.2 receptorEffective concentration for [3H]thymidine uptake in growing CHO cells stably expressing the dopamine D4.2 receptor
ChEMBL 334 4 1 4 2.6 c1ccc(C2=NCC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(03)00004-0
CHEMBL352925 119826 0 None 8511 4 Human 7.3 pEC50 = 7.3 Binding
Effective concentration for [3H]thymidine uptake in growing CHO cells stably expressing the dopamine D4.2 receptorEffective concentration for [3H]thymidine uptake in growing CHO cells stably expressing the dopamine D4.2 receptor
ChEMBL 334 4 1 4 2.6 c1ccc(C2=NCC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(03)00004-0
155552185 173489 0 None 2 16 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assayAgonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4544086 173489 0 None 2 16 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assayAgonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
9815072 17866 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 307 3 1 4 2.7 C[C@H]1CN(c2ccccn2)CCN1Cc1nc2ccccc2[nH]1 10.1021/jm030505a
CHEMBL126530 17866 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 307 3 1 4 2.7 C[C@H]1CN(c2ccccn2)CCN1Cc1nc2ccccc2[nH]1 10.1021/jm030505a
9836209 17865 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 307 3 1 4 2.7 C[C@@H]1CN(c2ccccn2)CCN1Cc1nc2ccccc2[nH]1 10.1021/jm030505a
CHEMBL126529 17865 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 307 3 1 4 2.7 C[C@@H]1CN(c2ccccn2)CCN1Cc1nc2ccccc2[nH]1 10.1021/jm030505a
168290235 192366 0 None -5 20 Human 5.2 pEC50 = 5.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5201074 192366 0 None -5 20 Human 5.2 pEC50 = 5.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222491 192366 0 None -5 20 Human 5.2 pEC50 = 5.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
168295528 192429 0 None -1 20 Human 6.2 pEC50 = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5206565 192429 0 None -1 20 Human 6.2 pEC50 = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222872 192429 0 None -1 20 Human 6.2 pEC50 = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
9945233 203383 1 None - 1 Human 8.1 pEC50 = 8.1 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 326 3 1 3 3.5 Clc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
CHEMBL77563 203383 1 None - 1 Human 8.1 pEC50 = 8.1 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 326 3 1 3 3.5 Clc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
9857887 18343 2 None - 0 Human 8.1 pEC50 = 8.1 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 311 3 1 4 2.4 Fc1ccc2[nH]c(CN3CCN(c4ccccn4)CC3)nc2c1 10.1021/jm030505a
CHEMBL127460 18343 2 None - 0 Human 8.1 pEC50 = 8.1 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 311 3 1 4 2.4 Fc1ccc2[nH]c(CN3CCN(c4ccccn4)CC3)nc2c1 10.1021/jm030505a
2 3210 19 None -2 28 Human 8.1 pEC50 = 8.1 Binding
Effective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm049269+
54562 3210 19 None -2 28 Human 8.1 pEC50 = 8.1 Binding
Effective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm049269+
CHEMBL240773 3210 19 None -2 28 Human 8.1 pEC50 = 8.1 Binding
Effective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm049269+
2 3210 19 None -2 28 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assayAgonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b01085
54562 3210 19 None -2 28 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assayAgonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b01085
CHEMBL240773 3210 19 None -2 28 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assayAgonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b01085
9881000 116439 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 338 4 1 4 3.6 CSc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
CHEMBL338547 116439 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 338 4 1 4 3.6 CSc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
1588 2294 24 None -23 43 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assayAgonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/acs.jmedchem.9b00412
28864 2294 24 None -23 43 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assayAgonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/acs.jmedchem.9b00412
43 2294 24 None -23 43 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assayAgonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/acs.jmedchem.9b00412
CHEMBL157138 2294 24 None -23 43 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assayAgonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/acs.jmedchem.9b00412
DB00589 2294 24 None -23 43 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assayAgonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/acs.jmedchem.9b00412
2 3210 19 None -2 28 Human 8.0 pEC50 = 8 Binding
Effective concentration for [3H]thymidine uptake in growing CHO cells stably expressing the dopamine D4.2 receptorEffective concentration for [3H]thymidine uptake in growing CHO cells stably expressing the dopamine D4.2 receptor
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(03)00004-0
54562 3210 19 None -2 28 Human 8.0 pEC50 = 8 Binding
Effective concentration for [3H]thymidine uptake in growing CHO cells stably expressing the dopamine D4.2 receptorEffective concentration for [3H]thymidine uptake in growing CHO cells stably expressing the dopamine D4.2 receptor
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(03)00004-0
CHEMBL240773 3210 19 None -2 28 Human 8.0 pEC50 = 8 Binding
Effective concentration for [3H]thymidine uptake in growing CHO cells stably expressing the dopamine D4.2 receptorEffective concentration for [3H]thymidine uptake in growing CHO cells stably expressing the dopamine D4.2 receptor
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(03)00004-0
681 1437 65 None -2 38 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b00265
940 1437 65 None -2 38 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b00265
947 1437 65 None -2 38 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b00265
CHEMBL59 1437 65 None -2 38 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b00265
DB00988 1437 65 None -2 38 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b00265
155536720 171621 0 None 77 3 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 359 4 1 3 3.9 Cc1cccc(NC(=O)CN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4473652 171621 0 None 77 3 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 359 4 1 3 3.9 Cc1cccc(NC(=O)CN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/acs.jmedchem.9b00231
3626837 205584 8 None 125 4 Human 10.2 pIC50 = 10.2 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 373 6 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm981041x
CHEMBL93403 205584 8 None 125 4 Human 10.2 pIC50 = 10.2 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 373 6 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm981041x
2470 3596 46 None -20 59 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2013.01.025
3300 3596 46 None -20 59 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2013.01.025
5265 3596 46 None -20 59 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2013.01.025
99 3596 46 None -20 59 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2013.01.025
CHEMBL267930 3596 46 None -20 59 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2013.01.025
14925759 157494 6 None 18 13 Human 9.1 pIC50 = 9.1 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4085780 157494 6 None 18 13 Human 9.1 pIC50 = 9.1 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
3303 2213 41 None 1 15 Human 9.0 pIC50 = 9 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00361-8
5311200 2213 41 None 1 15 Human 9.0 pIC50 = 9 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00361-8
CHEMBL267014 2213 41 None 1 15 Human 9.0 pIC50 = 9 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00361-8
10783358 39429 4 None 42 2 Human 9.0 pIC50 = 9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 340 6 1 5 1.6 COc1cccc(C(=O)NCCN2CCN(c3ccccn3)CC2)c1 10.1021/jm981041x
CHEMBL147483 39429 4 None 42 2 Human 9.0 pIC50 = 9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 340 6 1 5 1.6 COc1cccc(C(=O)NCCN2CCN(c3ccccn3)CC2)c1 10.1021/jm981041x
10406796 99540 9 None -19 5 Human 9.0 pIC50 = 9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 369 7 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm981041x
CHEMBL286725 99540 9 None -19 5 Human 9.0 pIC50 = 9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 369 7 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm981041x
11738728 18313 0 None - 1 Human 9.0 pIC50 = 9 Binding
In vitro inhibitory concentration tested on human D4.4 receptor in HEK293 cells using FLIPR assayIn vitro inhibitory concentration tested on human D4.4 receptor in HEK293 cells using FLIPR assay
ChEMBL 320 3 1 3 3.5 Cc1ccc(C)c(N2CCN(Cc3nc4ccccc4[nH]3)CC2)c1 10.1021/jm030505a
CHEMBL127290 18313 0 None - 1 Human 9.0 pIC50 = 9 Binding
In vitro inhibitory concentration tested on human D4.4 receptor in HEK293 cells using FLIPR assayIn vitro inhibitory concentration tested on human D4.4 receptor in HEK293 cells using FLIPR assay
ChEMBL 320 3 1 3 3.5 Cc1ccc(C)c(N2CCN(Cc3nc4ccccc4[nH]3)CC2)c1 10.1021/jm030505a
1353 1880 85 None -3 85 Human 8.9 pIC50 = 8.9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm981041x
3559 1880 85 None -3 85 Human 8.9 pIC50 = 8.9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm981041x
86 1880 85 None -3 85 Human 8.9 pIC50 = 8.9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm981041x
CHEMBL54 1880 85 None -3 85 Human 8.9 pIC50 = 8.9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm981041x
DB00502 1880 85 None -3 85 Human 8.9 pIC50 = 8.9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm981041x
9104271 202299 10 None 436 2 Human 8.8 pIC50 = 8.8 Binding
Inhibitory concentration against dopamine receptor D4Inhibitory concentration against dopamine receptor D4
ChEMBL 369 4 0 3 3.0 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccccc21 10.1021/jm058225d
CHEMBL69584 202299 10 None 436 2 Human 8.8 pIC50 = 8.8 Binding
Inhibitory concentration against dopamine receptor D4Inhibitory concentration against dopamine receptor D4
ChEMBL 369 4 0 3 3.0 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccccc21 10.1021/jm058225d
10497674 17823 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 344 4 0 2 4.4 Fc1ccc([C@H]2C[C@@H]2CN2CCN(c3ccccc3Cl)CC2)cc1 10.1021/jm990562x
CHEMBL1202219 17823 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 344 4 0 2 4.4 Fc1ccc([C@H]2C[C@@H]2CN2CCN(c3ccccc3Cl)CC2)cc1 10.1021/jm990562x
CHEMBL126322 17823 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 344 4 0 2 4.4 Fc1ccc([C@H]2C[C@@H]2CN2CCN(c3ccccc3Cl)CC2)cc1 10.1021/jm990562x
10570563 17846 0 None 15 2 Human 8.0 pIC50 = 8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1Cl 10.1021/jm990562x
CHEMBL1202212 17846 0 None 15 2 Human 8.0 pIC50 = 8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1Cl 10.1021/jm990562x
CHEMBL126429 17846 0 None 15 2 Human 8.0 pIC50 = 8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1Cl 10.1021/jm990562x
127030612 138800 0 None - 1 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 352 5 0 4 3.7 Clc1ccc(CN2CCO[C@H](COc3cccc(Cl)n3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792725 138800 0 None - 1 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 352 5 0 4 3.7 Clc1ccc(CN2CCO[C@H](COc3cccc(Cl)n3)C2)cc1 10.1016/j.bmcl.2016.03.102
127029391 138818 0 None - 1 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 372 6 0 5 3.5 COc1cc(CN2CCO[C@H](COc3cccc(C#N)c3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3792907 138818 0 None - 1 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 372 6 0 5 3.5 COc1cc(CN2CCO[C@H](COc3cccc(C#N)c3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
118714552 114029 0 None 97 2 Human 7.0 pIC50 = 7 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 297 5 1 3 3.2 Oc1ccc(CN2CCO[C@H](CCc3ccccc3)C2)cc1 10.1021/ml500267c
CHEMBL3335555 114029 0 None 97 2 Human 7.0 pIC50 = 7 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 297 5 1 3 3.2 Oc1ccc(CN2CCO[C@H](CCc3ccccc3)C2)cc1 10.1021/ml500267c
135512187 34376 6 None - 0 Human 5.0 pIC50 = 5 Binding
Receptor Binding Assay: Determination of binding to D4.4 receptor was performed using [3H]-YM-09151-2 (70-87 Ci/mmol, 0.3 nM), as a radioligand, in the presence of various concentrations of the tested compound. Reactions were carried out in 50 mM TRIS-HCl (pH 7.4) containing 5 mM MgCl2, 5 mM EDTA, 5 mM KCl and 1.5 mM CaCl2, for 60 minutes at 22° C. The reaction was terminated by rapid vacuum filtration onto glass fiber filters.Receptor Binding Assay: Determination of binding to D4.4 receptor was performed using [3H]-YM-09151-2 (70-87 Ci/mmol, 0.3 nM), as a radioligand, in the presence of various concentrations of the tested compound. Reactions were carried out in 50 mM TRIS-HCl (pH 7.4) containing 5 mM MgCl2, 5 mM EDTA, 5 mM KCl and 1.5 mM CaCl2, for 60 minutes at 22° C. The reaction was terminated by rapid vacuum filtration onto glass fiber filters.
ChEMBL 336 3 2 5 2.0 O=c1[nH]c(CN2CCN(c3ccccc3O)CC2)nc2ccccc12 nan
CHEMBL1429613 34376 6 None - 0 Human 5.0 pIC50 = 5 Binding
Receptor Binding Assay: Determination of binding to D4.4 receptor was performed using [3H]-YM-09151-2 (70-87 Ci/mmol, 0.3 nM), as a radioligand, in the presence of various concentrations of the tested compound. Reactions were carried out in 50 mM TRIS-HCl (pH 7.4) containing 5 mM MgCl2, 5 mM EDTA, 5 mM KCl and 1.5 mM CaCl2, for 60 minutes at 22° C. The reaction was terminated by rapid vacuum filtration onto glass fiber filters.Receptor Binding Assay: Determination of binding to D4.4 receptor was performed using [3H]-YM-09151-2 (70-87 Ci/mmol, 0.3 nM), as a radioligand, in the presence of various concentrations of the tested compound. Reactions were carried out in 50 mM TRIS-HCl (pH 7.4) containing 5 mM MgCl2, 5 mM EDTA, 5 mM KCl and 1.5 mM CaCl2, for 60 minutes at 22° C. The reaction was terminated by rapid vacuum filtration onto glass fiber filters.
ChEMBL 336 3 2 5 2.0 O=c1[nH]c(CN2CCN(c3ccccc3O)CC2)nc2ccccc12 nan
168276065 189626 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 320 5 0 3 4.0 Cc1ccc(CO[C@H]2CCCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2022.128615
CHEMBL5174753 189626 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 320 5 0 3 4.0 Cc1ccc(CO[C@H]2CCCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2022.128615
127030606 138832 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 318 5 0 4 3.0 Clc1ccc(CN2CCO[C@H](COc3cccnc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793033 138832 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 318 5 0 4 3.0 Clc1ccc(CN2CCO[C@H](COc3cccnc3)C2)cc1 10.1016/j.bmcl.2016.03.102
155516494 169554 0 None 269 2 Human 5.0 pIC50 = 5.0 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 358 5 1 4 3.1 CCc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4443848 169554 0 None 269 2 Human 5.0 pIC50 = 5.0 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 358 5 1 4 3.1 CCc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
168296347 191864 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 344 6 0 4 3.7 COc1ccc(CN2CCC[C@H](OCc3cccc(C)n3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5208643 191864 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 344 6 0 4 3.7 COc1ccc(CN2CCC[C@H](OCc3cccc(C)n3)C2)cc1F 10.1016/j.bmcl.2022.128615
109030343 170293 1 None 15 3 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 324 5 1 4 2.5 Cc1cccc(NC(=O)CCN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4454068 170293 1 None 15 3 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 324 5 1 4 2.5 Cc1cccc(NC(=O)CCN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
127028185 138806 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 375 5 1 4 3.6 Fc1ccc2c(CN3CCO[C@H](COc4cccc(Cl)n4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3792751 138806 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 375 5 1 4 3.6 Fc1ccc2c(CN3CCO[C@H](COc4cccc(Cl)n4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
16104 161368 15 None -1 5 Human 7.0 pIC50 = 7.0 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm991005d
CHEMBL415300 161368 15 None -1 5 Human 7.0 pIC50 = 7.0 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm991005d
135398737 944 89 None -13 91 Human 7.0 pIC50 = 7.0 Binding
Displacement of radiolabeled clozapine from human dopamine D4.4 receptorDisplacement of radiolabeled clozapine from human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm8007618
38 944 89 None -13 91 Human 7.0 pIC50 = 7.0 Binding
Displacement of radiolabeled clozapine from human dopamine D4.4 receptorDisplacement of radiolabeled clozapine from human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm8007618
722 944 89 None -13 91 Human 7.0 pIC50 = 7.0 Binding
Displacement of radiolabeled clozapine from human dopamine D4.4 receptorDisplacement of radiolabeled clozapine from human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm8007618
CHEMBL42 944 89 None -13 91 Human 7.0 pIC50 = 7.0 Binding
Displacement of radiolabeled clozapine from human dopamine D4.4 receptorDisplacement of radiolabeled clozapine from human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm8007618
DB00363 944 89 None -13 91 Human 7.0 pIC50 = 7.0 Binding
Displacement of radiolabeled clozapine from human dopamine D4.4 receptorDisplacement of radiolabeled clozapine from human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm8007618
10645208 35960 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 409 7 0 6 4.2 COc1cccc(-c2csc(CCN3CCN(c4ccccc4OC)CC3)n2)c1 10.1021/jm981041x
CHEMBL144494 35960 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 409 7 0 6 4.2 COc1cccc(-c2csc(CCN3CCN(c4ccccc4OC)CC3)n2)c1 10.1021/jm981041x
CHEMBL2373205 35960 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 409 7 0 6 4.2 COc1cccc(-c2csc(CCN3CCN(c4ccccc4OC)CC3)n2)c1 10.1021/jm981041x
9868793 96529 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Percent inhibition towards dopamine D4 receptorPercent inhibition towards dopamine D4 receptor
ChEMBL 458 8 1 8 2.8 COc1nsnc1N1CCN(C[C@@H](Cc2cccnc2)NC(=O)C2(C)CCCCC2)CC1 10.1016/s0960-894x(01)00151-2
CHEMBL266393 96529 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Percent inhibition towards dopamine D4 receptorPercent inhibition towards dopamine D4 receptor
ChEMBL 458 8 1 8 2.8 COc1nsnc1N1CCN(C[C@@H](Cc2cccnc2)NC(=O)C2(C)CCCCC2)CC1 10.1016/s0960-894x(01)00151-2
127053218 138948 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 334 5 0 4 3.5 c1ccc(OC[C@@H]2CN(Cc3ccc4ccccc4n3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3794336 138948 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 334 5 0 4 3.5 c1ccc(OC[C@@H]2CN(Cc3ccc4ccccc4n3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
1016 3690 75 None -28 35 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 3690 75 None -28 35 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 3690 75 None -28 35 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
5384 3690 75 None -28 35 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 3690 75 None -28 35 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 3690 75 None -28 35 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
70788951 26948 1 None -1 5 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL None None None None nan
CHEMBL1366 26948 1 None -1 5 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL None None None None nan
72737750 114025 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 299 5 0 2 3.7 Fc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
CHEMBL3335543 114025 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 299 5 0 2 3.7 Fc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
168288343 190861 0 None 1 2 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 440 6 1 3 5.3 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2022.128615
CHEMBL5193214 190861 0 None 1 2 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 440 6 1 3 5.3 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2022.128615
10236758 115272 3 None 208 13 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL3354065 115272 3 None 208 13 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
9954899 202758 15 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 440 2 1 7 3.3 CN1CCN(C2=Nc3ccccc3Nc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
CHEMBL72292 202758 15 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 440 2 1 7 3.3 CN1CCN(C2=Nc3ccccc3Nc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
44363755 121345 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 423 7 1 5 2.9 COc1ccccc1N1CCN(CCC(=O)NC2CCc3c(cccc3OC)C2)CC1 10.1021/jm981041x
CHEMBL359002 121345 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 423 7 1 5 2.9 COc1ccccc1N1CCN(CCC(=O)NC2CCc3c(cccc3OC)C2)CC1 10.1021/jm981041x
135398737 944 89 None -13 91 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human dopamine D4.4 receptorInhibition of human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2010.07.034
38 944 89 None -13 91 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human dopamine D4.4 receptorInhibition of human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2010.07.034
722 944 89 None -13 91 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human dopamine D4.4 receptorInhibition of human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2010.07.034
CHEMBL42 944 89 None -13 91 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human dopamine D4.4 receptorInhibition of human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2010.07.034
DB00363 944 89 None -13 91 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human dopamine D4.4 receptorInhibition of human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2010.07.034
168270809 189455 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 392 6 1 3 4.0 Cc1cc(NC(=O)CN2CCC(OCc3ccc(F)c(F)c3)CC2)ccc1F 10.1016/j.bmcl.2022.128615
CHEMBL5172055 189455 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 392 6 1 3 4.0 Cc1cc(NC(=O)CN2CCC(OCc3ccc(F)c(F)c3)CC2)ccc1F 10.1016/j.bmcl.2022.128615
118719926 115280 0 None 102 8 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL3354073 115280 0 None 102 8 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/acs.jmedchem.8b00265
3191 102385 93 None -10 25 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 102385 93 None -10 25 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
127032084 138811 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 322 5 1 3 3.4 c1ccc(OC[C@@H]2CN(Cc3cccc4cc[nH]c34)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792813 138811 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 322 5 1 3 3.4 c1ccc(OC[C@@H]2CN(Cc3cccc4cc[nH]c34)CCO2)cc1 10.1016/j.bmcl.2016.03.102
127031500 138820 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 323 5 0 5 2.6 c1ccc(OC[C@@H]2CN(Cc3ncn4ccccc34)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792931 138820 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 323 5 0 5 2.6 c1ccc(OC[C@@H]2CN(Cc3ncn4ccccc34)CCO2)cc1 10.1016/j.bmcl.2016.03.102
127031201 138845 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 372 6 0 5 3.5 COc1ccc(CN2CCO[C@H](COc3cccc(C#N)c3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3793131 138845 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 372 6 0 5 3.5 COc1ccc(CN2CCO[C@H](COc3cccc(C#N)c3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
127031830 138902 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 356 5 1 3 4.1 Clc1ccc2[nH]cc(CN3CCO[C@H](COc4ccccc4)C3)c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3793906 138902 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 356 5 1 3 4.1 Clc1ccc2[nH]cc(CN3CCO[C@H](COc4ccccc4)C3)c2c1 10.1016/j.bmcl.2016.03.102
127031513 138944 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1cccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)c1 10.1016/j.bmcl.2016.03.102
CHEMBL3794287 138944 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1cccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)c1 10.1016/j.bmcl.2016.03.102
72737723 2541 1 None - 1 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 315 5 0 2 4.2 Clc1ccc(cc1)CN1CCO[C@@H](C1)CCc1ccccc1 10.1021/ml500267c
8440 2541 1 None - 1 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 315 5 0 2 4.2 Clc1ccc(cc1)CN1CCO[C@@H](C1)CCc1ccccc1 10.1021/ml500267c
CHEMBL3335556 2541 1 None - 1 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 315 5 0 2 4.2 Clc1ccc(cc1)CN1CCO[C@@H](C1)CCc1ccccc1 10.1021/ml500267c
9904205 204135 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against Dopamine receptor D4Binding affinity against Dopamine receptor D4
ChEMBL 294 2 0 3 3.4 CN(C)CC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(02)00796-5
CHEMBL83658 204135 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against Dopamine receptor D4Binding affinity against Dopamine receptor D4
ChEMBL 294 2 0 3 3.4 CN(C)CC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(02)00796-5
9904205 204135 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 294 2 0 3 3.4 CN(C)CC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL83658 204135 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 294 2 0 3 3.4 CN(C)CC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
10594723 16863 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@@H]3C[C@H]3c3ccccc3)CC2)c(Cl)c1 10.1021/jm990562x
CHEMBL125455 16863 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@@H]3C[C@H]3c3ccccc3)CC2)c(Cl)c1 10.1021/jm990562x
163322330 190106 3 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5182191 190106 3 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
168287664 191056 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3cn4ccccc4n3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
CHEMBL5196102 191056 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3cn4ccccc4n3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
168273063 189691 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(CO[C@H]2CCCN(Cc3ncn4ccccc34)C2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5175728 189691 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(CO[C@H]2CCCN(Cc3ncn4ccccc34)C2)c1 10.1016/j.bmcl.2022.128615
16094666 81315 2 None 52 3 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL216393 81315 2 None 52 3 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/acs.jmedchem.9b00231
2726 906 64 None -8 72 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 906 64 None -8 72 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 906 64 None -8 72 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 906 64 None -8 72 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 906 64 None -8 72 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
135398737 944 89 None -13 91 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against dopamine receptor D4Inhibitory concentration against dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm058225d
38 944 89 None -13 91 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against dopamine receptor D4Inhibitory concentration against dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm058225d
722 944 89 None -13 91 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against dopamine receptor D4Inhibitory concentration against dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm058225d
CHEMBL42 944 89 None -13 91 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against dopamine receptor D4Inhibitory concentration against dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm058225d
DB00363 944 89 None -13 91 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against dopamine receptor D4Inhibitory concentration against dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm058225d
168293190 191532 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 363 5 0 2 5.5 Cc1ccc(CO[C@H]2CCCN(Cc3ccc(Cl)c(Cl)c3)C2)cc1 10.1016/j.bmcl.2022.128615
CHEMBL5203595 191532 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 363 5 0 2 5.5 Cc1ccc(CO[C@H]2CCCN(Cc3ccc(Cl)c(Cl)c3)C2)cc1 10.1016/j.bmcl.2022.128615
1613 2316 44 None -2 44 Human 7.9 pIC50 = 7.9 Binding
Compound was tested in vitro for its binding affinity towards human Dopamine receptor D4.2Compound was tested in vitro for its binding affinity towards human Dopamine receptor D4.2
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm991005d
205 2316 44 None -2 44 Human 7.9 pIC50 = 7.9 Binding
Compound was tested in vitro for its binding affinity towards human Dopamine receptor D4.2Compound was tested in vitro for its binding affinity towards human Dopamine receptor D4.2
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm991005d
3964 2316 44 None -2 44 Human 7.9 pIC50 = 7.9 Binding
Compound was tested in vitro for its binding affinity towards human Dopamine receptor D4.2Compound was tested in vitro for its binding affinity towards human Dopamine receptor D4.2
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm991005d
CHEMBL831 2316 44 None -2 44 Human 7.9 pIC50 = 7.9 Binding
Compound was tested in vitro for its binding affinity towards human Dopamine receptor D4.2Compound was tested in vitro for its binding affinity towards human Dopamine receptor D4.2
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm991005d
DB00408 2316 44 None -2 44 Human 7.9 pIC50 = 7.9 Binding
Compound was tested in vitro for its binding affinity towards human Dopamine receptor D4.2Compound was tested in vitro for its binding affinity towards human Dopamine receptor D4.2
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm991005d
44318454 204290 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 312 2 0 3 3.5 CN(C)CC1CC2c3ccccc3Cc3ccc(F)cc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL84931 204290 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 312 2 0 3 3.5 CN(C)CC1CC2c3ccccc3Cc3ccc(F)cc3N2O1 10.1016/s0960-894x(01)00721-1
10894144 110070 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 377 7 0 4 3.5 N#Cc1ccc(CCOC(=O)N2CCN(CCCc3ccccc3)CC2)cc1 10.1021/jm010878g
CHEMBL325258 110070 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 377 7 0 4 3.5 N#Cc1ccc(CCOC(=O)N2CCN(CCCc3ccccc3)CC2)cc1 10.1021/jm010878g
168277992 189535 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 371 5 0 4 4.0 Cn1cnc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
CHEMBL5173368 189535 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 371 5 0 4 4.0 Cn1cnc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
100 3745 52 None -8 55 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
2637 3745 52 None -8 55 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
5452 3745 52 None -8 55 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
CHEMBL479 3745 52 None -8 55 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
DB00679 3745 52 None -8 55 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
168269421 189369 0 None 6 3 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 390 5 1 2 5.3 Fc1ccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5170670 189369 0 None 6 3 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 390 5 1 2 5.3 Fc1ccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)cc1F 10.1016/j.bmcl.2022.128615
20354789 114026 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 281 5 0 2 3.5 c1ccc(CCC2CN(Cc3ccccc3)CCO2)cc1 10.1021/ml500267c
CHEMBL3335544 114026 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 281 5 0 2 3.5 c1ccc(CCC2CN(Cc3ccccc3)CCO2)cc1 10.1021/ml500267c
10026300 167271 15 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 441 2 0 7 3.3 CN1CCN(C2=Nc3ccccc3Oc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
CHEMBL430798 167271 15 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 441 2 0 7 3.3 CN1CCN(C2=Nc3ccccc3Oc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
93601125 138821 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 343 7 0 5 3.0 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1OC 10.1016/j.bmcl.2016.03.102
CHEMBL3792941 138821 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 343 7 0 5 3.0 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1OC 10.1016/j.bmcl.2016.03.102
127053198 138842 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 317 5 0 3 3.6 Clc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793112 138842 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 317 5 0 3 3.6 Clc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
127029390 138953 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1ccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3794421 138953 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1ccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
118719926 115280 0 None 102 8 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL3354073 115280 0 None 102 8 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/acs.jmedchem.8b00265
168282745 190501 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
CHEMBL5187721 190501 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
4189 205195 91 None -33 34 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 205195 91 None -33 34 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 205195 91 None -33 34 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
135398737 944 89 None -13 91 Human 6.8 pIC50 = 6.8 Binding
Percent inhibition against Dopamine receptor D4 at 1 uMPercent inhibition against Dopamine receptor D4 at 1 uM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm058018d
38 944 89 None -13 91 Human 6.8 pIC50 = 6.8 Binding
Percent inhibition against Dopamine receptor D4 at 1 uMPercent inhibition against Dopamine receptor D4 at 1 uM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm058018d
722 944 89 None -13 91 Human 6.8 pIC50 = 6.8 Binding
Percent inhibition against Dopamine receptor D4 at 1 uMPercent inhibition against Dopamine receptor D4 at 1 uM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm058018d
CHEMBL42 944 89 None -13 91 Human 6.8 pIC50 = 6.8 Binding
Percent inhibition against Dopamine receptor D4 at 1 uMPercent inhibition against Dopamine receptor D4 at 1 uM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm058018d
DB00363 944 89 None -13 91 Human 6.8 pIC50 = 6.8 Binding
Percent inhibition against Dopamine receptor D4 at 1 uMPercent inhibition against Dopamine receptor D4 at 1 uM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm058018d
168297637 191725 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3ncc4ccccn34)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
CHEMBL5206427 191725 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3ncc4ccccn34)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
21186194 201544 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 360 5 0 5 3.5 COc1ccccc1-c1cccc(CN2CCN(c3ncccn3)CC2)c1 10.1016/s0960-894x(98)00361-8
CHEMBL64487 201544 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 360 5 0 5 3.5 COc1ccccc1-c1cccc(CN2CCN(c3ncccn3)CC2)c1 10.1016/s0960-894x(98)00361-8
10739194 116326 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 390 5 0 3 4.9 COc1c(Cl)cc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1Cl 10.1021/jm990562x
CHEMBL1202204 116326 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 390 5 0 3 4.9 COc1c(Cl)cc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1Cl 10.1021/jm990562x
CHEMBL337951 116326 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 390 5 0 3 4.9 COc1c(Cl)cc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1Cl 10.1021/jm990562x
127053215 138894 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 313 6 0 4 3.0 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793858 138894 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 313 6 0 4 3.0 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
72737744 114020 0 None 64 3 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 365 6 0 3 4.4 FC(F)(F)Oc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
CHEMBL3335538 114020 0 None 64 3 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 365 6 0 3 4.4 FC(F)(F)Oc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
168275962 190025 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 353 5 0 4 4.0 Cc1cc(CO[C@H]2CCCN(Cc3ncn4ccccc34)C2)ccc1F 10.1016/j.bmcl.2022.128615
CHEMBL5180979 190025 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 353 5 0 4 4.0 Cc1cc(CO[C@H]2CCCN(Cc3ncn4ccccc34)C2)ccc1F 10.1016/j.bmcl.2022.128615
10713599 19204 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1cc(Cl)cc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c1 10.1021/jm990562x
CHEMBL1202225 19204 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1cc(Cl)cc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c1 10.1021/jm990562x
CHEMBL129324 19204 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1cc(Cl)cc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c1 10.1021/jm990562x
168275089 189902 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3cn4ccccc4n3)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5179198 189902 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3cn4ccccc4n3)CC2)c1 10.1016/j.bmcl.2022.128615
168279825 190222 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(COC2CCN(Cc3cn4ccccc4n3)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5183902 190222 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(COC2CCN(Cc3cn4ccccc4n3)CC2)c1 10.1016/j.bmcl.2022.128615
168283295 190641 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 327 5 0 2 4.6 Cc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1 10.1016/j.bmcl.2022.128615
CHEMBL5189986 190641 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 327 5 0 2 4.6 Cc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1 10.1016/j.bmcl.2022.128615
168291848 191276 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(COC2CCN(Cc3ncn4ccccc34)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5199552 191276 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(COC2CCN(Cc3ncn4ccccc34)CC2)c1 10.1016/j.bmcl.2022.128615
137640201 156419 2 None 177 13 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4072818 156419 2 None 177 13 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
168290895 191401 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 387 5 0 4 4.5 Cn1ncc2cc(CN3CCC(OCc4ccc(Cl)c(F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
CHEMBL5201507 191401 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 387 5 0 4 4.5 Cn1ncc2cc(CN3CCC(OCc4ccc(Cl)c(F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
168292124 191427 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 365 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccc(F)c(F)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5201917 191427 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 365 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccc(F)c(F)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
44342270 9837 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 355 3 1 4 4.5 Cc1ccc(CN2CCC(n3c(O)nc4ccccc43)CC2)c(Cl)c1 10.1021/jm010878g
CHEMBL114484 9837 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 355 3 1 4 4.5 Cc1ccc(CN2CCC(n3c(O)nc4ccccc43)CC2)c(Cl)c1 10.1021/jm010878g
21186143 201587 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 360 5 0 5 3.5 COc1cccc(-c2cccc(CN3CCN(c4ncccn4)CC3)c2)c1 10.1016/s0960-894x(98)00361-8
CHEMBL64671 201587 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 360 5 0 5 3.5 COc1cccc(-c2cccc(CN3CCN(c4ncccn4)CC3)c2)c1 10.1016/s0960-894x(98)00361-8
135398737 944 89 None -13 91 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm990562x
38 944 89 None -13 91 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm990562x
722 944 89 None -13 91 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm990562x
CHEMBL42 944 89 None -13 91 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm990562x
DB00363 944 89 None -13 91 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm990562x
9797161 116393 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 320 4 0 2 4.2 Cc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(C)c1 10.1021/jm990562x
CHEMBL1204119 116393 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 320 4 0 2 4.2 Cc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(C)c1 10.1021/jm990562x
CHEMBL338337 116393 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 320 4 0 2 4.2 Cc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(C)c1 10.1021/jm990562x
127032086 138792 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 337 5 0 5 2.9 Cn1ncc2cc(CN3CCO[C@H](COc4ccccc4)C3)ccc21 10.1016/j.bmcl.2016.03.102
CHEMBL3792637 138792 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 337 5 0 5 2.9 Cn1ncc2cc(CN3CCO[C@H](COc4ccccc4)C3)ccc21 10.1016/j.bmcl.2016.03.102
72737728 114021 0 None 60 2 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 311 6 0 3 3.5 COc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
CHEMBL3335539 114021 0 None 60 2 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 311 6 0 3 3.5 COc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
135398745 2869 108 None -10 65 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm960268u
47 2869 108 None -10 65 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm960268u
CHEMBL715 2869 108 None -10 65 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm960268u
DB00334 2869 108 None -10 65 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm960268u
168292951 191550 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5203807 191550 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)cc1F 10.1016/j.bmcl.2022.128615
176 394 63 None -4 31 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 394 63 None -4 31 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 394 63 None -4 31 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 394 63 None -4 31 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 394 63 None -4 31 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
53320010 56370 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in cellsDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in cells
ChEMBL 435 3 0 5 3.4 CN1CCN(c2cccc3c2C(=O)CCN3S(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2010.12.007
CHEMBL1642117 56370 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in cellsDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in cells
ChEMBL 435 3 0 5 3.4 CN1CCN(c2cccc3c2C(=O)CCN3S(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2010.12.007
127031832 138885 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 340 5 1 3 3.6 Fc1ccc2c(CN3CCO[C@H](COc4ccccc4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3793782 138885 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 340 5 1 3 3.6 Fc1ccc2c(CN3CCO[C@H](COc4ccccc4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
127030909 138951 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 367 6 0 4 3.9 FC(F)(F)Oc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3794375 138951 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 367 6 0 4 3.9 FC(F)(F)Oc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
60149678 114019 0 None 229 2 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 321 5 1 3 3.4 c1ccc(CC[C@@H]2CN(Cc3nc4ccccc4[nH]3)CCO2)cc1 10.1021/ml500267c
CHEMBL3335537 114019 0 None 229 2 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 321 5 1 3 3.4 c1ccc(CC[C@@H]2CN(Cc3nc4ccccc4[nH]3)CCO2)cc1 10.1021/ml500267c
42 2032 50 None - 17 Human 5.8 pIC50 = 5.8 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm040792y
56971 2032 50 None - 17 Human 5.8 pIC50 = 5.8 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm040792y
CHEMBL8412 2032 50 None - 17 Human 5.8 pIC50 = 5.8 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm040792y
168279082 190139 0 None -1 2 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5182602 190139 0 None -1 2 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)c1 10.1016/j.bmcl.2022.128615
168280464 190142 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 335 5 0 4 3.8 Cc1ccccc1CO[C@H]1CCCN(Cc2cn3ccccc3n2)C1 10.1016/j.bmcl.2022.128615
CHEMBL5182635 190142 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 335 5 0 4 3.8 Cc1ccccc1CO[C@H]1CCCN(Cc2cn3ccccc3n2)C1 10.1016/j.bmcl.2022.128615
45109862 7353 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 470 7 2 3 5.2 Cc1[nH]c(-c2ccccc2)cc1C(=O)NCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2010.01.093
CHEMBL1086626 7353 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 470 7 2 3 5.2 Cc1[nH]c(-c2ccccc2)cc1C(=O)NCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2010.01.093
168271806 189925 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 353 5 0 4 4.0 Cc1cc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)ccc1F 10.1016/j.bmcl.2022.128615
CHEMBL5179482 189925 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 353 5 0 4 4.0 Cc1cc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)ccc1F 10.1016/j.bmcl.2022.128615
10981761 110149 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 379 3 1 6 2.6 O=C1NCN(c2ccccc2)C12CCN(Cc1ccc3nsnc3c1)CC2 10.1021/jm010878g
CHEMBL325750 110149 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 379 3 1 6 2.6 O=C1NCN(c2ccccc2)C12CCN(Cc1ccc3nsnc3c1)CC2 10.1021/jm010878g
127031831 138810 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 352 6 1 4 3.5 COc1ccc2c(CN3CCO[C@H](COc4ccccc4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3792805 138810 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 352 6 1 4 3.5 COc1ccc2c(CN3CCO[C@H](COc4ccccc4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
10425450 199 23 None -1 4 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
3301 199 23 None -1 4 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
CHEMBL375596 199 23 None -1 4 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
168280776 190564 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5188602 190564 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.bmcl.2022.128615
6466372 169495 12 None 93 3 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 311 4 1 5 1.5 Cc1cccc(NC(=O)CN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4443054 169495 12 None 93 3 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 311 4 1 5 1.5 Cc1cccc(NC(=O)CN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
168275381 189676 0 None 4 2 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 403 5 0 4 4.8 Cn1ncc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
CHEMBL5175548 189676 0 None 4 2 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 403 5 0 4 4.8 Cn1ncc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
2812 4711 96 None -39 34 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 4711 96 None -39 34 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
168280974 190269 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5184607 190269 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
21186186 198946 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 348 4 0 4 3.6 Fc1ccc(-c2cccc(CN3CCN(c4ncccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
CHEMBL59942 198946 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 348 4 0 4 3.6 Fc1ccc(-c2cccc(CN3CCN(c4ncccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
44336061 108134 0 None 56 2 Human 8.7 pIC50 = 8.7 Binding
Inhibitory concentration against dopamine receptor D4Inhibitory concentration against dopamine receptor D4
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1021/jm058225d
CHEMBL320597 108134 0 None 56 2 Human 8.7 pIC50 = 8.7 Binding
Inhibitory concentration against dopamine receptor D4Inhibitory concentration against dopamine receptor D4
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1021/jm058225d
10381889 106586 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity against Dopamine receptor D4Binding affinity against Dopamine receptor D4
ChEMBL 328 2 0 3 4.1 CN(C)CC1CC2c3ccccc3Cc3ccc(Cl)cc3N2O1 10.1016/s0960-894x(02)00796-5
CHEMBL315772 106586 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity against Dopamine receptor D4Binding affinity against Dopamine receptor D4
ChEMBL 328 2 0 3 4.1 CN(C)CC1CC2c3ccccc3Cc3ccc(Cl)cc3N2O1 10.1016/s0960-894x(02)00796-5
10381889 106586 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 328 2 0 3 4.1 CN(C)CC1CC2c3ccccc3Cc3ccc(Cl)cc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL315772 106586 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 328 2 0 3 4.1 CN(C)CC1CC2c3ccccc3Cc3ccc(Cl)cc3N2O1 10.1016/s0960-894x(01)00721-1
10643697 120610 1 None 10 4 Human 8.6 pIC50 = 8.6 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 383 8 1 5 2.6 COc1cccc(C(=O)NCCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm981041x
CHEMBL357448 120610 1 None 10 4 Human 8.6 pIC50 = 8.6 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 383 8 1 5 2.6 COc1cccc(C(=O)NCCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm981041x
10450082 101844 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 342 3 0 4 3.4 c1cnc(N2CCN(Cc3cccc4c3Cc3ccccc3-4)CC2)nc1 10.1016/s0960-894x(98)00361-8
CHEMBL303519 101844 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 342 3 0 4 3.4 c1cnc(N2CCN(Cc3cccc4c3Cc3ccccc3-4)CC2)nc1 10.1016/s0960-894x(98)00361-8
168294958 191806 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 347 6 0 3 4.2 COc1ccc(CN2CCC[C@H](OCc3cccc(F)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5207898 191806 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 347 6 0 3 4.2 COc1ccc(CN2CCC[C@H](OCc3cccc(F)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
168289523 190903 0 None 5 2 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 422 5 1 2 6.0 FC(F)(F)c1cccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5193761 190903 0 None 5 2 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 422 5 1 2 6.0 FC(F)(F)c1cccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)c1 10.1016/j.bmcl.2022.128615
168285068 190987 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3ncc4ccccn34)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5195130 190987 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3ncc4ccccn34)CC2)c1 10.1016/j.bmcl.2022.128615
127027237 138856 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 314 6 0 5 2.4 COc1ccc(CN2CCO[C@H](COc3cccnc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793264 138856 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 314 6 0 5 2.4 COc1ccc(CN2CCO[C@H](COc3cccnc3)C2)cc1 10.1016/j.bmcl.2016.03.102
168275717 189625 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3ncc4ccccn34)CC2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5174731 189625 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3ncc4ccccn34)CC2)cc1F 10.1016/j.bmcl.2022.128615
135398737 944 89 None -13 91 Human 7.6 pIC50 = 7.6 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm981041x
38 944 89 None -13 91 Human 7.6 pIC50 = 7.6 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm981041x
722 944 89 None -13 91 Human 7.6 pIC50 = 7.6 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm981041x
CHEMBL42 944 89 None -13 91 Human 7.6 pIC50 = 7.6 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm981041x
DB00363 944 89 None -13 91 Human 7.6 pIC50 = 7.6 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm981041x
72737730 114028 0 None 42 3 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 365 6 0 3 4.4 FC(F)(F)Oc1ccc(CN2CCO[C@H](CCc3ccccc3)C2)cc1 10.1021/ml500267c
CHEMBL3335554 114028 0 None 42 3 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 365 6 0 3 4.4 FC(F)(F)Oc1ccc(CN2CCO[C@H](CCc3ccccc3)C2)cc1 10.1021/ml500267c
2274 3124 53 None -56 32 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 3124 53 None -56 32 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 3124 53 None -56 32 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 3124 53 None -56 32 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 3124 53 None -56 32 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
155568411 175506 0 None - 1 Human 4.6 pIC50 = 4.6 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 331 4 1 5 1.9 O=C(CN1CCN(c2ccc(Cl)cn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
CHEMBL4591118 175506 0 None - 1 Human 4.6 pIC50 = 4.6 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 331 4 1 5 1.9 O=C(CN1CCN(c2ccc(Cl)cn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
168281091 190477 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccc(C)cc3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5187429 190477 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccc(C)cc3)C2)cc1F 10.1016/j.bmcl.2022.128615
21186148 200504 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 349 4 0 5 3.0 Fc1ccc(-c2cncc(CN3CCN(c4cnccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
CHEMBL60957 200504 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 349 4 0 5 3.0 Fc1ccc(-c2cncc(CN3CCN(c4cnccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
10108561 112445 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against Dopamine receptor D4Binding affinity against Dopamine receptor D4
ChEMBL 295 2 0 4 2.8 CN(C)CC1CC2c3ccccc3Cc3ccncc3N2O1 10.1016/s0960-894x(02)00796-5
CHEMBL331077 112445 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against Dopamine receptor D4Binding affinity against Dopamine receptor D4
ChEMBL 295 2 0 4 2.8 CN(C)CC1CC2c3ccccc3Cc3ccncc3N2O1 10.1016/s0960-894x(02)00796-5
155568867 175580 0 None - 1 Human 4.6 pIC50 = 4.6 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 297 4 1 5 1.2 O=C(CN1CCN(c2ccccn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
CHEMBL4592753 175580 0 None - 1 Human 4.6 pIC50 = 4.6 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 297 4 1 5 1.2 O=C(CN1CCN(c2ccccn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
127028183 138786 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 366 6 0 5 3.2 COc1ccc(CN2CCO[C@H](COc3cccc(F)n3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3792532 138786 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 366 6 0 5 3.2 COc1ccc(CN2CCO[C@H](COc3cccc(F)n3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
127032085 138858 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 363 5 0 5 3.3 FC1(F)Oc2ccc(CN3CCO[C@H](COc4ccccc4)C3)cc2O1 10.1016/j.bmcl.2016.03.102
CHEMBL3793266 138858 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 363 5 0 5 3.3 FC1(F)Oc2ccc(CN3CCO[C@H](COc4ccccc4)C3)cc2O1 10.1016/j.bmcl.2016.03.102
155513053 169131 0 None 6 3 Human 5.6 pIC50 = 5.6 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 323 5 1 3 3.5 CCc1cccc(NC(=O)CN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4437912 169131 0 None 6 3 Human 5.6 pIC50 = 5.6 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 323 5 1 3 3.5 CCc1cccc(NC(=O)CN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
127027238 138881 0 None - 1 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 318 5 0 4 3.0 Clc1ccc(CN2CCO[C@H](COc3ccccn3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793709 138881 0 None - 1 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 318 5 0 4 3.0 Clc1ccc(CN2CCO[C@H](COc3ccccn3)C2)cc1 10.1016/j.bmcl.2016.03.102
45482789 197247 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of dopamine D4.4 receptorInhibition of dopamine D4.4 receptor
ChEMBL 428 4 2 2 4.5 CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 10.1016/j.bmcl.2009.09.002
CHEMBL584554 197247 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of dopamine D4.4 receptorInhibition of dopamine D4.4 receptor
ChEMBL 428 4 2 2 4.5 CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 10.1016/j.bmcl.2009.09.002
127027905 138926 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 327 5 0 3 4.3 Cc1ccc(CN2CCO[C@H](CSc3ccccc3)C2)cc1C 10.1016/j.bmcl.2016.03.102
CHEMBL3794079 138926 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 327 5 0 3 4.3 Cc1ccc(CN2CCO[C@H](CSc3ccccc3)C2)cc1C 10.1016/j.bmcl.2016.03.102
135418440 11963 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Inhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptorInhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptor
ChEMBL 351 5 1 6 2.3 c1ccc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL1183663 11963 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Inhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptorInhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptor
ChEMBL 351 5 1 6 2.3 c1ccc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL310311 11963 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Inhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptorInhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptor
ChEMBL 351 5 1 6 2.3 c1ccc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
168296363 191919 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 371 5 0 4 4.0 Cn1ncc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
CHEMBL5209344 191919 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 371 5 0 4 4.0 Cn1ncc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
10092041 164980 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 394 7 0 4 4.7 COc1ccc2c(c1)C(CCCN1CCN(c3ccccc3OC)CC1)CCC2 10.1021/jm981041x
CHEMBL424125 164980 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 394 7 0 4 4.7 COc1ccc2c(c1)C(CCCN1CCN(c3ccccc3OC)CC1)CCC2 10.1021/jm981041x
11730467 10925 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 476 10 0 2 6.0 O=C(CCCc1ccccc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
CHEMBL117537 10925 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 476 10 0 2 6.0 O=C(CCCc1ccccc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
10688858 17911 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 344 4 0 2 4.4 Fc1ccc([C@H]2C[C@@H]2CN2CCN(c3cccc(Cl)c3)CC2)cc1 10.1021/jm990562x
CHEMBL1202223 17911 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 344 4 0 2 4.4 Fc1ccc([C@H]2C[C@@H]2CN2CCN(c3cccc(Cl)c3)CC2)cc1 10.1021/jm990562x
CHEMBL126793 17911 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 344 4 0 2 4.4 Fc1ccc([C@H]2C[C@@H]2CN2CCN(c3cccc(Cl)c3)CC2)cc1 10.1021/jm990562x
131396 205008 6 None 1 5 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 435 6 0 5 4.6 CC1SC(C)(C)C(=O)N1CCCCN1CCN(c2csc3cc(F)ccc23)CC1 10.1021/jm960268u
CHEMBL89934 205008 6 None 1 5 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 435 6 0 5 4.6 CC1SC(C)(C)C(=O)N1CCCCN1CCN(c2csc3cc(F)ccc23)CC1 10.1021/jm960268u
44304600 201573 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 344 3 0 5 3.7 c1cnc(N2CCN(Cc3cccc4c3oc3ccccc34)CC2)nc1 10.1016/s0960-894x(98)00361-8
CHEMBL64622 201573 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 344 3 0 5 3.7 c1cnc(N2CCN(Cc3cccc4c3oc3ccccc34)CC2)nc1 10.1016/s0960-894x(98)00361-8
72737767 114022 4 None - 1 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 315 5 0 2 4.2 Clc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
CHEMBL3335540 114022 4 None - 1 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 315 5 0 2 4.2 Clc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
21186115 201018 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 365 4 0 3 4.3 Fc1ccc(-c2cncc(CN3CCN(c4ccccc4F)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
CHEMBL61682 201018 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 365 4 0 3 4.3 Fc1ccc(-c2cncc(CN3CCN(c4ccccc4F)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
9949655 201567 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 336 4 0 5 3.5 c1cnc(N2CCN(Cc3cccc(-c4ccsc4)c3)CC2)nc1 10.1016/s0960-894x(98)00361-8
CHEMBL64597 201567 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 336 4 0 5 3.5 c1cnc(N2CCN(Cc3cccc(-c4ccsc4)c3)CC2)nc1 10.1016/s0960-894x(98)00361-8
10666005 17770 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 356 5 0 3 4.3 COc1cc(Cl)ccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL1202211 17770 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 356 5 0 3 4.3 COc1cc(Cl)ccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL126032 17770 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 356 5 0 3 4.3 COc1cc(Cl)ccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
10829708 17860 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 322 5 0 3 3.6 COc1ccccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL1202216 17860 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 322 5 0 3 3.6 COc1ccccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL126509 17860 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 322 5 0 3 3.6 COc1ccccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
9799123 5543 0 None 35 2 Human 8.5 pIC50 = 8.5 Binding
Inhibitory concentration against dopamine receptor D4Inhibitory concentration against dopamine receptor D4
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1021/jm058225d
CHEMBL107742 5543 0 None 35 2 Human 8.5 pIC50 = 8.5 Binding
Inhibitory concentration against dopamine receptor D4Inhibitory concentration against dopamine receptor D4
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1021/jm058225d
11726532 96578 0 None -2 4 Human 8.5 pIC50 = 8.5 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 368 8 0 5 3.5 COc1cccc(C(=O)CCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm981041x
CHEMBL26677 96578 0 None -2 4 Human 8.5 pIC50 = 8.5 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 368 8 0 5 3.5 COc1cccc(C(=O)CCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm981041x
10688859 17910 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 344 4 0 2 4.4 Fc1ccc([C@H]2C[C@@H]2CN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1021/jm990562x
CHEMBL1202222 17910 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 344 4 0 2 4.4 Fc1ccc([C@H]2C[C@@H]2CN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1021/jm990562x
CHEMBL126792 17910 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 344 4 0 2 4.4 Fc1ccc([C@H]2C[C@@H]2CN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1021/jm990562x
44363676 39796 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 423 7 1 5 2.9 COc1ccc2c(c1)CC(NC(=O)CCN1CCN(c3ccccc3OC)CC1)CC2 10.1021/jm981041x
CHEMBL147897 39796 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 423 7 1 5 2.9 COc1ccc2c(c1)CC(NC(=O)CCN1CCN(c3ccccc3OC)CC1)CC2 10.1021/jm981041x
CHEMBL2373210 39796 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 423 7 1 5 2.9 COc1ccc2c(c1)CC(NC(=O)CCN1CCN(c3ccccc3OC)CC1)CC2 10.1021/jm981041x
10572037 120509 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 383 8 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(Cc3ccccc3OC)CC2)c1 10.1021/jm981041x
CHEMBL2373204 120509 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 383 8 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(Cc3ccccc3OC)CC2)c1 10.1021/jm981041x
CHEMBL356581 120509 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 383 8 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(Cc3ccccc3OC)CC2)c1 10.1021/jm981041x
135612922 143169 2 None - 0 Human 4.5 pIC50 = 4.5 Binding
Receptor Binding Assay: Determination of binding to D4.4 receptor was performed using [3H]-YM-09151-2 (70-87 Ci/mmol, 0.3 nM), as a radioligand, in the presence of various concentrations of the tested compound. Reactions were carried out in 50 mM TRIS-HCl (pH 7.4) containing 5 mM MgCl2, 5 mM EDTA, 5 mM KCl and 1.5 mM CaCl2, for 60 minutes at 22° C. The reaction was terminated by rapid vacuum filtration onto glass fiber filters.Receptor Binding Assay: Determination of binding to D4.4 receptor was performed using [3H]-YM-09151-2 (70-87 Ci/mmol, 0.3 nM), as a radioligand, in the presence of various concentrations of the tested compound. Reactions were carried out in 50 mM TRIS-HCl (pH 7.4) containing 5 mM MgCl2, 5 mM EDTA, 5 mM KCl and 1.5 mM CaCl2, for 60 minutes at 22° C. The reaction was terminated by rapid vacuum filtration onto glass fiber filters.
ChEMBL 336 3 2 5 2.0 O=c1[nH]c(CN2CCN(c3ccc(O)cc3)CC2)nc2ccccc12 nan
CHEMBL3900329 143169 2 None - 0 Human 4.5 pIC50 = 4.5 Binding
Receptor Binding Assay: Determination of binding to D4.4 receptor was performed using [3H]-YM-09151-2 (70-87 Ci/mmol, 0.3 nM), as a radioligand, in the presence of various concentrations of the tested compound. Reactions were carried out in 50 mM TRIS-HCl (pH 7.4) containing 5 mM MgCl2, 5 mM EDTA, 5 mM KCl and 1.5 mM CaCl2, for 60 minutes at 22° C. The reaction was terminated by rapid vacuum filtration onto glass fiber filters.Receptor Binding Assay: Determination of binding to D4.4 receptor was performed using [3H]-YM-09151-2 (70-87 Ci/mmol, 0.3 nM), as a radioligand, in the presence of various concentrations of the tested compound. Reactions were carried out in 50 mM TRIS-HCl (pH 7.4) containing 5 mM MgCl2, 5 mM EDTA, 5 mM KCl and 1.5 mM CaCl2, for 60 minutes at 22° C. The reaction was terminated by rapid vacuum filtration onto glass fiber filters.
ChEMBL 336 3 2 5 2.0 O=c1[nH]c(CN2CCN(c3ccc(O)cc3)CC2)nc2ccccc12 nan
19426635 203881 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 280 2 1 3 3.1 CNCC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL81485 203881 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 280 2 1 3 3.1 CNCC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
168271259 189921 0 None 2 2 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 403 5 0 4 4.8 Cc1nc(CN2CCC(OCc3cccc(C(F)(F)F)c3)CC2)c2ccccn12 10.1016/j.bmcl.2022.128615
CHEMBL5179459 189921 0 None 2 2 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 403 5 0 4 4.8 Cc1nc(CN2CCC(OCc3cccc(C(F)(F)F)c3)CC2)c2ccccn12 10.1016/j.bmcl.2022.128615
163322331 191617 3 None 8 2 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 408 6 1 3 4.5 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(F)c(F)c2)CC1 10.1016/j.bmcl.2022.128615
CHEMBL5204764 191617 3 None 8 2 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 408 6 1 3 4.5 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(F)c(F)c2)CC1 10.1016/j.bmcl.2022.128615
10688561 116367 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 340 4 0 2 4.6 Cc1cc(Cl)ccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL1202210 116367 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 340 4 0 2 4.6 Cc1cc(Cl)ccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL338183 116367 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 340 4 0 2 4.6 Cc1cc(Cl)ccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
4797946 169856 8 None 165 3 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 310 4 1 4 2.2 Cc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4448320 169856 8 None 165 3 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 310 4 1 4 2.2 Cc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
3117 206106 100 None -2 16 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
CHEMBL964 206106 100 None -2 16 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
168268918 189414 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 369 5 1 3 4.7 Cc1cccc(CO[C@H]2CCCN(Cc3cc4ccc(Cl)cc4[nH]3)C2)n1 10.1016/j.bmcl.2022.128615
CHEMBL5171398 189414 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 369 5 1 3 4.7 Cc1cccc(CO[C@H]2CCCN(Cc3cc4ccc(Cl)cc4[nH]3)C2)n1 10.1016/j.bmcl.2022.128615
135398737 944 89 None -13 91 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2013.03.016
38 944 89 None -13 91 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2013.03.016
722 944 89 None -13 91 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2013.03.016
CHEMBL42 944 89 None -13 91 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2013.03.016
DB00363 944 89 None -13 91 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2013.03.016
127053222 138839 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 369 5 0 3 4.1 Fc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1C(F)(F)F 10.1016/j.bmcl.2016.03.102
CHEMBL3793072 138839 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 369 5 0 3 4.1 Fc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1C(F)(F)F 10.1016/j.bmcl.2016.03.102
168270455 189440 0 None 1 2 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 406 5 1 2 5.8 Fc1cc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
CHEMBL5171772 189440 0 None 1 2 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 406 5 1 2 5.8 Fc1cc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
135 2496 38 None - 57 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
1796 2496 38 None - 57 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
4184 2496 38 None - 57 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
CHEMBL6437 2496 38 None - 57 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
DB06148 2496 38 None - 57 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
11071079 110104 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 496 9 0 3 6.0 O=C(OCCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
CHEMBL325516 110104 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 496 9 0 3 6.0 O=C(OCCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
168294968 191821 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3cn4ccccc4n3)CC2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5208124 191821 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3cn4ccccc4n3)CC2)cc1F 10.1016/j.bmcl.2022.128615
127028505 138803 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 333 5 0 3 4.3 Clc1ccc(CN2CCO[C@H](CSc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792731 138803 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 333 5 0 3 4.3 Clc1ccc(CN2CCO[C@H](CSc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
4223 3929 88 None - 3 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat dopamine D4 receptorInhibition of rat dopamine D4 receptor
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/jm040793q
6918314 3929 88 None - 3 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat dopamine D4 receptorInhibition of rat dopamine D4 receptor
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/jm040793q
7427 3929 88 None - 3 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat dopamine D4 receptorInhibition of rat dopamine D4 receptor
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/jm040793q
CHEMBL439849 3929 88 None - 3 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat dopamine D4 receptorInhibition of rat dopamine D4 receptor
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/jm040793q
DB06684 3929 88 None - 3 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat dopamine D4 receptorInhibition of rat dopamine D4 receptor
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/jm040793q
168291477 191284 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccccc3C)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5199649 191284 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccccc3C)C2)cc1F 10.1016/j.bmcl.2022.128615
19964406 114017 3 None 75 2 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 321 5 1 3 3.4 c1ccc(CCC2CN(Cc3nc4ccccc4[nH]3)CCO2)cc1 10.1021/ml500267c
CHEMBL3335535 114017 3 None 75 2 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 321 5 1 3 3.4 c1ccc(CCC2CN(Cc3nc4ccccc4[nH]3)CCO2)cc1 10.1021/ml500267c
53320009 56369 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in cellsDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in cells
ChEMBL 435 3 0 5 3.4 CN1CCN(c2ccc3c(c2)N(S(=O)(=O)c2ccc4ccccc4c2)CCC3=O)CC1 10.1016/j.bmcl.2010.12.007
CHEMBL1642116 56369 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in cellsDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in cells
ChEMBL 435 3 0 5 3.4 CN1CCN(c2ccc3c(c2)N(S(=O)(=O)c2ccc4ccccc4c2)CCC3=O)CC1 10.1016/j.bmcl.2010.12.007
72737772 114023 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 295 5 0 2 3.8 Cc1ccccc1CN1CCOC(CCc2ccccc2)C1 10.1021/ml500267c
CHEMBL3335541 114023 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 295 5 0 2 3.8 Cc1ccccc1CN1CCOC(CCc2ccccc2)C1 10.1021/ml500267c
10782111 17705 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 322 5 0 3 3.6 COc1cccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c1 10.1021/jm990562x
CHEMBL1202217 17705 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 322 5 0 3 3.6 COc1cccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c1 10.1021/jm990562x
CHEMBL125910 17705 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 322 5 0 3 3.6 COc1cccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c1 10.1021/jm990562x
127029388 138809 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 365 6 0 4 3.8 COc1cc(CN2CCO[C@H](COc3cccc(F)c3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3792803 138809 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 365 6 0 4 3.8 COc1cc(CN2CCO[C@H](COc3cccc(F)c3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
45361874 169454 2 None 48 3 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 324 5 1 4 2.4 CCc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4442548 169454 2 None 48 3 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 324 5 1 4 2.4 CCc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
168277394 189807 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5177641 189807 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)cc1F 10.1016/j.bmcl.2022.128615
127031516 138779 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3792438 138779 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
92988697 138937 1 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 335 5 0 3 3.8 Fc1ccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3794199 138937 1 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 335 5 0 3 3.8 Fc1ccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
92984956 138950 1 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 343 7 0 5 3.0 COc1ccc(CN2CCO[C@H](COc3ccc(OC)cc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3794363 138950 1 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 343 7 0 5 3.0 COc1ccc(CN2CCO[C@H](COc3ccc(OC)cc3)C2)cc1 10.1016/j.bmcl.2016.03.102
46885213 8375 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of dopamine D4 (receptor)Inhibition of dopamine D4 (receptor)
ChEMBL 549 8 2 5 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1093802 8375 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of dopamine D4 (receptor)Inhibition of dopamine D4 (receptor)
ChEMBL 549 8 2 5 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
155530763 171003 0 None 9 3 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 323 5 1 3 3.6 Cc1cccc(NC(=O)CCN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4464861 171003 0 None 9 3 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 323 5 1 3 3.6 Cc1cccc(NC(=O)CCN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
127031833 138865 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 340 5 1 3 3.6 Fc1cccc2[nH]cc(CN3CCO[C@H](COc4ccccc4)C3)c12 10.1016/j.bmcl.2016.03.102
CHEMBL3793347 138865 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 340 5 1 3 3.6 Fc1cccc2[nH]cc(CN3CCO[C@H](COc4ccccc4)C3)c12 10.1016/j.bmcl.2016.03.102
54477 84230 34 None -14 22 Human 5.4 pIC50 = 5.4 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC 10.1021/jm990562x
CHEMBL22242 84230 34 None -14 22 Human 5.4 pIC50 = 5.4 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC 10.1021/jm990562x
72737725 114027 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 317 5 0 2 3.8 Fc1cccc(F)c1CN1CCOC(CCc2ccccc2)C1 10.1021/ml500267c
CHEMBL3335545 114027 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 317 5 0 2 3.8 Fc1cccc(F)c1CN1CCOC(CCc2ccccc2)C1 10.1021/ml500267c
127029387 138877 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 365 6 0 4 3.8 COc1ccc(CN2CCO[C@H](COc3cccc(F)c3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3793612 138877 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 365 6 0 4 3.8 COc1ccc(CN2CCO[C@H](COc3cccc(F)c3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
72737734 114024 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 365 6 0 3 4.4 FC(F)(F)Oc1cccc(CN2CCOC(CCc3ccccc3)C2)c1 10.1021/ml500267c
CHEMBL3335542 114024 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 365 6 0 3 4.4 FC(F)(F)Oc1cccc(CN2CCOC(CCc3ccccc3)C2)c1 10.1021/ml500267c
10034684 69064 63 None 18 2 Human 4.4 pIC50 = 4.4 Binding
Inhibitory concentration against binding of [3H]spiperone to human D4 dopaminergic receptorInhibitory concentration against binding of [3H]spiperone to human D4 dopaminergic receptor
ChEMBL 135 0 2 2 1.4 Oc1ccc2c(c1)CCN2 10.1016/S0960-894X(97)00194-7
CHEMBL19331 69064 63 None 18 2 Human 4.4 pIC50 = 4.4 Binding
Inhibitory concentration against binding of [3H]spiperone to human D4 dopaminergic receptorInhibitory concentration against binding of [3H]spiperone to human D4 dopaminergic receptor
ChEMBL 135 0 2 2 1.4 Oc1ccc2c(c1)CCN2 10.1016/S0960-894X(97)00194-7
155562395 175375 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 323 4 1 3 3.5 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)nc1 10.1021/acs.jmedchem.9b00231
CHEMBL4587925 175375 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 323 4 1 3 3.5 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)nc1 10.1021/acs.jmedchem.9b00231
54577891 66242 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
inhibition of dopamine D4 receptor by competition binding assayinhibition of dopamine D4 receptor by competition binding assay
ChEMBL 471 6 1 5 4.3 Cc1nc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)c(C)n1-c1ccccc1 10.1021/jm200682b
CHEMBL1852516 66242 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
inhibition of dopamine D4 receptor by competition binding assayinhibition of dopamine D4 receptor by competition binding assay
ChEMBL 471 6 1 5 4.3 Cc1nc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)c(C)n1-c1ccccc1 10.1021/jm200682b
CHEMBL3216758 66242 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
inhibition of dopamine D4 receptor by competition binding assayinhibition of dopamine D4 receptor by competition binding assay
ChEMBL 471 6 1 5 4.3 Cc1nc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)c(C)n1-c1ccccc1 10.1021/jm200682b
17888044 201234 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 348 4 0 4 3.6 Fc1cccc(-c2cccc(CN3CCN(c4ncccn4)CC3)c2)c1 10.1016/s0960-894x(98)00361-8
CHEMBL62829 201234 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 348 4 0 4 3.6 Fc1cccc(-c2cccc(CN3CCN(c4ncccn4)CC3)c2)c1 10.1016/s0960-894x(98)00361-8
10832895 120481 8 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 369 7 1 5 2.3 COc1ccccc1C(=O)NCCN1CCN(c2ccccc2OC)CC1 10.1021/jm981041x
CHEMBL356358 120481 8 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 369 7 1 5 2.3 COc1ccccc1C(=O)NCCN1CCN(c2ccccc2OC)CC1 10.1021/jm981041x
135398737 944 89 None -13 91 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.01.044
38 944 89 None -13 91 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.01.044
722 944 89 None -13 91 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.01.044
CHEMBL42 944 89 None -13 91 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.01.044
DB00363 944 89 None -13 91 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.01.044
135398737 944 89 None -13 91 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]methylspiperone from human recombinant Dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human recombinant Dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2016.03.006
38 944 89 None -13 91 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]methylspiperone from human recombinant Dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human recombinant Dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2016.03.006
722 944 89 None -13 91 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]methylspiperone from human recombinant Dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human recombinant Dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2016.03.006
CHEMBL42 944 89 None -13 91 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]methylspiperone from human recombinant Dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human recombinant Dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2016.03.006
DB00363 944 89 None -13 91 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]methylspiperone from human recombinant Dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human recombinant Dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2016.03.006
127031518 138869 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3793389 138869 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
127029995 138967 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1F 10.1016/j.bmcl.2016.03.102
CHEMBL3794529 138967 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1F 10.1016/j.bmcl.2016.03.102
3303 2213 41 None 1 15 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.8b00265
5311200 2213 41 None 1 15 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.8b00265
CHEMBL267014 2213 41 None 1 15 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.8b00265
155511803 169038 0 None 229 2 Human 4.4 pIC50 = 4.4 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 342 4 1 2 4.5 Cc1cccc(NC(=O)CN2CCC(c3ccc(Cl)cc3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4436479 169038 0 None 229 2 Human 4.4 pIC50 = 4.4 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 342 4 1 2 4.5 Cc1cccc(NC(=O)CN2CCC(c3ccc(Cl)cc3)CC2)c1 10.1021/acs.jmedchem.9b00231
155536720 171621 0 None 77 3 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 359 4 1 3 3.9 Cc1cccc(NC(=O)CN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4473652 171621 0 None 77 3 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 359 4 1 3 3.9 Cc1cccc(NC(=O)CN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/acs.jmedchem.9b00231
168270563 189357 0 None -1 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5170381 189357 0 None -1 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)cc1F 10.1016/j.bmcl.2022.128615
11035765 9795 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 359 6 2 6 3.3 Oc1nc2ccccc2n1CCCNCc1cc2c(cc1Cl)OCO2 10.1021/jm010878g
CHEMBL114280 9795 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 359 6 2 6 3.3 Oc1nc2ccccc2n1CCCNCc1cc2c(cc1Cl)OCO2 10.1021/jm010878g
11793971 17783 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 376 4 1 3 4.6 Oc1ccc([C@H]2C[C@@H]2CN2CCN(c3ccc(Cl)cc3Cl)CC2)cc1 10.1021/jm990562x
CHEMBL1202202 17783 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 376 4 1 3 4.6 Oc1ccc([C@H]2C[C@@H]2CN2CCN(c3ccc(Cl)cc3Cl)CC2)cc1 10.1021/jm990562x
CHEMBL126126 17783 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 376 4 1 3 4.6 Oc1ccc([C@H]2C[C@@H]2CN2CCN(c3ccc(Cl)cc3Cl)CC2)cc1 10.1021/jm990562x
109030515 175412 1 None 12 3 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 325 5 1 5 1.9 Cc1cccc(NC(=O)CCN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4588808 175412 1 None 12 3 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 325 5 1 5 1.9 Cc1cccc(NC(=O)CCN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
168292271 191292 0 None 5 2 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 424 6 1 3 5.1 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(Cl)c(F)c2)CC1 10.1016/j.bmcl.2022.128615
CHEMBL5199815 191292 0 None 5 2 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 424 6 1 3 5.1 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(Cl)c(F)c2)CC1 10.1016/j.bmcl.2022.128615
168295019 191901 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(CO[C@H]2CCCN(Cc3ncn4ccccc34)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5209079 191901 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(CO[C@H]2CCCN(Cc3ncn4ccccc34)C2)cc1F 10.1016/j.bmcl.2022.128615
10668173 19243 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 390 5 0 3 4.9 COc1ccc([C@H]2C[C@@H]2CN2CCN(c3ccc(Cl)cc3Cl)CC2)cc1 10.1021/jm990562x
CHEMBL1202206 19243 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 390 5 0 3 4.9 COc1ccc([C@H]2C[C@@H]2CN2CCN(c3ccc(Cl)cc3Cl)CC2)cc1 10.1021/jm990562x
CHEMBL129556 19243 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 390 5 0 3 4.9 COc1ccc([C@H]2C[C@@H]2CN2CCN(c3ccc(Cl)cc3Cl)CC2)cc1 10.1021/jm990562x
127053214 138819 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 311 5 0 3 3.6 Cc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1C 10.1016/j.bmcl.2016.03.102
CHEMBL3792923 138819 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 311 5 0 3 3.6 Cc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1C 10.1016/j.bmcl.2016.03.102
155515982 169443 0 None 6 17 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as inhibition of quinpirole-induced beta-arrestin2 recruitment preincubated for 30 mins followed by quinpirole addition and further incubated for 6 hrs by Path-Hunter assayAntagonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as inhibition of quinpirole-induced beta-arrestin2 recruitment preincubated for 30 mins followed by quinpirole addition and further incubated for 6 hrs by Path-Hunter assay
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4442460 169443 0 None 6 17 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as inhibition of quinpirole-induced beta-arrestin2 recruitment preincubated for 30 mins followed by quinpirole addition and further incubated for 6 hrs by Path-Hunter assayAntagonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as inhibition of quinpirole-induced beta-arrestin2 recruitment preincubated for 30 mins followed by quinpirole addition and further incubated for 6 hrs by Path-Hunter assay
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
127031829 138898 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 352 6 1 4 3.5 COc1ccc2[nH]cc(CN3CCO[C@H](COc4ccccc4)C3)c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3793890 138898 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 352 6 1 4 3.5 COc1ccc2[nH]cc(CN3CCO[C@H](COc4ccccc4)C3)c2c1 10.1016/j.bmcl.2016.03.102
127028182 138932 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 336 5 0 4 3.2 Fc1cccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)n1 10.1016/j.bmcl.2016.03.102
CHEMBL3794158 138932 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 336 5 0 4 3.2 Fc1cccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)n1 10.1016/j.bmcl.2016.03.102
127029386 138867 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccc(F)cc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793375 138867 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccc(F)cc3)C2)cc1 10.1016/j.bmcl.2016.03.102
44363656 35247 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 409 6 1 5 2.5 COc1ccc2c(c1)CC(NC(=O)CN1CCN(c3ccccc3OC)CC1)CC2 10.1021/jm981041x
CHEMBL143835 35247 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 409 6 1 5 2.5 COc1ccc2c(c1)CC(NC(=O)CN1CCN(c3ccccc3OC)CC1)CC2 10.1021/jm981041x
CHEMBL2373208 35247 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 409 6 1 5 2.5 COc1ccc2c(c1)CC(NC(=O)CN1CCN(c3ccccc3OC)CC1)CC2 10.1021/jm981041x
71717830 85556 0 None 9 2 Human 4.3 pIC50 = 4.3 Binding
Inhibitory concentration against binding of [3H]spiperone to human D4 dopaminergic receptorInhibitory concentration against binding of [3H]spiperone to human D4 dopaminergic receptor
ChEMBL 433 5 7 9 -0.3 OC[C@H]1O[C@H](Oc2ccc(CC3NCCc4cc(O)c(O)cc43)cc2)[C@H](O)[C@H](O)[C@H]1O 10.1016/S0960-894X(97)00194-7
CHEMBL2303762 85556 0 None 9 2 Human 4.3 pIC50 = 4.3 Binding
Inhibitory concentration against binding of [3H]spiperone to human D4 dopaminergic receptorInhibitory concentration against binding of [3H]spiperone to human D4 dopaminergic receptor
ChEMBL 433 5 7 9 -0.3 OC[C@H]1O[C@H](Oc2ccc(CC3NCCc4cc(O)c(O)cc43)cc2)[C@H](O)[C@H](O)[C@H]1O 10.1016/S0960-894X(97)00194-7
168275515 189911 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 371 5 0 4 4.1 Cc1nc(CN2CCC(OCc3ccc(F)c(F)c3)CC2)c2ccccn12 10.1016/j.bmcl.2022.128615
CHEMBL5179340 189911 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 371 5 0 4 4.1 Cc1nc(CN2CCC(OCc3ccc(F)c(F)c3)CC2)c2ccccn12 10.1016/j.bmcl.2022.128615
10851217 118020 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 292 4 0 2 3.6 c1ccc([C@H]2C[C@@H]2CN2CCN(c3ccccc3)CC2)cc1 10.1021/jm990562x
CHEMBL341497 118020 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 292 4 0 2 3.6 c1ccc([C@H]2C[C@@H]2CN2CCN(c3ccccc3)CC2)cc1 10.1021/jm990562x
44304314 102219 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 342 3 0 4 3.4 c1cnc(N2CCN(Cc3cccc4c3-c3ccccc3C4)CC2)nc1 10.1016/s0960-894x(98)00361-8
CHEMBL304692 102219 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 342 3 0 4 3.4 c1cnc(N2CCN(Cc3cccc4c3-c3ccccc3C4)CC2)nc1 10.1016/s0960-894x(98)00361-8
155559617 174312 0 None 9 3 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as inhibition of quinpirole-induced beta-arrestin2 recruitment preincubated for 30 mins followed by quinpirole addition and further incubated for 6 hrs by Path-Hunter assayAntagonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as inhibition of quinpirole-induced beta-arrestin2 recruitment preincubated for 30 mins followed by quinpirole addition and further incubated for 6 hrs by Path-Hunter assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4563944 174312 0 None 9 3 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as inhibition of quinpirole-induced beta-arrestin2 recruitment preincubated for 30 mins followed by quinpirole addition and further incubated for 6 hrs by Path-Hunter assayAntagonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as inhibition of quinpirole-induced beta-arrestin2 recruitment preincubated for 30 mins followed by quinpirole addition and further incubated for 6 hrs by Path-Hunter assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
135514603 202414 13 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 474 2 1 7 4.0 CN1CCN(C2=Nc3cc(Cl)ccc3Nc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
CHEMBL70319 202414 13 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 474 2 1 7 4.0 CN1CCN(C2=Nc3cc(Cl)ccc3Nc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
3303 2213 41 None 1 15 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00361-8
5311200 2213 41 None 1 15 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00361-8
CHEMBL267014 2213 41 None 1 15 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00361-8
5615 3836 4 None - 1 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 339 6 0 4 4.0 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccccc1)C)C 10.1016/s0960-894x(98)00361-8
5781 3836 4 None - 1 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 339 6 0 4 4.0 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccccc1)C)C 10.1016/s0960-894x(98)00361-8
CHEMBL1179189 3836 4 None - 1 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 339 6 0 4 4.0 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccccc1)C)C 10.1016/s0960-894x(98)00361-8
1353 1880 85 None -3 85 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm990562x
3559 1880 85 None -3 85 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm990562x
86 1880 85 None -3 85 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm990562x
CHEMBL54 1880 85 None -3 85 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm990562x
DB00502 1880 85 None -3 85 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm990562x
9901894 162864 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 4 0 2 4.3 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1 10.1021/jm990562x
CHEMBL1202220 162864 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 4 0 2 4.3 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1 10.1021/jm990562x
CHEMBL419610 162864 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 4 0 2 4.3 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1 10.1021/jm990562x
11301655 198 31 None 245 4 Human 8.3 pIC50 = 8.3 Binding
In vitro inhibitory concentration tested on human D4.4 receptor in HEK293 cells using FLIPR assayIn vitro inhibitory concentration tested on human D4.4 receptor in HEK293 cells using FLIPR assay
ChEMBL 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 10.1021/jm030505a
8441 198 31 None 245 4 Human 8.3 pIC50 = 8.3 Binding
In vitro inhibitory concentration tested on human D4.4 receptor in HEK293 cells using FLIPR assayIn vitro inhibitory concentration tested on human D4.4 receptor in HEK293 cells using FLIPR assay
ChEMBL 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 10.1021/jm030505a
CHEMBL127257 198 31 None 245 4 Human 8.3 pIC50 = 8.3 Binding
In vitro inhibitory concentration tested on human D4.4 receptor in HEK293 cells using FLIPR assayIn vitro inhibitory concentration tested on human D4.4 receptor in HEK293 cells using FLIPR assay
ChEMBL 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 10.1021/jm030505a
127031515 138904 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL3793910 138904 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.bmcl.2022.128615
135620651 143975 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Receptor Binding Assay: Determination of binding to D4.4 receptor was performed using [3H]-YM-09151-2 (70-87 Ci/mmol, 0.3 nM), as a radioligand, in the presence of various concentrations of the tested compound. Reactions were carried out in 50 mM TRIS-HCl (pH 7.4) containing 5 mM MgCl2, 5 mM EDTA, 5 mM KCl and 1.5 mM CaCl2, for 60 minutes at 22° C. The reaction was terminated by rapid vacuum filtration onto glass fiber filters.Receptor Binding Assay: Determination of binding to D4.4 receptor was performed using [3H]-YM-09151-2 (70-87 Ci/mmol, 0.3 nM), as a radioligand, in the presence of various concentrations of the tested compound. Reactions were carried out in 50 mM TRIS-HCl (pH 7.4) containing 5 mM MgCl2, 5 mM EDTA, 5 mM KCl and 1.5 mM CaCl2, for 60 minutes at 22° C. The reaction was terminated by rapid vacuum filtration onto glass fiber filters.
ChEMBL 336 3 2 5 2.0 O=c1[nH]c(CN2CCN(c3cccc(O)c3)CC2)nc2ccccc12 nan
CHEMBL3906995 143975 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Receptor Binding Assay: Determination of binding to D4.4 receptor was performed using [3H]-YM-09151-2 (70-87 Ci/mmol, 0.3 nM), as a radioligand, in the presence of various concentrations of the tested compound. Reactions were carried out in 50 mM TRIS-HCl (pH 7.4) containing 5 mM MgCl2, 5 mM EDTA, 5 mM KCl and 1.5 mM CaCl2, for 60 minutes at 22° C. The reaction was terminated by rapid vacuum filtration onto glass fiber filters.Receptor Binding Assay: Determination of binding to D4.4 receptor was performed using [3H]-YM-09151-2 (70-87 Ci/mmol, 0.3 nM), as a radioligand, in the presence of various concentrations of the tested compound. Reactions were carried out in 50 mM TRIS-HCl (pH 7.4) containing 5 mM MgCl2, 5 mM EDTA, 5 mM KCl and 1.5 mM CaCl2, for 60 minutes at 22° C. The reaction was terminated by rapid vacuum filtration onto glass fiber filters.
ChEMBL 336 3 2 5 2.0 O=c1[nH]c(CN2CCN(c3cccc(O)c3)CC2)nc2ccccc12 nan
135398737 944 89 None -13 91 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991005d
38 944 89 None -13 91 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991005d
722 944 89 None -13 91 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991005d
CHEMBL42 944 89 None -13 91 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991005d
DB00363 944 89 None -13 91 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991005d
127053220 138837 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 319 5 0 3 3.2 Fc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.bmcl.2016.03.102
CHEMBL3793062 138837 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 319 5 0 3 3.2 Fc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.bmcl.2016.03.102
11005810 10367 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 517 10 1 4 6.2 N#Cc1ccc(CCOC(=O)NC2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
CHEMBL116463 10367 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 517 10 1 4 6.2 N#Cc1ccc(CCOC(=O)NC2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
51003551 56376 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in cellsDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in cells
ChEMBL 449 3 0 5 3.8 CC1CC(=O)c2c(N3CCN(C)CC3)cccc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
CHEMBL1642123 56376 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in cellsDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in cells
ChEMBL 449 3 0 5 3.8 CC1CC(=O)c2c(N3CCN(C)CC3)cccc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
127031515 138904 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.bmcl.2016.03.102
CHEMBL3793910 138904 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.bmcl.2016.03.102
1353 1880 85 None -3 85 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
3559 1880 85 None -3 85 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
86 1880 85 None -3 85 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
CHEMBL54 1880 85 None -3 85 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
DB00502 1880 85 None -3 85 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
10803754 17923 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 294 4 0 4 2.4 c1ccc([C@H]2C[C@@H]2CN2CCN(c3ncccn3)CC2)cc1 10.1021/jm990562x
CHEMBL1203257 17923 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 294 4 0 4 2.4 c1ccc([C@H]2C[C@@H]2CN2CCN(c3ncccn3)CC2)cc1 10.1021/jm990562x
CHEMBL126847 17923 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 294 4 0 4 2.4 c1ccc([C@H]2C[C@@H]2CN2CCN(c3ncccn3)CC2)cc1 10.1021/jm990562x
21186102 100310 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 360 5 0 5 3.5 COc1ccc(-c2cccc(CN3CCN(c4ncccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
CHEMBL292943 100310 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 360 5 0 5 3.5 COc1ccc(-c2cccc(CN3CCN(c4ncccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
10049758 202939 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 457 2 0 7 3.7 CN1CCN(C2=Nc3ccccc3Sc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
CHEMBL73589 202939 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 457 2 0 7 3.7 CN1CCN(C2=Nc3ccccc3Sc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
137640201 156419 2 None 177 13 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4072818 156419 2 None 177 13 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
168287735 191208 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
CHEMBL5198353 191208 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
127031519 138793 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 329 6 0 4 3.7 CSc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792638 138793 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 329 6 0 4 3.7 CSc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
127053221 138801 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 369 5 0 3 4.1 Fc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1C(F)(F)F 10.1016/j.bmcl.2016.03.102
CHEMBL3792728 138801 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 369 5 0 3 4.1 Fc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1C(F)(F)F 10.1016/j.bmcl.2016.03.102
127032383 138873 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 322 5 1 3 3.4 c1ccc(OC[C@@H]2CN(Cc3ccc4[nH]ccc4c3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793438 138873 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 322 5 1 3 3.4 c1ccc(OC[C@@H]2CN(Cc3ccc4[nH]ccc4c3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
135398737 944 89 None -13 91 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960268u
38 944 89 None -13 91 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960268u
722 944 89 None -13 91 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960268u
CHEMBL42 944 89 None -13 91 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960268u
DB00363 944 89 None -13 91 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960268u
1212 1632 45 None -77 65 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 1632 45 None -77 65 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 1632 45 None -77 65 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 1632 45 None -77 65 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 1632 45 None -77 65 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
127032082 138787 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 323 5 0 5 2.6 c1ccc(OC[C@@H]2CN(Cc3cn4ccccc4n3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792541 138787 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 323 5 0 5 2.6 c1ccc(OC[C@@H]2CN(Cc3cn4ccccc4n3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
21186124 101742 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 347 4 0 3 4.2 Fc1ccc(-c2cncc(CN3CCN(c4ccccc4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
CHEMBL302904 101742 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 347 4 0 3 4.2 Fc1ccc(-c2cncc(CN3CCN(c4ccccc4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
9949655 201567 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 336 4 0 5 3.5 c1cnc(N2CCN(Cc3cccc(-c4ccsc4)c3)CC2)nc1 10.1016/s0960-894x(98)00361-8
CHEMBL64597 201567 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 336 4 0 5 3.5 c1cnc(N2CCN(Cc3cccc(-c4ccsc4)c3)CC2)nc1 10.1016/s0960-894x(98)00361-8
10617133 17815 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 340 5 0 3 3.8 COc1cc(F)ccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL1202214 17815 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 340 5 0 3 3.8 COc1cc(F)ccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL126269 17815 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 340 5 0 3 3.8 COc1cc(F)ccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
9820304 101599 0 None 12 2 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(Cl)c1 10.1021/jm990562x
CHEMBL1204116 101599 0 None 12 2 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(Cl)c1 10.1021/jm990562x
CHEMBL302075 101599 0 None 12 2 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(Cl)c1 10.1021/jm990562x
1353 1880 85 None -3 85 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960268u
3559 1880 85 None -3 85 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960268u
86 1880 85 None -3 85 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960268u
CHEMBL54 1880 85 None -3 85 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960268u
DB00502 1880 85 None -3 85 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960268u
10236758 115272 3 None 208 13 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL3354065 115272 3 None 208 13 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
1353 1880 85 None -3 85 Human 8.2 pIC50 = 8.2 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991005d
3559 1880 85 None -3 85 Human 8.2 pIC50 = 8.2 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991005d
86 1880 85 None -3 85 Human 8.2 pIC50 = 8.2 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991005d
CHEMBL54 1880 85 None -3 85 Human 8.2 pIC50 = 8.2 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991005d
DB00502 1880 85 None -3 85 Human 8.2 pIC50 = 8.2 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991005d
10385977 96882 0 None -5 2 Human 7.2 pIC50 = 7.2 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 394 7 0 4 4.7 COc1ccccc1N1CCN(CCCC2CCCc3c(OC)cccc32)CC1 10.1021/jm981041x
CHEMBL26929 96882 0 None -5 2 Human 7.2 pIC50 = 7.2 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 394 7 0 4 4.7 COc1ccccc1N1CCN(CCCC2CCCc3c(OC)cccc32)CC1 10.1021/jm981041x
2247 502 77 None -63 41 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 502 77 None -63 41 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 502 77 None -63 41 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 502 77 None -63 41 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 502 77 None -63 41 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
127031508 138851 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 335 5 0 3 3.8 Fc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3793169 138851 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 335 5 0 3 3.8 Fc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
155552185 173489 0 None 2 16 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as inhibition of quinpirole-induced beta-arrestin2 recruitment preincubated for 30 mins followed by quinpirole addition and further incubated for 6 hrs by Path-Hunter assayAntagonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as inhibition of quinpirole-induced beta-arrestin2 recruitment preincubated for 30 mins followed by quinpirole addition and further incubated for 6 hrs by Path-Hunter assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4544086 173489 0 None 2 16 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as inhibition of quinpirole-induced beta-arrestin2 recruitment preincubated for 30 mins followed by quinpirole addition and further incubated for 6 hrs by Path-Hunter assayAntagonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as inhibition of quinpirole-induced beta-arrestin2 recruitment preincubated for 30 mins followed by quinpirole addition and further incubated for 6 hrs by Path-Hunter assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
127053217 138788 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 333 5 0 3 4.1 c1ccc(OC[C@@H]2CN(Cc3ccc4ccccc4c3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792556 138788 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 333 5 0 3 4.1 c1ccc(OC[C@@H]2CN(Cc3ccc4ccccc4c3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
45278882 7371 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 512 9 1 4 6.1 CCCn1c(-c2ccccc2)cc(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1C 10.1016/j.bmcl.2010.01.093
CHEMBL1086756 7371 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 512 9 1 4 6.1 CCCn1c(-c2ccccc2)cc(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1C 10.1016/j.bmcl.2010.01.093
168274850 189562 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 405 6 0 5 4.4 FC(F)(F)Oc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5173767 189562 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 405 6 0 5 4.4 FC(F)(F)Oc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.bmcl.2022.128615
168274755 190048 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 403 5 0 4 4.8 Cn1cnc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
CHEMBL5181334 190048 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 403 5 0 4 4.8 Cn1cnc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
127032083 138917 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 323 5 1 4 2.8 c1ccc(OC[C@@H]2CN(Cc3n[nH]c4ccccc34)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793996 138917 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 323 5 1 4 2.8 c1ccc(OC[C@@H]2CN(Cc3n[nH]c4ccccc34)CCO2)cc1 10.1016/j.bmcl.2016.03.102
72198754 90449 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Inhibition of dopamine D4 receptor (unknown origin)Inhibition of dopamine D4 receptor (unknown origin)
ChEMBL 443 8 0 4 4.8 COc1ccccc1N1CCN(CCCCCN2Cc3ccc4ccccc4c3C2=O)CC1 10.1016/j.ejmech.2013.01.044
CHEMBL2392349 90449 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Inhibition of dopamine D4 receptor (unknown origin)Inhibition of dopamine D4 receptor (unknown origin)
ChEMBL 443 8 0 4 4.8 COc1ccccc1N1CCN(CCCCCN2Cc3ccc4ccccc4c3C2=O)CC1 10.1016/j.ejmech.2013.01.044
10905740 110181 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 413 3 1 6 2.9 O=c1[nH]c2ccccc2n(C2CCN(Cc3cc4c(cc3Cl)OCO4)CC2)c1=O 10.1021/jm010878g
CHEMBL325945 110181 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 413 3 1 6 2.9 O=c1[nH]c2ccccc2n(C2CCN(Cc3cc4c(cc3Cl)OCO4)CC2)c1=O 10.1021/jm010878g
10615990 116802 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 324 4 0 2 4.1 Cc1cc(F)ccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL1202209 116802 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 324 4 0 2 4.1 Cc1cc(F)ccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL339674 116802 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 324 4 0 2 4.1 Cc1cc(F)ccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
127053219 138934 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 335 5 0 3 3.8 Fc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3794174 138934 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 335 5 0 3 3.8 Fc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
15840855 101619 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 349 4 0 5 3.0 Fc1ccc(-c2cncc(CN3CCN(c4ncccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
CHEMBL302183 101619 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 349 4 0 5 3.0 Fc1ccc(-c2cncc(CN3CCN(c4ncccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
21186186 198946 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 348 4 0 4 3.6 Fc1ccc(-c2cccc(CN3CCN(c4ncccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
CHEMBL59942 198946 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 348 4 0 4 3.6 Fc1ccc(-c2cccc(CN3CCN(c4ncccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
21186138 201010 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 348 4 0 4 3.6 Fc1ccc(-c2cncc(CN3CCN(c4ccccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
CHEMBL61657 201010 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 348 4 0 4 3.6 Fc1ccc(-c2cncc(CN3CCN(c4ccccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
21186115 201018 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 365 4 0 3 4.3 Fc1ccc(-c2cncc(CN3CCN(c4ccccc4F)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
CHEMBL61682 201018 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 365 4 0 3 4.3 Fc1ccc(-c2cncc(CN3CCN(c4ccccc4F)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
9797162 77938 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 320 4 0 2 4.2 Cc1ccc(N2CCN(CC3CC3c3ccccc3)CC2)c(C)c1 10.1021/jm990562x
CHEMBL2092961 77938 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 320 4 0 2 4.2 Cc1ccc(N2CCN(CC3CC3c3ccccc3)CC2)c(C)c1 10.1021/jm990562x
CHEMBL2109988 77938 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 320 4 0 2 4.2 Cc1ccc(N2CCN(CC3CC3c3ccccc3)CC2)c(C)c1 10.1021/jm990562x
10501113 36317 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 399 8 1 6 2.3 COc1ccc(OC)c(C(=O)NCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm981041x
CHEMBL144811 36317 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 399 8 1 6 2.3 COc1ccc(OC)c(C(=O)NCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm981041x
10762827 121413 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 387 7 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(Cc3ccc(Cl)cc3)CC2)c1 10.1021/jm981041x
CHEMBL2373207 121413 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 387 7 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(Cc3ccc(Cl)cc3)CC2)c1 10.1021/jm981041x
CHEMBL359051 121413 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 387 7 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(Cc3ccc(Cl)cc3)CC2)c1 10.1021/jm981041x
10411988 21210 0 None -29 2 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 461 6 0 5 5.2 CC1SC2(CCCC2)C(=O)N1CCCCN1CCN(c2csc3cc(F)ccc23)CC1 10.1021/jm960268u
CHEMBL131482 21210 0 None -29 2 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 461 6 0 5 5.2 CC1SC2(CCCC2)C(=O)N1CCCCN1CCN(c2csc3cc(F)ccc23)CC1 10.1021/jm960268u
11113605 10407 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 480 9 0 2 5.8 O=C(CCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
CHEMBL116735 10407 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 480 9 0 2 5.8 O=C(CCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
10496095 116330 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 322 5 0 3 3.6 COc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1 10.1021/jm990562x
CHEMBL1202224 116330 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 322 5 0 3 3.6 COc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1 10.1021/jm990562x
CHEMBL337983 116330 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 322 5 0 3 3.6 COc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1 10.1021/jm990562x
155536815 171641 0 None 33 3 Human 5.1 pIC50 = 5.1 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 322 4 1 2 4.1 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)cc1 10.1021/acs.jmedchem.9b00231
CHEMBL4473792 171641 0 None 33 3 Human 5.1 pIC50 = 5.1 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 322 4 1 2 4.1 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)cc1 10.1021/acs.jmedchem.9b00231
10739483 36391 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 395 6 0 6 4.2 COc1cccc(-c2csc(CN3CCN(c4ccccc4OC)CC3)n2)c1 10.1021/jm981041x
CHEMBL144868 36391 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 395 6 0 6 4.2 COc1cccc(-c2csc(CN3CCN(c4ccccc4OC)CC3)n2)c1 10.1021/jm981041x
CHEMBL2373206 36391 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 395 6 0 6 4.2 COc1cccc(-c2csc(CN3CCN(c4ccccc4OC)CC3)n2)c1 10.1021/jm981041x
127028181 138919 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 359 5 1 4 3.1 Fc1ccc2c(CN3CCO[C@H](COc4cccc(F)n4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3794013 138919 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 359 5 1 4 3.1 Fc1ccc2c(CN3CCO[C@H](COc4cccc(F)n4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
10885636 110527 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 503 9 0 4 5.7 N#Cc1ccc(CCOC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
CHEMBL326263 110527 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 503 9 0 4 5.7 N#Cc1ccc(CCOC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
155563301 174678 0 None - 1 Human 5.1 pIC50 = 5.1 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 344 4 1 4 2.8 Cc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4572245 174678 0 None - 1 Human 5.1 pIC50 = 5.1 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 344 4 1 4 2.8 Cc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
5615 3836 4 None - 1 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 339 6 0 4 4.0 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccccc1)C)C 10.1016/s0960-894x(98)00361-8
5781 3836 4 None - 1 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 339 6 0 4 4.0 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccccc1)C)C 10.1016/s0960-894x(98)00361-8
CHEMBL1179189 3836 4 None - 1 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 339 6 0 4 4.0 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccccc1)C)C 10.1016/s0960-894x(98)00361-8
21186098 100077 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 348 4 0 4 3.6 Fc1ccccc1-c1cccc(CN2CCN(c3ncccn3)CC2)c1 10.1016/s0960-894x(98)00361-8
CHEMBL291380 100077 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 348 4 0 4 3.6 Fc1ccccc1-c1cccc(CN2CCN(c3ncccn3)CC2)c1 10.1016/s0960-894x(98)00361-8
21186192 100137 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 365 4 0 3 4.3 Fc1ccc(-c2cncc(CN3CCN(c4ccc(F)cc4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
CHEMBL291824 100137 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 365 4 0 3 4.3 Fc1ccc(-c2cncc(CN3CCN(c4ccc(F)cc4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
10615684 17857 0 None 4 2 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 320 4 0 2 4.2 Cc1ccc(N2CCN(C[C@@H]3C[C@H]3c3ccccc3)CC2)c(C)c1 10.1021/jm990562x
CHEMBL1202208 17857 0 None 4 2 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 320 4 0 2 4.2 Cc1ccc(N2CCN(C[C@@H]3C[C@H]3c3ccccc3)CC2)c(C)c1 10.1021/jm990562x
CHEMBL126493 17857 0 None 4 2 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 320 4 0 2 4.2 Cc1ccc(N2CCN(C[C@@H]3C[C@H]3c3ccccc3)CC2)c(C)c1 10.1021/jm990562x
9967140 17883 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 4 0 2 4.3 Clc1ccccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL1202215 17883 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 4 0 2 4.3 Clc1ccccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL126633 17883 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 4 0 2 4.3 Clc1ccccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
127032384 138846 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 356 5 1 3 4.1 Clc1ccc2c(CN3CCO[C@H](COc4ccccc4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3793137 138846 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 356 5 1 3 4.1 Clc1ccc2c(CN3CCO[C@H](COc4ccccc4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
10568183 17795 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 4 0 2 4.3 Clc1cccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c1 10.1021/jm990562x
CHEMBL1202221 17795 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 4 0 2 4.3 Clc1cccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c1 10.1021/jm990562x
CHEMBL126182 17795 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 4 0 2 4.3 Clc1cccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c1 10.1021/jm990562x
44363675 118748 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 409 6 1 5 2.5 COc1ccccc1N1CCN(CC(=O)NC2CCc3c(cccc3OC)C2)CC1 10.1021/jm981041x
CHEMBL2373209 118748 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 409 6 1 5 2.5 COc1ccccc1N1CCN(CC(=O)NC2CCc3c(cccc3OC)C2)CC1 10.1021/jm981041x
CHEMBL343620 118748 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 409 6 1 5 2.5 COc1ccccc1N1CCN(CC(=O)NC2CCc3c(cccc3OC)C2)CC1 10.1021/jm981041x
168286314 191063 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5196213 191063 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)c1 10.1016/j.bmcl.2022.128615
15840855 101619 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 349 4 0 5 3.0 Fc1ccc(-c2cncc(CN3CCN(c4ncccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
CHEMBL302183 101619 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 349 4 0 5 3.0 Fc1ccc(-c2cncc(CN3CCN(c4ncccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
17888044 201234 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 348 4 0 4 3.6 Fc1cccc(-c2cccc(CN3CCN(c4ncccn4)CC3)c2)c1 10.1016/s0960-894x(98)00361-8
CHEMBL62829 201234 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 348 4 0 4 3.6 Fc1cccc(-c2cccc(CN3CCN(c4ncccn4)CC3)c2)c1 10.1016/s0960-894x(98)00361-8
10808230 17877 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 356 5 0 3 4.3 COc1ccc(Cl)cc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL1202205 17877 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 356 5 0 3 4.3 COc1ccc(Cl)cc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL126604 17877 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 356 5 0 3 4.3 COc1ccc(Cl)cc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
9820304 101599 0 None 12 2 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(Cl)c1 10.1021/jm990562x
CHEMBL1204116 101599 0 None 12 2 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(Cl)c1 10.1021/jm990562x
CHEMBL302075 101599 0 None 12 2 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(Cl)c1 10.1021/jm990562x
10761040 117966 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1cccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c1Cl 10.1021/jm990562x
CHEMBL1202213 117966 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1cccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c1Cl 10.1021/jm990562x
CHEMBL341310 117966 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1cccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c1Cl 10.1021/jm990562x
14925759 157494 6 None 18 13 Human 8.0 pIC50 = 8.0 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4085780 157494 6 None 18 13 Human 8.0 pIC50 = 8.0 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
127029389 138913 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3cccc(F)c3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793984 138913 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3cccc(F)c3)C2)cc1 10.1016/j.bmcl.2016.03.102
3303 2213 41 None 1 15 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.8b00265
5311200 2213 41 None 1 15 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.8b00265
CHEMBL267014 2213 41 None 1 15 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.8b00265
3198 203802 73 None -26 34 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 203802 73 None -26 34 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 203802 73 None -26 34 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
10948527 110867 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 365 3 1 5 2.3 O=C1NCN(c2ccccc2)C12CCN(Cc1ccc3c(c1)OCO3)CC2 10.1021/jm010878g
CHEMBL326962 110867 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 365 3 1 5 2.3 O=C1NCN(c2ccccc2)C12CCN(Cc1ccc3c(c1)OCO3)CC2 10.1021/jm010878g
135492584 11228 0 None 95 3 Human 7.0 pIC50 = 7.0 Binding
Inhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptorInhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptor
ChEMBL 380 7 1 7 2.5 c1cnc(N2CCN(CCCCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL1179503 11228 0 None 95 3 Human 7.0 pIC50 = 7.0 Binding
Inhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptorInhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptor
ChEMBL 380 7 1 7 2.5 c1cnc(N2CCN(CCCCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL80645 11228 0 None 95 3 Human 7.0 pIC50 = 7.0 Binding
Inhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptorInhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptor
ChEMBL 380 7 1 7 2.5 c1cnc(N2CCN(CCCCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
135481864 12244 0 None 112 3 Human 7.0 pIC50 = 7.0 Binding
Inhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptorInhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptor
ChEMBL 350 5 1 5 2.9 c1ccc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)cc1 10.1016/S0960-894X(97)00442-3
CHEMBL1185415 12244 0 None 112 3 Human 7.0 pIC50 = 7.0 Binding
Inhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptorInhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptor
ChEMBL 350 5 1 5 2.9 c1ccc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)cc1 10.1016/S0960-894X(97)00442-3
CHEMBL412665 12244 0 None 112 3 Human 7.0 pIC50 = 7.0 Binding
Inhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptorInhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptor
ChEMBL 350 5 1 5 2.9 c1ccc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)cc1 10.1016/S0960-894X(97)00442-3
168284020 190659 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 387 5 0 4 4.6 Cc1nc(CN2CCC(OCc3ccc(Cl)c(F)c3)CC2)c2ccccn12 10.1016/j.bmcl.2022.128615
CHEMBL5190239 190659 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 387 5 0 4 4.6 Cc1nc(CN2CCC(OCc3ccc(Cl)c(F)c3)CC2)c2ccccn12 10.1016/j.bmcl.2022.128615
10780076 17821 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 293 4 0 3 3.0 c1ccc([C@H]2C[C@@H]2CN2CCN(c3ccccn3)CC2)cc1 10.1021/jm990562x
CHEMBL1203260 17821 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 293 4 0 3 3.0 c1ccc([C@H]2C[C@@H]2CN2CCN(c3ccccn3)CC2)cc1 10.1021/jm990562x
CHEMBL126318 17821 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 293 4 0 3 3.0 c1ccc([C@H]2C[C@@H]2CN2CCN(c3ccccn3)CC2)cc1 10.1021/jm990562x
127031497 138961 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 351 5 0 3 4.3 Clc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3794469 138961 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 351 5 0 3 4.3 Clc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
4452 2721 18 None -7 18 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as inhibition of lisuride-induced beta arrestin2 recruitment preincubated for 30 mins followed by lisuride-stimulation and measured after 90 mins by coelenterazine-based beta-galactosidase reporter gene assayAntagonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as inhibition of lisuride-induced beta arrestin2 recruitment preincubated for 30 mins followed by lisuride-stimulation and measured after 90 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1021/acs.jmedchem.9b00412
983 2721 18 None -7 18 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as inhibition of lisuride-induced beta arrestin2 recruitment preincubated for 30 mins followed by lisuride-stimulation and measured after 90 mins by coelenterazine-based beta-galactosidase reporter gene assayAntagonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as inhibition of lisuride-induced beta arrestin2 recruitment preincubated for 30 mins followed by lisuride-stimulation and measured after 90 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1021/acs.jmedchem.9b00412
CHEMBL20734 2721 18 None -7 18 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as inhibition of lisuride-induced beta arrestin2 recruitment preincubated for 30 mins followed by lisuride-stimulation and measured after 90 mins by coelenterazine-based beta-galactosidase reporter gene assayAntagonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as inhibition of lisuride-induced beta arrestin2 recruitment preincubated for 30 mins followed by lisuride-stimulation and measured after 90 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1021/acs.jmedchem.9b00412
45278805 7369 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 484 7 1 4 5.2 Cc1c(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(-c2ccccc2)n1C 10.1016/j.bmcl.2010.01.093
CHEMBL1086754 7369 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 484 7 1 4 5.2 Cc1c(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(-c2ccccc2)n1C 10.1016/j.bmcl.2010.01.093
164612037 184795 0 None -1 20 Human 10.1 pKd = 10.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
CHEMBL4860528 184795 0 None -1 20 Human 10.1 pKd = 10.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
168290235 192366 0 None -5 20 Human 10.1 pKd = 10.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5201074 192366 0 None -5 20 Human 10.1 pKd = 10.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222491 192366 0 None -5 20 Human 10.1 pKd = 10.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
168294767 192417 0 None -1 20 Human 10.1 pKd = 10.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5207281 192417 0 None -1 20 Human 10.1 pKd = 10.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222802 192417 0 None -1 20 Human 10.1 pKd = 10.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168295528 192429 0 None -1 20 Human 10.1 pKd = 10.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5206565 192429 0 None -1 20 Human 10.1 pKd = 10.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222872 192429 0 None -1 20 Human 10.1 pKd = 10.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
4452 2721 18 None -7 18 Human 9.7 pKd = 9.7 Binding
Binding Affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding Affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1021/jm9601720
983 2721 18 None -7 18 Human 9.7 pKd = 9.7 Binding
Binding Affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding Affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1021/jm9601720
CHEMBL20734 2721 18 None -7 18 Human 9.7 pKd = 9.7 Binding
Binding Affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding Affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1021/jm9601720
9849682 94511 0 None -602 10 Human 6.9 pKd = 6.9 Binding
Binding affinity to human dopamine D4 receptorBinding affinity to human dopamine D4 receptor
ChEMBL 523 2 1 5 2.9 CN1C[C@H](C(=O)N2CCN(c3cccc(=O)n3C)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL254500 94511 0 None -602 10 Human 6.9 pKd = 6.9 Binding
Binding affinity to human dopamine D4 receptorBinding affinity to human dopamine D4 receptor
ChEMBL 523 2 1 5 2.9 CN1C[C@H](C(=O)N2CCN(c3cccc(=O)n3C)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
10162564 12433 0 None -218 8 Human 6.9 pKd = 6.9 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 475 7 0 3 5.1 CN(CCC(=O)N1CCN(c2ccc(F)c(F)c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL1186652 12433 0 None -218 8 Human 6.9 pKd = 6.9 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 475 7 0 3 5.1 CN(CCC(=O)N1CCN(c2ccc(F)c(F)c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL473763 12433 0 None -218 8 Human 6.9 pKd = 6.9 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 475 7 0 3 5.1 CN(CCC(=O)N1CCN(c2ccc(F)c(F)c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
3251 4009 50 None -43 12 Human 8.6 pKd = 8.6 Binding
Binding affinity to D4 receptor (unknown origin) assessed as dissociation constantBinding affinity to D4 receptor (unknown origin) assessed as dissociation constant
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/acs.jmedchem.2c00633
5684 4009 50 None -43 12 Human 8.6 pKd = 8.6 Binding
Binding affinity to D4 receptor (unknown origin) assessed as dissociation constantBinding affinity to D4 receptor (unknown origin) assessed as dissociation constant
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/acs.jmedchem.2c00633
80 4009 50 None -43 12 Human 8.6 pKd = 8.6 Binding
Binding affinity to D4 receptor (unknown origin) assessed as dissociation constantBinding affinity to D4 receptor (unknown origin) assessed as dissociation constant
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/acs.jmedchem.2c00633
CHEMBL31354 4009 50 None -43 12 Human 8.6 pKd = 8.6 Binding
Binding affinity to D4 receptor (unknown origin) assessed as dissociation constantBinding affinity to D4 receptor (unknown origin) assessed as dissociation constant
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/acs.jmedchem.2c00633
11724450 123330 4 None - 1 Human 8.4 pKd = 8.4 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL184158 123330 4 None - 1 Human 8.4 pKd = 8.4 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL362542 123330 4 None - 1 Human 8.4 pKd = 8.4 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.bmcl.2004.07.068
17955460 176201 0 None -630 9 Human 6.3 pKd = 6.3 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 491 7 0 4 5.3 CN(CCC(=O)N1CCN(c2ccc(F)c(F)c2)CC1)CCC1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL460542 176201 0 None -630 9 Human 6.3 pKd = 6.3 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 491 7 0 4 5.3 CN(CCC(=O)N1CCN(c2ccc(F)c(F)c2)CC1)CCC1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2009.01.072
2030 3615 7 None -7 10 Human 8.3 pKd = 8.3 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@H](CN([C@@H]1C2)C)C(=O)N1CCN(CC1)c1ccc(cc1)[N+](=O)[O-] 10.1016/j.bmcl.2009.01.072
5311377 3615 7 None -7 10 Human 8.3 pKd = 8.3 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@H](CN([C@@H]1C2)C)C(=O)N1CCN(CC1)c1ccc(cc1)[N+](=O)[O-] 10.1016/j.bmcl.2009.01.072
CHEMBL251541 3615 7 None -7 10 Human 8.3 pKd = 8.3 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@H](CN([C@@H]1C2)C)C(=O)N1CCN(CC1)c1ccc(cc1)[N+](=O)[O-] 10.1016/j.bmcl.2009.01.072
2030 3615 7 None -7 10 Human 8.3 pKd = 8.3 Binding
Binding affinity to human dopamine D4 receptorBinding affinity to human dopamine D4 receptor
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@H](CN([C@@H]1C2)C)C(=O)N1CCN(CC1)c1ccc(cc1)[N+](=O)[O-] 10.1016/j.bmcl.2007.04.086
5311377 3615 7 None -7 10 Human 8.3 pKd = 8.3 Binding
Binding affinity to human dopamine D4 receptorBinding affinity to human dopamine D4 receptor
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@H](CN([C@@H]1C2)C)C(=O)N1CCN(CC1)c1ccc(cc1)[N+](=O)[O-] 10.1016/j.bmcl.2007.04.086
CHEMBL251541 3615 7 None -7 10 Human 8.3 pKd = 8.3 Binding
Binding affinity to human dopamine D4 receptorBinding affinity to human dopamine D4 receptor
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@H](CN([C@@H]1C2)C)C(=O)N1CCN(CC1)c1ccc(cc1)[N+](=O)[O-] 10.1016/j.bmcl.2007.04.086
44447073 94114 0 None -208 10 Human 7.1 pKd = 7.1 Binding
Binding affinity to human dopamine D4 receptorBinding affinity to human dopamine D4 receptor
ChEMBL 534 2 1 6 3.8 CN1C[C@H](C(=O)N2CCN(c3ccc4nonc4c3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL251835 94114 0 None -208 10 Human 7.1 pKd = 7.1 Binding
Binding affinity to human dopamine D4 receptorBinding affinity to human dopamine D4 receptor
ChEMBL 534 2 1 6 3.8 CN1C[C@H](C(=O)N2CCN(c3ccc4nonc4c3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
11729231 49344 0 None 1584 4 Human 10.7 pKi = 10.7 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 407 6 1 4 3.6 COc1cccc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1021/jm020952a
CHEMBL156599 49344 0 None 1584 4 Human 10.7 pKi = 10.7 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 407 6 1 4 3.6 COc1cccc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1021/jm020952a
11131951 49651 1 None 363 4 Human 10.6 pKi = 10.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 353 6 1 4 2.6 COc1cccc(C(=O)NCCN2CCN(c3ccc(C)cc3)CC2)c1 10.1021/jm020952a
CHEMBL156845 49651 1 None 363 4 Human 10.6 pKi = 10.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 353 6 1 4 2.6 COc1cccc(C(=O)NCCN2CCN(c3ccc(C)cc3)CC2)c1 10.1021/jm020952a
4257 77868 26 None - 1 Human 10.5 pKi = 10.5 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
ChEMBL 478 4 1 4 4.7 O=C1NC2CCCCN2C12CCN(CCCN1c3ccccc3CCc3ccc(Cl)cc31)CC2 10.1016/j.ejmech.2019.111569
CHEMBL2106650 77868 26 None - 1 Human 10.5 pKi = 10.5 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
ChEMBL 478 4 1 4 4.7 O=C1NC2CCCCN2C12CCN(CCCN1c3ccccc3CCc3ccc(Cl)cc31)CC2 10.1016/j.ejmech.2019.111569
3504099 91728 5 None 3388 3 Human 10.5 pKi = 10.5 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 335 5 1 3 3.9 CCOc1ccccc1N1CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2013.07.033
CHEMBL2420894 91728 5 None 3388 3 Human 10.5 pKi = 10.5 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 335 5 1 3 3.9 CCOc1ccccc1N1CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2013.07.033
10948748 50185 0 None 676 3 Human 10.4 pKi = 10.4 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 373 6 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(c3ccccc3Cl)CC2)c1 10.1021/jm020952a
CHEMBL157322 50185 0 None 676 3 Human 10.4 pKi = 10.4 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 373 6 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(c3ccccc3Cl)CC2)c1 10.1021/jm020952a
3626837 205584 8 None 125 4 Human 10.4 pKi = 10.4 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 373 6 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm020952a
CHEMBL93403 205584 8 None 125 4 Human 10.4 pKi = 10.4 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 373 6 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm020952a
3626837 205584 8 None 125 4 Human 10.4 pKi = 10.4 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 373 6 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
CHEMBL93403 205584 8 None 125 4 Human 10.4 pKi = 10.4 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 373 6 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
16363 589 48 None -1 6 Human 10.2 pKi = 10.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand displacement assayBinding affinity to human dopamine D4 receptor by radioligand displacement assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1016/j.bmc.2016.06.011
312 589 48 None -1 6 Human 10.2 pKi = 10.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand displacement assayBinding affinity to human dopamine D4 receptor by radioligand displacement assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1016/j.bmc.2016.06.011
9215 589 48 None -1 6 Human 10.2 pKi = 10.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand displacement assayBinding affinity to human dopamine D4 receptor by radioligand displacement assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1016/j.bmc.2016.06.011
CHEMBL297302 589 48 None -1 6 Human 10.2 pKi = 10.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand displacement assayBinding affinity to human dopamine D4 receptor by radioligand displacement assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1016/j.bmc.2016.06.011
DB12867 589 48 None -1 6 Human 10.2 pKi = 10.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand displacement assayBinding affinity to human dopamine D4 receptor by radioligand displacement assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1016/j.bmc.2016.06.011
2470 3596 46 None -20 59 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2013.01.025
3300 3596 46 None -20 59 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2013.01.025
5265 3596 46 None -20 59 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2013.01.025
99 3596 46 None -20 59 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2013.01.025
CHEMBL267930 3596 46 None -20 59 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2013.01.025
72901200 119272 21 None 154 4 Human 9.7 pKi = 9.7 Binding
Selectivity interaction (BRET-Gi dissociation assay) EUB0000539a DRD4Selectivity interaction (BRET-Gi dissociation assay) EUB0000539a DRD4
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 nan
CHEMBL3480577 119272 21 None 154 4 Human 9.7 pKi = 9.7 Binding
Selectivity interaction (BRET-Gi dissociation assay) EUB0000539a DRD4Selectivity interaction (BRET-Gi dissociation assay) EUB0000539a DRD4
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 nan
11090403 119039 0 None 2 3 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 389 6 1 4 3.4 COc1cccc(C(=O)NCCN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/jm020952a
CHEMBL345848 119039 0 None 2 3 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 389 6 1 4 3.4 COc1cccc(C(=O)NCCN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/jm020952a
9977532 110703 0 None 6 4 Human 9.6 pKi = 9.6 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL326454 110703 0 None 6 4 Human 9.6 pKi = 9.6 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
11574902 78041 0 None 537 4 Human 9.6 pKi = 9.6 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
ChEMBL 400 4 0 5 3.4 COc1ccccc1N1CCN(Cc2cn3cc(Br)ccc3n2)CC1 10.1016/j.ejmech.2019.111569
CHEMBL211164 78041 0 None 537 4 Human 9.6 pKi = 9.6 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
ChEMBL 400 4 0 5 3.4 COc1ccccc1N1CCN(Cc2cn3cc(Br)ccc3n2)CC1 10.1016/j.ejmech.2019.111569
155515982 169443 0 None 6 17 Human 9.6 pKi = 9.6 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4442460 169443 0 None 6 17 Human 9.6 pKi = 9.6 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
11574902 78041 0 None 537 4 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 400 4 0 5 3.4 COc1ccccc1N1CCN(Cc2cn3cc(Br)ccc3n2)CC1 10.1021/jm060166w
CHEMBL211164 78041 0 None 537 4 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 400 4 0 5 3.4 COc1ccccc1N1CCN(Cc2cn3cc(Br)ccc3n2)CC1 10.1021/jm060166w
11036114 50250 0 None 134 3 Human 9.6 pKi = 9.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 373 6 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(c3cccc(Cl)c3)CC2)c1 10.1021/jm020952a
CHEMBL157388 50250 0 None 134 3 Human 9.6 pKi = 9.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 373 6 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(c3cccc(Cl)c3)CC2)c1 10.1021/jm020952a
17449900 139012 12 None 23 6 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 348 5 0 5 3.2 COc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2006.02.075
CHEMBL379602 139012 12 None 23 6 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 348 5 0 5 3.2 COc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2006.02.075
10733406 19241 0 None 70 2 Human 9.5 pKi = 9.5 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 305 9 1 3 3.8 Clc1cccc(OCCNCCCOc2ccccc2)c1 10.1016/j.bmcl.2005.02.012
CHEMBL129534 19241 0 None 70 2 Human 9.5 pKi = 9.5 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 305 9 1 3 3.8 Clc1cccc(OCCNCCCOc2ccccc2)c1 10.1016/j.bmcl.2005.02.012
10733406 19241 0 None 70 2 Human 9.5 pKi = 9.5 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 305 9 1 3 3.8 Clc1cccc(OCCNCCCOc2ccccc2)c1 10.1021/jm970422s
CHEMBL129534 19241 0 None 70 2 Human 9.5 pKi = 9.5 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 305 9 1 3 3.8 Clc1cccc(OCCNCCCOc2ccccc2)c1 10.1021/jm970422s
10546540 205507 0 None 288 3 Human 9.5 pKi = 9.5 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 361 4 1 4 4.7 Cc1cccc(CN2CCC(n3c(O)nc(-c4ccccc4)c3C)CC2)c1 10.1021/jm991029k
CHEMBL92859 205507 0 None 288 3 Human 9.5 pKi = 9.5 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 361 4 1 4 4.7 Cc1cccc(CN2CCC(n3c(O)nc(-c4ccccc4)c3C)CC2)c1 10.1021/jm991029k
11583188 138752 0 None 218 4 Human 9.5 pKi = 9.5 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
ChEMBL 448 4 0 5 3.3 COc1ccccc1N1CCN(Cc2cn3cc(I)ccc3n2)CC1 10.1016/j.ejmech.2019.111569
CHEMBL379125 138752 0 None 218 4 Human 9.5 pKi = 9.5 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
ChEMBL 448 4 0 5 3.3 COc1ccccc1N1CCN(Cc2cn3cc(I)ccc3n2)CC1 10.1016/j.ejmech.2019.111569
2470 3596 46 None -20 59 Human 9.5 pKi = 9.5 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm049612a
3300 3596 46 None -20 59 Human 9.5 pKi = 9.5 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm049612a
5265 3596 46 None -20 59 Human 9.5 pKi = 9.5 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm049612a
99 3596 46 None -20 59 Human 9.5 pKi = 9.5 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm049612a
CHEMBL267930 3596 46 None -20 59 Human 9.5 pKi = 9.5 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm049612a
11583188 138752 0 None 218 4 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 448 4 0 5 3.3 COc1ccccc1N1CCN(Cc2cn3cc(I)ccc3n2)CC1 10.1021/jm060166w
CHEMBL379125 138752 0 None 218 4 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 448 4 0 5 3.3 COc1ccccc1N1CCN(Cc2cn3cc(I)ccc3n2)CC1 10.1021/jm060166w
5041 3242 5 None -1 5 Human 9.5 pKi = 9.5 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 10.1021/acs.jmedchem.7b00151
981 3242 5 None -1 5 Human 9.5 pKi = 9.5 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 10.1021/acs.jmedchem.7b00151
CHEMBL4096543 3242 5 None -1 5 Human 9.5 pKi = 9.5 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 10.1021/acs.jmedchem.7b00151
5041 3242 5 None -1 5 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 10.1021/acs.jmedchem.8b00265
981 3242 5 None -1 5 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 10.1021/acs.jmedchem.8b00265
CHEMBL4096543 3242 5 None -1 5 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 10.1021/acs.jmedchem.8b00265
49788939 18075 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 368 5 1 5 2.5 O=C(NCCN1CCN(c2noc3ccccc23)CC1)c1ccc(F)cc1 10.1021/jm100925m
CHEMBL1270323 18075 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 368 5 1 5 2.5 O=C(NCCN1CCN(c2noc3ccccc23)CC1)c1ccc(F)cc1 10.1021/jm100925m
10780510 19297 0 None 208 3 Human 9.5 pKi = 9.5 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCNCCCOc2ccccc2)cc1C 10.1016/j.bmcl.2005.02.012
CHEMBL129927 19297 0 None 208 3 Human 9.5 pKi = 9.5 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCNCCCOc2ccccc2)cc1C 10.1016/j.bmcl.2005.02.012
10780510 19297 0 None 208 3 Human 9.5 pKi = 9.5 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCNCCCOc2ccccc2)cc1C 10.1021/jm970422s
CHEMBL129927 19297 0 None 208 3 Human 9.5 pKi = 9.5 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCNCCCOc2ccccc2)cc1C 10.1021/jm970422s
44400585 68313 0 None 26 5 Human 9.4 pKi = 9.4 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
CHEMBL191962 68313 0 None 26 5 Human 9.4 pKi = 9.4 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
21219157 98443 0 None 15 3 Human 9.4 pKi = 9.4 Binding
Binding affinity of compound towards human Dopamine receptor D4 by displacing [125I]-iodosulpiride expressed in CHO cellsBinding affinity of compound towards human Dopamine receptor D4 by displacing [125I]-iodosulpiride expressed in CHO cells
ChEMBL 331 4 0 3 4.7 Cc1nn(C2CCN(Cc3ccccc3)CC2)cc1-c1ccccc1 10.1021/jm030836n
CHEMBL279247 98443 0 None 15 3 Human 9.4 pKi = 9.4 Binding
Binding affinity of compound towards human Dopamine receptor D4 by displacing [125I]-iodosulpiride expressed in CHO cellsBinding affinity of compound towards human Dopamine receptor D4 by displacing [125I]-iodosulpiride expressed in CHO cells
ChEMBL 331 4 0 3 4.7 Cc1nn(C2CCN(Cc3ccccc3)CC2)cc1-c1ccccc1 10.1021/jm030836n
21219157 98443 0 None 15 3 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 331 4 0 3 4.7 Cc1nn(C2CCN(Cc3ccccc3)CC2)cc1-c1ccccc1 10.1016/s0960-894x(99)00169-9
CHEMBL279247 98443 0 None 15 3 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 331 4 0 3 4.7 Cc1nn(C2CCN(Cc3ccccc3)CC2)cc1-c1ccccc1 10.1016/s0960-894x(99)00169-9
3303 2213 41 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm0305669
5311200 2213 41 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm0305669
CHEMBL267014 2213 41 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm0305669
3716121 83667 14 None 70 5 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 332 4 0 3 4.1 COc1ccccc1N1CCN(Cc2ccc3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207643 83667 14 None 70 5 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 332 4 0 3 4.1 COc1ccccc1N1CCN(Cc2ccc3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
168287284 192333 0 None 316 3 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 394 6 0 5 3.1 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2[N+](=O)[O-])CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5198170 192333 0 None 316 3 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 394 6 0 5 3.1 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2[N+](=O)[O-])CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222300 192333 0 None 316 3 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 394 6 0 5 3.1 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2[N+](=O)[O-])CC1 10.1021/acs.jmedchem.2c00840
3303 2213 41 None 1 15 Human 9.4 pKi = 9.4 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(99)00025-6
5311200 2213 41 None 1 15 Human 9.4 pKi = 9.4 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(99)00025-6
CHEMBL267014 2213 41 None 1 15 Human 9.4 pKi = 9.4 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(99)00025-6
3303 2213 41 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmcl.2004.09.046
5311200 2213 41 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmcl.2004.09.046
CHEMBL267014 2213 41 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmcl.2004.09.046
3303 2213 41 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm9600712
5311200 2213 41 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm9600712
CHEMBL267014 2213 41 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm9600712
3303 2213 41 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm0002432
5311200 2213 41 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm0002432
CHEMBL267014 2213 41 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm0002432
3303 2213 41 None 1 15 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmc.2008.12.054
5311200 2213 41 None 1 15 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmc.2008.12.054
CHEMBL267014 2213 41 None 1 15 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmc.2008.12.054
3303 2213 41 None -1 15 Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmc.2014.04.026
5311200 2213 41 None -1 15 Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmc.2014.04.026
CHEMBL267014 2213 41 None -1 15 Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmc.2014.04.026
3303 2213 41 None 1 15 Human 9.4 pKi = 9.4 Binding
In vitro binding affinity to human Dopamine receptor D4In vitro binding affinity to human Dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00241-4
5311200 2213 41 None 1 15 Human 9.4 pKi = 9.4 Binding
In vitro binding affinity to human Dopamine receptor D4In vitro binding affinity to human Dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00241-4
CHEMBL267014 2213 41 None 1 15 Human 9.4 pKi = 9.4 Binding
In vitro binding affinity to human Dopamine receptor D4In vitro binding affinity to human Dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00241-4
3303 2213 41 None 1 15 Human 9.4 pKi = 9.4 Binding
In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm981041x
5311200 2213 41 None 1 15 Human 9.4 pKi = 9.4 Binding
In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm981041x
CHEMBL267014 2213 41 None 1 15 Human 9.4 pKi = 9.4 Binding
In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm981041x
3303 2213 41 None 1 15 Human 9.4 pKi = 9.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.7b00151
5311200 2213 41 None 1 15 Human 9.4 pKi = 9.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.7b00151
CHEMBL267014 2213 41 None 1 15 Human 9.4 pKi = 9.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.7b00151
44412482 77797 0 None 79 4 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 349 5 0 6 2.6 COc1ccccc1N1CCN(Cc2cnn(-c3ccccn3)c2)CC1 10.1021/jm0611152
CHEMBL210404 77797 0 None 79 4 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 349 5 0 6 2.6 COc1ccccc1N1CCN(Cc2cnn(-c3ccccn3)c2)CC1 10.1021/jm0611152
44412482 77797 0 None 79 4 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 349 5 0 6 2.6 COc1ccccc1N1CCN(Cc2cnn(-c3ccccn3)c2)CC1 10.1016/j.bmcl.2006.02.075
CHEMBL210404 77797 0 None 79 4 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 349 5 0 6 2.6 COc1ccccc1N1CCN(Cc2cnn(-c3ccccn3)c2)CC1 10.1016/j.bmcl.2006.02.075
2470 3596 46 None -20 59 Human 9.4 pKi = 9.4 Binding
Binding affinity to dopamine D4 receptor (unknown origin)Binding affinity to dopamine D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/acs.jmedchem.7b01248
3300 3596 46 None -20 59 Human 9.4 pKi = 9.4 Binding
Binding affinity to dopamine D4 receptor (unknown origin)Binding affinity to dopamine D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/acs.jmedchem.7b01248
5265 3596 46 None -20 59 Human 9.4 pKi = 9.4 Binding
Binding affinity to dopamine D4 receptor (unknown origin)Binding affinity to dopamine D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/acs.jmedchem.7b01248
99 3596 46 None -20 59 Human 9.4 pKi = 9.4 Binding
Binding affinity to dopamine D4 receptor (unknown origin)Binding affinity to dopamine D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/acs.jmedchem.7b01248
CHEMBL267930 3596 46 None -20 59 Human 9.4 pKi = 9.4 Binding
Binding affinity to dopamine D4 receptor (unknown origin)Binding affinity to dopamine D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/acs.jmedchem.7b01248
44436598 148763 0 None 112 4 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 401 5 1 3 3.5 C#Cc1cccc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmc.2007.08.038
CHEMBL394473 148763 0 None 112 4 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 401 5 1 3 3.5 C#Cc1cccc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmc.2007.08.038
2470 3596 46 None -20 59 Human 9.4 pKi = 9.4 Binding
Inhibition of D4 receptor (unknown origin)Inhibition of D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/acs.jmedchem.9b00412
3300 3596 46 None -20 59 Human 9.4 pKi = 9.4 Binding
Inhibition of D4 receptor (unknown origin)Inhibition of D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/acs.jmedchem.9b00412
5265 3596 46 None -20 59 Human 9.4 pKi = 9.4 Binding
Inhibition of D4 receptor (unknown origin)Inhibition of D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/acs.jmedchem.9b00412
99 3596 46 None -20 59 Human 9.4 pKi = 9.4 Binding
Inhibition of D4 receptor (unknown origin)Inhibition of D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/acs.jmedchem.9b00412
CHEMBL267930 3596 46 None -20 59 Human 9.4 pKi = 9.4 Binding
Inhibition of D4 receptor (unknown origin)Inhibition of D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/acs.jmedchem.9b00412
10660814 18684 2 None 134 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 285 9 1 3 3.4 Cc1cccc(OCCNCCCOc2ccccc2)c1 10.1016/j.bmcl.2005.02.012
CHEMBL128232 18684 2 None 134 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 285 9 1 3 3.4 Cc1cccc(OCCNCCCOc2ccccc2)c1 10.1016/j.bmcl.2005.02.012
10667579 205654 0 None 2818 2 Human 9.3 pKi = 9.3 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 381 4 1 4 5.1 Cc1c(-c2ccccc2)nc(O)n1C1CCN(Cc2cccc(Cl)c2)CC1 10.1021/jm991029k
CHEMBL93832 205654 0 None 2818 2 Human 9.3 pKi = 9.3 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 381 4 1 4 5.1 Cc1c(-c2ccccc2)nc(O)n1C1CCN(Cc2cccc(Cl)c2)CC1 10.1021/jm991029k
10660814 18684 2 None 134 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 285 9 1 3 3.4 Cc1cccc(OCCNCCCOc2ccccc2)c1 10.1021/jm970422s
CHEMBL128232 18684 2 None 134 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 285 9 1 3 3.4 Cc1cccc(OCCNCCCOc2ccccc2)c1 10.1021/jm970422s
119570 3110 90 None -10 40 Human 9.3 pKi = 9.3 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
2233 3110 90 None -10 40 Human 9.3 pKi = 9.3 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
953 3110 90 None -10 40 Human 9.3 pKi = 9.3 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
CHEMBL301265 3110 90 None -10 40 Human 9.3 pKi = 9.3 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
DB00413 3110 90 None -10 40 Human 9.3 pKi = 9.3 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
6603897 2216 19 None -5 2 Human 9.3 pKi = 9.3 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 418 3 1 3 3.5 Ic1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm9600712
978 2216 19 None -5 2 Human 9.3 pKi = 9.3 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 418 3 1 3 3.5 Ic1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm9600712
CHEMBL60518 2216 19 None -5 2 Human 9.3 pKi = 9.3 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 418 3 1 3 3.5 Ic1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm9600712
168268758 192163 0 None 107 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting methodDisplacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2Cl)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5172201 192163 0 None 107 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting methodDisplacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2Cl)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5221189 192163 0 None 107 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting methodDisplacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2Cl)CC1 10.1021/acs.jmedchem.2c00840
10708280 18761 1 None 323 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 285 9 1 3 3.4 Cc1ccc(OCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
CHEMBL128647 18761 1 None 323 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 285 9 1 3 3.4 Cc1ccc(OCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
10450892 21671 0 None 7 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 319 9 1 3 4.1 Cc1ccc(OCCNCCCOc2ccccc2)cc1Cl 10.1021/jm970422s
CHEMBL131997 21671 0 None 7 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 319 9 1 3 4.1 Cc1ccc(OCCNCCCOc2ccccc2)cc1Cl 10.1021/jm970422s
9995904 31004 2 None 1047 5 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4)CC3)cc2c1 10.1021/jm0009989
CHEMBL140099 31004 2 None 1047 5 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4)CC3)cc2c1 10.1021/jm0009989
9995904 31004 2 None 1047 5 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4)CC3)cc2c1 10.1021/jm060166w
CHEMBL140099 31004 2 None 1047 5 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4)CC3)cc2c1 10.1021/jm060166w
44400674 124669 0 None -1 5 Human 9.3 pKi = 9.3 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
CHEMBL364516 124669 0 None -1 5 Human 9.3 pKi = 9.3 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
10708280 18761 1 None 323 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 285 9 1 3 3.4 Cc1ccc(OCCNCCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL128647 18761 1 None 323 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 285 9 1 3 3.4 Cc1ccc(OCCNCCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
10450892 21671 0 None 7 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 319 9 1 3 4.1 Cc1ccc(OCCNCCCOc2ccccc2)cc1Cl 10.1016/j.bmcl.2005.02.012
CHEMBL131997 21671 0 None 7 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 319 9 1 3 4.1 Cc1ccc(OCCNCCCOc2ccccc2)cc1Cl 10.1016/j.bmcl.2005.02.012
10315310 22681 0 None 58 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 305 9 1 3 3.8 Clc1ccc(OCCNCCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL132884 22681 0 None 58 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 305 9 1 3 3.8 Clc1ccc(OCCNCCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
10315310 22681 0 None 58 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 305 9 1 3 3.8 Clc1ccc(OCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
CHEMBL132884 22681 0 None 58 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 305 9 1 3 3.8 Clc1ccc(OCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
11655570 79316 0 None 173 4 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 462 4 0 5 3.6 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(I)c3n2)CC1 10.1021/jm060166w
CHEMBL211590 79316 0 None 173 4 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 462 4 0 5 3.6 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(I)c3n2)CC1 10.1021/jm060166w
32224 205178 3 None 4 3 Human 9.3 pKi = 9.3 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 326 1 0 3 4.2 CN1CCN(C2=Cc3ccccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm00004a016
CHEMBL90882 205178 3 None 4 3 Human 9.3 pKi = 9.3 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 326 1 0 3 4.2 CN1CCN(C2=Cc3ccccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm00004a016
32224 205178 3 None 4 3 Human 9.3 pKi = 9.3 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 326 1 0 3 4.2 CN1CCN(C2=Cc3ccccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm00043a008
CHEMBL90882 205178 3 None 4 3 Human 9.3 pKi = 9.3 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 326 1 0 3 4.2 CN1CCN(C2=Cc3ccccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm00043a008
44326285 111054 0 None 2 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 359 5 2 4 2.9 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
CHEMBL327984 111054 0 None 2 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 359 5 2 4 2.9 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
9888765 189026 1 None 3 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to human cloned dopamine D4.4 receptorBinding affinity to human cloned dopamine D4.4 receptor
ChEMBL 427 7 1 5 5.1 Nc1nc(-c2ccc(F)cc2)c([C@@H]2CCN(CCCC(=O)c3ccc(F)cc3)C2)s1 10.1016/j.bmc.2008.02.091
CHEMBL514848 189026 1 None 3 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to human cloned dopamine D4.4 receptorBinding affinity to human cloned dopamine D4.4 receptor
ChEMBL 427 7 1 5 5.1 Nc1nc(-c2ccc(F)cc2)c([C@@H]2CCN(CCCC(=O)c3ccc(F)cc3)C2)s1 10.1016/j.bmc.2008.02.091
155552185 173489 0 None 2 16 Human 9.3 pKi = 9.3 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4544086 173489 0 None 2 16 Human 9.3 pKi = 9.3 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
155559617 174312 0 None 9 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4563944 174312 0 None 9 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
10522613 205230 0 None 389 2 Human 9.3 pKi = 9.3 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 361 5 1 4 4.4 Cc1c(-c2ccccc2)nc(O)n1C1CCN(CCc2ccccc2)CC1 10.1021/jm991029k
CHEMBL91229 205230 0 None 389 2 Human 9.3 pKi = 9.3 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 361 5 1 4 4.4 Cc1c(-c2ccccc2)nc(O)n1C1CCN(CCc2ccccc2)CC1 10.1021/jm991029k
44419065 83906 0 None 56 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 317 4 0 3 4.3 c1ccc(C2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1021/jm0611152
CHEMBL221600 83906 0 None 56 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 317 4 0 3 4.3 c1ccc(C2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1021/jm0611152
11983282 138414 0 None 56 6 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 315 4 0 3 4.2 C1=C(c2ccccc2)CCN(Cc2cnn(-c3ccccc3)c2)C1 10.1016/j.bmcl.2006.02.075
CHEMBL378455 138414 0 None 56 6 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 315 4 0 3 4.2 C1=C(c2ccccc2)CCN(Cc2cnn(-c3ccccc3)c2)C1 10.1016/j.bmcl.2006.02.075
9950165 205221 0 None 93 3 Human 9.2 pKi = 9.2 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 347 4 1 4 4.4 Cc1c(-c2ccccc2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL91162 205221 0 None 93 3 Human 9.2 pKi = 9.2 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 347 4 1 4 4.4 Cc1c(-c2ccccc2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
3303 2213 41 None 1 15 Human 9.2 pKi = 9.2 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00692-1
5311200 2213 41 None 1 15 Human 9.2 pKi = 9.2 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00692-1
CHEMBL267014 2213 41 None 1 15 Human 9.2 pKi = 9.2 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00692-1
44400519 132608 0 None 1 5 Human 9.2 pKi = 9.2 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
CHEMBL370297 132608 0 None 1 5 Human 9.2 pKi = 9.2 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
168268758 192163 0 None 107 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2Cl)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5172201 192163 0 None 107 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2Cl)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5221189 192163 0 None 107 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2Cl)CC1 10.1021/acs.jmedchem.2c00840
9977022 192289 0 None 131 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 379 6 0 4 3.2 COc1ccccc1N1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5189614 192289 0 None 131 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 379 6 0 4 3.2 COc1ccccc1N1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222031 192289 0 None 131 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 379 6 0 4 3.2 COc1ccccc1N1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.2c00840
3303 2213 41 None 1 15 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm0611152
5311200 2213 41 None 1 15 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm0611152
CHEMBL267014 2213 41 None 1 15 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm0611152
3303 2213 41 None 1 15 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmc.2009.05.015
5311200 2213 41 None 1 15 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmc.2009.05.015
CHEMBL267014 2213 41 None 1 15 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmc.2009.05.015
3303 2213 41 None 1 15 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00814-9
5311200 2213 41 None 1 15 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00814-9
CHEMBL267014 2213 41 None 1 15 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00814-9
10783358 39429 4 None 42 2 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 340 6 1 5 1.6 COc1cccc(C(=O)NCCN2CCN(c3ccccn3)CC2)c1 10.1021/jm020952a
CHEMBL147483 39429 4 None 42 2 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 340 6 1 5 1.6 COc1cccc(C(=O)NCCN2CCN(c3ccccn3)CC2)c1 10.1021/jm020952a
11676195 193478 0 None 1 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 423 8 1 6 3.4 CSc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm900690y
CHEMBL550222 193478 0 None 1 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 423 8 1 6 3.4 CSc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm900690y
44400626 70059 0 None 38 5 Human 9.2 pKi = 9.2 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
CHEMBL194555 70059 0 None 38 5 Human 9.2 pKi = 9.2 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
10547607 205218 0 None 1380 2 Human 9.2 pKi = 9.2 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 377 5 1 5 4.4 COc1cccc(CN2CCC(n3c(O)nc(-c4ccccc4)c3C)CC2)c1 10.1021/jm991029k
CHEMBL91155 205218 0 None 1380 2 Human 9.2 pKi = 9.2 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 377 5 1 5 4.4 COc1cccc(CN2CCC(n3c(O)nc(-c4ccccc4)c3C)CC2)c1 10.1021/jm991029k
168285556 192315 0 None 2454 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5196870 192315 0 None 2454 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222200 192315 0 None 2454 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
11057969 33052 0 None 223 5 Human 9.2 pKi = 9.2 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 379 6 1 6 1.9 COc1ccccc1N1CCN(CCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm049612a
CHEMBL141845 33052 0 None 223 5 Human 9.2 pKi = 9.2 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 379 6 1 6 1.9 COc1ccccc1N1CCN(CCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm049612a
11057969 33052 0 None 223 5 Human 9.2 pKi = 9.2 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 379 6 1 6 1.9 COc1ccccc1N1CCN(CCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
CHEMBL141845 33052 0 None 223 5 Human 9.2 pKi = 9.2 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 379 6 1 6 1.9 COc1ccccc1N1CCN(CCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
10669042 107658 0 None -2 3 Human 9.2 pKi = 9.2 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 405 5 2 4 4.2 CNc1cc(OC)c(C(=O)N[C@H]2CCN(C3C4CCCC3CCC4)C2)cc1Cl 10.1021/jm9601720
CHEMBL319597 107658 0 None -2 3 Human 9.2 pKi = 9.2 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 405 5 2 4 4.2 CNc1cc(OC)c(C(=O)N[C@H]2CCN(C3C4CCCC3CCC4)C2)cc1Cl 10.1021/jm9601720
168268850 192182 0 None 741 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 417 5 0 3 4.5 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2Cl)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5179930 192182 0 None 741 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 417 5 0 3 4.5 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2Cl)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5221350 192182 0 None 741 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 417 5 0 3 4.5 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2Cl)CC1 10.1021/acs.jmedchem.2c00840
11057969 33052 0 None 223 5 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 379 6 1 6 1.9 COc1ccccc1N1CCN(CCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm0611152
CHEMBL141845 33052 0 None 223 5 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 379 6 1 6 1.9 COc1ccccc1N1CCN(CCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm0611152
25072633 158675 0 None 1 5 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccc3ccnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4098803 158675 0 None 1 5 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccc3ccnn3c2)CC1 10.1021/acs.jmedchem.6b01857
168268839 192179 0 None 30 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 417 5 0 3 4.5 O=C1CCc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5177462 192179 0 None 30 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 417 5 0 3 4.5 O=C1CCc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5221334 192179 0 None 30 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 417 5 0 3 4.5 O=C1CCc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/acs.jmedchem.2c00840
792584 91720 7 None 58 3 Human 9.2 pKi = 9.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 297 5 0 4 2.8 CCOc1ccccc1N1CCN(Cc2cccnc2)CC1 10.1016/j.bmcl.2013.07.033
CHEMBL2420779 91720 7 None 58 3 Human 9.2 pKi = 9.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 297 5 0 4 2.8 CCOc1ccccc1N1CCN(Cc2cccnc2)CC1 10.1016/j.bmcl.2013.07.033
3303 2213 41 None 1 15 Human 9.2 pKi = 9.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.9b01085
5311200 2213 41 None 1 15 Human 9.2 pKi = 9.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.9b01085
CHEMBL267014 2213 41 None 1 15 Human 9.2 pKi = 9.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.9b01085
41532205 77880 1 None 69 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 336 4 0 4 3.3 Fc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2006.02.075
CHEMBL210717 77880 1 None 69 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 336 4 0 4 3.3 Fc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2006.02.075
2653640 65887 12 None - 1 Human 9.2 pKi = 9.2 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4 alleleIn vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4 allele
ChEMBL 339 5 1 4 2.8 COc1ccccc1N1CCN(CC(=O)Nc2cccc(C)c2)CC1 10.1016/j.bmcl.2004.07.068
CHEMBL184486 65887 12 None - 1 Human 9.2 pKi = 9.2 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4 alleleIn vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4 allele
ChEMBL 339 5 1 4 2.8 COc1ccccc1N1CCN(CC(=O)Nc2cccc(C)c2)CC1 10.1016/j.bmcl.2004.07.068
10450375 99031 0 None -1 4 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.
ChEMBL 347 5 0 4 3.8 COc1ccccc1N1CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1021/jm981041x
CHEMBL28321 99031 0 None -1 4 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.
ChEMBL 347 5 0 4 3.8 COc1ccccc1N1CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1021/jm981041x
41532205 77880 1 None 69 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 336 4 0 4 3.3 Fc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1021/jm0611152
CHEMBL210717 77880 1 None 69 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 336 4 0 4 3.3 Fc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1021/jm0611152
10643588 205690 0 None 239 3 Human 9.2 pKi = 9.2 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 381 4 1 4 5.1 Cc1c(-c2ccc(Cl)cc2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL94023 205690 0 None 239 3 Human 9.2 pKi = 9.2 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 381 4 1 4 5.1 Cc1c(-c2ccc(Cl)cc2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
71456045 83659 0 None 141 6 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 362 5 1 4 3.6 COc1ccccc1N1CCN(Cc2cc(CO)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207635 83659 0 None 141 6 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 362 5 1 4 3.6 COc1ccccc1N1CCN(Cc2cc(CO)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
49782398 17270 0 None 5 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 471 6 1 3 5.7 O=C(CCCN1CCC(O)(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1ccc(F)cc1 10.1021/jm100899z
CHEMBL1257688 17270 0 None 5 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 471 6 1 3 5.7 O=C(CCCN1CCC(O)(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1ccc(F)cc1 10.1021/jm100899z
122191607 123205 0 None 74 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells
ChEMBL 468 9 1 3 5.0 CCCN(CCN1CCN(CCc2c[nH]c3ccccc23)CC1)c1ccc(Br)cc1 10.1021/acsmedchemlett.5b00131
CHEMBL3622099 123205 0 None 74 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells
ChEMBL 468 9 1 3 5.0 CCCN(CCN1CCN(CCc2c[nH]c3ccccc23)CC1)c1ccc(Br)cc1 10.1021/acsmedchemlett.5b00131
25093832 155339 0 None -3 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4060461 155339 0 None -3 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
1353 1880 85 None -3 85 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm020952a
3559 1880 85 None -3 85 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm020952a
86 1880 85 None -3 85 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm020952a
CHEMBL54 1880 85 None -3 85 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm020952a
DB00502 1880 85 None -3 85 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm020952a
10594764 111281 0 None 19 3 Human 9.1 pKi = 9.1 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 361 4 0 4 4.0 Cc1c(-c2ccccc2)n(C)c(=O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL328739 111281 0 None 19 3 Human 9.1 pKi = 9.1 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 361 4 0 4 4.0 Cc1c(-c2ccccc2)n(C)c(=O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
4452 2721 18 None -7 18 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1016/j.bmcl.2021.128047
983 2721 18 None -7 18 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1016/j.bmcl.2021.128047
CHEMBL20734 2721 18 None -7 18 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1016/j.bmcl.2021.128047
44340097 9349 0 None 8 4 Human 9.1 pKi = 9.1 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL111749 9349 0 None 8 4 Human 9.1 pKi = 9.1 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
102505294 192397 0 None 309 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting methodDisplacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5204418 192397 0 None 309 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting methodDisplacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222691 192397 0 None 309 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting methodDisplacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2)CC1 10.1021/acs.jmedchem.2c00840
71454295 83665 0 None 30 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 536 8 0 6 5.5 COc1ccccc1N1CCN(Cc2cc(CN3CCN(c4ccccc4OC)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207641 83665 0 None 30 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 536 8 0 6 5.5 COc1ccccc1N1CCN(Cc2cc(CN3CCN(c4ccccc4OC)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
10638052 19892 0 None 70 3 Human 9.1 pKi = 9.1 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 301 9 1 3 4.1 Cc1ccc(OCCNCCCSc2ccccc2)cc1 10.1021/jm970422s
CHEMBL130402 19892 0 None 70 3 Human 9.1 pKi = 9.1 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 301 9 1 3 4.1 Cc1ccc(OCCNCCCSc2ccccc2)cc1 10.1021/jm970422s
60165418 74999 0 None 8 6 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 353 6 0 6 3.2 c1cnc(N2CCN(CCCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.ejmech.2012.03.042
CHEMBL2037521 74999 0 None 8 6 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 353 6 0 6 3.2 c1cnc(N2CCN(CCCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.ejmech.2012.03.042
10734727 19262 0 None 117 3 Human 9.1 pKi = 9.1 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 323 9 1 3 3.9 Fc1ccc(OCCCNCCOc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL129757 19262 0 None 117 3 Human 9.1 pKi = 9.1 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 323 9 1 3 3.9 Fc1ccc(OCCCNCCOc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2005.02.012
9977532 110703 0 None 6 4 Human 9.1 pKi = 9.1 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL326454 110703 0 None 6 4 Human 9.1 pKi = 9.1 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
10783874 205318 0 None 13 3 Human 9.1 pKi = 9.1 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 347 4 0 4 3.7 Cn1c(-c2ccccc2)cn(C2CCN(Cc3ccccc3)CC2)c1=O 10.1021/jm991029k
CHEMBL91669 205318 0 None 13 3 Human 9.1 pKi = 9.1 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 347 4 0 4 3.7 Cn1c(-c2ccccc2)cn(C2CCN(Cc3ccccc3)CC2)c1=O 10.1021/jm991029k
10734727 19262 0 None 117 3 Human 9.1 pKi = 9.1 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 323 9 1 3 3.9 Fc1ccc(OCCCNCCOc2ccc(Cl)cc2)cc1 10.1021/jm970422s
CHEMBL129757 19262 0 None 117 3 Human 9.1 pKi = 9.1 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 323 9 1 3 3.9 Fc1ccc(OCCCNCCOc2ccc(Cl)cc2)cc1 10.1021/jm970422s
60165418 74999 0 None 8 6 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 353 6 0 6 3.2 c1cnc(N2CCN(CCCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL2037521 74999 0 None 8 6 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 353 6 0 6 3.2 c1cnc(N2CCN(CCCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
11697270 76957 0 None 44 4 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 412 5 0 5 4.6 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(-c4ccccc4)c3n2)CC1 10.1021/jm060166w
CHEMBL208274 76957 0 None 44 4 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 412 5 0 5 4.6 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(-c4ccccc4)c3n2)CC1 10.1021/jm060166w
10522614 205289 0 None 30 3 Human 9.1 pKi = 9.1 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 361 5 1 4 4.7 CCc1c(-c2ccccc2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL91498 205289 0 None 30 3 Human 9.1 pKi = 9.1 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 361 5 1 4 4.7 CCc1c(-c2ccccc2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
4452 2721 18 None -7 18 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-N-Methylspiperone from human dopamine D4 receptor expressed in stable HEK cells incubated for 90 mins by microbeta counting methodDisplacement of [3H]-N-Methylspiperone from human dopamine D4 receptor expressed in stable HEK cells incubated for 90 mins by microbeta counting method
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1016/j.bmc.2020.115578
983 2721 18 None -7 18 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-N-Methylspiperone from human dopamine D4 receptor expressed in stable HEK cells incubated for 90 mins by microbeta counting methodDisplacement of [3H]-N-Methylspiperone from human dopamine D4 receptor expressed in stable HEK cells incubated for 90 mins by microbeta counting method
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1016/j.bmc.2020.115578
CHEMBL20734 2721 18 None -7 18 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-N-Methylspiperone from human dopamine D4 receptor expressed in stable HEK cells incubated for 90 mins by microbeta counting methodDisplacement of [3H]-N-Methylspiperone from human dopamine D4 receptor expressed in stable HEK cells incubated for 90 mins by microbeta counting method
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1016/j.bmc.2020.115578
168274496 192210 0 None 724 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 417 5 0 3 4.5 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5175054 192210 0 None 724 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 417 5 0 3 4.5 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5221490 192210 0 None 724 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 417 5 0 3 4.5 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1021/acs.jmedchem.2c00840
12765116 204793 1 None 6 3 Human 9.1 pKi = 9.1 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 326 1 0 3 4.2 CN1CCN(C2=Cc3cc(Cl)ccc3Oc3ccccc32)CC1 10.1021/jm00043a008
CHEMBL88464 204793 1 None 6 3 Human 9.1 pKi = 9.1 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 326 1 0 3 4.2 CN1CCN(C2=Cc3cc(Cl)ccc3Oc3ccccc32)CC1 10.1021/jm00043a008
3303 2213 41 None 1 15 Human 9.0 pKi = 9.0 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm990277d
5311200 2213 41 None 1 15 Human 9.0 pKi = 9.0 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm990277d
CHEMBL267014 2213 41 None 1 15 Human 9.0 pKi = 9.0 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm990277d
3303 2213 41 None 1 15 Human 9.0 pKi = 9.0 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00252-2
5311200 2213 41 None 1 15 Human 9.0 pKi = 9.0 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00252-2
CHEMBL267014 2213 41 None 1 15 Human 9.0 pKi = 9.0 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00252-2
44400553 70435 0 None 3 5 Human 9.0 pKi = 9.0 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
CHEMBL195083 70435 0 None 3 5 Human 9.0 pKi = 9.0 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
49788941 18090 0 None - 1 Rat 9.0 pKi = 9.0 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 353 5 1 5 1.6 N#Cc1cccnc1N1CCN(CCNC(=O)c2ccc(F)cc2)CC1 10.1021/jm100925m
CHEMBL1270423 18090 0 None - 1 Rat 9.0 pKi = 9.0 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 353 5 1 5 1.6 N#Cc1cccnc1N1CCN(CCNC(=O)c2ccc(F)cc2)CC1 10.1021/jm100925m
11689612 79429 0 None 436 4 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 388 5 0 7 2.9 COc1ccccc1N1CCN(Cc2cn3c(-n4cccn4)cccc3n2)CC1 10.1021/jm060166w
CHEMBL212160 79429 0 None 436 4 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 388 5 0 7 2.9 COc1ccccc1N1CCN(Cc2cn3c(-n4cccn4)cccc3n2)CC1 10.1021/jm060166w
10247720 12943 0 None 2 5 Human 9.0 pKi = 9.0 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; High binding affinityIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; High binding affinity
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL1190042 12943 0 None 2 5 Human 9.0 pKi = 9.0 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; High binding affinityIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; High binding affinity
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL540039 12943 0 None 2 5 Human 9.0 pKi = 9.0 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; High binding affinityIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; High binding affinity
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
10447709 21086 1 None 245 3 Human 9.0 pKi = 9.0 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 303 9 1 3 3.6 Cc1ccc(OCCNCCCOc2ccc(F)cc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL131357 21086 1 None 245 3 Human 9.0 pKi = 9.0 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 303 9 1 3 3.6 Cc1ccc(OCCNCCCOc2ccc(F)cc2)cc1 10.1016/j.bmcl.2005.02.012
76325150 105941 0 None 5 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
CHEMBL3115575 105941 0 None 5 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
CHEMBL3139554 105941 0 None 5 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
10248715 167314 0 None - 1 Human 9.0 pKi = 9.0 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 372 4 1 5 4.3 Cc1c(-c2ccccc2)nc(O)n1C1CCN(Cc2cccc(C#N)c2)CC1 10.1021/jm991029k
CHEMBL431095 167314 0 None - 1 Human 9.0 pKi = 9.0 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 372 4 1 5 4.3 Cc1c(-c2ccccc2)nc(O)n1C1CCN(Cc2cccc(C#N)c2)CC1 10.1021/jm991029k
10447709 21086 1 None 245 3 Human 9.0 pKi = 9.0 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 303 9 1 3 3.6 Cc1ccc(OCCNCCCOc2ccc(F)cc2)cc1 10.1021/jm970422s
CHEMBL131357 21086 1 None 245 3 Human 9.0 pKi = 9.0 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 303 9 1 3 3.6 Cc1ccc(OCCNCCCOc2ccc(F)cc2)cc1 10.1021/jm970422s
76325150 105941 0 None 5 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
CHEMBL3115575 105941 0 None 5 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
CHEMBL3139554 105941 0 None 5 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
10236758 115272 3 None 208 13 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL3354065 115272 3 None 208 13 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.2c00840
168268756 192162 0 None 1737 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5171439 192162 0 None 1737 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5221187 192162 0 None 1737 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
10236758 115272 3 None 208 13 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL3354065 115272 3 None 208 13 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
11516033 138588 5 None 1023 6 Human 9.0 pKi = 9 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
ChEMBL 360 3 0 4 4.0 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1Cl 10.1016/j.ejmech.2019.111569
CHEMBL378680 138588 5 None 1023 6 Human 9.0 pKi = 9 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
ChEMBL 360 3 0 4 4.0 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1Cl 10.1016/j.ejmech.2019.111569
122180954 121255 0 None 1 3 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 368 7 1 3 4.5 CCCN(CCNC(=O)/N=N/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3589575 121255 0 None 1 3 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 368 7 1 3 4.5 CCCN(CCNC(=O)/N=N/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
11575799 77775 0 None 1000 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 438 3 0 4 4.7 Clc1ccc(N2CCN(Cc3cn4cc(Br)ccc4n3)CC2)cc1Cl 10.1021/jm060166w
CHEMBL210341 77775 0 None 1000 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 438 3 0 4 4.7 Clc1ccc(N2CCN(Cc3cn4cc(Br)ccc4n3)CC2)cc1Cl 10.1021/jm060166w
11661609 79283 0 None 190 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 414 4 0 5 3.7 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(Br)c3n2)CC1 10.1021/jm060166w
CHEMBL211539 79283 0 None 190 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 414 4 0 5 3.7 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(Br)c3n2)CC1 10.1021/jm060166w
9951735 203544 0 None 8 3 Human 9.0 pKi = 9 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 378 4 1 4 4.8 Nc1nc(-c2ccc(Cl)cc2)cc(C2CCN(Cc3ccccc3)CC2)n1 10.1021/jm970111h
CHEMBL78923 203544 0 None 8 3 Human 9.0 pKi = 9 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 378 4 1 4 4.8 Nc1nc(-c2ccc(Cl)cc2)cc(C2CCN(Cc3ccccc3)CC2)n1 10.1021/jm970111h
10594242 205021 0 None 7 3 Human 9.0 pKi = 9 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 353 4 1 5 4.5 Cc1c(-c2cccs2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL90005 205021 0 None 7 3 Human 9.0 pKi = 9 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 353 4 1 5 4.5 Cc1c(-c2cccs2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
13014692 203213 1 None -1 4 Human 9.0 pKi = 9 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 324 1 0 2 4.0 CN1CCN(C2=Cc3ccccc3Cc3ccc(Cl)cc32)CC1 10.1021/jm00043a008
CHEMBL7617 203213 1 None -1 4 Human 9.0 pKi = 9 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 324 1 0 2 4.0 CN1CCN(C2=Cc3ccccc3Cc3ccc(Cl)cc32)CC1 10.1021/jm00043a008
1353 1880 85 None -3 85 Human 9.0 pKi = 9 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960268u
3559 1880 85 None -3 85 Human 9.0 pKi = 9 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960268u
86 1880 85 None -3 85 Human 9.0 pKi = 9 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960268u
CHEMBL54 1880 85 None -3 85 Human 9.0 pKi = 9 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960268u
DB00502 1880 85 None -3 85 Human 9.0 pKi = 9 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960268u
10314824 35153 1 None 8511 5 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(F)cc4)CC3)cc2c1 10.1021/jm0009989
CHEMBL143761 35153 1 None 8511 5 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(F)cc4)CC3)cc2c1 10.1021/jm0009989
44412182 76913 0 None 54 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 332 4 0 4 3.5 Cc1nn(-c2ccccc2)cc1CN1CCN(c2ccccc2)CC1 10.1016/j.bmcl.2006.02.075
CHEMBL208018 76913 0 None 54 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 332 4 0 4 3.5 Cc1nn(-c2ccccc2)cc1CN1CCN(c2ccccc2)CC1 10.1016/j.bmcl.2006.02.075
10403608 77798 6 None 50 6 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 318 4 0 4 3.2 c1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL210405 77798 6 None 50 6 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 318 4 0 4 3.2 c1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
44412182 76913 0 None 54 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 332 4 0 4 3.5 Cc1nn(-c2ccccc2)cc1CN1CCN(c2ccccc2)CC1 10.1021/jm0611152
CHEMBL208018 76913 0 None 54 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 332 4 0 4 3.5 Cc1nn(-c2ccccc2)cc1CN1CCN(c2ccccc2)CC1 10.1021/jm0611152
10403608 77798 6 None 50 6 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 318 4 0 4 3.2 c1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1021/jm0611152
CHEMBL210405 77798 6 None 50 6 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 318 4 0 4 3.2 c1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1021/jm0611152
10403608 77798 6 None 50 6 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 318 4 0 4 3.2 c1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmc.2013.01.065
CHEMBL210405 77798 6 None 50 6 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 318 4 0 4 3.2 c1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmc.2013.01.065
10314824 35153 1 None 8511 5 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(F)cc4)CC3)cc2c1 10.1021/jm060166w
CHEMBL143761 35153 1 None 8511 5 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(F)cc4)CC3)cc2c1 10.1021/jm060166w
1353 1880 85 None -3 85 Human 9.0 pKi = 9 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991138z
3559 1880 85 None -3 85 Human 9.0 pKi = 9 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991138z
86 1880 85 None -3 85 Human 9.0 pKi = 9 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991138z
CHEMBL54 1880 85 None -3 85 Human 9.0 pKi = 9 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991138z
DB00502 1880 85 None -3 85 Human 9.0 pKi = 9 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991138z
102505294 192397 0 None 309 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5204418 192397 0 None 309 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222691 192397 0 None 309 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2)CC1 10.1021/acs.jmedchem.2c00840
168289100 192349 0 None 316 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 374 5 0 4 3.1 N#Cc1ccccc1N1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5191299 192349 0 None 316 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 374 5 0 4 3.1 N#Cc1ccccc1N1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222419 192349 0 None 316 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 374 5 0 4 3.1 N#Cc1ccccc1N1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.2c00840
10732925 114718 1 None 269 3 Human 9.0 pKi = 9.0 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCNCCCOc2ccccc2C)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL334545 114718 1 None 269 3 Human 9.0 pKi = 9.0 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCNCCCOc2ccccc2C)cc1 10.1016/j.bmcl.2005.02.012
90644061 111541 0 None 177 5 Rat 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 329 6 0 4 3.1 Cc1ccc(N2CCN(CCCOc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289646 111541 0 None 177 5 Rat 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 329 6 0 4 3.1 Cc1ccc(N2CCN(CCCOc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
10666315 96141 0 None 47 3 Human 9.0 pKi = 9.0 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 361 4 1 4 4.7 Cc1ccc(-c2nc(O)n(C3CCN(Cc4ccccc4)CC3)c2C)cc1 10.1021/jm991029k
CHEMBL263162 96141 0 None 47 3 Human 9.0 pKi = 9.0 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 361 4 1 4 4.7 Cc1ccc(-c2nc(O)n(C3CCN(Cc4ccccc4)CC3)c2C)cc1 10.1021/jm991029k
10809899 205018 0 None 34 3 Human 9.0 pKi = 9.0 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 381 4 1 4 5.1 Cc1c(-c2ccccc2Cl)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL89971 205018 0 None 34 3 Human 9.0 pKi = 9.0 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 381 4 1 4 5.1 Cc1c(-c2ccccc2Cl)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
511482 96803 5 None 53 5 Human 9.0 pKi = 9.0 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 325 3 1 2 4.1 Clc1ccc(N2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL268799 96803 5 None 53 5 Human 9.0 pKi = 9.0 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 325 3 1 2 4.1 Clc1ccc(N2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
10570479 111782 0 None -1 3 Human 9.0 pKi = 9.0 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 359 5 2 4 2.9 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
CHEMBL329106 111782 0 None -1 3 Human 9.0 pKi = 9.0 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 359 5 2 4 2.9 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
10732925 114718 1 None 269 3 Human 9.0 pKi = 9.0 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCNCCCOc2ccccc2C)cc1 10.1021/jm970422s
CHEMBL334545 114718 1 None 269 3 Human 9.0 pKi = 9.0 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCNCCCOc2ccccc2C)cc1 10.1021/jm970422s
10406796 99540 9 None -19 5 Human 9.0 pKi = 9.0 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 369 7 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm020952a
CHEMBL286725 99540 9 None -19 5 Human 9.0 pKi = 9.0 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 369 7 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm020952a
9805944 55934 31 None -1 9 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptorDisplacement of [3H]N-methylspiperone from dopamine D4 receptor
ChEMBL 462 7 2 3 4.7 CNC(=O)C(CCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm800510m
CHEMBL1627 55934 31 None -1 9 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptorDisplacement of [3H]N-methylspiperone from dopamine D4 receptor
ChEMBL 462 7 2 3 4.7 CNC(=O)C(CCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm800510m
90644061 111541 0 None 177 5 Rat 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 329 6 0 4 3.1 Cc1ccc(N2CCN(CCCOc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289646 111541 0 None 177 5 Rat 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 329 6 0 4 3.1 Cc1ccc(N2CCN(CCCOc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
9797495 68662 0 None 3548 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 328 3 0 4 2.9 Fc1ccc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)cc1 10.1021/jm200762g
CHEMBL1923292 68662 0 None 3548 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 328 3 0 4 2.9 Fc1ccc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)cc1 10.1021/jm200762g
44340227 110152 0 None 16 4 Human 8.9 pKi = 8.9 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 486 5 1 3 4.5 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(I)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL325772 110152 0 None 16 4 Human 8.9 pKi = 8.9 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 486 5 1 3 4.5 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(I)c2ccccc12 10.1016/s0960-894x(03)00678-4
10619737 200712 0 None 239 3 Human 8.9 pKi = 8.9 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 379 5 1 2 5.5 Cc1c(C2CCN(CCc3ccccc3)CC2)n[nH]c1-c1ccc(Cl)cc1 10.1021/jm970111h
CHEMBL61079 200712 0 None 239 3 Human 8.9 pKi = 8.9 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 379 5 1 2 5.5 Cc1c(C2CCN(CCc3ccccc3)CC2)n[nH]c1-c1ccc(Cl)cc1 10.1021/jm970111h
681 1437 65 None -2 38 Human 8.9 pKi = 8.9 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
940 1437 65 None -2 38 Human 8.9 pKi = 8.9 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
947 1437 65 None -2 38 Human 8.9 pKi = 8.9 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
CHEMBL59 1437 65 None -2 38 Human 8.9 pKi = 8.9 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
DB00988 1437 65 None -2 38 Human 8.9 pKi = 8.9 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
10494394 167984 1 None 158 3 Human 8.9 pKi = 8.9 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCNCCCOc2cccc(C)c2)cc1 10.1021/jm970422s
CHEMBL435598 167984 1 None 158 3 Human 8.9 pKi = 8.9 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCNCCCOc2cccc(C)c2)cc1 10.1021/jm970422s
137651936 156850 0 None -1 5 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4078348 156850 0 None -1 5 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
21219176 95844 0 None 12 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 356 4 0 4 4.6 Cc1nn(C2CCN(Cc3cccc(C#N)c3)CC2)cc1-c1ccccc1 10.1016/s0960-894x(99)00169-9
CHEMBL26120 95844 0 None 12 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 356 4 0 4 4.6 Cc1nn(C2CCN(Cc3cccc(C#N)c3)CC2)cc1-c1ccccc1 10.1016/s0960-894x(99)00169-9
10619737 200712 0 None 239 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 379 5 1 2 5.5 Cc1c(C2CCN(CCc3ccccc3)CC2)n[nH]c1-c1ccc(Cl)cc1 10.1021/jm960072u
CHEMBL61079 200712 0 None 239 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 379 5 1 2 5.5 Cc1c(C2CCN(CCc3ccccc3)CC2)n[nH]c1-c1ccc(Cl)cc1 10.1021/jm960072u
45273045 194702 0 None 199 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cc3ccccn3n2)CC1 10.1021/jm900690y
CHEMBL562620 194702 0 None 199 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cc3ccccn3n2)CC1 10.1021/jm900690y
10427977 54180 0 None 660 4 Human 8.9 pKi = 8.9 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 350 3 0 4 3.3 C#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
CHEMBL160952 54180 0 None 660 4 Human 8.9 pKi = 8.9 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 350 3 0 4 3.3 C#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
10494394 167984 1 None 158 3 Human 8.9 pKi = 8.9 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCNCCCOc2cccc(C)c2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL435598 167984 1 None 158 3 Human 8.9 pKi = 8.9 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCNCCCOc2cccc(C)c2)cc1 10.1016/j.bmcl.2005.02.012
10088259 101443 3 None 134 3 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 334 4 1 4 2.4 Cc1ccc(C(=O)NCN2CCN(c3ccccc3C#N)CC2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL300956 101443 3 None 134 3 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 334 4 1 4 2.4 Cc1ccc(C(=O)NCN2CCN(c3ccccc3C#N)CC2)cc1 10.1016/j.bmcl.2005.02.012
10427977 54180 0 None 660 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 350 3 0 4 3.3 C#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1021/jm0611152
CHEMBL160952 54180 0 None 660 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 350 3 0 4 3.3 C#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1021/jm0611152
137640201 156419 2 None 177 13 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4072818 156419 2 None 177 13 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
9905249 99440 0 None 2 3 Human 8.9 pKi = 8.9 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 322 4 1 4 2.9 COc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(99)00025-6
CHEMBL28607 99440 0 None 2 3 Human 8.9 pKi = 8.9 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 322 4 1 4 2.9 COc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(99)00025-6
10762432 205680 0 None 46 3 Human 8.9 pKi = 8.9 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 381 4 1 4 5.1 Cc1c(-c2ccccc2)nc(O)n1C1CCN(Cc2ccc(Cl)cc2)CC1 10.1021/jm991029k
CHEMBL93969 205680 0 None 46 3 Human 8.9 pKi = 8.9 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 381 4 1 4 5.1 Cc1c(-c2ccccc2)nc(O)n1C1CCN(Cc2ccc(Cl)cc2)CC1 10.1021/jm991029k
10740483 205402 0 None 3 3 Human 8.9 pKi = 8.9 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 413 7 2 4 3.5 C=CC(=O)Nc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)C2)cc1Cl 10.1021/jm9601720
CHEMBL92192 205402 0 None 3 3 Human 8.9 pKi = 8.9 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 413 7 2 4 3.5 C=CC(=O)Nc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)C2)cc1Cl 10.1021/jm9601720
44454709 97069 0 None 72 5 Human 8.9 pKi = 8.9 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 404 9 0 6 3.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)c(OCCF)cc1OC 10.1016/j.bmcl.2007.12.026
CHEMBL270406 97069 0 None 72 5 Human 8.9 pKi = 8.9 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 404 9 0 6 3.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)c(OCCF)cc1OC 10.1016/j.bmcl.2007.12.026
10450375 99031 0 None -1 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 347 5 0 4 3.8 COc1ccccc1N1CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1021/jm00025a013
CHEMBL28321 99031 0 None -1 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 347 5 0 4 3.8 COc1ccccc1N1CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1021/jm00025a013
16094698 137343 4 None 20 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 338 5 1 3 3.6 COc1ccccc1C1CCN(CNC(=O)c2cccc(C)c2)CC1 10.1021/jm060662k
CHEMBL376092 137343 4 None 20 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 338 5 1 3 3.6 COc1ccccc1C1CCN(CNC(=O)c2cccc(C)c2)CC1 10.1021/jm060662k
25256816 181026 0 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 407 7 0 4 3.7 COc1ccccc1N1CCN(CCCCN2CCCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL477206 181026 0 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 407 7 0 4 3.7 COc1ccccc1N1CCN(CCCCN2CCCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
10450375 99031 0 None -1 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 347 5 0 4 3.8 COc1ccccc1N1CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1016/S0960-894X(97)00218-7
CHEMBL28321 99031 0 None -1 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 347 5 0 4 3.8 COc1ccccc1N1CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1016/S0960-894X(97)00218-7
10406796 99540 9 None -19 5 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 369 7 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/S0960-894X(97)00218-7
CHEMBL286725 99540 9 None -19 5 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 369 7 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/S0960-894X(97)00218-7
25072002 155573 0 None -6 5 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C#N)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4063235 155573 0 None -6 5 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C#N)c3c2)CC1 10.1021/acs.jmedchem.6b01857
11696910 77394 0 None 281 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 395 3 0 5 4.0 Clc1ccc2nc(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)cn2n1 10.1021/jm060166w
CHEMBL209034 77394 0 None 281 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 395 3 0 5 4.0 Clc1ccc2nc(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)cn2n1 10.1021/jm060166w
11631892 77757 0 None 2630 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 361 4 0 6 2.8 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(C#N)c3n2)CC1 10.1021/jm060166w
CHEMBL210283 77757 0 None 2630 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 361 4 0 6 2.8 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(C#N)c3n2)CC1 10.1021/jm060166w
10359942 102463 4 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 340 3 0 3 5.2 Clc1ccc(CN2CC=C(c3nc4ccccc4s3)CC2)cc1 10.1016/S0960-894X(97)00402-2
CHEMBL306265 102463 4 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 340 3 0 3 5.2 Clc1ccc(CN2CC=C(c3nc4ccccc4s3)CC2)cc1 10.1016/S0960-894X(97)00402-2
168294165 192410 0 None 204 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 363 5 0 3 3.5 Cc1ccccc1N1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5209074 192410 0 None 204 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 363 5 0 3 3.5 Cc1ccccc1N1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222773 192410 0 None 204 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 363 5 0 3 3.5 Cc1ccccc1N1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.2c00840
137645938 157041 0 None 204 8 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 342 8 0 2 4.6 CCCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4080675 157041 0 None 204 8 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 342 8 0 2 4.6 CCCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
9863333 202662 0 None 1 10 Rat 8.9 pKi = 8.9 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 352 5 0 4 3.5 COc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/jm960084f
CHEMBL71724 202662 0 None 1 10 Rat 8.9 pKi = 8.9 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 352 5 0 4 3.5 COc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/jm960084f
2470 3596 46 None -20 59 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D4 receptor (unknown origin)Binding affinity to dopamine D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmc.2016.06.011
3300 3596 46 None -20 59 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D4 receptor (unknown origin)Binding affinity to dopamine D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmc.2016.06.011
5265 3596 46 None -20 59 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D4 receptor (unknown origin)Binding affinity to dopamine D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmc.2016.06.011
99 3596 46 None -20 59 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D4 receptor (unknown origin)Binding affinity to dopamine D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmc.2016.06.011
CHEMBL267930 3596 46 None -20 59 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D4 receptor (unknown origin)Binding affinity to dopamine D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmc.2016.06.011
10615787 116263 0 None 67 3 Human 8.9 pKi = 8.9 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 321 9 1 3 4.5 Clc1ccc(OCCNCCCSc2ccccc2)cc1 10.1021/jm970422s
CHEMBL337627 116263 0 None 67 3 Human 8.9 pKi = 8.9 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 321 9 1 3 4.5 Clc1ccc(OCCNCCCSc2ccccc2)cc1 10.1021/jm970422s
16094666 81315 2 None 52 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL216393 81315 2 None 52 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/acs.jmedchem.9b00231
10498094 32102 1 None 1047 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4Cl)CC3)cc2c1 10.1021/jm0009989
CHEMBL141035 32102 1 None 1047 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4Cl)CC3)cc2c1 10.1021/jm0009989
122181333 121360 0 None 10 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 366 8 1 2 3.8 CCCN(CCNC(=O)/C=C/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3590084 121360 0 None 10 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 366 8 1 2 3.8 CCCN(CCNC(=O)/C=C/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
11516033 138588 5 None 1023 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 360 3 0 4 4.0 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1Cl 10.1021/jm060166w
CHEMBL378680 138588 5 None 1023 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 360 3 0 4 4.0 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1Cl 10.1021/jm060166w
1353 1880 85 None -3 85 Human 8.9 pKi = 8.9 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2004.07.068
3559 1880 85 None -3 85 Human 8.9 pKi = 8.9 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2004.07.068
86 1880 85 None -3 85 Human 8.9 pKi = 8.9 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2004.07.068
CHEMBL54 1880 85 None -3 85 Human 8.9 pKi = 8.9 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2004.07.068
DB00502 1880 85 None -3 85 Human 8.9 pKi = 8.9 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2004.07.068
10314060 168035 0 None 72 7 Rat 8.9 pKi = 8.9 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 322 4 1 4 2.9 COc1ccccc1N1CCN(Cc2c[nH]c3ncccc23)CC1 10.1016/s0960-894x(01)00241-4
CHEMBL435949 168035 0 None 72 7 Rat 8.9 pKi = 8.9 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 322 4 1 4 2.9 COc1ccccc1N1CCN(Cc2c[nH]c3ncccc23)CC1 10.1016/s0960-894x(01)00241-4
1353 1880 85 None -3 85 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.1c00611
3559 1880 85 None -3 85 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.1c00611
86 1880 85 None -3 85 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.1c00611
CHEMBL54 1880 85 None -3 85 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.1c00611
DB00502 1880 85 None -3 85 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.1c00611
168285556 192315 0 None 2454 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting methodDisplacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5196870 192315 0 None 2454 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting methodDisplacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222200 192315 0 None 2454 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting methodDisplacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
9883587 111067 0 None 39 3 Human 8.8 pKi = 8.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 321 3 0 4 3.4 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccccc1)CC3 10.1021/jm970170v
CHEMBL328054 111067 0 None 39 3 Human 8.8 pKi = 8.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 321 3 0 4 3.4 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccccc1)CC3 10.1021/jm970170v
44394743 122585 0 None 39 3 Human 8.8 pKi = 8.8 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@H]1CCN(Cc2ccccc2)C1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2004.07.045
CHEMBL361035 122585 0 None 39 3 Human 8.8 pKi = 8.8 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@H]1CCN(Cc2ccccc2)C1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2004.07.045
10595908 203547 0 None 22 3 Human 8.8 pKi = 8.8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 379 5 1 2 5.7 CCc1c(C2CCN(Cc3ccccc3)CC2)n[nH]c1-c1ccc(Cl)cc1 10.1021/jm970111h
CHEMBL78933 203547 0 None 22 3 Human 8.8 pKi = 8.8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 379 5 1 2 5.7 CCc1c(C2CCN(Cc3ccccc3)CC2)n[nH]c1-c1ccc(Cl)cc1 10.1021/jm970111h
10716772 205555 0 None 3 3 Human 8.8 pKi = 8.8 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 415 7 2 4 3.7 CCC(=O)Nc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)C2)cc1Cl 10.1021/jm9601720
CHEMBL93198 205555 0 None 3 3 Human 8.8 pKi = 8.8 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 415 7 2 4 3.7 CCC(=O)Nc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)C2)cc1Cl 10.1021/jm9601720
12765746 101810 3 None -14 10 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 344 1 0 3 4.3 CN1CCN([C@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm020938y
CHEMBL303313 101810 3 None -14 10 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 344 1 0 3 4.3 CN1CCN([C@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm020938y
57403525 69811 0 None 6 10 Rat 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 361 6 1 2 4.8 OC1(c2ccc(Cl)cc2)CCN(CCCCc2ccc(F)cc2)CC1 10.1016/j.bmc.2011.12.019
57403525 69811 0 None 6 10 Rat 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 361 6 1 2 4.8 OC1(c2ccc(Cl)cc2)CCN(CCCCc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
CHEMBL1940402 69811 0 None 6 10 Rat 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 361 6 1 2 4.8 OC1(c2ccc(Cl)cc2)CCN(CCCCc2ccc(F)cc2)CC1 10.1016/j.bmc.2011.12.019
CHEMBL1940402 69811 0 None 6 10 Rat 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 361 6 1 2 4.8 OC1(c2ccc(Cl)cc2)CCN(CCCCc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
44394743 122585 0 None 39 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@H]1CCN(Cc2ccccc2)C1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2005.08.051
CHEMBL361035 122585 0 None 39 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@H]1CCN(Cc2ccccc2)C1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2005.08.051
25093832 155339 0 None -3 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4060461 155339 0 None -3 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
137660837 158534 0 None -2 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4097330 158534 0 None -2 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
71456046 83661 0 None 114 7 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 389 6 0 4 4.2 COc1ccccc1N1CCN(Cc2cc(CN(C)C)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207637 83661 0 None 114 7 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 389 6 0 4 4.2 COc1ccccc1N1CCN(Cc2cc(CN(C)C)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
44381216 119826 0 None 8511 4 Human 8.8 pKi = 8.8 Binding
In vitro ability to displace [3H]spiperone from the cloned human dopamine D4 receptor expressed in CHO cellsIn vitro ability to displace [3H]spiperone from the cloned human dopamine D4 receptor expressed in CHO cells
ChEMBL 334 4 1 4 2.6 c1ccc(C2=NCC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(03)00004-0
CHEMBL352925 119826 0 None 8511 4 Human 8.8 pKi = 8.8 Binding
In vitro ability to displace [3H]spiperone from the cloned human dopamine D4 receptor expressed in CHO cellsIn vitro ability to displace [3H]spiperone from the cloned human dopamine D4 receptor expressed in CHO cells
ChEMBL 334 4 1 4 2.6 c1ccc(C2=NCC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(03)00004-0
44371997 49660 0 None 10000 4 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 364 3 0 4 3.6 C#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)c(C)nn12 10.1016/s0960-894x(01)00814-9
CHEMBL156851 49660 0 None 10000 4 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 364 3 0 4 3.6 C#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)c(C)nn12 10.1016/s0960-894x(01)00814-9
11725531 53769 1 None 1445 5 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 351 3 0 5 3.2 N#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
CHEMBL160626 53769 1 None 1445 5 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 351 3 0 5 3.2 N#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
11301655 198 31 None 245 4 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity tested on HEK293 cells co-transfected with human D4.4 receptor using [3H]spiperone as a radioligand in FLIPR assayIn vitro binding affinity tested on HEK293 cells co-transfected with human D4.4 receptor using [3H]spiperone as a radioligand in FLIPR assay
ChEMBL 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 10.1021/jm030505a
8441 198 31 None 245 4 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity tested on HEK293 cells co-transfected with human D4.4 receptor using [3H]spiperone as a radioligand in FLIPR assayIn vitro binding affinity tested on HEK293 cells co-transfected with human D4.4 receptor using [3H]spiperone as a radioligand in FLIPR assay
ChEMBL 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 10.1021/jm030505a
CHEMBL127257 198 31 None 245 4 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity tested on HEK293 cells co-transfected with human D4.4 receptor using [3H]spiperone as a radioligand in FLIPR assayIn vitro binding affinity tested on HEK293 cells co-transfected with human D4.4 receptor using [3H]spiperone as a radioligand in FLIPR assay
ChEMBL 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 10.1021/jm030505a
11301655 198 31 None 245 4 Human 8.8 pKi = 8.8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 10.1021/acs.jmedchem.7b00151
8441 198 31 None 245 4 Human 8.8 pKi = 8.8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 10.1021/acs.jmedchem.7b00151
CHEMBL127257 198 31 None 245 4 Human 8.8 pKi = 8.8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 10.1021/acs.jmedchem.7b00151
49788869 18040 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 365 6 1 6 1.5 COc1cccc(C(=O)NCCN2CCN(c3ncccc3C#N)CC2)c1 10.1021/jm100925m
CHEMBL1270121 18040 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 365 6 1 6 1.5 COc1cccc(C(=O)NCCN2CCN(c3ncccc3C#N)CC2)c1 10.1021/jm100925m
127049060 140244 0 None 13 7 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 402 6 2 3 3.9 O=C1NCN(c2ccccc2)C12CCN(CCCCc1c[nH]c3ccccc13)CC2 10.1016/j.bmc.2016.06.011
CHEMBL3818478 140244 0 None 13 7 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 402 6 2 3 3.9 O=C1NCN(c2ccccc2)C12CCN(CCCCc1c[nH]c3ccccc13)CC2 10.1016/j.bmc.2016.06.011
76321554 105922 0 None 5 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
CHEMBL3115574 105922 0 None 5 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
CHEMBL3139450 105922 0 None 5 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
9954003 71356 18 None -3 9 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 422 5 2 4 3.8 C[C@H]1Oc2c(cccc2N2CCN(CCCc3c[nH]c4ccc(F)cc34)CC2)NC1=O 10.1021/jm070516u
CHEMBL196514 71356 18 None -3 9 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 422 5 2 4 3.8 C[C@H]1Oc2c(cccc2N2CCN(CCCc3c[nH]c4ccc(F)cc34)CC2)NC1=O 10.1021/jm070516u
1353 1880 85 None -3 85 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity for Dopamine receptor D4In vitro binding affinity for Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(01)00200-1
3559 1880 85 None -3 85 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity for Dopamine receptor D4In vitro binding affinity for Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(01)00200-1
86 1880 85 None -3 85 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity for Dopamine receptor D4In vitro binding affinity for Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(01)00200-1
CHEMBL54 1880 85 None -3 85 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity for Dopamine receptor D4In vitro binding affinity for Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(01)00200-1
DB00502 1880 85 None -3 85 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity for Dopamine receptor D4In vitro binding affinity for Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(01)00200-1
76321554 105922 0 None 5 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
CHEMBL3115574 105922 0 None 5 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
CHEMBL3139450 105922 0 None 5 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
44340084 9000 0 None 6 4 Human 8.8 pKi = 8.8 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 401 6 2 4 4.0 CNc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL109912 9000 0 None 6 4 Human 8.8 pKi = 8.8 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 401 6 2 4 4.0 CNc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
10618875 103745 0 None 125 3 Human 8.8 pKi = 8.8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 365 4 1 2 5.4 Cc1c(C2CCN(Cc3ccccc3)CC2)n[nH]c1-c1ccc(Cl)cc1 10.1021/jm970111h
CHEMBL309901 103745 0 None 125 3 Human 8.8 pKi = 8.8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 365 4 1 2 5.4 Cc1c(C2CCN(Cc3ccccc3)CC2)n[nH]c1-c1ccc(Cl)cc1 10.1021/jm970111h
9104271 202299 10 None 436 2 Human 8.8 pKi = 8.8 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 369 4 0 3 3.0 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccccc21 10.1016/s0960-894x(00)00421-2
CHEMBL69584 202299 10 None 436 2 Human 8.8 pKi = 8.8 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 369 4 0 3 3.0 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccccc21 10.1016/s0960-894x(00)00421-2
44454711 97070 0 None 36 5 Human 8.8 pKi = 8.8 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 344 7 0 4 3.4 COc1ccccc1N1CCN(Cc2cccc(OCCF)c2)CC1 10.1016/j.bmcl.2007.12.026
CHEMBL270408 97070 0 None 36 5 Human 8.8 pKi = 8.8 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 344 7 0 4 3.4 COc1ccccc1N1CCN(Cc2cccc(OCCF)c2)CC1 10.1016/j.bmcl.2007.12.026
511482 96803 5 None 53 5 Human 8.8 pKi = 8.8 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 325 3 1 2 4.1 Clc1ccc(N2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1021/jm9600712
CHEMBL268799 96803 5 None 53 5 Human 8.8 pKi = 8.8 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 325 3 1 2 4.1 Clc1ccc(N2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1021/jm9600712
9104271 202299 10 None 436 2 Human 8.8 pKi = 8.8 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 369 4 0 3 3.0 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccccc21 10.1016/s0960-894x(02)00655-8
CHEMBL69584 202299 10 None 436 2 Human 8.8 pKi = 8.8 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 369 4 0 3 3.0 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccccc21 10.1016/s0960-894x(02)00655-8
9104271 202299 10 None 436 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 369 4 0 3 3.0 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccccc21 10.1016/s0960-894x(02)01056-9
CHEMBL69584 202299 10 None 436 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 369 4 0 3 3.0 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccccc21 10.1016/s0960-894x(02)01056-9
10336039 118730 1 None 15 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 318 4 0 4 3.2 c1ccc(-n2ccc(CN3CCN(c4ccccn4)CC3)c2)cc1 10.1021/jm00025a013
CHEMBL343466 118730 1 None 15 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 318 4 0 4 3.2 c1ccc(-n2ccc(CN3CCN(c4ccccn4)CC3)c2)cc1 10.1021/jm00025a013
127049060 140244 0 None 13 7 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 402 6 2 3 3.9 O=C1NCN(c2ccccc2)C12CCN(CCCCc1c[nH]c3ccccc13)CC2 10.1016/j.bmc.2016.06.011
CHEMBL3818478 140244 0 None 13 7 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 402 6 2 3 3.9 O=C1NCN(c2ccccc2)C12CCN(CCCCc1c[nH]c3ccccc13)CC2 10.1016/j.bmc.2016.06.011
11682812 77835 0 None 239 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 402 5 0 7 3.2 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(-n4cccn4)c3n2)CC1 10.1021/jm060166w
CHEMBL210551 77835 0 None 239 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 402 5 0 7 3.2 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(-n4cccn4)c3n2)CC1 10.1021/jm060166w
11581237 138429 0 None 15 6 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 357 4 0 6 2.7 COc1ccccc1N1CCN(Cc2cn3nc(Cl)ccc3n2)CC1 10.1021/jm060166w
CHEMBL378515 138429 0 None 15 6 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 357 4 0 6 2.7 COc1ccccc1N1CCN(Cc2cn3nc(Cl)ccc3n2)CC1 10.1021/jm060166w
44376876 119667 0 None 27 2 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 322 4 0 3 3.7 c1ccc(OC[C@@H]2CC[C@H]3CN(c4ccccc4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL351611 119667 0 None 27 2 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 322 4 0 3 3.7 c1ccc(OC[C@@H]2CC[C@H]3CN(c4ccccc4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
155536720 171621 0 None 77 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 359 4 1 3 3.9 Cc1cccc(NC(=O)CN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4473652 171621 0 None 77 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 359 4 1 3 3.9 Cc1cccc(NC(=O)CN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/acs.jmedchem.9b00231
10690200 205400 0 None 169 3 Human 8.8 pKi = 8.8 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 365 4 1 4 4.5 Cc1c(-c2ccc(F)cc2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL92189 205400 0 None 169 3 Human 8.8 pKi = 8.8 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 365 4 1 4 4.5 Cc1c(-c2ccc(F)cc2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
44323978 104804 0 None 11 4 Human 8.8 pKi = 8.8 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 325 3 1 2 4.1 Clc1ccc2[nH]ccc2c1N1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(98)00474-0
CHEMBL311539 104804 0 None 11 4 Human 8.8 pKi = 8.8 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 325 3 1 2 4.1 Clc1ccc2[nH]ccc2c1N1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(98)00474-0
76316875 85460 0 None 18 3 Human 8.8 pKi = 8.8 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 321 3 1 0 3.4 Clc1ccc2[nH]ccc2c1-[n+]1cc[n+](Cc2ccccc2)cc1 10.1007/s00044-012-0055-5
CHEMBL2298810 85460 0 None 18 3 Human 8.8 pKi = 8.8 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 321 3 1 0 3.4 Clc1ccc2[nH]ccc2c1-[n+]1cc[n+](Cc2ccccc2)cc1 10.1007/s00044-012-0055-5
24882561 94897 0 None 58 5 Human 8.8 pKi = 8.8 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 408 8 0 5 4.0 COc1cc(CN2CCN(c3ccc(Cl)cc3)CC2)c(OCCF)cc1OC 10.1016/j.bmcl.2007.12.026
CHEMBL256637 94897 0 None 58 5 Human 8.8 pKi = 8.8 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 408 8 0 5 4.0 COc1cc(CN2CCN(c3ccc(Cl)cc3)CC2)c(OCCF)cc1OC 10.1016/j.bmcl.2007.12.026
155527714 170730 0 None 16 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 503 11 2 6 4.1 COc1ccc(N(Cc2ccccc2)NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1021/acs.jmedchem.9b01085
CHEMBL4460743 170730 0 None 16 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 503 11 2 6 4.1 COc1ccc(N(Cc2ccccc2)NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1021/acs.jmedchem.9b01085
11726532 96578 0 None -2 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 368 8 0 5 3.5 COc1cccc(C(=O)CCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/S0960-894X(97)00218-7
CHEMBL26677 96578 0 None -2 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 368 8 0 5 3.5 COc1cccc(C(=O)CCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/S0960-894X(97)00218-7
44376569 57140 0 None 19 2 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 324 4 0 5 2.5 c1ccc(OC[C@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL165504 57140 0 None 19 2 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 324 4 0 5 2.5 c1ccc(OC[C@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
44376918 119507 0 None 109 2 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 323 4 0 4 3.1 c1ccc(OC[C@@H]2CC[C@H]3CN(c4ccccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL350160 119507 0 None 109 2 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 323 4 0 4 3.1 c1ccc(OC[C@@H]2CC[C@H]3CN(c4ccccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
42266988 18061 2 None - 1 Rat 8.8 pKi = 8.8 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 361 5 1 3 3.0 O=C(NCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1021/jm100925m
CHEMBL1270227 18061 2 None - 1 Rat 8.8 pKi = 8.8 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 361 5 1 3 3.0 O=C(NCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1021/jm100925m
168268695 192172 0 None 446 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 363 5 0 3 3.5 Cc1cccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)c1 10.1021/acs.jmedchem.2c00840
CHEMBL5170580 192172 0 None 446 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 363 5 0 3 3.5 Cc1cccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)c1 10.1021/acs.jmedchem.2c00840
CHEMBL5221253 192172 0 None 446 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 363 5 0 3 3.5 Cc1cccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)c1 10.1021/acs.jmedchem.2c00840
21462964 47921 0 None 602 3 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 319 5 1 2 4.4 c1ccc(CCC2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(99)00025-6
CHEMBL155207 47921 0 None 602 3 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 319 5 1 2 4.4 c1ccc(CCC2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(99)00025-6
11792163 41831 0 None 316 2 Human 8.7 pKi = 8.7 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 350 3 1 3 4.0 Cc1ccc(C2CCN(Cc3ccc4c(c3)NC(=O)CO4)CC2)cc1C 10.1021/jm990277d
CHEMBL149596 41831 0 None 316 2 Human 8.7 pKi = 8.7 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 350 3 1 3 4.0 Cc1ccc(C2CCN(Cc3ccc4c(c3)NC(=O)CO4)CC2)cc1C 10.1021/jm990277d
44454735 94873 0 None 169 5 Human 8.7 pKi = 8.7 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 374 8 0 5 3.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCF 10.1016/j.bmcl.2007.12.026
CHEMBL256492 94873 0 None 169 5 Human 8.7 pKi = 8.7 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 374 8 0 5 3.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCF 10.1016/j.bmcl.2007.12.026
10643697 120610 1 None 10 4 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 383 8 1 5 2.6 COc1cccc(C(=O)NCCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm020952a
CHEMBL357448 120610 1 None 10 4 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 383 8 1 5 2.6 COc1cccc(C(=O)NCCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm020952a
44209472 69829 2 None 1 11 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 315 6 0 4 2.8 Fc1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940420 69829 2 None 1 11 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 315 6 0 4 2.8 Fc1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
44209472 69829 2 None 1 11 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 315 6 0 4 2.8 Fc1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940420 69829 2 None 1 11 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 315 6 0 4 2.8 Fc1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
2 3210 19 None -2 28 Human 8.7 pKi = 8.7 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0503805
54562 3210 19 None -2 28 Human 8.7 pKi = 8.7 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0503805
CHEMBL240773 3210 19 None -2 28 Human 8.7 pKi = 8.7 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0503805
2 3210 19 None -2 28 Human 8.7 pKi = 8.7 Binding
High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsHigh inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm049269+
54562 3210 19 None -2 28 Human 8.7 pKi = 8.7 Binding
High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsHigh inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm049269+
CHEMBL240773 3210 19 None -2 28 Human 8.7 pKi = 8.7 Binding
High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsHigh inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm049269+
2653640 65887 12 None - 1 Human 8.7 pKi = 8.7 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 339 5 1 4 2.8 COc1ccccc1N1CCN(CC(=O)Nc2cccc(C)c2)CC1 10.1016/j.bmcl.2004.07.068
CHEMBL184486 65887 12 None - 1 Human 8.7 pKi = 8.7 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 339 5 1 4 2.8 COc1ccccc1N1CCN(CC(=O)Nc2cccc(C)c2)CC1 10.1016/j.bmcl.2004.07.068
2 3210 19 None -2 28 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(03)00004-0
54562 3210 19 None -2 28 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(03)00004-0
CHEMBL240773 3210 19 None -2 28 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(03)00004-0
2 3210 19 None -2 28 Human 8.7 pKi = 8.7 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; high binding affinityIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; high binding affinity
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(01)00484-x
54562 3210 19 None -2 28 Human 8.7 pKi = 8.7 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; high binding affinityIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; high binding affinity
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(01)00484-x
CHEMBL240773 3210 19 None -2 28 Human 8.7 pKi = 8.7 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; high binding affinityIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; high binding affinity
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(01)00484-x
4797946 169856 8 None 165 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 310 4 1 4 2.2 Cc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4448320 169856 8 None 165 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 310 4 1 4 2.2 Cc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
10837488 112155 0 None 2 3 Human 8.7 pKi = 8.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 455 6 2 4 3.9 COc1cc(NC(=O)C(F)(F)F)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
CHEMBL330318 112155 0 None 2 3 Human 8.7 pKi = 8.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 455 6 2 4 3.9 COc1cc(NC(=O)C(F)(F)F)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
22065971 120584 1 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 292 3 1 3 2.9 c1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1021/jm0002432
CHEMBL357182 120584 1 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 292 3 1 3 2.9 c1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1021/jm0002432
25256814 181030 0 None 1 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 393 7 0 4 3.3 COc1ccccc1N1CCN(CCCCN2CCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL477250 181030 0 None 1 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 393 7 0 4 3.3 COc1ccccc1N1CCN(CCCCN2CCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
71457844 83662 0 None 22 7 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 429 6 0 4 5.1 COc1ccccc1N1CCN(Cc2cc(CN3CCCCC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207638 83662 0 None 22 7 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 429 6 0 4 5.1 COc1ccccc1N1CCN(Cc2cc(CN3CCCCC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
1353 1880 85 None -3 85 Human 8.7 pKi = 8.7 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2004.07.068
3559 1880 85 None -3 85 Human 8.7 pKi = 8.7 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2004.07.068
86 1880 85 None -3 85 Human 8.7 pKi = 8.7 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2004.07.068
CHEMBL54 1880 85 None -3 85 Human 8.7 pKi = 8.7 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2004.07.068
DB00502 1880 85 None -3 85 Human 8.7 pKi = 8.7 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2004.07.068
56652776 192406 0 None 257 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 319 5 0 3 3.9 c1ccc(N2CCN(CCCn3ccc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5205590 192406 0 None 257 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 319 5 0 3 3.9 c1ccc(N2CCN(CCCn3ccc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5222747 192406 0 None 257 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 319 5 0 3 3.9 c1ccc(N2CCN(CCCn3ccc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
49788867 18022 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 380 6 1 6 2.4 COc1cccc(C(=O)NCCN2CCN(c3noc4ccccc34)CC2)c1 10.1021/jm100925m
CHEMBL1270013 18022 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 380 6 1 6 2.4 COc1cccc(C(=O)NCCN2CCN(c3noc4ccccc34)CC2)c1 10.1021/jm100925m
137642607 157972 0 None 234 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 348 5 0 2 4.2 O=C1CCc2ccccc2N1CCCN1CCC(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4091231 157972 0 None 234 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 348 5 0 2 4.2 O=C1CCc2ccccc2N1CCCN1CCC(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
10588194 18732 3 None 67 3 Human 8.7 pKi = 8.7 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 271 9 1 3 3.1 c1ccc(OCCCNCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL128524 18732 3 None 67 3 Human 8.7 pKi = 8.7 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 271 9 1 3 3.1 c1ccc(OCCCNCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
44336061 108134 0 None 56 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1021/acs.jmedchem.8b00265
CHEMBL320597 108134 0 None 56 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1021/acs.jmedchem.8b00265
135398737 944 89 None -13 91 Human 8.0 pKi = 8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970111h
38 944 89 None -13 91 Human 8.0 pKi = 8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970111h
722 944 89 None -13 91 Human 8.0 pKi = 8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970111h
CHEMBL42 944 89 None -13 91 Human 8.0 pKi = 8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970111h
DB00363 944 89 None -13 91 Human 8.0 pKi = 8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970111h
10520941 203402 0 None 6 3 Human 8.0 pKi = 8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 337 5 1 2 4.9 c1ccc(CCN2CCC(c3cc(C4CCCCC4)n[nH]3)CC2)cc1 10.1021/jm970111h
CHEMBL77744 203402 0 None 6 3 Human 8.0 pKi = 8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 337 5 1 2 4.9 c1ccc(CCN2CCC(c3cc(C4CCCCC4)n[nH]3)CC2)cc1 10.1021/jm970111h
9948584 205647 0 None -10 4 Human 8.0 pKi = 8 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 309 4 3 4 2.8 Oc1nc2c3c(ccc2[nH]1)CCC(CNCc1ccccc1)O3 10.1016/s0960-894x(01)00778-8
CHEMBL93779 205647 0 None -10 4 Human 8.0 pKi = 8 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 309 4 3 4 2.8 Oc1nc2c3c(ccc2[nH]1)CCC(CNCc1ccccc1)O3 10.1016/s0960-894x(01)00778-8
44273720 74845 0 None 100 2 Human 8.0 pKi = 8 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 391 7 1 3 4.3 CC1(C(=O)NCCCCN2CCN(c3ccc(Cl)cc3)CC2)CCCCC1 10.1016/0960-894X(96)00198-9
CHEMBL20367 74845 0 None 100 2 Human 8.0 pKi = 8 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 391 7 1 3 4.3 CC1(C(=O)NCCCCN2CCN(c3ccc(Cl)cc3)CC2)CCCCC1 10.1016/0960-894X(96)00198-9
9801098 5329 0 None 301 2 Human 8.0 pKi = 8 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 399 5 1 4 2.4 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1c2ccccc2C[C@H]1CO 10.1016/s0960-894x(02)00656-x
CHEMBL107151 5329 0 None 301 2 Human 8.0 pKi = 8 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 399 5 1 4 2.4 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1c2ccccc2C[C@H]1CO 10.1016/s0960-894x(02)00656-x
44335908 5912 0 None 21 2 Human 8.0 pKi = 8 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 425 5 0 3 4.6 CC(C)c1ccc(Cl)cc1CN1CCN(CC(=O)N2c3ccccc3C[C@H]2C)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL108011 5912 0 None 21 2 Human 8.0 pKi = 8 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 425 5 0 3 4.6 CC(C)c1ccc(Cl)cc1CN1CCN(CC(=O)N2c3ccccc3C[C@H]2C)CC1 10.1016/s0960-894x(02)00656-x
135398737 944 89 None -13 91 Human 8.0 pKi = 8 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9600712
38 944 89 None -13 91 Human 8.0 pKi = 8 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9600712
722 944 89 None -13 91 Human 8.0 pKi = 8 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9600712
CHEMBL42 944 89 None -13 91 Human 8.0 pKi = 8 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9600712
DB00363 944 89 None -13 91 Human 8.0 pKi = 8 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9600712
135398737 944 89 None -13 91 Human 8.0 pKi = 8 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960268u
38 944 89 None -13 91 Human 8.0 pKi = 8 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960268u
722 944 89 None -13 91 Human 8.0 pKi = 8 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960268u
CHEMBL42 944 89 None -13 91 Human 8.0 pKi = 8 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960268u
DB00363 944 89 None -13 91 Human 8.0 pKi = 8 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960268u
44336075 4840 0 None 15 2 Human 8.0 pKi = 8 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 378 5 0 3 4.3 COc1ccc(CN2CCC(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
CHEMBL104579 4840 0 None 15 2 Human 8.0 pKi = 8 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 378 5 0 3 4.3 COc1ccc(CN2CCC(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
9948546 16148 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 308 6 2 4 3.3 Cc1ccc(NCCNCc2ccc3ccc(=O)oc3c2)cc1 10.1021/jm990266k
CHEMBL122754 16148 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 308 6 2 4 3.3 Cc1ccc(NCCNCc2ccc3ccc(=O)oc3c2)cc1 10.1021/jm990266k
44374827 118992 0 None 2 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 389 3 0 3 3.4 Cc1ccc(CN2CCN(C3CCc4cccc5c4N(C3=O)C(C)C5)CC2)cc1 10.1016/s0960-894x(02)01056-9
CHEMBL345438 118992 0 None 2 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 389 3 0 3 3.4 Cc1ccc(CN2CCN(C3CCc4cccc5c4N(C3=O)C(C)C5)CC2)cc1 10.1016/s0960-894x(02)01056-9
164627977 185851 0 None -1 7 Human 8.0 pKi = 8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 355 4 0 4 3.3 O=C1c2cc(Cl)ccc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL4876297 185851 0 None -1 7 Human 8.0 pKi = 8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 355 4 0 4 3.3 O=C1c2cc(Cl)ccc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
1353 1880 85 None -4 85 Rat 8.0 pKi = 8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.07.018
3559 1880 85 None -4 85 Rat 8.0 pKi = 8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.07.018
86 1880 85 None -4 85 Rat 8.0 pKi = 8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.07.018
CHEMBL54 1880 85 None -4 85 Rat 8.0 pKi = 8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.07.018
DB00502 1880 85 None -4 85 Rat 8.0 pKi = 8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.07.018
52940985 17404 0 None 17 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 369 6 0 2 5.8 Cc1ccc(C)c(C(=O)CCCN2CCC(c3ccc(Cl)cc3)CC2)c1 10.1021/jm100899z
CHEMBL1258155 17404 0 None 17 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 369 6 0 2 5.8 Cc1ccc(C)c(C(=O)CCCN2CCC(c3ccc(Cl)cc3)CC2)c1 10.1021/jm100899z
137651322 156933 0 None -11 6 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 465 8 2 9 2.2 O=Cc1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCC(=O)N5)CC3)cc12 10.1016/j.bmc.2017.08.037
CHEMBL4079375 156933 0 None -11 6 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 465 8 2 9 2.2 O=Cc1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCC(=O)N5)CC3)cc12 10.1016/j.bmc.2017.08.037
135398737 944 89 None -13 91 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00169-9
135398737 944 89 None -13 91 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960072u
38 944 89 None -13 91 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00169-9
38 944 89 None -13 91 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960072u
722 944 89 None -13 91 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00169-9
722 944 89 None -13 91 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960072u
CHEMBL42 944 89 None -13 91 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00169-9
CHEMBL42 944 89 None -13 91 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960072u
DB00363 944 89 None -13 91 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00169-9
DB00363 944 89 None -13 91 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960072u
122180956 121257 0 None 8 6 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 404 7 1 3 4.8 CCCN(CCNC(=O)/N=N/c1cc(F)c(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3589577 121257 0 None 8 6 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 404 7 1 3 4.8 CCCN(CCNC(=O)/N=N/c1cc(F)c(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
2389 3279 114 None -21 67 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm070516u
5073 3279 114 None -21 67 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm070516u
96 3279 114 None -21 67 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm070516u
CHEMBL85 3279 114 None -21 67 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm070516u
DB00734 3279 114 None -21 67 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm070516u
9887537 83927 38 None -12 9 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 405 4 0 5 4.0 Fc1ccc(-c2cncc(CN3CCN(c4cccc5c4OCCO5)CC3)c2)cc1 10.1021/jm070516u
CHEMBL221692 83927 38 None -12 9 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 405 4 0 5 4.0 Fc1ccc(-c2cncc(CN3CCN(c4cccc5c4OCCO5)CC3)c2)cc1 10.1021/jm070516u
CHEMBL4751170 83927 38 None -12 9 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 405 4 0 5 4.0 Fc1ccc(-c2cncc(CN3CCN(c4cccc5c4OCCO5)CC3)c2)cc1 10.1021/jm070516u
11725909 202565 0 None 33 3 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 357 3 1 2 5.2 Clc1ccc(CN2CC=C(c3nc4cc(Cl)ccc4[nH]3)CC2)cc1 10.1016/S0960-894X(97)00402-2
CHEMBL71216 202565 0 None 33 3 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 357 3 1 2 5.2 Clc1ccc(CN2CC=C(c3nc4cc(Cl)ccc4[nH]3)CC2)cc1 10.1016/S0960-894X(97)00402-2
1353 1880 85 None -3 85 Human 8.0 pKi = 8 Binding
In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss miceIn vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2003.07.015
3559 1880 85 None -3 85 Human 8.0 pKi = 8 Binding
In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss miceIn vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2003.07.015
86 1880 85 None -3 85 Human 8.0 pKi = 8 Binding
In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss miceIn vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2003.07.015
CHEMBL54 1880 85 None -3 85 Human 8.0 pKi = 8 Binding
In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss miceIn vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2003.07.015
DB00502 1880 85 None -3 85 Human 8.0 pKi = 8 Binding
In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss miceIn vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2003.07.015
9907461 133719 0 None - 1 Human 8.0 pKi = 8 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 371 4 1 3 3.8 O=C1NC(CCN2CCN(c3ccc4ccccc4c3)CC2)c2ccccc21 10.1016/s0960-894x(98)00252-2
CHEMBL37169 133719 0 None - 1 Human 8.0 pKi = 8 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 371 4 1 3 3.8 O=C1NC(CCN2CCN(c3ccc4ccccc4c3)CC2)c2ccccc21 10.1016/s0960-894x(98)00252-2
9903877 198642 1 None -6 5 Human 8.0 pKi = 8 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 282 6 2 3 2.4 O=C1Cc2c(cccc2OCCNCc2ccccc2)N1 10.1016/s0960-894x(99)00434-5
CHEMBL59752 198642 1 None -6 5 Human 8.0 pKi = 8 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 282 6 2 3 2.4 O=C1Cc2c(cccc2OCCNCc2ccccc2)N1 10.1016/s0960-894x(99)00434-5
135398737 944 89 None -13 91 Human 8.0 pKi = 8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/acs.jmedchem.7b00151
38 944 89 None -13 91 Human 8.0 pKi = 8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/acs.jmedchem.7b00151
722 944 89 None -13 91 Human 8.0 pKi = 8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/acs.jmedchem.7b00151
CHEMBL42 944 89 None -13 91 Human 8.0 pKi = 8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/acs.jmedchem.7b00151
DB00363 944 89 None -13 91 Human 8.0 pKi = 8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/acs.jmedchem.7b00151
135398737 944 89 None -13 91 Human 8.0 pKi = 8 Binding
compound was tested for its affinity to displace [3H]spiperone cloned human Dopamine receptor D4 stably expressed in HEK393 cell linescompound was tested for its affinity to displace [3H]spiperone cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991029k
38 944 89 None -13 91 Human 8.0 pKi = 8 Binding
compound was tested for its affinity to displace [3H]spiperone cloned human Dopamine receptor D4 stably expressed in HEK393 cell linescompound was tested for its affinity to displace [3H]spiperone cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991029k
722 944 89 None -13 91 Human 8.0 pKi = 8 Binding
compound was tested for its affinity to displace [3H]spiperone cloned human Dopamine receptor D4 stably expressed in HEK393 cell linescompound was tested for its affinity to displace [3H]spiperone cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991029k
CHEMBL42 944 89 None -13 91 Human 8.0 pKi = 8 Binding
compound was tested for its affinity to displace [3H]spiperone cloned human Dopamine receptor D4 stably expressed in HEK393 cell linescompound was tested for its affinity to displace [3H]spiperone cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991029k
DB00363 944 89 None -13 91 Human 8.0 pKi = 8 Binding
compound was tested for its affinity to displace [3H]spiperone cloned human Dopamine receptor D4 stably expressed in HEK393 cell linescompound was tested for its affinity to displace [3H]spiperone cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991029k
127029388 138809 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 365 6 0 4 3.8 COc1cc(CN2CCO[C@H](COc3cccc(F)c3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3792803 138809 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 365 6 0 4 3.8 COc1cc(CN2CCO[C@H](COc3cccc(F)c3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
164938016 192367 0 None 67 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 337 5 0 4 4.1 c1ccc(N2CCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5200816 192367 0 None 67 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 337 5 0 4 4.1 c1ccc(N2CCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5222506 192367 0 None 67 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 337 5 0 4 4.1 c1ccc(N2CCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1021/acs.jmedchem.2c00840
164627977 185851 0 None -1 7 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 355 4 0 4 3.3 O=C1c2cc(Cl)ccc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL4876297 185851 0 None -1 7 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 355 4 0 4 3.3 O=C1c2cc(Cl)ccc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
127031516 138779 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3792438 138779 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
92988697 138937 1 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 335 5 0 3 3.8 Fc1ccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3794199 138937 1 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 335 5 0 3 3.8 Fc1ccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
1353 1880 85 None -3 85 Human 8.0 pKi = 8.0 Binding
Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar testCataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2003.07.015
3559 1880 85 None -3 85 Human 8.0 pKi = 8.0 Binding
Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar testCataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2003.07.015
86 1880 85 None -3 85 Human 8.0 pKi = 8.0 Binding
Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar testCataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2003.07.015
CHEMBL54 1880 85 None -3 85 Human 8.0 pKi = 8.0 Binding
Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar testCataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2003.07.015
DB00502 1880 85 None -3 85 Human 8.0 pKi = 8.0 Binding
Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar testCataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2003.07.015
9902382 42480 1 None 19 3 Human 8.0 pKi = 8.0 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 337 3 1 4 2.6 Cc1ccc(N2CCN(Cc3ccc4c(c3)OCC(=O)N4)CC2)cc1 10.1021/jm990277d
CHEMBL150173 42480 1 None 19 3 Human 8.0 pKi = 8.0 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 337 3 1 4 2.6 Cc1ccc(N2CCN(Cc3ccc4c(c3)OCC(=O)N4)CC2)cc1 10.1021/jm990277d
127029387 138877 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 365 6 0 4 3.8 COc1ccc(CN2CCO[C@H](COc3cccc(F)c3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3793612 138877 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 365 6 0 4 3.8 COc1ccc(CN2CCO[C@H](COc3cccc(F)c3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
10590285 19854 1 None 21 3 Human 8.0 pKi = 8.0 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCCNCCOc2ccc(C)cc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL130370 19854 1 None 21 3 Human 8.0 pKi = 8.0 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCCNCCOc2ccc(C)cc2)cc1 10.1016/j.bmcl.2005.02.012
12997400 100535 7 None 5 4 Human 7.0 pKi = 7 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 241 3 1 2 2.3 c1ccc(N2CCN(Cc3ccc[nH]3)CC2)cc1 10.1016/s0960-894x(02)00316-5
CHEMBL294394 100535 7 None 5 4 Human 7.0 pKi = 7 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 241 3 1 2 2.3 c1ccc(N2CCN(Cc3ccc[nH]3)CC2)cc1 10.1016/s0960-894x(02)00316-5
11726130 56182 0 None 4 3 Human 7.0 pKi = 7 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 361 1 0 1 6.3 CC(C)=C1c2ccccc2C=C(C2=CCN(C)CC2)c2cc(Cl)ccc21 10.1021/jm00004a016
CHEMBL163239 56182 0 None 4 3 Human 7.0 pKi = 7 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 361 1 0 1 6.3 CC(C)=C1c2ccccc2C=C(C2=CCN(C)CC2)c2cc(Cl)ccc21 10.1021/jm00004a016
44273884 76705 0 None 2 2 Human 7.0 pKi = 7 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 351 6 1 3 3.4 CC(C)(C)C(=O)NCCCCN1CCN(c2cccc(Cl)c2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL20729 76705 0 None 2 2 Human 7.0 pKi = 7 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 351 6 1 3 3.4 CC(C)(C)C(=O)NCCCCN1CCN(c2cccc(Cl)c2)CC1 10.1016/0960-894X(96)00198-9
9820048 201948 0 None 13 2 Human 7.0 pKi = 7 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 355 3 1 3 3.0 O=C1Nc2ccccc2CC1N1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(00)00421-2
CHEMBL67222 201948 0 None 13 2 Human 7.0 pKi = 7 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 355 3 1 3 3.0 O=C1Nc2ccccc2CC1N1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(00)00421-2
10811059 203902 4 None 23 4 Rat 7.0 pKi = 7 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 401 5 1 5 2.2 NS(=O)(=O)c1ccc(N2CCN(CC[C@H]3OCCc4ccccc43)CC2)cc1 10.1021/jm960084f
CHEMBL81649 203902 4 None 23 4 Rat 7.0 pKi = 7 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 401 5 1 5 2.2 NS(=O)(=O)c1ccc(N2CCN(CC[C@H]3OCCc4ccccc43)CC2)cc1 10.1021/jm960084f
135398737 944 89 None -13 91 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
38 944 89 None -13 91 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
722 944 89 None -13 91 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
CHEMBL42 944 89 None -13 91 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
DB00363 944 89 None -13 91 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
135398745 2869 108 None -10 65 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
47 2869 108 None -10 65 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
CHEMBL715 2869 108 None -10 65 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
DB00334 2869 108 None -10 65 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
2389 3279 114 None -21 67 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
5073 3279 114 None -21 67 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
96 3279 114 None -21 67 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
CHEMBL85 3279 114 None -21 67 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
DB00734 3279 114 None -21 67 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
44403219 71560 0 None -91 5 Human 7.0 pKi = 7 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 424 7 1 4 3.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(F)nc1 10.1016/j.bmcl.2005.07.037
CHEMBL197162 71560 0 None -91 5 Human 7.0 pKi = 7 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 424 7 1 4 3.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(F)nc1 10.1016/j.bmcl.2005.07.037
242 467 117 None -117 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
34 467 117 None -117 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
60795 467 117 None -117 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL1112 467 117 None -117 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
DB01238 467 117 None -117 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
72205043 91512 0 None 1 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 396 7 0 5 3.9 Clc1ccc(-n2cc(COCCN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2013.05.027
CHEMBL2414354 91512 0 None 1 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 396 7 0 5 3.9 Clc1ccc(-n2cc(COCCN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2013.05.027
118719927 115281 0 None 2 8 Human 7.0 pKi = 7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 386 11 1 3 4.4 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCO)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL3354074 115281 0 None 2 8 Human 7.0 pKi = 7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 386 11 1 3 4.4 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCO)CC1 10.1021/acs.jmedchem.8b00265
60165681 75006 0 None -3 6 Rat 7.0 pKi = 7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 413 7 0 5 5.1 O=C(CCCCN1CCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL2037528 75006 0 None -3 6 Rat 7.0 pKi = 7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 413 7 0 5 5.1 O=C(CCCCN1CCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
25139335 183736 0 None 2 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 314 8 0 4 3.6 CC#CC1=CCC(N(CCC)CCCCn2cc(C)nn2)CC1 10.1021/jm800895v
CHEMBL484203 183736 0 None 2 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 314 8 0 4 3.6 CC#CC1=CCC(N(CCC)CCCCn2cc(C)nn2)CC1 10.1021/jm800895v
57402366 68973 0 None -199 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1033 32 2 17 5.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cnn3ccc(COCCOCCOCCOCCOCc4ccn5ncc(C(=O)NCCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928139 68973 0 None -199 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1033 32 2 17 5.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cnn3ccc(COCCOCCOCCOCCOCc4ccn5ncc(C(=O)NCCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
72545239 92696 0 None 1 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 499 14 0 9 3.0 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCOCCOCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443006 92696 0 None 1 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 499 14 0 9 3.0 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCOCCOCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
44436621 90600 0 None -17 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 443 8 1 3 4.7 C#Cc1cccc(C(=O)NCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmc.2007.08.038
CHEMBL239733 90600 0 None -17 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 443 8 1 3 4.7 C#Cc1cccc(C(=O)NCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmc.2007.08.038
242 467 117 None -117 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm070516u
34 467 117 None -117 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm070516u
60795 467 117 None -117 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm070516u
CHEMBL1112 467 117 None -117 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm070516u
DB01238 467 117 None -117 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm070516u
11245414 5050 0 None - 1 Human 7.0 pKi = 7 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 362 6 1 5 3.2 COc1ccc(N)cc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL105661 5050 0 None - 1 Human 7.0 pKi = 7 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 362 6 1 5 3.2 COc1ccc(N)cc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
154703647 175791 1 None -1 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 12 0 6 5.6 CCOc1ccc(F)cc1C1CC1CN(CC)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4450429 175791 1 None -1 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 12 0 6 5.6 CCOc1ccc(F)cc1C1CC1CN(CC)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4595728 175791 1 None -1 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 12 0 6 5.6 CCOc1ccc(F)cc1C1CC1CN(CC)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
242 467 117 None -117 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
34 467 117 None -117 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
60795 467 117 None -117 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL1112 467 117 None -117 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
DB01238 467 117 None -117 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
13014683 96894 0 None 1 2 Human 6.0 pKi = 6 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 323 1 0 1 5.5 CC1CCN(C2=Cc3cc(Cl)ccc3Cc3ccccc32)CC1 10.1021/jm00043a008
CHEMBL269396 96894 0 None 1 2 Human 6.0 pKi = 6 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 323 1 0 1 5.5 CC1CCN(C2=Cc3cc(Cl)ccc3Cc3ccccc32)CC1 10.1021/jm00043a008
1687 103930 15 None -275 5 Human 6.0 pKi = 6 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 341 4 0 2 5.1 CN1C2CCC1CC(OC(c1ccccc1)c1ccc(Cl)cc1)C2 10.1021/jm010146o
CHEMBL310310 103930 15 None -275 5 Human 6.0 pKi = 6 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 341 4 0 2 5.1 CN1C2CCC1CC(OC(c1ccccc1)c1ccc(Cl)cc1)C2 10.1021/jm010146o
CHEMBL540034 103930 15 None -275 5 Human 6.0 pKi = 6 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 341 4 0 2 5.1 CN1C2CCC1CC(OC(c1ccccc1)c1ccc(Cl)cc1)C2 10.1021/jm010146o
242 467 117 None -117 51 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
34 467 117 None -117 51 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
60795 467 117 None -117 51 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
CHEMBL1112 467 117 None -117 51 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
DB01238 467 117 None -117 51 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
33630 178379 94 None -13 27 Human 6.0 pKi = 6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
ChEMBL 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL47050 178379 94 None -13 27 Human 6.0 pKi = 6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
ChEMBL 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
127046951 139372 0 None -21 6 Human 6.0 pKi = 6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3799427 139372 0 None -21 6 Human 6.0 pKi = 6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
11360927 4902 0 None - 1 Human 6.0 pKi = 6 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 377 7 0 5 3.6 COc1cccc(OCC2CN(Cc3ccc(Cl)cc3)CCO2)c1OC 10.1021/jm031111m
CHEMBL104844 4902 0 None - 1 Human 6.0 pKi = 6 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 377 7 0 5 3.6 COc1cccc(OCC2CN(Cc3ccc(Cl)cc3)CCO2)c1OC 10.1021/jm031111m
145980271 165939 0 None -19 16 Human 5.0 pKi = 5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
ChEMBL 538 8 1 3 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL4278465 165939 0 None -19 16 Human 5.0 pKi = 5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
ChEMBL 538 8 1 3 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
46216855 198694 0 None -11220 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 395 1 1 3 5.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccs4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL597900 198694 0 None -11220 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 395 1 1 3 5.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccs4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
46231994 198724 0 None -16595 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 414 1 1 3 5.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccc(C#N)c4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL598105 198724 0 None -16595 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 414 1 1 3 5.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccc(C#N)c4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
46231848 198854 0 None -3235 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 396 1 1 3 4.1 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(N4CCCC4=O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL598949 198854 0 None -3235 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 396 1 1 3 4.1 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(N4CCCC4=O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
46231845 199049 0 None -3311 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 391 0 1 2 4.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(Br)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL600083 199049 0 None -3311 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 391 0 1 2 4.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(Br)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
46232066 199571 0 None -14125 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 419 2 1 3 5.7 COc1ccc(-c2cccc3c2CC[C@H]2[C@H]3c3cc(O)c(Cl)cc3CCN2C)cc1 10.1016/j.bmcl.2009.12.094
CHEMBL603872 199571 0 None -14125 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 419 2 1 3 5.7 COc1ccc(-c2cccc3c2CC[C@H]2[C@H]3c3cc(O)c(Cl)cc3CCN2C)cc1 10.1016/j.bmcl.2009.12.094
11439190 199620 0 None -3548 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 338 0 1 3 3.9 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(C#N)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL604127 199620 0 None -3548 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 338 0 1 3 3.9 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(C#N)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
46231995 199849 0 None -16595 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 434 2 1 4 5.6 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccc([N+](=O)[O-])c4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL605339 199849 0 None -16595 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 434 2 1 4 5.6 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccc([N+](=O)[O-])c4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
46231927 199851 0 None -10000 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 432 3 1 4 5.4 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(/C=N/Oc4ccccc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL605354 199851 0 None -10000 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 432 3 1 4 5.4 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(/C=N/Oc4ccccc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
164627027 185845 0 None -50 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 466 5 3 4 4.3 O=C(NCc1ccccc1CN1CCc2cc(O)c(O)cc2C1)c1cccc(Br)c1 10.1016/j.bmcl.2021.128047
CHEMBL4876260 185845 0 None -50 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 466 5 3 4 4.3 O=C(NCc1ccccc1CN1CCc2cc(O)c(O)cc2C1)c1cccc(Br)c1 10.1016/j.bmcl.2021.128047
863787 65959 13 None - 1 Human 7.0 pKi = 7 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 339 5 1 4 2.8 COc1ccc(N2CCN(CC(=O)Nc3cccc(C)c3)CC2)cc1 10.1016/j.bmcl.2004.07.068
CHEMBL184772 65959 13 None - 1 Human 7.0 pKi = 7 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 339 5 1 4 2.8 COc1ccc(N2CCN(CC(=O)Nc3cccc(C)c3)CC2)cc1 10.1016/j.bmcl.2004.07.068
168276065 189626 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 320 5 0 3 4.0 Cc1ccc(CO[C@H]2CCCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2022.128615
CHEMBL5174753 189626 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 320 5 0 3 4.0 Cc1ccc(CO[C@H]2CCCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2022.128615
44395711 174327 0 None -5 3 Human 6.0 pKi = 6.0 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 345 3 1 2 4.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
CHEMBL456430 174327 0 None -5 3 Human 6.0 pKi = 6.0 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 345 3 1 2 4.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
CHEMBL537183 174327 0 None -5 3 Human 6.0 pKi = 6.0 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 345 3 1 2 4.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
44395711 174327 0 None -5 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 345 3 1 2 4.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1ccc(F)cc1 10.1016/j.bmc.2008.12.054
CHEMBL456430 174327 0 None -5 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 345 3 1 2 4.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1ccc(F)cc1 10.1016/j.bmc.2008.12.054
CHEMBL537183 174327 0 None -5 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 345 3 1 2 4.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1ccc(F)cc1 10.1016/j.bmc.2008.12.054
CHEMBL5085974 213231 0 None -123 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CN(C)C(=O)C(CCN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
44309775 102205 0 None -288 8 Human 6.0 pKi = 6.0 Binding
Binding affinity for human dopamine D4 receptorBinding affinity for human dopamine D4 receptor
ChEMBL 491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm049465g
CHEMBL304605 102205 0 None -288 8 Human 6.0 pKi = 6.0 Binding
Binding affinity for human dopamine D4 receptorBinding affinity for human dopamine D4 receptor
ChEMBL 491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm049465g
44309775 102205 0 None -288 8 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm0704200
CHEMBL304605 102205 0 None -288 8 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm0704200
44309775 102205 0 None -288 8 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cellsInhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cells
ChEMBL 491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm040190e
CHEMBL304605 102205 0 None -288 8 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cellsInhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cells
ChEMBL 491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm040190e
72737772 114023 0 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 295 5 0 2 3.8 Cc1ccccc1CN1CCOC(CCc2ccccc2)C1 10.1021/ml500267c
CHEMBL3335541 114023 0 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 295 5 0 2 3.8 Cc1ccccc1CN1CCOC(CCc2ccccc2)C1 10.1021/ml500267c
56664948 66100 0 None -7 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 434 7 2 5 3.7 O=C1CCc2ccc(OCCCCN3CCC(n4c(=O)[nH]c5ccccc54)CC3)cc2N1 10.1016/j.bmc.2011.04.021
CHEMBL1813587 66100 0 None -7 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 434 7 2 5 3.7 O=C1CCc2ccc(OCCCCN3CCC(n4c(=O)[nH]c5ccccc54)CC3)cc2N1 10.1016/j.bmc.2011.04.021
CHEMBL1851962 66100 0 None -7 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 434 7 2 5 3.7 O=C1CCc2ccc(OCCCCN3CCC(n4c(=O)[nH]c5ccccc54)CC3)cc2N1 10.1016/j.bmc.2011.04.021
44431482 87608 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 412 4 1 2 5.3 O=C(NC1CCN(Cc2cccc(C(F)(F)F)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
CHEMBL234473 87608 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 412 4 1 2 5.3 O=C(NC1CCN(Cc2cccc(C(F)(F)F)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
1353 1880 85 None -3 85 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.ejmech.2006.12.030
3559 1880 85 None -3 85 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.ejmech.2006.12.030
86 1880 85 None -3 85 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.ejmech.2006.12.030
CHEMBL54 1880 85 None -3 85 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.ejmech.2006.12.030
DB00502 1880 85 None -3 85 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.ejmech.2006.12.030
10512444 24706 0 None -1445 3 Human 6.0 pKi = 6.0 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 205 2 1 2 2.2 CCN(C)C1CCc2ccc(O)cc2C1 10.1021/jm960345l
CHEMBL134571 24706 0 None -1445 3 Human 6.0 pKi = 6.0 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 205 2 1 2 2.2 CCN(C)C1CCc2ccc(O)cc2C1 10.1021/jm960345l
155536631 171654 0 None -2 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 339 4 0 3 3.5 Fc1ccc2c(c1)CC(CCN1CCCN(c3ccccn3)CC1)C2 10.1016/j.bmc.2020.115943
CHEMBL4474014 171654 0 None -2 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 339 4 0 3 3.5 Fc1ccc2c(c1)CC(CCN1CCCN(c3ccccn3)CC1)C2 10.1016/j.bmc.2020.115943
155536631 171654 0 None -2 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 339 4 0 3 3.5 Fc1ccc2c(c1)CC(CCN1CCCN(c3ccccn3)CC1)C2 10.1016/j.bmc.2020.115943
CHEMBL4474014 171654 0 None -2 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 339 4 0 3 3.5 Fc1ccc2c(c1)CC(CCN1CCCN(c3ccccn3)CC1)C2 10.1016/j.bmc.2020.115943
42625295 55958 0 None -4073 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 460 7 3 4 3.8 O=C(NCC(O)CCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
CHEMBL1627321 55958 0 None -4073 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 460 7 3 4 3.8 O=C(NCC(O)CCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
164612428 184580 0 None -14 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 432 7 2 5 3.9 COc1ccc(C(=O)NCc2ccccc2CN2CCc3cc(OC)c(O)cc3C2)cc1 10.1016/j.bmcl.2021.128047
CHEMBL4857166 184580 0 None -14 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 432 7 2 5 3.9 COc1ccc(C(=O)NCc2ccccc2CN2CCc3cc(OC)c(O)cc3C2)cc1 10.1016/j.bmcl.2021.128047
168296347 191864 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 344 6 0 4 3.7 COc1ccc(CN2CCC[C@H](OCc3cccc(C)n3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5208643 191864 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 344 6 0 4 3.7 COc1ccc(CN2CCC[C@H](OCc3cccc(C)n3)C2)cc1F 10.1016/j.bmcl.2022.128615
154725484 175891 1 None -478 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4439544 175891 1 None -478 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4596514 175891 1 None -478 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
10983150 102515 0 None -18 5 Human 7.0 pKi = 7.0 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 445 7 0 4 4.6 O=C1c2ccccc2C(=O)N1CCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/jm010146o
CHEMBL306672 102515 0 None -18 5 Human 7.0 pKi = 7.0 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 445 7 0 4 4.6 O=C1c2ccccc2C(=O)N1CCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/jm010146o
763625 91716 7 None 19 2 Human 7.0 pKi = 7.0 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 276 3 0 3 3.2 Fc1ccc(N2CCN(Cc3cccs3)CC2)cc1 10.1016/j.bmcl.2013.07.033
CHEMBL2420775 91716 7 None 19 2 Human 7.0 pKi = 7.0 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 276 3 0 3 3.2 Fc1ccc(N2CCN(Cc3cccs3)CC2)cc1 10.1016/j.bmcl.2013.07.033
60165412 75009 0 None -28 6 Rat 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 379 7 0 5 4.5 O=C(CCCCN1CCN(c2ccccc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL2037530 75009 0 None -28 6 Rat 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 379 7 0 5 4.5 O=C(CCCCN1CCN(c2ccccc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
130431351 172600 0 None -3090 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 468 9 2 4 4.7 CCc1cc(Cl)c(OC)c(N2CCN(CCCCNC(=O)c3cc4ccccc4[nH]3)CC2)c1 10.1021/acs.jmedchem.6b00860
CHEMBL4521947 172600 0 None -3090 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 468 9 2 4 4.7 CCc1cc(Cl)c(OC)c(N2CCN(CCCCNC(=O)c3cc4ccccc4[nH]3)CC2)c1 10.1021/acs.jmedchem.6b00860
23288790 202266 0 None -123 6 Human 6.0 pKi = 6.0 Binding
The compound was tested for CNS binding affinity towards Dopamine receptor D4 from cloned Human membranesThe compound was tested for CNS binding affinity towards Dopamine receptor D4 from cloned Human membranes
ChEMBL 395 6 1 5 2.6 COc1ccc(N2CCN(CCC3OCCc4cc(C(N)=O)ccc43)CC2)cc1 10.1021/jm980137o
CHEMBL69385 202266 0 None -123 6 Human 6.0 pKi = 6.0 Binding
The compound was tested for CNS binding affinity towards Dopamine receptor D4 from cloned Human membranesThe compound was tested for CNS binding affinity towards Dopamine receptor D4 from cloned Human membranes
ChEMBL 395 6 1 5 2.6 COc1ccc(N2CCN(CCC3OCCc4cc(C(N)=O)ccc43)CC2)cc1 10.1021/jm980137o
9885219 55982 0 None 1 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 360 4 0 5 2.7 Fc1ccc(OC[C@H]2CC[C@@H]3CN(c4ncc(F)cn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL162873 55982 0 None 1 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 360 4 0 5 2.7 Fc1ccc(OC[C@H]2CC[C@@H]3CN(c4ncc(F)cn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
127031833 138865 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 340 5 1 3 3.6 Fc1cccc2[nH]cc(CN3CCO[C@H](COc4ccccc4)C3)c12 10.1016/j.bmcl.2016.03.102
CHEMBL3793347 138865 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 340 5 1 3 3.6 Fc1cccc2[nH]cc(CN3CCO[C@H](COc4ccccc4)C3)c12 10.1016/j.bmcl.2016.03.102
135506137 11229 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 352 5 1 7 1.7 c1cnc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL1179504 11229 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 352 5 1 7 1.7 c1cnc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL80655 11229 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 352 5 1 7 1.7 c1cnc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
10065188 101133 0 None 3 3 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 329 4 1 3 2.9 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccccc1 10.1016/j.bmcl.2005.02.012
CHEMBL298763 101133 0 None 3 3 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 329 4 1 3 2.9 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccccc1 10.1016/j.bmcl.2005.02.012
11408148 128198 0 None -275 5 Human 6.0 pKi = 6.0 Binding
Binding affinity for human dopamine D4 receptorBinding affinity for human dopamine D4 receptor
ChEMBL 443 6 1 4 4.8 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm049465g
CHEMBL366904 128198 0 None -275 5 Human 6.0 pKi = 6.0 Binding
Binding affinity for human dopamine D4 receptorBinding affinity for human dopamine D4 receptor
ChEMBL 443 6 1 4 4.8 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm049465g
11408148 128198 0 None -275 5 Human 6.0 pKi = 6.0 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 443 6 1 4 4.8 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm900095y
CHEMBL366904 128198 0 None -275 5 Human 6.0 pKi = 6.0 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 443 6 1 4 4.8 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm900095y
164623294 185241 0 None -7 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 432 7 2 5 3.9 COc1cccc(C(=O)NCc2ccccc2CN2CCc3cc(OC)c(O)cc3C2)c1 10.1016/j.bmcl.2021.128047
CHEMBL4867331 185241 0 None -7 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 432 7 2 5 3.9 COc1cccc(C(=O)NCc2ccccc2CN2CCc3cc(OC)c(O)cc3C2)c1 10.1016/j.bmcl.2021.128047
11408148 128198 0 None -275 5 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cellsInhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cells
ChEMBL 443 6 1 4 4.8 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
CHEMBL366904 128198 0 None -275 5 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cellsInhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cells
ChEMBL 443 6 1 4 4.8 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
72737725 114027 0 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 317 5 0 2 3.8 Fc1cccc(F)c1CN1CCOC(CCc2ccccc2)C1 10.1021/ml500267c
CHEMBL3335545 114027 0 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 317 5 0 2 3.8 Fc1cccc(F)c1CN1CCOC(CCc2ccccc2)C1 10.1021/ml500267c
4350931 168747 39 None -1348 7 Human 7.0 pKi = 7.0 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1039/C5MD00258C
CHEMBL441618 168747 39 None -1348 7 Human 7.0 pKi = 7.0 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1039/C5MD00258C
44336154 5367 0 None 8 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 411 4 0 3 4.2 CC1N(C(=O)CN2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc2C1(C)C 10.1016/s0960-894x(02)00655-8
CHEMBL107384 5367 0 None 8 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 411 4 0 3 4.2 CC1N(C(=O)CN2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc2C1(C)C 10.1016/s0960-894x(02)00655-8
4350931 168747 39 None -1348 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human D4 dopamine receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 dopamine receptor expressed in CHO cells
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
CHEMBL441618 168747 39 None -1348 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human D4 dopamine receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 dopamine receptor expressed in CHO cells
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
21302490 112308 26 None -12 9 Human 7.0 pKi = 7.0 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 393 5 0 4 3.9 CN1CCN2c3c(cccc31)[C@@H]1CN(CCCC(=O)c3ccc(F)cc3)CC[C@@H]12 10.1021/jm401958n
CHEMBL3233142 112308 26 None -12 9 Human 7.0 pKi = 7.0 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 393 5 0 4 3.9 CN1CCN2c3c(cccc31)[C@@H]1CN(CCCC(=O)c3ccc(F)cc3)CC[C@@H]12 10.1021/jm401958n
CHEMBL3306803 112308 26 None -12 9 Human 7.0 pKi = 7.0 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 393 5 0 4 3.9 CN1CCN2c3c(cccc31)[C@@H]1CN(CCCC(=O)c3ccc(F)cc3)CC[C@@H]12 10.1021/jm401958n
188249 39415 4 None 1 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 328 0 0 5 3.2 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ncccc32)CC1 10.1021/jm2013419
CHEMBL147463 39415 4 None 1 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 328 0 0 5 3.2 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ncccc32)CC1 10.1021/jm2013419
CHEMBL2022280 39415 4 None 1 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 328 0 0 5 3.2 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ncccc32)CC1 10.1021/jm2013419
10363821 38801 0 None 91 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 403 2 1 5 4.7 Clc1ccc2c(c1)C(N1CCN(Cc3ccccc3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL146856 38801 0 None 91 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 403 2 1 5 4.7 Clc1ccc2c(c1)C(N1CCN(Cc3ccccc3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
10807035 205005 0 None 107 2 Human 8.0 pKi = 8.0 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 339 2 0 3 4.3 Cc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(Cl)cc1)CC3 10.1021/jm970170v
CHEMBL89921 205005 0 None 107 2 Human 8.0 pKi = 8.0 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 339 2 0 3 4.3 Cc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(Cl)cc1)CC3 10.1021/jm970170v
10615437 95495 1 None 6 3 Human 8.0 pKi = 8.0 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 317 4 1 2 4.5 c1ccc(CN2CCC(c3cc(-c4ccccc4)[nH]n3)CC2)cc1 10.1021/jm970111h
CHEMBL25938 95495 1 None 6 3 Human 8.0 pKi = 8.0 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 317 4 1 2 4.5 c1ccc(CN2CCC(c3cc(-c4ccccc4)[nH]n3)CC2)cc1 10.1021/jm970111h
15467370 101848 0 None 2818 4 Human 8.0 pKi = 8.0 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 351 4 1 4 3.4 N#CC(C#N)=Cc1ccc(CN2CCN(c3ccc(Cl)cc3)CC2)[nH]1 10.1016/s0960-894x(99)00302-9
CHEMBL303538 101848 0 None 2818 4 Human 8.0 pKi = 8.0 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 351 4 1 4 3.4 N#CC(C#N)=Cc1ccc(CN2CCN(c3ccc(Cl)cc3)CC2)[nH]1 10.1016/s0960-894x(99)00302-9
289 240 6 None 1 14 Human 8.0 pKi = 8.0 Binding
Binding affinity to human D4.4 receptor by radioligand displacement assayBinding affinity to human D4.4 receptor by radioligand displacement assay
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm100697g
9948320 240 6 None 1 14 Human 8.0 pKi = 8.0 Binding
Binding affinity to human D4.4 receptor by radioligand displacement assayBinding affinity to human D4.4 receptor by radioligand displacement assay
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm100697g
CHEMBL1242950 240 6 None 1 14 Human 8.0 pKi = 8.0 Binding
Binding affinity to human D4.4 receptor by radioligand displacement assayBinding affinity to human D4.4 receptor by radioligand displacement assay
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm100697g
72164301 91727 0 None 3 3 Human 8.0 pKi = 8.0 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 320 3 0 2 4.3 Clc1cccc(N2CCN(Cc3ccccc3)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
CHEMBL2420893 91727 0 None 3 3 Human 8.0 pKi = 8.0 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 320 3 0 2 4.3 Clc1cccc(N2CCN(Cc3ccccc3)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
44330553 167636 0 None 2 2 Human 8.0 pKi = 8.0 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 216 0 0 3 2.8 Cc1oc(C)c2c1CCCc1cnn(C)c1-2 10.1016/s0960-894x(03)00587-0
CHEMBL433376 167636 0 None 2 2 Human 8.0 pKi = 8.0 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 216 0 0 3 2.8 Cc1oc(C)c2c1CCCc1cnn(C)c1-2 10.1016/s0960-894x(03)00587-0
10590285 19854 1 None 21 3 Human 8.0 pKi = 8.0 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCCNCCOc2ccc(C)cc2)cc1 10.1021/jm970422s
CHEMBL130370 19854 1 None 21 3 Human 8.0 pKi = 8.0 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCCNCCOc2ccc(C)cc2)cc1 10.1021/jm970422s
44335909 110851 0 None 12 2 Human 8.0 pKi = 8.0 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 427 6 0 4 3.8 CCOc1ccc(Cl)cc1CN1CCN(CC(=O)N2c3ccccc3C[C@H]2C)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL326863 110851 0 None 12 2 Human 8.0 pKi = 8.0 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 427 6 0 4 3.8 CCOc1ccc(Cl)cc1CN1CCN(CC(=O)N2c3ccccc3C[C@H]2C)CC1 10.1016/s0960-894x(02)00656-x
10926404 46597 8 None 28 2 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 357 6 1 4 2.4 COc1cccc(C(=O)NCCN2CCN(c3ccc(F)cc3)CC2)c1 10.1021/jm020952a
CHEMBL154050 46597 8 None 28 2 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 357 6 1 4 2.4 COc1cccc(C(=O)NCCN2CCN(c3ccc(F)cc3)CC2)c1 10.1021/jm020952a
44335853 4790 0 None 478 2 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 417 4 0 3 3.8 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104321 4790 0 None 478 2 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 417 4 0 3 3.8 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/s0960-894x(02)00655-8
1353 1880 85 None -3 85 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm030480f
3559 1880 85 None -3 85 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm030480f
86 1880 85 None -3 85 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm030480f
CHEMBL54 1880 85 None -3 85 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm030480f
DB00502 1880 85 None -3 85 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm030480f
10782946 15397 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 3 0 4 3.4 Cc1ccc(N2CCN(Cc3ccc4oc(=O)ccc4c3)CC2)cc1 10.1021/jm990266k
CHEMBL122049 15397 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 3 0 4 3.4 Cc1ccc(N2CCN(Cc3ccc4oc(=O)ccc4c3)CC2)cc1 10.1021/jm990266k
9906978 42466 1 None 1 12 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmc.2008.12.054
CHEMBL150161 42466 1 None 1 12 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmc.2008.12.054
2435 3533 78 None -10 48 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
60149 3533 78 None -10 48 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
98 3533 78 None -10 48 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
CHEMBL12713 3533 78 None -10 48 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
DB06144 3533 78 None -10 48 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
145969934 164493 0 None 1 6 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 261 7 1 2 4.2 CCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4226336 164493 0 None 1 6 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 261 7 1 2 4.2 CCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
11504230 77840 0 None -12 7 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 497 8 1 4 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm100899z
CHEMBL210567 77840 0 None -12 7 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 497 8 1 4 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm100899z
11393666 192384 0 None -28 19 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
CHEMBL5201983 192384 0 None -28 19 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
CHEMBL5222597 192384 0 None -28 19 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
CHEMBL4435399 212176 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysis
ChEMBL None None None O=[N+]([O-])c1ccc(CN2CCC(n3cc(Cc4ccc(Br)cc4)nn3)CC2)cc1 10.1016/j.bmc.2022.116851
16725912 85302 13 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 344 4 1 2 4.2 O=C(NC1CCN(Cc2ccccc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.096
16725912 85302 13 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 344 4 1 2 4.2 O=C(NC1CCN(Cc2ccccc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
CHEMBL228972 85302 13 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 344 4 1 2 4.2 O=C(NC1CCN(Cc2ccccc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.096
CHEMBL228972 85302 13 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 344 4 1 2 4.2 O=C(NC1CCN(Cc2ccccc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
44431489 87843 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.5 Cc1cccc(CN2CCC(NC(=O)c3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.12.106
CHEMBL234825 87843 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.5 Cc1cccc(CN2CCC(NC(=O)c3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.12.106
53364155 63513 0 None 1 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1041 33 0 16 10.2 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCCc1cn(CCCCCCCCCCn2cc(CCCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803026 63513 0 None 1 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1041 33 0 16 10.2 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCCc1cn(CCCCCCCCCCn2cc(CCCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
137632761 156033 0 None -13 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 476 8 3 9 2.7 O=c1ccc2c(N3CCN(CCCCOc4ccn5ncc(/C=N/O)c5c4)CC3)ccc(O)c2[nH]1 10.1016/j.bmc.2017.08.037
CHEMBL4068561 156033 0 None -13 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 476 8 3 9 2.7 O=c1ccc2c(N3CCN(CCCCOc4ccn5ncc(/C=N/O)c5c4)CC3)ccc(O)c2[nH]1 10.1016/j.bmc.2017.08.037
137640203 156420 0 None -1 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 452 10 0 8 3.5 CCOC(=O)c1cc2cc(OCCCCN3CCN(c4ccccc4OC)CC3)ccn2n1 10.1021/acs.jmedchem.6b01857
CHEMBL4072821 156420 0 None -1 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 452 10 0 8 3.5 CCOC(=O)c1cc2cc(OCCCCN3CCN(c4ccccc4OC)CC3)ccn2n1 10.1021/acs.jmedchem.6b01857
10615437 95495 1 None 6 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 317 4 1 2 4.5 c1ccc(CN2CCC(c3cc(-c4ccccc4)[nH]n3)CC2)cc1 10.1016/s0960-894x(99)00169-9
CHEMBL25938 95495 1 None 6 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 317 4 1 2 4.5 c1ccc(CN2CCC(c3cc(-c4ccccc4)[nH]n3)CC2)cc1 10.1016/s0960-894x(99)00169-9
71733935 90552 0 None -43 6 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm400520c
CHEMBL2396663 90552 0 None -43 6 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm400520c
10615437 95495 1 None 6 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from recombinant human D4 receptor stably expressed in HEK293 cellsDisplacement of [3H]spiperone from recombinant human D4 receptor stably expressed in HEK293 cells
ChEMBL 317 4 1 2 4.5 c1ccc(CN2CCC(c3cc(-c4ccccc4)[nH]n3)CC2)cc1 10.1016/j.bmc.2022.116851
CHEMBL25938 95495 1 None 6 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from recombinant human D4 receptor stably expressed in HEK293 cellsDisplacement of [3H]spiperone from recombinant human D4 receptor stably expressed in HEK293 cells
ChEMBL 317 4 1 2 4.5 c1ccc(CN2CCC(c3cc(-c4ccccc4)[nH]n3)CC2)cc1 10.1016/j.bmc.2022.116851
9865446 123533 0 None - 1 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 394 6 2 4 3.7 OCc1ccc(N2CCN(CCC(O)c3ccc(Cl)cc3)CC2)cc1Cl 10.1016/s0960-894x(98)00252-2
CHEMBL36313 123533 0 None - 1 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 394 6 2 4 3.7 OCc1ccc(N2CCN(CCC(O)c3ccc(Cl)cc3)CC2)cc1Cl 10.1016/s0960-894x(98)00252-2
10479188 201184 0 None 5 4 Human 8.0 pKi = 8.0 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 455 8 1 5 4.7 COc1ccc(Br)cc1-c1nc(CNC[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL62602 201184 0 None 5 4 Human 8.0 pKi = 8.0 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 455 8 1 5 4.7 COc1ccc(Br)cc1-c1nc(CNC[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
9949531 204883 0 None -11 4 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 333 6 3 4 3.7 Sc1nc2c(OCCNCc3ccccc3)cc(Cl)cc2[nH]1 10.1016/s0960-894x(99)00434-5
CHEMBL89037 204883 0 None -11 4 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 333 6 3 4 3.7 Sc1nc2c(OCCNCc3ccccc3)cc(Cl)cc2[nH]1 10.1016/s0960-894x(99)00434-5
44369020 118954 0 None -2 3 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 374 6 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/jm100925m
CHEMBL345111 118954 0 None -2 3 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 374 6 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/jm100925m
11558055 72805 1 None -17 6 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1039/C5MD00258C
CHEMBL1204122 72805 1 None -17 6 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1039/C5MD00258C
CHEMBL201170 72805 1 None -17 6 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1039/C5MD00258C
11558055 72805 1 None -17 6 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmc.2009.08.028
CHEMBL1204122 72805 1 None -17 6 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmc.2009.08.028
CHEMBL201170 72805 1 None -17 6 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmc.2009.08.028
11558055 72805 1 None -17 6 Human 8.0 pKi = 8.0 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm050846j
CHEMBL1204122 72805 1 None -17 6 Human 8.0 pKi = 8.0 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm050846j
CHEMBL201170 72805 1 None -17 6 Human 8.0 pKi = 8.0 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm050846j
11772112 168251 0 None 9 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 338 6 0 5 3.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1C 10.1021/jm060279f
CHEMBL437687 168251 0 None 9 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 338 6 0 5 3.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1C 10.1021/jm060279f
44278427 98883 0 None 39 3 Human 7.9 pKi = 7.9 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 327 7 1 4 3.0 O[C@H](COc1ccccc1)CN1CCC(Oc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
CHEMBL282323 98883 0 None 39 3 Human 7.9 pKi = 7.9 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 327 7 1 4 3.0 O[C@H](COc1ccccc1)CN1CCC(Oc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
127031518 138869 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3793389 138869 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
127029995 138967 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1F 10.1016/j.bmcl.2016.03.102
CHEMBL3794529 138967 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1F 10.1016/j.bmcl.2016.03.102
11849266 80657 0 None 5 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 372 6 0 5 3.6 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)c(C)c1 10.1021/jm060279f
CHEMBL215450 80657 0 None 5 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 372 6 0 5 3.6 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)c(C)c1 10.1021/jm060279f
44370047 119171 0 None 4 3 Human 7.9 pKi = 7.9 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 340 4 1 3 3.5 Clc1ccc(N2CCN(CCc3cc4ccc[nH]c-4n3)CC2)cc1 10.1016/s0960-894x(99)00025-6
CHEMBL347155 119171 0 None 4 3 Human 7.9 pKi = 7.9 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 340 4 1 3 3.5 Clc1ccc(N2CCN(CCc3cc4ccc[nH]c-4n3)CC2)cc1 10.1016/s0960-894x(99)00025-6
13091268 77845 0 None -8 14 Human 7.9 pKi = 7.9 Binding
Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar testCataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2003.07.015
CHEMBL210578 77845 0 None -8 14 Human 7.9 pKi = 7.9 Binding
Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar testCataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2003.07.015
10378389 201554 1 None -53 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
CHEMBL134807 201554 1 None -53 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
CHEMBL64553 201554 1 None -53 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
10378389 201554 1 None -53 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
CHEMBL134807 201554 1 None -53 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
CHEMBL64553 201554 1 None -53 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
10497193 203229 0 None 1 3 Human 7.0 pKi = 7.0 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 337 4 1 2 4.7 Clc1ccc(-c2cc(C3CCN(Cc4ccccc4)C3)[nH]n2)cc1 10.1021/jm970111h
CHEMBL76355 203229 0 None 1 3 Human 7.0 pKi = 7.0 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 337 4 1 2 4.7 Clc1ccc(-c2cc(C3CCN(Cc4ccccc4)C3)[nH]n2)cc1 10.1021/jm970111h
10738530 203326 0 None 5 3 Human 7.0 pKi = 7.0 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 379 6 1 2 5.5 Clc1ccc(-c2cc(C3CCN(CCCc4ccccc4)CC3)[nH]n2)cc1 10.1021/jm970111h
CHEMBL77017 203326 0 None 5 3 Human 7.0 pKi = 7.0 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 379 6 1 2 5.5 Clc1ccc(-c2cc(C3CCN(CCCc4ccccc4)CC3)[nH]n2)cc1 10.1021/jm970111h
10790517 205878 0 None 1 3 Human 7.0 pKi = 7.0 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 469 7 2 4 4.9 COc1cc(NC(=O)C2CCCCC2)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
CHEMBL95096 205878 0 None 1 3 Human 7.0 pKi = 7.0 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 469 7 2 4 4.9 COc1cc(NC(=O)C2CCCCC2)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
6603867 101524 16 None -56 7 Human 7.0 pKi = 7.0 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 247 5 1 2 3.4 CCCN(CCC)[C@@H]1CCc2ccc(O)cc2C1 10.1021/jm960345l
CHEMBL301559 101524 16 None -56 7 Human 7.0 pKi = 7.0 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 247 5 1 2 3.4 CCCN(CCC)[C@@H]1CCc2ccc(O)cc2C1 10.1021/jm960345l
57345618 70116 0 None -1 6 Rat 7.0 pKi = 7.0 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 362 6 0 3 4.5 Fc1ccc(OCCCN2CCCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2012.01.022
CHEMBL1946126 70116 0 None -1 6 Rat 7.0 pKi = 7.0 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 362 6 0 3 4.5 Fc1ccc(OCCCN2CCCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2012.01.022
92984956 138950 1 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 343 7 0 5 3.0 COc1ccc(CN2CCO[C@H](COc3ccc(OC)cc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3794363 138950 1 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 343 7 0 5 3.0 COc1ccc(CN2CCO[C@H](COc3ccc(OC)cc3)C2)cc1 10.1016/j.bmcl.2016.03.102
11164276 79342 0 None 1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 360 6 0 5 2.9 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cc(F)cc(F)c1 10.1021/jm060279f
CHEMBL211732 79342 0 None 1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 360 6 0 5 2.9 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cc(F)cc(F)c1 10.1021/jm060279f
11154555 788 57 None -501 12 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
5037 788 57 None -501 12 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
7671 788 57 None -501 12 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
CHEMBL2028019 788 57 None -501 12 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
CHEMBL3085826 788 57 None -501 12 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
DB06016 788 57 None -501 12 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
11154555 788 57 None -501 12 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.04.036
5037 788 57 None -501 12 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.04.036
7671 788 57 None -501 12 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.04.036
CHEMBL2028019 788 57 None -501 12 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.04.036
CHEMBL3085826 788 57 None -501 12 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.04.036
DB06016 788 57 None -501 12 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.04.036
10830557 31086 0 None 4 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]cc(CN3CCN(c4ccc(F)cc4)CC3)c2c1 10.1021/jm0009989
CHEMBL140165 31086 0 None 4 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]cc(CN3CCN(c4ccc(F)cc4)CC3)c2c1 10.1021/jm0009989
44436600 91370 0 None -109 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 391 8 1 4 3.0 C#Cc1ccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2007.08.038
CHEMBL241212 91370 0 None -109 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 391 8 1 4 3.0 C#Cc1ccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2007.08.038
71734126 90623 0 None -10 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm400520c
CHEMBL2397391 90623 0 None -10 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm400520c
44372312 53503 0 None 43 3 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 356 4 1 5 2.8 OCc1cccn2ncc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1016/s0960-894x(01)00814-9
CHEMBL160396 53503 0 None 43 3 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 356 4 1 5 2.8 OCc1cccn2ncc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1016/s0960-894x(01)00814-9
72737734 114024 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 365 6 0 3 4.4 FC(F)(F)Oc1cccc(CN2CCOC(CCc3ccccc3)C2)c1 10.1021/ml500267c
CHEMBL3335542 114024 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 365 6 0 3 4.4 FC(F)(F)Oc1cccc(CN2CCOC(CCc3ccccc3)C2)c1 10.1021/ml500267c
155536815 171641 0 None 33 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 322 4 1 2 4.1 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)cc1 10.1021/acs.jmedchem.9b00231
CHEMBL4473792 171641 0 None 33 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 322 4 1 2 4.1 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)cc1 10.1021/acs.jmedchem.9b00231
133633 2210 46 None -104 8 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]IABN from human dopamine D4 receptorDisplacement of [125I]IABN from human dopamine D4 receptor
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1021/jm800532x
177 2210 46 None -104 8 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]IABN from human dopamine D4 receptorDisplacement of [125I]IABN from human dopamine D4 receptor
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1021/jm800532x
CHEMBL445102 2210 46 None -104 8 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]IABN from human dopamine D4 receptorDisplacement of [125I]IABN from human dopamine D4 receptor
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1021/jm800532x
44438201 93174 2 None -158 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 374 3 2 2 5.0 OC1(c2ccc(Cl)c(Cl)c2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246637 93174 2 None -158 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 374 3 2 2 5.0 OC1(c2ccc(Cl)c(Cl)c2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
25139329 186520 0 None -7 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 514 10 0 4 7.6 CCCN(CCCCn1cc(-c2ccc(-c3ccccc3)cc2)nn1)C1CC=C(C#Cc2ccccc2)CC1 10.1021/jm800895v
CHEMBL491466 186520 0 None -7 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 514 10 0 4 7.6 CCCN(CCCCn1cc(-c2ccc(-c3ccccc3)cc2)nn1)C1CC=C(C#Cc2ccccc2)CC1 10.1021/jm800895v
2779264 110854 36 None 8 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 240 3 0 2 3.3 c1ccc(CN2CCC(n3cccc3)CC2)cc1 10.1016/s0960-894x(99)00540-5
CHEMBL326877 110854 36 None 8 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 240 3 0 2 3.3 c1ccc(CN2CCC(n3cccc3)CC2)cc1 10.1016/s0960-894x(99)00540-5
134151428 154015 0 None -44 9 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 291 3 0 2 3.5 O=C1c2ccccc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
CHEMBL3978642 154015 0 None -44 9 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 291 3 0 2 3.5 O=C1c2ccccc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
CHEMBL3991094 154015 0 None -44 9 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 291 3 0 2 3.5 O=C1c2ccccc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
17755999 142353 1 None -190 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)CCCN(C)CCc1ccccc1C2 10.1021/jm070388+
CHEMBL389357 142353 1 None -190 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)CCCN(C)CCc1ccccc1C2 10.1021/jm070388+
3117 206106 100 None -2 16 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
CHEMBL964 206106 100 None -2 16 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
44304644 201560 0 None 1 4 Human 6.0 pKi = 6.0 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 454 8 2 4 4.5 COc1ccc(Br)cc1-c1nc(CNC[C@@H]2CCN(Cc3ccccc3)C2)c[nH]1 10.1016/s0960-894x(00)00405-4
CHEMBL64566 201560 0 None 1 4 Human 6.0 pKi = 6.0 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 454 8 2 4 4.5 COc1ccc(Br)cc1-c1nc(CNC[C@@H]2CCN(Cc3ccccc3)C2)c[nH]1 10.1016/s0960-894x(00)00405-4
10436285 101482 0 None -954 5 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cellsInhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cells
ChEMBL 507 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2=O 10.1021/jm040190e
CHEMBL301242 101482 0 None -954 5 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cellsInhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cells
ChEMBL 507 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2=O 10.1021/jm040190e
10301202 13391 0 None -70 3 Human 6.0 pKi = 6.0 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 511 11 0 6 6.1 COc1ccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)c(OC)c1 10.1016/s0960-894x(02)00179-8
CHEMBL1193508 13391 0 None -70 3 Human 6.0 pKi = 6.0 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 511 11 0 6 6.1 COc1ccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)c(OC)c1 10.1016/s0960-894x(02)00179-8
CHEMBL544925 13391 0 None -70 3 Human 6.0 pKi = 6.0 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 511 11 0 6 6.1 COc1ccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)c(OC)c1 10.1016/s0960-894x(02)00179-8
11211058 79924 0 None 8 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 374 6 1 6 2.3 CO/N=C(\c1ccc(Cl)cc1)C(O)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
CHEMBL214247 79924 0 None 8 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 374 6 1 6 2.3 CO/N=C(\c1ccc(Cl)cc1)C(O)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
44393737 65430 0 None - 1 Human 7.0 pKi = 7.0 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 646 4 1 4 5.7 Cc1c(Br)cc(Br)c(NC(=O)CN2CCN(c3ccc(Br)cc3C#N)CC2)c1Br 10.1016/j.bmcl.2004.07.068
CHEMBL183466 65430 0 None - 1 Human 7.0 pKi = 7.0 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 646 4 1 4 5.7 Cc1c(Br)cc(Br)c(NC(=O)CN2CCN(c3ccc(Br)cc3C#N)CC2)c1Br 10.1016/j.bmcl.2004.07.068
154703824 176052 1 None -436 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4456007 176052 1 None -436 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4597876 176052 1 None -436 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
145967904 164545 0 None 1 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 247 6 1 2 3.8 CCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4227192 164545 0 None 1 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 247 6 1 2 3.8 CCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
11812838 202187 0 None -47 5 Human 5.9 pKi = 5.9 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 479 6 1 3 5.4 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)C1c2ccccc2-c2ccccc21 10.1021/jm010146o
CHEMBL68860 202187 0 None -47 5 Human 5.9 pKi = 5.9 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 479 6 1 3 5.4 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)C1c2ccccc2-c2ccccc21 10.1021/jm010146o
154726046 175737 1 None -288 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4442408 175737 1 None -288 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4595266 175737 1 None -288 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
136094867 40328 0 None 1 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 443 3 2 5 5.7 Clc1ccc2c(c1)C(NC1CC3CCC(C1)N3Cc1ccccc1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL148353 40328 0 None 1 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 443 3 2 5 5.7 Clc1ccc2c(c1)C(NC1CC3CCC(C1)N3Cc1ccccc1)=Nc1cccnc1N2 10.1021/jm0104825
155511803 169038 0 None 229 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 342 4 1 2 4.5 Cc1cccc(NC(=O)CN2CCC(c3ccc(Cl)cc3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4436479 169038 0 None 229 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 342 4 1 2 4.5 Cc1cccc(NC(=O)CN2CCC(c3ccc(Cl)cc3)CC2)c1 10.1021/acs.jmedchem.9b00231
164622586 184954 0 None -4 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 470 6 2 4 5.2 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1cccc(Cl)c1Cl)CC2 10.1016/j.bmcl.2021.128047
CHEMBL4862839 184954 0 None -4 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 470 6 2 4 5.2 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1cccc(Cl)c1Cl)CC2 10.1016/j.bmcl.2021.128047
168288343 190861 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 440 6 1 3 5.3 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2022.128615
CHEMBL5193214 190861 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 440 6 1 3 5.3 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2022.128615
10378389 201554 1 None -53 7 Human 6.9 pKi = 6.9 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1016/s0960-894x(01)00778-8
CHEMBL134807 201554 1 None -53 7 Human 6.9 pKi = 6.9 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1016/s0960-894x(01)00778-8
CHEMBL64553 201554 1 None -53 7 Human 6.9 pKi = 6.9 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1016/s0960-894x(01)00778-8
10378389 201554 1 None -53 7 Human 6.9 pKi = 6.9 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm9703653
CHEMBL134807 201554 1 None -53 7 Human 6.9 pKi = 6.9 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm9703653
CHEMBL64553 201554 1 None -53 7 Human 6.9 pKi = 6.9 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm9703653
10378389 201554 1 None -53 7 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1016/s0960-894x(98)00014-6
CHEMBL134807 201554 1 None -53 7 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1016/s0960-894x(98)00014-6
CHEMBL64553 201554 1 None -53 7 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1016/s0960-894x(98)00014-6
44431462 87641 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 378 4 1 2 4.9 O=C(NC1CCN(Cc2cccc(Cl)c2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
CHEMBL234640 87641 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 378 4 1 2 4.9 O=C(NC1CCN(Cc2cccc(Cl)c2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
10411988 21210 0 None -29 2 Human 6.9 pKi = 6.9 Binding
Binding affinity against human Dopamine receptor D4.2 in CHO cellsBinding affinity against human Dopamine receptor D4.2 in CHO cells
ChEMBL 461 6 0 5 5.2 CC1SC2(CCCC2)C(=O)N1CCCCN1CCN(c2csc3cc(F)ccc23)CC1 10.1021/jm960268u
CHEMBL131482 21210 0 None -29 2 Human 6.9 pKi = 6.9 Binding
Binding affinity against human Dopamine receptor D4.2 in CHO cellsBinding affinity against human Dopamine receptor D4.2 in CHO cells
ChEMBL 461 6 0 5 5.2 CC1SC2(CCCC2)C(=O)N1CCCCN1CCN(c2csc3cc(F)ccc23)CC1 10.1021/jm960268u
122334 319 19 None -2 8 Human 6.9 pKi = 6.9 Binding
Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)
ChEMBL 233 4 1 2 3.1 CCCN[C@@H]1CCc2c([C@@H]1C)cccc2OC 10.1016/S0960-894X(01)80181-5
970 319 19 None -2 8 Human 6.9 pKi = 6.9 Binding
Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)
ChEMBL 233 4 1 2 3.1 CCCN[C@@H]1CCc2c([C@@H]1C)cccc2OC 10.1016/S0960-894X(01)80181-5
CHEMBL27441 319 19 None -2 8 Human 6.9 pKi = 6.9 Binding
Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)
ChEMBL 233 4 1 2 3.1 CCCN[C@@H]1CCc2c([C@@H]1C)cccc2OC 10.1016/S0960-894X(01)80181-5
122334 319 19 None -2 8 Human 6.9 pKi = 6.9 Binding
Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone
ChEMBL 233 4 1 2 3.1 CCCN[C@@H]1CCc2c([C@@H]1C)cccc2OC 10.1021/jm00073a021
970 319 19 None -2 8 Human 6.9 pKi = 6.9 Binding
Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone
ChEMBL 233 4 1 2 3.1 CCCN[C@@H]1CCc2c([C@@H]1C)cccc2OC 10.1021/jm00073a021
CHEMBL27441 319 19 None -2 8 Human 6.9 pKi = 6.9 Binding
Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone
ChEMBL 233 4 1 2 3.1 CCCN[C@@H]1CCc2c([C@@H]1C)cccc2OC 10.1021/jm00073a021
22727358 13113 0 None -7 3 Human 6.9 pKi = 6.9 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 367 7 0 5 4.5 c1ccc(N2CCN(CCCCc3cc(-c4cccs4)no3)CC2)cc1 10.1016/s0960-894x(02)00179-8
CHEMBL1191251 13113 0 None -7 3 Human 6.9 pKi = 6.9 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 367 7 0 5 4.5 c1ccc(N2CCN(CCCCc3cc(-c4cccs4)no3)CC2)cc1 10.1016/s0960-894x(02)00179-8
CHEMBL542324 13113 0 None -7 3 Human 6.9 pKi = 6.9 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 367 7 0 5 4.5 c1ccc(N2CCN(CCCCc3cc(-c4cccs4)no3)CC2)cc1 10.1016/s0960-894x(02)00179-8
127049059 140282 0 None -11 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 404 6 1 5 3.6 O=C1NCN(c2ccccc2)C12CCN(CCCCc1nc3ccccc3o1)CC2 10.1016/j.bmc.2016.06.011
CHEMBL3818935 140282 0 None -11 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 404 6 1 5 3.6 O=C1NCN(c2ccccc2)C12CCN(CCCCc1nc3ccccc3o1)CC2 10.1016/j.bmc.2016.06.011
85658088 164451 0 None -3 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 219 4 1 2 3.0 CCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4225830 164451 0 None -3 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 219 4 1 2 3.0 CCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
127049059 140282 0 None -11 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 404 6 1 5 3.6 O=C1NCN(c2ccccc2)C12CCN(CCCCc1nc3ccccc3o1)CC2 10.1016/j.bmc.2016.06.011
CHEMBL3818935 140282 0 None -11 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 404 6 1 5 3.6 O=C1NCN(c2ccccc2)C12CCN(CCCCc1nc3ccccc3o1)CC2 10.1016/j.bmc.2016.06.011
72205222 91516 0 None -7 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 408 8 0 4 5.1 Clc1ccc(-n2cc(CCCCCN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2013.05.027
CHEMBL2414358 91516 0 None -7 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 408 8 0 4 5.1 Clc1ccc(-n2cc(CCCCCN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2013.05.027
162669562 182120 0 None -2 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 387 6 0 4 4.2 O=C(CCCN1C2CCC1CN(c1ccc(Cl)cn1)C2)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL4789472 182120 0 None -2 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 387 6 0 4 4.2 O=C(CCCN1C2CCC1CN(c1ccc(Cl)cn1)C2)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
44431467 153896 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 412 4 1 2 5.3 O=C(NC1CCN(Cc2cccc(C(F)(F)F)c2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
CHEMBL398990 153896 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 412 4 1 2 5.3 O=C(NC1CCN(Cc2cccc(C(F)(F)F)c2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
44438229 154360 0 None -7 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 380 6 1 2 5.5 C=CCOC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL400826 154360 0 None -7 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 380 6 1 2 5.5 C=CCOC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
142590728 180940 0 None -3 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 446 7 1 3 5.4 CC(C)(C)C(=O)N1CCC(NCCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2020.112674
CHEMBL4765081 180940 0 None -3 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 446 7 1 3 5.4 CC(C)(C)C(=O)N1CCC(NCCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2020.112674
10618211 78193 0 None 10 3 Human 7.9 pKi = 7.9 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 355 5 1 3 4.7 O=C(/C=C(\O)c1ccc(Cl)cc1)C1CCN(Cc2ccccc2)CC1 10.1021/jm970111h
CHEMBL2112285 78193 0 None 10 3 Human 7.9 pKi = 7.9 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 355 5 1 3 4.7 O=C(/C=C(\O)c1ccc(Cl)cc1)C1CCN(Cc2ccccc2)CC1 10.1021/jm970111h
44300865 200310 0 None 16 7 Human 7.9 pKi = 7.9 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 317 4 1 2 4.0 c1ccc(-c2c[nH]c(CN3CCN(c4ccccc4)CC3)c2)cc1 10.1016/s0960-894x(02)00316-5
CHEMBL60815 200310 0 None 16 7 Human 7.9 pKi = 7.9 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 317 4 1 2 4.0 c1ccc(-c2c[nH]c(CN3CCN(c4ccccc4)CC3)c2)cc1 10.1016/s0960-894x(02)00316-5
10424172 13676 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 287 1 0 1 4.4 CN1CC=C(C2=Cc3ccccc3Cc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL1195497 13676 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 287 1 0 1 4.4 CN1CC=C(C2=Cc3ccccc3Cc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL554670 13676 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 287 1 0 1 4.4 CN1CC=C(C2=Cc3ccccc3Cc3ccccc32)CC1 10.1021/jm00004a016
44323894 167537 0 None 1 4 Human 7.9 pKi = 7.9 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 304 1 0 2 3.9 CC1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00004a016
CHEMBL432762 167537 0 None 1 4 Human 7.9 pKi = 7.9 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 304 1 0 2 3.9 CC1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00004a016
10619612 172111 0 None 9 3 Human 7.9 pKi = 7.9 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 377 5 1 5 4.4 COc1ccc(-c2nc(O)n(C3CCN(Cc4ccccc4)CC3)c2C)cc1 10.1021/jm991029k
CHEMBL450021 172111 0 None 9 3 Human 7.9 pKi = 7.9 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 377 5 1 5 4.4 COc1ccc(-c2nc(O)n(C3CCN(Cc4ccccc4)CC3)c2C)cc1 10.1021/jm991029k
44323894 167537 0 None 1 4 Human 7.9 pKi = 7.9 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 304 1 0 2 3.9 CC1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL432762 167537 0 None 1 4 Human 7.9 pKi = 7.9 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 304 1 0 2 3.9 CC1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
10617381 189094 0 None -1 3 Human 7.9 pKi = 7.9 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 343 4 1 3 3.2 Cc1ccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)cc1 10.1021/jm970021c
CHEMBL51536 189094 0 None -1 3 Human 7.9 pKi = 7.9 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 343 4 1 3 3.2 Cc1ccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)cc1 10.1021/jm970021c
44454710 155125 0 None 70 5 Human 7.9 pKi = 7.9 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 378 7 0 4 4.0 COc1cc(CN2CCN(c3ccc(Cl)cc3)CC2)ccc1OCCF 10.1016/j.bmcl.2007.12.026
CHEMBL404888 155125 0 None 70 5 Human 7.9 pKi = 7.9 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 378 7 0 4 4.0 COc1cc(CN2CCN(c3ccc(Cl)cc3)CC2)ccc1OCCF 10.1016/j.bmcl.2007.12.026
9859861 167517 1 None 173 2 Human 7.9 pKi = 7.9 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 218 0 1 2 3.2 Cc1sc(C)c2c1CCCc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
CHEMBL432579 167517 1 None 173 2 Human 7.9 pKi = 7.9 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 218 0 1 2 3.2 Cc1sc(C)c2c1CCCc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
44335973 4965 0 None 7 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 417 4 0 3 4.1 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2cc(Cl)ccc2Cl)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL105172 4965 0 None 7 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 417 4 0 3 4.1 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2cc(Cl)ccc2Cl)CC1 10.1016/s0960-894x(02)00656-x
44335893 108118 0 None 16 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 419 4 0 3 3.7 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(F)c(F)c2Cl)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL320515 108118 0 None 16 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 419 4 0 3 3.7 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(F)c(F)c2Cl)CC1 10.1016/s0960-894x(02)00656-x
44335746 5623 0 None 251 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 385 4 0 3 3.1 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2cc(F)cc(F)c2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL107804 5623 0 None 251 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 385 4 0 3 3.1 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2cc(F)cc(F)c2)CC1 10.1016/s0960-894x(02)00655-8
44335829 108109 0 None 147 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 391 5 0 3 3.9 CC(C)c1ccc(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
CHEMBL320440 108109 0 None 147 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 391 5 0 3 3.9 CC(C)c1ccc(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
44335828 162905 0 None 158 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 405 4 0 3 4.1 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(C(C)(C)C)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL419916 162905 0 None 158 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 405 4 0 3 4.1 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(C(C)(C)C)cc2)CC1 10.1016/s0960-894x(02)00655-8
155561779 175192 0 None 9 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 566 10 2 6 5.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(C#N)cc2)c2ccc(Cl)cc2Cl)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4583596 175192 0 None 9 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 566 10 2 6 5.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(C#N)cc2)c2ccc(Cl)cc2Cl)CC1 10.1021/acs.jmedchem.9b01085
44374863 119702 0 None 13 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 403 3 0 3 3.8 Cc1ccc(CN2CCN(C3CCc4cccc5c4N(C3=O)C(C)(C)C5)CC2)cc1 10.1016/s0960-894x(02)01056-9
CHEMBL351989 119702 0 None 13 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 403 3 0 3 3.8 Cc1ccc(CN2CCN(C3CCc4cccc5c4N(C3=O)C(C)(C)C5)CC2)cc1 10.1016/s0960-894x(02)01056-9
90644057 111540 0 None 28 4 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 365 6 0 4 3.7 FC(F)(F)c1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289645 111540 0 None 28 4 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 365 6 0 4 3.7 FC(F)(F)c1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
13091268 77845 0 None -13 14 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
CHEMBL210578 77845 0 None -13 14 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
53364226 63515 0 None -3 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 989 29 0 18 6.3 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCOCCOCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803028 63515 0 None -3 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 989 29 0 18 6.3 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCOCCOCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
53363201 63524 0 None -1 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 893 27 0 15 7.0 COc1cc(CN2CCN(C)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803054 63524 0 None -1 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 893 27 0 15 7.0 COc1cc(CN2CCN(C)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
44300865 200310 0 None 16 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 317 4 1 2 4.0 c1ccc(-c2c[nH]c(CN3CCN(c4ccccc4)CC3)c2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL60815 200310 0 None 16 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 317 4 1 2 4.0 c1ccc(-c2c[nH]c(CN3CCN(c4ccccc4)CC3)c2)cc1 10.1016/j.bmcl.2006.02.075
44436599 91369 0 None 5 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 477 5 1 3 4.9 O=C(NCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc(C#Cc2ccccc2)c1 10.1016/j.bmc.2007.08.038
CHEMBL241211 91369 0 None 5 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 477 5 1 3 4.9 O=C(NCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc(C#Cc2ccccc2)c1 10.1016/j.bmc.2007.08.038
44222483 194577 0 None -2 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 409 7 1 6 3.0 CSc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm900690y
CHEMBL561763 194577 0 None -2 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 409 7 1 6 3.0 CSc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm900690y
45271653 193565 0 None 851 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 351 4 0 6 2.7 COc1ccc(N2CCN(Cc3c(C)nc4cc(C)ncn34)CC2)cc1 10.1016/j.bmc.2009.05.015
CHEMBL550920 193565 0 None 851 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 351 4 0 6 2.7 COc1ccc(N2CCN(Cc3c(C)nc4cc(C)ncn34)CC2)cc1 10.1016/j.bmc.2009.05.015
10251080 13846 0 None -3 3 Human 7.9 pKi = 7.9 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 411 9 0 6 4.9 CCOc1ccccc1N1CCN(CCCCc2cc(-c3cccs3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL1196692 13846 0 None -3 3 Human 7.9 pKi = 7.9 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 411 9 0 6 4.9 CCOc1ccccc1N1CCN(CCCCc2cc(-c3cccs3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL557829 13846 0 None -3 3 Human 7.9 pKi = 7.9 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 411 9 0 6 4.9 CCOc1ccccc1N1CCN(CCCCc2cc(-c3cccs3)no2)CC1 10.1016/s0960-894x(02)00179-8
13091268 77845 0 None -8 14 Human 7.9 pKi = 7.9 Binding
In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss miceIn vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2003.07.015
CHEMBL210578 77845 0 None -8 14 Human 7.9 pKi = 7.9 Binding
In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss miceIn vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2003.07.015
10617381 189094 0 None -1 3 Human 7.9 pKi = 7.9 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 343 4 1 3 3.2 Cc1ccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL51536 189094 0 None -1 3 Human 7.9 pKi = 7.9 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 343 4 1 3 3.2 Cc1ccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)cc1 10.1016/j.bmcl.2005.02.012
11792373 119317 0 None 457 2 Human 7.9 pKi = 7.9 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 353 4 1 5 2.3 COc1ccc(N2CCN(Cc3ccc4c(c3)NC(=O)CO4)CC2)cc1 10.1021/jm990277d
CHEMBL348435 119317 0 None 457 2 Human 7.9 pKi = 7.9 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 353 4 1 5 2.3 COc1ccc(N2CCN(Cc3ccc4c(c3)NC(=O)CO4)CC2)cc1 10.1021/jm990277d
127053214 138819 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 311 5 0 3 3.6 Cc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1C 10.1016/j.bmcl.2016.03.102
CHEMBL3792923 138819 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 311 5 0 3 3.6 Cc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1C 10.1016/j.bmcl.2016.03.102
76282192 192431 0 None 724 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 320 5 0 4 3.2 c1ccc(N2CCN(CCCn3cnc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5207313 192431 0 None 724 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 320 5 0 4 3.2 c1ccc(N2CCN(CCCn3cnc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5222877 192431 0 None 724 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 320 5 0 4 3.2 c1ccc(N2CCN(CCCn3cnc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
9949601 99591 0 None - 1 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 335 4 1 3 3.0 Cc1ccc(N2CCN(CCC3NC(=O)c4ccccc43)CC2)cc1 10.1016/s0960-894x(98)00252-2
CHEMBL287078 99591 0 None - 1 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 335 4 1 3 3.0 Cc1ccc(N2CCN(CCC3NC(=O)c4ccccc43)CC2)cc1 10.1016/s0960-894x(98)00252-2
44264644 203035 0 None 87 4 Human 7.9 pKi = 7.9 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 330 3 0 4 3.2 Clc1ccc(N2CCN(Cc3cnn4c3CCCC4)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL7442 203035 0 None 87 4 Human 7.9 pKi = 7.9 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 330 3 0 4 3.2 Clc1ccc(N2CCN(Cc3cnn4c3CCCC4)CC2)cc1 10.1016/s0960-894x(98)00692-1
155563301 174678 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 344 4 1 4 2.8 Cc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4572245 174678 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 344 4 1 4 2.8 Cc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
44273927 75194 0 None 125 2 Human 7.9 pKi = 7.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 379 9 1 3 4.2 CCCC(C)(C)C(=O)NCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL20444 75194 0 None 125 2 Human 7.9 pKi = 7.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 379 9 1 3 4.2 CCCC(C)(C)C(=O)NCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
44273924 75554 0 None 199 2 Human 7.9 pKi = 7.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 351 6 1 3 3.4 CC(C)(C)C(=O)NCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL20493 75554 0 None 199 2 Human 7.9 pKi = 7.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 351 6 1 3 3.4 CC(C)(C)C(=O)NCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
9863108 77722 0 None -12 3 Human 7.9 pKi = 7.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 347 7 1 4 2.8 COc1ccccc1N1CCN(CCCCNC(=O)C(C)(C)C)CC1 10.1016/0960-894X(96)00198-9
CHEMBL21008 77722 0 None -12 3 Human 7.9 pKi = 7.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 347 7 1 4 2.8 COc1ccccc1N1CCN(CCCCNC(=O)C(C)(C)C)CC1 10.1016/0960-894X(96)00198-9
90644057 111540 0 None 28 4 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 365 6 0 4 3.7 FC(F)(F)c1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289645 111540 0 None 28 4 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 365 6 0 4 3.7 FC(F)(F)c1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
1353 1880 85 None -3 85 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.12.054
3559 1880 85 None -3 85 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.12.054
86 1880 85 None -3 85 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.12.054
CHEMBL54 1880 85 None -3 85 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.12.054
DB00502 1880 85 None -3 85 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.12.054
10382581 100828 0 None 151 3 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2cccc(C)c2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL296506 100828 0 None 151 3 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2cccc(C)c2)CC1 10.1016/j.bmcl.2005.02.012
90644067 111528 0 None 48 3 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 380 6 0 3 3.8 [O-][S+](CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289383 111528 0 None 48 3 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 380 6 0 3 3.8 [O-][S+](CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2014.04.026
11724853 96572 0 None -1 4 Human 6.9 pKi = 6.9 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 340 0 0 4 3.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(C)c3ccccc32)CC1 10.1021/jm00043a008
CHEMBL266723 96572 0 None -1 4 Human 6.9 pKi = 6.9 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 340 0 0 4 3.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(C)c3ccccc32)CC1 10.1021/jm00043a008
12066264 14297 0 None -1 4 Human 6.9 pKi = 6.9 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 469 6 0 2 7.4 Fc1ccc(C(OC2CC3CCC(C2)N3Cc2cccc3ccccc23)c2ccc(F)cc2)cc1 10.1021/jm010146o
CHEMBL12004 14297 0 None -1 4 Human 6.9 pKi = 6.9 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 469 6 0 2 7.4 Fc1ccc(C(OC2CC3CCC(C2)N3Cc2cccc3ccccc23)c2ccc(F)cc2)cc1 10.1021/jm010146o
11849182 79459 0 None 1 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 417 9 1 7 2.7 CO/N=C(/c1ccc(Cl)cc1)C(CNOC)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
CHEMBL212288 79459 0 None 1 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 417 9 1 7 2.7 CO/N=C(/c1ccc(Cl)cc1)C(CNOC)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
49782836 17370 0 None -12 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 456 6 0 3 5.5 O=C(CCCN1CCN(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1ccc(F)cc1 10.1021/jm100899z
CHEMBL1258036 17370 0 None -12 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 456 6 0 3 5.5 O=C(CCCN1CCN(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1ccc(F)cc1 10.1021/jm100899z
49782837 17403 0 None 3 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 472 6 0 3 6.0 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
CHEMBL1258154 17403 0 None 3 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 472 6 0 3 6.0 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
11706497 77812 0 None -33 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 535 7 1 3 6.2 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm060138d
CHEMBL210461 77812 0 None -33 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 535 7 1 3 6.2 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm060138d
44436605 148531 0 None -389 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 429 7 1 3 4.3 C#Cc1ccc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.bmc.2007.08.038
CHEMBL394292 148531 0 None -389 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 429 7 1 3 4.3 C#Cc1ccc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.bmc.2007.08.038
11517928 76750 0 None 7 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 444 4 0 6 4.3 Clc1ccc(N2CCN(Cc3cn4nc(N5CCCCC5)ccc4n3)CC2)cc1Cl 10.1021/jm060166w
CHEMBL207543 76750 0 None 7 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 444 4 0 6 4.3 Clc1ccc(N2CCN(Cc3cn4nc(N5CCCCC5)ccc4n3)CC2)cc1Cl 10.1021/jm060166w
45269161 194661 0 None 5 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 336 3 0 6 2.4 Cc1cc2nc(C)c(CN3CCN(c4ccccn4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
CHEMBL562384 194661 0 None 5 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 336 3 0 6 2.4 Cc1cc2nc(C)c(CN3CCN(c4ccccn4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
44381424 58762 0 None 53 4 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 334 3 1 4 2.6 c1ccc(C2=NC[C@H](N3CCN(c4ccccc4)CC3)CCN2)cc1 10.1016/s0960-894x(03)00004-0
CHEMBL169562 58762 0 None 53 4 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 334 3 1 4 2.6 c1ccc(C2=NC[C@H](N3CCN(c4ccccc4)CC3)CCN2)cc1 10.1016/s0960-894x(03)00004-0
162669562 182120 0 None -2 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 387 6 0 4 4.2 O=C(CCCN1C2CCC1CN(c1ccc(Cl)cn1)C2)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL4789472 182120 0 None -2 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 387 6 0 4 4.2 O=C(CCCN1C2CCC1CN(c1ccc(Cl)cn1)C2)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
164623862 185423 0 None -6 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 351 6 0 5 2.8 O=C1CCc2cc(OCCCN3CCN(c4ccccn4)CC3)ccc21 10.1016/j.ejmech.2021.113243
CHEMBL4870361 185423 0 None -6 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 351 6 0 5 2.8 O=C1CCc2cc(OCCCN3CCN(c4ccccn4)CC3)ccc21 10.1016/j.ejmech.2021.113243
168270809 189455 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 392 6 1 3 4.0 Cc1cc(NC(=O)CN2CCC(OCc3ccc(F)c(F)c3)CC2)ccc1F 10.1016/j.bmcl.2022.128615
CHEMBL5172055 189455 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 392 6 1 3 4.0 Cc1cc(NC(=O)CN2CCC(OCc3ccc(F)c(F)c3)CC2)ccc1F 10.1016/j.bmcl.2022.128615
10826290 203772 0 None - 1 Human 5.9 pKi = 5.9 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 275 2 1 2 3.5 CN1CCC(c2cc(-c3ccc(Cl)cc3)[nH]n2)CC1 10.1021/jm970111h
CHEMBL80552 203772 0 None - 1 Human 5.9 pKi = 5.9 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 275 2 1 2 3.5 CN1CCC(c2cc(-c3ccc(Cl)cc3)[nH]n2)CC1 10.1021/jm970111h
21219173 93022 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 319 4 0 5 3.2 c1ccc(CN2CCC(n3nnnc3-c3ccccc3)CC2)cc1 10.1016/s0960-894x(99)00169-9
CHEMBL24603 93022 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 319 4 0 5 3.2 c1ccc(CN2CCC(n3nnnc3-c3ccccc3)CC2)cc1 10.1016/s0960-894x(99)00169-9
44319361 204007 0 None -1 4 Human 5.9 pKi = 5.9 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 337 4 0 4 3.4 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CS2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL82527 204007 0 None -1 4 Human 5.9 pKi = 5.9 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 337 4 0 4 3.4 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CS2)cc1 10.1016/s0960-894x(01)00484-x
71717830 85556 0 None 9 2 Human 5.9 pKi = 5.9 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 433 5 7 9 -0.3 OC[C@H]1O[C@H](Oc2ccc(CC3NCCc4cc(O)c(O)cc43)cc2)[C@H](O)[C@H](O)[C@H]1O 10.1016/S0960-894X(97)00194-7
CHEMBL2303762 85556 0 None 9 2 Human 5.9 pKi = 5.9 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 433 5 7 9 -0.3 OC[C@H]1O[C@H](Oc2ccc(CC3NCCc4cc(O)c(O)cc43)cc2)[C@H](O)[C@H](O)[C@H]1O 10.1016/S0960-894X(97)00194-7
44374637 54978 0 None -3 3 Human 6.9 pKi = 6.9 Binding
Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)
ChEMBL 393 7 0 4 4.5 CCCN(CCC)[C@@H]1CCc2c(OS(=O)(=O)C(F)(F)F)cccc2[C@@H]1C 10.1016/S0960-894X(01)80181-5
CHEMBL161811 54978 0 None -3 3 Human 6.9 pKi = 6.9 Binding
Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)
ChEMBL 393 7 0 4 4.5 CCCN(CCC)[C@@H]1CCc2c(OS(=O)(=O)C(F)(F)F)cccc2[C@@H]1C 10.1016/S0960-894X(01)80181-5
164623862 185423 0 None -6 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 351 6 0 5 2.8 O=C1CCc2cc(OCCCN3CCN(c4ccccn4)CC3)ccc21 10.1016/j.ejmech.2021.113243
CHEMBL4870361 185423 0 None -6 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 351 6 0 5 2.8 O=C1CCc2cc(OCCCN3CCN(c4ccccn4)CC3)ccc21 10.1016/j.ejmech.2021.113243
44591089 188892 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 3 2 3 3.3 OC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ncccc23)C1 10.1016/j.bmc.2008.12.054
CHEMBL513776 188892 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 3 2 3 3.3 OC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ncccc23)C1 10.1016/j.bmc.2008.12.054
57390695 70123 0 None -9 8 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 427 7 0 5 5.5 O=C(CCCCN1CCCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.bmc.2012.01.022
CHEMBL1946257 70123 0 None -9 8 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 427 7 0 5 5.5 O=C(CCCCN1CCCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.bmc.2012.01.022
57390695 70123 0 None -9 8 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 427 7 0 5 5.5 O=C(CCCCN1CCCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL1946257 70123 0 None -9 8 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 427 7 0 5 5.5 O=C(CCCCN1CCCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
127052778 140314 0 None -7 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 505 9 0 5 6.3 O=C(CCCCN1CCN(C(c2ccc(F)cc2)c2ccc(F)cc2)CC1)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL3819403 140314 0 None -7 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 505 9 0 5 6.3 O=C(CCCCN1CCN(C(c2ccc(F)cc2)c2ccc(F)cc2)CC1)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
164623991 184955 0 None -5 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 410 10 2 4 4.2 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4862890 184955 0 None -5 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 410 10 2 4 4.2 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
9980998 30819 0 None -1148 8 Human 5.9 pKi = 5.9 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm900095y
CHEMBL139926 30819 0 None -1148 8 Human 5.9 pKi = 5.9 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm900095y
CHEMBL2112911 30819 0 None -1148 8 Human 5.9 pKi = 5.9 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm900095y
3695490 100129 1 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 355 8 1 4 3.4 COc1ccc(OCC(O)CN2CCC(Cc3ccccc3)CC2)cc1 10.1016/S0960-894X(97)00233-3
CHEMBL29179 100129 1 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 355 8 1 4 3.4 COc1ccc(OCC(O)CN2CCC(Cc3ccccc3)CC2)cc1 10.1016/S0960-894X(97)00233-3
57345619 70120 0 None -1 7 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 360 6 0 2 5.0 Fc1ccc(CCCCN2CCCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2012.01.022
CHEMBL1946253 70120 0 None -1 7 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 360 6 0 2 5.0 Fc1ccc(CCCCN2CCCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2012.01.022
127050699 140341 0 None -1 7 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 3 0 1 4.0 Fc1ccc2c(c1)CC(CCN1CCc3ccccc3C1)C2 10.1016/j.bmc.2016.05.053
CHEMBL3819082 140341 0 None -1 7 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 3 0 1 4.0 Fc1ccc2c(c1)CC(CCN1CCc3ccccc3C1)C2 10.1016/j.bmc.2016.05.053
CHEMBL3819726 140341 0 None -1 7 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 3 0 1 4.0 Fc1ccc2c(c1)CC(CCN1CCc3ccccc3C1)C2 10.1016/j.bmc.2016.05.053
164623991 184955 0 None -5 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 410 10 2 4 4.2 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4862890 184955 0 None -5 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 410 10 2 4 4.2 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
25141533 91735 0 None -676 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 471 8 2 5 3.6 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2ccc3c(c2)Cc2ccccc2-3)CC1 10.1021/jm0704200
CHEMBL242218 91735 0 None -676 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 471 8 2 5 3.6 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2ccc3c(c2)Cc2ccccc2-3)CC1 10.1021/jm0704200
9888494 97719 0 None -549 13 Human 5.9 pKi = 5.9 Binding
Binding affinity towards cloned human dopamine D4 receptor was determinedBinding affinity towards cloned human dopamine D4 receptor was determined
ChEMBL 422 4 1 5 3.6 O=C1c2ccccc2CCCN1CCN1CCC(n2c(O)nc3cc(F)ccc32)CC1 10.1016/s0960-894x(03)00077-5
CHEMBL273921 97719 0 None -549 13 Human 5.9 pKi = 5.9 Binding
Binding affinity towards cloned human dopamine D4 receptor was determinedBinding affinity towards cloned human dopamine D4 receptor was determined
ChEMBL 422 4 1 5 3.6 O=C1c2ccccc2CCCN1CCN1CCC(n2c(O)nc3cc(F)ccc32)CC1 10.1016/s0960-894x(03)00077-5
73213196 103981 1 None -12 13 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104093 103981 1 None -12 13 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
127052778 140314 0 None -7 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 505 9 0 5 6.3 O=C(CCCCN1CCN(C(c2ccc(F)cc2)c2ccc(F)cc2)CC1)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL3819403 140314 0 None -7 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 505 9 0 5 6.3 O=C(CCCCN1CCN(C(c2ccc(F)cc2)c2ccc(F)cc2)CC1)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL5086258 213246 0 None -199 6 Human 5.9 pKi = 5.9 Binding
Binding affinity to human D4 receptor by radioligand binding assayBinding affinity to human D4 receptor by radioligand binding assay
ChEMBL None None None Cc1cc(I)cc(-c2nc(NC(=O)c3cccnc3)sc2-c2ccncc2)c1 10.1021/acsmedchemlett.1c00685
136094687 13327 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 429 7 1 6 4.2 c1ccc2c(c1)N=C(NCCCCCN1CCN(c3ccc4ccccc4n3)CC1)CO2 10.1016/S0960-894X(97)00442-3
CHEMBL1192972 13327 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 429 7 1 6 4.2 c1ccc2c(c1)N=C(NCCCCCN1CCN(c3ccc4ccccc4n3)CC1)CO2 10.1016/S0960-894X(97)00442-3
CHEMBL544296 13327 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 429 7 1 6 4.2 c1ccc2c(c1)N=C(NCCCCCN1CCN(c3ccc4ccccc4n3)CC1)CO2 10.1016/S0960-894X(97)00442-3
15467373 101384 0 None 60 4 Human 6.9 pKi = 6.9 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 351 4 1 4 3.4 N#CC(C#N)=Cc1[nH]ccc1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(99)00302-9
CHEMBL300553 101384 0 None 60 4 Human 6.9 pKi = 6.9 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 351 4 1 4 3.4 N#CC(C#N)=Cc1[nH]ccc1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(99)00302-9
44273715 72776 0 None 15 2 Human 6.9 pKi = 6.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 337 7 1 3 3.0 CC(C)C(=O)NCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL20114 72776 0 None 15 2 Human 6.9 pKi = 6.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 337 7 1 3 3.0 CC(C)C(=O)NCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
44273877 98281 0 None 15 2 Human 6.9 pKi = 6.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 335 6 1 3 2.9 CC(C)(C)C(=O)NCCCCN1CCN(c2ccc(F)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL277937 98281 0 None 15 2 Human 6.9 pKi = 6.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 335 6 1 3 2.9 CC(C)(C)C(=O)NCCCCN1CCN(c2ccc(F)cc2)CC1 10.1016/0960-894X(96)00198-9
44273553 98332 0 None 3 2 Human 6.9 pKi = 6.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 365 7 1 3 3.8 CC(C)(C)C(=O)NCCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL278288 98332 0 None 3 2 Human 6.9 pKi = 6.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 365 7 1 3 3.8 CC(C)(C)C(=O)NCCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
134155461 153950 0 None -1 6 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 291 4 1 2 3.6 c1ccc2c(c1)CCN(CCCc1nc3ccccc3[nH]1)C2 10.1016/j.bmc.2016.09.019
CHEMBL3959209 153950 0 None -1 6 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 291 4 1 2 3.6 c1ccc2c(c1)CCN(CCCc1nc3ccccc3[nH]1)C2 10.1016/j.bmc.2016.09.019
CHEMBL3990475 153950 0 None -1 6 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 291 4 1 2 3.6 c1ccc2c(c1)CCN(CCCc1nc3ccccc3[nH]1)C2 10.1016/j.bmc.2016.09.019
44273552 79520 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 309 6 1 3 2.4 CC(=O)NCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL21252 79520 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 309 6 1 3 2.4 CC(=O)NCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
9827938 11666 0 None -50 12 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpirideBinding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpiride
ChEMBL 517 13 1 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL1181680 11666 0 None -50 12 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpirideBinding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpiride
ChEMBL 517 13 1 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL188486 11666 0 None -50 12 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpirideBinding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpiride
ChEMBL 517 13 1 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
57402951 70124 0 None 2 4 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 413 6 0 5 5.1 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.bmc.2012.01.022
CHEMBL1946258 70124 0 None 2 4 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 413 6 0 5 5.1 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.bmc.2012.01.022
57402951 70124 0 None 2 4 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 413 6 0 5 5.1 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL1946258 70124 0 None 2 4 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 413 6 0 5 5.1 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL5071238 212482 0 None -10 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCc1cccc(N2CCN(CC(O)CCNCCC(C(=O)N(C)C)(c3ccccc3)c3ccccc3)CC2)c1Cl 10.1021/acs.jmedchem.1c00611
CHEMBL5070377 212464 0 None -251 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CN(C)C(=O)C(CCNCCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
11335419 66764 1 None -125 6 Human 5.9 pKi = 5.9 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 295 7 0 2 4.1 c1ccc(Cc2ccccc2OCCCN2CCCC2)cc1 10.1021/jm049720x
CHEMBL187367 66764 1 None -125 6 Human 5.9 pKi = 5.9 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 295 7 0 2 4.1 c1ccc(Cc2ccccc2OCCCN2CCCC2)cc1 10.1021/jm049720x
134155461 153950 0 None -1 6 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 291 4 1 2 3.6 c1ccc2c(c1)CCN(CCCc1nc3ccccc3[nH]1)C2 10.1016/j.bmc.2016.09.019
CHEMBL3959209 153950 0 None -1 6 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 291 4 1 2 3.6 c1ccc2c(c1)CCN(CCCc1nc3ccccc3[nH]1)C2 10.1016/j.bmc.2016.09.019
CHEMBL3990475 153950 0 None -1 6 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 291 4 1 2 3.6 c1ccc2c(c1)CCN(CCCc1nc3ccccc3[nH]1)C2 10.1016/j.bmc.2016.09.019
44376921 57027 0 None 2 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 382 5 0 7 2.2 COC(=O)c1ccc(OC[C@@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL165113 57027 0 None 2 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 382 5 0 7 2.2 COC(=O)c1ccc(OC[C@@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
49783415 17496 0 None -1698 13 Rat 5.9 pKi = 5.9 Binding
Binding affinity to rat dopamine D4 receptorBinding affinity to rat dopamine D4 receptor
ChEMBL 320 7 1 5 2.9 CCCCN1CCC(COC(=O)c2ccc(N)c(OC)c2)CC1 10.1021/jm100668r
CHEMBL1258452 17496 0 None -1698 13 Rat 5.9 pKi = 5.9 Binding
Binding affinity to rat dopamine D4 receptorBinding affinity to rat dopamine D4 receptor
ChEMBL 320 7 1 5 2.9 CCCCN1CCC(COC(=O)c2ccc(N)c(OC)c2)CC1 10.1021/jm100668r
134133968 153986 0 None -4 9 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 356 5 0 3 5.3 Clc1cccc2c1CN(CCCCc1nc3ccccc3s1)CC2 10.1016/j.bmc.2016.09.019
CHEMBL3899099 153986 0 None -4 9 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 356 5 0 3 5.3 Clc1cccc2c1CN(CCCCc1nc3ccccc3s1)CC2 10.1016/j.bmc.2016.09.019
CHEMBL3990801 153986 0 None -4 9 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 356 5 0 3 5.3 Clc1cccc2c1CN(CCCCc1nc3ccccc3s1)CC2 10.1016/j.bmc.2016.09.019
10476504 33268 1 None -1 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm0611152
CHEMBL142020 33268 1 None -1 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm0611152
11663604 82760 0 None -10 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 520 13 1 8 3.6 CCCc1c(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)nnn1Cc1ccc(OC)cc1 10.1021/jm0611152
CHEMBL218351 82760 0 None -10 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 520 13 1 8 3.6 CCCc1c(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)nnn1Cc1ccc(OC)cc1 10.1021/jm0611152
155539605 172276 0 None -5 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 receptor by radioligand binding assay
ChEMBL 313 1 0 4 2.1 CC1=NC2(CCN(C)CC2)C(=O)N(c2c(C)cccc2C)C1=O 10.1016/j.ejmech.2018.12.048
CHEMBL4514672 172276 0 None -5 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 receptor by radioligand binding assay
ChEMBL 313 1 0 4 2.1 CC1=NC2(CCN(C)CC2)C(=O)N(c2c(C)cccc2C)C1=O 10.1016/j.ejmech.2018.12.048
46912548 14278 0 None -144 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 462 4 2 3 4.3 COc1ccc2[nH]cc(CN3CCC(O)(c4ccc(I)cc4)CC3)c2c1 10.1016/j.bmc.2010.05.052
CHEMBL1173288 14278 0 None -144 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 462 4 2 3 4.3 COc1ccc2[nH]cc(CN3CCC(O)(c4ccc(I)cc4)CC3)c2c1 10.1016/j.bmc.2010.05.052
CHEMBL1200271 14278 0 None -144 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 462 4 2 3 4.3 COc1ccc2[nH]cc(CN3CCC(O)(c4ccc(I)cc4)CC3)c2c1 10.1016/j.bmc.2010.05.052
44438210 92939 2 None -1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 382 4 2 2 5.3 OC1(c2ccc(-c3ccccc3)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL245615 92939 2 None -1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 382 4 2 2 5.3 OC1(c2ccc(-c3ccccc3)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
134133968 153986 0 None -4 9 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 356 5 0 3 5.3 Clc1cccc2c1CN(CCCCc1nc3ccccc3s1)CC2 10.1016/j.bmc.2016.09.019
CHEMBL3899099 153986 0 None -4 9 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 356 5 0 3 5.3 Clc1cccc2c1CN(CCCCc1nc3ccccc3s1)CC2 10.1016/j.bmc.2016.09.019
CHEMBL3990801 153986 0 None -4 9 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 356 5 0 3 5.3 Clc1cccc2c1CN(CCCCc1nc3ccccc3s1)CC2 10.1016/j.bmc.2016.09.019
42625293 55956 0 None -316 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 549 8 2 6 3.3 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3cc(I)ccc3o2)CC1 10.1021/jm900095y
CHEMBL1627319 55956 0 None -316 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 549 8 2 6 3.3 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3cc(I)ccc3o2)CC1 10.1021/jm900095y
44330292 4441 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 232 0 0 3 3.3 Cc1sc(C)c2c1CCCc1ncn(C)c1-2 10.1016/s0960-894x(03)00587-0
CHEMBL102162 4441 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 232 0 0 3 3.3 Cc1sc(C)c2c1CCCc1ncn(C)c1-2 10.1016/s0960-894x(03)00587-0
44330515 206657 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 246 0 1 2 3.9 Cc1sc(C)c2c1CC(C)(C)Cc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
CHEMBL99654 206657 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 246 0 1 2 3.9 Cc1sc(C)c2c1CC(C)(C)Cc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
154706711 175941 1 None -47 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 432 11 1 2 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4439535 175941 1 None -47 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 432 11 1 2 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4596930 175941 1 None -47 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 432 11 1 2 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
10760813 163537 5 None 9 3 Human 7.9 pKi = 7.9 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 357 4 1 2 5.5 Clc1ccc(-c2cc(C3CCN(CC4CCCCC4)CC3)[nH]n2)cc1 10.1021/jm970111h
CHEMBL420954 163537 5 None 9 3 Human 7.9 pKi = 7.9 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 357 4 1 2 5.5 Clc1ccc(-c2cc(C3CCN(CC4CCCCC4)CC3)[nH]n2)cc1 10.1021/jm970111h
44264623 203304 0 None 407 4 Human 7.9 pKi = 7.9 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnc4ccccn34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL7686 203304 0 None 407 4 Human 7.9 pKi = 7.9 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnc4ccccn34)CC2)cc1 10.1016/s0960-894x(98)00692-1
44336138 4804 0 None 75 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 419 6 0 4 3.2 O=S1(=O)Cc2ccccc2N1CCCN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104380 4804 0 None 75 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 419 6 0 4 3.2 O=S1(=O)Cc2ccccc2N1CCCN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
90644067 111528 0 None 48 3 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 380 6 0 3 3.8 [O-][S+](CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289383 111528 0 None 48 3 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 380 6 0 3 3.8 [O-][S+](CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2014.04.026
90644060 111539 0 None 64 4 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 358 4 0 2 4.4 Fc1ccc2c(c1)CC(CCN1CCN(c3ccc(Cl)cc3)CC1)C2 10.1016/j.bmc.2014.04.026
CHEMBL3289644 111539 0 None 64 4 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 358 4 0 2 4.4 Fc1ccc2c(c1)CC(CCN1CCN(c3ccc(Cl)cc3)CC1)C2 10.1016/j.bmc.2014.04.026
135398737 944 89 None -13 91 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/S0960-894X(97)00218-7
38 944 89 None -13 91 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/S0960-894X(97)00218-7
722 944 89 None -13 91 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/S0960-894X(97)00218-7
CHEMBL42 944 89 None -13 91 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/S0960-894X(97)00218-7
DB00363 944 89 None -13 91 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/S0960-894X(97)00218-7
53363110 63520 0 None 4 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 507 14 0 8 4.8 CCCCn1cc(CCCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
CHEMBL1803050 63520 0 None 4 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 507 14 0 8 4.8 CCCCn1cc(CCCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
24936042 157047 0 None 1 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccn3nccc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4080762 157047 0 None 1 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccn3nccc3c2)CC1 10.1021/acs.jmedchem.6b01857
6603820 95330 13 None -1 13 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from rat dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from rat dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1016/j.bmc.2009.08.028
CHEMBL25856 95330 13 None -1 13 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from rat dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from rat dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1016/j.bmc.2009.08.028
11428416 5223 0 None - 1 Human 7.9 pKi = 7.9 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 361 7 0 4 4.0 CCOc1ccccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL106599 5223 0 None - 1 Human 7.9 pKi = 7.9 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 361 7 0 4 4.0 CCOc1ccccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
11406804 163910 0 None - 1 Human 7.9 pKi = 7.9 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 395 7 0 4 4.7 CCOc1cc(Cl)ccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL421403 163910 0 None - 1 Human 7.9 pKi = 7.9 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 395 7 0 4 4.7 CCOc1cc(Cl)ccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
127029386 138867 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccc(F)cc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793375 138867 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccc(F)cc3)C2)cc1 10.1016/j.bmcl.2016.03.102
11772767 79592 0 None 7 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 358 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(Cl)c1 10.1021/jm060279f
CHEMBL212784 79592 0 None 7 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 358 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(Cl)c1 10.1021/jm060279f
164628817 185695 0 None -2 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 349 6 0 4 3.4 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc2c(c1)CCC2 10.1016/j.ejmech.2021.113243
CHEMBL4874069 185695 0 None -2 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 349 6 0 4 3.4 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc2c(c1)CCC2 10.1016/j.ejmech.2021.113243
11849775 165643 0 None 7 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 342 6 0 5 2.8 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(F)c1 10.1021/jm060279f
CHEMBL426510 165643 0 None 7 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 342 6 0 5 2.8 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(F)c1 10.1021/jm060279f
44340376 110157 0 None 6 4 Human 6.9 pKi = 6.9 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 452 6 1 3 4.9 COc1c(C(=O)NC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL325818 110157 0 None 6 4 Human 6.9 pKi = 6.9 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 452 6 1 3 4.9 COc1c(C(=O)NC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
10476504 33268 1 None -1 7 Human 6.9 pKi = 6.9 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
CHEMBL142020 33268 1 None -1 7 Human 6.9 pKi = 6.9 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
44403214 72148 0 None -9 5 Human 6.9 pKi = 6.9 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 386 8 1 5 2.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(F)nc2)CC1 10.1016/j.bmcl.2005.07.037
CHEMBL198993 72148 0 None -9 5 Human 6.9 pKi = 6.9 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 386 8 1 5 2.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(F)nc2)CC1 10.1016/j.bmcl.2005.07.037
44393393 123156 0 None -91 5 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 537 7 1 4 5.0 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(I)s1 10.1016/j.bmcl.2004.05.052
CHEMBL362101 123156 0 None -91 5 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 537 7 1 4 5.0 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(I)s1 10.1016/j.bmcl.2004.05.052
44381147 58421 0 None -3 4 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@@H]1CN(Cc2ccccc2)C[C@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
CHEMBL168544 58421 0 None -3 4 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@@H]1CN(Cc2ccccc2)C[C@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
55445 98096 16 None -1 4 Human 6.9 pKi = 6.9 Binding
Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone
ChEMBL 219 3 1 2 3.0 CCCN1CCCC(c2cccc(O)c2)C1 10.1021/jm00073a021
CHEMBL276500 98096 16 None -1 4 Human 6.9 pKi = 6.9 Binding
Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone
ChEMBL 219 3 1 2 3.0 CCCN1CCCC(c2cccc(O)c2)C1 10.1021/jm00073a021
154724369 176115 1 None -3 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 484 12 0 6 6.1 CCCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4584372 176115 1 None -3 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 484 12 0 6 6.1 CCCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4598389 176115 1 None -3 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 484 12 0 6 6.1 CCCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
127031829 138898 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 352 6 1 4 3.5 COc1ccc2[nH]cc(CN3CCO[C@H](COc4ccccc4)C3)c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3793890 138898 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 352 6 1 4 3.5 COc1ccc2[nH]cc(CN3CCO[C@H](COc4ccccc4)C3)c2c1 10.1016/j.bmcl.2016.03.102
127028182 138932 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 336 5 0 4 3.2 Fc1cccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)n1 10.1016/j.bmcl.2016.03.102
CHEMBL3794158 138932 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 336 5 0 4 3.2 Fc1cccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)n1 10.1016/j.bmcl.2016.03.102
11370781 79461 0 None 14 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 325 6 0 6 2.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccnc1 10.1021/jm060279f
CHEMBL212291 79461 0 None 14 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 325 6 0 6 2.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccnc1 10.1021/jm060279f
25071066 111282 0 None -18 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c1Cl 10.1021/jm5004039
CHEMBL3287390 111282 0 None -18 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c1Cl 10.1021/jm5004039
56837634 68964 0 None -295 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1041 38 2 15 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928130 68964 0 None -295 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1041 38 2 15 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
118709172 112920 0 None -2 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 493 8 0 4 6.6 Cc1ccc(C(=O)OC2(c3ccc(Cl)cc3)CCN(CCCC(=O)c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2014.06.079
CHEMBL3318844 112920 0 None -2 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 493 8 0 4 6.6 Cc1ccc(C(=O)OC2(c3ccc(Cl)cc3)CCN(CCCC(=O)c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2014.06.079
137655029 158400 0 None -31 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 452 8 1 9 2.6 O=Cc1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCCO5)CC3)cc12 10.1016/j.bmc.2017.08.037
CHEMBL4095881 158400 0 None -31 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 452 8 1 9 2.6 O=Cc1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCCO5)CC3)cc12 10.1016/j.bmc.2017.08.037
9995378 5399 0 None 25 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 307 4 0 4 4.0 c1ccc(CN2CCC(n3ccc(-c4cnco4)c3)CC2)cc1 10.1016/s0960-894x(99)00540-5
CHEMBL107529 5399 0 None 25 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 307 4 0 4 4.0 c1ccc(CN2CCC(n3ccc(-c4cnco4)c3)CC2)cc1 10.1016/s0960-894x(99)00540-5
276 3457 45 None -87 13 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptorDisplacement of [3H]spiperone from human cloned dopamine D4 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2007.11.045
5312149 3457 45 None -87 13 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptorDisplacement of [3H]spiperone from human cloned dopamine D4 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2007.11.045
CHEMBL431298 3457 45 None -87 13 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptorDisplacement of [3H]spiperone from human cloned dopamine D4 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2007.11.045
10476504 33268 1 None -1 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm900690y
CHEMBL142020 33268 1 None -1 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm900690y
122189388 122727 0 None -25 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 483 7 0 8 3.8 O=Cc1cnn2ccc(-n3cc(CCCN4CCN(c5cccc(Cl)c5Cl)CC4)nn3)cc12 10.1016/j.bmc.2015.07.050
CHEMBL3613874 122727 0 None -25 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 483 7 0 8 3.8 O=Cc1cnn2ccc(-n3cc(CCCN4CCN(c5cccc(Cl)c5Cl)CC4)nn3)cc12 10.1016/j.bmc.2015.07.050
119570 3110 90 None -10 40 Human 6.9 pKi = 6.9 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm0503805
2233 3110 90 None -10 40 Human 6.9 pKi = 6.9 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm0503805
953 3110 90 None -10 40 Human 6.9 pKi = 6.9 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm0503805
CHEMBL301265 3110 90 None -10 40 Human 6.9 pKi = 6.9 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm0503805
DB00413 3110 90 None -10 40 Human 6.9 pKi = 6.9 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm0503805
119570 3110 90 None -10 40 Human 6.9 pKi = 6.9 Binding
Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsLow inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
2233 3110 90 None -10 40 Human 6.9 pKi = 6.9 Binding
Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsLow inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
953 3110 90 None -10 40 Human 6.9 pKi = 6.9 Binding
Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsLow inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
CHEMBL301265 3110 90 None -10 40 Human 6.9 pKi = 6.9 Binding
Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsLow inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
DB00413 3110 90 None -10 40 Human 6.9 pKi = 6.9 Binding
Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsLow inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
11077918 204868 0 None 7 4 Human 5.9 pKi = 5.9 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cccc4ccnn34)CC2)cc1 10.1021/jm015522j
CHEMBL88937 204868 0 None 7 4 Human 5.9 pKi = 5.9 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cccc4ccnn34)CC2)cc1 10.1021/jm015522j
11077918 204868 0 None 7 4 Human 5.9 pKi = 5.9 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cccc4ccnn34)CC2)cc1 10.1021/jm049612a
CHEMBL88937 204868 0 None 7 4 Human 5.9 pKi = 5.9 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cccc4ccnn34)CC2)cc1 10.1021/jm049612a
10021692 145849 12 None -1698 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 364 10 1 4 3.0 C=CCN1CCC[C@H]1CNC(=O)c1cc(CCCF)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
CHEMBL392158 145849 12 None -1698 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 364 10 1 4 3.0 C=CCN1CCC[C@H]1CNC(=O)c1cc(CCCF)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
11708363 71558 1 None -5 4 Human 4.9 pKi = 4.9 Binding
Binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandBinding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 221 5 0 3 2.3 CCCN(CCC)[C@@H]1CCn2nccc2C1 10.1021/jm0503805
CHEMBL197159 71558 1 None -5 4 Human 4.9 pKi = 4.9 Binding
Binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandBinding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 221 5 0 3 2.3 CCCN(CCC)[C@@H]1CCn2nccc2C1 10.1021/jm0503805
76336022 105898 0 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 386 6 1 5 3.3 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3115581 105898 0 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 386 6 1 5 3.3 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139316 105898 0 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 386 6 1 5 3.3 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
136094866 40718 0 None 1 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 423 3 2 5 5.3 Cc1ccc2c(c1)C(NC1CC3CCC(C1)N3Cc1ccccc1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL148694 40718 0 None 1 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 423 3 2 5 5.3 Cc1ccc2c(c1)C(NC1CC3CCC(C1)N3Cc1ccccc1)=Nc1cccnc1N2 10.1021/jm0104825
127051516 140326 0 None -5 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 420 6 1 5 4.0 O=C1NCN(c2ccccc2)C12CCN(CCCCc1nc3ccccc3s1)CC2 10.1016/j.bmc.2016.06.011
CHEMBL3819567 140326 0 None -5 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 420 6 1 5 4.0 O=C1NCN(c2ccccc2)C12CCN(CCCCc1nc3ccccc3s1)CC2 10.1016/j.bmc.2016.06.011
56678599 66089 0 None 1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 428 7 2 4 4.4 O=C1CCc2ccc(OCCCCN3CCC(O)(c4ccc(Cl)cc4)CC3)cc2N1 10.1016/j.bmc.2011.04.021
CHEMBL1813586 66089 0 None 1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 428 7 2 4 4.4 O=C1CCc2ccc(OCCCCN3CCC(O)(c4ccc(Cl)cc4)CC3)cc2N1 10.1016/j.bmc.2011.04.021
CHEMBL1851900 66089 0 None 1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 428 7 2 4 4.4 O=C1CCc2ccc(OCCCCN3CCC(O)(c4ccc(Cl)cc4)CC3)cc2N1 10.1016/j.bmc.2011.04.021
154725001 176073 1 None -85 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 2 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4525624 176073 1 None -85 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 2 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4598002 176073 1 None -85 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 2 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
145980875 166154 0 None 3 11 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
ChEMBL 443 7 1 2 6.2 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCCc2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL4282702 166154 0 None 3 11 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
ChEMBL 443 7 1 2 6.2 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCCc2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
127051516 140326 0 None -5 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 420 6 1 5 4.0 O=C1NCN(c2ccccc2)C12CCN(CCCCc1nc3ccccc3s1)CC2 10.1016/j.bmc.2016.06.011
CHEMBL3819567 140326 0 None -5 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 420 6 1 5 4.0 O=C1NCN(c2ccccc2)C12CCN(CCCCc1nc3ccccc3s1)CC2 10.1016/j.bmc.2016.06.011
71062646 149011 0 None -218 13 Mouse 6.9 pKi = 6.9 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 338 6 0 4 2.8 c1ccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)cc1 nan
CHEMBL3946661 149011 0 None -218 13 Mouse 6.9 pKi = 6.9 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 338 6 0 4 2.8 c1ccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)cc1 nan
154727713 175790 1 None -1 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 426 10 1 6 4.5 COc1ccc(F)cc1C1CC1CNCCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4514586 175790 1 None -1 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 426 10 1 6 4.5 COc1ccc(F)cc1C1CC1CNCCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4595727 175790 1 None -1 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 426 10 1 6 4.5 COc1ccc(F)cc1C1CC1CNCCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
168287664 191056 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3cn4ccccc4n3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
CHEMBL5196102 191056 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3cn4ccccc4n3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
154703922 175715 1 None -676 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4590211 175715 1 None -676 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4595146 175715 1 None -676 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
44335972 109259 0 None 38 2 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 5 0 3 3.5 CC1Cc2ccccc2N1C(=O)CN1CCN(CCc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL323022 109259 0 None 38 2 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 5 0 3 3.5 CC1Cc2ccccc2N1C(=O)CN1CCN(CCc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
44355355 23977 0 None 1 3 Human 6.9 pKi = 6.9 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 329 7 0 3 4.6 CCCN(CCc1cccs1)[C@H]1CCc2ccc(OC)cc2C1 10.1021/jm960345l
CHEMBL133938 23977 0 None 1 3 Human 6.9 pKi = 6.9 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 329 7 0 3 4.6 CCCN(CCc1cccs1)[C@H]1CCc2ccc(OC)cc2C1 10.1021/jm960345l
11849816 77725 0 None -5 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 357 6 0 4 4.4 CO/N=C(\CCN1CCC(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL210101 77725 0 None -5 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 357 6 0 4 4.4 CO/N=C(\CCN1CCC(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
5249956 73048 1 None -70 6 Human 6.9 pKi = 6.9 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1021/jm050846j
CHEMBL201525 73048 1 None -70 6 Human 6.9 pKi = 6.9 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1021/jm050846j
164611932 184619 0 None -33 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 364 6 1 4 3.1 O=C1CCc2cc(CCCCN3CCN(c4ccccn4)CC3)ccc2N1 10.1016/j.ejmech.2021.113243
CHEMBL4857597 184619 0 None -33 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 364 6 1 4 3.1 O=C1CCc2cc(CCCCN3CCN(c4ccccn4)CC3)ccc2N1 10.1016/j.ejmech.2021.113243
168273063 189691 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(CO[C@H]2CCCN(Cc3ncn4ccccc34)C2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5175728 189691 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(CO[C@H]2CCCN(Cc3ncn4ccccc34)C2)c1 10.1016/j.bmcl.2022.128615
11028157 201033 0 None -128 4 Human 5.9 pKi = 5.9 Binding
Binding affinity for human dopamine receptor D4 using [125I]IABN as radioligandBinding affinity for human dopamine receptor D4 using [125I]IABN as radioligand
ChEMBL 563 8 1 4 6.3 COc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(Br)c2ccccc12 10.1016/j.bmcl.2003.09.083
CHEMBL61789 201033 0 None -128 4 Human 5.9 pKi = 5.9 Binding
Binding affinity for human dopamine receptor D4 using [125I]IABN as radioligandBinding affinity for human dopamine receptor D4 using [125I]IABN as radioligand
ChEMBL 563 8 1 4 6.3 COc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(Br)c2ccccc12 10.1016/j.bmcl.2003.09.083
10183626 12937 0 None -44 3 Human 5.9 pKi = 5.9 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 469 9 0 4 6.2 Fc1ccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)cc1 10.1016/s0960-894x(02)00179-8
CHEMBL1190010 12937 0 None -44 3 Human 5.9 pKi = 5.9 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 469 9 0 4 6.2 Fc1ccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)cc1 10.1016/s0960-894x(02)00179-8
CHEMBL539999 12937 0 None -44 3 Human 5.9 pKi = 5.9 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 469 9 0 4 6.2 Fc1ccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)cc1 10.1016/s0960-894x(02)00179-8
127052466 140255 0 None -8 2 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 320 5 0 3 3.1 O=C1c2ccccc2C(=O)N1CCCCN1Cc2ccccc2C1 10.1016/j.bmc.2016.05.053
CHEMBL3818669 140255 0 None -8 2 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 320 5 0 3 3.1 O=C1c2ccccc2C(=O)N1CCCCN1Cc2ccccc2C1 10.1016/j.bmc.2016.05.053
163322330 190106 3 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5182191 190106 3 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
145968810 164486 0 None -5 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 381 8 2 4 3.5 CN(C)c1ccc(C(=O)NCCCCN2CCC(c3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2018.03.084
CHEMBL4226226 164486 0 None -5 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 381 8 2 4 3.5 CN(C)c1ccc(C(=O)NCCCCN2CCC(c3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2018.03.084
56658006 66038 0 None -4 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 468 7 2 5 4.4 O=C1CCc2ccc(OCCCCN3CCC(n4c(=O)[nH]c5cc(Cl)ccc54)CC3)cc2N1 10.1016/j.bmc.2011.04.021
CHEMBL1813588 66038 0 None -4 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 468 7 2 5 4.4 O=C1CCc2ccc(OCCCCN3CCC(n4c(=O)[nH]c5cc(Cl)ccc54)CC3)cc2N1 10.1016/j.bmc.2011.04.021
CHEMBL1851643 66038 0 None -4 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 468 7 2 5 4.4 O=C1CCc2ccc(OCCCCN3CCC(n4c(=O)[nH]c5cc(Cl)ccc54)CC3)cc2N1 10.1016/j.bmc.2011.04.021
44436300 148304 0 None -10 4 Human 6.9 pKi = 6.9 Binding
Binding affinity to human D4RBinding affinity to human D4R
ChEMBL 399 6 0 5 2.4 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2ccccc2)CC1 10.1016/j.bmcl.2021.128028
CHEMBL394110 148304 0 None -10 4 Human 6.9 pKi = 6.9 Binding
Binding affinity to human D4RBinding affinity to human D4R
ChEMBL 399 6 0 5 2.4 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2ccccc2)CC1 10.1016/j.bmcl.2021.128028
44438206 146676 3 None 3 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 322 3 3 3 3.4 Oc1ccc(C2(O)CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.10.076
CHEMBL392823 146676 3 None 3 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 322 3 3 3 3.4 Oc1ccc(C2(O)CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.10.076
44336046 4737 0 None 3 2 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 398 4 0 2 3.6 C[C@@H]1CN(Cc2ccc(Cl)cc2)CC[N@@+]1(C)CC(=O)N1CCc2ccccc21 10.1016/s0960-894x(02)00655-8
CHEMBL104138 4737 0 None 3 2 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 398 4 0 2 3.6 C[C@@H]1CN(Cc2ccc(Cl)cc2)CC[N@@+]1(C)CC(=O)N1CCc2ccccc21 10.1016/s0960-894x(02)00655-8
127052466 140255 0 None -8 2 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 320 5 0 3 3.1 O=C1c2ccccc2C(=O)N1CCCCN1Cc2ccccc2C1 10.1016/j.bmc.2016.05.053
CHEMBL3818669 140255 0 None -8 2 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 320 5 0 3 3.1 O=C1c2ccccc2C(=O)N1CCCCN1Cc2ccccc2C1 10.1016/j.bmc.2016.05.053
44332701 4495 0 None -35 4 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 360 8 2 5 2.9 CS(=O)(=O)Nc1cc(OCCNCc2cccs2)ccc1Cl 10.1016/s0960-894x(98)00014-6
CHEMBL102490 4495 0 None -35 4 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 360 8 2 5 2.9 CS(=O)(=O)Nc1cc(OCCNCc2cccs2)ccc1Cl 10.1016/s0960-894x(98)00014-6
10276451 198601 33 None -2754 10 Human 5.9 pKi = 5.9 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm900095y
CHEMBL2112910 198601 33 None -2754 10 Human 5.9 pKi = 5.9 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm900095y
CHEMBL59725 198601 33 None -2754 10 Human 5.9 pKi = 5.9 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm900095y
73213196 103981 1 None -12 13 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104093 103981 1 None -12 13 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
44330514 206655 0 None 3 2 Human 6.9 pKi = 6.9 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 260 1 0 3 4.3 Cc1sc(C)c2c1CCCc1cnn(C(C)C)c1-2 10.1016/s0960-894x(03)00587-0
CHEMBL99649 206655 0 None 3 2 Human 6.9 pKi = 6.9 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 260 1 0 3 4.3 Cc1sc(C)c2c1CCCc1cnn(C(C)C)c1-2 10.1016/s0960-894x(03)00587-0
119570 3110 90 None -10 40 Human 6.9 pKi = 6.9 Binding
in vitro low binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro low binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
2233 3110 90 None -10 40 Human 6.9 pKi = 6.9 Binding
in vitro low binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro low binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
953 3110 90 None -10 40 Human 6.9 pKi = 6.9 Binding
in vitro low binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro low binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
CHEMBL301265 3110 90 None -10 40 Human 6.9 pKi = 6.9 Binding
in vitro low binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro low binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
DB00413 3110 90 None -10 40 Human 6.9 pKi = 6.9 Binding
in vitro low binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro low binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
11026289 109046 0 None -3 3 Human 5.9 pKi = 5.9 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 425 6 1 4 3.8 O=C(NCCCN1CCN(c2ccccc2)CC1)c1cccc2c1-c1ccccc1C2=O 10.1021/jm010146o
CHEMBL322179 109046 0 None -3 3 Human 5.9 pKi = 5.9 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 425 6 1 4 3.8 O=C(NCCCN1CCN(c2ccccc2)CC1)c1cccc2c1-c1ccccc1C2=O 10.1021/jm010146o
155532148 171135 0 None -794 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting
ChEMBL 444 6 0 5 4.2 COc1ccccc1N1CCN(CC2COCC(c3ccccc3)(c3ccccc3)O2)CC1 10.1016/j.ejmech.2019.02.056
CHEMBL4466677 171135 0 None -794 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting
ChEMBL 444 6 0 5 4.2 COc1ccccc1N1CCN(CC2COCC(c3ccccc3)(c3ccccc3)O2)CC1 10.1016/j.ejmech.2019.02.056
CHEMBL5082465 213032 0 None -239 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCOC(=O)/C=C1\[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2CCCCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.1c00611
44336062 5135 0 None 67 2 Human 6.9 pKi = 6.9 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 383 4 0 3 3.4 C[C@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL106119 5135 0 None 67 2 Human 6.9 pKi = 6.9 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 383 4 0 3 3.4 C[C@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00656-x
35296170 141808 4 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 5 1 2 4.3 O=C(NC1CCN(CCc2ccccc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.096
CHEMBL388620 141808 4 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 5 1 2 4.3 O=C(NC1CCN(CCc2ccccc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.096
49799695 14283 0 None -58 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 376 4 2 4 3.7 COc1cccc2[nH]cc(CN3CCC(n4c(=O)[nH]c5ccccc54)CC3)c12 10.1016/j.bmc.2010.05.052
CHEMBL1173436 14283 0 None -58 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 376 4 2 4 3.7 COc1cccc2[nH]cc(CN3CCC(n4c(=O)[nH]c5ccccc54)CC3)c12 10.1016/j.bmc.2010.05.052
CHEMBL1200285 14283 0 None -58 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 376 4 2 4 3.7 COc1cccc2[nH]cc(CN3CCC(n4c(=O)[nH]c5ccccc54)CC3)c12 10.1016/j.bmc.2010.05.052
CHEMBL5090346 213483 0 None -11 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None N#CC(CCNCCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
130431318 171817 2 None -1905 5 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 484 9 3 5 3.7 CCc1cc(Cl)c(OC)c(N2CCN(CC(O)CCNC(=O)c3cc4ccccc4[nH]3)CC2)c1 10.1021/acs.jmedchem.6b00860
CHEMBL4476394 171817 2 None -1905 5 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 484 9 3 5 3.7 CCc1cc(Cl)c(OC)c(N2CCN(CC(O)CCNC(=O)c3cc4ccccc4[nH]3)CC2)c1 10.1021/acs.jmedchem.6b00860
168293190 191532 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 363 5 0 2 5.5 Cc1ccc(CO[C@H]2CCCN(Cc3ccc(Cl)c(Cl)c3)C2)cc1 10.1016/j.bmcl.2022.128615
CHEMBL5203595 191532 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 363 5 0 2 5.5 Cc1ccc(CO[C@H]2CCCN(Cc3ccc(Cl)c(Cl)c3)C2)cc1 10.1016/j.bmcl.2022.128615
11036641 31562 0 None -1 4 Human 7.9 pKi = 7.9 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 393 7 1 6 2.3 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
CHEMBL140612 31562 0 None -1 4 Human 7.9 pKi = 7.9 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 393 7 1 6 2.3 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
10473658 186610 3 None 38 3 Human 7.9 pKi = 7.9 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1021/jm970021c
CHEMBL49231 186610 3 None 38 3 Human 7.9 pKi = 7.9 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1021/jm970021c
44330567 206540 0 None 29 2 Human 7.9 pKi = 7.9 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 272 0 0 3 3.9 Cn1ncc2c1-c1c(Cl)sc(Cl)c1CCC2 10.1016/s0960-894x(03)00587-0
CHEMBL98946 206540 0 None 29 2 Human 7.9 pKi = 7.9 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 272 0 0 3 3.9 Cn1ncc2c1-c1c(Cl)sc(Cl)c1CCC2 10.1016/s0960-894x(03)00587-0
44336036 4807 0 None 416 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 C[C@@H]1CN(Cc2ccc(Cl)cc2)CCN1CC(=O)N1CCc2ccccc21 10.1016/s0960-894x(02)00655-8
CHEMBL104399 4807 0 None 416 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 C[C@@H]1CN(Cc2ccc(Cl)cc2)CCN1CC(=O)N1CCc2ccccc21 10.1016/s0960-894x(02)00655-8
9841249 16218 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 348 3 0 4 3.7 Cc1ccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)cc1C 10.1021/jm990266k
CHEMBL123030 16218 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 348 3 0 4 3.7 Cc1ccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)cc1C 10.1021/jm990266k
9840412 117594 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 328 6 2 4 3.6 O=c1ccc2ccc(CNCCNc3ccc(Cl)cc3)cc2o1 10.1021/jm990266k
CHEMBL340669 117594 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 328 6 2 4 3.6 O=c1ccc2ccc(CNCCNc3ccc(Cl)cc3)cc2o1 10.1021/jm990266k
155538349 171810 0 None 43 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 521 9 2 4 4.9 O=C(NCCCN1CCN(c2ccc(Br)cc2)CC1)NN(Cc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
CHEMBL4476278 171810 0 None 43 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 521 9 2 4 4.9 O=C(NCCCN1CCN(c2ccc(Br)cc2)CC1)NN(Cc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
145988180 164679 0 None -1 6 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 303 10 1 2 5.3 CCCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4229178 164679 0 None -1 6 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 303 10 1 2 5.3 CCCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
164628817 185695 0 None -2 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 349 6 0 4 3.4 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc2c(c1)CCC2 10.1016/j.ejmech.2021.113243
CHEMBL4874069 185695 0 None -2 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 349 6 0 4 3.4 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc2c(c1)CCC2 10.1016/j.ejmech.2021.113243
56944383 111627 0 None -25 12 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cells
ChEMBL 487 8 1 6 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
CHEMBL3290012 111627 0 None -25 12 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cells
ChEMBL 487 8 1 6 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
44405455 72023 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 398 5 1 3 4.7 O=C(N[C@H]1CCN(Cc2ccc(F)c(F)c2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
CHEMBL198580 72023 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 398 5 1 3 4.7 O=C(N[C@H]1CCN(Cc2ccc(F)c(F)c2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
44405489 132295 0 None 9 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 430 5 1 3 5.4 O=C(N[C@H]1CCN(Cc2ccc(C(F)(F)F)cc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
CHEMBL370134 132295 0 None 9 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 430 5 1 3 5.4 O=C(N[C@H]1CCN(Cc2ccc(C(F)(F)F)cc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
44405466 165827 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 392 6 1 4 4.4 COc1cccc(CN2CC[C@H](NC(=O)c3ccc(-c4cccs4)cc3)C2)c1 10.1016/j.bmcl.2005.08.051
CHEMBL427555 165827 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 392 6 1 4 4.4 COc1cccc(CN2CC[C@H](NC(=O)c3ccc(-c4cccs4)cc3)C2)c1 10.1016/j.bmcl.2005.08.051
53364083 63523 0 None 2 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 658 21 0 11 6.2 CCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803053 63523 0 None 2 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 658 21 0 11 6.2 CCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
72545011 92694 0 None 8 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 411 8 0 7 2.9 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443004 92694 0 None 8 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 411 8 0 7 2.9 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
137636460 155579 0 None 2 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 7 1 6 2.9 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3nccc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4063282 155579 0 None 2 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 7 1 6 2.9 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3nccc3c2)CC1 10.1021/acs.jmedchem.6b01857
137642380 157961 0 None -2 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 431 6 1 5 4.2 O=C(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)Nc1ccn2nccc2c1 10.1021/acs.jmedchem.6b01857
CHEMBL4091155 157961 0 None -2 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 431 6 1 5 4.2 O=C(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)Nc1ccn2nccc2c1 10.1021/acs.jmedchem.6b01857
11036641 31562 0 None -1 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 393 7 1 6 2.3 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm900690y
CHEMBL140612 31562 0 None -1 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 393 7 1 6 2.3 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm900690y
71734029 90624 0 None -4 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm400520c
CHEMBL2397392 90624 0 None -4 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm400520c
45272537 194851 0 None 181 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 365 4 0 6 3.0 COc1ccccc1N1CCN(Cc2c(C)nc3cc(C)nc(C)n23)CC1 10.1016/j.bmc.2009.05.015
CHEMBL563614 194851 0 None 181 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 365 4 0 6 3.0 COc1ccccc1N1CCN(Cc2c(C)nc3cc(C)nc(C)n23)CC1 10.1016/j.bmc.2009.05.015
44393775 65972 0 None - 1 Human 7.9 pKi = 7.9 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 490 4 1 4 4.2 Cc1cc(NC(=O)CN2CCN(c3ccc(Br)cc3C#N)CC2)ccc1Br 10.1016/j.bmcl.2004.07.068
CHEMBL184853 65972 0 None - 1 Human 7.9 pKi = 7.9 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 490 4 1 4 4.2 Cc1cc(NC(=O)CN2CCN(c3ccc(Br)cc3C#N)CC2)ccc1Br 10.1016/j.bmcl.2004.07.068
10200496 83180 0 None -25 5 Human 7.9 pKi = 7.9 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 391 6 1 3 3.6 O=C(CCCN1CC[Si](O)(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1021/jm1013693
CHEMBL2204343 83180 0 None -25 5 Human 7.9 pKi = 7.9 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 391 6 1 3 3.6 O=C(CCCN1CC[Si](O)(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1021/jm1013693
10473658 186610 3 None 38 3 Human 7.9 pKi = 7.9 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL49231 186610 3 None 38 3 Human 7.9 pKi = 7.9 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2005.02.012
9909055 4773 5 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 401 4 0 4 3.6 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCSc2ccccc21 10.1016/s0960-894x(02)00655-8
CHEMBL104238 4773 5 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 401 4 0 4 3.6 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCSc2ccccc21 10.1016/s0960-894x(02)00655-8
11325334 79641 0 None 11 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 342 6 0 5 2.8 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL212969 79641 0 None 11 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 342 6 0 5 2.8 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
127031515 138904 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.bmcl.2016.03.102
CHEMBL3793910 138904 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.bmcl.2016.03.102
76314268 105953 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 450 3 1 4 3.5 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3115577 105953 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 450 3 1 4 3.5 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139633 105953 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 450 3 1 4 3.5 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
18414156 106602 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 308 3 2 4 2.6 Oc1nc2c(N3CCN(Cc4ccccc4)CC3)cccc2[nH]1 10.1016/s0960-894x(98)00474-0
CHEMBL315864 106602 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 308 3 2 4 2.6 Oc1nc2c(N3CCN(Cc4ccccc4)CC3)cccc2[nH]1 10.1016/s0960-894x(98)00474-0
18414156 106602 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 308 3 2 4 2.6 Oc1nc2c(N3CCN(Cc4ccccc4)CC3)cccc2[nH]1 10.1007/s00044-012-0055-5
CHEMBL315864 106602 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 308 3 2 4 2.6 Oc1nc2c(N3CCN(Cc4ccccc4)CC3)cccc2[nH]1 10.1007/s00044-012-0055-5
76314268 105953 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 450 3 1 4 3.5 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3115577 105953 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 450 3 1 4 3.5 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139633 105953 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 450 3 1 4 3.5 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
11724450 123330 4 None - 1 Human 7.8 pKi = 7.8 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL184158 123330 4 None - 1 Human 7.8 pKi = 7.8 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL362542 123330 4 None - 1 Human 7.8 pKi = 7.8 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.bmcl.2004.07.068
2728532 111066 2 None -1 4 Human 7.8 pKi = 7.8 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 291 3 1 2 3.5 c1ccc(CN2CCN(c3cccc4[nH]ccc34)CC2)cc1 10.1016/s0960-894x(98)00474-0
CHEMBL328051 111066 2 None -1 4 Human 7.8 pKi = 7.8 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 291 3 1 2 3.5 c1ccc(CN2CCN(c3cccc4[nH]ccc34)CC2)cc1 10.1016/s0960-894x(98)00474-0
76331467 85458 0 None -1 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 287 3 1 0 2.8 c1ccc(C[n+]2cc[n+](-c3cccc4[nH]ccc34)cc2)cc1 10.1007/s00044-012-0055-5
CHEMBL2298808 85458 0 None -1 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 287 3 1 0 2.8 c1ccc(C[n+]2cc[n+](-c3cccc4[nH]ccc34)cc2)cc1 10.1007/s00044-012-0055-5
10064981 203319 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)cc1 10.1021/jm0305669
CHEMBL76982 203319 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)cc1 10.1021/jm0305669
44264629 96917 0 None 33 4 Human 6.9 pKi = 6.9 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 376 3 0 4 4.5 Clc1ccc(N2CCN(Cc3cnn4c3ccc3ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL269576 96917 0 None 33 4 Human 6.9 pKi = 6.9 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 376 3 0 4 4.5 Clc1ccc(N2CCN(Cc3cnn4c3ccc3ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
44380685 58427 0 None 4 4 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 373 6 2 4 3.2 COc1cc(N)c(Cl)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL168566 58427 0 None 4 4 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 373 6 2 4 3.2 COc1cc(N)c(Cl)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
25128757 102829 0 None -38 6 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]IABN from human dopamine D4 receptorDisplacement of [125I]IABN from human dopamine D4 receptor
ChEMBL 383 3 1 3 5.6 O[C@]1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2Cc1csc2ccccc12 10.1021/jm800532x
CHEMBL3084512 102829 0 None -38 6 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]IABN from human dopamine D4 receptorDisplacement of [125I]IABN from human dopamine D4 receptor
ChEMBL 383 3 1 3 5.6 O[C@]1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2Cc1csc2ccccc12 10.1021/jm800532x
134154387 151928 0 None -2 9 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 289 3 0 1 4.5 C1=C(CCN2CCc3ccccc3C2)CCc2ccccc21 10.1016/j.bmc.2016.09.019
CHEMBL3970994 151928 0 None -2 9 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 289 3 0 1 4.5 C1=C(CCN2CCc3ccccc3C2)CCc2ccccc21 10.1016/j.bmc.2016.09.019
164626655 186011 0 None -41 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 441 7 1 5 4.1 COc1cc2c(cc1OC)CN(Cc1ccccc1CNC(=O)c1ccc(C#N)cc1)CC2 10.1016/j.bmcl.2021.128047
CHEMBL4878587 186011 0 None -41 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 441 7 1 5 4.1 COc1cc2c(cc1OC)CN(Cc1ccccc1CNC(=O)c1ccc(C#N)cc1)CC2 10.1016/j.bmcl.2021.128047
145990141 166226 0 None -67 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 388 7 2 4 3.6 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(Cl)cc1)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4283982 166226 0 None -67 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 388 7 2 4 3.6 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(Cl)cc1)CC2 10.1021/acsmedchemlett.8b00229
60167309 74947 0 None 1 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 400 6 1 4 5.3 OC1(c2ccc(Cl)cc2)CCN(CCCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
CHEMBL2037432 74947 0 None 1 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 400 6 1 4 5.3 OC1(c2ccc(Cl)cc2)CCN(CCCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
60167309 74947 0 None -1 7 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 400 6 1 4 5.3 OC1(c2ccc(Cl)cc2)CCN(CCCCc2nc3ccccc3s2)CC1 10.1016/j.ejmech.2012.03.042
CHEMBL2037432 74947 0 None -1 7 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 400 6 1 4 5.3 OC1(c2ccc(Cl)cc2)CCN(CCCCc2nc3ccccc3s2)CC1 10.1016/j.ejmech.2012.03.042
11699469 77299 0 None -8 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 537 8 1 5 5.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3c4ccc(c3o2)CCc2ccc(cc2)CC4)CC1 10.1021/jm060138d
CHEMBL208847 77299 0 None -8 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 537 8 1 5 5.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3c4ccc(c3o2)CCc2ccc(cc2)CC4)CC1 10.1021/jm060138d
57402365 68953 0 None -10 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 441 12 1 6 3.1 CCOCCOc1cccc(C(=O)NCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/j.bmc.2011.10.063
CHEMBL1928119 68953 0 None -10 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 441 12 1 6 3.1 CCOCCOc1cccc(C(=O)NCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/j.bmc.2011.10.063
56837635 68966 0 None -467 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1129 44 2 17 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928132 68966 0 None -467 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1129 44 2 17 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
57398875 68972 0 None -40 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1005 30 2 17 4.7 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccc(COCCOCCOCCOCCOCc4ccn5ncc(C(=O)NCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928138 68972 0 None -40 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1005 30 2 17 4.7 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccc(COCCOCCOCCOCCOCc4ccn5ncc(C(=O)NCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
127046950 139515 0 None -7 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800303 139515 0 None -7 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
137643122 157491 0 None -17 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 467 8 2 10 2.6 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCCO5)CC3)cc12 10.1016/j.bmc.2017.08.037
CHEMBL4085752 157491 0 None -17 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 467 8 2 10 2.6 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCCO5)CC3)cc12 10.1016/j.bmc.2017.08.037
44459452 93460 0 None 2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 331 4 0 3 4.7 Cc1cc(-c2ccccc2)n(C2CCN(Cc3ccccc3)CC2)n1 10.1016/s0960-894x(99)00169-9
CHEMBL24809 93460 0 None 2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 331 4 0 3 4.7 Cc1cc(-c2ccccc2)n(C2CCN(Cc3ccccc3)CC2)n1 10.1016/s0960-894x(99)00169-9
19964406 114017 3 None 75 2 Human 6.9 pKi = 6.9 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 321 5 1 3 3.4 c1ccc(CCC2CN(Cc3nc4ccccc4[nH]3)CCO2)cc1 10.1021/ml500267c
CHEMBL3335535 114017 3 None 75 2 Human 6.9 pKi = 6.9 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 321 5 1 3 3.4 c1ccc(CCC2CN(Cc3nc4ccccc4[nH]3)CCO2)cc1 10.1021/ml500267c
10524751 57056 0 None 1 4 Human 5.9 pKi = 5.9 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 395 5 0 1 6.5 CCCN(CCC)C1CCC(=C(C#Cc2ccccc2)C#Cc2ccccc2)CC1 10.1021/jm991098z
CHEMBL165171 57056 0 None 1 4 Human 5.9 pKi = 5.9 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 395 5 0 1 6.5 CCCN(CCC)C1CCC(=C(C#Cc2ccccc2)C#Cc2ccccc2)CC1 10.1021/jm991098z
10543696 4513 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 320 4 1 5 2.2 c1ccc(-c2nc(CN3CCN(c4ccncn4)CC3)c[nH]2)cc1 10.1021/jm960637m
CHEMBL102599 4513 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 320 4 1 5 2.2 c1ccc(-c2nc(CN3CCN(c4ccncn4)CC3)c[nH]2)cc1 10.1021/jm960637m
51354277 59897 0 None -1288 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 429 11 1 5 3.4 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(OCCF)cc2)CC1 10.1021/jm101323b
CHEMBL1688992 59897 0 None -1288 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 429 11 1 5 3.4 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(OCCF)cc2)CC1 10.1021/jm101323b
CHEMBL1739996 59897 0 None -1288 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 429 11 1 5 3.4 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(OCCF)cc2)CC1 10.1021/jm101323b
145993220 166211 0 None -58 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 355 7 2 5 2.4 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccncc1)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4283709 166211 0 None -58 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 355 7 2 5 2.4 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccncc1)CC2 10.1021/acsmedchemlett.8b00229
168277992 189535 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 371 5 0 4 4.0 Cn1cnc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
CHEMBL5173368 189535 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 371 5 0 4 4.0 Cn1cnc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
25139332 183737 0 None -1 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 352 11 1 2 5.0 CCCN(CCC)CCCCNC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800895v
CHEMBL484204 183737 0 None -1 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 352 11 1 2 5.0 CCCN(CCC)CCCCNC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800895v
127045853 139263 0 None -5623 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 492 12 4 7 3.6 COc1cc(CCNC[C@H](O)c2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3798748 139263 0 None -5623 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 492 12 4 7 3.6 COc1cc(CCNC[C@H](O)c2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
118709168 112916 0 None -7 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1000 29 0 8 14.4 O=C(CCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318840 112916 0 None -7 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1000 29 0 8 14.4 O=C(CCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
122189389 122728 0 None -323 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 497 8 0 8 4.2 O=Cc1cnn2ccc(-n3cc(CCCCN4CCN(c5cccc(Cl)c5Cl)CC4)nn3)cc12 10.1016/j.bmc.2015.07.050
CHEMBL3613875 122728 0 None -323 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 497 8 0 8 4.2 O=Cc1cnn2ccc(-n3cc(CCCCN4CCN(c5cccc(Cl)c5Cl)CC4)nn3)cc12 10.1016/j.bmc.2015.07.050
11694483 71899 0 None -2 3 Human 4.9 pKi = 4.9 Binding
Binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandBinding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 249 6 0 4 2.1 CCCN(CCC)C1CCn2ncc(C=O)c2C1 10.1021/jm0503805
CHEMBL198174 71899 0 None -2 3 Human 4.9 pKi = 4.9 Binding
Binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandBinding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 249 6 0 4 2.1 CCCN(CCC)C1CCn2ncc(C=O)c2C1 10.1021/jm0503805
90644069 111546 0 None -1 2 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 341 4 0 4 3.8 Clc1ccc(N2CCN(CCc3nc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289651 111546 0 None -1 2 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 341 4 0 4 3.8 Clc1ccc(N2CCN(CCc3nc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
60165537 75001 0 None -1 4 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 308 5 0 3 4.6 c1ccc2c(c1)CN(CCCCc1nc3ccccc3s1)C2 10.1016/j.ejmech.2012.03.042
CHEMBL2037523 75001 0 None -1 4 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 308 5 0 3 4.6 c1ccc2c(c1)CN(CCCCc1nc3ccccc3s1)C2 10.1016/j.ejmech.2012.03.042
10548967 112234 0 None -12 3 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 399 5 0 4 3.2 COc1ccc2c(c1)C(=O)N(CCN1CCN(c3ccc(Cl)cc3)CC1)CC2 10.1021/jm991138z
CHEMBL330470 112234 0 None -12 3 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 399 5 0 4 3.2 COc1ccc2c(c1)C(=O)N(CCN1CCN(c3ccc(Cl)cc3)CC1)CC2 10.1021/jm991138z
134154387 151928 0 None -2 9 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 289 3 0 1 4.5 C1=C(CCN2CCc3ccccc3C2)CCc2ccccc21 10.1016/j.bmc.2016.09.019
CHEMBL3970994 151928 0 None -2 9 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 289 3 0 1 4.5 C1=C(CCN2CCc3ccccc3C2)CCc2ccccc21 10.1016/j.bmc.2016.09.019
60167309 74947 0 None 1 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 400 6 1 4 5.3 OC1(c2ccc(Cl)cc2)CCN(CCCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
CHEMBL2037432 74947 0 None 1 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 400 6 1 4 5.3 OC1(c2ccc(Cl)cc2)CCN(CCCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
154724650 175763 1 None -79 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 475 12 1 3 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4543870 175763 1 None -79 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 475 12 1 3 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4595492 175763 1 None -79 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 475 12 1 3 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
44192200 193719 2 None -380 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells
ChEMBL 451 3 0 7 3.9 Cc1ccc2c3c(ccc2n1)OC[C@H](CN1CCN(c2ccc4cc(C#N)ccc4n2)CC1)O3 10.1021/jm900374r
CHEMBL551964 193719 2 None -380 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells
ChEMBL 451 3 0 7 3.9 Cc1ccc2c3c(ccc2n1)OC[C@H](CN1CCN(c2ccc4cc(C#N)ccc4n2)CC1)O3 10.1021/jm900374r
44396235 167972 1 None -91 5 Human 5.8 pKi = 5.8 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 281 6 0 2 3.8 c1ccc(Cc2ccccc2OCCN2CCCC2)cc1 10.1021/jm049720x
CHEMBL435505 167972 1 None -91 5 Human 5.8 pKi = 5.8 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 281 6 0 2 3.8 c1ccc(Cc2ccccc2OCCN2CCCC2)cc1 10.1021/jm049720x
164622973 185541 0 None -61 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 397 6 0 4 4.5 CC1(CCCCN2CCN(c3ccccn3)CC2)Cc2cc(Cl)ccc2C1=O 10.1016/j.ejmech.2021.113243
CHEMBL4871868 185541 0 None -61 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 397 6 0 4 4.5 CC1(CCCCN2CCN(c3ccccn3)CC2)Cc2cc(Cl)ccc2C1=O 10.1016/j.ejmech.2021.113243
155564667 174908 0 None -154 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 459 8 1 6 4.3 CCc1cccc(N2CCN(CCCCNC(=O)c3nc4sccn4c3C)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4577414 174908 0 None -154 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 459 8 1 6 4.3 CCc1cccc(N2CCN(CCCCNC(=O)c3nc4sccn4c3C)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4444356 212184 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysis
ChEMBL None None None Nc1ccc(CN2CCC(n3cc(Cc4ccc(Br)cc4)nn3)CC2)cc1 10.1016/j.bmc.2022.116851
9926401 140344 0 None -2 8 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 301 5 0 2 4.4 Fc1ccc(SCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819556 140344 0 None -2 8 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 301 5 0 2 4.4 Fc1ccc(SCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819732 140344 0 None -2 8 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 301 5 0 2 4.4 Fc1ccc(SCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
16094676 230 17 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 325 4 1 3 2.2 Cc1cccc(c1)C(=O)NCN1CCC(CC1)c1cccc[n+]1[O-] 10.1021/jm060662k
8439 230 17 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 325 4 1 3 2.2 Cc1cccc(c1)C(=O)NCN1CCC(CC1)c1cccc[n+]1[O-] 10.1021/jm060662k
CHEMBL219182 230 17 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 325 4 1 3 2.2 Cc1cccc(c1)C(=O)NCN1CCC(CC1)c1cccc[n+]1[O-] 10.1021/jm060662k
5493357 205099 4 None - 1 Human 6.8 pKi = 6.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 321 2 1 4 3.4 Cc1cc(O)c2c3c(c(=O)oc2c1)CN(Cc1ccccc1)CC3 10.1021/jm970170v
CHEMBL90466 205099 4 None - 1 Human 6.8 pKi = 6.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 321 2 1 4 3.4 Cc1cc(O)c2c3c(c(=O)oc2c1)CN(Cc1ccccc1)CC3 10.1021/jm970170v
9952218 4812 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 387 4 0 3 3.2 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2c(F)cccc21 10.1016/s0960-894x(02)00655-8
CHEMBL104432 4812 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 387 4 0 3 3.2 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2c(F)cccc21 10.1016/s0960-894x(02)00655-8
90644065 111170 0 None 1 4 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 355 5 0 4 4.2 Clc1ccc(N2CCN(CCCc3nc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3286429 111170 0 None 1 4 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 355 5 0 4 4.2 Clc1ccc(N2CCN(CCCc3nc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
12050194 201202 1 None 5 4 Human 5.8 pKi = 5.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 333 5 0 4 3.7 c1ccc(CN2CCN(Cc3coc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
CHEMBL62703 201202 1 None 5 4 Human 5.8 pKi = 5.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 333 5 0 4 3.7 c1ccc(CN2CCN(Cc3coc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
9926401 140344 0 None -2 8 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 301 5 0 2 4.4 Fc1ccc(SCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819556 140344 0 None -2 8 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 301 5 0 2 4.4 Fc1ccc(SCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819732 140344 0 None -2 8 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 301 5 0 2 4.4 Fc1ccc(SCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
71061709 148995 0 None 3 12 Mouse 6.8 pKi = 6.8 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 372 6 0 4 3.5 Clc1cccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL3946540 148995 0 None 3 12 Mouse 6.8 pKi = 6.8 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 372 6 0 4 3.5 Clc1cccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
164611932 184619 0 None -33 7 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 364 6 1 4 3.1 O=C1CCc2cc(CCCCN3CCN(c4ccccn4)CC3)ccc2N1 10.1016/j.ejmech.2021.113243
CHEMBL4857597 184619 0 None -33 7 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 364 6 1 4 3.1 O=C1CCc2cc(CCCCN3CCN(c4ccccn4)CC3)ccc2N1 10.1016/j.ejmech.2021.113243
44427842 149276 0 None -9 6 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 494 7 1 4 5.2 O=C(NC[C@H]1C[C@H]1CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm0704200
CHEMBL394863 149276 0 None -9 6 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 494 7 1 4 5.2 O=C(NC[C@H]1C[C@H]1CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm0704200
49862238 14839 13 None -1 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 367 6 0 5 3.6 COc1cccc(F)c1OC1CN(Cc2cnn(-c3ccccc3)c2C)C1 10.1016/j.bmcl.2010.06.033
CHEMBL1209158 14839 13 None -1 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 367 6 0 5 3.6 COc1cccc(F)c1OC1CN(Cc2cnn(-c3ccccc3)c2C)C1 10.1016/j.bmcl.2010.06.033
5249956 73048 1 None -70 6 Human 6.8 pKi = 6.8 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1039/C5MD00258C
CHEMBL201525 73048 1 None -70 6 Human 6.8 pKi = 6.8 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1039/C5MD00258C
44278111 99670 0 None 13 2 Rat 6.8 pKi = 6.8 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 368 4 1 3 4.6 c1ccc(-c2ccc(N3CCN(Cc4c[nH]c5ncccc45)CC3)cc2)cc1 10.1016/s0960-894x(01)00241-4
CHEMBL287671 99670 0 None 13 2 Rat 6.8 pKi = 6.8 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 368 4 1 3 4.6 c1ccc(-c2ccc(N3CCN(Cc4c[nH]c5ncccc45)CC3)cc2)cc1 10.1016/s0960-894x(01)00241-4
11957566 183 20 None -79 9 Human 6.8 pKi = 6.8 Binding
Tested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cellsTested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cells
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1016/S0960-894X(97)10068-3
1219 183 20 None -79 9 Human 6.8 pKi = 6.8 Binding
Tested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cellsTested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cells
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1016/S0960-894X(97)10068-3
3296 183 20 None -79 9 Human 6.8 pKi = 6.8 Binding
Tested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cellsTested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cells
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1016/S0960-894X(97)10068-3
950 183 20 None -79 9 Human 6.8 pKi = 6.8 Binding
Tested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cellsTested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cells
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1016/S0960-894X(97)10068-3
CHEMBL285755 183 20 None -79 9 Human 6.8 pKi = 6.8 Binding
Tested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cellsTested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cells
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1016/S0960-894X(97)10068-3
168269421 189369 0 None 6 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 390 5 1 2 5.3 Fc1ccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5170670 189369 0 None 6 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 390 5 1 2 5.3 Fc1ccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)cc1F 10.1016/j.bmcl.2022.128615
53248212 61704 0 None -154 5 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 424 8 2 4 3.5 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm200288r
CHEMBL1774534 61704 0 None -154 5 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 424 8 2 4 3.5 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm200288r
44427831 91807 0 None -338 6 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 460 9 2 6 3.1 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2ccc(-c3ccccn3)cc2)CC1 10.1021/jm0704200
CHEMBL242644 91807 0 None -338 6 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 460 9 2 6 3.1 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2ccc(-c3ccccn3)cc2)CC1 10.1021/jm0704200
44438209 153428 0 None -9 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 406 9 2 3 5.6 CCCCCCOc1ccc(C2(O)CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.10.076
CHEMBL398368 153428 0 None -9 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 406 9 2 3 5.6 CCCCCCOc1ccc(C2(O)CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.10.076
9888555 165052 11 None -208 8 Human 7.8 pKi = 7.8 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm025558r
CHEMBL424294 165052 11 None -208 8 Human 7.8 pKi = 7.8 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm025558r
10642239 186077 1 None 53 3 Human 7.8 pKi = 7.8 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1021/jm970021c
CHEMBL48819 186077 1 None 53 3 Human 7.8 pKi = 7.8 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1021/jm970021c
135398737 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.01.044
38 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.01.044
722 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.01.044
CHEMBL42 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.01.044
DB00363 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.01.044
44335907 5307 0 None 14 2 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 417 4 0 3 4.1 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2cc(Cl)cc(Cl)c2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL107020 5307 0 None 14 2 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 417 4 0 3 4.1 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2cc(Cl)cc(Cl)c2)CC1 10.1016/s0960-894x(02)00655-8
44335800 109558 0 None 138 2 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 379 5 0 4 2.8 COc1ccc(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
CHEMBL323525 109558 0 None 138 2 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 379 5 0 4 2.8 COc1ccc(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
155537361 171732 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 541 10 2 5 5.4 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(Cl)cc2Cl)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4475042 171732 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 541 10 2 5 5.4 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(Cl)cc2Cl)CC1 10.1021/acs.jmedchem.9b01085
155542182 172539 0 None 10 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 516 10 2 6 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(C#N)cc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4520460 172539 0 None 10 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 516 10 2 6 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(C#N)cc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
71449737 81413 0 None -6 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 468 7 0 7 3.5 COc1ccccc1N1CCN(CCN(C(=O)c2cnc3ccccc3n2)c2ccccn2)CC1 10.1016/j.bmcl.2012.05.119
CHEMBL2164349 81413 0 None -6 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 468 7 0 7 3.5 COc1ccccc1N1CCN(CCN(C(=O)c2cnc3ccccc3n2)c2ccccn2)CC1 10.1016/j.bmcl.2012.05.119
44405452 72211 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 430 5 1 3 5.7 O=C(N[C@H]1CCN(Cc2ccc(Cl)c(Cl)c2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
CHEMBL199186 72211 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 430 5 1 3 5.7 O=C(N[C@H]1CCN(Cc2ccc(Cl)c(Cl)c2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
53361301 63511 0 None 2 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 985 29 0 16 8.6 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803024 63511 0 None 2 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 985 29 0 16 8.6 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
21219154 88135 0 None 33 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 317 4 0 3 4.4 c1ccc(CN2CCC(n3nccc3-c3ccccc3)CC2)cc1 10.1016/s0960-894x(99)00169-9
CHEMBL23537 88135 0 None 33 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 317 4 0 3 4.4 c1ccc(CN2CCC(n3nccc3-c3ccccc3)CC2)cc1 10.1016/s0960-894x(99)00169-9
56926587 68668 0 None 380 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 329 3 0 5 2.3 Fc1ccc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)cn1 10.1021/jm200762g
CHEMBL1923416 68668 0 None 380 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 329 3 0 5 2.3 Fc1ccc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)cn1 10.1021/jm200762g
53361301 63511 0 None 2 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 985 29 0 16 8.6 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2009919
CHEMBL1803024 63511 0 None 2 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 985 29 0 16 8.6 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2009919
10642239 186077 1 None 53 3 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL48819 186077 1 None 53 3 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.02.012
10642239 186077 1 None 53 3 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL48819 186077 1 None 53 3 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.02.012
9888555 165052 11 None -208 8 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm0611152
CHEMBL424294 165052 11 None -208 8 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm0611152
9861786 111853 0 None -19 4 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 317 6 3 4 3.1 Oc1nc2c(OCCNCc3ccccc3)cc(Cl)cc2[nH]1 10.1016/s0960-894x(99)00434-5
CHEMBL329398 111853 0 None -19 4 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 317 6 3 4 3.1 Oc1nc2c(OCCNCc3ccccc3)cc(Cl)cc2[nH]1 10.1016/s0960-894x(99)00434-5
44273855 74053 0 None 10 2 Human 7.8 pKi = 7.8 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 381 7 1 4 3.4 COc1cc(Cl)ccc1N1CCN(CCCCNC(=O)C(C)(C)C)CC1 10.1016/0960-894X(96)00198-9
CHEMBL20251 74053 0 None 10 2 Human 7.8 pKi = 7.8 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 381 7 1 4 3.4 COc1cc(Cl)ccc1N1CCN(CCCCNC(=O)C(C)(C)C)CC1 10.1016/0960-894X(96)00198-9
44273928 77727 0 None 63 2 Human 7.8 pKi = 7.8 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 365 8 1 3 3.8 CCC(C)(C)C(=O)NCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL21011 77727 0 None 63 2 Human 7.8 pKi = 7.8 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 365 8 1 3 3.8 CCC(C)(C)C(=O)NCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
10665101 101055 0 None 22 3 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 343 4 1 3 3.2 Cc1cccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)c1 10.1016/j.bmcl.2005.02.012
CHEMBL298166 101055 0 None 22 3 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 343 4 1 3 3.2 Cc1cccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)c1 10.1016/j.bmcl.2005.02.012
10413085 82777 0 None -64 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 484 8 2 4 4.3 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(Br)ccc3[nH]2)CC1 10.1021/jm0611152
CHEMBL218444 82777 0 None -64 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 484 8 2 4 4.3 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(Br)ccc3[nH]2)CC1 10.1021/jm0611152
135398737 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity for Dopamine receptor D4In vitro binding affinity for Dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00200-1
38 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity for Dopamine receptor D4In vitro binding affinity for Dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00200-1
722 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity for Dopamine receptor D4In vitro binding affinity for Dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00200-1
CHEMBL42 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity for Dopamine receptor D4In vitro binding affinity for Dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00200-1
DB00363 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity for Dopamine receptor D4In vitro binding affinity for Dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00200-1
127032383 138873 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 322 5 1 3 3.4 c1ccc(OC[C@@H]2CN(Cc3ccc4[nH]ccc4c3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793438 138873 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 322 5 1 3 3.4 c1ccc(OC[C@@H]2CN(Cc3ccc4[nH]ccc4c3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
10852461 205235 2 None 1 3 Human 6.8 pKi = 6.8 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 310 4 2 3 2.9 O=C(Nc1ccccn1)NC1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL91272 205235 2 None 1 3 Human 6.8 pKi = 6.8 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 310 4 2 3 2.9 O=C(Nc1ccccn1)NC1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
10449136 205698 0 None 1 3 Human 6.8 pKi = 6.8 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 327 1 0 1 5.6 CC(C)=C1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL94067 205698 0 None 1 3 Human 6.8 pKi = 6.8 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 327 1 0 1 5.6 CC(C)=C1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
10053476 116246 0 None -275 5 Human 6.8 pKi = 6.8 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 559 7 1 3 4.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[te]1 10.1021/jm025558r
CHEMBL337531 116246 0 None -275 5 Human 6.8 pKi = 6.8 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 559 7 1 3 4.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[te]1 10.1021/jm025558r
44380802 161142 0 None 1 4 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
CHEMBL413343 161142 0 None 1 4 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
127053220 138837 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 319 5 0 3 3.2 Fc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.bmcl.2016.03.102
CHEMBL3793062 138837 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 319 5 0 3 3.2 Fc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.bmcl.2016.03.102
11849821 168734 0 None 2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 374 6 1 6 2.3 CO/N=C(/c1ccc(Cl)cc1)C(O)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
CHEMBL441529 168734 0 None 2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 374 6 1 6 2.3 CO/N=C(/c1ccc(Cl)cc1)C(O)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
145991769 166328 0 None -12 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 384 8 2 5 3.0 COc1cccc(C(=O)NCCCCN2CCc3cc(OC)c(O)cc3C2)c1 10.1021/acsmedchemlett.8b00229
CHEMBL4285984 166328 0 None -12 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 384 8 2 5 3.0 COc1cccc(C(=O)NCCCCN2CCc3cc(OC)c(O)cc3C2)c1 10.1021/acsmedchemlett.8b00229
10476504 33268 1 None -1 7 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1016/j.bmc.2017.04.036
CHEMBL142020 33268 1 None -1 7 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1016/j.bmc.2017.04.036
72545007 92690 0 None 3 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 407 12 0 8 1.6 COc1ccccc1N1CCN(Cc2cn(CCOCCOCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443000 92690 0 None 3 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 407 12 0 8 1.6 COc1ccccc1N1CCN(Cc2cn(CCOCCOCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
71456214 78276 0 None - 1 Human 6.8 pKi = 6.8 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 450 8 1 4 4.7 CCCNC(=O)c1cc(C)c(OCC2CN(Cc3ccc(Cl)cc3)CCO2)cc1Cl 10.1021/jm031111m
CHEMBL2112466 78276 0 None - 1 Human 6.8 pKi = 6.8 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 450 8 1 4 4.7 CCCNC(=O)c1cc(C)c(OCC2CN(Cc3ccc(Cl)cc3)CCO2)cc1Cl 10.1021/jm031111m
71457956 78015 0 None -1 4 Human 6.8 pKi = 6.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 469 9 1 5 5.1 COc1ccc(Br)cc1-c1nc(CNCCC2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL2111527 78015 0 None -1 4 Human 6.8 pKi = 6.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 469 9 1 5 5.1 COc1ccc(Br)cc1-c1nc(CNCCC2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
71454405 78016 0 None -1 4 Human 6.8 pKi = 6.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 471 8 1 5 5.2 COc1ccc(Br)cc1-c1nc(CNCC2CCN(Cc3ccccc3)C2)cs1 10.1016/s0960-894x(00)00405-4
CHEMBL2111528 78016 0 None -1 4 Human 6.8 pKi = 6.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 471 8 1 5 5.2 COc1ccc(Br)cc1-c1nc(CNCC2CCN(Cc3ccccc3)C2)cs1 10.1016/s0960-894x(00)00405-4
44340415 8492 0 None 1 4 Human 5.8 pKi = 5.8 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 460 5 1 3 5.3 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(C#Cc2ccccc2)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL109472 8492 0 None 1 4 Human 5.8 pKi = 5.8 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 460 5 1 3 5.3 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(C#Cc2ccccc2)c2ccccc12 10.1016/s0960-894x(03)00678-4
72205044 91513 0 None -4 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 410 8 0 5 4.3 Clc1ccc(-n2cc(COCCCN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2013.05.027
CHEMBL2414355 91513 0 None -4 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 410 8 0 5 4.3 Clc1ccc(-n2cc(COCCCN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2013.05.027
145979897 166053 0 None -151 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 480 7 2 4 3.6 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(I)cc1)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4280542 166053 0 None -151 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 480 7 2 4 3.6 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(I)cc1)CC2 10.1021/acsmedchemlett.8b00229
15508243 5231 20 None 1 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 366 3 0 2 3.9 Ic1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
CHEMBL106635 5231 20 None 1 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 366 3 0 2 3.9 Ic1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
10682854 24432 1 None -2 3 Human 5.8 pKi = 5.8 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 261 6 0 2 3.7 CCCN(CCC)[C@@H]1CCc2ccc(OC)cc2C1 10.1021/jm960345l
CHEMBL134326 24432 1 None -2 3 Human 5.8 pKi = 5.8 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 261 6 0 2 3.7 CCCN(CCC)[C@@H]1CCc2ccc(OC)cc2C1 10.1021/jm960345l
44419056 82764 0 None -398 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 447 8 1 5 4.2 C#Cc1ccc2cc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)sc2c1 10.1021/jm0611152
CHEMBL218368 82764 0 None -398 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 447 8 1 5 4.2 C#Cc1ccc2cc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)sc2c1 10.1021/jm0611152
9930722 201977 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 397 4 0 3 3.8 CCN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)CCc2ccccc21 10.1016/s0960-894x(00)00421-2
CHEMBL67414 201977 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 397 4 0 3 3.8 CCN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)CCc2ccccc21 10.1016/s0960-894x(00)00421-2
9930722 201977 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 397 4 0 3 3.8 CCN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)CCc2ccccc21 10.1016/s0960-894x(02)01056-9
CHEMBL67414 201977 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 397 4 0 3 3.8 CCN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)CCc2ccccc21 10.1016/s0960-894x(02)01056-9
127050632 140212 0 None -87 9 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 454 6 1 5 4.7 O=C1NCN(c2ccccc2)C12CCN(CCCCc1nc3cc(Cl)ccc3s1)CC2 10.1016/j.bmc.2016.06.011
CHEMBL3818124 140212 0 None -87 9 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 454 6 1 5 4.7 O=C1NCN(c2ccccc2)C12CCN(CCCCc1nc3cc(Cl)ccc3s1)CC2 10.1016/j.bmc.2016.06.011
168282745 190501 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
CHEMBL5187721 190501 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
12581156 24946 15 None -8 3 Human 5.8 pKi = 5.8 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 205 3 1 2 2.2 CCNC1CCc2c(cccc2OC)C1 10.1021/jm960345l
CHEMBL134759 24946 15 None -8 3 Human 5.8 pKi = 5.8 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 205 3 1 2 2.2 CCNC1CCc2c(cccc2OC)C1 10.1021/jm960345l
72164183 91719 0 None 1 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 274 3 1 4 2.8 Oc1ccc(N2CCN(Cc3cccs3)CC2)cc1 10.1016/j.bmcl.2013.07.033
CHEMBL2420778 91719 0 None 1 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 274 3 1 4 2.8 Oc1ccc(N2CCN(Cc3cccs3)CC2)cc1 10.1016/j.bmcl.2013.07.033
133633 2210 46 None -104 8 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1016/j.bmcl.2006.10.076
177 2210 46 None -104 8 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1016/j.bmcl.2006.10.076
CHEMBL445102 2210 46 None -104 8 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1016/j.bmcl.2006.10.076
155195311 173775 0 None -208 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1C[C@H]1C[C@@H]1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
CHEMBL4551160 173775 0 None -208 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1C[C@H]1C[C@@H]1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
133633 2210 46 None -104 8 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1016/j.bmc.2008.12.054
177 2210 46 None -104 8 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1016/j.bmc.2008.12.054
CHEMBL445102 2210 46 None -104 8 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1016/j.bmc.2008.12.054
44438235 93225 2 None -2 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 353 4 1 4 4.6 CSc1ccc(C2(O)CCN(Cc3coc4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.10.076
CHEMBL246854 93225 2 None -2 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 353 4 1 4 4.6 CSc1ccc(C2(O)CCN(Cc3coc4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.10.076
42626381 55952 0 None -645 2 Human 5.8 pKi = 5.8 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 452 9 3 6 2.5 COc1ccc2[nH]c(C(=O)NCCC(O)CN3CCN(c4ccccc4OC)CC3)cc2c1 10.1021/jm900095y
CHEMBL1627315 55952 0 None -645 2 Human 5.8 pKi = 5.8 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 452 9 3 6 2.5 COc1ccc2[nH]c(C(=O)NCCC(O)CN3CCN(c4ccccc4OC)CC3)cc2c1 10.1021/jm900095y
44431473 150206 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.5 Cc1ccccc1CN1CCC(NC(=O)c2cccc3ccccc23)CC1 10.1016/j.bmcl.2006.12.106
CHEMBL395632 150206 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.5 Cc1ccccc1CN1CCC(NC(=O)c2cccc3ccccc23)CC1 10.1016/j.bmcl.2006.12.106
44438197 152738 2 None -58 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 374 3 2 2 5.0 OC1(c2cccc(Cl)c2Cl)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL397770 152738 2 None -58 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 374 3 2 2 5.0 OC1(c2cccc(Cl)c2Cl)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
44304814 201183 0 None -2 4 Human 4.8 pKi = 4.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 505 8 1 5 5.9 COc1c(-c2nc(CNC[C@@H]3CCN(Cc4ccccc4)C3)co2)cc(Br)c2ccccc12 10.1016/s0960-894x(00)00405-4
CHEMBL62601 201183 0 None -2 4 Human 4.8 pKi = 4.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 505 8 1 5 5.9 COc1c(-c2nc(CNC[C@@H]3CCN(Cc4ccccc4)C3)co2)cc(Br)c2ccccc12 10.1016/s0960-894x(00)00405-4
44330564 106898 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 300 1 0 3 5.0 CC(C)n1ncc2c1-c1c(Cl)sc(Cl)c1CCC2 10.1016/s0960-894x(03)00587-0
CHEMBL317825 106898 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 300 1 0 3 5.0 CC(C)n1ncc2c1-c1c(Cl)sc(Cl)c1CCC2 10.1016/s0960-894x(03)00587-0
44336057 5831 0 None 2 2 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 437 4 0 3 4.8 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1c2ccccc2CC12CCCCC2 10.1016/s0960-894x(02)00655-8
CHEMBL107962 5831 0 None 2 2 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 437 4 0 3 4.8 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1c2ccccc2CC12CCCCC2 10.1016/s0960-894x(02)00655-8
168297637 191725 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3ncc4ccccn34)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
CHEMBL5206427 191725 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3ncc4ccccn34)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
9801858 63116 0 None -23 3 Rat 5.8 pKi = 5.8 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 413 6 1 3 4.5 O=C(NCCCCN1CCN2c3ccccc3CCC2C1)c1ccc2ccccc2c1 10.1021/jm049031l
CHEMBL179757 63116 0 None -23 3 Rat 5.8 pKi = 5.8 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 413 6 1 3 4.5 O=C(NCCCCN1CCN2c3ccccc3CCC2C1)c1ccc2ccccc2c1 10.1021/jm049031l
9817612 106772 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 294 1 0 3 4.7 Cc1sc(C)c2c1CCCc1cnn(-c3ccccc3)c1-2 10.1016/s0960-894x(03)00587-0
CHEMBL316942 106772 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 294 1 0 3 4.7 Cc1sc(C)c2c1CCCc1cnn(-c3ccccc3)c1-2 10.1016/s0960-894x(03)00587-0
44273876 79405 0 None 2 2 Human 6.8 pKi = 6.8 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 371 7 1 3 3.7 O=C(NCCCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccccc1 10.1016/0960-894X(96)00198-9
CHEMBL21205 79405 0 None 2 2 Human 6.8 pKi = 6.8 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 371 7 1 3 3.7 O=C(NCCCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccccc1 10.1016/0960-894X(96)00198-9
44517726 194348 0 None -63 4 Human 6.8 pKi = 6.8 Binding
Binding affinity to DAD4 receptorBinding affinity to DAD4 receptor
ChEMBL 341 4 0 2 3.6 O=C1N(CCN2Cc3ccccc3C2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2009.07.055
CHEMBL560177 194348 0 None -63 4 Human 6.8 pKi = 6.8 Binding
Binding affinity to DAD4 receptorBinding affinity to DAD4 receptor
ChEMBL 341 4 0 2 3.6 O=C1N(CCN2Cc3ccccc3C2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2009.07.055
164622973 185541 0 None -61 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 397 6 0 4 4.5 CC1(CCCCN2CCN(c3ccccn3)CC2)Cc2cc(Cl)ccc2C1=O 10.1016/j.ejmech.2021.113243
CHEMBL4871868 185541 0 None -61 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 397 6 0 4 4.5 CC1(CCCCN2CCN(c3ccccn3)CC2)Cc2cc(Cl)ccc2C1=O 10.1016/j.ejmech.2021.113243
127051015 140343 0 None -5 9 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 283 5 0 1 4.2 Fc1ccc(CCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818128 140343 0 None -5 9 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 283 5 0 1 4.2 Fc1ccc(CCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819731 140343 0 None -5 9 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 283 5 0 1 4.2 Fc1ccc(CCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
11576528 83904 0 None -32 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 476 11 1 7 3.4 COc1ccccc1N1CCN(CCCCCNC(=O)c2nnn(Cc3ccccc3)c2C)CC1 10.1021/jm0611152
CHEMBL221587 83904 0 None -32 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 476 11 1 7 3.4 COc1ccccc1N1CCN(CCCCCNC(=O)c2nnn(Cc3ccccc3)c2C)CC1 10.1021/jm0611152
9952528 98979 0 None -1 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity for Dopamine receptor D4In vitro binding affinity for Dopamine receptor D4
ChEMBL 394 5 1 3 3.8 NC(=O)C1CCC(CN2CCC(=C(c3ccccc3)c3ccc(F)cc3)CC2)O1 10.1016/s0960-894x(01)00200-1
CHEMBL282927 98979 0 None -1 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity for Dopamine receptor D4In vitro binding affinity for Dopamine receptor D4
ChEMBL 394 5 1 3 3.8 NC(=O)C1CCC(CN2CCC(=C(c3ccccc3)c3ccc(F)cc3)CC2)O1 10.1016/s0960-894x(01)00200-1
11191906 11662 0 None -31 12 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpirideBinding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpiride
ChEMBL 537 12 1 3 7.3 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
CHEMBL1181665 11662 0 None -31 12 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpirideBinding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpiride
ChEMBL 537 12 1 3 7.3 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
CHEMBL187928 11662 0 None -31 12 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpirideBinding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpiride
ChEMBL 537 12 1 3 7.3 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
127050632 140212 0 None -87 9 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 454 6 1 5 4.7 O=C1NCN(c2ccccc2)C12CCN(CCCCc1nc3cc(Cl)ccc3s1)CC2 10.1016/j.bmc.2016.06.011
CHEMBL3818124 140212 0 None -87 9 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 454 6 1 5 4.7 O=C1NCN(c2ccccc2)C12CCN(CCCCc1nc3cc(Cl)ccc3s1)CC2 10.1016/j.bmc.2016.06.011
126534204 137903 0 None -1412 5 Human 4.8 pKi = 4.8 Binding
Binding affinity to dopamine D4 receptor (unknown origin)Binding affinity to dopamine D4 receptor (unknown origin)
ChEMBL 504 7 1 7 3.9 Cn1c(SCCCN2CC3CCN(c4ccc(C(F)(F)F)cc4)C3C2)nnc1-c1cc[nH]c(=O)c1 10.1016/j.bmc.2016.02.031
CHEMBL3774411 137903 0 None -1412 5 Human 4.8 pKi = 4.8 Binding
Binding affinity to dopamine D4 receptor (unknown origin)Binding affinity to dopamine D4 receptor (unknown origin)
ChEMBL 504 7 1 7 3.9 Cn1c(SCCCN2CC3CCN(c4ccc(C(F)(F)F)cc4)C3C2)nnc1-c1cc[nH]c(=O)c1 10.1016/j.bmc.2016.02.031
154705884 175789 1 None -48 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 2 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4469584 175789 1 None -48 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 2 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4595726 175789 1 None -48 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 2 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
71658072 89967 0 None -18 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 399 8 1 4 3.6 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386611 89967 0 None -18 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 399 8 1 4 3.6 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmc.2013.03.074
44374431 54667 0 None -6 4 Human 5.8 pKi = 5.8 Binding
Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)
ChEMBL 261 4 1 3 2.9 CCCN[C@@H]1CCc2c(C(=O)OC)cccc2[C@@H]1C 10.1016/S0960-894X(01)80181-5
CHEMBL161507 54667 0 None -6 4 Human 5.8 pKi = 5.8 Binding
Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)
ChEMBL 261 4 1 3 2.9 CCCN[C@@H]1CCc2c(C(=O)OC)cccc2[C@@H]1C 10.1016/S0960-894X(01)80181-5
135398737 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970170v
38 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970170v
722 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970170v
CHEMBL42 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970170v
DB00363 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970170v
10665626 112080 0 None 41 3 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 351 4 0 5 3.4 COc1ccc2c3c(c(=O)oc2c1OC)CN(Cc1ccccc1)CC3 10.1021/jm970170v
CHEMBL330100 112080 0 None 41 3 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 351 4 0 5 3.4 COc1ccc2c3c(c(=O)oc2c1OC)CN(Cc1ccccc1)CC3 10.1021/jm970170v
135398737 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00316-5
38 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00316-5
722 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00316-5
CHEMBL42 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00316-5
DB00363 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00316-5
16104 161368 15 None -1 5 Human 7.8 pKi = 7.8 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm00043a008
CHEMBL415300 161368 15 None -1 5 Human 7.8 pKi = 7.8 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm00043a008
135398737 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm015522j
38 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm015522j
722 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm015522j
CHEMBL42 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm015522j
DB00363 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm015522j
135398737 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00692-1
38 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00692-1
722 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00692-1
CHEMBL42 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00692-1
DB00363 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00692-1
5311189 203133 4 None -1 27 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 16/1300)Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 16/1300)
ChEMBL 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 10.1016/s0960-894x(02)00390-6
CHEMBL7549 203133 4 None -1 27 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 16/1300)Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 16/1300)
ChEMBL 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 10.1016/s0960-894x(02)00390-6
135398737 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00302-9
38 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00302-9
722 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00302-9
CHEMBL42 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00302-9
DB00363 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00302-9
135398737 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970422s
38 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970422s
722 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970422s
CHEMBL42 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970422s
DB00363 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970422s
2389 3279 114 None -21 67 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm0002432
5073 3279 114 None -21 67 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm0002432
96 3279 114 None -21 67 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm0002432
CHEMBL85 3279 114 None -21 67 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm0002432
DB00734 3279 114 None -21 67 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm0002432
2389 3279 114 None -21 67 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm030480f
5073 3279 114 None -21 67 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm030480f
96 3279 114 None -21 67 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm030480f
CHEMBL85 3279 114 None -21 67 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm030480f
DB00734 3279 114 None -21 67 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm030480f
9906071 16131 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 342 6 2 4 4.0 Cc1ccc(NCCNCc2ccc3ccc(=O)oc3c2)cc1Cl 10.1021/jm990266k
CHEMBL122597 16131 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 342 6 2 4 4.0 Cc1ccc(NCCNCc2ccc3ccc(=O)oc3c2)cc1Cl 10.1021/jm990266k
10854185 114041 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 3 0 4 3.4 Cc1ccccc1N1CCN(Cc2ccc3ccc(=O)oc3c2)CC1 10.1021/jm990266k
CHEMBL333658 114041 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 3 0 4 3.4 Cc1ccccc1N1CCN(Cc2ccc3ccc(=O)oc3c2)CC1 10.1021/jm990266k
135398737 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Competitive binding affinity against human Dopamine receptor D4 by displacing [3H]spiperone from CHO cellsCompetitive binding affinity against human Dopamine receptor D4 by displacing [3H]spiperone from CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009989
38 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Competitive binding affinity against human Dopamine receptor D4 by displacing [3H]spiperone from CHO cellsCompetitive binding affinity against human Dopamine receptor D4 by displacing [3H]spiperone from CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009989
722 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Competitive binding affinity against human Dopamine receptor D4 by displacing [3H]spiperone from CHO cellsCompetitive binding affinity against human Dopamine receptor D4 by displacing [3H]spiperone from CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009989
CHEMBL42 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Competitive binding affinity against human Dopamine receptor D4 by displacing [3H]spiperone from CHO cellsCompetitive binding affinity against human Dopamine receptor D4 by displacing [3H]spiperone from CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009989
DB00363 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Competitive binding affinity against human Dopamine receptor D4 by displacing [3H]spiperone from CHO cellsCompetitive binding affinity against human Dopamine receptor D4 by displacing [3H]spiperone from CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009989
155518026 169670 0 None 10 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 528 11 2 7 4.0 COc1ccc(N(Cc2ccc(C#N)cc2)NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1021/acs.jmedchem.9b01085
CHEMBL4445706 169670 0 None 10 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 528 11 2 7 4.0 COc1ccc(N(Cc2ccc(C#N)cc2)NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1021/acs.jmedchem.9b01085
162653993 183086 0 None 1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3cccnc3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4753809 183086 0 None 1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3cccnc3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4802865 183086 0 None 1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3cccnc3)CC2)cc1 10.1016/j.bmc.2020.115943
3251 4009 50 None -43 12 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2011.06.023
5684 4009 50 None -43 12 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2011.06.023
80 4009 50 None -43 12 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2011.06.023
CHEMBL31354 4009 50 None -43 12 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2011.06.023
127052487 140269 0 None 3 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 422 6 2 3 5.1 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2016.06.011
CHEMBL3818805 140269 0 None 3 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 422 6 2 3 5.1 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2016.06.011
25070740 111283 0 None -1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3cccn4nccc34)CC2)c1Cl 10.1021/jm5004039
CHEMBL3287391 111283 0 None -1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3cccn4nccc34)CC2)c1Cl 10.1021/jm5004039
25072943 111285 0 None -2 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3cccc4ccnn34)CC2)c1Cl 10.1021/jm5004039
CHEMBL3287393 111285 0 None -2 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3cccc4ccnn34)CC2)c1Cl 10.1021/jm5004039
44431486 87645 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 374 5 1 3 4.2 COc1cccc(CN2CCC(NC(=O)c3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.12.106
CHEMBL234645 87645 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 374 5 1 3 4.2 COc1cccc(CN2CCC(NC(=O)c3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.12.106
44405469 71642 0 None 14 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 396 5 1 3 5.1 O=C(N[C@H]1CCN(Cc2ccc(Cl)cc2)C1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2005.08.051
CHEMBL197381 71642 0 None 14 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 396 5 1 3 5.1 O=C(N[C@H]1CCN(Cc2ccc(Cl)cc2)C1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2005.08.051
72545240 92697 0 None 16 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 469 12 0 8 3.4 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCCOCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443007 92697 0 None 16 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 469 12 0 8 3.4 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCCOCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
135398737 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00540-5
38 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00540-5
722 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00540-5
CHEMBL42 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00540-5
DB00363 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00540-5
44436602 144680 0 None -2 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 391 8 1 4 3.0 C#Cc1cccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/j.bmc.2007.08.038
CHEMBL391256 144680 0 None -2 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 391 8 1 4 3.0 C#Cc1cccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/j.bmc.2007.08.038
2 3210 19 None -2 28 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm901120h
54562 3210 19 None -2 28 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm901120h
CHEMBL240773 3210 19 None -2 28 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm901120h
122181329 121356 0 None -51 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 394 10 1 2 4.6 CCCN(CCCCNC(=O)/C=C/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3590080 121356 0 None -51 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 394 10 1 2 4.6 CCCN(CCCCNC(=O)/C=C/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
71459759 83657 0 None 4 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 432 4 0 3 5.5 COc1ccccc1N1CCN(Cc2cc(C#Cc3ccccc3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207633 83657 0 None 4 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 432 4 0 3 5.5 COc1ccccc1N1CCN(Cc2cc(C#Cc3ccccc3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
135398737 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm060166w
38 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm060166w
722 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm060166w
CHEMBL42 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm060166w
DB00363 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm060166w
135398737 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2009.05.015
38 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2009.05.015
722 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2009.05.015
CHEMBL42 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2009.05.015
DB00363 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2009.05.015
45269168 194256 0 None 10 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 410 4 1 6 2.3 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccc(F)cc4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
CHEMBL559399 194256 0 None 10 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 410 4 1 6 2.3 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccc(F)cc4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
135398737 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00814-9
38 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00814-9
722 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00814-9
CHEMBL42 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00814-9
DB00363 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00814-9
135398737 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00405-4
38 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00405-4
722 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00405-4
CHEMBL42 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00405-4
DB00363 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00405-4
3251 4009 50 None -43 12 Human 7.8 pKi = 7.8 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm1009956
5684 4009 50 None -43 12 Human 7.8 pKi = 7.8 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm1009956
80 4009 50 None -43 12 Human 7.8 pKi = 7.8 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm1009956
CHEMBL31354 4009 50 None -43 12 Human 7.8 pKi = 7.8 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm1009956
127031519 138793 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 329 6 0 4 3.7 CSc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792638 138793 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 329 6 0 4 3.7 CSc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
127053221 138801 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 369 5 0 3 4.1 Fc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1C(F)(F)F 10.1016/j.bmcl.2016.03.102
CHEMBL3792728 138801 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 369 5 0 3 4.1 Fc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1C(F)(F)F 10.1016/j.bmcl.2016.03.102
127052487 140269 0 None 3 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 422 6 2 3 5.1 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2016.06.011
CHEMBL3818805 140269 0 None 3 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 422 6 2 3 5.1 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2016.06.011
10612157 101387 1 None -15 5 Human 7.8 pKi = 7.8 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 271 4 2 4 2.3 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CO2 10.1021/jm9703653
CHEMBL300571 101387 1 None -15 5 Human 7.8 pKi = 7.8 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 271 4 2 4 2.3 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CO2 10.1021/jm9703653
CHEMBL423890 101387 1 None -15 5 Human 7.8 pKi = 7.8 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 271 4 2 4 2.3 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CO2 10.1021/jm9703653
10612157 101387 1 None -15 5 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 271 4 2 4 2.3 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CO2 10.1016/s0960-894x(98)00014-6
CHEMBL300571 101387 1 None -15 5 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 271 4 2 4 2.3 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CO2 10.1016/s0960-894x(98)00014-6
CHEMBL423890 101387 1 None -15 5 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 271 4 2 4 2.3 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CO2 10.1016/s0960-894x(98)00014-6
162653993 183086 0 None 1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3cccnc3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4753809 183086 0 None 1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3cccnc3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4802865 183086 0 None 1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3cccnc3)CC2)cc1 10.1016/j.bmc.2020.115943
3645619 2985 13 None -4 9 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/j.bmcl.2005.02.012
975 2985 13 None -4 9 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/j.bmcl.2005.02.012
CHEMBL45244 2985 13 None -4 9 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/j.bmcl.2005.02.012
9982854 83923 0 None -24 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 485 8 1 5 4.5 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(Br)ccc3o2)CC1 10.1021/jm0611152
CHEMBL221681 83923 0 None -24 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 485 8 1 5 4.5 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(Br)ccc3o2)CC1 10.1021/jm0611152
10687967 203343 0 None 1 3 Human 6.8 pKi = 6.8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 331 5 1 2 4.4 c1ccc(Cc2cc(C3CCN(Cc4ccccc4)CC3)[nH]n2)cc1 10.1021/jm970111h
CHEMBL77148 203343 0 None 1 3 Human 6.8 pKi = 6.8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 331 5 1 2 4.4 c1ccc(Cc2cc(C3CCN(Cc4ccccc4)CC3)[nH]n2)cc1 10.1021/jm970111h
10039198 56055 0 None -4 4 Human 6.8 pKi = 6.8 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 277 5 0 1 4.5 CCCN(CCC)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm991098z
CHEMBL163087 56055 0 None -4 4 Human 6.8 pKi = 6.8 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 277 5 0 1 4.5 CCCN(CCC)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm991098z
15467372 168544 0 None 43 4 Human 6.8 pKi = 6.8 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 317 4 1 4 2.8 N#CC(C#N)=Cc1[nH]ccc1CN1CCN(c2ccccc2)CC1 10.1016/s0960-894x(99)00302-9
CHEMBL440120 168544 0 None 43 4 Human 6.8 pKi = 6.8 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 317 4 1 4 2.8 N#CC(C#N)=Cc1[nH]ccc1CN1CCN(c2ccccc2)CC1 10.1016/s0960-894x(99)00302-9
127032082 138787 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 323 5 0 5 2.6 c1ccc(OC[C@@H]2CN(Cc3cn4ccccc4n3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792541 138787 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 323 5 0 5 2.6 c1ccc(OC[C@@H]2CN(Cc3cn4ccccc4n3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
127051015 140343 0 None -5 9 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 283 5 0 1 4.2 Fc1ccc(CCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818128 140343 0 None -5 9 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 283 5 0 1 4.2 Fc1ccc(CCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819731 140343 0 None -5 9 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 283 5 0 1 4.2 Fc1ccc(CCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
137635364 155719 0 None -512 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 439 10 1 6 3.0 O=C(NCCCCN1CCN(c2ccccc2OCCF)CC1)c1cc2ccccn2n1 10.1016/j.bmc.2017.04.036
CHEMBL4064974 155719 0 None -512 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 439 10 1 6 3.0 O=C(NCCCCN1CCN(c2ccccc2OCCF)CC1)c1cc2ccccn2n1 10.1016/j.bmc.2017.04.036
CHEMBL4074669 155719 0 None -512 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 439 10 1 6 3.0 O=C(NCCCCN1CCN(c2ccccc2OCCF)CC1)c1cc2ccccn2n1 10.1016/j.bmc.2017.04.036
57391896 68963 0 None -24 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1013 36 2 15 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928129 68963 0 None -24 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1013 36 2 15 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
57400557 68970 0 None -131 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 509 14 1 8 3.2 CCOCCOCc1ccn2ncc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
CHEMBL1928136 68970 0 None -131 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 509 14 1 8 3.2 CCOCCOCc1ccn2ncc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
118709170 112918 0 None -6 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1057 33 0 8 16.0 O=C(CCCCCCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318842 112918 0 None -6 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1057 33 0 8 16.0 O=C(CCCCCCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
137645830 157310 0 None -3 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 424 7 1 8 2.8 Oc1ccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c2c1OCCO2 10.1021/acs.jmedchem.7b00363
CHEMBL4083727 157310 0 None -3 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 424 7 1 8 2.8 Oc1ccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c2c1OCCO2 10.1021/acs.jmedchem.7b00363
10924369 9246 1 None -1000 6 Human 6.8 pKi = 6.8 Binding
The binding affinity at the Dopamine receptor D4 determined using [3H]YM-09151-2The binding affinity at the Dopamine receptor D4 determined using [3H]YM-09151-2
ChEMBL 294 1 0 3 3.1 COc1cccc2c1N1CCN(C)C[C@@H]1c1ccccc1C2 10.1021/jm010566d
CHEMBL111184 9246 1 None -1000 6 Human 6.8 pKi = 6.8 Binding
The binding affinity at the Dopamine receptor D4 determined using [3H]YM-09151-2The binding affinity at the Dopamine receptor D4 determined using [3H]YM-09151-2
ChEMBL 294 1 0 3 3.1 COc1cccc2c1N1CCN(C)C[C@@H]1c1ccccc1C2 10.1021/jm010566d
11747350 106848 0 None -79 10 Human 5.8 pKi = 5.8 Binding
Binding affinity against dopamine receptor D4 cloned in HEK 293 cells using [3H]spiperone radioligandBinding affinity against dopamine receptor D4 cloned in HEK 293 cells using [3H]spiperone radioligand
ChEMBL 260 5 1 3 2.4 CCOC(=O)c1[nH]c2ccccc2c1CCN(C)C 10.1021/jm010943m
CHEMBL317535 106848 0 None -79 10 Human 5.8 pKi = 5.8 Binding
Binding affinity against dopamine receptor D4 cloned in HEK 293 cells using [3H]spiperone radioligandBinding affinity against dopamine receptor D4 cloned in HEK 293 cells using [3H]spiperone radioligand
ChEMBL 260 5 1 3 2.4 CCOC(=O)c1[nH]c2ccccc2c1CCN(C)C 10.1021/jm010943m
2337 3205 72 None -114 62 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm0002432
50 3205 72 None -114 62 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm0002432
5002 3205 72 None -114 62 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm0002432
CHEMBL716 3205 72 None -114 62 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm0002432
DB01224 3205 72 None -114 62 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm0002432
2337 3205 72 None -114 62 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm030480f
50 3205 72 None -114 62 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm030480f
5002 3205 72 None -114 62 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm030480f
CHEMBL716 3205 72 None -114 62 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm030480f
DB01224 3205 72 None -114 62 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm030480f
CHEMBL5075726 212624 0 None -30 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCOC(=O)/C=C1\[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2CCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/acs.jmedchem.1c00611
44335635 4728 0 None - 1 Human 5.8 pKi = 5.8 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 381 6 0 4 4.3 COc1cc(Cl)ccc1OC[C@H]1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL104099 4728 0 None - 1 Human 5.8 pKi = 5.8 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 381 6 0 4 4.3 COc1cc(Cl)ccc1OC[C@H]1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
44381217 58834 0 None 4 4 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 442 5 1 5 3.4 COc1ccc(Br)cc1C1=NCC[C@H](CN2CCN(c3ccccc3)CC2)N1 10.1016/s0960-894x(03)00004-0
CHEMBL169889 58834 0 None 4 4 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 442 5 1 5 3.4 COc1ccc(Br)cc1C1=NCC[C@H](CN2CCN(c3ccccc3)CC2)N1 10.1016/s0960-894x(03)00004-0
44319368 105584 0 None -1 4 Human 5.8 pKi = 5.8 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 429 5 0 5 3.4 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)CO1 10.1016/s0960-894x(01)00484-x
CHEMBL313320 105584 0 None -1 4 Human 5.8 pKi = 5.8 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 429 5 0 5 3.4 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)CO1 10.1016/s0960-894x(01)00484-x
11356479 71493 0 None -8 3 Human 5.8 pKi = 5.8 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 221 5 0 3 2.3 CCCN(CCC)C1CCn2nccc2C1 10.1021/jm0503805
CHEMBL196928 71493 0 None -8 3 Human 5.8 pKi = 5.8 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 221 5 0 3 2.3 CCCN(CCC)C1CCn2nccc2C1 10.1021/jm0503805
10564794 57235 0 None -4 3 Human 4.8 pKi = 4.8 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 281 5 0 1 4.6 CCCN(CCC)C1CC=C(C#Cc2ccccc2)CC1 10.1021/jm991098z
CHEMBL166325 57235 0 None -4 3 Human 4.8 pKi = 4.8 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 281 5 0 1 4.6 CCCN(CCC)C1CC=C(C#Cc2ccccc2)CC1 10.1021/jm991098z
11615782 71882 0 None - 1 Human 4.8 pKi = 4.8 Binding
Binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandBinding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 251 6 1 4 1.8 CCCN(CCC)C1CCn2ncc(CO)c2C1 10.1021/jm0503805
CHEMBL198125 71882 0 None - 1 Human 4.8 pKi = 4.8 Binding
Binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandBinding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 251 6 1 4 1.8 CCCN(CCC)C1CCn2ncc(CO)c2C1 10.1021/jm0503805
154704368 175897 1 None -35 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 421 11 2 2 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4569006 175897 1 None -35 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 421 11 2 2 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4596571 175897 1 None -35 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 421 11 2 2 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
135469096 11961 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 366 6 1 7 2.1 c1cnc(N2CCN(CCCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL1183656 11961 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 366 6 1 7 2.1 c1cnc(N2CCN(CCCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL309843 11961 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 366 6 1 7 2.1 c1cnc(N2CCN(CCCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
71658074 89969 0 None -64 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 420 8 2 4 3.9 COc1ccccc1N1CCCN(CCCCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386613 89969 0 None -64 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 420 8 2 4 3.9 COc1ccccc1N1CCCN(CCCCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1016/j.bmc.2013.03.074
76325764 105819 0 None -37 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 434 8 2 5 3.3 COc1ccc2[nH]c(C(=O)NC/C=C/CN3CCN(c4ccccc4OC)CC3)cc2c1 10.1039/c3md00098b
CHEMBL3133866 105819 0 None -37 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 434 8 2 5 3.3 COc1ccc2[nH]c(C(=O)NC/C=C/CN3CCN(c4ccccc4OC)CC3)cc2c1 10.1039/c3md00098b
CHEMBL3139064 105819 0 None -37 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 434 8 2 5 3.3 COc1ccc2[nH]c(C(=O)NC/C=C/CN3CCN(c4ccccc4OC)CC3)cc2c1 10.1039/c3md00098b
60167452 75004 0 None -9 8 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 448 7 1 6 4.1 O=C(CCCCN1CCC2(CC1)C(=O)NCN2c1ccccc1)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL2037526 75004 0 None -9 8 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 448 7 1 6 4.1 O=C(CCCCN1CCC2(CC1)C(=O)NCN2c1ccccc1)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
60167452 75004 0 None -9 8 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 448 7 1 6 4.1 O=C(CCCCN1CCC2(CC1)C(=O)NCN2c1ccccc1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL2037526 75004 0 None -9 8 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 448 7 1 6 4.1 O=C(CCCCN1CCC2(CC1)C(=O)NCN2c1ccccc1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
4064333 85313 17 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 344 4 1 2 4.2 O=C(NC1CCN(Cc2ccccc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.096
4064333 85313 17 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 344 4 1 2 4.2 O=C(NC1CCN(Cc2ccccc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
CHEMBL229019 85313 17 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 344 4 1 2 4.2 O=C(NC1CCN(Cc2ccccc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.096
CHEMBL229019 85313 17 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 344 4 1 2 4.2 O=C(NC1CCN(Cc2ccccc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
3038495 700 30 None -109 19 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm049031l
7625 700 30 None -109 19 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm049031l
CHEMBL25236 700 30 None -109 19 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm049031l
60167452 75004 0 None -9 8 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 448 7 1 6 4.1 O=C(CCCCN1CCC2(CC1)C(=O)NCN2c1ccccc1)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL2037526 75004 0 None -9 8 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 448 7 1 6 4.1 O=C(CCCCN1CCC2(CC1)C(=O)NCN2c1ccccc1)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
127051016 140345 0 None -5 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 386 5 1 4 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
CHEMBL3819642 140345 0 None -5 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 386 5 1 4 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
CHEMBL3819734 140345 0 None -5 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 386 5 1 4 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
49798839 14247 0 None -53 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 347 3 1 4 3.9 O=c1[nH]c2ccccc2n1C1CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1172214 14247 0 None -53 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 347 3 1 4 3.9 O=c1[nH]c2ccccc2n1C1CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1200154 14247 0 None -53 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 347 3 1 4 3.9 O=c1[nH]c2ccccc2n1C1CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmc.2010.05.052
154703438 175807 1 None -6 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 496 12 0 6 6.1 COc1ccc(Cl)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1 10.1021/acs.jmedchem.9b01835
CHEMBL4475699 175807 1 None -6 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 496 12 0 6 6.1 COc1ccc(Cl)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1 10.1021/acs.jmedchem.9b01835
CHEMBL4595859 175807 1 None -6 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 496 12 0 6 6.1 COc1ccc(Cl)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1 10.1021/acs.jmedchem.9b01835
127051016 140345 0 None -5 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 386 5 1 4 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
CHEMBL3819642 140345 0 None -5 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 386 5 1 4 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
CHEMBL3819734 140345 0 None -5 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 386 5 1 4 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
118719799 115226 0 None -25 4 Human 6.8 pKi = 6.8 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 487 10 0 7 5.5 COc1ccccc1N1CCN(CCCCCc2cn(-c3ccc(-c4ccsc4)cc3)nn2)CC1 10.1016/j.bmcl.2014.12.023
CHEMBL3353902 115226 0 None -25 4 Human 6.8 pKi = 6.8 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 487 10 0 7 5.5 COc1ccccc1N1CCN(CCCCCc2cn(-c3ccc(-c4ccsc4)cc3)nn2)CC1 10.1016/j.bmcl.2014.12.023
10893228 39974 0 None 117 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 341 0 1 5 3.5 CN1CCCN(C2=Nc3cccnc3Nc3ccc(Cl)cc32)CC1 10.1021/jm0104825
CHEMBL148042 39974 0 None 117 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 341 0 1 5 3.5 CN1CCCN(C2=Nc3cccnc3Nc3ccc(Cl)cc32)CC1 10.1021/jm0104825
145970938 164604 0 None -1 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 233 5 1 2 3.4 CCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4228054 164604 0 None -1 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 233 5 1 2 3.4 CCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
145992489 166424 0 None -5 12 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
ChEMBL 535 7 1 2 7.8 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC=C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL4287623 166424 0 None -5 12 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
ChEMBL 535 7 1 2 7.8 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC=C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
9992499 73039 0 None -6 4 Human 5.8 pKi = 5.8 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 254 0 0 2 2.6 CN1CCc2ccccc2Cc2ccn(C)c2CC1 10.1021/jm050846j
CHEMBL201483 73039 0 None -6 4 Human 5.8 pKi = 5.8 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 254 0 0 2 2.6 CN1CCc2ccccc2Cc2ccn(C)c2CC1 10.1021/jm050846j
11566745 74345 0 None -3 4 Human 6.8 pKi = 6.8 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 283 0 2 3 2.7 CN1CCc2ccccc2Cc2cc(O)c(O)cc2CC1 10.1021/jm050846j
CHEMBL1202298 74345 0 None -3 4 Human 6.8 pKi = 6.8 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 283 0 2 3 2.7 CN1CCc2ccccc2Cc2cc(O)c(O)cc2CC1 10.1021/jm050846j
CHEMBL203029 74345 0 None -3 4 Human 6.8 pKi = 6.8 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 283 0 2 3 2.7 CN1CCc2ccccc2Cc2cc(O)c(O)cc2CC1 10.1021/jm050846j
168283295 190641 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 327 5 0 2 4.6 Cc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1 10.1016/j.bmcl.2022.128615
CHEMBL5189986 190641 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 327 5 0 2 4.6 Cc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1 10.1016/j.bmcl.2022.128615
168275962 190025 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 353 5 0 4 4.0 Cc1cc(CO[C@H]2CCCN(Cc3ncn4ccccc34)C2)ccc1F 10.1016/j.bmcl.2022.128615
CHEMBL5180979 190025 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 353 5 0 4 4.0 Cc1cc(CO[C@H]2CCCN(Cc3ncn4ccccc34)C2)ccc1F 10.1016/j.bmcl.2022.128615
168291848 191276 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(COC2CCN(Cc3ncn4ccccc34)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5199552 191276 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(COC2CCN(Cc3ncn4ccccc34)CC2)c1 10.1016/j.bmcl.2022.128615
168275089 189902 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3cn4ccccc4n3)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5179198 189902 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3cn4ccccc4n3)CC2)c1 10.1016/j.bmcl.2022.128615
71061729 160396 0 None 1 4 Mouse 5.8 pKi = 5.8 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 372 6 0 4 3.5 Clc1cccc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL4115493 160396 0 None 1 4 Mouse 5.8 pKi = 5.8 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 372 6 0 4 3.5 Clc1cccc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
5025739 168630 40 None 30 2 Human 6.8 pKi = 6.8 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm0305669
CHEMBL440687 168630 40 None 30 2 Human 6.8 pKi = 6.8 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm0305669
44438233 93177 2 None -7 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 375 3 1 3 5.2 OC1(c2ccc(Cl)c(Cl)c2)CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246643 93177 2 None -7 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 375 3 1 3 5.2 OC1(c2ccc(Cl)c(Cl)c2)CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
168279825 190222 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(COC2CCN(Cc3cn4ccccc4n3)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5183902 190222 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(COC2CCN(Cc3cn4ccccc4n3)CC2)c1 10.1016/j.bmcl.2022.128615
44426511 136770 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 344 4 1 2 4.2 O=C(c1ccc2ccccc2c1)N1CCC(NCc2ccccc2)CC1 10.1016/j.bmcl.2006.12.096
CHEMBL375238 136770 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 344 4 1 2 4.2 O=C(c1ccc2ccccc2c1)N1CCC(NCc2ccccc2)CC1 10.1016/j.bmcl.2006.12.096
44330566 206539 0 None 2 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 286 1 0 3 4.4 CCn1ncc2c1-c1c(Cl)sc(Cl)c1CCC2 10.1016/s0960-894x(03)00587-0
CHEMBL98945 206539 0 None 2 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 286 1 0 3 4.4 CCn1ncc2c1-c1c(Cl)sc(Cl)c1CCC2 10.1016/s0960-894x(03)00587-0
11133533 44962 0 None -17 4 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 418 8 1 5 3.6 COc1cccc(C(=O)NCCCCN2CCN(c3nccc4ccccc34)CC2)c1 10.1021/jm020952a
CHEMBL152587 44962 0 None -17 4 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 418 8 1 5 3.6 COc1cccc(C(=O)NCCCCN2CCN(c3nccc4ccccc34)CC2)c1 10.1021/jm020952a
242 467 117 None -117 51 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2011.04.021
34 467 117 None -117 51 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2011.04.021
60795 467 117 None -117 51 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2011.04.021
CHEMBL1112 467 117 None -117 51 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2011.04.021
DB01238 467 117 None -117 51 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2011.04.021
11849736 137887 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 344 7 0 6 3.1 CCO/N=C(\CCN1CCN(c2nccs2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL377388 137887 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 344 7 0 6 3.1 CCO/N=C(\CCN1CCN(c2nccs2)CC1)c1ccccc1 10.1021/jm060279f
44431471 167814 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 374 5 1 3 4.2 COc1cccc(CN2CCC(NC(=O)c3cccc4ccccc34)CC2)c1 10.1016/j.bmcl.2006.12.106
CHEMBL434583 167814 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 374 5 1 3 4.2 COc1cccc(CN2CCC(NC(=O)c3cccc4ccccc34)CC2)c1 10.1016/j.bmcl.2006.12.106
155195496 170149 0 None -72 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 407 7 3 5 3.1 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1CCCCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
CHEMBL4452064 170149 0 None -72 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 407 7 3 5 3.1 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1CCCCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
122442272 137820 0 None -60 15 Human 5.8 pKi = 5.8 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769968 137820 0 None -60 15 Human 5.8 pKi = 5.8 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771384 137820 0 None -60 15 Human 5.8 pKi = 5.8 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
44330386 106890 0 None 3 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 258 0 1 2 3.9 Clc1sc(Cl)c2c1CCCc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
CHEMBL317770 106890 0 None 3 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 258 0 1 2 3.9 Clc1sc(Cl)c2c1CCCc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
5311346 202453 22 None -19 5 Human 6.8 pKi = 6.8 Binding
Tested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cellsTested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cells
ChEMBL 249 2 1 4 1.9 CCCN1CCO[C@@H]2c3cc(O)ccc3OC[C@H]21 10.1021/jm0000113
CHEMBL1256778 202453 22 None -19 5 Human 6.8 pKi = 6.8 Binding
Tested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cellsTested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cells
ChEMBL 249 2 1 4 1.9 CCCN1CCO[C@@H]2c3cc(O)ccc3OC[C@H]21 10.1021/jm0000113
CHEMBL70565 202453 22 None -19 5 Human 6.8 pKi = 6.8 Binding
Tested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cellsTested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cells
ChEMBL 249 2 1 4 1.9 CCCN1CCO[C@@H]2c3cc(O)ccc3OC[C@H]21 10.1021/jm0000113
168292124 191427 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 365 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccc(F)c(F)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5201917 191427 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 365 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccc(F)c(F)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
11453253 83897 0 None -54 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 431 9 1 5 3.7 COc1ccc(C(=O)NCCCCN2CCN(c3ccccc3Cl)CC2)cc1OC 10.1021/jm0611152
CHEMBL221549 83897 0 None -54 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 431 9 1 5 3.7 COc1ccc(C(=O)NCCCCN2CCN(c3ccccc3Cl)CC2)cc1OC 10.1021/jm0611152
22727351 12872 0 None -28 3 Human 5.8 pKi = 5.8 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 406 8 0 6 4.4 O=[N+]([O-])c1cccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)c1 10.1016/s0960-894x(02)00179-8
CHEMBL1189537 12872 0 None -28 3 Human 5.8 pKi = 5.8 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 406 8 0 6 4.4 O=[N+]([O-])c1cccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)c1 10.1016/s0960-894x(02)00179-8
CHEMBL538977 12872 0 None -28 3 Human 5.8 pKi = 5.8 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 406 8 0 6 4.4 O=[N+]([O-])c1cccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)c1 10.1016/s0960-894x(02)00179-8
122442272 137820 0 None -60 15 Human 5.8 pKi = 5.8 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769968 137820 0 None -60 15 Human 5.8 pKi = 5.8 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771384 137820 0 None -60 15 Human 5.8 pKi = 5.8 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
60167451 74998 0 None -26 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 468 7 1 6 5.3 O=C(CCCCN1CCC(n2c(=O)[nH]c3cc(Cl)ccc32)CC1)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL2037520 74998 0 None -26 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 468 7 1 6 5.3 O=C(CCCCN1CCC(n2c(=O)[nH]c3cc(Cl)ccc32)CC1)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
10456166 119128 0 None -2754 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 444 7 2 3 4.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm0611152
CHEMBL346692 119128 0 None -2754 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 444 7 2 3 4.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm0611152
CHEMBL4285942 119128 0 None -2754 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 444 7 2 3 4.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm0611152
44339984 167234 0 None 10 4 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL430522 167234 0 None 10 4 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
10641955 205121 0 None 154 3 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 355 3 0 4 4.0 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1cccc(Cl)c1)CC3 10.1021/jm970170v
CHEMBL90569 205121 0 None 154 3 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 355 3 0 4 4.0 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1cccc(Cl)c1)CC3 10.1021/jm970170v
44394820 64520 0 None 234 2 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 402 6 1 3 5.1 CSc1ccc(-c2ccc(C(=O)NC3CCN(Cc4ccccc4)C3)cc2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL182075 64520 0 None 234 2 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 402 6 1 3 5.1 CSc1ccc(-c2ccc(C(=O)NC3CCN(Cc4ccccc4)C3)cc2)cc1 10.1016/j.bmcl.2004.07.045
44394629 65244 0 None 234 2 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 374 5 1 2 4.5 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2cccc(F)c2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL183160 65244 0 None 234 2 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 374 5 1 2 4.5 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2cccc(F)c2)cc1 10.1016/j.bmcl.2004.07.045
44214764 66863 0 None 467 2 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 424 5 1 2 5.4 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL187804 66863 0 None 467 2 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 424 5 1 2 5.4 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2004.07.045
135398737 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00421-2
38 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00421-2
722 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00421-2
CHEMBL42 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00421-2
DB00363 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00421-2
15522515 97709 0 None 93 4 Human 7.8 pKi = 7.8 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 292 3 0 4 2.7 c1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL273860 97709 0 None 93 4 Human 7.8 pKi = 7.8 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 292 3 0 4 2.7 c1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
44403232 70732 0 None -1 5 Human 7.8 pKi = 7.8 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 459 8 1 4 4.0 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2005.07.037
CHEMBL195247 70732 0 None -1 5 Human 7.8 pKi = 7.8 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 459 8 1 4 4.0 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2005.07.037
9949554 16674 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 3 0 4 3.4 Cc1ccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)cc1 10.1021/jm990266k
CHEMBL124835 16674 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 3 0 4 3.4 Cc1ccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)cc1 10.1021/jm990266k
44395741 180999 0 None 1 10 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.12.054
CHEMBL476935 180999 0 None 1 10 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.12.054
CHEMBL558392 180999 0 None 1 10 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.12.054
155567971 175448 0 None 25 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 495 9 2 4 4.9 O=C(NCCCN1CCN(c2ccc(Cl)cc2)CC1)NN(Cc1ccc(F)cc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
CHEMBL4589982 175448 0 None 25 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 495 9 2 4 4.9 O=C(NCCCN1CCN(c2ccc(Cl)cc2)CC1)NN(Cc1ccc(F)cc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
135398737 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)01056-9
38 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)01056-9
722 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)01056-9
CHEMBL42 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)01056-9
DB00363 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)01056-9
9861462 82921 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 309 3 2 5 2.0 Oc1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm060662k
CHEMBL219179 82921 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 309 3 2 5 2.0 Oc1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm060662k
52945819 17371 0 None -1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 354 6 0 3 4.2 Cc1ccc(C)c(N2CCN(CCCC(=O)c3ccc(F)cc3)CC2)c1 10.1021/jm100899z
CHEMBL1258037 17371 0 None -1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 354 6 0 3 4.2 Cc1ccc(C)c(N2CCN(CCCC(=O)c3ccc(F)cc3)CC2)c1 10.1021/jm100899z
135398737 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2014.12.045
38 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2014.12.045
722 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2014.12.045
CHEMBL42 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2014.12.045
DB00363 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2014.12.045
135398737 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401895u
38 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401895u
722 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401895u
CHEMBL42 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401895u
DB00363 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401895u
137640391 156164 0 None -21 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 418 7 1 7 2.8 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(C#N)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4070091 156164 0 None -21 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 418 7 1 7 2.8 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(C#N)c3c2)CC1 10.1021/acs.jmedchem.6b01857
21219167 99192 0 None 93 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 332 4 0 4 4.1 Cc1c(-c2ccccc2)nnn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00169-9
CHEMBL284346 99192 0 None 93 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 332 4 0 4 4.1 Cc1c(-c2ccccc2)nnn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00169-9
10665598 34857 1 None 30 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]cc(CN3CCN(c4ccccc4Cl)CC3)c2c1 10.1021/jm0009989
CHEMBL143355 34857 1 None 30 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]cc(CN3CCN(c4ccccc4Cl)CC3)c2c1 10.1021/jm0009989
22100964 202257 4 None 93 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 324 3 0 3 4.8 Clc1ccc2oc(C3=CCN(Cc4ccccc4)CC3)nc2c1 10.1016/S0960-894X(97)00402-2
CHEMBL69356 202257 4 None 93 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 324 3 0 3 4.8 Clc1ccc2oc(C3=CCN(Cc4ccccc4)CC3)nc2c1 10.1016/S0960-894X(97)00402-2
44395741 180999 0 None 1 10 Human 7.8 pKi = 7.8 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
CHEMBL476935 180999 0 None 1 10 Human 7.8 pKi = 7.8 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
CHEMBL558392 180999 0 None 1 10 Human 7.8 pKi = 7.8 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
44395741 180999 0 None 1 10 Human 7.8 pKi = 7.8 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL476935 180999 0 None 1 10 Human 7.8 pKi = 7.8 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL558392 180999 0 None 1 10 Human 7.8 pKi = 7.8 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
44395741 180999 0 None -1 10 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2014.04.026
CHEMBL476935 180999 0 None -1 10 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2014.04.026
CHEMBL558392 180999 0 None -1 10 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2014.04.026
10015731 206428 0 None -15 4 Human 7.8 pKi = 7.8 Binding
Tested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cellsTested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cells
ChEMBL 265 2 1 4 2.7 CCCN1CCO[C@@H]2c3cc(O)ccc3SC[C@H]21 10.1021/jm0000113
CHEMBL98305 206428 0 None -15 4 Human 7.8 pKi = 7.8 Binding
Tested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cellsTested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cells
ChEMBL 265 2 1 4 2.7 CCCN1CCO[C@@H]2c3cc(O)ccc3SC[C@H]21 10.1021/jm0000113
127053217 138788 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 333 5 0 3 4.1 c1ccc(OC[C@@H]2CN(Cc3ccc4ccccc4c3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792556 138788 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 333 5 0 3 4.1 c1ccc(OC[C@@H]2CN(Cc3ccc4ccccc4c3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
11581443 95954 0 None -85 4 Human 6.8 pKi = 6.8 Binding
Binding affinity to D4 receptorBinding affinity to D4 receptor
ChEMBL 367 8 1 4 3.0 COc1ccccc1N1CCN(CCCCNC(=O)c2ccccc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL26188 95954 0 None -85 4 Human 6.8 pKi = 6.8 Binding
Binding affinity to D4 receptorBinding affinity to D4 receptor
ChEMBL 367 8 1 4 3.0 COc1ccccc1N1CCN(CCCCNC(=O)c2ccccc2)CC1 10.1016/j.bmc.2011.10.063
9837137 111834 0 None 24 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 204 0 1 2 2.9 Cc1sc(C)c2c1CCc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
CHEMBL329276 111834 0 None 24 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 204 0 1 2 2.9 Cc1sc(C)c2c1CCc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
127031508 138851 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 335 5 0 3 3.8 Fc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3793169 138851 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 335 5 0 3 3.8 Fc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
11624518 198659 3 None -1 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation counting
ChEMBL 352 4 0 4 3.8 Clc1ccc(-n2cc(CN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2012.08.011
CHEMBL597601 198659 3 None -1 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation counting
ChEMBL 352 4 0 4 3.8 Clc1ccc(-n2cc(CN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2012.08.011
145990453 166392 0 None -63 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 404 7 2 4 4.1 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc3ccccc3c1)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4287062 166392 0 None -63 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 404 7 2 4 4.1 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc3ccccc3c1)CC2 10.1021/acsmedchemlett.8b00229
168290895 191401 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 387 5 0 4 4.5 Cn1ncc2cc(CN3CCC(OCc4ccc(Cl)c(F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
CHEMBL5201507 191401 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 387 5 0 4 4.5 Cn1ncc2cc(CN3CCC(OCc4ccc(Cl)c(F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
49783041 16989 0 None -42 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 597 7 1 3 6.8 O=C(NCCCCN1CCN(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
CHEMBL1256171 16989 0 None -42 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 597 7 1 3 6.8 O=C(NCCCCN1CCN(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
44436603 144683 0 None -7 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 467 8 1 4 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(C#Cc3ccccc3)c2)CC1 10.1016/j.bmc.2007.08.038
CHEMBL391257 144683 0 None -7 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 467 8 1 4 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(C#Cc3ccccc3)c2)CC1 10.1016/j.bmc.2007.08.038
44249745 193772 0 None -229 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 366 4 0 3 3.1 N#Cc1cccc(N2CCN(CCN3CCC(C(F)(F)F)CC3)C2=O)c1 10.1016/j.bmcl.2010.09.142
CHEMBL552373 193772 0 None -229 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 366 4 0 3 3.1 N#Cc1cccc(N2CCN(CCN3CCC(C(F)(F)F)CC3)C2=O)c1 10.1016/j.bmcl.2010.09.142
CHEMBL567286 193772 0 None -229 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 366 4 0 3 3.1 N#Cc1cccc(N2CCN(CCN3CCC(C(F)(F)F)CC3)C2=O)c1 10.1016/j.bmcl.2010.09.142
4420454 55966 6 None 1 5 Human 6.8 pKi = 6.8 Binding
Dissociation constant of compound on one-site model Dopamine receptor D4.4Dissociation constant of compound on one-site model Dopamine receptor D4.4
ChEMBL 205 5 0 1 3.2 C#CC1=CCC(N(CCC)CCC)CC1 10.1021/jm991098z
CHEMBL162762 55966 6 None 1 5 Human 6.8 pKi = 6.8 Binding
Dissociation constant of compound on one-site model Dopamine receptor D4.4Dissociation constant of compound on one-site model Dopamine receptor D4.4
ChEMBL 205 5 0 1 3.2 C#CC1=CCC(N(CCC)CCC)CC1 10.1021/jm991098z
44304603 201448 0 None -1 4 Human 6.8 pKi = 6.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 471 8 1 5 5.2 COc1ccc(Br)cc1-c1nc(CNC[C@@H]2CCN(Cc3ccccc3)C2)cs1 10.1016/s0960-894x(00)00405-4
CHEMBL64139 201448 0 None -1 4 Human 6.8 pKi = 6.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 471 8 1 5 5.2 COc1ccc(Br)cc1-c1nc(CNC[C@@H]2CCN(Cc3ccccc3)C2)cs1 10.1016/s0960-894x(00)00405-4
44304621 201728 0 None -1 4 Human 6.8 pKi = 6.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 469 9 1 5 5.1 COc1ccc(Br)cc1-c1nc(CNCC[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL65641 201728 0 None -1 4 Human 6.8 pKi = 6.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 469 9 1 5 5.1 COc1ccc(Br)cc1-c1nc(CNCC[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
10276451 198601 33 None -2754 10 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in Sf9 cellsInhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in Sf9 cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm040190e
CHEMBL2112910 198601 33 None -2754 10 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in Sf9 cellsInhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in Sf9 cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm040190e
CHEMBL59725 198601 33 None -2754 10 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in Sf9 cellsInhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in Sf9 cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm040190e
44437897 152519 0 None -77 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 352 6 1 3 2.8 C=CCN1CCC[C@H]1CNC(=O)c1cc(Br)ccc1OC 10.1016/j.bmc.2007.07.017
CHEMBL397592 152519 0 None -77 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 352 6 1 3 2.8 C=CCN1CCC[C@H]1CNC(=O)c1cc(Br)ccc1OC 10.1016/j.bmc.2007.07.017
11615489 69100 1 None -3 4 Human 5.8 pKi = 5.8 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 221 5 0 3 2.3 CCCN(CCC)[C@H]1CCn2nccc2C1 10.1021/jm0503805
CHEMBL193337 69100 1 None -3 4 Human 5.8 pKi = 5.8 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 221 5 0 3 2.3 CCCN(CCC)[C@H]1CCn2nccc2C1 10.1021/jm0503805
11708363 71558 1 None -5 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 221 5 0 3 2.3 CCCN(CCC)[C@@H]1CCn2nccc2C1 10.1021/jm101639t
CHEMBL197159 71558 1 None -5 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 221 5 0 3 2.3 CCCN(CCC)[C@@H]1CCn2nccc2C1 10.1021/jm101639t
60167451 74998 0 None -26 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 468 7 1 6 5.3 O=C(CCCCN1CCC(n2c(=O)[nH]c3cc(Cl)ccc32)CC1)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL2037520 74998 0 None -26 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 468 7 1 6 5.3 O=C(CCCCN1CCC(n2c(=O)[nH]c3cc(Cl)ccc32)CC1)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
60167451 74998 0 None -26 7 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 468 7 1 6 5.3 O=C(CCCCN1CCC(n2c(=O)[nH]c3cc(Cl)ccc32)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL2037520 74998 0 None -26 7 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 468 7 1 6 5.3 O=C(CCCCN1CCC(n2c(=O)[nH]c3cc(Cl)ccc32)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
44338248 8267 0 None -3 3 Human 6.8 pKi = 6.8 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 458 6 1 2 6.7 Fc1ccc(C(OC2CC3CCC(C2)N3Cc2cc3ccccc3[nH]2)c2ccc(F)cc2)cc1 10.1021/jm010146o
CHEMBL109299 8267 0 None -3 3 Human 6.8 pKi = 6.8 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 458 6 1 2 6.7 Fc1ccc(C(OC2CC3CCC(C2)N3Cc2cc3ccccc3[nH]2)c2ccc(F)cc2)cc1 10.1021/jm010146o
155516494 169554 0 None 269 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 358 5 1 4 3.1 CCc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4443848 169554 0 None 269 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 358 5 1 4 3.1 CCc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
10438027 65857 0 None -645 6 Human 5.8 pKi = 5.8 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 571 7 1 4 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2o1 10.1021/jm900095y
CHEMBL184383 65857 0 None -645 6 Human 5.8 pKi = 5.8 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 571 7 1 4 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2o1 10.1021/jm900095y
11408135 123669 0 None -39 3 Rat 5.8 pKi = 5.8 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 443 7 1 4 4.5 COc1ccc2c(c1)N1CCN(CCCCNC(=O)c3ccc4ccccc4c3)C[C@H]1CC2 10.1021/jm049031l
CHEMBL363406 123669 0 None -39 3 Rat 5.8 pKi = 5.8 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 443 7 1 4 4.5 COc1ccc2c(c1)N1CCN(CCCCNC(=O)c3ccc4ccccc4c3)C[C@H]1CC2 10.1021/jm049031l
168292951 191550 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5203807 191550 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)cc1F 10.1016/j.bmcl.2022.128615
44582676 189187 0 None -1 17 Human 6.8 pKi = 6.8 Binding
Inhibition of human cloned dopamine D4 receptor by competitive binding experimentInhibition of human cloned dopamine D4 receptor by competitive binding experiment
ChEMBL 403 9 0 4 4.3 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL516088 189187 0 None -1 17 Human 6.8 pKi = 6.8 Binding
Inhibition of human cloned dopamine D4 receptor by competitive binding experimentInhibition of human cloned dopamine D4 receptor by competitive binding experiment
ChEMBL 403 9 0 4 4.3 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
44393658 123576 0 None - 1 Human 6.8 pKi = 6.8 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 475 7 1 3 5.9 Cc1cccc(NC(=O)CN2CCN(c3ccc(C(c4ccccc4)c4ccccc4)cc3)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL363308 123576 0 None - 1 Human 6.8 pKi = 6.8 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 475 7 1 3 5.9 Cc1cccc(NC(=O)CN2CCN(c3ccc(C(c4ccccc4)c4ccccc4)cc3)CC2)c1 10.1016/j.bmcl.2004.07.068
118643968 145437 0 None -22 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 498 10 1 4 4.0 [O-][S+](CCN1CCN(CC(O)Cc2ccccc2)CC1)C(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.ejmech.2020.112674
CHEMBL3918282 145437 0 None -22 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 498 10 1 4 4.0 [O-][S+](CCN1CCN(CC(O)Cc2ccccc2)CC1)C(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.ejmech.2020.112674
118643968 145437 0 None -22 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 498 10 1 4 4.0 [O-][S+](CCN1CCN(CC(O)Cc2ccccc2)CC1)C(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/acs.jmedchem.6b01373
CHEMBL3918282 145437 0 None -22 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 498 10 1 4 4.0 [O-][S+](CCN1CCN(CC(O)Cc2ccccc2)CC1)C(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/acs.jmedchem.6b01373
42626317 55959 0 None -346 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 422 8 3 5 2.5 COc1ccccc1N1CCN(CCC(O)CNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm900095y
CHEMBL1627322 55959 0 None -346 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 422 8 3 5 2.5 COc1ccccc1N1CCN(CCC(O)CNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm900095y
44350664 117646 0 None -1 6 Human 6.8 pKi = 6.8 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 351 6 0 2 5.2 O=C(CCCN1C2CCC1CC(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
CHEMBL340816 117646 0 None -1 6 Human 6.8 pKi = 6.8 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 351 6 0 2 5.2 O=C(CCCN1C2CCC1CC(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
CHEMBL553417 117646 0 None -1 6 Human 6.8 pKi = 6.8 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 351 6 0 2 5.2 O=C(CCCN1C2CCC1CC(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
44350664 117646 0 None -1 6 Human 6.8 pKi = 6.8 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 351 6 0 2 5.2 O=C(CCCN1C2CCC1CC(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL340816 117646 0 None -1 6 Human 6.8 pKi = 6.8 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 351 6 0 2 5.2 O=C(CCCN1C2CCC1CC(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL553417 117646 0 None -1 6 Human 6.8 pKi = 6.8 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 351 6 0 2 5.2 O=C(CCCN1C2CCC1CC(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
9931571 5263 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 413 5 1 4 2.5 O=C(O)[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL106827 5263 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 413 5 1 4 2.5 O=C(O)[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL5086564 213262 0 None -316 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCOC(=O)/C=C1\[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2C[C@@H]1C[C@H]1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.1c00611
71658204 89974 0 None -37 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 465 8 1 5 4.2 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(Br)s2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386618 89974 0 None -37 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 465 8 1 5 4.2 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(Br)s2)CC1 10.1016/j.bmc.2013.03.074
11351639 60200 0 None -95 5 Human 5.8 pKi = 5.8 Binding
Binding affinity for human dopamine D4 receptorBinding affinity for human dopamine D4 receptor
ChEMBL 459 6 1 4 5.3 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm049465g
CHEMBL175734 60200 0 None -95 5 Human 5.8 pKi = 5.8 Binding
Binding affinity for human dopamine D4 receptorBinding affinity for human dopamine D4 receptor
ChEMBL 459 6 1 4 5.3 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm049465g
11351639 60200 0 None -95 5 Human 5.8 pKi = 5.8 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 459 6 1 4 5.3 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm900095y
CHEMBL175734 60200 0 None -95 5 Human 5.8 pKi = 5.8 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 459 6 1 4 5.3 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm900095y
56593482 3878 1 None -162 9 Human 6.8 pKi = 6.8 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 462 7 1 5 4.6 O=C1CCc2c(N1)nc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
7650 3878 1 None -162 9 Human 6.8 pKi = 6.8 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 462 7 1 5 4.6 O=C1CCc2c(N1)nc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
CHEMBL2165119 3878 1 None -162 9 Human 6.8 pKi = 6.8 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 462 7 1 5 4.6 O=C1CCc2c(N1)nc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
3037308 43829 19 None -74 6 Human 6.8 pKi = 6.8 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 452 7 1 7 4.2 O=c1c(CO)coc2cc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)ccc12 10.1021/jm9810396
CHEMBL151475 43829 19 None -74 6 Human 6.8 pKi = 6.8 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 452 7 1 7 4.2 O=c1c(CO)coc2cc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)ccc12 10.1021/jm9810396
154727843 175859 1 None -1 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 486 13 0 6 5.6 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.9b01835
CHEMBL4448853 175859 1 None -1 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 486 13 0 6 5.6 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.9b01835
CHEMBL4596221 175859 1 None -1 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 486 13 0 6 5.6 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.9b01835
44394590 127027 0 None 50 2 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@@H]1CCN(Cc2ccccc2)C1)c1ccc(-c2ccsc2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL366304 127027 0 None 50 2 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@@H]1CCN(Cc2ccccc2)C1)c1ccc(-c2ccsc2)cc1 10.1016/j.bmcl.2004.07.045
71458071 79090 0 None 43 6 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 266 3 1 3 2.2 N#Cc1cc(CN2CCN(c3ccccc3)CC2)c[nH]1 10.1016/s0960-894x(02)00316-5
CHEMBL2113718 79090 0 None 43 6 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 266 3 1 3 2.2 N#Cc1cc(CN2CCN(c3ccccc3)CC2)c[nH]1 10.1016/s0960-894x(02)00316-5
10735405 205678 0 None 4 3 Human 7.8 pKi = 7.8 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 333 4 1 4 4.1 Oc1nc(-c2ccccc2)cn1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL93958 205678 0 None 4 3 Human 7.8 pKi = 7.8 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 333 4 1 4 4.1 Oc1nc(-c2ccccc2)cn1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
10947658 28490 0 None -16 16 Human 7.8 pKi = 7.8 Binding
Binding affinity against Dopamine receptor D4Binding affinity against Dopamine receptor D4
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
CHEMBL137781 28490 0 None -16 16 Human 7.8 pKi = 7.8 Binding
Binding affinity against Dopamine receptor D4Binding affinity against Dopamine receptor D4
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
44278789 99455 0 None 131 2 Human 7.8 pKi = 7.8 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 377 7 1 4 4.1 OC(COc1cccc2ccccc12)CN1CCC(Oc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
CHEMBL286177 99455 0 None 131 2 Human 7.8 pKi = 7.8 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 377 7 1 4 4.1 OC(COc1cccc2ccccc12)CN1CCC(Oc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
4088306 100171 6 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 359 7 1 3 4.0 OC(COc1ccc(Cl)cc1)CN1CCC(Cc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
CHEMBL29206 100171 6 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 359 7 1 3 4.0 OC(COc1ccc(Cl)cc1)CN1CCC(Cc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
135481864 12244 0 None 112 3 Human 7.8 pKi = 7.8 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 350 5 1 5 2.9 c1ccc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)cc1 10.1016/S0960-894X(97)00442-3
CHEMBL1185415 12244 0 None 112 3 Human 7.8 pKi = 7.8 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 350 5 1 5 2.9 c1ccc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)cc1 10.1016/S0960-894X(97)00442-3
CHEMBL412665 12244 0 None 112 3 Human 7.8 pKi = 7.8 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 350 5 1 5 2.9 c1ccc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)cc1 10.1016/S0960-894X(97)00442-3
10837494 205721 0 None 8 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 455 7 2 4 4.5 COc1cc(NC(=O)C2CCCC2)c(Cl)cc1C(=O)N[C@@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
CHEMBL94200 205721 0 None 8 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 455 7 2 4 4.5 COc1cc(NC(=O)C2CCCC2)c(Cl)cc1C(=O)N[C@@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
155516873 169561 0 None 28 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 445 9 2 6 2.9 O=C(NCCCN1CCN(c2ncccn2)CC1)NN(Cc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
CHEMBL4443944 169561 0 None 28 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 445 9 2 6 2.9 O=C(NCCCN1CCN(c2ncccn2)CC1)NN(Cc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
135398737 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm2013419
38 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm2013419
722 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm2013419
CHEMBL42 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm2013419
DB00363 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm2013419
25072635 111291 0 None -8 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccc12 10.1021/jm5004039
CHEMBL3287399 111291 0 None -8 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccc12 10.1021/jm5004039
11720302 165705 0 None -9 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 503 7 1 3 5.2 O=C(NCCCCN1CCN(c2cccc(F)c2F)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm060138d
CHEMBL426863 165705 0 None -9 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 503 7 1 3 5.2 O=C(NCCCCN1CCN(c2cccc(F)c2F)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm060138d
21219156 95382 0 None 67 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 332 4 0 4 4.1 Cc1nnn(C2CCN(Cc3ccccc3)CC2)c1-c1ccccc1 10.1016/s0960-894x(99)00169-9
CHEMBL25887 95382 0 None 67 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 332 4 0 4 4.1 Cc1nnn(C2CCN(Cc3ccccc3)CC2)c1-c1ccccc1 10.1016/s0960-894x(99)00169-9
44376241 119610 0 None 51 2 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 354 5 0 6 2.5 COc1ccc(OC[C@@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL351098 119610 0 None 51 2 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 354 5 0 6 2.5 COc1ccc(OC[C@@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
135398737 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0104825
38 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0104825
722 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0104825
CHEMBL42 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0104825
DB00363 944 89 None -13 91 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0104825
127032083 138917 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 323 5 1 4 2.8 c1ccc(OC[C@@H]2CN(Cc3n[nH]c4ccccc34)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793996 138917 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 323 5 1 4 2.8 c1ccc(OC[C@@H]2CN(Cc3n[nH]c4ccccc34)CCO2)cc1 10.1016/j.bmcl.2016.03.102
9967004 39120 1 None 45 3 Human 7.7 pKi = 7.7 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 323 3 1 4 2.3 O=C1COc2ccc(CN3CCN(c4ccccc4)CC3)cc2N1 10.1021/jm990277d
CHEMBL147130 39120 1 None 45 3 Human 7.7 pKi = 7.7 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 323 3 1 4 2.3 O=C1COc2ccc(CN3CCN(c4ccccc4)CC3)cc2N1 10.1021/jm990277d
44591045 176163 0 None 19 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 340 3 1 3 3.9 Clc1ccc(N2CCCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/j.bmc.2008.12.054
CHEMBL460223 176163 0 None 19 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 340 3 1 3 3.9 Clc1ccc(N2CCCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/j.bmc.2008.12.054
11681599 74823 0 None -338 6 Human 7.7 pKi = 7.7 Binding
Binding affinity to D4 dopamine receptor by radioligand binding assayBinding affinity to D4 dopamine receptor by radioligand binding assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2ccc(O)c(Cl)c2CC1 10.1021/jm051237e
CHEMBL203637 74823 0 None -338 6 Human 7.7 pKi = 7.7 Binding
Binding affinity to D4 dopamine receptor by radioligand binding assayBinding affinity to D4 dopamine receptor by radioligand binding assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2ccc(O)c(Cl)c2CC1 10.1021/jm051237e
44380697 57787 0 None 3 4 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 373 6 2 4 3.2 COc1cc(N)c(Cl)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL167414 57787 0 None 3 4 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 373 6 2 4 3.2 COc1cc(N)c(Cl)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
11624518 198659 3 None -1 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 352 4 0 4 3.8 Clc1ccc(-n2cc(CN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2013.05.027
CHEMBL597601 198659 3 None -1 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 352 4 0 4 3.8 Clc1ccc(-n2cc(CN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2013.05.027
60165413 75010 0 None -52 7 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 378 7 0 4 5.5 O=C(CCCCN1CCC(c2ccccc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL2037531 75010 0 None -52 7 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 378 7 0 4 5.5 O=C(CCCCN1CCC(c2ccccc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
122189392 122731 0 None -81 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 441 5 0 7 3.6 Clc1cccc(N2CCN(CCc3cn(-c4ccn5nccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.07.050
CHEMBL3613878 122731 0 None -81 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 441 5 0 7 3.6 Clc1cccc(N2CCN(CCc3cn(-c4ccn5nccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.07.050
122177642 120697 0 None -81 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 551 18 1 8 4.6 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cn(CCCC)nn3)c(OC)c2)CO1 10.1021/jm501889t
CHEMBL3577343 120697 0 None -81 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 551 18 1 8 4.6 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cn(CCCC)nn3)c(OC)c2)CO1 10.1021/jm501889t
11348526 6284 0 None - 1 Human 6.8 pKi = 6.8 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 345 7 0 4 3.5 CCOc1ccccc1OCC1CN(Cc2ccc(F)cc2)CCO1 10.1021/jm031111m
CHEMBL108211 6284 0 None - 1 Human 6.8 pKi = 6.8 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 345 7 0 4 3.5 CCOc1ccccc1OCC1CN(Cc2ccc(F)cc2)CCO1 10.1021/jm031111m
10786474 205441 0 None - 1 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 387 6 0 4 3.2 COc1cccc(C(=O)N(C)CCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
CHEMBL92411 205441 0 None - 1 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 387 6 0 4 3.2 COc1cccc(C(=O)N(C)CCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
44371996 53341 0 None 2 4 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 500 6 0 6 4.6 Clc1ccc(N2CCN(Cc3cnn4c(N5CCN(Cc6ccccc6)CC5)cccc34)CC2)cc1 10.1016/s0960-894x(01)00814-9
CHEMBL160266 53341 0 None 2 4 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 500 6 0 6 4.6 Clc1ccc(N2CCN(Cc3cnn4c(N5CCN(Cc6ccccc6)CC5)cccc34)CC2)cc1 10.1016/s0960-894x(01)00814-9
11223708 165756 0 None -11 3 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 413 6 1 3 4.5 O=C(NCCCCN1CCN2c3ccccc3CC[C@H]2C1)c1ccc2ccccc2c1 10.1021/jm049031l
CHEMBL427173 165756 0 None -11 3 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 413 6 1 3 4.5 O=C(NCCCCN1CCN2c3ccccc3CC[C@H]2C1)c1ccc2ccccc2c1 10.1021/jm049031l
44263882 96776 0 None 2 3 Human 5.8 pKi = 5.8 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 376 3 0 4 4.5 Clc1ccc(N2CCN(Cc3cnn4ccc5ccccc5c34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL268558 96776 0 None 2 3 Human 5.8 pKi = 5.8 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 376 3 0 4 4.5 Clc1ccc(N2CCN(Cc3cnn4ccc5ccccc5c34)CC2)cc1 10.1016/s0960-894x(98)00692-1
45482180 196227 0 None -218 4 Human 5.8 pKi = 5.8 Binding
Binding affinity to human cloned dopamine D4.4 expressed in CHO cellsBinding affinity to human cloned dopamine D4.4 expressed in CHO cells
ChEMBL 544 12 1 7 4.6 COc1ccc(-n2cc(CCCC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)nn2)cc1 10.1016/j.bmc.2009.06.041
CHEMBL572867 196227 0 None -218 4 Human 5.8 pKi = 5.8 Binding
Binding affinity to human cloned dopamine D4.4 expressed in CHO cellsBinding affinity to human cloned dopamine D4.4 expressed in CHO cells
ChEMBL 544 12 1 7 4.6 COc1ccc(-n2cc(CCCC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)nn2)cc1 10.1016/j.bmc.2009.06.041
25139478 184373 0 None -138 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 510 10 0 4 7.5 CCCN(CCCCn1cc(-c2ccc(-c3ccccc3)cc2)nn1)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm800895v
CHEMBL485384 184373 0 None -138 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 510 10 0 4 7.5 CCCN(CCCCn1cc(-c2ccc(-c3ccccc3)cc2)nn1)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm800895v
44319361 204007 0 None -1 4 Human 5.8 pKi = 5.8 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 337 4 0 4 3.4 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CS2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL82527 204007 0 None -1 4 Human 5.8 pKi = 5.8 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 337 4 0 4 3.4 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CS2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL5084145 213126 0 None -977 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CN(C)C(=O)C(CCN1CCc2ccc(C#N)cc2C1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
21559988 112928 2 None -28 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 389 5 1 3 4.0 O=C(CCC(=O)N1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2014.06.079
CHEMBL3318852 112928 2 None -28 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 389 5 1 3 4.0 O=C(CCC(=O)N1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2014.06.079
168279082 190139 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5182602 190139 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)c1 10.1016/j.bmcl.2022.128615
44431485 87644 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 389 5 1 4 4.1 O=C(NC1CCN(Cc2ccc([N+](=O)[O-])cc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
CHEMBL234644 87644 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 389 5 1 4 4.1 O=C(NC1CCN(Cc2ccc([N+](=O)[O-])cc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
44415569 165381 0 None -1148 6 Human 5.7 pKi = 5.7 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 505 4 1 7 4.5 COc1cccc(OC)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
CHEMBL425069 165381 0 None -1148 6 Human 5.7 pKi = 5.7 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 505 4 1 7 4.5 COc1cccc(OC)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
51354275 59868 0 None -165 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 479 10 1 5 4.9 O=C(NC/C=C/CN1CCN(c2ccccc2OCCF)CC1)c1ccc(-c2ccsc2)cc1 10.1021/jm101323b
CHEMBL1689012 59868 0 None -165 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 479 10 1 5 4.9 O=C(NC/C=C/CN1CCN(c2ccccc2OCCF)CC1)c1ccc(-c2ccsc2)cc1 10.1021/jm101323b
CHEMBL1739787 59868 0 None -165 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 479 10 1 5 4.9 O=C(NC/C=C/CN1CCN(c2ccccc2OCCF)CC1)c1ccc(-c2ccsc2)cc1 10.1021/jm101323b
12280580 43819 1 None -2 3 Human 6.7 pKi = 6.7 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 247 5 1 2 3.4 CCCN(CCC)[C@@H]1CCc2c(O)cccc2C1 10.1021/jm960345l
CHEMBL15146 43819 1 None -2 3 Human 6.7 pKi = 6.7 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 247 5 1 2 3.4 CCCN(CCC)[C@@H]1CCc2c(O)cccc2C1 10.1021/jm960345l
71062889 147742 0 None 19 5 Mouse 6.7 pKi = 6.7 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 5 0 5 1.8 O=C(CN1CCO[C@H](COc2cccnc2)C1)N1CCc2ccccc21 nan
CHEMBL3936595 147742 0 None 19 5 Mouse 6.7 pKi = 6.7 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 5 0 5 1.8 O=C(CN1CCO[C@H](COc2cccnc2)C1)N1CCc2ccccc21 nan
10894276 41082 0 None - 1 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 383 2 1 5 4.3 Cc1ccc2c(c1)C(N1CCN(Cc3ccccc3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL148965 41082 0 None - 1 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 383 2 1 5 4.3 Cc1ccc2c(c1)C(N1CCN(Cc3ccccc3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
168280464 190142 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 335 5 0 4 3.8 Cc1ccccc1CO[C@H]1CCCN(Cc2cn3ccccc3n2)C1 10.1016/j.bmcl.2022.128615
CHEMBL5182635 190142 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 335 5 0 4 3.8 Cc1ccccc1CO[C@H]1CCCN(Cc2cn3ccccc3n2)C1 10.1016/j.bmcl.2022.128615
154703764 175736 1 None -46 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 505 13 1 4 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4455719 175736 1 None -46 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 505 13 1 4 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4595265 175736 1 None -46 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 505 13 1 4 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
71458739 81411 0 None -112 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 466 7 0 5 4.7 COc1ccccc1N1CCN(CCN(C(=O)c2ccc3ccccc3c2)c2ccccn2)CC1 10.1016/j.bmcl.2012.05.119
CHEMBL2164347 81411 0 None -112 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 466 7 0 5 4.7 COc1ccccc1N1CCN(CCN(C(=O)c2ccc3ccccc3c2)c2ccccn2)CC1 10.1016/j.bmcl.2012.05.119
16090821 81421 0 None -47 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human D4 dopamine receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 dopamine receptor expressed in CHO cells
ChEMBL 304 0 1 1 4.2 CN1CCCc2c([nH]c3ccccc23)Cc2ccccc2CC1 10.1021/jm060213k
CHEMBL216439 81421 0 None -47 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human D4 dopamine receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 dopamine receptor expressed in CHO cells
ChEMBL 304 0 1 1 4.2 CN1CCCc2c([nH]c3ccccc23)Cc2ccccc2CC1 10.1021/jm060213k
53248673 66071 0 None -724 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 441 10 1 5 3.9 O=C1CCc2ccc(OCCCCN3CCN(c4ccccc4OCCF)CC3)cc2N1 10.1016/j.bmc.2011.04.021
CHEMBL1813591 66071 0 None -724 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 441 10 1 5 3.9 O=C1CCc2ccc(OCCCCN3CCN(c4ccccc4OCCF)CC3)cc2N1 10.1016/j.bmc.2011.04.021
CHEMBL1851831 66071 0 None -724 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 441 10 1 5 3.9 O=C1CCc2ccc(OCCCCN3CCN(c4ccccc4OCCF)CC3)cc2N1 10.1016/j.bmc.2011.04.021
90644071 111550 0 None 1 5 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 368 5 0 3 5.2 Clc1ccc(N2CCCN(CCCc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289655 111550 0 None 1 5 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 368 5 0 3 5.2 Clc1ccc(N2CCCN(CCCc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
37461 16953 10 None -208 8 Human 6.7 pKi = 6.7 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 361 0 1 2 4.8 CC(C)(C)[C@@]1(O)CCN2C[C@@H]3c4ccccc4CCc4cccc(c43)[C@H]2C1 10.1016/S0960-894X(97)00194-7
CHEMBL1255588 16953 10 None -208 8 Human 6.7 pKi = 6.7 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 361 0 1 2 4.8 CC(C)(C)[C@@]1(O)CCN2C[C@@H]3c4ccccc4CCc4cccc(c43)[C@H]2C1 10.1016/S0960-894X(97)00194-7
10436285 101482 0 None -954 5 Human 5.7 pKi = 5.7 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 507 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2=O 10.1021/jm010146o
CHEMBL301242 101482 0 None -954 5 Human 5.7 pKi = 5.7 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 507 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2=O 10.1021/jm010146o
1599 2309 47 None -2238 15 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
3955 2309 47 None -2238 15 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
7215 2309 47 None -2238 15 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
CHEMBL841 2309 47 None -2238 15 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
DB00836 2309 47 None -2238 15 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
10436285 101482 0 None -954 5 Human 5.7 pKi = 5.7 Binding
Inhibition of [3H]YM-09151-2 binding to human Dopamine D4 receptor expressed in CHO cellsInhibition of [3H]YM-09151-2 binding to human Dopamine D4 receptor expressed in CHO cells
ChEMBL 507 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2=O 10.1021/jm040190e
CHEMBL301242 101482 0 None -954 5 Human 5.7 pKi = 5.7 Binding
Inhibition of [3H]YM-09151-2 binding to human Dopamine D4 receptor expressed in CHO cellsInhibition of [3H]YM-09151-2 binding to human Dopamine D4 receptor expressed in CHO cells
ChEMBL 507 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2=O 10.1021/jm040190e
118719796 115223 0 None -102 4 Human 6.7 pKi = 6.7 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 456 9 0 7 4.4 COc1ccccc1N1CCN(CCCCCc2cn(-c3cccc4cnccc34)nn2)CC1 10.1016/j.bmcl.2014.12.023
CHEMBL3353899 115223 0 None -102 4 Human 6.7 pKi = 6.7 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 456 9 0 7 4.4 COc1ccccc1N1CCN(CCCCCc2cn(-c3cccc4cnccc34)nn2)CC1 10.1016/j.bmcl.2014.12.023
164608999 183802 0 None -141 6 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 310 6 1 4 2.8 Nc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
CHEMBL4845741 183802 0 None -141 6 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 310 6 1 4 2.8 Nc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
71659909 89960 0 None -263 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 463 9 1 5 5.1 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(-c3ccsc3)cc2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386604 89960 0 None -263 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 463 9 1 5 5.1 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(-c3ccsc3)cc2)CC1 10.1016/j.bmc.2013.03.074
168271806 189925 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 353 5 0 4 4.0 Cc1cc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)ccc1F 10.1016/j.bmcl.2022.128615
CHEMBL5179482 189925 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 353 5 0 4 4.0 Cc1cc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)ccc1F 10.1016/j.bmcl.2022.128615
44415690 79727 0 None -851 6 Human 5.7 pKi = 5.7 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 473 2 1 5 5.1 Cc1cccc(C)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
CHEMBL213336 79727 0 None -851 6 Human 5.7 pKi = 5.7 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 473 2 1 5 5.1 Cc1cccc(C)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
164608999 183802 0 None -141 6 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 310 6 1 4 2.8 Nc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
CHEMBL4845741 183802 0 None -141 6 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 310 6 1 4 2.8 Nc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
135887931 11962 0 None 14 2 Human 6.7 pKi = 6.7 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 364 6 1 5 3.3 c1ccc(N2CCN(CCCCNC3=Nc4ccccc4OC3)CC2)cc1 10.1016/S0960-894X(97)00442-3
CHEMBL1183657 11962 0 None 14 2 Human 6.7 pKi = 6.7 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 364 6 1 5 3.3 c1ccc(N2CCN(CCCCNC3=Nc4ccccc4OC3)CC2)cc1 10.1016/S0960-894X(97)00442-3
CHEMBL309858 11962 0 None 14 2 Human 6.7 pKi = 6.7 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 364 6 1 5 3.3 c1ccc(N2CCN(CCCCNC3=Nc4ccccc4OC3)CC2)cc1 10.1016/S0960-894X(97)00442-3
122205437 136787 0 None -61 5 Human 6.7 pKi = 6.7 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2sccc2CC1 10.1039/C5MD00258C
CHEMBL3752512 136787 0 None -61 5 Human 6.7 pKi = 6.7 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2sccc2CC1 10.1039/C5MD00258C
71658073 89968 0 None -24 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 401 8 1 5 3.8 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(C)s2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386612 89968 0 None -24 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 401 8 1 5 3.8 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(C)s2)CC1 10.1016/j.bmc.2013.03.074
72191067 91924 0 None -14 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-spiperone from cloned human dopamine D4 receptorDisplacement of [3H]-spiperone from cloned human dopamine D4 receptor
ChEMBL 392 8 0 7 3.0 COc1ccccc1N1CCN(CCCCn2cc(-c3cccnc3)nn2)CC1 10.1016/j.bmcl.2013.08.047
CHEMBL2430439 91924 0 None -14 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-spiperone from cloned human dopamine D4 receptorDisplacement of [3H]-spiperone from cloned human dopamine D4 receptor
ChEMBL 392 8 0 7 3.0 COc1ccccc1N1CCN(CCCCn2cc(-c3cccnc3)nn2)CC1 10.1016/j.bmcl.2013.08.047
10497179 203401 1 None 3 3 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 337 5 1 3 4.6 c1ccc(CCN2CCC(c3cc(-c4cccs4)[nH]n3)CC2)cc1 10.1021/jm970111h
CHEMBL77743 203401 1 None 3 3 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 337 5 1 3 4.6 c1ccc(CCN2CCC(c3cc(-c4cccs4)[nH]n3)CC2)cc1 10.1021/jm970111h
135492584 11228 0 None 95 3 Human 7.7 pKi = 7.7 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 380 7 1 7 2.5 c1cnc(N2CCN(CCCCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL1179503 11228 0 None 95 3 Human 7.7 pKi = 7.7 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 380 7 1 7 2.5 c1cnc(N2CCN(CCCCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL80645 11228 0 None 95 3 Human 7.7 pKi = 7.7 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 380 7 1 7 2.5 c1cnc(N2CCN(CCCCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
44380715 58704 0 None 2 4 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 387 7 2 4 3.6 CNc1cc(OC)c(C(=O)NC[C@@H]2CCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(99)00086-4
CHEMBL169222 58704 0 None 2 4 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 387 7 2 4 3.6 CNc1cc(OC)c(C(=O)NC[C@@H]2CCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(99)00086-4
10639353 114298 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 319 3 0 3 4.2 O=c1ccc2ccc(CN3CCC(c4ccccc4)CC3)cc2o1 10.1021/jm990266k
CHEMBL333983 114298 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 319 3 0 3 4.2 O=c1ccc2ccc(CN3CCC(c4ccccc4)CC3)cc2o1 10.1021/jm990266k
155560295 174475 0 None 19 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 463 9 2 6 3.0 O=C(NCCCN1CCN(c2ncccn2)CC1)NN(Cc1ccc(F)cc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
CHEMBL4567758 174475 0 None 19 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 463 9 2 6 3.0 O=C(NCCCN1CCN(c2ncccn2)CC1)NN(Cc1ccc(F)cc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
10224165 168493 0 None 10 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 423 3 0 3 4.1 CC1(C)Cc2cccc3c2N1C(=O)C(N1CCN(Cc2ccc(Cl)cc2)CC1)CC3 10.1016/s0960-894x(02)01056-9
CHEMBL439646 168493 0 None 10 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 423 3 0 3 4.1 CC1(C)Cc2cccc3c2N1C(=O)C(N1CCN(Cc2ccc(Cl)cc2)CC1)CC3 10.1016/s0960-894x(02)01056-9
135398745 2869 108 None -10 65 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C5MD00258C
47 2869 108 None -10 65 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C5MD00258C
CHEMBL715 2869 108 None -10 65 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C5MD00258C
DB00334 2869 108 None -10 65 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C5MD00258C
52947756 16988 0 None -4 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 567 6 0 2 8.3 O=C(CCCN1CCC(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
CHEMBL1256170 16988 0 None -4 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 567 6 0 2 8.3 O=C(CCCN1CCC(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
11742798 96666 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 418 7 2 6 2.5 COc1cc(N)c(Cl)cc1C(=O)NCCN1CCN(c2ccccc2OC)CC1 10.1016/S0960-894X(97)00218-7
CHEMBL26758 96666 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 418 7 2 6 2.5 COc1cc(N)c(Cl)cc1C(=O)NCCN1CCN(c2ccccc2OC)CC1 10.1016/S0960-894X(97)00218-7
53364154 63512 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1013 31 0 16 9.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803025 63512 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1013 31 0 16 9.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
53364227 63516 0 None -3 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1033 32 0 19 6.3 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCOCCOCCOCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803029 63516 0 None -3 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1033 32 0 19 6.3 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCOCCOCCOCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
53363202 63525 0 None -1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 961 28 0 15 8.7 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(C5CCCCC5)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803055 63525 0 None -1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 961 28 0 15 8.7 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(C5CCCCC5)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
118709176 112925 0 None -13 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1106 29 0 14 11.8 O=C(CCc1cn(CCCCCCCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318849 112925 0 None -13 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1106 29 0 14 11.8 O=C(CCc1cn(CCCCCCCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
137644833 157594 0 None -3 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C=O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4087187 157594 0 None -3 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C=O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
71459760 83658 0 None 3 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 398 5 0 3 5.3 CCCC#Cc1cc(CN2CCN(c3ccccc3OC)CC2)c2cccccc1-2 10.1016/j.bmcl.2012.09.064
CHEMBL2207634 83658 0 None 3 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 398 5 0 3 5.3 CCCC#Cc1cc(CN2CCN(c3ccccc3OC)CC2)c2cccccc1-2 10.1016/j.bmcl.2012.09.064
13091273 181856 0 None -8 6 Human 7.7 pKi = 7.7 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 367 6 1 3 4.3 O=C(CCCN1C2CCC1CC(O)(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
CHEMBL478617 181856 0 None -8 6 Human 7.7 pKi = 7.7 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 367 6 1 3 4.3 O=C(CCCN1C2CCC1CC(O)(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
CHEMBL553327 181856 0 None -8 6 Human 7.7 pKi = 7.7 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 367 6 1 3 4.3 O=C(CCCN1C2CCC1CC(O)(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
127053219 138934 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 335 5 0 3 3.8 Fc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3794174 138934 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 335 5 0 3 3.8 Fc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
13091273 181856 0 None -8 6 Human 7.7 pKi = 7.7 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 367 6 1 3 4.3 O=C(CCCN1C2CCC1CC(O)(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL478617 181856 0 None -8 6 Human 7.7 pKi = 7.7 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 367 6 1 3 4.3 O=C(CCCN1C2CCC1CC(O)(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL553327 181856 0 None -8 6 Human 7.7 pKi = 7.7 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 367 6 1 3 4.3 O=C(CCCN1C2CCC1CC(O)(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL5083441 213087 0 None 9 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCc1cccc(N2CCN(CCC(c3cccc(O)c3)c3cccc(O)c3)CC2)c1Cl 10.1021/acs.jmedchem.1c00611
90644062 111542 0 None 8 5 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 345 6 0 4 3.8 Cc1ccc(N2CCN(CCCSc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289647 111542 0 None 8 5 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 345 6 0 4 3.8 Cc1ccc(N2CCN(CCCSc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
44372296 118982 0 None 72 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 356 4 1 5 2.8 OCc1ccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn2c1 10.1021/jm0611152
CHEMBL345357 118982 0 None 72 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 356 4 1 5 2.8 OCc1ccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn2c1 10.1021/jm0611152
10690882 195857 0 None 501 2 Human 7.7 pKi = 7.7 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 375 6 0 4 4.5 COc1cc2ccccc2cc1C(=O)OCC1CCN(Cc2ccccc2)C1 10.1021/jm960017l
CHEMBL57019 195857 0 None 501 2 Human 7.7 pKi = 7.7 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 375 6 0 4 4.5 COc1cc2ccccc2cc1C(=O)OCC1CCN(Cc2ccccc2)C1 10.1021/jm960017l
10548329 200941 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 388 6 1 3 4.5 COc1cc2ccccc2cc1C(=O)NCC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
CHEMBL61248 200941 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 388 6 1 3 4.5 COc1cc2ccccc2cc1C(=O)NCC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
44273741 78098 0 None 31 2 Human 7.7 pKi = 7.7 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 429 7 1 3 4.6 O=C(NCCCCN1CCN(c2ccc(Cl)cc2)CC1)C12CC3CC(CC(C3)C1)C2 10.1016/0960-894X(96)00198-9
CHEMBL21119 78098 0 None 31 2 Human 7.7 pKi = 7.7 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 429 7 1 3 4.6 O=C(NCCCCN1CCN(c2ccc(Cl)cc2)CC1)C12CC3CC(CC(C3)C1)C2 10.1016/0960-894X(96)00198-9
137644962 157947 0 None 74 8 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 363 6 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4091058 157947 0 None 74 8 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 363 6 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
135398745 2869 108 None -10 65 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
47 2869 108 None -10 65 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
CHEMBL715 2869 108 None -10 65 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
DB00334 2869 108 None -10 65 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
11779642 205132 0 None -2 3 Human 6.7 pKi = 6.7 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 301 1 0 1 5.0 C[C@@H]1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL90654 205132 0 None -2 3 Human 6.7 pKi = 6.7 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 301 1 0 1 5.0 C[C@@H]1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
25139479 183735 0 None -21 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 438 10 0 4 6.2 C#CC1=CCC(N(CCC)CCCCn2cc(-c3ccc(-c4ccccc4)cc3)nn2)CC1 10.1021/jm800895v
CHEMBL484202 183735 0 None -21 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 438 10 0 4 6.2 C#CC1=CCC(N(CCC)CCCCn2cc(-c3ccc(-c4ccccc4)cc3)nn2)CC1 10.1021/jm800895v
57390119 68961 0 None -45 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 969 33 2 14 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928127 68961 0 None -45 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 969 33 2 14 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
137655556 157993 0 None -56 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 447 7 2 7 3.3 O=c1ccc2c(N3CCCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2[nH]1 10.1021/acs.jmedchem.7b00363
CHEMBL4091507 157993 0 None -56 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 447 7 2 7 3.3 O=c1ccc2c(N3CCCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2[nH]1 10.1021/acs.jmedchem.7b00363
44436610 91517 0 None -25 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 505 7 1 3 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc(C#Cc2ccccc2)c1 10.1016/j.bmc.2007.08.038
CHEMBL241436 91517 0 None -25 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 505 7 1 3 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc(C#Cc2ccccc2)c1 10.1016/j.bmc.2007.08.038
52937777 60843 0 None -323 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 464 10 1 4 5.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCn2ncc(Cl)c2C1 10.1021/jm101639t
CHEMBL1765630 60843 0 None -323 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 464 10 1 4 5.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCn2ncc(Cl)c2C1 10.1021/jm101639t
155562543 174600 0 None -3 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 353 4 0 4 3.2 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccccn2)CC1 10.1016/j.bmc.2020.115943
CHEMBL4570411 174600 0 None -3 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 353 4 0 4 3.2 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccccn2)CC1 10.1016/j.bmc.2020.115943
10667966 56865 0 None 1 4 Human 5.7 pKi = 5.7 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 387 5 0 1 6.1 CCCN(CCC)C1CCC(=C(C#C[Si](C)(C)C)C#C[Si](C)(C)C)CC1 10.1021/jm991098z
CHEMBL164736 56865 0 None 1 4 Human 5.7 pKi = 5.7 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 387 5 0 1 6.1 CCCN(CCC)C1CCC(=C(C#C[Si](C)(C)C)C#C[Si](C)(C)C)CC1 10.1021/jm991098z
42626240 55944 0 None -239 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in human HEK293 cell membrane for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in human HEK293 cell membrane for 1 hr by liquid scintillation counting analysis
ChEMBL 460 7 3 4 3.8 O=C(NCC[C@H](O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/ml500006v
CHEMBL1627307 55944 0 None -239 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in human HEK293 cell membrane for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in human HEK293 cell membrane for 1 hr by liquid scintillation counting analysis
ChEMBL 460 7 3 4 3.8 O=C(NCC[C@H](O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/ml500006v
11626748 139629 0 None -2 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 459 4 0 7 3.1 CN1CCN(c2ccc3nc(CN4CCN(c5ccc(Cl)c(Cl)c5)CC4)cn3n2)CC1 10.1021/jm060166w
CHEMBL380287 139629 0 None -2 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 459 4 0 7 3.1 CN1CCN(c2ccc3nc(CN4CCN(c5ccc(Cl)c(Cl)c5)CC4)cn3n2)CC1 10.1021/jm060166w
155562543 174600 0 None -3 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 353 4 0 4 3.2 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccccn2)CC1 10.1016/j.bmc.2020.115943
CHEMBL4570411 174600 0 None -3 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 353 4 0 4 3.2 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccccn2)CC1 10.1016/j.bmc.2020.115943
22910005 11494 1 None -147 5 Human 6.7 pKi = 6.7 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)OC(CNCc1ccccc1)CC2 10.1021/jm9703653
CHEMBL1180629 11494 1 None -147 5 Human 6.7 pKi = 6.7 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)OC(CNCc1ccccc1)CC2 10.1021/jm9703653
CHEMBL135395 11494 1 None -147 5 Human 6.7 pKi = 6.7 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)OC(CNCc1ccccc1)CC2 10.1021/jm9703653
25141535 55945 0 None -1380 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 422 8 3 5 2.5 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm900095y
CHEMBL1627308 55945 0 None -1380 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 422 8 3 5 2.5 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm900095y
10515841 206524 0 None -54 3 Human 6.7 pKi = 6.7 Binding
Tested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cellsTested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cells
ChEMBL 265 2 1 4 2.7 CCCN1CCO[C@@H]2c3cc(O)ccc3SC[C@@H]21 10.1021/jm0000113
CHEMBL98836 206524 0 None -54 3 Human 6.7 pKi = 6.7 Binding
Tested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cellsTested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cells
ChEMBL 265 2 1 4 2.7 CCCN1CCO[C@@H]2c3cc(O)ccc3SC[C@@H]21 10.1021/jm0000113
71062567 159868 0 None -2 2 Mouse 5.7 pKi = 5.7 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 6 0 5 2.5 Cc1ccnc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL4111349 159868 0 None -2 2 Mouse 5.7 pKi = 5.7 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 6 0 5 2.5 Cc1ccnc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
168280776 190564 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5188602 190564 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.bmcl.2022.128615
134136246 142006 0 None -2 6 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 275 3 0 1 4.1 C1=C(CCN2CCc3ccccc3C2)Cc2ccccc21 10.1016/j.bmc.2016.09.019
CHEMBL3890841 142006 0 None -2 6 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 275 3 0 1 4.1 C1=C(CCN2CCc3ccccc3C2)Cc2ccccc21 10.1016/j.bmc.2016.09.019
134136246 142006 0 None -2 6 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 275 3 0 1 4.1 C1=C(CCN2CCc3ccccc3C2)Cc2ccccc21 10.1016/j.bmc.2016.09.019
CHEMBL3890841 142006 0 None -2 6 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 275 3 0 1 4.1 C1=C(CCN2CCc3ccccc3C2)Cc2ccccc21 10.1016/j.bmc.2016.09.019
44438227 93122 0 None -18 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 354 4 2 2 4.3 OCC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246437 93122 0 None -18 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 354 4 2 2 4.3 OCC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
25130157 102832 0 None -275 6 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]IABN from human dopamine D4 receptorDisplacement of [125I]IABN from human dopamine D4 receptor
ChEMBL 367 3 1 3 5.1 O[C@]1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2Cc1coc2ccccc12 10.1021/jm800532x
CHEMBL3084515 102832 0 None -275 6 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]IABN from human dopamine D4 receptorDisplacement of [125I]IABN from human dopamine D4 receptor
ChEMBL 367 3 1 3 5.1 O[C@]1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2Cc1coc2ccccc12 10.1021/jm800532x
130431303 172368 0 None -173 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 419 8 3 5 2.2 CCc1cccc(N2CCN(CC(O)CCNC(=O)c3nc(C)c[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4516799 172368 0 None -173 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 419 8 3 5 2.2 CCc1cccc(N2CCN(CC(O)CCNC(=O)c3nc(C)c[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
3246443 37453 2 None -316 6 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor after 1 hrDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor after 1 hr
ChEMBL 325 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmcl.2017.01.090
CHEMBL1457510 37453 2 None -316 6 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor after 1 hrDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor after 1 hr
ChEMBL 325 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmcl.2017.01.090
1353 1880 85 None -3 85 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
3559 1880 85 None -3 85 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
86 1880 85 None -3 85 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
CHEMBL54 1880 85 None -3 85 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
DB00502 1880 85 None -3 85 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
22727335 13374 0 None -20 3 Human 6.7 pKi = 6.7 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 391 8 0 5 4.5 COc1ccccc1N1CCN(CCCCc2cc(-c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL1193307 13374 0 None -20 3 Human 6.7 pKi = 6.7 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 391 8 0 5 4.5 COc1ccccc1N1CCN(CCCCc2cc(-c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL544689 13374 0 None -20 3 Human 6.7 pKi = 6.7 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 391 8 0 5 4.5 COc1ccccc1N1CCN(CCCCc2cc(-c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
168280974 190269 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5184607 190269 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
10524285 200734 0 None 6 2 Human 6.7 pKi = 6.7 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 387 7 0 3 5.3 COc1cc2ccccc2cc1CC(=O)CC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
CHEMBL61090 200734 0 None 6 2 Human 6.7 pKi = 6.7 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 387 7 0 3 5.3 COc1cc2ccccc2cc1CC(=O)CC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
42273483 164743 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 337 5 1 3 3.0 CC(C)(C)C(=O)NCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL423287 164743 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 337 5 1 3 3.0 CC(C)(C)C(=O)NCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
75306277 108767 0 None -99 23 Human 6.7 pKi = 6.7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
CHEMBL3217984 108767 0 None -99 23 Human 6.7 pKi = 6.7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
11384664 82699 0 None -234 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 421 7 1 3 4.8 O=C(NCCCCN1CCN(c2ccccc2Cl)CC1)c1ccc2ccccc2c1 10.1021/jm0611152
CHEMBL218203 82699 0 None -234 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 421 7 1 3 4.8 O=C(NCCCCN1CCN(c2ccccc2Cl)CC1)c1ccc2ccccc2c1 10.1021/jm0611152
153287574 174675 0 None -26 10 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-methylspiperone from human recombinant dopamine D4 receptor expressed in Stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-methylspiperone from human recombinant dopamine D4 receptor expressed in Stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 266 2 1 2 4.0 CC[C@H]1c2ccccc2N(c2ccccc2)C[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
CHEMBL4572167 174675 0 None -26 10 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-methylspiperone from human recombinant dopamine D4 receptor expressed in Stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-methylspiperone from human recombinant dopamine D4 receptor expressed in Stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 266 2 1 2 4.0 CC[C@H]1c2ccccc2N(c2ccccc2)C[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
10245409 49520 0 None 99 3 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 319 5 1 2 4.4 c1ccc(CCC2CCN(Cc3cc4ccc[nH]c-4n3)CC2)cc1 10.1016/s0960-894x(99)00025-6
CHEMBL156732 49520 0 None 99 3 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 319 5 1 2 4.4 c1ccc(CCC2CCN(Cc3cc4ccc[nH]c-4n3)CC2)cc1 10.1016/s0960-894x(99)00025-6
44214767 66707 0 None 602 2 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2ccsc2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL187122 66707 0 None 602 2 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2ccsc2)cc1 10.1016/j.bmcl.2004.07.045
44394666 125271 0 None 501 2 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@H]1CCN(Cc2ccccc2)C1)c1ccc(-c2ccsc2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL364782 125271 0 None 501 2 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@H]1CCN(Cc2ccccc2)C1)c1ccc(-c2ccsc2)cc1 10.1016/j.bmcl.2004.07.045
44394742 165568 0 None 34 2 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@H]1CCN(Cc2ccccc2)C1)c1cccc(-c2ccsc2)c1 10.1016/j.bmcl.2004.07.045
CHEMBL426062 165568 0 None 34 2 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@H]1CCN(Cc2ccccc2)C1)c1cccc(-c2ccsc2)c1 10.1016/j.bmcl.2004.07.045
210956 205017 5 None 3 3 Human 8.7 pKi = 8.7 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 292 1 0 3 3.5 CN1CCN(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL89970 205017 5 None 3 3 Human 8.7 pKi = 8.7 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 292 1 0 3 3.5 CN1CCN(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
10570080 106650 0 None 41 3 Human 8.7 pKi = 8.7 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 353 4 1 4 4.8 Cc1c(-c2ccccc2)nc(O)n1C1CCN(CC2CCCCC2)CC1 10.1021/jm991029k
CHEMBL316125 106650 0 None 41 3 Human 8.7 pKi = 8.7 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 353 4 1 4 4.8 Cc1c(-c2ccccc2)nc(O)n1C1CCN(CC2CCCCC2)CC1 10.1021/jm991029k
210956 205017 5 None 3 3 Human 8.7 pKi = 8.7 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 292 1 0 3 3.5 CN1CCN(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00043a008
CHEMBL89970 205017 5 None 3 3 Human 8.7 pKi = 8.7 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 292 1 0 3 3.5 CN1CCN(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00043a008
9840365 107966 0 None 109 3 Human 8.7 pKi = 8.7 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 327 7 1 4 3.0 O[C@@H](COc1ccccc1)CN1CCC(Oc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
CHEMBL31991 107966 0 None 109 3 Human 8.7 pKi = 8.7 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 327 7 1 4 3.0 O[C@@H](COc1ccccc1)CN1CCC(Oc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
10404144 203591 19 None 1 10 Human 8.7 pKi = 8.7 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL7927 203591 19 None 1 10 Human 8.7 pKi = 8.7 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
792265 91722 8 None 29 3 Human 8.7 pKi = 8.7 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 346 5 0 3 4.6 CCOc1ccccc1N1CCN(Cc2cccc3ccccc23)CC1 10.1016/j.bmcl.2013.07.033
CHEMBL2420781 91722 8 None 29 3 Human 8.7 pKi = 8.7 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 346 5 0 3 4.6 CCOc1ccccc1N1CCN(Cc2cccc3ccccc23)CC1 10.1016/j.bmcl.2013.07.033
9860183 106745 0 None 89 2 Human 8.7 pKi = 8.7 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 232 0 0 3 3.3 Cc1sc(C)c2c1CCCc1cnn(C)c1-2 10.1016/s0960-894x(03)00587-0
CHEMBL316727 106745 0 None 89 2 Human 8.7 pKi = 8.7 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 232 0 0 3 3.3 Cc1sc(C)c2c1CCCc1cnn(C)c1-2 10.1016/s0960-894x(03)00587-0
10588194 18732 3 None 67 3 Human 8.7 pKi = 8.7 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 271 9 1 3 3.1 c1ccc(OCCCNCCOc2ccccc2)cc1 10.1021/jm970422s
CHEMBL128524 18732 3 None 67 3 Human 8.7 pKi = 8.7 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 271 9 1 3 3.1 c1ccc(OCCCNCCOc2ccccc2)cc1 10.1021/jm970422s
44336061 108134 0 None 56 2 Human 8.7 pKi = 8.7 Binding
Binding affinity towards Dopamine receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1016/s0960-894x(02)00656-x
CHEMBL320597 108134 0 None 56 2 Human 8.7 pKi = 8.7 Binding
Binding affinity towards Dopamine receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1016/s0960-894x(02)00656-x
44335889 106870 0 None 354 2 Human 8.7 pKi = 8.7 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 381 4 0 3 3.2 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1F 10.1016/s0960-894x(02)00656-x
CHEMBL317670 106870 0 None 354 2 Human 8.7 pKi = 8.7 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 381 4 0 3 3.2 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1F 10.1016/s0960-894x(02)00656-x
44336074 4825 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 393 5 0 4 4.2 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccc([N+](=O)[O-])cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104497 4825 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 393 5 0 4 4.2 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccc([N+](=O)[O-])cc2)CC1 10.1016/s0960-894x(02)00655-8
44335812 4869 0 None 19 2 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 362 4 0 2 4.6 Cc1ccc(CN2CCC(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
CHEMBL104716 4869 0 None 19 2 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 362 4 0 2 4.6 Cc1ccc(CN2CCC(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
137659990 158684 0 None -3 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccn2ncc(/C=N\O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4098859 158684 0 None -3 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccn2ncc(/C=N\O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
122180955 121256 0 None 1 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 386 7 1 3 4.6 CCCN(CCNC(=O)/N=N/c1ccc(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3589576 121256 0 None 1 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 386 7 1 3 4.6 CCCN(CCNC(=O)/N=N/c1ccc(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
11559581 78009 0 None 194 6 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 361 3 0 5 3.4 Clc1ccc(N2CCN(Cc3cn4nc(Cl)ccc4n3)CC2)cc1 10.1021/jm060166w
CHEMBL211135 78009 0 None 194 6 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 361 3 0 5 3.4 Clc1ccc(N2CCN(Cc3cn4nc(Cl)ccc4n3)CC2)cc1 10.1021/jm060166w
10476504 33268 1 None -1 7 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm900690y
CHEMBL142020 33268 1 None -1 7 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm900690y
11464857 4713 0 None - 1 Human 8.7 pKi = 8.7 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 439 6 0 4 4.8 COc1cc(Cl)ccc1OCC1CN(Cc2ccc(Br)cc2)CCCO1 10.1021/jm031111m
CHEMBL104035 4713 0 None - 1 Human 8.7 pKi = 8.7 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 439 6 0 4 4.8 COc1cc(Cl)ccc1OCC1CN(Cc2ccc(Br)cc2)CCCO1 10.1021/jm031111m
44376209 56039 0 None 33 2 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 360 4 0 5 2.7 Fc1ccc(OC[C@H]2CC[C@H]3CN(c4ncc(F)cn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL163009 56039 0 None 33 2 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 360 4 0 5 2.7 Fc1ccc(OC[C@H]2CC[C@H]3CN(c4ncc(F)cn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
44336061 108134 0 None 56 2 Human 8.7 pKi = 8.7 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1021/acs.jmedchem.7b00151
CHEMBL320597 108134 0 None 56 2 Human 8.7 pKi = 8.7 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1021/acs.jmedchem.7b00151
119570 3110 90 None -10 40 Human 8.7 pKi = 8.7 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
2233 3110 90 None -10 40 Human 8.7 pKi = 8.7 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
953 3110 90 None -10 40 Human 8.7 pKi = 8.7 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
CHEMBL301265 3110 90 None -10 40 Human 8.7 pKi = 8.7 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
DB00413 3110 90 None -10 40 Human 8.7 pKi = 8.7 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
10571927 205681 0 None - 1 Human 8.7 pKi = 8.7 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 381 4 1 4 5.1 Cc1c(-c2ccccc2)nc(O)n1C1CCN(Cc2ccccc2Cl)CC1 10.1021/jm991029k
CHEMBL93970 205681 0 None - 1 Human 8.7 pKi = 8.7 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 381 4 1 4 5.1 Cc1c(-c2ccccc2)nc(O)n1C1CCN(Cc2ccccc2Cl)CC1 10.1021/jm991029k
1353 1880 85 None -3 85 Human 8.7 pKi = 8.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9601720
3559 1880 85 None -3 85 Human 8.7 pKi = 8.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9601720
86 1880 85 None -3 85 Human 8.7 pKi = 8.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9601720
CHEMBL54 1880 85 None -3 85 Human 8.7 pKi = 8.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9601720
DB00502 1880 85 None -3 85 Human 8.7 pKi = 8.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9601720
9802631 111505 1 None 10 5 Human 8.7 pKi = 8.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 427 7 2 4 3.7 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
CHEMBL328866 111505 1 None 10 5 Human 8.7 pKi = 8.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 427 7 2 4 3.7 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
10716980 206102 0 None 2 3 Human 8.7 pKi = 8.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 419 6 2 4 3.8 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(C2CCCCC2)C1 10.1021/jm9601720
CHEMBL96369 206102 0 None 2 3 Human 8.7 pKi = 8.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 419 6 2 4 3.8 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(C2CCCCC2)C1 10.1021/jm9601720
18624462 166390 0 None 10 2 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human Dopamine receptor D4Binding affinity towards human Dopamine receptor D4
ChEMBL 427 7 2 4 3.7 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)C1 10.1021/jm030480f
CHEMBL428705 166390 0 None 10 2 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human Dopamine receptor D4Binding affinity towards human Dopamine receptor D4
ChEMBL 427 7 2 4 3.7 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)C1 10.1021/jm030480f
10831735 31540 0 None 2511 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(Cl)cc4)CC3)cc2c1 10.1021/jm0009989
CHEMBL140594 31540 0 None 2511 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(Cl)cc4)CC3)cc2c1 10.1021/jm0009989
137655636 158190 0 None 93 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 376 7 0 2 4.7 O=C1CCc2ccccc2N1CCCN1CCC(CCc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4093527 158190 0 None 93 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 376 7 0 2 4.7 O=C1CCc2ccccc2N1CCCN1CCC(CCc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
10336538 1595 44 None -3 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm0611152
974 1595 44 None -3 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm0611152
CHEMBL310843 1595 44 None -3 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm0611152
1353 1880 85 None -3 85 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970170v
3559 1880 85 None -3 85 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970170v
86 1880 85 None -3 85 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970170v
CHEMBL54 1880 85 None -3 85 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970170v
DB00502 1880 85 None -3 85 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970170v
10336538 1595 44 None -3 8 Human 8.7 pKi = 8.7 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm015522j
974 1595 44 None -3 8 Human 8.7 pKi = 8.7 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm015522j
CHEMBL310843 1595 44 None -3 8 Human 8.7 pKi = 8.7 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm015522j
10336538 1595 44 None -3 8 Human 8.7 pKi = 8.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm049612a
974 1595 44 None -3 8 Human 8.7 pKi = 8.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm049612a
CHEMBL310843 1595 44 None -3 8 Human 8.7 pKi = 8.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm049612a
10784211 103705 0 None 223 4 Rat 8.7 pKi = 8.7 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 352 5 0 4 3.5 COc1ccc(N2CCN(CC[C@@H]3OCCc4ccccc43)CC2)cc1 10.1021/jm960084f
CHEMBL309730 103705 0 None 223 4 Rat 8.7 pKi = 8.7 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 352 5 0 4 3.5 COc1ccc(N2CCN(CC[C@@H]3OCCc4ccccc43)CC2)cc1 10.1021/jm960084f
10336538 1595 44 None -3 8 Human 8.7 pKi = 8.7 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1016/j.bmcl.2007.12.026
974 1595 44 None -3 8 Human 8.7 pKi = 8.7 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1016/j.bmcl.2007.12.026
CHEMBL310843 1595 44 None -3 8 Human 8.7 pKi = 8.7 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1016/j.bmcl.2007.12.026
1353 1880 85 None -3 85 Human 8.7 pKi = 8.7 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970422s
3559 1880 85 None -3 85 Human 8.7 pKi = 8.7 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970422s
86 1880 85 None -3 85 Human 8.7 pKi = 8.7 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970422s
CHEMBL54 1880 85 None -3 85 Human 8.7 pKi = 8.7 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970422s
DB00502 1880 85 None -3 85 Human 8.7 pKi = 8.7 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970422s
778880 50076 11 None 26 3 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 339 6 1 4 2.2 COc1cccc(C(=O)NCCN2CCN(c3ccccc3)CC2)c1 10.1021/jm020952a
CHEMBL157222 50076 11 None 26 3 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 339 6 1 4 2.2 COc1cccc(C(=O)NCCN2CCN(c3ccccc3)CC2)c1 10.1021/jm020952a
1353 1880 85 None -3 85 Human 8.7 pKi = 8.7 Binding
Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00073a021
3559 1880 85 None -3 85 Human 8.7 pKi = 8.7 Binding
Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00073a021
86 1880 85 None -3 85 Human 8.7 pKi = 8.7 Binding
Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00073a021
CHEMBL54 1880 85 None -3 85 Human 8.7 pKi = 8.7 Binding
Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00073a021
DB00502 1880 85 None -3 85 Human 8.7 pKi = 8.7 Binding
Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00073a021
127032384 138846 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 356 5 1 3 4.1 Clc1ccc2c(CN3CCO[C@H](COc4ccccc4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3793137 138846 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 356 5 1 3 4.1 Clc1ccc2c(CN3CCO[C@H](COc4ccccc4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
137643309 157869 0 None -1 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccn2ncc(C=O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4090208 157869 0 None -1 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccn2ncc(C=O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
10336538 1595 44 None -3 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm900690y
974 1595 44 None -3 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm900690y
CHEMBL310843 1595 44 None -3 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm900690y
1353 1880 85 None -3 85 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0104825
3559 1880 85 None -3 85 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0104825
86 1880 85 None -3 85 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0104825
CHEMBL54 1880 85 None -3 85 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0104825
DB00502 1880 85 None -3 85 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0104825
45361874 169454 2 None 48 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 324 5 1 4 2.4 CCc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4442548 169454 2 None 48 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 324 5 1 4 2.4 CCc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
3303 2213 41 None 1 15 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.2c00840
5311200 2213 41 None 1 15 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.2c00840
CHEMBL267014 2213 41 None 1 15 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.2c00840
168285560 192316 0 None 1148 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 350 5 0 4 2.6 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccn2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5196873 192316 0 None 1148 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 350 5 0 4 2.6 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccn2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222201 192316 0 None 1148 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 350 5 0 4 2.6 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccn2)CC1 10.1021/acs.jmedchem.2c00840
3303 2213 41 None 1 15 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.8b00265
5311200 2213 41 None 1 15 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.8b00265
CHEMBL267014 2213 41 None 1 15 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.8b00265
10404144 203591 19 None 1 10 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm0611152
CHEMBL7927 203591 19 None 1 10 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm0611152
1353 1880 85 None -3 85 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970111h
3559 1880 85 None -3 85 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970111h
86 1880 85 None -3 85 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970111h
CHEMBL54 1880 85 None -3 85 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970111h
DB00502 1880 85 None -3 85 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970111h
9847013 45104 0 None 26 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 458 6 1 5 6.3 Cc1nc(Cl)c(Sc2ccc(Cl)cc2)c(NC2CCN(Cc3ccccc3)CC2)n1 10.1016/s0960-894x(01)00167-6
CHEMBL15270 45104 0 None 26 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 458 6 1 5 6.3 Cc1nc(Cl)c(Sc2ccc(Cl)cc2)c(NC2CCN(Cc3ccccc3)CC2)n1 10.1016/s0960-894x(01)00167-6
1353 1880 85 None -3 85 Human 8.6 pKi = 8.6 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9600712
3559 1880 85 None -3 85 Human 8.6 pKi = 8.6 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9600712
86 1880 85 None -3 85 Human 8.6 pKi = 8.6 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9600712
CHEMBL54 1880 85 None -3 85 Human 8.6 pKi = 8.6 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9600712
DB00502 1880 85 None -3 85 Human 8.6 pKi = 8.6 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9600712
11811808 45161 0 None -5 4 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 417 8 1 4 4.2 COc1cccc(C(=O)NCCCCN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/jm020952a
CHEMBL152756 45161 0 None -5 4 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 417 8 1 4 4.2 COc1cccc(C(=O)NCCCCN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/jm020952a
3645619 2985 13 None -4 9 Human 8.6 pKi = 8.6 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/acs.jmedchem.9b01085
975 2985 13 None -4 9 Human 8.6 pKi = 8.6 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/acs.jmedchem.9b01085
CHEMBL45244 2985 13 None -4 9 Human 8.6 pKi = 8.6 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/acs.jmedchem.9b01085
27620 140287 13 None 5 8 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 297 5 0 2 3.8 O=C(CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818994 140287 13 None 5 8 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 297 5 0 2 3.8 O=C(CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
46893146 61278 0 None -19 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 475 8 0 5 5.0 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4cccs4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771110 61278 0 None -19 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 475 8 0 5 5.0 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4cccs4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
137634397 155564 0 None -8 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 480 8 3 10 2.2 O=C1COc2c(N3CCN(CCCCOc4ccn5ncc(/C=N/O)c5c4)CC3)ccc(O)c2N1 10.1016/j.bmc.2017.08.037
CHEMBL4063145 155564 0 None -8 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 480 8 3 10 2.2 O=C1COc2c(N3CCN(CCCCOc4ccn5ncc(/C=N/O)c5c4)CC3)ccc(O)c2N1 10.1016/j.bmc.2017.08.037
1353 1880 85 None -3 85 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960072u
3559 1880 85 None -3 85 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960072u
86 1880 85 None -3 85 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960072u
CHEMBL54 1880 85 None -3 85 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960072u
DB00502 1880 85 None -3 85 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960072u
11633170 78003 0 None 63 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 421 5 0 7 2.8 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(N4CCOCC4)c3n2)CC1 10.1021/jm060166w
CHEMBL211118 78003 0 None 63 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 421 5 0 7 2.8 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(N4CCOCC4)c3n2)CC1 10.1021/jm060166w
45273045 194702 0 None 199 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cc3ccccn3n2)CC1 10.1021/jm900690y
CHEMBL562620 194702 0 None 199 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cc3ccccn3n2)CC1 10.1021/jm900690y
10361512 54154 0 None 1949 5 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 365 3 0 5 3.5 Cc1nn2c(C#N)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
CHEMBL160932 54154 0 None 1949 5 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 365 3 0 5 3.5 Cc1nn2c(C#N)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
10267394 99923 3 None 102 4 Rat 8.6 pKi = 8.6 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 310 3 1 3 3.0 Fc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
CHEMBL28997 99923 3 None 102 4 Rat 8.6 pKi = 8.6 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 310 3 1 3 3.0 Fc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
1353 1880 85 None -3 85 Human 8.6 pKi = 8.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b00151
3559 1880 85 None -3 85 Human 8.6 pKi = 8.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b00151
86 1880 85 None -3 85 Human 8.6 pKi = 8.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b00151
CHEMBL54 1880 85 None -3 85 Human 8.6 pKi = 8.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b00151
DB00502 1880 85 None -3 85 Human 8.6 pKi = 8.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b00151
10042972 106058 0 None 131 3 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 341 2 1 4 3.7 O=c1oc2cc(O)ccc2c2c1CN(Cc1ccc(Cl)cc1)CC2 10.1021/jm970170v
CHEMBL314095 106058 0 None 131 3 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 341 2 1 4 3.7 O=c1oc2cc(O)ccc2c2c1CN(Cc1ccc(Cl)cc1)CC2 10.1021/jm970170v
21533446 69812 0 None -6 10 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 379 6 1 3 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
CHEMBL1940403 69812 0 None -6 10 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 379 6 1 3 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
21527771 69813 0 None -1 10 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 363 6 1 3 4.2 OC1(c2ccc(Cl)cc2)CCN(CCCOc2ccc(F)cc2)CC1 10.1016/j.bmc.2011.12.019
CHEMBL1940404 69813 0 None -1 10 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 363 6 1 3 4.2 OC1(c2ccc(Cl)cc2)CCN(CCCOc2ccc(F)cc2)CC1 10.1016/j.bmc.2011.12.019
71463207 83660 0 None 7 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 357 4 0 4 4.0 COc1ccccc1N1CCN(Cc2cc(C#N)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207636 83660 0 None 7 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 357 4 0 4 4.0 COc1ccccc1N1CCN(Cc2cc(C#N)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
135524323 193755 0 None 61 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 382 5 2 6 1.6 COc1ccccc1N1CCN(Cc2cc3c(=O)[nH]c(N(C)C)nc3[nH]2)CC1 10.1016/j.bmc.2009.05.015
CHEMBL552268 193755 0 None 61 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 382 5 2 6 1.6 COc1ccccc1N1CCN(Cc2cc3c(=O)[nH]c(N(C)C)nc3[nH]2)CC1 10.1016/j.bmc.2009.05.015
9863333 202662 0 None -1 10 Human 8.6 pKi = 8.6 Binding
The compound was tested for CNS binding affinity towards Dopamine receptor D4 from cloned Human membranes.The compound was tested for CNS binding affinity towards Dopamine receptor D4 from cloned Human membranes.
ChEMBL 352 5 0 4 3.5 COc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/jm980137o
CHEMBL71724 202662 0 None -1 10 Human 8.6 pKi = 8.6 Binding
The compound was tested for CNS binding affinity towards Dopamine receptor D4 from cloned Human membranes.The compound was tested for CNS binding affinity towards Dopamine receptor D4 from cloned Human membranes.
ChEMBL 352 5 0 4 3.5 COc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/jm980137o
44340333 9571 0 None 19 4 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 384 5 1 3 3.8 C#Cc1cc(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)c(OC)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL112833 9571 0 None 19 4 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 384 5 1 3 3.8 C#Cc1cc(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)c(OC)c2ccccc12 10.1016/s0960-894x(03)00678-4
5029739 100359 1 None 190 2 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 380 5 0 3 5.7 Cc1c(-c2ccc(Cl)cc2)noc1C1CCN(CCc2ccccc2)CC1 10.1021/jm970111h
CHEMBL293341 100359 1 None 190 2 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 380 5 0 3 5.7 Cc1c(-c2ccc(Cl)cc2)noc1C1CCN(CCc2ccccc2)CC1 10.1021/jm970111h
13869641 112904 0 None -1 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 431 8 0 4 5.4 CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318824 112904 0 None -1 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 431 8 0 4 5.4 CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
9949442 95140 0 None 56 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 331 4 0 3 4.7 Cc1c(-c2ccccc2)cnn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00169-9
CHEMBL25772 95140 0 None 56 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 331 4 0 3 4.7 Cc1c(-c2ccccc2)cnn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00169-9
5029739 100359 1 None 190 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 380 5 0 3 5.7 Cc1c(-c2ccc(Cl)cc2)noc1C1CCN(CCc2ccccc2)CC1 10.1021/jm960072u
CHEMBL293341 100359 1 None 190 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 380 5 0 3 5.7 Cc1c(-c2ccc(Cl)cc2)noc1C1CCN(CCc2ccccc2)CC1 10.1021/jm960072u
71583848 87303 0 None 6 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 448 4 0 4 5.1 c1ccc(N2CCN(Cc3cnn(-c4cc5ccc4CCc4ccc(cc4)CC5)c3)CC2)cc1 10.1016/j.bmc.2013.01.065
CHEMBL2336892 87303 0 None 6 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 448 4 0 4 5.1 c1ccc(N2CCN(Cc3cnn(-c4cc5ccc4CCc4ccc(cc4)CC5)c3)CC2)cc1 10.1016/j.bmc.2013.01.065
133008 2211 16 None 204 2 Human 8.6 pKi = 8.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/acs.jmedchem.7b00151
3302 2211 16 None 204 2 Human 8.6 pKi = 8.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/acs.jmedchem.7b00151
CHEMBL444309 2211 16 None 204 2 Human 8.6 pKi = 8.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/acs.jmedchem.7b00151
44412468 165377 0 None 61 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 319 4 0 5 2.6 c1ccc(N2CCN(Cc3cnn(-c4ccccn4)c3)CC2)cc1 10.1021/jm0611152
CHEMBL425057 165377 0 None 61 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 319 4 0 5 2.6 c1ccc(N2CCN(Cc3cnn(-c4ccccn4)c3)CC2)cc1 10.1021/jm0611152
10640530 111797 0 None 190 3 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 335 3 0 4 3.7 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(C)cc1)CC3 10.1021/jm970170v
CHEMBL329126 111797 0 None 190 3 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 335 3 0 4 3.7 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(C)cc1)CC3 10.1021/jm970170v
44323962 205103 0 None 7 4 Human 8.6 pKi = 8.6 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 369 3 1 2 4.3 Brc1ccc(N2CCN(Cc3ccccc3)CC2)c2cc[nH]c12 10.1016/s0960-894x(98)00474-0
CHEMBL90476 205103 0 None 7 4 Human 8.6 pKi = 8.6 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 369 3 1 2 4.3 Brc1ccc(N2CCN(Cc3ccccc3)CC2)c2cc[nH]c12 10.1016/s0960-894x(98)00474-0
10807795 39033 0 None 239 3 Human 8.6 pKi = 8.6 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 350 3 1 3 4.0 Cc1ccc(C2CCN(Cc3ccc4c(c3)OCC(=O)N4)CC2)cc1C 10.1021/jm990277d
CHEMBL147059 39033 0 None 239 3 Human 8.6 pKi = 8.6 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 350 3 1 3 4.0 Cc1ccc(C2CCN(Cc3ccc4c(c3)OCC(=O)N4)CC2)cc1C 10.1021/jm990277d
10664621 43712 0 None 91 3 Human 8.6 pKi = 8.6 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 336 3 1 3 3.7 Cc1ccc(C2CCN(Cc3ccc4c(c3)OCC(=O)N4)CC2)cc1 10.1021/jm990277d
CHEMBL151286 43712 0 None 91 3 Human 8.6 pKi = 8.6 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 336 3 1 3 3.7 Cc1ccc(C2CCN(Cc3ccc4c(c3)OCC(=O)N4)CC2)cc1 10.1021/jm990277d
76320592 85459 0 None 9 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 365 3 1 0 3.5 Brc1ccc(-[n+]2cc[n+](Cc3ccccc3)cc2)c2cc[nH]c12 10.1007/s00044-012-0055-5
CHEMBL2298809 85459 0 None 9 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 365 3 1 0 3.5 Brc1ccc(-[n+]2cc[n+](Cc3ccccc3)cc2)c2cc[nH]c12 10.1007/s00044-012-0055-5
10404144 203591 19 None -1 10 Rat 8.6 pKi = 8.6 Binding
Binding affinity to dopamine D4 receptor in Wistar rat brain slicesBinding affinity to dopamine D4 receptor in Wistar rat brain slices
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm200762g
CHEMBL7927 203591 19 None -1 10 Rat 8.6 pKi = 8.6 Binding
Binding affinity to dopamine D4 receptor in Wistar rat brain slicesBinding affinity to dopamine D4 receptor in Wistar rat brain slices
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm200762g
155510756 168945 0 None 10 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 521 11 2 6 4.3 COc1ccc(N(Cc2ccccc2F)NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1021/acs.jmedchem.9b01085
CHEMBL4434714 168945 0 None 10 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 521 11 2 6 4.3 COc1ccc(N(Cc2ccccc2F)NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1021/acs.jmedchem.9b01085
155564308 174581 0 None 12 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 525 10 2 5 4.9 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2F)c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4570073 174581 0 None 12 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 525 10 2 5 4.9 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2F)c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.9b01085
44412468 165377 0 None 61 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 319 4 0 5 2.6 c1ccc(N2CCN(Cc3cnn(-c4ccccn4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL425057 165377 0 None 61 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 319 4 0 5 2.6 c1ccc(N2CCN(Cc3cnn(-c4ccccn4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
44371932 119143 0 None 467 4 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 354 4 0 5 3.1 O=Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
CHEMBL346805 119143 0 None 467 4 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 354 4 0 5 3.1 O=Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
168268770 192170 0 None 213 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 335 5 0 3 3.7 c1ccc(N2CCN(CCCN3CCCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5169993 192170 0 None 213 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 335 5 0 3 3.7 c1ccc(N2CCN(CCCN3CCCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5221238 192170 0 None 213 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 335 5 0 3 3.7 c1ccc(N2CCN(CCCN3CCCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
49788870 18074 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 341 5 1 3 2.7 Cc1ccc(N2CCN(CCNC(=O)c3ccc(F)cc3)CC2)cc1 10.1021/jm100925m
CHEMBL1270322 18074 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 341 5 1 3 2.7 Cc1ccc(N2CCN(CCNC(=O)c3ccc(F)cc3)CC2)cc1 10.1021/jm100925m
10589218 21010 0 None 23 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 285 9 1 3 3.4 Cc1ccc(OCCCNCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL131299 21010 0 None 23 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 285 9 1 3 3.4 Cc1ccc(OCCCNCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
44270558 164736 0 None 812 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 340 3 0 4 3.6 Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1021/jm0611152
CHEMBL423247 164736 0 None 812 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 340 3 0 4 3.6 Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1021/jm0611152
44339992 108697 0 None 22 4 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL321492 108697 0 None 22 4 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
10336538 1595 44 None -3 8 Human 8.6 pKi = 8.6 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm0305669
974 1595 44 None -3 8 Human 8.6 pKi = 8.6 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm0305669
CHEMBL310843 1595 44 None -3 8 Human 8.6 pKi = 8.6 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm0305669
10646459 205403 0 None -1 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 433 6 2 4 4.2 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(C2CCCCCC2)C1 10.1021/jm9601720
CHEMBL92199 205403 0 None -1 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 433 6 2 4 4.2 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(C2CCCCCC2)C1 10.1021/jm9601720
10589218 21010 0 None 23 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 285 9 1 3 3.4 Cc1ccc(OCCCNCCOc2ccccc2)cc1 10.1021/jm970422s
CHEMBL131299 21010 0 None 23 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 285 9 1 3 3.4 Cc1ccc(OCCCNCCOc2ccccc2)cc1 10.1021/jm970422s
44412269 77746 0 None 33 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 349 5 0 6 2.6 COc1ccccc1N1CCN(Cc2cn(-c3ccccc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL210232 77746 0 None 33 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 349 5 0 6 2.6 COc1ccccc1N1CCN(Cc2cn(-c3ccccc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
44412269 77746 0 None 33 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 349 5 0 6 2.6 COc1ccccc1N1CCN(Cc2cn(-c3ccccc3)nn2)CC1 10.1016/j.bmcl.2006.02.075
CHEMBL210232 77746 0 None 33 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 349 5 0 6 2.6 COc1ccccc1N1CCN(Cc2cn(-c3ccccc3)nn2)CC1 10.1016/j.bmcl.2006.02.075
11724450 123330 4 None - 1 Human 8.6 pKi = 8.6 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL184158 123330 4 None - 1 Human 8.6 pKi = 8.6 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL362542 123330 4 None - 1 Human 8.6 pKi = 8.6 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.bmcl.2004.07.068
44270558 164736 0 None 812 4 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 340 3 0 4 3.6 Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
CHEMBL423247 164736 0 None 812 4 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 340 3 0 4 3.6 Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
119570 3110 90 None -10 40 Human 8.6 pKi = 8.6 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
2233 3110 90 None -10 40 Human 8.6 pKi = 8.6 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
953 3110 90 None -10 40 Human 8.6 pKi = 8.6 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
CHEMBL301265 3110 90 None -10 40 Human 8.6 pKi = 8.6 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
DB00413 3110 90 None -10 40 Human 8.6 pKi = 8.6 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
6469693 79545 17 None 158 6 Human 8.6 pKi = 8.6 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cn3ccccc3n2)CC1 10.1016/j.ejmech.2019.111569
CHEMBL212631 79545 17 None 158 6 Human 8.6 pKi = 8.6 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cn3ccccc3n2)CC1 10.1016/j.ejmech.2019.111569
10854370 119101 0 None 18 2 Human 8.6 pKi = 8.6 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 336 3 1 3 3.7 Cc1ccc(C2CCN(Cc3ccc4c(c3)NC(=O)CO4)CC2)cc1 10.1021/jm990277d
CHEMBL346398 119101 0 None 18 2 Human 8.6 pKi = 8.6 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 336 3 1 3 3.7 Cc1ccc(C2CCN(Cc3ccc4c(c3)NC(=O)CO4)CC2)cc1 10.1021/jm990277d
54583897 61273 0 None -1 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 411 7 0 4 3.4 COc1ccccc1N1CCN(CCCCN2CCc3cc(F)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771106 61273 0 None -1 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 411 7 0 4 3.4 COc1ccccc1N1CCN(CCCCN2CCc3cc(F)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
6469693 79545 17 None 158 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cn3ccccc3n2)CC1 10.1021/jm060166w
CHEMBL212631 79545 17 None 158 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cn3ccccc3n2)CC1 10.1021/jm060166w
44241718 193594 0 None 70 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 393 4 1 7 1.6 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccccn4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
CHEMBL551199 193594 0 None 70 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 393 4 1 7 1.6 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccccn4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
10249308 4834 0 None - 1 Human 8.6 pKi = 8.6 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 381 6 0 4 4.3 COc1cc(Cl)ccc1OC[C@@H]1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL104550 4834 0 None - 1 Human 8.6 pKi = 8.6 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 381 6 0 4 4.3 COc1cc(Cl)ccc1OC[C@@H]1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
15512070 52961 0 None 426 2 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 342 4 0 5 2.6 Fc1ccc(OC[C@@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL159903 52961 0 None 426 2 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 342 4 0 5 2.6 Fc1ccc(OC[C@@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
44372338 53563 0 None 707 4 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 398 4 0 4 3.9 C[Si](C)(C)c1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
CHEMBL160454 53563 0 None 707 4 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 398 4 0 4 3.9 C[Si](C)(C)c1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
44278115 101049 0 None 181 3 Rat 8.6 pKi = 8.6 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 318 4 1 3 3.5 C=Cc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
CHEMBL29808 101049 0 None 181 3 Rat 8.6 pKi = 8.6 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 318 4 1 3 3.5 C=Cc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
137649896 156991 0 None 46 2 Human 8.6 pKi = 8.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 381 6 0 4 4.3 COc1ccc(Cl)cc1OC[C@@H]1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/acs.jmedchem.7b00151
CHEMBL4080034 156991 0 None 46 2 Human 8.6 pKi = 8.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 381 6 0 4 4.3 COc1ccc(Cl)cc1OC[C@@H]1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/acs.jmedchem.7b00151
137649896 156991 0 None 46 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 381 6 0 4 4.3 COc1ccc(Cl)cc1OC[C@@H]1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/acs.jmedchem.8b00265
CHEMBL4080034 156991 0 None 46 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 381 6 0 4 4.3 COc1ccc(Cl)cc1OC[C@@H]1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/acs.jmedchem.8b00265
14925759 157494 6 None 18 13 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL4085780 157494 6 None 18 13 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.2c00840
14925759 157494 6 None 18 13 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4085780 157494 6 None 18 13 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
44412494 77918 0 None 131 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 352 4 0 4 3.8 Clc1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1021/jm0611152
CHEMBL210955 77918 0 None 131 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 352 4 0 4 3.8 Clc1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1021/jm0611152
17475863 168219 3 None 41 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 336 4 0 4 3.3 Fc1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1021/jm0611152
CHEMBL437490 168219 3 None 41 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 336 4 0 4 3.3 Fc1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1021/jm0611152
44323763 204767 0 None -2 4 Human 8.5 pKi = 8.5 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 360 3 1 3 3.9 FC(F)(F)c1nc2c(N3CCN(Cc4ccccc4)CC3)cccc2[nH]1 10.1016/s0960-894x(98)00474-0
CHEMBL88289 204767 0 None -2 4 Human 8.5 pKi = 8.5 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 360 3 1 3 3.9 FC(F)(F)c1nc2c(N3CCN(Cc4ccccc4)CC3)cccc2[nH]1 10.1016/s0960-894x(98)00474-0
76309673 85462 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 356 3 1 1 3.2 FC(F)(F)c1nc2c(-[n+]3cc[n+](Cc4ccccc4)cc3)cccc2[nH]1 10.1007/s00044-012-0055-5
CHEMBL2298812 85462 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 356 3 1 1 3.2 FC(F)(F)c1nc2c(-[n+]3cc[n+](Cc4ccccc4)cc3)cccc2[nH]1 10.1007/s00044-012-0055-5
60785 204177 42 None -23 7 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 425 5 0 4 3.7 O=S1(=O)c2cccc3cccc(c23)N1CCCN1CCN(c2ccc(F)cc2)CC1 10.1021/jm0002432
CHEMBL83894 204177 42 None -23 7 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 425 5 0 4 3.7 O=S1(=O)c2cccc3cccc(c23)N1CCCN1CCN(c2ccc(F)cc2)CC1 10.1021/jm0002432
155534246 171365 0 None 9 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 507 10 2 5 4.8 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4470231 171365 0 None 9 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 507 10 2 5 4.8 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.9b01085
155566058 175127 0 None 45 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 521 11 2 6 4.3 COc1ccc(N(Cc2ccc(F)cc2)NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1021/acs.jmedchem.9b01085
CHEMBL4582096 175127 0 None 45 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 521 11 2 6 4.3 COc1ccc(N(Cc2ccc(F)cc2)NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1021/acs.jmedchem.9b01085
54581964 61279 0 None -10 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 489 8 0 5 5.4 COc1ccccc1N1CCN(CCCCN2CCCc3cc(-c4cccs4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771111 61279 0 None -10 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 489 8 0 5 5.4 COc1ccccc1N1CCN(CCCCN2CCCc3cc(-c4cccs4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
60785 204177 42 None -23 7 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 425 5 0 4 3.7 O=S1(=O)c2cccc3cccc(c23)N1CCCN1CCN(c2ccc(F)cc2)CC1 10.1016/j.bmcl.2005.08.051
CHEMBL83894 204177 42 None -23 7 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 425 5 0 4 3.7 O=S1(=O)c2cccc3cccc(c23)N1CCCN1CCN(c2ccc(F)cc2)CC1 10.1016/j.bmcl.2005.08.051
44412494 77918 0 None 131 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 352 4 0 4 3.8 Clc1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL210955 77918 0 None 131 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 352 4 0 4 3.8 Clc1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
17475863 168219 3 None 41 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 336 4 0 4 3.3 Fc1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL437490 168219 3 None 41 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 336 4 0 4 3.3 Fc1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
11372852 5059 0 None - 1 Human 8.5 pKi = 8.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 395 7 0 4 4.7 CCOc1ccc(Cl)cc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL105696 5059 0 None - 1 Human 8.5 pKi = 8.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 395 7 0 4 4.7 CCOc1ccc(Cl)cc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
49788942 18105 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 362 5 1 4 2.4 O=C(NCCN1CCN(c2ccc(Cl)cn2)CC1)c1ccc(F)cc1 10.1021/jm100925m
CHEMBL1270516 18105 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 362 5 1 4 2.4 O=C(NCCN1CCN(c2ccc(Cl)cn2)CC1)c1ccc(F)cc1 10.1021/jm100925m
10691523 105131 0 None 34 3 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 385 4 1 2 5.8 Clc1ccc(-c2cc(C3CCN(Cc4ccccc4Cl)CC3)[nH]n2)cc1 10.1021/jm970111h
CHEMBL312255 105131 0 None 34 3 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 385 4 1 2 5.8 Clc1ccc(-c2cc(C3CCN(Cc4ccccc4Cl)CC3)[nH]n2)cc1 10.1021/jm970111h
10837493 205375 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 455 7 2 4 4.5 COc1cc(NC(=O)C2CCCC2)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
CHEMBL92030 205375 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 455 7 2 4 4.5 COc1cc(NC(=O)C2CCCC2)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
155547128 173089 0 None 3 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 399 7 1 5 3.8 COc1ccccc1N1CCN(CCCNC(=O)/N=N/c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4534703 173089 0 None 3 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 399 7 1 5 3.8 COc1ccccc1N1CCN(CCCNC(=O)/N=N/c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
90644062 111542 0 None 8 5 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 345 6 0 4 3.8 Cc1ccc(N2CCN(CCCSc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289647 111542 0 None 8 5 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 345 6 0 4 3.8 Cc1ccc(N2CCN(CCCSc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
49782600 17271 0 None -4 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 369 6 1 3 4.4 Cc1ccc(C)c(C2(O)CCN(CCCC(=O)c3ccc(F)cc3)CC2)c1 10.1021/jm100899z
CHEMBL1257689 17271 0 None -4 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 369 6 1 3 4.4 Cc1ccc(C)c(C2(O)CCN(CCCC(=O)c3ccc(F)cc3)CC2)c1 10.1021/jm100899z
10548329 200941 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 388 6 1 3 4.5 COc1cc2ccccc2cc1C(=O)NCC1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2006.12.096
CHEMBL61248 200941 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 388 6 1 3 4.5 COc1cc2ccccc2cc1C(=O)NCC1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2006.12.096
72544566 92699 0 None 5 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 375 10 0 6 3.1 COc1ccccc1N1CCN(Cc2cn(CCCCCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443009 92699 0 None 5 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 375 10 0 6 3.1 COc1ccccc1N1CCN(Cc2cn(CCCCCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
25333445 77769 5 None 104 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 318 4 0 4 3.2 c1ccc(N2CCN(Cc3ccc(-n4cccn4)cc3)CC2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL210318 77769 5 None 104 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 318 4 0 4 3.2 c1ccc(N2CCN(Cc3ccc(-n4cccn4)cc3)CC2)cc1 10.1016/j.bmcl.2006.02.075
122191605 123203 0 None 2 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells
ChEMBL 426 7 2 3 4.2 Brc1ccc(NCCN2CCN(CCc3c[nH]c4ccccc34)CC2)cc1 10.1021/acsmedchemlett.5b00131
CHEMBL3622097 123203 0 None 2 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells
ChEMBL 426 7 2 3 4.2 Brc1ccc(NCCN2CCN(CCc3c[nH]c4ccccc34)CC2)cc1 10.1021/acsmedchemlett.5b00131
44376230 119482 0 None 87 2 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 380 4 0 5 3.8 CC(C)(C)c1ccc(OC[C@@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL349904 119482 0 None 87 2 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 380 4 0 5 3.8 CC(C)(C)c1ccc(OC[C@@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
44372296 118982 0 None 72 4 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 356 4 1 5 2.8 OCc1ccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn2c1 10.1016/s0960-894x(01)00814-9
CHEMBL345357 118982 0 None 72 4 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 356 4 1 5 2.8 OCc1ccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn2c1 10.1016/s0960-894x(01)00814-9
71450812 78013 0 None 4 4 Human 7.7 pKi = 7.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 455 8 1 5 4.7 COc1ccc(Br)cc1-c1nc(CNCC2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL2111525 78013 0 None 4 4 Human 7.7 pKi = 7.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 455 8 1 5 4.7 COc1ccc(Br)cc1-c1nc(CNCC2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
11849776 79362 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 349 6 0 6 2.5 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(C#N)c1 10.1021/jm060279f
CHEMBL211836 79362 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 349 6 0 6 2.5 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(C#N)c1 10.1021/jm060279f
667675 203422 3 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 322 4 1 4 2.9 COc1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)cc1 10.1021/jm0305669
CHEMBL77969 203422 3 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 322 4 1 4 2.9 COc1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)cc1 10.1021/jm0305669
9820085 140799 0 None - 1 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 356 4 1 5 2.8 Cc1nc(N2CCN(CCC3NC(=O)c4ccccc43)CC2)sc1C 10.1016/s0960-894x(98)00252-2
CHEMBL38349 140799 0 None - 1 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 356 4 1 5 2.8 Cc1nc(N2CCN(CCC3NC(=O)c4ccccc43)CC2)sc1C 10.1016/s0960-894x(98)00252-2
44340186 9569 0 None 8 4 Human 6.7 pKi = 6.7 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCCN(Cc2ccccc2)C1 10.1016/s0960-894x(03)00678-4
CHEMBL112831 9569 0 None 8 4 Human 6.7 pKi = 6.7 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCCN(Cc2ccccc2)C1 10.1016/s0960-894x(03)00678-4
44380770 165159 0 None -6 4 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@@H]1CN(Cc2ccccc2)C[C@@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
CHEMBL424575 165159 0 None -6 4 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@@H]1CN(Cc2ccccc2)C[C@@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
3156990 8046 19 None 7 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 268 4 0 3 3.1 O=Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
CHEMBL109173 8046 19 None 7 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 268 4 0 3 3.1 O=Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
76441180 115237 0 None -95 4 Human 6.7 pKi = 6.7 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 437 9 0 7 4.1 COc1ccccc1N1CCN(CCCCc2cn(-c3ccc(SC)cc3)nn2)CC1 10.1016/j.bmcl.2014.12.023
CHEMBL3353913 115237 0 None -95 4 Human 6.7 pKi = 6.7 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 437 9 0 7 4.1 COc1ccccc1N1CCN(CCCCc2cn(-c3ccc(SC)cc3)nn2)CC1 10.1016/j.bmcl.2014.12.023
11658914 69897 0 None -30 3 Human 6.7 pKi = 6.7 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 255 5 0 3 3.0 CCCN(CCC)C1CCn2ncc(Cl)c2C1 10.1021/jm0503805
CHEMBL194099 69897 0 None -30 3 Human 6.7 pKi = 6.7 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 255 5 0 3 3.0 CCCN(CCC)C1CCn2ncc(Cl)c2C1 10.1021/jm0503805
11405182 108047 0 None - 1 Human 6.7 pKi = 6.7 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 343 5 0 3 4.3 COc1ccccc1/C=C/C1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL320071 108047 0 None - 1 Human 6.7 pKi = 6.7 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 343 5 0 3 4.3 COc1ccccc1/C=C/C1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
56597938 3877 1 None -204 9 Human 6.7 pKi = 6.7 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
7651 3877 1 None -204 9 Human 6.7 pKi = 6.7 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
CHEMBL2165126 3877 1 None -204 9 Human 6.7 pKi = 6.7 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
168275381 189676 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 403 5 0 4 4.8 Cn1ncc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
CHEMBL5175548 189676 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 403 5 0 4 4.8 Cn1ncc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
44415672 79764 0 None -1659 6 Human 5.7 pKi = 5.7 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 531 2 1 5 5.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3c(F)cccc3C(F)(F)F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL213492 79764 0 None -1659 6 Human 5.7 pKi = 5.7 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 531 2 1 5 5.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3c(F)cccc3C(F)(F)F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
42605994 17692 0 None 8 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptorDisplacement of [3H]Spiperone from human dopamine D4.4 receptor
ChEMBL 425 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc(Br)cs3)CC2)nc1 10.1021/jm100835q
CHEMBL1259071 17692 0 None 8 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptorDisplacement of [3H]Spiperone from human dopamine D4.4 receptor
ChEMBL 425 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc(Br)cs3)CC2)nc1 10.1021/jm100835q
9865384 172923 27 None -2344 7 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptorDisplacement of [3H]Spiperone from human dopamine D4.4 receptor
ChEMBL 393 5 1 3 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1 10.1021/jm100835q
CHEMBL45305 172923 27 None -2344 7 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptorDisplacement of [3H]Spiperone from human dopamine D4.4 receptor
ChEMBL 393 5 1 3 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1 10.1021/jm100835q
56658008 66087 0 None -52 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 421 9 1 5 3.9 COc1ccccc1N1CCN(CCCCCOc2ccc3ccc(=O)[nH]c3c2)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1813599 66087 0 None -52 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 421 9 1 5 3.9 COc1ccccc1N1CCN(CCCCCOc2ccc3ccc(=O)[nH]c3c2)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1851895 66087 0 None -52 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 421 9 1 5 3.9 COc1ccccc1N1CCN(CCCCCOc2ccc3ccc(=O)[nH]c3c2)CC1 10.1016/j.bmc.2011.04.021
10572229 120504 0 None -5 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 386 4 1 4 3.4 O=C1NCN(c2ccccc2)C12CCN(Cc1ccn(-c3ccccc3)c1)CC2 10.1021/jm00025a013
CHEMBL356542 120504 0 None -5 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 386 4 1 4 3.4 O=C1NCN(c2ccccc2)C12CCN(Cc1ccn(-c3ccccc3)c1)CC2 10.1021/jm00025a013
154725766 176071 1 None -1659 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4527244 176071 1 None -1659 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4598000 176071 1 None -1659 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL5094044 213689 2 None -30 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CN(C)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
10737150 107050 0 None 2 3 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 358 7 0 3 4.5 COc1cccc(CCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
CHEMBL318747 107050 0 None 2 3 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 358 7 0 3 4.5 COc1cccc(CCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
127051844 140316 0 None -16 9 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 322 6 1 3 2.8 NC(=O)c1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819427 140316 0 None -16 9 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 322 6 1 3 2.8 NC(=O)c1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
42626172 55951 0 None -1949 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 490 8 3 5 3.8 COc1ccc2[nH]c(C(=O)NCCC(O)CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2c1 10.1021/jm501512b
CHEMBL1627314 55951 0 None -1949 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 490 8 3 5 3.8 COc1ccc2[nH]c(C(=O)NCCC(O)CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2c1 10.1021/jm501512b
162659314 183114 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccncc3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4762416 183114 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccncc3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4803145 183114 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccncc3)CC2)cc1 10.1016/j.bmc.2020.115943
127051844 140316 0 None -16 9 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 322 6 1 3 2.8 NC(=O)c1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819427 140316 0 None -16 9 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 322 6 1 3 2.8 NC(=O)c1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
168294958 191806 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 347 6 0 3 4.2 COc1ccc(CN2CCC[C@H](OCc3cccc(F)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5207898 191806 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 347 6 0 3 4.2 COc1ccc(CN2CCC[C@H](OCc3cccc(F)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
11771801 79619 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 328 5 0 5 2.4 CO/N=C(\CN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL212891 79619 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 328 5 0 5 2.4 CO/N=C(\CN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
162659314 183114 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccncc3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4762416 183114 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccncc3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4803145 183114 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccncc3)CC2)cc1 10.1016/j.bmc.2020.115943
22953120 107983 0 None -1 2 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 4 0 3 4.0 C[C@H]1c2ccccc2N(C(=O)CN2CCN(Cc3ccc(Cl)cc3)CC2)[C@@H]1C 10.1016/s0960-894x(02)00655-8
CHEMBL319927 107983 0 None -1 2 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 4 0 3 4.0 C[C@H]1c2ccccc2N(C(=O)CN2CCN(Cc3ccc(Cl)cc3)CC2)[C@@H]1C 10.1016/s0960-894x(02)00655-8
1212 1632 45 None -77 65 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 1632 45 None -77 65 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 1632 45 None -77 65 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 1632 45 None -77 65 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 1632 45 None -77 65 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
168285068 190987 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3ncc4ccccn34)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5195130 190987 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3ncc4ccccn34)CC2)c1 10.1016/j.bmcl.2022.128615
154705038 176072 1 None -63 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.2 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4584481 176072 1 None -63 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.2 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4598001 176072 1 None -63 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.2 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
127051845 140198 0 None -12 9 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 309 6 0 3 3.7 COc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3817898 140198 0 None -12 9 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 309 6 0 3 3.7 COc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
10551026 101146 0 None -6 6 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 438 5 1 3 4.6 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL298875 101146 0 None -6 6 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 438 5 1 3 4.6 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
44301054 194474 0 None 21 6 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 266 3 1 3 2.2 N#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1 10.1016/s0960-894x(02)00316-5
CHEMBL56118 194474 0 None 21 6 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 266 3 1 3 2.2 N#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1 10.1016/s0960-894x(02)00316-5
135398737 944 89 None -13 91 Human 7.7 pKi = 7.7 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00004a016
38 944 89 None -13 91 Human 7.7 pKi = 7.7 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00004a016
722 944 89 None -13 91 Human 7.7 pKi = 7.7 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00004a016
CHEMBL42 944 89 None -13 91 Human 7.7 pKi = 7.7 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00004a016
DB00363 944 89 None -13 91 Human 7.7 pKi = 7.7 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00004a016
135398737 944 89 None -13 91 Human 7.7 pKi = 7.7 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00043a008
38 944 89 None -13 91 Human 7.7 pKi = 7.7 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00043a008
722 944 89 None -13 91 Human 7.7 pKi = 7.7 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00043a008
CHEMBL42 944 89 None -13 91 Human 7.7 pKi = 7.7 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00043a008
DB00363 944 89 None -13 91 Human 7.7 pKi = 7.7 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00043a008
135418440 11963 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 351 5 1 6 2.3 c1ccc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL1183663 11963 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 351 5 1 6 2.3 c1ccc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL310311 11963 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 351 5 1 6 2.3 c1ccc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
3802 201334 16 None 1 5 Rat 7.7 pKi = 7.7 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 307 0 1 5 2.8 Cc1ccc2c(c1)C(N1CCN(C)CC1)=Nc1cccnc1N2 10.1021/jm960084f
CHEMBL63329 201334 16 None 1 5 Rat 7.7 pKi = 7.7 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 307 0 1 5 2.8 Cc1ccc2c(c1)C(N1CCN(C)CC1)=Nc1cccnc1N2 10.1021/jm960084f
21830793 91403 5 None -138 46 Human 7.7 pKi = 7.7 Binding
Binding affinity to dopamine 4 receptor (unknown origin)Binding affinity to dopamine 4 receptor (unknown origin)
ChEMBL 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 10.1016/j.bmc.2013.05.050
CHEMBL2413154 91403 5 None -138 46 Human 7.7 pKi = 7.7 Binding
Binding affinity to dopamine 4 receptor (unknown origin)Binding affinity to dopamine 4 receptor (unknown origin)
ChEMBL 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 10.1016/j.bmc.2013.05.050
9930934 108150 0 None 52 2 Human 7.7 pKi = 7.7 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 401 5 0 3 3.4 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1c2ccccc2C[C@H]1CF 10.1016/s0960-894x(02)00656-x
CHEMBL320721 108150 0 None 52 2 Human 7.7 pKi = 7.7 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 401 5 0 3 3.4 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1c2ccccc2C[C@H]1CF 10.1016/s0960-894x(02)00656-x
44336109 110461 0 None 24 2 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 400 4 0 2 5.1 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccc(F)cc2Cl)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL326202 110461 0 None 24 2 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 400 4 0 2 5.1 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccc(F)cc2Cl)CC1 10.1016/s0960-894x(02)00655-8
2435 3533 78 None -10 48 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm030480f
60149 3533 78 None -10 48 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm030480f
98 3533 78 None -10 48 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm030480f
CHEMBL12713 3533 78 None -10 48 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm030480f
DB06144 3533 78 None -10 48 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm030480f
9905246 16162 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 322 6 2 4 3.6 Cc1ccc(NCCNCc2ccc3ccc(=O)oc3c2)cc1C 10.1021/jm990266k
CHEMBL122862 16162 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 322 6 2 4 3.6 Cc1ccc(NCCNCc2ccc3ccc(=O)oc3c2)cc1C 10.1021/jm990266k
155563950 174701 0 None 32 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 569 9 2 4 4.7 O=C(NCCCN1CCN(c2ccc(I)cc2)CC1)NN(Cc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
CHEMBL4572646 174701 0 None 32 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 569 9 2 4 4.7 O=C(NCCCN1CCN(c2ccc(I)cc2)CC1)NN(Cc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
127028181 138919 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 359 5 1 4 3.1 Fc1ccc2c(CN3CCO[C@H](COc4cccc(F)n4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3794013 138919 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 359 5 1 4 3.1 Fc1ccc2c(CN3CCO[C@H](COc4cccc(F)n4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
57391216 69825 0 None 1 8 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 332 6 0 5 2.9 Fc1ccc(SCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940416 69825 0 None 1 8 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 332 6 0 5 2.9 Fc1ccc(SCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
57391216 69825 0 None 1 8 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 332 6 0 5 2.9 Fc1ccc(SCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940416 69825 0 None 1 8 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 332 6 0 5 2.9 Fc1ccc(SCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
44431490 87844 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.5 Cc1ccc(CN2CCC(NC(=O)c3ccc4ccccc4c3)CC2)cc1 10.1016/j.bmcl.2006.12.106
CHEMBL234826 87844 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.5 Cc1ccc(CN2CCC(NC(=O)c3ccc4ccccc4c3)CC2)cc1 10.1016/j.bmcl.2006.12.106
44405490 132929 0 None 35 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 430 5 1 3 5.4 O=C(N[C@H]1CCN(Cc2ccc(C(F)(F)F)cc2)C1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2005.08.051
CHEMBL370652 132929 0 None 35 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 430 5 1 3 5.4 O=C(N[C@H]1CCN(Cc2ccc(C(F)(F)F)cc2)C1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2005.08.051
137659303 158757 0 None -3 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 410 9 1 7 2.8 COc1ccccc1N1CCN(CCCCOc2ccn3nc(CO)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4099711 158757 0 None -3 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 410 9 1 7 2.8 COc1ccccc1N1CCN(CCCCOc2ccn3nc(CO)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
22100932 202396 0 None 31 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 374 3 0 3 5.9 Clc1ccc(CN2CC=C(c3nc4cc(Cl)ccc4s3)CC2)cc1 10.1016/S0960-894X(97)00402-2
CHEMBL70215 202396 0 None 31 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 374 3 0 3 5.9 Clc1ccc(CN2CC=C(c3nc4cc(Cl)ccc4s3)CC2)cc1 10.1016/S0960-894X(97)00402-2
45273442 194777 0 None 61 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 403 3 0 5 4.3 Cc1cc2nc(C)c(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
CHEMBL563078 194777 0 None 61 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 403 3 0 5 4.3 Cc1cc2nc(C)c(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
44276075 13114 0 None -4 3 Human 7.7 pKi = 7.7 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 397 8 0 6 4.6 COc1ccccc1N1CCN(CCCCc2cc(-c3cccs3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL1191252 13114 0 None -4 3 Human 7.7 pKi = 7.7 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 397 8 0 6 4.6 COc1ccccc1N1CCN(CCCCc2cc(-c3cccs3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL542325 13114 0 None -4 3 Human 7.7 pKi = 7.7 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 397 8 0 6 4.6 COc1ccccc1N1CCN(CCCCc2cc(-c3cccs3)no2)CC1 10.1016/s0960-894x(02)00179-8
10715225 205389 0 None 1 2 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 386 8 0 4 4.5 COc1cccc(C(=O)CCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
CHEMBL92121 205389 0 None 1 2 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 386 8 0 4 4.5 COc1cccc(C(=O)CCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
44400594 133052 0 None -1 5 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
CHEMBL371165 133052 0 None -1 5 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
11948707 165614 0 None -53 13 Human 7.7 pKi = 7.7 Binding
Binding affinity to D4 receptor (unknown origin) assessed as inhibition constantBinding affinity to D4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 373 7 0 8 0.6 COc1cccc(N2CCN(CCCCn3ncc(=O)n(C)c3=O)CC2)c1 10.1021/acs.jmedchem.2c00633
CHEMBL426317 165614 0 None -53 13 Human 7.7 pKi = 7.7 Binding
Binding affinity to D4 receptor (unknown origin) assessed as inhibition constantBinding affinity to D4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 373 7 0 8 0.6 COc1cccc(N2CCN(CCCCn3ncc(=O)n(C)c3=O)CC2)c1 10.1021/acs.jmedchem.2c00633
10616050 186064 3 None 81 3 Human 7.7 pKi = 7.7 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 325 5 1 4 2.2 COc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL48807 186064 3 None 81 3 Human 7.7 pKi = 7.7 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 325 5 1 4 2.2 COc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1016/j.bmcl.2005.02.012
57326583 73715 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 404 2 0 5 4.7 Clc1ccc2c(c1)N=C(N1CCN(Cc3ccccc3)CC1)c1cccnc1O2 10.1021/jm2013419
CHEMBL2022271 73715 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 404 2 0 5 4.7 Clc1ccc2c(c1)N=C(N1CCN(Cc3ccccc3)CC1)c1cccnc1O2 10.1021/jm2013419
127051845 140198 0 None -12 9 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 309 6 0 3 3.7 COc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3817898 140198 0 None -12 9 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 309 6 0 3 3.7 COc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
44426512 85318 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 5 1 2 4.3 O=C(c1ccc2ccccc2c1)N1CCC(NCCc2ccccc2)CC1 10.1016/j.bmcl.2006.12.096
CHEMBL229076 85318 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 5 1 2 4.3 O=C(c1ccc2ccccc2c1)N1CCC(NCCc2ccccc2)CC1 10.1016/j.bmcl.2006.12.096
14665503 90803 0 None -346 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 382 7 1 4 2.8 C=CCN1CCC[C@H]1CNC(=O)c1cc(Br)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
CHEMBL240106 90803 0 None -346 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 382 7 1 4 2.8 C=CCN1CCC[C@H]1CNC(=O)c1cc(Br)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
9977478 203235 2 None -3235 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 386 6 2 5 2.4 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Br)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
CHEMBL76402 203235 2 None -3235 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 386 6 2 5 2.4 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Br)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
137632607 155798 0 None -56 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 305 3 2 5 1.6 CCCN1CCCN(c2ccc(O)c3c2OCC(=O)N3)CC1 10.1016/j.bmc.2017.08.037
CHEMBL4065797 155798 0 None -56 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 305 3 2 5 1.6 CCCN1CCCN(c2ccc(O)c3c2OCC(=O)N3)CC1 10.1016/j.bmc.2017.08.037
1577 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
164512405 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
2537 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
5355 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
5501 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
643497 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
688272 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
958 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
960 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
CHEMBL196677 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
CHEMBL26 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
CHEMBL267044 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
DB00391 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
DB16021 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
51354851 59858 0 None -501 3 Human 5.7 pKi = 5.7 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 517 17 1 7 3.4 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(OCCOCCOCCF)cc2)CC1 10.1021/jm101323b
CHEMBL1688994 59858 0 None -501 3 Human 5.7 pKi = 5.7 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 517 17 1 7 3.4 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(OCCOCCOCCF)cc2)CC1 10.1021/jm101323b
CHEMBL1739761 59858 0 None -501 3 Human 5.7 pKi = 5.7 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 517 17 1 7 3.4 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(OCCOCCOCCF)cc2)CC1 10.1021/jm101323b
44578445 180997 0 None -13 3 Human 5.7 pKi = 5.7 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 352 6 0 3 4.1 O=C(CCCN1CC2CCC(C1)N2c1ccccc1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL476933 180997 0 None -13 3 Human 5.7 pKi = 5.7 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 352 6 0 3 4.1 O=C(CCCN1CC2CCC(C1)N2c1ccccc1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
1577 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
164512405 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
2537 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
5355 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
5501 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
643497 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
688272 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
958 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
960 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
CHEMBL196677 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
CHEMBL26 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
CHEMBL267044 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
DB00391 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
DB16021 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
137633454 156050 0 None -645 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 645 16 3 10 4.4 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN3CCCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2OC)nn1 10.1021/acs.jmedchem.7b00363
CHEMBL4068702 156050 0 None -645 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 645 16 3 10 4.4 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN3CCCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2OC)nn1 10.1021/acs.jmedchem.7b00363
1577 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
164512405 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
2537 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
5355 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
5501 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
643497 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
688272 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
958 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
960 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
CHEMBL196677 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
CHEMBL26 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
CHEMBL267044 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
DB00391 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
DB16021 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
168289523 190903 0 None 5 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 422 5 1 2 6.0 FC(F)(F)c1cccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5193761 190903 0 None 5 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 422 5 1 2 6.0 FC(F)(F)c1cccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)c1 10.1016/j.bmcl.2022.128615
10692886 53372 2 None -776 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 409 8 1 5 3.6 COc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1016/j.bmc.2011.04.021
CHEMBL160296 53372 2 None -776 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 409 8 1 5 3.6 COc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1813590 53372 2 None -776 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 409 8 1 5 3.6 COc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1016/j.bmc.2011.04.021
4797946 169856 8 None 165 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 310 4 1 4 2.2 Cc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4448320 169856 8 None 165 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 310 4 1 4 2.2 Cc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
2247 502 77 None -63 41 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 502 77 None -63 41 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 502 77 None -63 41 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 502 77 None -63 41 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 502 77 None -63 41 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
763774 91717 4 None 16 2 Human 6.7 pKi = 6.7 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 292 3 0 3 3.7 Clc1ccc(N2CCN(Cc3cccs3)CC2)cc1 10.1016/j.bmcl.2013.07.033
CHEMBL2420776 91717 4 None 16 2 Human 6.7 pKi = 6.7 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 292 3 0 3 3.7 Clc1ccc(N2CCN(Cc3cccs3)CC2)cc1 10.1016/j.bmcl.2013.07.033
42626313 55954 0 None -338 2 Human 5.7 pKi = 5.7 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 423 8 2 6 2.7 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm900095y
CHEMBL1627317 55954 0 None -338 2 Human 5.7 pKi = 5.7 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 423 8 2 6 2.7 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm900095y
10161526 13192 0 None -40 3 Human 5.7 pKi = 5.7 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 457 9 0 5 6.1 c1ccc(C(c2ccccc2)N2CCN(CCCCc3cc(-c4cccs4)no3)CC2)cc1 10.1016/s0960-894x(02)00179-8
CHEMBL1191882 13192 0 None -40 3 Human 5.7 pKi = 5.7 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 457 9 0 5 6.1 c1ccc(C(c2ccccc2)N2CCN(CCCCc3cc(-c4cccs4)no3)CC2)cc1 10.1016/s0960-894x(02)00179-8
CHEMBL543040 13192 0 None -40 3 Human 5.7 pKi = 5.7 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 457 9 0 5 6.1 c1ccc(C(c2ccccc2)N2CCN(CCCCc3cc(-c4cccs4)no3)CC2)cc1 10.1016/s0960-894x(02)00179-8
44438232 148249 3 None -4 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 341 3 2 3 3.7 OC1(c2ccc(Cl)cc2)CCN(Cc2n[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL394066 148249 3 None -4 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 341 3 2 3 3.7 OC1(c2ccc(Cl)cc2)CCN(Cc2n[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
154705296 175820 1 None -5 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 6.9 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4444691 175820 1 None -5 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 6.9 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4595970 175820 1 None -5 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 6.9 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
168275717 189625 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3ncc4ccccn34)CC2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5174731 189625 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3ncc4ccccn34)CC2)cc1F 10.1016/j.bmcl.2022.128615
11133385 101716 0 None -25 5 Human 5.7 pKi = 5.7 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 411 6 1 3 4.1 O=C(NCCCN1CCN(c2ccccc2)CC1)C1c2ccccc2-c2ccccc21 10.1021/jm010146o
CHEMBL302796 101716 0 None -25 5 Human 5.7 pKi = 5.7 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 411 6 1 3 4.1 O=C(NCCCN1CCN(c2ccccc2)CC1)C1c2ccccc2-c2ccccc21 10.1021/jm010146o
154706703 175658 1 None -38 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 432 11 1 2 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4550187 175658 1 None -38 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 432 11 1 2 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4594691 175658 1 None -38 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 432 11 1 2 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
154706461 175774 1 None -93 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 6.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4470439 175774 1 None -93 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 6.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4595600 175774 1 None -93 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 6.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
10613605 199263 0 None -5495 5 Human 5.7 pKi = 5.7 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 292 4 2 2 3.7 c1ccc(CNC[C@H]2CCc3ccc4[nH]ccc4c3O2)cc1 10.1016/s0960-894x(01)00778-8
CHEMBL60185 199263 0 None -5495 5 Human 5.7 pKi = 5.7 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 292 4 2 2 3.7 c1ccc(CNC[C@H]2CCc3ccc4[nH]ccc4c3O2)cc1 10.1016/s0960-894x(01)00778-8
10617381 189094 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 343 4 1 3 3.2 Cc1ccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL51536 189094 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 343 4 1 3 3.2 Cc1ccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)cc1 10.1016/j.bmcl.2005.02.012
11649431 165429 0 None -91 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 528 11 1 6 4.9 CCCc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)nnn1Cc1ccccc1 10.1021/jm0611152
CHEMBL425285 165429 0 None -91 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 528 11 1 6 4.9 CCCc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)nnn1Cc1ccccc1 10.1021/jm0611152
10688035 104290 1 None 38 3 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 332 5 1 3 3.9 c1ccc(CCN2CCC(c3cc(-c4ccccn4)[nH]n3)CC2)cc1 10.1021/jm970111h
CHEMBL310819 104290 1 None 38 3 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 332 5 1 3 3.9 c1ccc(CCN2CCC(c3cc(-c4ccccn4)[nH]n3)CC2)cc1 10.1021/jm970111h
4420454 55966 6 None 1 5 Human 7.7 pKi = 7.7 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 205 5 0 1 3.2 C#CC1=CCC(N(CCC)CCC)CC1 10.1021/jm991098z
CHEMBL162762 55966 6 None 1 5 Human 7.7 pKi = 7.7 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 205 5 0 1 3.2 C#CC1=CCC(N(CCC)CCC)CC1 10.1021/jm991098z
10616050 186064 3 None 81 3 Human 7.7 pKi = 7.7 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 325 5 1 4 2.2 COc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1021/jm970021c
CHEMBL48807 186064 3 None 81 3 Human 7.7 pKi = 7.7 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 325 5 1 4 2.2 COc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1021/jm970021c
10131111 206585 0 None 18 2 Human 7.7 pKi = 7.7 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 246 1 0 3 3.7 CCn1ncc2c1-c1c(C)sc(C)c1CCC2 10.1016/s0960-894x(03)00587-0
CHEMBL99208 206585 0 None 18 2 Human 7.7 pKi = 7.7 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 246 1 0 3 3.7 CCn1ncc2c1-c1c(C)sc(C)c1CCC2 10.1016/s0960-894x(03)00587-0
10041417 26213 4 None -28 3 Human 7.7 pKi = 7.7 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 315 6 1 3 4.3 CCCN(CCc1cccs1)C1CCc2ccc(O)cc2C1 10.1021/jm960345l
CHEMBL135954 26213 4 None -28 3 Human 7.7 pKi = 7.7 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 315 6 1 3 4.3 CCCN(CCc1cccs1)C1CCc2ccc(O)cc2C1 10.1021/jm960345l
10740968 96275 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 423 7 1 5 3.1 COc1ccccc1N1CCN(CCNC(=O)C2CCCc3c(OC)cccc32)CC1 10.1016/S0960-894X(97)00218-7
CHEMBL26426 96275 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 423 7 1 5 3.1 COc1ccccc1N1CCN(CCNC(=O)C2CCCc3c(OC)cccc32)CC1 10.1016/S0960-894X(97)00218-7
44405451 134825 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 430 5 1 3 5.4 O=C(N[C@H]1CCN(Cc2cccc(C(F)(F)F)c2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
CHEMBL372770 134825 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 430 5 1 3 5.4 O=C(N[C@H]1CCN(Cc2cccc(C(F)(F)F)c2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
9908125 118839 0 None 20 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 384 3 1 3 4.7 N#Cc1ccc2[nH]cc(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)c2c1 10.1021/jm0009989
CHEMBL344270 118839 0 None 20 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 384 3 1 3 4.7 N#Cc1ccc2[nH]cc(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)c2c1 10.1021/jm0009989
44436597 91368 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 477 5 1 3 4.9 O=C(NCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(C#Cc2ccccc2)cc1 10.1016/j.bmc.2007.08.038
CHEMBL241210 91368 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 477 5 1 3 4.9 O=C(NCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(C#Cc2ccccc2)cc1 10.1016/j.bmc.2007.08.038
71734127 90626 0 None -4 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm400520c
CHEMBL2397476 90626 0 None -4 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm400520c
46917637 67990 0 None -18 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 1053 34 1 15 9.7 CCCN(CCCCNC(=O)c1ccc(OCCCc2cn(CCCCCCCCn3cc(CCCOc4ccc(CN5CCN(c6ccccc6OC)CC5)cc4OC)nn3)nn2)c(OC)c1)C1Cc2ccccc2C1 10.1021/jm2009919
CHEMBL1916548 67990 0 None -18 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 1053 34 1 15 9.7 CCCN(CCCCNC(=O)c1ccc(OCCCc2cn(CCCCCCCCn3cc(CCCOc4ccc(CN5CCN(c6ccccc6OC)CC5)cc4OC)nn3)nn2)c(OC)c1)C1Cc2ccccc2C1 10.1021/jm2009919
10861560 45078 9 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 369 7 1 5 2.3 COc1ccc(N2CCN(CCNC(=O)c3cccc(OC)c3)CC2)cc1 10.1021/jm020952a
CHEMBL152679 45078 9 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 369 7 1 5 2.3 COc1ccc(N2CCN(CCNC(=O)c3cccc(OC)c3)CC2)cc1 10.1021/jm020952a
11280344 91725 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 376 3 0 3 5.5 Clc1cccc(N2CCN(Cc3csc4ccccc34)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
CHEMBL2420891 91725 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 376 3 0 3 5.5 Clc1cccc(N2CCN(Cc3csc4ccccc34)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
44283941 137403 0 None - 1 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 336 4 1 4 2.4 Cc1ccnc(N2CCN(CCC3NC(=O)c4ccccc43)CC2)c1 10.1016/s0960-894x(98)00252-2
CHEMBL37638 137403 0 None - 1 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 336 4 1 4 2.4 Cc1ccnc(N2CCN(CCC3NC(=O)c4ccccc43)CC2)c1 10.1016/s0960-894x(98)00252-2
11324794 137731 0 None 7 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 324 6 0 5 2.6 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL377050 137731 0 None 7 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 324 6 0 5 2.6 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
90644063 111543 0 None 1 10 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 3 3.7 Cc1ccc(N2CCN(CCCCc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2020.115943
CHEMBL3289648 111543 0 None 1 10 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 3 3.7 Cc1ccc(N2CCN(CCCCc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2020.115943
90644063 111543 0 None -1 10 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 327 6 0 3 3.7 Cc1ccc(N2CCN(CCCCc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289648 111543 0 None -1 10 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 327 6 0 3 3.7 Cc1ccc(N2CCN(CCCCc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
76328715 105891 0 None -2 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 429 9 2 6 2.8 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3115582 105891 0 None -2 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 429 9 2 6 2.8 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139265 105891 0 None -2 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 429 9 2 6 2.8 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
133633 2210 46 None -104 8 Human 6.7 pKi = 6.7 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1021/jm9600712
177 2210 46 None -104 8 Human 6.7 pKi = 6.7 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1021/jm9600712
CHEMBL445102 2210 46 None -104 8 Human 6.7 pKi = 6.7 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1021/jm9600712
44380774 119969 0 None -13 4 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
CHEMBL354180 119969 0 None -13 4 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
154704141 176105 1 None -9 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 3 5.0 CCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4561808 176105 1 None -9 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 3 5.0 CCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4598299 176105 1 None -9 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 3 5.0 CCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
49783042 17509 0 None -7 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 393 7 1 3 4.3 Cc1ccc(C)c(C(=O)NCCCCN2CCN(c3cc(C)ccc3C)CC2)c1 10.1021/jm100899z
CHEMBL1258495 17509 0 None -7 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 393 7 1 3 4.3 Cc1ccc(C)c(C(=O)NCCCCN2CCN(c3cc(C)ccc3C)CC2)c1 10.1021/jm100899z
57390115 68954 0 None -44 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 455 13 1 6 3.4 CCOCCOc1cccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/j.bmc.2011.10.063
CHEMBL1928120 68954 0 None -44 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 455 13 1 6 3.4 CCOCCOc1cccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/j.bmc.2011.10.063
44436601 91511 0 None -21 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 467 8 1 4 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(C#Cc3ccccc3)cc2)CC1 10.1016/j.bmc.2007.08.038
CHEMBL241424 91511 0 None -21 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 467 8 1 4 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(C#Cc3ccccc3)cc2)CC1 10.1016/j.bmc.2007.08.038
10830804 206185 0 None 1 3 Human 5.7 pKi = 5.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 337 5 3 4 1.8 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCNC1 10.1021/jm9601720
CHEMBL96792 206185 0 None 1 3 Human 5.7 pKi = 5.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 337 5 3 4 1.8 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCNC1 10.1021/jm9601720
2337 3205 72 None -114 62 Human 5.7 pKi = 5.7 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
50 3205 72 None -114 62 Human 5.7 pKi = 5.7 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
5002 3205 72 None -114 62 Human 5.7 pKi = 5.7 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
CHEMBL716 3205 72 None -114 62 Human 5.7 pKi = 5.7 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
DB01224 3205 72 None -114 62 Human 5.7 pKi = 5.7 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
10438027 65857 0 None -645 6 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 571 7 1 4 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2o1 10.1016/j.bmcl.2004.05.052
CHEMBL184383 65857 0 None -645 6 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 571 7 1 4 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2o1 10.1016/j.bmcl.2004.05.052
142590710 179690 0 None -3 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 496 11 2 4 5.4 OC(Cc1ccccc1)CN1CCC(NCCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2020.112674
CHEMBL4750607 179690 0 None -3 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 496 11 2 4 5.4 OC(Cc1ccccc1)CN1CCC(NCCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2020.112674
118709166 112913 0 None -39 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 944 25 0 8 12.9 O=C(CCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318838 112913 0 None -39 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 944 25 0 8 12.9 O=C(CCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
12071089 5233 0 None -3 3 Human 6.7 pKi = 6.7 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 445 8 0 2 7.1 Clc1cccc(C(OC2CC3CCC(C2)N3CCCc2ccccc2)c2ccccc2)c1 10.1021/jm010146o
CHEMBL106660 5233 0 None -3 3 Human 6.7 pKi = 6.7 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 445 8 0 2 7.1 Clc1cccc(C(OC2CC3CCC(C2)N3CCCc2ccccc2)c2ccccc2)c1 10.1021/jm010146o
122180610 121224 0 None -40 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 430 8 1 6 4.0 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc4[nH]ccc4c3)nn2)CC1 10.1016/j.bmc.2015.01.017
CHEMBL3588981 121224 0 None -40 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 430 8 1 6 4.0 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc4[nH]ccc4c3)nn2)CC1 10.1016/j.bmc.2015.01.017
44426513 85319 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 372 6 1 2 4.7 O=C(c1ccc2ccccc2c1)N1CCC(NCCCc2ccccc2)CC1 10.1016/j.bmcl.2006.12.096
CHEMBL229077 85319 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 372 6 1 2 4.7 O=C(c1ccc2ccccc2c1)N1CCC(NCCCc2ccccc2)CC1 10.1016/j.bmcl.2006.12.096
154706546 175872 1 None -48 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 459 12 1 3 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4452329 175872 1 None -48 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 459 12 1 3 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4596339 175872 1 None -48 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 459 12 1 3 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
44431472 87054 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 374 5 1 3 4.2 COc1ccc(CN2CCC(NC(=O)c3cccc4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.12.106
CHEMBL233403 87054 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 374 5 1 3 4.2 COc1ccc(CN2CCC(NC(=O)c3cccc4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.12.106
49799713 14294 0 None -177 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 376 4 2 4 3.7 COc1ccc2[nH]cc(CN3CCC(n4c(=O)[nH]c5ccccc54)CC3)c2c1 10.1016/j.bmc.2010.05.052
CHEMBL1173778 14294 0 None -177 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 376 4 2 4 3.7 COc1ccc2[nH]cc(CN3CCC(n4c(=O)[nH]c5ccccc54)CC3)c2c1 10.1016/j.bmc.2010.05.052
CHEMBL1200306 14294 0 None -177 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 376 4 2 4 3.7 COc1ccc2[nH]cc(CN3CCC(n4c(=O)[nH]c5ccccc54)CC3)c2c1 10.1016/j.bmc.2010.05.052
162666450 181707 0 None -15 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 389 7 0 3 5.0 Fc1ccc(CCCCN2CCN(c3ccc(-c4ccccc4)cn3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4783987 181707 0 None -15 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 389 7 0 3 5.0 Fc1ccc(CCCCN2CCN(c3ccc(-c4ccccc4)cn3)CC2)cc1 10.1016/j.bmc.2020.115943
10225942 13043 0 None -147 3 Human 5.7 pKi = 5.7 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 451 9 0 4 6.1 c1ccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)cc1 10.1016/s0960-894x(02)00179-8
CHEMBL1190732 13043 0 None -147 3 Human 5.7 pKi = 5.7 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 451 9 0 4 6.1 c1ccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)cc1 10.1016/s0960-894x(02)00179-8
CHEMBL541524 13043 0 None -147 3 Human 5.7 pKi = 5.7 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 451 9 0 4 6.1 c1ccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)cc1 10.1016/s0960-894x(02)00179-8
45379370 7442 0 None -21 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]radioligand from human recombinant dopamine D4.4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]radioligand from human recombinant dopamine D4.4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2c([nH]c3ccccc23)CC1 10.1021/jm901291r
CHEMBL1087301 7442 0 None -21 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]radioligand from human recombinant dopamine D4.4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]radioligand from human recombinant dopamine D4.4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2c([nH]c3ccccc23)CC1 10.1021/jm901291r
16744003 92126 0 None -43 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 453 10 0 7 4.2 CCOc1ccccc1N1CCN(CCC[C@H]2CC(c3ccc(OC)c(OC)c3)=NO2)CC1 10.1016/j.ejmech.2006.12.030
CHEMBL243225 92126 0 None -43 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 453 10 0 7 4.2 CCOc1ccccc1N1CCN(CCC[C@H]2CC(c3ccc(OC)c(OC)c3)=NO2)CC1 10.1016/j.ejmech.2006.12.030
162666450 181707 0 None -15 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 389 7 0 3 5.0 Fc1ccc(CCCCN2CCN(c3ccc(-c4ccccc4)cn3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4783987 181707 0 None -15 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 389 7 0 3 5.0 Fc1ccc(CCCCN2CCN(c3ccc(-c4ccccc4)cn3)CC2)cc1 10.1016/j.bmc.2020.115943
17755866 142352 1 None -162 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 281 0 1 2 3.4 CN1CCCc2cc(O)ccc2Cc2ccccc2CC1 10.1021/jm070388+
CHEMBL389356 142352 1 None -162 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 281 0 1 2 3.4 CN1CCCc2cc(O)ccc2Cc2ccccc2CC1 10.1021/jm070388+
9929581 16337 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 376 3 0 4 4.4 CC(C)(C)c1ccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)cc1 10.1021/jm990266k
CHEMBL123663 16337 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 376 3 0 4 4.4 CC(C)(C)c1ccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)cc1 10.1021/jm990266k
118719810 115238 0 None -100 4 Human 6.6 pKi = 6.6 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 451 10 0 7 4.5 COc1ccccc1N1CCN(CCCCCc2cn(-c3ccc(SC)cc3)nn2)CC1 10.1016/j.bmcl.2014.12.023
CHEMBL3353914 115238 0 None -100 4 Human 6.6 pKi = 6.6 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 451 10 0 7 4.5 COc1ccccc1N1CCN(CCCCCc2cn(-c3ccc(SC)cc3)nn2)CC1 10.1016/j.bmcl.2014.12.023
44438222 93058 0 None -11 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 349 3 1 2 4.9 N#CC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246230 93058 0 None -11 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 349 3 1 2 4.9 N#CC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
10425024 7057 4 None -40 3 Human 6.6 pKi = 6.6 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 302 3 1 2 3.8 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)cc1 10.1021/jm950721m
CHEMBL108531 7057 4 None -40 3 Human 6.6 pKi = 6.6 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 302 3 1 2 3.8 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)cc1 10.1021/jm950721m
9794644 106797 0 None 2 2 Human 6.6 pKi = 6.6 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 232 0 0 3 3.3 Cc1sc(C)c2c1CCCc1cn(C)nc1-2 10.1016/s0960-894x(03)00587-0
CHEMBL317078 106797 0 None 2 2 Human 6.6 pKi = 6.6 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 232 0 0 3 3.3 Cc1sc(C)c2c1CCCc1cn(C)nc1-2 10.1016/s0960-894x(03)00587-0
127051863 140283 0 None 1 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 384 6 1 4 4.8 OC1(c2ccc(Cl)cc2)CCN(CCCCc2nc3ccccc3o2)CC1 10.1016/j.bmc.2016.06.011
CHEMBL3818940 140283 0 None 1 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 384 6 1 4 4.8 OC1(c2ccc(Cl)cc2)CCN(CCCCc2nc3ccccc3o2)CC1 10.1016/j.bmc.2016.06.011
10425024 7057 4 None -40 3 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human dopamine receptor D4 was determinedBinding affinity towards human dopamine receptor D4 was determined
ChEMBL 302 3 1 2 3.8 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL108531 7057 4 None -40 3 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human dopamine receptor D4 was determinedBinding affinity towards human dopamine receptor D4 was determined
ChEMBL 302 3 1 2 3.8 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)cc1 10.1016/j.bmcl.2005.02.012
44438219 167112 0 None -12 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 339 3 2 2 4.3 NC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL430198 167112 0 None -12 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 339 3 2 2 4.3 NC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
10688036 103668 0 None 38 2 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 332 5 1 3 3.9 c1ccc(CCN2CCC(c3cc(-c4cccnc4)[nH]n3)CC2)cc1 10.1021/jm970111h
CHEMBL309460 103668 0 None 38 2 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 332 5 1 3 3.9 c1ccc(CCN2CCC(c3cc(-c4cccnc4)[nH]n3)CC2)cc1 10.1021/jm970111h
10735344 104379 0 None 52 2 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 332 5 1 3 3.4 c1ccc(CCN2CCN(c3cc(-c4ccccc4)[nH]n3)CC2)cc1 10.1021/jm970111h
CHEMBL310985 104379 0 None 52 2 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 332 5 1 3 3.4 c1ccc(CCN2CCN(c3cc(-c4ccccc4)[nH]n3)CC2)cc1 10.1021/jm970111h
10381810 203463 0 None -1 5 Human 7.6 pKi = 7.6 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ccccc32)CC1 10.1021/jm00043a008
CHEMBL7828 203463 0 None -1 5 Human 7.6 pKi = 7.6 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ccccc32)CC1 10.1021/jm00043a008
44381118 57265 0 None 4 4 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 387 7 2 4 3.6 CNc1cc(OC)c(C(=O)NC[C@H]2CCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(99)00086-4
CHEMBL166587 57265 0 None 4 4 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 387 7 2 4 3.6 CNc1cc(OC)c(C(=O)NC[C@H]2CCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(99)00086-4
44356064 116046 0 None 4 3 Human 7.6 pKi = 7.6 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 329 7 0 3 4.6 CCCN(CCc1cccs1)[C@@H]1CCc2ccc(OC)cc2C1 10.1021/jm960345l
CHEMBL336295 116046 0 None 4 3 Human 7.6 pKi = 7.6 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 329 7 0 3 4.6 CCCN(CCc1cccs1)[C@@H]1CCc2ccc(OC)cc2C1 10.1021/jm960345l
90644063 111543 0 None 1 10 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 3 3.7 Cc1ccc(N2CCN(CCCCc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2020.115943
CHEMBL3289648 111543 0 None 1 10 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 3 3.7 Cc1ccc(N2CCN(CCCCc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2020.115943
90644063 111543 0 None -1 10 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 327 6 0 3 3.7 Cc1ccc(N2CCN(CCCCc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289648 111543 0 None -1 10 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 327 6 0 3 3.7 Cc1ccc(N2CCN(CCCCc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
49783040 17508 0 None -4 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 395 8 1 4 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cc(C)ccc2C)CC1 10.1021/jm100899z
CHEMBL1258494 17508 0 None -4 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 395 8 1 4 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cc(C)ccc2C)CC1 10.1021/jm100899z
72544789 92700 0 None 9 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 363 9 0 7 1.6 COc1ccccc1N1CCN(Cc2cn(CCOCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443010 92700 0 None 9 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 363 9 0 7 1.6 COc1ccccc1N1CCN(Cc2cn(CCOCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
11417962 4905 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 392 7 0 6 3.5 COc1ccc([N+](=O)[O-])cc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL104873 4905 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 392 7 0 6 3.5 COc1ccc([N+](=O)[O-])cc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
10832341 206117 0 None 218 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 359 7 1 4 3.3 COc1cccc(CNCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
CHEMBL96462 206117 0 None 218 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 359 7 1 4 3.3 COc1cccc(CNCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
168278360 192245 0 None 8 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 377 7 0 3 4.0 O=C1CCc2ccccc2N1CCCCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5188796 192245 0 None 8 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 377 7 0 3 4.0 O=C1CCc2ccccc2N1CCCCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5221749 192245 0 None 8 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 377 7 0 3 4.0 O=C1CCc2ccccc2N1CCCCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.2c00840
11089541 83966 0 None 2 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 354 6 1 5 2.0 COc1cccc(C(=O)NCCN2CCN(c3cc(C)ccn3)CC2)c1 10.1021/jm020952a
CHEMBL2112905 83966 0 None 2 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 354 6 1 5 2.0 COc1cccc(C(=O)NCCN2CCN(c3cc(C)ccn3)CC2)c1 10.1021/jm020952a
CHEMBL2219567 83966 0 None 2 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 354 6 1 5 2.0 COc1cccc(C(=O)NCCN2CCN(c3cc(C)ccn3)CC2)c1 10.1021/jm020952a
9883554 164802 0 None 141 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 320 4 1 4 2.1 N#Cc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL423659 164802 0 None 141 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 320 4 1 4 2.1 N#Cc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1016/j.bmcl.2005.02.012
10071413 83556 0 None -41 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 431 8 2 5 3.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(C#N)ccc3[nH]2)CC1 10.1021/jm0611152
CHEMBL220700 83556 0 None -41 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 431 8 2 5 3.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(C#N)ccc3[nH]2)CC1 10.1021/jm0611152
35295787 85314 4 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 5 1 2 4.3 O=C(NC1CCN(CCc2ccccc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.096
CHEMBL229021 85314 4 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 5 1 2 4.3 O=C(NC1CCN(CCc2ccccc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.096
44336571 4762 0 None 30 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 316 4 0 4 3.8 N#CC(C#N)=Cc1ccn(C2CCN(Cc3ccccc3)CC2)c1 10.1016/s0960-894x(99)00540-5
CHEMBL104201 4762 0 None 30 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 316 4 0 4 3.8 N#CC(C#N)=Cc1ccn(C2CCN(Cc3ccccc3)CC2)c1 10.1016/s0960-894x(99)00540-5
52937680 60845 0 None -416 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 466 10 1 4 5.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1Cc2cccn3ncc(c23)C1 10.1021/jm101639t
CHEMBL1765632 60845 0 None -416 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 466 10 1 4 5.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1Cc2cccn3ncc(c23)C1 10.1021/jm101639t
9838216 201498 1 None -12 5 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 266 6 2 2 3.3 c1ccc(CNCCOc2cccc3[nH]ccc23)cc1 10.1016/s0960-894x(99)00434-5
CHEMBL64283 201498 1 None -12 5 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 266 6 2 2 3.3 c1ccc(CNCCOc2cccc3[nH]ccc23)cc1 10.1016/s0960-894x(99)00434-5
130431279 175311 0 None -102 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 254 3 1 3 2.3 CCc1cc(Cl)c(OC)c(N2CCNCC2)c1 10.1021/acs.jmedchem.6b00860
CHEMBL4586327 175311 0 None -102 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 254 3 1 3 2.3 CCc1cc(Cl)c(OC)c(N2CCNCC2)c1 10.1021/acs.jmedchem.6b00860
44264741 203034 0 None 1 3 Human 4.6 pKi = 4.6 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 340 2 0 4 3.0 O=C(c1cnn2ccccc12)N1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(98)00692-1
CHEMBL7441 203034 0 None 1 3 Human 4.6 pKi = 4.6 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 340 2 0 4 3.0 O=C(c1cnn2ccccc12)N1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(98)00692-1
10300403 13618 0 None -120 3 Human 5.6 pKi = 5.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 496 10 0 6 6.0 O=[N+]([O-])c1cccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)c1 10.1016/s0960-894x(02)00179-8
CHEMBL1195074 13618 0 None -120 3 Human 5.6 pKi = 5.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 496 10 0 6 6.0 O=[N+]([O-])c1cccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)c1 10.1016/s0960-894x(02)00179-8
CHEMBL553810 13618 0 None -120 3 Human 5.6 pKi = 5.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 496 10 0 6 6.0 O=[N+]([O-])c1cccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)c1 10.1016/s0960-894x(02)00179-8
122180575 121213 0 None -21 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 441 8 0 6 4.7 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc4ccccc4c3)nn2)CC1 10.1016/j.bmc.2015.01.017
CHEMBL3588920 121213 0 None -21 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 441 8 0 6 4.7 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc4ccccc4c3)nn2)CC1 10.1016/j.bmc.2015.01.017
24060 119150 7 None -6 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 264 5 0 2 3.4 CN(C)CCC(C#N)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
CHEMBL346898 119150 7 None -6 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 264 5 0 2 3.4 CN(C)CCC(C#N)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
154725813 175952 1 None -89 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 475 12 1 3 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4568916 175952 1 None -89 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 475 12 1 3 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4597047 175952 1 None -89 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 475 12 1 3 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
44276079 13688 0 None -11 3 Human 6.6 pKi = 6.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 439 9 0 6 4.6 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4F)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
CHEMBL1195587 13688 0 None -11 3 Human 6.6 pKi = 6.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 439 9 0 6 4.6 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4F)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
CHEMBL554897 13688 0 None -11 3 Human 6.6 pKi = 6.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 439 9 0 6 4.6 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4F)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
56664952 66052 0 None -33 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 423 9 1 5 4.0 COc1ccccc1N1CCN(CCCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1813598 66052 0 None -33 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 423 9 1 5 4.0 COc1ccccc1N1CCN(CCCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1851753 66052 0 None -33 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 423 9 1 5 4.0 COc1ccccc1N1CCN(CCCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1016/j.bmc.2011.04.021
9928332 96732 4 None -117 9 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D4Inhibition of [3H]spiperone binding to Dopamine receptor D4
ChEMBL 349 6 0 3 5.0 COc1cccc2c1CCC[C@H]2CN(C)CCc1ccc2ccoc2c1 10.1021/jm049619s
CHEMBL268258 96732 4 None -117 9 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D4Inhibition of [3H]spiperone binding to Dopamine receptor D4
ChEMBL 349 6 0 3 5.0 COc1cccc2c1CCC[C@H]2CN(C)CCc1ccc2ccoc2c1 10.1021/jm049619s
CHEMBL5083186 213078 0 None -1202 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCOC(=O)/C=C1\[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2CC1CC1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.1c00611
44336172 5289 0 None 16 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 476 6 0 5 2.3 CN(C)S(=O)(=O)c1ccc2c(c1)CCN2C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL106917 5289 0 None 16 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 476 6 0 5 2.3 CN(C)S(=O)(=O)c1ccc2c(c1)CCN2C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
44336194 107053 0 None 16 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 415 5 0 4 3.8 CSc1ccc2c(c1)CCN2C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL318760 107053 0 None 16 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 415 5 0 4 3.8 CSc1ccc2c(c1)CCN2C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
122181334 121362 0 None -954 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 442 7 2 5 3.4 Cc1ccc(Cl)c(N2CCN(CCCCNC(=O)c3ccc4oc(=O)[nH]c4c3)CC2)c1 10.1021/jm501512b
CHEMBL3590086 121362 0 None -954 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 442 7 2 5 3.4 Cc1ccc(Cl)c(N2CCN(CCCCNC(=O)c3ccc4oc(=O)[nH]c4c3)CC2)c1 10.1021/jm501512b
130431317 172381 0 None -2454 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 455 8 2 5 4.0 CCc1cccc(N2CCN(CC(O)CCNC(=O)c3cc4ccccc4o3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4517102 172381 0 None -2454 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 455 8 2 5 4.0 CCc1cccc(N2CCN(CC(O)CCNC(=O)c3cc4ccccc4o3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
164628177 188026 0 None -25 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 366 7 1 5 2.8 CC(=O)Nc1ccc(C(=O)CCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
CHEMBL4875079 188026 0 None -25 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 366 7 1 5 2.8 CC(=O)Nc1ccc(C(=O)CCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
CHEMBL5029038 188026 0 None -25 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 366 7 1 5 2.8 CC(=O)Nc1ccc(C(=O)CCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
10404657 97619 0 None -28 5 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 334 5 0 3 3.1 O=C1c2ccccc2C(=O)N1CCCCN1CCc2ccccc2C1 10.1016/j.bmc.2016.05.053
CHEMBL273241 97619 0 None -28 5 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 334 5 0 3 3.1 O=C1c2ccccc2C(=O)N1CCCCN1CCc2ccccc2C1 10.1016/j.bmc.2016.05.053
11213037 136579 0 None -851 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 447 8 1 3 5.3 O=C(NCCCCN1CCN(c2ccccc2Cl)CC1)c1ccc(-c2ccccc2)cc1 10.1021/jm0611152
CHEMBL374749 136579 0 None -851 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 447 8 1 3 5.3 O=C(NCCCCN1CCN(c2ccccc2Cl)CC1)c1ccc(-c2ccccc2)cc1 10.1021/jm0611152
71618702 142850 0 None -5 4 Mouse 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 400 5 0 4 3.4 CC1Cc2ccccc2N1C(=O)CN1CCO[C@H](COc2cccc(Cl)c2)C1 nan
CHEMBL3897835 142850 0 None -5 4 Mouse 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 400 5 0 4 3.4 CC1Cc2ccccc2N1C(=O)CN1CCO[C@H](COc2cccc(Cl)c2)C1 nan
90644070 111549 0 None -3 2 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 366 5 0 3 5.0 Clc1ccc(N2C[C@H]3C[C@@H]2CN3CCCc2cc3ccccc3o2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289654 111549 0 None -3 2 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 366 5 0 3 5.0 Clc1ccc(N2C[C@H]3C[C@@H]2CN3CCCc2cc3ccccc3o2)cc1 10.1016/j.bmc.2014.04.026
164628177 188026 0 None -25 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 366 7 1 5 2.8 CC(=O)Nc1ccc(C(=O)CCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
CHEMBL4875079 188026 0 None -25 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 366 7 1 5 2.8 CC(=O)Nc1ccc(C(=O)CCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
CHEMBL5029038 188026 0 None -25 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 366 7 1 5 2.8 CC(=O)Nc1ccc(C(=O)CCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
44394636 66584 0 None 63 2 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@@H]1CCN(Cc2ccccc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL186558 66584 0 None 63 2 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@@H]1CCN(Cc2ccccc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2004.07.045
44214765 165247 0 None 208 2 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 371 5 2 3 3.9 Nc1cccc(-c2ccc(C(=O)NC3CCN(Cc4ccccc4)C3)cc2)c1 10.1016/j.bmcl.2004.07.045
CHEMBL424808 165247 0 None 208 2 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 371 5 2 3 3.9 Nc1cccc(-c2ccc(C(=O)NC3CCN(Cc4ccccc4)C3)cc2)c1 10.1016/j.bmcl.2004.07.045
219050 3321 21 None -58 21 Human 7.6 pKi = 7.6 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 10.1021/jm950721m
52 3321 21 None -58 21 Human 7.6 pKi = 7.6 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 10.1021/jm950721m
CHEMBL431367 3321 21 None -58 21 Human 7.6 pKi = 7.6 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 10.1021/jm950721m
13015797 204181 0 None 1 4 Rat 7.6 pKi = 7.6 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 400 6 0 5 3.7 COc1cc2c(cc1OC)C(CCN1CCN(c3ccc(F)cc3)CC1)OCC2 10.1021/jm960084f
CHEMBL83915 204181 0 None 1 4 Rat 7.6 pKi = 7.6 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 400 6 0 5 3.7 COc1cc2c(cc1OC)C(CCN1CCN(c3ccc(F)cc3)CC1)OCC2 10.1021/jm960084f
9888555 165052 11 None -208 8 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm100899z
CHEMBL424294 165052 11 None -208 8 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm100899z
136056636 111296 0 None -28 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287404 111296 0 None -28 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
118709159 112906 0 None -3 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 832 17 0 8 9.7 O=C(CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318831 112906 0 None -3 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 832 17 0 8 9.7 O=C(CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
11156017 5057 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 487 7 0 4 4.6 CCOc1cc(I)ccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL105686 5057 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 487 7 0 4 4.6 CCOc1cc(I)ccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
9927411 201364 0 None 4 4 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 327 0 1 5 3.1 CN1CCN(C2=Nc3cccnc3Nc3ccc(Cl)cc32)CC1 10.1021/jm0104825
CHEMBL63576 201364 0 None 4 4 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 327 0 1 5 3.1 CN1CCN(C2=Nc3cccnc3Nc3ccc(Cl)cc32)CC1 10.1021/jm0104825
9797200 118466 0 None 109 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 321 4 1 3 2.7 O=C1NC(CCN2CCN(c3ccccc3)CC2)c2ccccc21 10.1016/s0960-894x(98)00252-2
CHEMBL34239 118466 0 None 109 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 321 4 1 3 2.7 O=C1NC(CCN2CCN(c3ccccc3)CC2)c2ccccc21 10.1016/s0960-894x(98)00252-2
45482153 196361 0 None -5 4 Human 6.6 pKi = 6.6 Binding
Binding affinity to human cloned dopamine D4.4 expressed in CHO cellsBinding affinity to human cloned dopamine D4.4 expressed in CHO cells
ChEMBL 502 9 1 7 3.9 COc1ccc(-n2cc(C(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)nn2)cc1 10.1016/j.bmc.2009.06.041
CHEMBL574030 196361 0 None -5 4 Human 6.6 pKi = 6.6 Binding
Binding affinity to human cloned dopamine D4.4 expressed in CHO cellsBinding affinity to human cloned dopamine D4.4 expressed in CHO cells
ChEMBL 502 9 1 7 3.9 COc1ccc(-n2cc(C(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)nn2)cc1 10.1016/j.bmc.2009.06.041
44380785 120290 0 None -7 4 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
CHEMBL355566 120290 0 None -7 4 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
10404657 97619 0 None -28 5 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 334 5 0 3 3.1 O=C1c2ccccc2C(=O)N1CCCCN1CCc2ccccc2C1 10.1016/j.bmc.2016.05.053
CHEMBL273241 97619 0 None -28 5 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 334 5 0 3 3.1 O=C1c2ccccc2C(=O)N1CCCCN1CCc2ccccc2C1 10.1016/j.bmc.2016.05.053
90644064 111544 0 None -1 4 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 383 7 0 4 5.0 Clc1ccc(N2CCN(CCCCCc3nc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289649 111544 0 None -1 4 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 383 7 0 4 5.0 Clc1ccc(N2CCN(CCCCCc3nc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
57390117 68957 0 None -16 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 455 13 1 6 3.2 CCOCCOCc1ccc(C(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2011.10.063
CHEMBL1928123 68957 0 None -16 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 455 13 1 6 3.2 CCOCCOCc1ccc(C(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2011.10.063
127047221 139400 0 None 1 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
CHEMBL3799593 139400 0 None 1 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
57400562 68976 0 None -2 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 469 14 1 6 3.6 CCOCCOCc1ccc(N2CCN(CCCCNC(=O)c3ccccc3)CC2)c(OC)c1 10.1016/j.bmc.2011.10.063
CHEMBL1928247 68976 0 None -2 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 469 14 1 6 3.6 CCOCCOCc1ccc(N2CCN(CCCCNC(=O)c3ccccc3)CC2)c(OC)c1 10.1016/j.bmc.2011.10.063
71086389 159861 0 None 1 2 Mouse 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 339 6 0 5 2.2 c1cncc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL4111289 159861 0 None 1 2 Mouse 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 339 6 0 5 2.2 c1cncc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
10811814 205732 0 None -6 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 415 9 1 4 4.1 COc1cccc(C(=O)NCCCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm020952a
CHEMBL94265 205732 0 None -6 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 415 9 1 4 4.1 COc1cccc(C(=O)NCCCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm020952a
154704941 176053 1 None -7 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 470 11 0 6 5.8 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4578364 176053 1 None -7 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 470 11 0 6 5.8 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4597877 176053 1 None -7 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 470 11 0 6 5.8 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
10811814 205732 0 None -6 2 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 415 9 1 4 4.1 COc1cccc(C(=O)NCCCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
CHEMBL94265 205732 0 None -6 2 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 415 9 1 4 4.1 COc1cccc(C(=O)NCCCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
168281091 190477 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccc(C)cc3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5187429 190477 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccc(C)cc3)C2)cc1F 10.1016/j.bmcl.2022.128615
182600 118239 2 None -2 4 Rat 6.6 pKi = 6.6 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 352 5 0 3 3.9 O=C(CCCN1CCN2c3ccccc3CCC2C1)c1ccc(F)cc1 10.1021/jm049031l
CHEMBL341774 118239 2 None -2 4 Rat 6.6 pKi = 6.6 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 352 5 0 3 3.9 O=C(CCCN1CCN2c3ccccc3CCC2C1)c1ccc(F)cc1 10.1021/jm049031l
10229397 13145 0 None -123 3 Human 5.6 pKi = 5.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 511 11 0 6 6.1 COc1ccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
CHEMBL1191467 13145 0 None -123 3 Human 5.6 pKi = 5.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 511 11 0 6 6.1 COc1ccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
CHEMBL542571 13145 0 None -123 3 Human 5.6 pKi = 5.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 511 11 0 6 6.1 COc1ccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
44438215 92977 5 None 1 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 340 3 2 2 4.3 OC1(c2ccc(Cl)cc2)CCCN(Cc2c[nH]c3ccccc23)C1 10.1016/j.bmcl.2006.10.076
CHEMBL245816 92977 5 None 1 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 340 3 2 2 4.3 OC1(c2ccc(Cl)cc2)CCCN(Cc2c[nH]c3ccccc23)C1 10.1016/j.bmcl.2006.10.076
9906978 42466 1 None 1 12 Human 6.6 pKi = 6.6 Binding
Binding affinity to human cloned dopamine D4.4 receptor by radioligand binding assayBinding affinity to human cloned dopamine D4.4 receptor by radioligand binding assay
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmcl.2006.03.057
CHEMBL150161 42466 1 None 1 12 Human 6.6 pKi = 6.6 Binding
Binding affinity to human cloned dopamine D4.4 receptor by radioligand binding assayBinding affinity to human cloned dopamine D4.4 receptor by radioligand binding assay
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmcl.2006.03.057
49798812 14205 0 None -16 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 433 3 1 3 4.5 OC1(c2ccc(I)cc2)CCN(Cc2cc3ccccc3o2)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1170456 14205 0 None -16 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 433 3 1 3 4.5 OC1(c2ccc(I)cc2)CCN(Cc2cc3ccccc3o2)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1199971 14205 0 None -16 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 433 3 1 3 4.5 OC1(c2ccc(I)cc2)CCN(Cc2cc3ccccc3o2)CC1 10.1016/j.bmc.2010.05.052
9906978 42466 1 None 1 12 Human 6.6 pKi = 6.6 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL150161 42466 1 None 1 12 Human 6.6 pKi = 6.6 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
23290944 81414 0 None -323 7 Human 6.6 pKi = 6.6 Binding
Binding affinity to dopamine D4 receptor by radioligand binding assayBinding affinity to dopamine D4 receptor by radioligand binding assay
ChEMBL 392 6 0 4 3.8 O=C(C1CCCCC1)N(CCN1CCN(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL2164350 81414 0 None -323 7 Human 6.6 pKi = 6.6 Binding
Binding affinity to dopamine D4 receptor by radioligand binding assayBinding affinity to dopamine D4 receptor by radioligand binding assay
ChEMBL 392 6 0 4 3.8 O=C(C1CCCCC1)N(CCN1CCN(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
51353989 59893 0 None -112 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 481 11 1 5 5.1 O=C(NCCCCN1CCN(c2ccccc2OCCF)CC1)c1ccc(-c2ccsc2)cc1 10.1021/jm101323b
CHEMBL1689006 59893 0 None -112 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 481 11 1 5 5.1 O=C(NCCCCN1CCN(c2ccccc2OCCF)CC1)c1ccc(-c2ccsc2)cc1 10.1021/jm101323b
CHEMBL1739963 59893 0 None -112 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 481 11 1 5 5.1 O=C(NCCCCN1CCN(c2ccccc2OCCF)CC1)c1ccc(-c2ccsc2)cc1 10.1021/jm101323b
9908071 201315 0 None 3 2 Human 5.6 pKi = 5.6 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 383 3 0 3 3.4 CN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)CCc2ccccc21 10.1016/s0960-894x(00)00421-2
CHEMBL63209 201315 0 None 3 2 Human 5.6 pKi = 5.6 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 383 3 0 3 3.4 CN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)CCc2ccccc21 10.1016/s0960-894x(00)00421-2
21533446 69812 0 None -6 10 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 379 6 1 3 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmc.2011.12.019
CHEMBL1940403 69812 0 None -6 10 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 379 6 1 3 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmc.2011.12.019
90181059 159684 0 None -1 4 Mouse 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 382 6 0 5 2.4 COc1cccc(OC[C@H]2CN(CC(=O)N3CCc4ccccc43)CCO2)c1 nan
CHEMBL4109801 159684 0 None -1 4 Mouse 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 382 6 0 5 2.4 COc1cccc(OC[C@H]2CN(CC(=O)N3CCc4ccccc43)CCO2)c1 nan
44339879 171716 0 None 4 4 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.8 CNc1cc(OC)c(C(=O)N[C@H]2CCCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL447476 171716 0 None 4 4 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.8 CNc1cc(OC)c(C(=O)N[C@H]2CCCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(03)00678-4
11792324 204016 0 None 8 2 Rat 7.6 pKi = 7.6 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 352 5 0 4 3.5 COc1ccc(N2CCN(CC[C@H]3OCCc4ccccc43)CC2)cc1 10.1021/jm960084f
CHEMBL82591 204016 0 None 8 2 Rat 7.6 pKi = 7.6 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 352 5 0 4 3.5 COc1ccc(N2CCN(CC[C@H]3OCCc4ccccc43)CC2)cc1 10.1021/jm960084f
10851078 197709 1 None 3 3 Human 7.6 pKi = 7.6 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 290 3 1 1 4.5 c1ccc(C2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1021/jm9600712
CHEMBL59103 197709 1 None 3 3 Human 7.6 pKi = 7.6 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 290 3 1 1 4.5 c1ccc(C2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1021/jm9600712
10644771 106605 0 None -61 4 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 401 8 1 4 3.7 COc1cccc(C(=O)NCCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm020952a
CHEMBL315879 106605 0 None -61 4 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 401 8 1 4 3.7 COc1cccc(C(=O)NCCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm020952a
44335761 108734 0 None 8 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 379 5 0 4 2.8 COc1ccccc1CN1CCN(CC(=O)N2c3ccccc3CC2C)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL321734 108734 0 None 8 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 379 5 0 4 2.8 COc1ccccc1CN1CCN(CC(=O)N2c3ccccc3CC2C)CC1 10.1016/s0960-894x(02)00655-8
10851078 197709 1 None 3 3 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 290 3 1 1 4.5 c1ccc(C2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1021/jm0002432
CHEMBL59103 197709 1 None 3 3 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 290 3 1 1 4.5 c1ccc(C2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1021/jm0002432
145988693 166613 0 None 5 17 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
ChEMBL 524 7 1 3 7.1 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL4291048 166613 0 None 5 17 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
ChEMBL 524 7 1 3 7.1 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
45268293 194461 0 None 20 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 408 4 1 7 1.4 Cn1c(N2CCOCC2)nc2c(CN3CCN(c4ccccc4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
CHEMBL561123 194461 0 None 20 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 408 4 1 7 1.4 Cn1c(N2CCOCC2)nc2c(CN3CCN(c4ccccc4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
10644771 106605 0 None -61 4 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 401 8 1 4 3.7 COc1cccc(C(=O)NCCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
CHEMBL315879 106605 0 None -61 4 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 401 8 1 4 3.7 COc1cccc(C(=O)NCCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
44301157 101236 0 None 79 2 Human 7.6 pKi = 7.6 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 343 5 0 3 4.4 O=C(OCC1CCN(Cc2ccccc2)CC1)c1ccc(Cl)cc1 10.1021/jm960017l
CHEMBL299479 101236 0 None 79 2 Human 7.6 pKi = 7.6 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 343 5 0 3 4.4 O=C(OCC1CCN(Cc2ccccc2)CC1)c1ccc(Cl)cc1 10.1021/jm960017l
10595646 197677 0 None 63 2 Human 7.6 pKi = 7.6 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 375 7 0 3 5.5 COc1cc2ccccc2cc1OCCC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
CHEMBL59075 197677 0 None 63 2 Human 7.6 pKi = 7.6 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 375 7 0 3 5.5 COc1cc2ccccc2cc1OCCC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
42266974 98838 8 None 100 2 Human 7.6 pKi = 7.6 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 323 4 1 3 2.6 CC(C)(C)C(=O)NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL282008 98838 8 None 100 2 Human 7.6 pKi = 7.6 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 323 4 1 3 2.6 CC(C)(C)C(=O)NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
2726 906 64 None -8 72 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
621 906 64 None -8 72 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
83 906 64 None -8 72 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
CHEMBL71 906 64 None -8 72 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
DB00477 906 64 None -8 72 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
11185987 79938 0 None 10 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 310 5 1 5 2.5 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL214314 79938 0 None 10 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 310 5 1 5 2.5 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
16094666 81315 2 None 52 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL216393 81315 2 None 52 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL5089655 213446 0 None 2 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None N#CC(CCNCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
10089203 41112 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 349 4 1 6 3.1 CNc1nc(Cl)c(Sc2ccccc2)c(N2CCN(C)CC2)n1 10.1016/s0960-894x(01)00167-6
CHEMBL14899 41112 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 349 4 1 6 3.1 CNc1nc(Cl)c(Sc2ccccc2)c(N2CCN(C)CC2)n1 10.1016/s0960-894x(01)00167-6
233199 155071 15 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 286 3 0 2 3.7 Clc1ccc(N2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.12.026
CHEMBL404570 155071 15 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 286 3 0 2 3.7 Clc1ccc(N2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.12.026
44380717 119843 0 None 10 4 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 415 7 2 4 3.6 COc1cc(NC(C)=O)c(Cl)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL353087 119843 0 None 10 4 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 415 7 2 4 3.6 COc1cc(NC(C)=O)c(Cl)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
23642427 91367 0 None -549 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 430 7 1 4 2.7 C=CCN1CCC[C@H]1CNC(=O)c1cc(I)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
CHEMBL241169 91367 0 None -549 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 430 7 1 4 2.7 C=CCN1CCC[C@H]1CNC(=O)c1cc(I)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
57395340 68958 0 None -28 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 469 14 1 6 3.6 CCOCCOCc1ccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2011.10.063
CHEMBL1928124 68958 0 None -28 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 469 14 1 6 3.6 CCOCCOCc1ccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2011.10.063
11774358 5084 0 None - 1 Human 6.6 pKi = 6.6 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 415 6 0 4 4.6 COc1ccc(C(F)(F)F)cc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL105836 5084 0 None - 1 Human 6.6 pKi = 6.6 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 415 6 0 4 4.6 COc1ccc(C(F)(F)F)cc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
12049520 100596 6 None 9 4 Human 6.6 pKi = 6.6 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 319 4 0 4 3.7 c1ccc(-c2nc(CN3CCN(c4ccccc4)CC3)co2)cc1 10.1016/s0960-894x(00)00405-4
CHEMBL294780 100596 6 None 9 4 Human 6.6 pKi = 6.6 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 319 4 0 4 3.7 c1ccc(-c2nc(CN3CCN(c4ccccc4)CC3)co2)cc1 10.1016/s0960-894x(00)00405-4
10449136 205698 0 None 1 3 Human 5.6 pKi = 5.6 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 327 1 0 1 5.6 CC(C)=C1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL94067 205698 0 None 1 3 Human 5.6 pKi = 5.6 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 327 1 0 1 5.6 CC(C)=C1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
10014924 106787 0 None -16 5 Human 5.6 pKi = 5.6 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1 10.1021/jm0503805
CHEMBL316983 106787 0 None -16 5 Human 5.6 pKi = 5.6 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1 10.1021/jm0503805
10014924 106787 0 None -16 5 Human 5.6 pKi = 5.6 Binding
Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsLow inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1 10.1021/jm049269+
CHEMBL316983 106787 0 None -16 5 Human 5.6 pKi = 5.6 Binding
Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsLow inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1 10.1021/jm049269+
18519 67318 26 None 1 2 Human 5.6 pKi = 5.6 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 287 2 5 5 1.9 Oc1ccc(CC2NCCc3cc(O)c(O)cc32)cc1O 10.1016/S0960-894X(97)00194-7
CHEMBL19068 67318 26 None 1 2 Human 5.6 pKi = 5.6 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 287 2 5 5 1.9 Oc1ccc(CC2NCCc3cc(O)c(O)cc32)cc1O 10.1016/S0960-894X(97)00194-7
134155116 150436 0 None -158 7 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 309 3 0 2 3.6 O=C1c2ccc(F)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
CHEMBL3958215 150436 0 None -158 7 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 309 3 0 2 3.6 O=C1c2ccc(F)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
242 467 117 None -117 51 Human 6.6 pKi = 6.6 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
34 467 117 None -117 51 Human 6.6 pKi = 6.6 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
60795 467 117 None -117 51 Human 6.6 pKi = 6.6 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
CHEMBL1112 467 117 None -117 51 Human 6.6 pKi = 6.6 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
DB01238 467 117 None -117 51 Human 6.6 pKi = 6.6 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
155547197 173023 0 None -208 7 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 341 6 0 4 3.4 O=C(CCCN1CCCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL4533305 173023 0 None -208 7 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 341 6 0 4 3.4 O=C(CCCN1CCCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
134155116 150436 0 None -158 7 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 309 3 0 2 3.6 O=C1c2ccc(F)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
CHEMBL3958215 150436 0 None -158 7 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 309 3 0 2 3.6 O=C1c2ccc(F)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
11540842 83953 0 None -29 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 514 10 1 6 4.7 Cc1c(C(=O)NCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)nnn1Cc1ccccc1 10.1021/jm0611152
CHEMBL221897 83953 0 None -29 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 514 10 1 6 4.7 Cc1c(C(=O)NCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)nnn1Cc1ccccc1 10.1021/jm0611152
9872676 77826 0 None -6309 17 Human 5.6 pKi = 5.6 Binding
Binding affinity to human D4.4 receptorBinding affinity to human D4.4 receptor
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
CHEMBL210514 77826 0 None -6309 17 Human 5.6 pKi = 5.6 Binding
Binding affinity to human D4.4 receptorBinding affinity to human D4.4 receptor
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
11522476 74174 0 None -4 3 Human 5.6 pKi = 5.6 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 311 2 0 3 3.3 COc1cc2c(cc1OC)Cc1ccccc1CCN(C)CC2 10.1021/jm050846j
CHEMBL202924 74174 0 None -4 3 Human 5.6 pKi = 5.6 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 311 2 0 3 3.3 COc1cc2c(cc1OC)Cc1ccccc1CCN(C)CC2 10.1021/jm050846j
71453386 81409 0 None -17 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 433 6 0 3 5.7 O=C(c1cccc2ccccc12)N(CCN1CC=C(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL2164345 81409 0 None -17 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 433 6 0 3 5.7 O=C(c1cccc2ccccc12)N(CCN1CC=C(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
4987774 14244 1 None -14 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 385 3 1 3 4.7 OC1(c2ccc(Br)cc2)CCN(Cc2cc3ccccc3o2)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1172210 14244 1 None -14 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 385 3 1 3 4.7 OC1(c2ccc(Br)cc2)CCN(Cc2cc3ccccc3o2)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1200151 14244 1 None -14 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 385 3 1 3 4.7 OC1(c2ccc(Br)cc2)CCN(Cc2cc3ccccc3o2)CC1 10.1016/j.bmc.2010.05.052
10801925 11519 1 None -9 5 Human 6.6 pKi = 6.6 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@H](CNCc1ccccc1)CC2 10.1021/jm9703653
CHEMBL1180675 11519 1 None -9 5 Human 6.6 pKi = 6.6 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@H](CNCc1ccccc1)CC2 10.1021/jm9703653
CHEMBL138016 11519 1 None -9 5 Human 6.6 pKi = 6.6 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@H](CNCc1ccccc1)CC2 10.1021/jm9703653
44330340 106989 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 275 2 1 3 3.3 Cc1sc(C)c2c1CCCc1c(CN(C)C)n[nH]c1-2 10.1016/s0960-894x(03)00587-0
CHEMBL318415 106989 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 275 2 1 3 3.3 Cc1sc(C)c2c1CCCc1c(CN(C)C)n[nH]c1-2 10.1016/s0960-894x(03)00587-0
46227317 198479 0 None -14 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 265 1 0 2 3.4 COc1ccc2c(c1)CCN1Cc3ccccc3CC21 10.1016/j.bmc.2009.08.028
CHEMBL596448 198479 0 None -14 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 265 1 0 2 3.4 COc1ccc2c(c1)CCN1Cc3ccccc3CC21 10.1016/j.bmc.2009.08.028
155547197 173023 0 None -208 7 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 341 6 0 4 3.4 O=C(CCCN1CCCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL4533305 173023 0 None -208 7 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 341 6 0 4 3.4 O=C(CCCN1CCCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
11633816 13014 2 None -48 3 Human 6.6 pKi = 6.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 451 10 0 7 4.5 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4OC)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
CHEMBL1190494 13014 2 None -48 3 Human 6.6 pKi = 6.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 451 10 0 7 4.5 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4OC)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
CHEMBL541025 13014 2 None -48 3 Human 6.6 pKi = 6.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 451 10 0 7 4.5 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4OC)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
137640511 156524 0 None 14 8 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 286 4 0 2 3.1 CC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4074104 156524 0 None 14 8 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 286 4 0 2 3.1 CC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
23363843 109183 0 None 4 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 5 0 4 2.7 O=C1C(=O)N(CCN2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/s0960-894x(02)00655-8
CHEMBL322567 109183 0 None 4 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 5 0 4 2.7 O=C1C(=O)N(CCN2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/s0960-894x(02)00655-8
44370058 119189 0 None 19 3 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 336 5 1 4 2.9 COc1ccc(N2CCN(CCc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(99)00025-6
CHEMBL347291 119189 0 None 19 3 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 336 5 1 4 2.9 COc1ccc(N2CCN(CCc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(99)00025-6
10357628 13810 0 None -1 3 Human 7.6 pKi = 7.6 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 303 2 0 2 5.0 CCN1CC=C(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL1196433 13810 0 None -1 3 Human 7.6 pKi = 7.6 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 303 2 0 2 5.0 CCN1CC=C(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL556969 13810 0 None -1 3 Human 7.6 pKi = 7.6 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 303 2 0 2 5.0 CCN1CC=C(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
10474613 162740 0 None 54 2 Human 7.6 pKi = 7.6 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 375 7 1 3 4.5 OC(COc1cccc2ccccc12)CN1CCC(Cc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
CHEMBL418758 162740 0 None 54 2 Human 7.6 pKi = 7.6 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 375 7 1 3 4.5 OC(COc1cccc2ccccc12)CN1CCC(Cc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
10176799 206521 0 None 17 2 Human 7.6 pKi = 7.6 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 218 0 0 3 2.9 Cc1sc(C)c2c1CCc1cnn(C)c1-2 10.1016/s0960-894x(03)00587-0
CHEMBL98830 206521 0 None 17 2 Human 7.6 pKi = 7.6 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 218 0 0 3 2.9 Cc1sc(C)c2c1CCc1cnn(C)c1-2 10.1016/s0960-894x(03)00587-0
127029389 138913 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3cccc(F)c3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793984 138913 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3cccc(F)c3)C2)cc1 10.1016/j.bmcl.2016.03.102
44431488 87647 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.5 Cc1ccccc1CN1CCC(NC(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2006.12.106
CHEMBL234647 87647 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.5 Cc1ccccc1CN1CCC(NC(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2006.12.106
22100933 202587 4 None 22 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 323 3 1 2 4.5 Clc1ccc2[nH]c(C3=CCN(Cc4ccccc4)CC3)nc2c1 10.1016/S0960-894X(97)00402-2
CHEMBL71324 202587 4 None 22 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 323 3 1 2 4.5 Clc1ccc2[nH]c(C3=CCN(Cc4ccccc4)CC3)nc2c1 10.1016/S0960-894X(97)00402-2
44371980 53652 0 None 7 4 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 514 6 0 6 4.9 Cc1nn2c(N3CCN(Cc4ccccc4)CC3)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
CHEMBL160536 53652 0 None 7 4 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 514 6 0 6 4.9 Cc1nn2c(N3CCN(Cc4ccccc4)CC3)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
1353 1880 85 None -3 85 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.1c01327
3559 1880 85 None -3 85 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.1c01327
86 1880 85 None -3 85 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL54 1880 85 None -3 85 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.1c01327
DB00502 1880 85 None -3 85 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.1c01327
11220975 102519 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 322 4 1 4 2.9 COc1cccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)c1 10.1021/jm0305669
CHEMBL306711 102519 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 322 4 1 4 2.9 COc1cccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)c1 10.1021/jm0305669
5311346 202453 22 None -19 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 249 2 1 4 1.9 CCCN1CCO[C@@H]2c3cc(O)ccc3OC[C@H]21 10.1021/acs.jmedchem.9b00702
CHEMBL1256778 202453 22 None -19 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 249 2 1 4 1.9 CCCN1CCO[C@@H]2c3cc(O)ccc3OC[C@H]21 10.1021/acs.jmedchem.9b00702
CHEMBL70565 202453 22 None -19 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 249 2 1 4 1.9 CCCN1CCO[C@@H]2c3cc(O)ccc3OC[C@H]21 10.1021/acs.jmedchem.9b00702
10665101 101055 0 None 22 3 Human 7.6 pKi = 7.6 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 343 4 1 3 3.2 Cc1cccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)c1 10.1016/j.bmcl.2005.02.012
CHEMBL298166 101055 0 None 22 3 Human 7.6 pKi = 7.6 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 343 4 1 3 3.2 Cc1cccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)c1 10.1016/j.bmcl.2005.02.012
9883554 164802 0 None 141 2 Human 7.6 pKi = 7.6 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 320 4 1 4 2.1 N#Cc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL423659 164802 0 None 141 2 Human 7.6 pKi = 7.6 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 320 4 1 4 2.1 N#Cc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1016/j.bmcl.2005.02.012
10498972 117955 1 None 63 3 Human 7.6 pKi = 7.6 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 363 9 1 3 4.2 Cc1ccc(OCCNCCCOc2ccc(Br)cc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL341225 117955 1 None 63 3 Human 7.6 pKi = 7.6 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 363 9 1 3 4.2 Cc1ccc(OCCNCCCOc2ccc(Br)cc2)cc1 10.1016/j.bmcl.2005.02.012
44269825 42267 0 None -4 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 368 3 0 5 4.0 Cc1nc(Cl)c(Sc2ccc(Cl)cc2)c(N2CCN(C)CC2)n1 10.1016/s0960-894x(01)00167-6
CHEMBL14998 42267 0 None -4 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 368 3 0 5 4.0 Cc1nc(Cl)c(Sc2ccc(Cl)cc2)c(N2CCN(C)CC2)n1 10.1016/s0960-894x(01)00167-6
CHEMBL4434865 212175 1 None 23 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysis
ChEMBL None None None c1ccc(Cc2cn(C3CCN(Cc4ccccc4)CC3)nn2)cc1 10.1016/j.bmc.2022.116851
25141534 55942 0 None -1698 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 460 7 3 4 3.8 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1016/j.bmc.2015.01.017
CHEMBL1627305 55942 0 None -1698 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 460 7 3 4 3.8 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1016/j.bmc.2015.01.017
25141534 55942 0 None -1698 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in human HEK293 cell membrane for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in human HEK293 cell membrane for 1 hr by liquid scintillation counting analysis
ChEMBL 460 7 3 4 3.8 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/ml500006v
CHEMBL1627305 55942 0 None -1698 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in human HEK293 cell membrane for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in human HEK293 cell membrane for 1 hr by liquid scintillation counting analysis
ChEMBL 460 7 3 4 3.8 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/ml500006v
137637428 155695 0 None -3 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 250 1 1 5 0.9 CN1CCN(c2ccc(O)c3c2OCCO3)CC1 10.1016/j.bmc.2017.08.037
CHEMBL4064759 155695 0 None -3 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 250 1 1 5 0.9 CN1CCN(c2ccc(O)c3c2OCCO3)CC1 10.1016/j.bmc.2017.08.037
CHEMBL5076359 212661 0 None -77 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None COc1cccc(C(=CCNCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c2cccc(OC)c2)c1 10.1021/acs.jmedchem.1c00611
181743 177997 3 None -131 22 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptorDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2009.11.053
CHEMBL467094 177997 3 None -131 22 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptorDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2009.11.053
1605 2462 21 None -8511 9 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)CC(N(C)C)C 10.1021/acs.jmedchem.1c00611
1728 2462 21 None -8511 9 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)CC(N(C)C)C 10.1021/acs.jmedchem.1c00611
22267 2462 21 None -8511 9 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)CC(N(C)C)C 10.1021/acs.jmedchem.1c00611
4095 2462 21 None -8511 9 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)CC(N(C)C)C 10.1021/acs.jmedchem.1c00611
4586 2462 21 None -8511 9 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)CC(N(C)C)C 10.1021/acs.jmedchem.1c00611
5458 2462 21 None -8511 9 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)CC(N(C)C)C 10.1021/acs.jmedchem.1c00611
643985 2462 21 None -8511 9 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)CC(N(C)C)C 10.1021/acs.jmedchem.1c00611
CHEMBL159659 2462 21 None -8511 9 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)CC(N(C)C)C 10.1021/acs.jmedchem.1c00611
CHEMBL651 2462 21 None -8511 9 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)CC(N(C)C)C 10.1021/acs.jmedchem.1c00611
DB00333 2462 21 None -8511 9 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)CC(N(C)C)C 10.1021/acs.jmedchem.1c00611
DB13515 2462 21 None -8511 9 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)CC(N(C)C)C 10.1021/acs.jmedchem.1c00611
11488451 201460 0 None -12 3 Human 6.6 pKi = 6.6 Binding
Binding affinity for human dopamine receptor D4 using [125I]IABN as radioligandBinding affinity for human dopamine receptor D4 using [125I]IABN as radioligand
ChEMBL 478 8 1 6 3.3 COc1cc2c(cc1OC)CN(CCNC(=O)c1cc(Br)cc(OC)c1OC)CC2 10.1016/j.bmcl.2003.09.083
CHEMBL64176 201460 0 None -12 3 Human 6.6 pKi = 6.6 Binding
Binding affinity for human dopamine receptor D4 using [125I]IABN as radioligandBinding affinity for human dopamine receptor D4 using [125I]IABN as radioligand
ChEMBL 478 8 1 6 3.3 COc1cc2c(cc1OC)CN(CCNC(=O)c1cc(Br)cc(OC)c1OC)CC2 10.1016/j.bmcl.2003.09.083
10782097 113765 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 322 7 1 4 3.4 CCN(CCNCc1ccc2ccc(=O)oc2c1)c1ccccc1 10.1021/jm990266k
CHEMBL333057 113765 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 322 7 1 4 3.4 CCN(CCNCc1ccc2ccc(=O)oc2c1)c1ccccc1 10.1021/jm990266k
511484 4278 66 None -6 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 252 3 0 2 3.0 c1ccc(CN2CCN(c3ccccc3)CC2)cc1 10.1016/s0960-894x(98)00014-6
CHEMBL101032 4278 66 None -6 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 252 3 0 2 3.0 c1ccc(CN2CCN(c3ccccc3)CC2)cc1 10.1016/s0960-894x(98)00014-6
142590755 182844 0 None -3 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 496 11 2 4 5.4 OC(CNC1CCN(CCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1)Cc1ccccc1 10.1016/j.ejmech.2020.112674
CHEMBL4798638 182844 0 None -3 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 496 11 2 4 5.4 OC(CNC1CCN(CCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1)Cc1ccccc1 10.1016/j.ejmech.2020.112674
10058787 116094 0 None -407 3 Human 6.6 pKi = 6.6 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 205 3 2 2 2.2 CCCNC1CCc2ccc(O)cc2C1 10.1021/jm960345l
CHEMBL336652 116094 0 None -407 3 Human 6.6 pKi = 6.6 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 205 3 2 2 2.2 CCCNC1CCc2ccc(O)cc2C1 10.1021/jm960345l
122180611 121225 0 None -39 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 442 8 0 7 4.1 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc4ncccc4c3)nn2)CC1 10.1016/j.bmc.2015.01.017
CHEMBL3588982 121225 0 None -39 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 442 8 0 7 4.1 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc4ncccc4c3)nn2)CC1 10.1016/j.bmc.2015.01.017
134154680 154025 0 None -38 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 416 7 0 5 5.3 COc1cc2c(cc1OC)CN(CCCCc1nc3cc(Cl)ccc3s1)CC2 10.1016/j.bmc.2016.09.019
CHEMBL3959919 154025 0 None -38 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 416 7 0 5 5.3 COc1cc2c(cc1OC)CN(CCCCc1nc3cc(Cl)ccc3s1)CC2 10.1016/j.bmc.2016.09.019
CHEMBL3991166 154025 0 None -38 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 416 7 0 5 5.3 COc1cc2c(cc1OC)CN(CCCCc1nc3cc(Cl)ccc3s1)CC2 10.1016/j.bmc.2016.09.019
11613105 83654 0 None -39 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 506 12 1 8 3.4 COc1ccc(Cn2nnc(C(=O)NCCCCCN3CCN(c4ccccc4OC)CC3)c2C)cc1 10.1021/jm0611152
CHEMBL220754 83654 0 None -39 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 506 12 1 8 3.4 COc1ccc(Cn2nnc(C(=O)NCCCCCN3CCN(c4ccccc4OC)CC3)c2C)cc1 10.1021/jm0611152
44339992 108697 0 None 22 4 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL321492 108697 0 None 22 4 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
10665101 101055 0 None 22 3 Human 7.6 pKi = 7.6 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 343 4 1 3 3.2 Cc1cccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)c1 10.1021/jm970021c
CHEMBL298166 101055 0 None 22 3 Human 7.6 pKi = 7.6 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 343 4 1 3 3.2 Cc1cccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)c1 10.1021/jm970021c
9883554 164802 0 None 141 2 Human 7.6 pKi = 7.6 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 320 4 1 4 2.1 N#Cc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1021/jm970021c
CHEMBL423659 164802 0 None 141 2 Human 7.6 pKi = 7.6 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 320 4 1 4 2.1 N#Cc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1021/jm970021c
10498972 117955 1 None 63 3 Human 7.6 pKi = 7.6 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 363 9 1 3 4.2 Cc1ccc(OCCNCCCOc2ccc(Br)cc2)cc1 10.1021/jm970422s
CHEMBL341225 117955 1 None 63 3 Human 7.6 pKi = 7.6 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 363 9 1 3 4.2 Cc1ccc(OCCNCCCOc2ccc(Br)cc2)cc1 10.1021/jm970422s
44336313 9154 1 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 367 4 0 3 2.9 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccccc2F)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL110712 9154 1 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 367 4 0 3 2.9 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccccc2F)CC1 10.1016/s0960-894x(02)00656-x
9883552 15410 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 320 3 0 4 3.1 O=c1ccc2ccc(CN3CCN(c4ccccc4)CC3)cc2o1 10.1021/jm990266k
CHEMBL122140 15410 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 320 3 0 4 3.1 O=c1ccc2ccc(CN3CCN(c4ccccc4)CC3)cc2o1 10.1021/jm990266k
127031497 138961 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 351 5 0 3 4.3 Clc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3794469 138961 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 351 5 0 3 4.3 Clc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
145969667 164413 0 None -1 6 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 289 9 1 2 4.9 CCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4225278 164413 0 None -1 6 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 289 9 1 2 4.9 CCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
118709751 113042 0 None -20 10 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1ccccc1F 10.1016/j.bmcl.2014.07.018
CHEMBL3321792 113042 0 None -20 10 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1ccccc1F 10.1016/j.bmcl.2014.07.018
21219144 92908 0 None 40 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 319 4 0 5 3.2 c1ccc(CN2CCC(n3nnc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(99)00169-9
CHEMBL24539 92908 0 None 40 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 319 4 0 5 3.2 c1ccc(CN2CCC(n3nnc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(99)00169-9
10939167 9409 0 None -7 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 443 9 1 4 4.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm101639t
CHEMBL112065 9409 0 None -7 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 443 9 1 4 4.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm101639t
CHEMBL129483 9409 0 None -7 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 443 9 1 4 4.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm101639t
44332566 107873 0 None 8 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 276 6 2 3 3.1 Nc1cc(OCCNCc2ccccc2)ccc1Cl 10.1016/s0960-894x(98)00014-6
CHEMBL319816 107873 0 None 8 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 276 6 2 3 3.1 Nc1cc(OCCNCc2ccccc2)ccc1Cl 10.1016/s0960-894x(98)00014-6
56681927 66064 1 None -5 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 423 8 1 5 3.9 COc1cc(C)ccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1813593 66064 1 None -5 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 423 8 1 5 3.9 COc1cc(C)ccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1851787 66064 1 None -5 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 423 8 1 5 3.9 COc1cc(C)ccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1016/j.bmc.2011.04.021
11221906 79501 0 None 5 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 352 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(C)c(C)c1 10.1021/jm060279f
CHEMBL212444 79501 0 None 5 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 352 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(C)c(C)c1 10.1021/jm060279f
76328715 105891 0 None -2 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 429 9 2 6 2.8 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3115582 105891 0 None -2 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 429 9 2 6 2.8 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139265 105891 0 None -2 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 429 9 2 6 2.8 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
9841608 99957 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 355 4 1 3 3.3 O=C1NC(CCN2CCN(c3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/s0960-894x(98)00252-2
CHEMBL290351 99957 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 355 4 1 3 3.3 O=C1NC(CCN2CCN(c3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/s0960-894x(98)00252-2
10449136 205698 0 None 1 3 Human 6.6 pKi = 6.6 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 327 1 0 1 5.6 CC(C)=C1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00004a016
CHEMBL94067 205698 0 None 1 3 Human 6.6 pKi = 6.6 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 327 1 0 1 5.6 CC(C)=C1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00004a016
10449136 205698 0 None 1 3 Human 6.6 pKi = 6.6 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 327 1 0 1 5.6 CC(C)=C1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL94067 205698 0 None 1 3 Human 6.6 pKi = 6.6 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 327 1 0 1 5.6 CC(C)=C1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
137640836 156464 0 None -31 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 434 7 1 8 3.1 O=c1ccc2c(N3CCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2o1 10.1021/acs.jmedchem.7b00363
CHEMBL4073330 156464 0 None -31 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 434 7 1 8 3.1 O=c1ccc2c(N3CCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2o1 10.1021/acs.jmedchem.7b00363
17987129 110931 2 None - 1 Human 5.6 pKi = 5.6 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 323 5 2 2 3.2 O=C(NCc1ccccc1)NC1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL327339 110931 2 None - 1 Human 5.6 pKi = 5.6 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 323 5 2 2 3.2 O=C(NCc1ccccc1)NC1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
13014681 203022 0 None -891 3 Human 5.6 pKi = 5.6 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 323 1 0 1 5.1 CN1CCC(C2=Cc3cc(Cl)ccc3Cc3ccccc32)CC1 10.1021/jm00043a008
CHEMBL7430 203022 0 None -891 3 Human 5.6 pKi = 5.6 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 323 1 0 1 5.1 CN1CCC(C2=Cc3cc(Cl)ccc3Cc3ccccc32)CC1 10.1021/jm00043a008
44323876 204856 0 None -22 4 Human 5.6 pKi = 5.6 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 330 1 0 2 4.6 CC(C)=C1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL88870 204856 0 None -22 4 Human 5.6 pKi = 5.6 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 330 1 0 2 4.6 CC(C)=C1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
10568740 15381 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 4 0 4 3.1 O=c1ccc2ccc(CN3CCN(Cc4ccccc4)CC3)cc2o1 10.1021/jm990266k
CHEMBL121967 15381 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 4 0 4 3.1 O=c1ccc2ccc(CN3CCN(Cc4ccccc4)CC3)cc2o1 10.1021/jm990266k
15508239 6179 0 None 2 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 336 3 0 2 4.6 C[Si](C)(C)C#Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
CHEMBL108160 6179 0 None 2 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 336 3 0 2 4.6 C[Si](C)(C)C#Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
44582678 180992 0 None -18 10 Human 5.6 pKi = 5.6 Binding
Inhibition of human cloned dopamine D4 receptor by competitive binding experimentInhibition of human cloned dopamine D4 receptor by competitive binding experiment
ChEMBL 401 9 1 4 4.3 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL476839 180992 0 None -18 10 Human 5.6 pKi = 5.6 Binding
Inhibition of human cloned dopamine D4 receptor by competitive binding experimentInhibition of human cloned dopamine D4 receptor by competitive binding experiment
ChEMBL 401 9 1 4 4.3 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
17756101 98132 1 None -79 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)CCN(C)CCCc1ccccc1C2 10.1021/jm070388+
CHEMBL276778 98132 1 None -79 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)CCN(C)CCCc1ccccc1C2 10.1021/jm070388+
134154680 154025 0 None -38 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 416 7 0 5 5.3 COc1cc2c(cc1OC)CN(CCCCc1nc3cc(Cl)ccc3s1)CC2 10.1016/j.bmc.2016.09.019
CHEMBL3959919 154025 0 None -38 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 416 7 0 5 5.3 COc1cc2c(cc1OC)CN(CCCCc1nc3cc(Cl)ccc3s1)CC2 10.1016/j.bmc.2016.09.019
CHEMBL3991166 154025 0 None -38 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 416 7 0 5 5.3 COc1cc2c(cc1OC)CN(CCCCc1nc3cc(Cl)ccc3s1)CC2 10.1016/j.bmc.2016.09.019
9904074 110139 1 None -190 3 Human 6.6 pKi = 6.6 Binding
in vitro binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 289 5 1 4 3.5 CCCN(CCC)C1Cc2cc3nc(N)sc3cc2C1 10.1021/jm000087z
CHEMBL325710 110139 1 None -190 3 Human 6.6 pKi = 6.6 Binding
in vitro binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 289 5 1 4 3.5 CCCN(CCC)C1Cc2cc3nc(N)sc3cc2C1 10.1021/jm000087z
44330692 111875 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 202 0 1 2 2.8 Cc1oc(C)c2c1CCCc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
CHEMBL329503 111875 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 202 0 1 2 2.8 Cc1oc(C)c2c1CCCc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
10357631 7907 0 None -38 4 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human dopamine receptor D4 was determinedBinding affinity towards human dopamine receptor D4 was determined
ChEMBL 303 3 1 3 3.2 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)cn1 10.1016/j.bmcl.2005.02.012
CHEMBL109063 7907 0 None -38 4 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human dopamine receptor D4 was determinedBinding affinity towards human dopamine receptor D4 was determined
ChEMBL 303 3 1 3 3.2 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)cn1 10.1016/j.bmcl.2005.02.012
155557792 174113 0 None -69 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting
ChEMBL 419 9 1 5 4.0 COc1ccccc1OCCNCC1OCCOC1(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2019.02.056
CHEMBL4559278 174113 0 None -69 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting
ChEMBL 419 9 1 5 4.0 COc1ccccc1OCCNCC1OCCOC1(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2019.02.056
44438218 93016 0 None -2 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 338 3 1 1 5.4 CC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246020 93016 0 None -2 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 338 3 1 1 5.4 CC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
168296363 191919 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 371 5 0 4 4.0 Cn1ncc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
CHEMBL5209344 191919 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 371 5 0 4 4.0 Cn1ncc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
17756212 85941 1 None -36 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)Cc1ccccc1CCCN(C)CC2 10.1021/jm070388+
CHEMBL231374 85941 1 None -36 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)Cc1ccccc1CCCN(C)CC2 10.1021/jm070388+
7077 66625 24 None -10 5 Human 5.6 pKi = 5.6 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 10.1021/jm049720x
CHEMBL186720 66625 24 None -10 5 Human 5.6 pKi = 5.6 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 10.1021/jm049720x
CHEMBL3925724 66625 24 None -10 5 Human 5.6 pKi = 5.6 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 10.1021/jm049720x
15034333 4185 1 None -2 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 243 6 2 3 2.6 Oc1ccc(OCCNCc2ccccc2)cc1 10.1016/s0960-894x(98)00014-6
CHEMBL100461 4185 1 None -2 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 243 6 2 3 2.6 Oc1ccc(OCCNCc2ccccc2)cc1 10.1016/s0960-894x(98)00014-6
44591042 176237 0 None -15 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 380 4 2 2 4.9 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCc1c[nH]c2ccccc12 10.1016/j.bmc.2008.12.054
CHEMBL460854 176237 0 None -15 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 380 4 2 2 4.9 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCc1c[nH]c2ccccc12 10.1016/j.bmc.2008.12.054
10357631 7907 0 None -38 4 Human 6.6 pKi = 6.6 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 303 3 1 3 3.2 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)cn1 10.1021/jm950721m
CHEMBL109063 7907 0 None -38 4 Human 6.6 pKi = 6.6 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 303 3 1 3 3.2 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)cn1 10.1021/jm950721m
CHEMBL5087543 213333 0 None -46 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CN(C)C(=O)C(CCNCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
134153539 153968 0 None -6 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 390 5 0 3 6.0 Clc1ccc2sc(CCCCN3CCc4c(Cl)cccc4C3)nc2c1 10.1016/j.bmc.2016.09.019
CHEMBL3971383 153968 0 None -6 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 390 5 0 3 6.0 Clc1ccc2sc(CCCCN3CCc4c(Cl)cccc4C3)nc2c1 10.1016/j.bmc.2016.09.019
CHEMBL3990611 153968 0 None -6 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 390 5 0 3 6.0 Clc1ccc2sc(CCCCN3CCc4c(Cl)cccc4C3)nc2c1 10.1016/j.bmc.2016.09.019
10017758 13073 0 None -3 3 Human 7.6 pKi = 7.6 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 301 2 0 1 4.8 CCN1CC=C(C2=Cc3ccccc3Cc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL1190993 13073 0 None -3 3 Human 7.6 pKi = 7.6 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 301 2 0 1 4.8 CCN1CC=C(C2=Cc3ccccc3Cc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL542029 13073 0 None -3 3 Human 7.6 pKi = 7.6 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 301 2 0 1 4.8 CCN1CC=C(C2=Cc3ccccc3Cc3ccccc32)CC1 10.1021/jm00004a016
45482169 196161 0 None 1 4 Human 7.6 pKi = 7.6 Binding
Binding affinity to human cloned dopamine D4.4 expressed in CHO cellsBinding affinity to human cloned dopamine D4.4 expressed in CHO cells
ChEMBL 559 12 1 8 4.5 O=C(CCCc1cn(-c2ccc([N+](=O)[O-])cc2)nn1)NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmc.2009.06.041
CHEMBL572379 196161 0 None 1 4 Human 7.6 pKi = 7.6 Binding
Binding affinity to human cloned dopamine D4.4 expressed in CHO cellsBinding affinity to human cloned dopamine D4.4 expressed in CHO cells
ChEMBL 559 12 1 8 4.5 O=C(CCCc1cn(-c2ccc([N+](=O)[O-])cc2)nn1)NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmc.2009.06.041
135398745 2869 108 None -10 65 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm0002432
47 2869 108 None -10 65 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm0002432
CHEMBL715 2869 108 None -10 65 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm0002432
DB00334 2869 108 None -10 65 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm0002432
135398745 2869 108 None -10 65 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm030480f
47 2869 108 None -10 65 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm030480f
CHEMBL715 2869 108 None -10 65 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm030480f
DB00334 2869 108 None -10 65 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm030480f
155548336 173168 0 None 14 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 507 8 2 4 4.5 O=C(NCCN1CCN(c2ccc(Br)cc2)CC1)NN(Cc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
CHEMBL4536530 173168 0 None 14 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 507 8 2 4 4.5 O=C(NCCN1CCN(c2ccc(Br)cc2)CC1)NN(Cc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
127029391 138818 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 372 6 0 5 3.5 COc1cc(CN2CCO[C@H](COc3cccc(C#N)c3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3792907 138818 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 372 6 0 5 3.5 COc1cc(CN2CCO[C@H](COc3cccc(C#N)c3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
118709750 113041 0 None -2 9 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1cccc(F)c1 10.1016/j.bmcl.2014.07.018
CHEMBL3321791 113041 0 None -2 9 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1cccc(F)c1 10.1016/j.bmcl.2014.07.018
16105548 82286 0 None -75 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 462 9 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3cccc(F)n3)cc2)CC1 10.1021/jm0611152
CHEMBL217964 82286 0 None -75 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 462 9 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3cccc(F)n3)cc2)CC1 10.1021/jm0611152
CHEMBL221652 82286 0 None -75 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 462 9 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3cccc(F)n3)cc2)CC1 10.1021/jm0611152
10073194 12854 0 None -10 3 Human 7.6 pKi = 7.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 465 11 0 7 4.9 CCOc1ccccc1N1CCN(CCCCc2cc(-c3ccc(OC)c(OC)c3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL1189407 12854 0 None -10 3 Human 7.6 pKi = 7.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 465 11 0 7 4.9 CCOc1ccccc1N1CCN(CCCCc2cc(-c3ccc(OC)c(OC)c3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL538723 12854 0 None -10 3 Human 7.6 pKi = 7.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 465 11 0 7 4.9 CCOc1ccccc1N1CCN(CCCCc2cc(-c3ccc(OC)c(OC)c3)no2)CC1 10.1016/s0960-894x(02)00179-8
135398745 2869 108 None -10 65 Human 7.6 pKi = 7.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm401958n
47 2869 108 None -10 65 Human 7.6 pKi = 7.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm401958n
CHEMBL715 2869 108 None -10 65 Human 7.6 pKi = 7.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm401958n
DB00334 2869 108 None -10 65 Human 7.6 pKi = 7.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm401958n
118714552 114029 0 None 97 2 Human 7.6 pKi = 7.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 297 5 1 3 3.2 Oc1ccc(CN2CCO[C@H](CCc3ccccc3)C2)cc1 10.1021/ml500267c
CHEMBL3335555 114029 0 None 97 2 Human 7.6 pKi = 7.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 297 5 1 3 3.2 Oc1ccc(CN2CCO[C@H](CCc3ccccc3)C2)cc1 10.1021/ml500267c
10430935 105314 1 None 2 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 397 10 1 2 6.0 Fc1ccc(C(SCCNCCCc2ccccc2)c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.6b01373
CHEMBL3126735 105314 1 None 2 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 397 10 1 2 6.0 Fc1ccc(C(SCCNCCCc2ccccc2)c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.6b01373
155536720 171621 0 None 77 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 359 4 1 3 3.9 Cc1cccc(NC(=O)CN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4473652 171621 0 None 77 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 359 4 1 3 3.9 Cc1cccc(NC(=O)CN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/acs.jmedchem.9b00231
135398737 944 89 None -13 91 Human 7.6 pKi = 7.6 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.07.068
38 944 89 None -13 91 Human 7.6 pKi = 7.6 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.07.068
722 944 89 None -13 91 Human 7.6 pKi = 7.6 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.07.068
CHEMBL42 944 89 None -13 91 Human 7.6 pKi = 7.6 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.07.068
DB00363 944 89 None -13 91 Human 7.6 pKi = 7.6 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.07.068
57399432 70121 0 None 2 8 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 399 6 0 4 5.5 Clc1ccc(N2CCCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2012.01.022
CHEMBL1946254 70121 0 None 2 8 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 399 6 0 4 5.5 Clc1ccc(N2CCCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2012.01.022
57399432 70121 0 None 2 8 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 399 6 0 4 5.5 Clc1ccc(N2CCCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.ejmech.2012.03.042
CHEMBL1946254 70121 0 None 2 8 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 399 6 0 4 5.5 Clc1ccc(N2CCCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.ejmech.2012.03.042
137635734 155571 0 None 61 8 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 377 7 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(CCc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4063176 155571 0 None 61 8 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 377 7 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(CCc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
44336552 110852 0 None 18 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 316 4 0 4 3.8 N#CC(C#N)=Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
CHEMBL326864 110852 0 None 18 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 316 4 0 4 3.8 N#CC(C#N)=Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
10573099 206093 0 None -6 2 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 400 9 0 4 4.9 COc1cccc(C(=O)CCCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
CHEMBL96322 206093 0 None -6 2 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 400 9 0 4 4.9 COc1cccc(C(=O)CCCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
164628883 185869 0 None -14 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 427 6 2 5 3.8 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1ccc(C#N)cc1)CC2 10.1016/j.bmcl.2021.128047
CHEMBL4876546 185869 0 None -14 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 427 6 2 5 3.8 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1ccc(C#N)cc1)CC2 10.1016/j.bmcl.2021.128047
11652518 165379 0 None 16 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 311 3 0 5 2.2 Fc1ccc(N2CCN(Cc3cn4cccnc4n3)CC2)cc1 10.1021/jm060166w
CHEMBL425064 165379 0 None 16 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 311 3 0 5 2.2 Fc1ccc(N2CCN(Cc3cn4cccnc4n3)CC2)cc1 10.1021/jm060166w
16277250 110003 5 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 CC(C(=O)N1CCc2ccccc21)N1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL324867 110003 5 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 CC(C(=O)N1CCc2ccccc21)N1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
44426510 85317 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 386 7 1 2 5.1 O=C(NC1CCN(CCCCc2ccccc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.096
CHEMBL229025 85317 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 386 7 1 2 5.1 O=C(NC1CCN(CCCCc2ccccc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.096
134153539 153968 0 None -6 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 390 5 0 3 6.0 Clc1ccc2sc(CCCCN3CCc4c(Cl)cccc4C3)nc2c1 10.1016/j.bmc.2016.09.019
CHEMBL3971383 153968 0 None -6 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 390 5 0 3 6.0 Clc1ccc2sc(CCCCN3CCc4c(Cl)cccc4C3)nc2c1 10.1016/j.bmc.2016.09.019
CHEMBL3990611 153968 0 None -6 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 390 5 0 3 6.0 Clc1ccc2sc(CCCCN3CCc4c(Cl)cccc4C3)nc2c1 10.1016/j.bmc.2016.09.019
11384207 82939 0 None -165 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 405 7 1 3 4.3 O=C(NCCCCN1CCN(c2ccccc2Cl)CC1)c1ccc(Cl)cc1 10.1021/jm0611152
CHEMBL219274 82939 0 None -165 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 405 7 1 3 4.3 O=C(NCCCCN1CCN(c2ccccc2Cl)CC1)c1ccc(Cl)cc1 10.1021/jm0611152
11569619 136040 0 None -66 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 500 9 1 6 4.3 Cc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)nnn1Cc1ccccc1 10.1021/jm0611152
CHEMBL373873 136040 0 None -66 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 500 9 1 6 4.3 Cc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)nnn1Cc1ccccc1 10.1021/jm0611152
11670421 168230 0 None -10 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 492 11 1 8 3.0 COc1ccc(Cn2nnc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)c2C)cc1 10.1021/jm0611152
CHEMBL437525 168230 0 None -10 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 492 11 1 8 3.0 COc1ccc(Cn2nnc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)c2C)cc1 10.1021/jm0611152
90644072 111547 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 340 4 0 3 4.5 Clc1ccc(N2CCN(CCc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289652 111547 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 340 4 0 3 4.5 Clc1ccc(N2CCN(CCc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
44438186 146675 3 None -7 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 340 3 2 2 4.3 OC1(c2ccccc2Cl)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL392822 146675 3 None -7 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 340 3 2 2 4.3 OC1(c2ccccc2Cl)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
11016342 102331 0 None -281 4 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 481 8 1 3 6.0 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccc2)cc1 10.1021/jm020952a
CHEMBL305362 102331 0 None -281 4 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 481 8 1 3 6.0 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccc2)cc1 10.1021/jm020952a
76311262 105812 0 None -660 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 468 11 2 5 3.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(OCCF)ccc3[nH]2)CC1 10.1039/c3md00098b
CHEMBL3133779 105812 0 None -660 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 468 11 2 5 3.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(OCCF)ccc3[nH]2)CC1 10.1039/c3md00098b
CHEMBL3139053 105812 0 None -660 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 468 11 2 5 3.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(OCCF)ccc3[nH]2)CC1 10.1039/c3md00098b
71061724 145019 0 None -2 5 Mouse 5.5 pKi = 5.5 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 386 5 0 4 3.0 O=C(CN1CCO[C@H](COc2cccc(Cl)c2)C1)N1CCc2ccccc21 nan
CHEMBL3915107 145019 0 None -2 5 Mouse 5.5 pKi = 5.5 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 386 5 0 4 3.0 O=C(CN1CCO[C@H](COc2cccc(Cl)c2)C1)N1CCc2ccccc21 nan
56664950 66292 1 None -11 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 439 9 1 6 3.6 COc1ccc(N2CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)c(OC)c1 10.1016/j.bmc.2011.04.021
CHEMBL1813592 66292 1 None -11 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 439 9 1 6 3.6 COc1ccc(N2CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)c(OC)c1 10.1016/j.bmc.2011.04.021
CHEMBL1852737 66292 1 None -11 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 439 9 1 6 3.6 COc1ccc(N2CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)c(OC)c1 10.1016/j.bmc.2011.04.021
155195311 173775 0 None -208 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1C[C@H]1C[C@@H]1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
CHEMBL4551160 173775 0 None -208 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1C[C@H]1C[C@@H]1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
44330554 206481 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 218 0 0 3 2.9 Cc1sc(C)c2c1CCc1cn(C)nc1-2 10.1016/s0960-894x(03)00587-0
CHEMBL98578 206481 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 218 0 0 3 2.9 Cc1sc(C)c2c1CCc1cn(C)nc1-2 10.1016/s0960-894x(03)00587-0
17756102 85717 0 None -123 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 309 1 0 2 4.1 COc1ccc2c(c1)CCCN(C)CCCc1ccccc1C2 10.1021/jm070388+
CHEMBL231171 85717 0 None -123 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 309 1 0 2 4.1 COc1ccc2c(c1)CCCN(C)CCCc1ccccc1C2 10.1021/jm070388+
11512263 83949 0 None -89 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 544 11 1 7 4.7 COc1ccc(Cn2nnc(C(=O)NCCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c2C)cc1 10.1021/jm0611152
CHEMBL221866 83949 0 None -89 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 544 11 1 7 4.7 COc1ccc(Cn2nnc(C(=O)NCCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c2C)cc1 10.1021/jm0611152
154726529 175871 1 None -26 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 459 12 1 3 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4467486 175871 1 None -26 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 459 12 1 3 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4596338 175871 1 None -26 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 459 12 1 3 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
10469437 56247 1 None -1 3 Human 7.5 pKi = 7.5 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 289 1 0 2 4.6 CN1CC=C(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL163863 56247 1 None -1 3 Human 7.5 pKi = 7.5 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 289 1 0 2 4.6 CN1CC=C(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
135398737 944 89 None -7 91 Rat 7.5 pKi = 7.5 Binding
Binding affinity of [3H]YM-09151 towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]YM-09151 towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
38 944 89 None -7 91 Rat 7.5 pKi = 7.5 Binding
Binding affinity of [3H]YM-09151 towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]YM-09151 towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
722 944 89 None -7 91 Rat 7.5 pKi = 7.5 Binding
Binding affinity of [3H]YM-09151 towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]YM-09151 towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
CHEMBL42 944 89 None -7 91 Rat 7.5 pKi = 7.5 Binding
Binding affinity of [3H]YM-09151 towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]YM-09151 towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
DB00363 944 89 None -7 91 Rat 7.5 pKi = 7.5 Binding
Binding affinity of [3H]YM-09151 towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]YM-09151 towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
30740059 107182 1 None 2 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 409 6 0 5 2.8 COc1ccc(OC)c(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)c1 10.1016/s0960-894x(02)00656-x
CHEMBL319043 107182 1 None 2 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 409 6 0 5 2.8 COc1ccc(OC)c(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)c1 10.1016/s0960-894x(02)00656-x
135398745 2869 108 None -10 65 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm960268u
47 2869 108 None -10 65 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm960268u
CHEMBL715 2869 108 None -10 65 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm960268u
DB00334 2869 108 None -10 65 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm960268u
44335813 5287 0 None 28 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 382 4 0 2 4.9 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccccc2Cl)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL106914 5287 0 None 28 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 382 4 0 2 4.9 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccccc2Cl)CC1 10.1016/s0960-894x(02)00655-8
127030612 138800 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 352 5 0 4 3.7 Clc1ccc(CN2CCO[C@H](COc3cccc(Cl)n3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792725 138800 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 352 5 0 4 3.7 Clc1ccc(CN2CCO[C@H](COc3cccc(Cl)n3)C2)cc1 10.1016/j.bmcl.2016.03.102
10115074 120162 0 None 7 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 453 4 0 4 4.1 COc1ccc(Cl)cc1CN1CCN(C2CCc3cccc4c3N(C2=O)C(C)(C)C4)CC1 10.1016/s0960-894x(02)01056-9
CHEMBL354699 120162 0 None 7 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 453 4 0 4 4.1 COc1ccc(Cl)cc1CN1CCN(C2CCc3cccc4c3N(C2=O)C(C)(C)C4)CC1 10.1016/s0960-894x(02)01056-9
25070416 111293 0 None -4 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1c(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)nn2ccccc12 10.1021/jm5004039
CHEMBL3287401 111293 0 None -4 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1c(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)nn2ccccc12 10.1021/jm5004039
44426508 85315 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.8 CC(c1ccccc1)N1CCC(NC(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2006.12.096
CHEMBL229023 85315 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.8 CC(c1ccccc1)N1CCC(NC(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2006.12.096
118709174 112923 0 None -10 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 946 23 0 10 9.6 CN(CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)CCN(C)CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318847 112923 0 None -10 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 946 23 0 10 9.6 CN(CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)CCN(C)CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
10641637 118275 0 None 19 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]cc(CN3CCN(c4ccc(Cl)cc4)CC3)c2c1 10.1021/jm0009989
CHEMBL342001 118275 0 None 19 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]cc(CN3CCN(c4ccc(Cl)cc4)CC3)c2c1 10.1021/jm0009989
11290928 5234 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 345 6 0 3 4.2 COc1ccccc1CCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL106665 5234 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 345 6 0 3 4.2 COc1ccccc1CCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
44372198 48875 0 None 199 4 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 420 4 0 4 5.1 Fc1ccc(-c2cccc3c(CN4CCN(c5ccc(Cl)cc5)CC4)cnn23)cc1 10.1016/s0960-894x(01)00814-9
CHEMBL156198 48875 0 None 199 4 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 420 4 0 4 5.1 Fc1ccc(-c2cccc3c(CN4CCN(c5ccc(Cl)cc5)CC4)cnn23)cc1 10.1016/s0960-894x(01)00814-9
162671033 183173 0 None 3 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2cccnc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL4793296 183173 0 None 3 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2cccnc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL4803797 183173 0 None 3 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2cccnc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
44264622 96695 5 None 22 4 Human 6.5 pKi = 6.5 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 327 3 0 5 2.7 Clc1ccc(N2CCN(Cc3cnc4ncccn34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL267853 96695 5 None 22 4 Human 6.5 pKi = 6.5 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 327 3 0 5 2.7 Clc1ccc(N2CCN(Cc3cnc4ncccn34)CC2)cc1 10.1016/s0960-894x(98)00692-1
122177644 120699 0 None -239 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 591 18 2 8 5.6 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)[C@@H]3CCc4c(O)cccc4C3)cc2OC)nn1 10.1021/jm501889t
CHEMBL3577345 120699 0 None -239 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 591 18 2 8 5.6 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)[C@@H]3CCc4c(O)cccc4C3)cc2OC)nn1 10.1021/jm501889t
44335569 5090 0 None - 1 Human 6.5 pKi = 6.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 395 7 0 4 4.7 CCOc1ccccc1OCC1CN(Cc2ccc(Cl)cc2Cl)CCO1 10.1021/jm031111m
CHEMBL105894 5090 0 None - 1 Human 6.5 pKi = 6.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 395 7 0 4 4.7 CCOc1ccccc1OCC1CN(Cc2ccc(Cl)cc2Cl)CCO1 10.1021/jm031111m
44319370 106564 0 None 1 4 Human 6.5 pKi = 6.5 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 443 5 0 5 3.8 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)[C@@H](C)O1 10.1016/s0960-894x(01)00484-x
CHEMBL315564 106564 0 None 1 4 Human 6.5 pKi = 6.5 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 443 5 0 5 3.8 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)[C@@H](C)O1 10.1016/s0960-894x(01)00484-x
13014680 97993 1 None -407 4 Human 5.5 pKi = 5.5 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 324 1 0 2 4.0 CN1CCN(C2=Cc3cc(Cl)ccc3Cc3ccccc32)CC1 10.1021/jm00043a008
CHEMBL275696 97993 1 None -407 4 Human 5.5 pKi = 5.5 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 324 1 0 2 4.0 CN1CCN(C2=Cc3cc(Cl)ccc3Cc3ccccc32)CC1 10.1021/jm00043a008
1499 2060 43 None -18 17 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2016.04.028
3779 2060 43 None -18 17 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2016.04.028
536 2060 43 None -18 17 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2016.04.028
CHEMBL434 2060 43 None -18 17 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2016.04.028
DB01064 2060 43 None -18 17 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2016.04.028
71462266 81419 0 None -34 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 433 6 0 3 5.7 O=C(c1ccc2ccccc2c1)N(CCN1CC=C(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL2164355 81419 0 None -34 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 433 6 0 3 5.7 O=C(c1ccc2ccccc2c1)N(CCN1CC=C(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
154706513 176012 1 None -4 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 480 12 0 6 5.6 COc1ccc(F)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1 10.1021/acs.jmedchem.9b01835
CHEMBL4440698 176012 1 None -4 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 480 12 0 6 5.6 COc1ccc(F)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1 10.1021/acs.jmedchem.9b01835
CHEMBL4597532 176012 1 None -4 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 480 12 0 6 5.6 COc1ccc(F)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1 10.1021/acs.jmedchem.9b01835
10803829 11500 1 None -288 5 Human 6.5 pKi = 6.5 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 295 2 1 3 3.1 Oc1ccc2c(c1)O[C@H](CN1CCc3ccccc3C1)CC2 10.1021/jm9703653
CHEMBL1180636 11500 1 None -288 5 Human 6.5 pKi = 6.5 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 295 2 1 3 3.1 Oc1ccc2c(c1)O[C@H](CN1CCc3ccccc3C1)CC2 10.1021/jm9703653
CHEMBL135725 11500 1 None -288 5 Human 6.5 pKi = 6.5 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 295 2 1 3 3.1 Oc1ccc2c(c1)O[C@H](CN1CCc3ccccc3C1)CC2 10.1021/jm9703653
57587922 170946 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 235 3 1 4 1.8 CCCN1CC(c2ccc(N)nc2)OC[C@@H]1C 10.1021/acs.jmedchem.9b00702
CHEMBL4464060 170946 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 235 3 1 4 1.8 CCCN1CC(c2ccc(N)nc2)OC[C@@H]1C 10.1021/acs.jmedchem.9b00702
CHEMBL5077114 212711 0 None -2137 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCOC(=O)/C=C1\[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2C[C@H]1C[C@@H]1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.1c00611
155195486 169120 0 None -14 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1C[C@@H]1C[C@H]1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
CHEMBL4437740 169120 0 None -14 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1C[C@@H]1C[C@H]1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
16094677 82923 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 325 4 1 3 2.4 Cc1cccc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
CHEMBL219185 82923 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 325 4 1 3 2.4 Cc1cccc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
9929629 101646 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 377 4 0 3 3.5 CCN1C(=O)C(N2CCN(Cc3ccc(C)cc3)CC2)CCc2ccccc21 10.1016/s0960-894x(00)00421-2
CHEMBL302340 101646 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 377 4 0 3 3.5 CCN1C(=O)C(N2CCN(Cc3ccc(C)cc3)CC2)CCc2ccccc21 10.1016/s0960-894x(00)00421-2
44332581 4315 0 None -6 4 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 243 6 2 3 2.6 Oc1ccccc1OCCNCc1ccccc1 10.1016/s0960-894x(98)00014-6
CHEMBL101285 4315 0 None -6 4 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 243 6 2 3 2.6 Oc1ccccc1OCCNCc1ccccc1 10.1016/s0960-894x(98)00014-6
71658075 89970 0 None -194 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 437 8 1 5 4.6 COc1ccccc1N1CCCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386614 89970 0 None -194 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 437 8 1 5 4.6 COc1ccccc1N1CCCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1016/j.bmc.2013.03.074
109030343 170293 1 None 15 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 324 5 1 4 2.5 Cc1cccc(NC(=O)CCN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4454068 170293 1 None 15 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 324 5 1 4 2.5 Cc1cccc(NC(=O)CCN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
122180568 121206 0 None -102 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 441 8 0 6 4.6 COc1ccccc1N1CCN(CCCCc2cn(-c3ccc4ccccc4c3)nn2)CC1 10.1016/j.bmc.2015.01.017
CHEMBL3588913 121206 0 None -102 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 441 8 0 6 4.6 COc1ccccc1N1CCN(CCCCc2cn(-c3ccc4ccccc4c3)nn2)CC1 10.1016/j.bmc.2015.01.017
44431492 87848 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 345 4 1 3 3.6 O=C(NC1CCN(Cc2ccccn2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
CHEMBL234827 87848 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 345 4 1 3 3.6 O=C(NC1CCN(Cc2ccccn2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
11637457 72740 1 None -8 5 Human 6.5 pKi = 6.5 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2ccsc2CC1 10.1021/jm050846j
CHEMBL201093 72740 1 None -8 5 Human 6.5 pKi = 6.5 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2ccsc2CC1 10.1021/jm050846j
163322331 191617 3 None 8 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 408 6 1 3 4.5 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(F)c(F)c2)CC1 10.1016/j.bmcl.2022.128615
CHEMBL5204764 191617 3 None 8 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 408 6 1 3 4.5 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(F)c(F)c2)CC1 10.1016/j.bmcl.2022.128615
44438230 93124 3 None -194 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 354 3 2 2 4.6 Cc1[nH]c2ccccc2c1CN1CCC(O)(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246439 93124 3 None -194 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 354 3 2 2 4.6 Cc1[nH]c2ccccc2c1CN1CCC(O)(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2006.10.076
10021193 66031 0 None 199 2 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 356 5 1 2 4.4 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL185156 66031 0 None 199 2 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 356 5 1 2 4.4 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2004.07.045
44214766 66730 0 None 275 2 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL187236 66730 0 None 275 2 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2004.07.045
11559589 122192 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@H]1CCN(Cc2ccccc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL360424 122192 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@H]1CCN(Cc2ccccc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2004.07.045
72901200 119272 21 None 154 4 Human 8.5 pKi = 8.5 Binding
Affinity Biochemical interaction (Radioligand binding assay) EUB0000539a DRD4Affinity Biochemical interaction (Radioligand binding assay) EUB0000539a DRD4
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 nan
CHEMBL3480577 119272 21 None 154 4 Human 8.5 pKi = 8.5 Binding
Affinity Biochemical interaction (Radioligand binding assay) EUB0000539a DRD4Affinity Biochemical interaction (Radioligand binding assay) EUB0000539a DRD4
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 nan
9995379 106467 0 None 1 4 Human 8.5 pKi = 8.5 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 307 3 1 3 2.5 O=C1Cc2c(cccc2N2CCN(Cc3ccccc3)CC2)N1 10.1016/s0960-894x(98)00474-0
CHEMBL314952 106467 0 None 1 4 Human 8.5 pKi = 8.5 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 307 3 1 3 2.5 O=C1Cc2c(cccc2N2CCN(Cc3ccccc3)CC2)N1 10.1016/s0960-894x(98)00474-0
135887940 11230 0 None 93 2 Human 8.5 pKi = 8.5 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 380 6 1 6 2.9 COc1ccccc1N1CCN(CCCNC2=Nc3ccccc3OC2)CC1 10.1016/S0960-894X(97)00442-3
CHEMBL1179506 11230 0 None 93 2 Human 8.5 pKi = 8.5 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 380 6 1 6 2.9 COc1ccccc1N1CCN(CCCNC2=Nc3ccccc3OC2)CC1 10.1016/S0960-894X(97)00442-3
CHEMBL80711 11230 0 None 93 2 Human 8.5 pKi = 8.5 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 380 6 1 6 2.9 COc1ccccc1N1CCN(CCCNC2=Nc3ccccc3OC2)CC1 10.1016/S0960-894X(97)00442-3
44264642 203095 0 None 75 4 Human 8.5 pKi = 8.5 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccccc1N1CCN(Cc2cnn3ccccc23)CC1 10.1016/s0960-894x(98)00692-1
CHEMBL7506 203095 0 None 75 4 Human 8.5 pKi = 8.5 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccccc1N1CCN(Cc2cnn3ccccc23)CC1 10.1016/s0960-894x(98)00692-1
10454684 203097 0 None 467 4 Human 8.5 pKi = 8.5 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 418 3 0 4 3.3 Ic1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL7508 203097 0 None 467 4 Human 8.5 pKi = 8.5 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 418 3 0 4 3.3 Ic1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
9909648 203861 1 None -1 12 Rat 8.5 pKi = 8.5 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 340 4 0 3 3.7 Fc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/jm960084f
CHEMBL81330 203861 1 None -1 12 Rat 8.5 pKi = 8.5 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 340 4 0 3 3.7 Fc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/jm960084f
9995379 106467 0 None 1 4 Human 8.5 pKi = 8.5 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 307 3 1 3 2.5 O=C1Cc2c(cccc2N2CCN(Cc3ccccc3)CC2)N1 10.1007/s00044-012-0055-5
CHEMBL314952 106467 0 None 1 4 Human 8.5 pKi = 8.5 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 307 3 1 3 2.5 O=C1Cc2c(cccc2N2CCN(Cc3ccccc3)CC2)N1 10.1007/s00044-012-0055-5
10836365 205532 0 None 5 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 429 7 2 4 3.9 COc1cc(NC(=O)C(C)C)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
CHEMBL93021 205532 0 None 5 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 429 7 2 4 3.9 COc1cc(NC(=O)C(C)C)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
231915 91726 7 None 14 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 296 5 0 3 3.4 CCOc1ccccc1N1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2013.07.033
CHEMBL2420892 91726 7 None 14 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 296 5 0 3 3.4 CCOc1ccccc1N1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2013.07.033
10220333 4143 0 None 36 2 Human 8.5 pKi = 8.5 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 236 0 0 4 3.4 Cc1sc(C)c2c1SCc1cnn(C)c1-2 10.1016/s0960-894x(03)00587-0
CHEMBL100203 4143 0 None 36 2 Human 8.5 pKi = 8.5 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 236 0 0 4 3.4 Cc1sc(C)c2c1SCc1cnn(C)c1-2 10.1016/s0960-894x(03)00587-0
44336030 5140 0 None 251 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 377 5 0 3 3.3 CCc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1016/s0960-894x(02)00656-x
CHEMBL106169 5140 0 None 251 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 377 5 0 3 3.3 CCc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1016/s0960-894x(02)00656-x
10001810 5269 0 None 91 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 413 5 0 4 3.4 COc1cc(Cl)ccc1CN1CCN(CC(=O)N2c3ccccc3C[C@H]2C)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL106862 5269 0 None 91 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 413 5 0 4 3.4 COc1cc(Cl)ccc1CN1CCN(CC(=O)N2c3ccccc3C[C@H]2C)CC1 10.1016/s0960-894x(02)00656-x
44335919 108441 0 None 31 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 377 5 0 3 3.5 CC[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(C)cc2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL321121 108441 0 None 31 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 377 5 0 3 3.5 CC[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(C)cc2)CC1 10.1016/s0960-894x(02)00656-x
1946142 109133 2 None 478 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 393 4 0 5 2.5 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL322222 109133 2 None 478 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 393 4 0 5 2.5 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/s0960-894x(02)00656-x
44335739 4778 0 None 7 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 380 4 0 2 4.7 Cc1ccc(CN2CCC(CC(=O)N3c4ccccc4CC3C)CC2)cc1F 10.1016/s0960-894x(02)00655-8
CHEMBL104273 4778 0 None 7 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 380 4 0 2 4.7 Cc1ccc(CN2CCC(CC(=O)N3c4ccccc4CC3C)CC2)cc1F 10.1016/s0960-894x(02)00655-8
9799123 5543 0 None 35 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
CHEMBL107742 5543 0 None 35 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
44336006 6174 0 None 398 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 387 5 0 5 3.5 O=c1sc2ccccc2n1CCN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL108157 6174 0 None 398 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 387 5 0 5 3.5 O=c1sc2ccccc2n1CCN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
54581963 61272 0 None -11 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 437 8 0 5 3.7 COc1ccc2c(c1)CCCN(CCCCN1CCN(c3ccccc3OC)CC1)C2=O 10.1016/j.bmcl.2010.12.083
CHEMBL1771105 61272 0 None -11 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 437 8 0 5 3.7 COc1ccc2c(c1)CCCN(CCCCN1CCN(c3ccccc3OC)CC1)C2=O 10.1016/j.bmcl.2010.12.083
11559589 122192 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@H]1CCN(Cc2ccccc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
CHEMBL360424 122192 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@H]1CCN(Cc2ccccc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
135921193 39954 0 None 93 2 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.
ChEMBL 366 5 1 6 2.5 COc1ccccc1N1CCN(CCNC2=Nc3ccccc3OC2)CC1 10.1021/jm981041x
CHEMBL148024 39954 0 None 93 2 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.
ChEMBL 366 5 1 6 2.5 COc1ccccc1N1CCN(CCNC2=Nc3ccccc3OC2)CC1 10.1021/jm981041x
9909648 203861 1 None 1 12 Human 8.5 pKi = 8.5 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 340 4 0 3 3.7 Fc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.7b00151
CHEMBL81330 203861 1 None 1 12 Human 8.5 pKi = 8.5 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 340 4 0 3 3.7 Fc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.7b00151
10684706 85295 0 None 75 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 287 9 2 4 2.8 Oc1ccc(OCCNCCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL22892 85295 0 None 75 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 287 9 2 4 2.8 Oc1ccc(OCCNCCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
10617366 203731 0 None 28 3 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 343 5 1 2 4.7 Cc1c(-c2ccccc2)n[nH]c1C1=CCN(CCc2ccccc2)CC1 10.1021/jm970111h
CHEMBL80318 203731 0 None 28 3 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 343 5 1 2 4.7 Cc1c(-c2ccccc2)n[nH]c1C1=CCN(CCc2ccccc2)CC1 10.1021/jm970111h
10404144 203591 19 None 1 10 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(02)00316-5
CHEMBL7927 203591 19 None 1 10 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(02)00316-5
10980338 167445 0 None 1584 4 Human 8.5 pKi = 8.5 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3ccc4ccnn4c3)CC2)cc1 10.1021/jm015522j
CHEMBL432059 167445 0 None 1584 4 Human 8.5 pKi = 8.5 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3ccc4ccnn4c3)CC2)cc1 10.1021/jm015522j
10336538 1595 44 None -3 8 Human 8.5 pKi = 8.5 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1016/j.bmcl.2013.07.033
974 1595 44 None -3 8 Human 8.5 pKi = 8.5 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1016/j.bmcl.2013.07.033
CHEMBL310843 1595 44 None -3 8 Human 8.5 pKi = 8.5 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1016/j.bmcl.2013.07.033
10684706 85295 0 None 75 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 287 9 2 4 2.8 Oc1ccc(OCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
CHEMBL22892 85295 0 None 75 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 287 9 2 4 2.8 Oc1ccc(OCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
11003833 44510 0 None -1 4 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 397 9 1 5 3.0 COc1cccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm020952a
CHEMBL152159 44510 0 None -1 4 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 397 9 1 5 3.0 COc1cccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm020952a
10404144 203591 19 None -1 10 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL7927 203591 19 None -1 10 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/j.bmc.2014.04.026
21219164 91119 0 None 120 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 365 4 0 3 5.3 Cc1c(-c2ccccc2)cnn1C1CCN(Cc2cccc(Cl)c2)CC1 10.1016/s0960-894x(99)00169-9
CHEMBL24051 91119 0 None 120 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 365 4 0 3 5.3 Cc1c(-c2ccccc2)cnn1C1CCN(Cc2cccc(Cl)c2)CC1 10.1016/s0960-894x(99)00169-9
12052258 99632 0 None 4 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 365 4 0 3 5.3 Cc1nn(C2CCN(Cc3cccc(Cl)c3)CC2)cc1-c1ccccc1 10.1016/s0960-894x(99)00169-9
CHEMBL287412 99632 0 None 4 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 365 4 0 3 5.3 Cc1nn(C2CCN(Cc3cccc(Cl)c3)CC2)cc1-c1ccccc1 10.1016/s0960-894x(99)00169-9
10404144 203591 19 None 1 10 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(01)00814-9
CHEMBL7927 203591 19 None 1 10 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(01)00814-9
9840672 204594 0 None -5 4 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 335 6 2 3 3.8 FC(F)(F)c1nc2c(OCCNCc3ccccc3)cccc2[nH]1 10.1016/s0960-894x(99)00434-5
CHEMBL87192 204594 0 None -5 4 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 335 6 2 3 3.8 FC(F)(F)c1nc2c(OCCNCc3ccccc3)cccc2[nH]1 10.1016/s0960-894x(99)00434-5
2780 110040 32 None -4 11 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(03)00678-4
CHEMBL325109 110040 32 None -4 11 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(03)00678-4
44412458 138764 3 None 28 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 316 4 0 4 3.6 C1=C(c2ccccc2)CCN(Cc2cn(-c3ccccc3)nn2)C1 10.1016/j.bmcl.2006.02.075
CHEMBL379177 138764 3 None 28 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 316 4 0 4 3.6 C1=C(c2ccccc2)CCN(Cc2cn(-c3ccccc3)nn2)C1 10.1016/j.bmcl.2006.02.075
9821010 55167 0 None 575 2 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 375 4 0 4 3.9 Fc1ccc(OC[C@@H]2CC[C@H]3CN(c4ccc(Cl)cn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL161982 55167 0 None 575 2 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 375 4 0 4 3.9 Fc1ccc(OC[C@@H]2CC[C@H]3CN(c4ccc(Cl)cn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
44419066 83944 0 None 28 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 318 4 0 4 3.6 c1ccc(C2CCN(Cc3cn(-c4ccccc4)nn3)CC2)cc1 10.1021/jm0611152
CHEMBL221814 83944 0 None 28 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 318 4 0 4 3.6 c1ccc(C2CCN(Cc3cn(-c4ccccc4)nn3)CC2)cc1 10.1021/jm0611152
44340227 110152 0 None 16 4 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 486 5 1 3 4.5 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(I)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL325772 110152 0 None 16 4 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 486 5 1 3 4.5 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(I)c2ccccc12 10.1016/s0960-894x(03)00678-4
10574818 206164 0 None 1 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 433 7 2 4 4.1 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(CC2CCCCC2)C1 10.1021/jm9601720
CHEMBL96703 206164 0 None 1 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 433 7 2 4 4.1 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(CC2CCCCC2)C1 10.1021/jm9601720
1353 1880 85 None -3 85 Human 8.5 pKi = 8.5 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.06.030
3559 1880 85 None -3 85 Human 8.5 pKi = 8.5 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.06.030
86 1880 85 None -3 85 Human 8.5 pKi = 8.5 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.06.030
CHEMBL54 1880 85 None -3 85 Human 8.5 pKi = 8.5 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.06.030
DB00502 1880 85 None -3 85 Human 8.5 pKi = 8.5 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.06.030
9948461 19301 1 None 5 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 269 9 1 2 3.7 c1ccc(CCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
CHEMBL129931 19301 1 None 5 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 269 9 1 2 3.7 c1ccc(CCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
155532505 171192 0 None 9 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 569 10 2 5 5.0 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2F)c2ccc(Br)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4467437 171192 0 None 9 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 569 10 2 5 5.0 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2F)c2ccc(Br)cc2)CC1 10.1021/acs.jmedchem.9b01085
127028185 138806 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 375 5 1 4 3.6 Fc1ccc2c(CN3CCO[C@H](COc4cccc(Cl)n4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3792751 138806 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 375 5 1 4 3.6 Fc1ccc2c(CN3CCO[C@H](COc4cccc(Cl)n4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
54580906 61276 0 None -15 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 459 8 0 5 4.6 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccco4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771109 61276 0 None -15 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 459 8 0 5 4.6 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccco4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
53363109 63517 0 None 19 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 465 11 0 8 4.0 CCCCn1cc(COc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
CHEMBL1803030 63517 0 None 19 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 465 11 0 8 4.0 CCCCn1cc(COc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
1353 1880 85 None -3 85 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(98)00108-5
3559 1880 85 None -3 85 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(98)00108-5
86 1880 85 None -3 85 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(98)00108-5
CHEMBL54 1880 85 None -3 85 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(98)00108-5
DB00502 1880 85 None -3 85 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(98)00108-5
22065997 98896 0 None 64 4 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 310 3 1 3 3.0 Fc1ccccc1N1CCN(Cc2c[nH]c3ncccc23)CC1 10.1016/s0960-894x(01)00241-4
CHEMBL282424 98896 0 None 64 4 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 310 3 1 3 3.0 Fc1ccccc1N1CCN(Cc2c[nH]c3ncccc23)CC1 10.1016/s0960-894x(01)00241-4
44400500 165507 0 None -1 5 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
CHEMBL425731 165507 0 None -1 5 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
10593191 188519 0 None 33 3 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2ccc(C)cc2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL51023 188519 0 None 33 3 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2ccc(C)cc2)CC1 10.1016/j.bmcl.2005.02.012
44394667 66704 0 None 27 2 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@@H]1CCN(Cc2ccccc2)C1)c1cccc(-c2ccsc2)c1 10.1016/j.bmcl.2004.07.045
CHEMBL187113 66704 0 None 27 2 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@@H]1CCN(Cc2ccccc2)C1)c1cccc(-c2ccsc2)c1 10.1016/j.bmcl.2004.07.045
10741841 205351 0 None 9 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 441 8 2 4 3.7 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(CCc2ccccc2)C1 10.1021/jm9601720
CHEMBL91859 205351 0 None 9 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 441 8 2 4 3.7 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(CCc2ccccc2)C1 10.1021/jm9601720
155513773 169257 0 None 12 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 551 10 2 5 4.9 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(Br)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4439644 169257 0 None 12 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 551 10 2 5 4.9 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(Br)cc2)CC1 10.1021/acs.jmedchem.9b01085
54580905 61274 0 None -13 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 469 8 0 4 5.0 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccccc4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771107 61274 0 None -13 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 469 8 0 4 5.0 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccccc4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
53327908 61280 0 None -28 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 470 8 0 5 4.4 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccncc4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771112 61280 0 None -28 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 470 8 0 5 4.4 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccncc4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
10594054 31198 1 None 97 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2cc(CN3CCN(c4ccccc4Cl)CC3)[nH]c2c1 10.1021/jm0009989
CHEMBL140258 31198 1 None 97 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2cc(CN3CCN(c4ccccc4Cl)CC3)[nH]c2c1 10.1021/jm0009989
45268292 195012 0 None 138 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 460 4 1 6 3.5 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
CHEMBL564688 195012 0 None 138 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 460 4 1 6 3.5 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
977 1155 3 None -10 4 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 360 4 0 5 2.7 Fc1ccc(cc1)OC[C@@H]1CC[C@@H]2N(C1)CCN(C2)c1ncc(cn1)F 10.1016/s0960-894x(98)00108-5
9820261 1155 3 None -10 4 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 360 4 0 5 2.7 Fc1ccc(cc1)OC[C@@H]1CC[C@@H]2N(C1)CCN(C2)c1ncc(cn1)F 10.1016/s0960-894x(98)00108-5
CHEMBL66227 1155 3 None -10 4 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 360 4 0 5 2.7 Fc1ccc(cc1)OC[C@@H]1CC[C@@H]2N(C1)CCN(C2)c1ncc(cn1)F 10.1016/s0960-894x(98)00108-5
10473658 186610 3 None 38 3 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL49231 186610 3 None 38 3 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2005.02.012
133008 2211 16 None 204 2 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/jm970111h
3302 2211 16 None 204 2 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/jm970111h
CHEMBL444309 2211 16 None 204 2 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/jm970111h
133008 2211 16 None 204 2 Human 8.5 pKi = 8.5 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/jm991029k
3302 2211 16 None 204 2 Human 8.5 pKi = 8.5 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/jm991029k
CHEMBL444309 2211 16 None 204 2 Human 8.5 pKi = 8.5 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/jm991029k
1524 2150 89 None -3 51 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm0002432
197 2150 89 None -3 51 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm0002432
3822 2150 89 None -3 51 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm0002432
88 2150 89 None -3 51 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm0002432
CHEMBL51 2150 89 None -3 51 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm0002432
DB12465 2150 89 None -3 51 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm0002432
133008 2211 16 None 204 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/jm0002432
3302 2211 16 None 204 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/jm0002432
CHEMBL444309 2211 16 None 204 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/jm0002432
44209480 69827 0 None -3 11 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL1940418 69827 0 None -3 11 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2020.115943
44209480 69827 0 None -3 11 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
CHEMBL1940418 69827 0 None -3 11 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
44209480 69827 0 None -3 11 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940418 69827 0 None -3 11 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
44209480 69827 0 None -3 11 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940418 69827 0 None -3 11 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
133008 2211 16 None 204 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/jm960072u
3302 2211 16 None 204 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/jm960072u
CHEMBL444309 2211 16 None 204 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/jm960072u
15817410 57231 0 None 331 2 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 324 4 0 5 2.5 c1ccc(OC[C@@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL166269 57231 0 None 331 2 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 324 4 0 5 2.5 c1ccc(OC[C@@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
168275783 192225 0 None 354 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 394 6 0 5 3.1 O=C1CCc2ccccc2N1CCCN1CCN(c2cccc([N+](=O)[O-])c2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5176100 192225 0 None 354 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 394 6 0 5 3.1 O=C1CCc2ccccc2N1CCCN1CCN(c2cccc([N+](=O)[O-])c2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5221583 192225 0 None 354 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 394 6 0 5 3.1 O=C1CCc2ccccc2N1CCCN1CCN(c2cccc([N+](=O)[O-])c2)CC1 10.1021/acs.jmedchem.2c00840
9995264 205454 0 None 93 3 Human 8.4 pKi = 8.4 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 305 2 0 3 3.7 Cc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccccc1)CC3 10.1021/jm970170v
CHEMBL92489 205454 0 None 93 3 Human 8.4 pKi = 8.4 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 305 2 0 3 3.7 Cc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccccc1)CC3 10.1021/jm970170v
10691599 200902 0 None 22 3 Human 8.4 pKi = 8.4 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 386 4 0 3 6.0 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)no3)CC2)cc1 10.1021/jm970111h
CHEMBL61195 200902 0 None 22 3 Human 8.4 pKi = 8.4 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 386 4 0 3 6.0 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)no3)CC2)cc1 10.1021/jm970111h
44278788 109849 1 None 147 3 Human 8.4 pKi = 8.4 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 327 7 1 4 3.0 OC(COc1ccccc1)CN1CCC(Oc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
CHEMBL32402 109849 1 None 147 3 Human 8.4 pKi = 8.4 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 327 7 1 4 3.0 OC(COc1ccccc1)CN1CCC(Oc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
10404144 203591 19 None 1 10 Human 8.4 pKi = 8.4 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm015522j
CHEMBL7927 203591 19 None 1 10 Human 8.4 pKi = 8.4 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm015522j
10404144 203591 19 None 1 10 Human 8.4 pKi = 8.4 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm049612a
CHEMBL7927 203591 19 None 1 10 Human 8.4 pKi = 8.4 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm049612a
9906978 42466 1 None 1 12 Human 8.4 pKi = 8.4 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL150161 42466 1 None 1 12 Human 8.4 pKi = 8.4 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
9906978 42466 1 None 1 12 Human 8.4 pKi = 8.4 Binding
Binding affinity to human cloned dopamine D4.4 receptor by radioligand binding assayBinding affinity to human cloned dopamine D4.4 receptor by radioligand binding assay
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmcl.2006.03.057
CHEMBL150161 42466 1 None 1 12 Human 8.4 pKi = 8.4 Binding
Binding affinity to human cloned dopamine D4.4 receptor by radioligand binding assayBinding affinity to human cloned dopamine D4.4 receptor by radioligand binding assay
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmcl.2006.03.057
973 1154 33 None -9 6 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human D4.4 receptorBinding affinity towards human D4.4 receptor
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm030505a
9796720 1154 33 None -9 6 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human D4.4 receptorBinding affinity towards human D4.4 receptor
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm030505a
CHEMBL77395 1154 33 None -9 6 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human D4.4 receptorBinding affinity towards human D4.4 receptor
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm030505a
188942 2778 38 None -12 4 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 10.1021/jm0002432
3297 2778 38 None -12 4 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 10.1021/jm0002432
979 2778 38 None -12 4 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 10.1021/jm0002432
CHEMBL103772 2778 38 None -12 4 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 10.1021/jm0002432
155515931 169444 0 None 17 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 509 10 2 5 4.4 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2F)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4442470 169444 0 None 17 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 509 10 2 5 4.4 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2F)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
1353 1880 85 None -3 85 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/S0960-894X(97)00218-7
3559 1880 85 None -3 85 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/S0960-894X(97)00218-7
86 1880 85 None -3 85 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/S0960-894X(97)00218-7
CHEMBL54 1880 85 None -3 85 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/S0960-894X(97)00218-7
DB00502 1880 85 None -3 85 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/S0960-894X(97)00218-7
10691599 200902 0 None 22 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 386 4 0 3 6.0 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)no3)CC2)cc1 10.1021/jm960072u
CHEMBL61195 200902 0 None 22 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 386 4 0 3 6.0 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)no3)CC2)cc1 10.1021/jm960072u
10567430 118788 1 None 851 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2cc(CN3CCN(c4ccccc4)CC3)[nH]c2c1 10.1021/jm0009989
CHEMBL343880 118788 1 None 851 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2cc(CN3CCN(c4ccccc4)CC3)[nH]c2c1 10.1021/jm0009989
10404144 203591 19 None 1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm060166w
CHEMBL7927 203591 19 None 1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm060166w
9905249 99440 0 None -2 3 Rat 8.4 pKi = 8.4 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 322 4 1 4 2.9 COc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
CHEMBL28607 99440 0 None -2 3 Rat 8.4 pKi = 8.4 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 322 4 1 4 2.9 COc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
133079 3581 33 None 1 4 Human 8.4 pKi = 8.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 10.1021/acs.jmedchem.7b00151
980 3581 33 None 1 4 Human 8.4 pKi = 8.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 10.1021/acs.jmedchem.7b00151
CHEMBL69759 3581 33 None 1 4 Human 8.4 pKi = 8.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 10.1021/acs.jmedchem.7b00151
44454734 97278 0 None 20 5 Human 8.4 pKi = 8.4 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 344 7 0 4 3.4 COc1ccccc1N1CCN(Cc2ccc(OCCF)cc2)CC1 10.1016/j.bmcl.2007.12.026
CHEMBL271513 97278 0 None 20 5 Human 8.4 pKi = 8.4 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 344 7 0 4 3.4 COc1ccccc1N1CCN(Cc2ccc(OCCF)cc2)CC1 10.1016/j.bmcl.2007.12.026
3303 2213 41 None -1 15 Rat 8.4 pKi = 8.4 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00241-4
5311200 2213 41 None -1 15 Rat 8.4 pKi = 8.4 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00241-4
CHEMBL267014 2213 41 None -1 15 Rat 8.4 pKi = 8.4 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00241-4
10545941 38689 0 None 181 2 Human 8.4 pKi = 8.4 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 352 4 1 4 3.4 COc1ccc(C2CCN(Cc3ccc4c(c3)NC(=O)CO4)CC2)cc1 10.1021/jm990277d
CHEMBL146757 38689 0 None 181 2 Human 8.4 pKi = 8.4 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 352 4 1 4 3.4 COc1ccc(C2CCN(Cc3ccc4c(c3)NC(=O)CO4)CC2)cc1 10.1021/jm990277d
188942 2778 38 None -12 4 Human 8.4 pKi = 8.4 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 10.1021/jm960637m
3297 2778 38 None -12 4 Human 8.4 pKi = 8.4 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 10.1021/jm960637m
979 2778 38 None -12 4 Human 8.4 pKi = 8.4 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 10.1021/jm960637m
CHEMBL103772 2778 38 None -12 4 Human 8.4 pKi = 8.4 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 10.1021/jm960637m
44326212 205695 0 None -1 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 459 6 2 4 4.5 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(C2C3CCCC2CCC3)C1 10.1021/jm9601720
CHEMBL94050 205695 0 None -1 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 459 6 2 4 4.5 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(C2C3CCCC2CCC3)C1 10.1021/jm9601720
155512259 169081 0 None 15 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 509 10 2 5 4.4 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2cccc(F)c2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4437233 169081 0 None 15 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 509 10 2 5 4.4 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2cccc(F)c2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
132060812 161487 0 None 16 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human dopamine D4 expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 329 4 0 2 4.9 COc1cccc(-c2ccc3c(c2)CCN(Cc2ccccc2)C3)c1 10.1016/j.ejmech.2018.02.024
CHEMBL4160064 161487 0 None 16 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human dopamine D4 expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 329 4 0 2 4.9 COc1cccc(-c2ccc3c(c2)CCN(Cc2ccccc2)C3)c1 10.1016/j.ejmech.2018.02.024
71450707 83664 0 None 15 7 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 444 6 0 5 3.9 COc1ccccc1N1CCN(Cc2cc(CN3CCN(C)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207640 83664 0 None 15 7 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 444 6 0 5 3.9 COc1ccccc1N1CCN(Cc2cc(CN3CCN(C)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
45273443 193958 0 None 66 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 392 4 1 6 2.2 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccccc4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
CHEMBL556288 193958 0 None 66 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 392 4 1 6 2.2 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccccc4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
21997225 55494 0 None 48 2 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 324 4 0 5 2.5 c1ccc(OCC2CCC3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL162265 55494 0 None 48 2 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 324 4 0 5 2.5 c1ccc(OCC2CCC3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
11738728 18313 0 None - 1 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity tested on HEK293 cells co-transfected with human D4.4 receptor using [3H]spiperone as a radioligand in FLIPR assayIn vitro binding affinity tested on HEK293 cells co-transfected with human D4.4 receptor using [3H]spiperone as a radioligand in FLIPR assay
ChEMBL 320 3 1 3 3.5 Cc1ccc(C)c(N2CCN(Cc3nc4ccccc4[nH]3)CC2)c1 10.1021/jm030505a
CHEMBL127290 18313 0 None - 1 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity tested on HEK293 cells co-transfected with human D4.4 receptor using [3H]spiperone as a radioligand in FLIPR assayIn vitro binding affinity tested on HEK293 cells co-transfected with human D4.4 receptor using [3H]spiperone as a radioligand in FLIPR assay
ChEMBL 320 3 1 3 3.5 Cc1ccc(C)c(N2CCN(Cc3nc4ccccc4[nH]3)CC2)c1 10.1021/jm030505a
9817774 111009 0 None -5 4 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 299 6 3 4 3.0 Sc1nc2c(OCCNCc3ccccc3)cccc2[nH]1 10.1016/s0960-894x(99)00434-5
CHEMBL327782 111009 0 None -5 4 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 299 6 3 4 3.0 Sc1nc2c(OCCNCc3ccccc3)cccc2[nH]1 10.1016/s0960-894x(99)00434-5
1353 1880 85 None -3 85 Human 8.4 pKi = 8.4 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/S0960-894X(97)00194-7
3559 1880 85 None -3 85 Human 8.4 pKi = 8.4 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/S0960-894X(97)00194-7
86 1880 85 None -3 85 Human 8.4 pKi = 8.4 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/S0960-894X(97)00194-7
CHEMBL54 1880 85 None -3 85 Human 8.4 pKi = 8.4 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/S0960-894X(97)00194-7
DB00502 1880 85 None -3 85 Human 8.4 pKi = 8.4 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/S0960-894X(97)00194-7
10760638 187593 0 None 131 3 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL49876 187593 0 None 131 3 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2005.02.012
56852956 111551 1 None 10 9 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289656 111551 1 None 10 9 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
10425969 100539 3 None 346 4 Human 8.4 pKi = 8.4 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 317 4 1 4 2.8 N#CC(C#N)=Cc1cc(CN2CCN(c3ccccc3)CC2)c[nH]1 10.1016/s0960-894x(99)00302-9
CHEMBL294459 100539 3 None 346 4 Human 8.4 pKi = 8.4 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 317 4 1 4 2.8 N#CC(C#N)=Cc1cc(CN2CCN(c3ccccc3)CC2)c[nH]1 10.1016/s0960-894x(99)00302-9
792460 91714 7 None 28 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 302 5 0 4 3.5 CCOc1ccccc1N1CCN(Cc2cccs2)CC1 10.1016/j.bmcl.2013.07.033
CHEMBL2420773 91714 7 None 28 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 302 5 0 4 3.5 CCOc1ccccc1N1CCN(Cc2cccs2)CC1 10.1016/j.bmcl.2013.07.033
56852956 111551 1 None 10 9 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289656 111551 1 None 10 9 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
137634397 155564 0 None -8 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 480 8 3 10 2.2 O=C1COc2c(N3CCN(CCCCOc4ccn5ncc(/C=N/O)c5c4)CC3)ccc(O)c2N1 10.1016/j.bmc.2017.08.037
CHEMBL4063145 155564 0 None -8 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 480 8 3 10 2.2 O=C1COc2c(N3CCN(CCCCOc4ccn5ncc(/C=N/O)c5c4)CC3)ccc(O)c2N1 10.1016/j.bmc.2017.08.037
10069973 52120 0 None -4 5 Human 8.4 pKi = 8.4 Binding
Binding affinity of compound was tested for Dopamine receptor D4Binding affinity of compound was tested for Dopamine receptor D4
ChEMBL 407 9 0 6 4.4 COc1ccccc1C(=O)CCCCCN1CCN(c2noc3ccccc23)CC1 10.1021/jm020994z
CHEMBL159022 52120 0 None -4 5 Human 8.4 pKi = 8.4 Binding
Binding affinity of compound was tested for Dopamine receptor D4Binding affinity of compound was tested for Dopamine receptor D4
ChEMBL 407 9 0 6 4.4 COc1ccccc1C(=O)CCCCCN1CCN(c2noc3ccccc23)CC1 10.1021/jm020994z
44369020 118954 0 None 2 3 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 374 6 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/jm020952a
CHEMBL345111 118954 0 None 2 3 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 374 6 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/jm020952a
10425450 199 23 None -1 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
3301 199 23 None -1 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
CHEMBL375596 199 23 None -1 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
17461770 200155 1 None 10 2 Human 8.4 pKi = 8.4 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 360 5 1 3 3.9 COc1cc2ccccc2cc1C(=O)NC1CCN(Cc2ccccc2)C1 10.1021/jm960017l
CHEMBL60708 200155 1 None 10 2 Human 8.4 pKi = 8.4 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 360 5 1 3 3.9 COc1cc2ccccc2cc1C(=O)NC1CCN(Cc2ccccc2)C1 10.1021/jm960017l
44370032 47125 0 None -1 3 Human 7.5 pKi = 7.5 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 329 5 1 2 4.4 C1=C(/C=C/c2ccccc2)CCN(CCc2cc3ccc[nH]c-3n2)C1 10.1016/s0960-894x(99)00025-6
CHEMBL154482 47125 0 None -1 3 Human 7.5 pKi = 7.5 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 329 5 1 2 4.4 C1=C(/C=C/c2ccccc2)CCN(CCc2cc3ccc[nH]c-3n2)C1 10.1016/s0960-894x(99)00025-6
10092819 16594 0 None -28 12 Human 7.5 pKi = 7.5 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm049612a
CHEMBL124444 16594 0 None -28 12 Human 7.5 pKi = 7.5 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm049612a
10092819 16594 0 None -28 12 Human 7.5 pKi = 7.5 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm025558r
CHEMBL124444 16594 0 None -28 12 Human 7.5 pKi = 7.5 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm025558r
11068912 30648 0 None 8 4 Human 7.5 pKi = 7.5 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 379 6 1 6 1.9 COc1ccccc1N1CCN(CCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
CHEMBL139722 30648 0 None 8 4 Human 7.5 pKi = 7.5 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 379 6 1 6 1.9 COc1ccccc1N1CCN(CCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
10542345 18692 0 None 7 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 301 9 1 3 4.1 Cc1ccc(SCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
CHEMBL128281 18692 0 None 7 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 301 9 1 3 4.1 Cc1ccc(SCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
135398737 944 89 None -13 91 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm020952a
38 944 89 None -13 91 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm020952a
722 944 89 None -13 91 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm020952a
CHEMBL42 944 89 None -13 91 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm020952a
DB00363 944 89 None -13 91 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm020952a
10781960 15384 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 320 3 0 4 3.1 O=c1ccc2cc(CN3CCN(c4ccccc4)CC3)ccc2o1 10.1021/jm990266k
CHEMBL121993 15384 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 320 3 0 4 3.1 O=c1ccc2cc(CN3CCN(c4ccccc4)CC3)ccc2o1 10.1021/jm990266k
162671033 183173 0 None 3 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2cccnc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL4793296 183173 0 None 3 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2cccnc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL4803797 183173 0 None 3 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2cccnc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
154726793 175659 1 None 1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 454 11 0 6 5.2 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4590966 175659 1 None 1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 454 11 0 6 5.2 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4594692 175659 1 None 1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 454 11 0 6 5.2 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
135398737 944 89 None -13 91 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm020938y
38 944 89 None -13 91 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm020938y
722 944 89 None -13 91 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm020938y
CHEMBL42 944 89 None -13 91 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm020938y
DB00363 944 89 None -13 91 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm020938y
2726 906 64 None -8 72 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
621 906 64 None -8 72 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
83 906 64 None -8 72 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
CHEMBL71 906 64 None -8 72 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
DB00477 906 64 None -8 72 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
49782602 16987 0 None 1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 583 6 1 3 7.4 O=C(CCCN1CCC(O)(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
CHEMBL1256169 16987 0 None 1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 583 6 1 3 7.4 O=C(CCCN1CCC(O)(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
49782604 17341 0 None 1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 379 6 1 3 4.9 Cc1ccc(C)c(C(=O)CCCN2CCC(O)(c3cc(C)ccc3C)CC2)c1 10.1021/jm100899z
CHEMBL1257927 17341 0 None 1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 379 6 1 3 4.9 Cc1ccc(C)c(C(=O)CCCN2CCC(O)(c3cc(C)ccc3C)CC2)c1 10.1021/jm100899z
137636351 155332 0 None -87 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 459 7 1 6 4.0 O=Cc1cnn2ccc(NC(=O)CCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/acs.jmedchem.6b01857
CHEMBL4060403 155332 0 None -87 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 459 7 1 6 4.0 O=Cc1cnn2ccc(NC(=O)CCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/acs.jmedchem.6b01857
73347474 90628 0 None -30 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 549 18 1 7 5.4 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cnn(CCCC)n3)c(OC)c2)CC1 10.1021/jm400520c
CHEMBL2397478 90628 0 None -30 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 549 18 1 7 5.4 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cnn(CCCC)n3)c(OC)c2)CC1 10.1021/jm400520c
71733935 90552 0 None -43 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm501889t
CHEMBL2396663 90552 0 None -43 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm501889t
122177641 120696 0 None -47 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 551 18 1 8 4.6 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cn(CCCC)nn3)c(OC)c2)CO1 10.1021/jm501889t
CHEMBL3577342 120696 0 None -47 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 551 18 1 8 4.6 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cn(CCCC)nn3)c(OC)c2)CO1 10.1021/jm501889t
11474021 4726 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 365 6 0 4 3.8 COc1ccc(F)cc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL104089 4726 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 365 6 0 4 3.8 COc1ccc(F)cc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
135398737 944 89 None -13 91 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991138z
38 944 89 None -13 91 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991138z
722 944 89 None -13 91 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991138z
CHEMBL42 944 89 None -13 91 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991138z
DB00363 944 89 None -13 91 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991138z
53248675 66037 0 None -213 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 407 8 1 5 3.5 COc1ccccc1N1CCN(CCCCOc2ccc3ccc(=O)[nH]c3c2)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1813594 66037 0 None -213 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 407 8 1 5 3.5 COc1ccccc1N1CCN(CCCCOc2ccc3ccc(=O)[nH]c3c2)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1851639 66037 0 None -213 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 407 8 1 5 3.5 COc1ccccc1N1CCN(CCCCOc2ccc3ccc(=O)[nH]c3c2)CC1 10.1016/j.bmc.2011.04.021
168293632 192398 0 None 27 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 320 5 1 3 3.3 c1ccc(N2CCN(CCCc3nc4ccccc4[nH]3)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5203856 192398 0 None 27 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 320 5 1 3 3.3 c1ccc(N2CCN(CCCc3nc4ccccc4[nH]3)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5222695 192398 0 None 27 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 320 5 1 3 3.3 c1ccc(N2CCN(CCCc3nc4ccccc4[nH]3)CC2)cc1 10.1021/acs.jmedchem.2c00840
10092819 16594 0 None -28 12 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm0611152
CHEMBL124444 16594 0 None -28 12 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm0611152
11068912 30648 0 None 8 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 379 6 1 6 1.9 COc1ccccc1N1CCN(CCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm0611152
CHEMBL139722 30648 0 None 8 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 379 6 1 6 1.9 COc1ccccc1N1CCN(CCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm0611152
135398737 944 89 None -13 91 Human 7.5 pKi = 7.5 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.07.068
38 944 89 None -13 91 Human 7.5 pKi = 7.5 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.07.068
722 944 89 None -13 91 Human 7.5 pKi = 7.5 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.07.068
CHEMBL42 944 89 None -13 91 Human 7.5 pKi = 7.5 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.07.068
DB00363 944 89 None -13 91 Human 7.5 pKi = 7.5 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.07.068
90644068 111545 0 None 1 2 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 369 6 0 4 4.6 Clc1ccc(N2CCN(CCCCc3nc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289650 111545 0 None 1 2 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 369 6 0 4 4.6 Clc1ccc(N2CCN(CCCCc3nc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
10616050 186064 3 None 81 3 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 325 5 1 4 2.2 COc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL48807 186064 3 None 81 3 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 325 5 1 4 2.2 COc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1016/j.bmcl.2005.02.012
164621627 184901 0 None -13 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 369 5 0 4 3.7 O=C1c2ccc(Cl)cc2CC1CCCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL4862180 184901 0 None -13 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 369 5 0 4 3.7 O=C1c2ccc(Cl)cc2CC1CCCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
44419053 83871 0 None -79 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 447 8 1 5 4.2 C#Cc1ccc2sc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)cc2c1 10.1021/jm0611152
CHEMBL221397 83871 0 None -79 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 447 8 1 5 4.2 C#Cc1ccc2sc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)cc2c1 10.1021/jm0611152
44323890 205190 0 None -4 4 Human 6.5 pKi = 6.5 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 316 1 0 2 4.2 C/C=C1/c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL90977 205190 0 None -4 4 Human 6.5 pKi = 6.5 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 316 1 0 2 4.2 C/C=C1/c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
49783039 17471 0 None -120 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 421 7 1 4 4.9 Cc1ccc(C)c(N2CCN(CCCCNC(=O)c3cc4ccccc4s3)CC2)c1 10.1021/jm100899z
CHEMBL1258383 17471 0 None -120 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 421 7 1 4 4.9 Cc1ccc(C)c(N2CCN(CCCCNC(=O)c3cc4ccccc4s3)CC2)c1 10.1021/jm100899z
127045855 139134 0 None -3 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
CHEMBL3797876 139134 0 None -3 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
118709163 112910 0 None -112 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 888 21 0 8 11.3 O=C(CCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318835 112910 0 None -112 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 888 21 0 8 11.3 O=C(CCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
137655795 158036 0 None -120 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 453 7 2 7 3.0 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCCO5)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4091933 158036 0 None -120 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 453 7 2 7 3.0 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCCO5)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
3038495 700 30 None -91 19 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]YM-09151-2 binding to human Dopamine D4 receptor expressed in CHO cellsInhibition of [3H]YM-09151-2 binding to human Dopamine D4 receptor expressed in CHO cells
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm040190e
7625 700 30 None -91 19 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]YM-09151-2 binding to human Dopamine D4 receptor expressed in CHO cellsInhibition of [3H]YM-09151-2 binding to human Dopamine D4 receptor expressed in CHO cells
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm040190e
CHEMBL25236 700 30 None -91 19 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]YM-09151-2 binding to human Dopamine D4 receptor expressed in CHO cellsInhibition of [3H]YM-09151-2 binding to human Dopamine D4 receptor expressed in CHO cells
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm040190e
10917920 110958 0 None -3801 10 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 487 6 1 6 3.8 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL327527 110958 0 None -3801 10 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 487 6 1 6 3.8 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
10404663 166308 8 None -100 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 334 9 1 3 3.0 C=CCN1CCC[C@H]1CNC(=O)c1cc(CCCF)ccc1OC 10.1016/j.bmc.2007.07.017
CHEMBL428561 166308 8 None -100 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 334 9 1 3 3.0 C=CCN1CCC[C@H]1CNC(=O)c1cc(CCCF)ccc1OC 10.1016/j.bmc.2007.07.017
122189390 122729 0 None -323 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 469 6 0 8 3.4 O=Cc1cnn2ccc(-n3cc(CCN4CCN(c5cccc(Cl)c5Cl)CC4)nn3)cc12 10.1016/j.bmc.2015.07.050
CHEMBL3613876 122729 0 None -323 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 469 6 0 8 3.4 O=Cc1cnn2ccc(-n3cc(CCN4CCN(c5cccc(Cl)c5Cl)CC4)nn3)cc12 10.1016/j.bmc.2015.07.050
25129807 102819 0 None -154 5 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 366 3 2 2 4.8 O[C@@]1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2Cc1c[nH]c2ccccc12 10.1016/j.bmc.2008.12.054
CHEMBL3084502 102819 0 None -154 5 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 366 3 2 2 4.8 O[C@@]1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2Cc1c[nH]c2ccccc12 10.1016/j.bmc.2008.12.054
44330640 206560 1 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 218 0 0 3 3.0 Cc1sc(C)c2c1CCCc1nccn1-2 10.1016/s0960-894x(03)00587-0
CHEMBL99054 206560 1 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 218 0 0 3 3.0 Cc1sc(C)c2c1CCCc1nccn1-2 10.1016/s0960-894x(03)00587-0
164619170 185019 0 None -45 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4863832 185019 0 None -45 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
11720119 82813 0 None -27 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 490 12 1 7 3.6 CCCc1c(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)nnn1Cc1ccccc1 10.1021/jm0611152
CHEMBL218607 82813 0 None -27 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 490 12 1 7 3.6 CCCc1c(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)nnn1Cc1ccccc1 10.1021/jm0611152
164619170 185019 0 None -45 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4863832 185019 0 None -45 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
9888555 165052 11 None -208 8 Human 6.5 pKi = 6.5 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm900095y
CHEMBL424294 165052 11 None -208 8 Human 6.5 pKi = 6.5 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm900095y
130431334 173854 0 None -1513 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 454 8 3 4 3.7 CCc1cccc(N2CCN(CCC(O)CNC(=O)c3cc4ccccc4[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4552939 173854 0 None -1513 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 454 8 3 4 3.7 CCc1cccc(N2CCN(CCC(O)CNC(=O)c3cc4ccccc4[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
168271259 189921 0 None 2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 403 5 0 4 4.8 Cc1nc(CN2CCC(OCc3cccc(C(F)(F)F)c3)CC2)c2ccccn12 10.1016/j.bmcl.2022.128615
CHEMBL5179459 189921 0 None 2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 403 5 0 4 4.8 Cc1nc(CN2CCC(OCc3cccc(C(F)(F)F)c3)CC2)c2ccccn12 10.1016/j.bmcl.2022.128615
53248159 61660 0 None -501 5 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 500 8 1 4 5.3 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm200288r
CHEMBL1774384 61660 0 None -501 5 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 500 8 1 4 5.3 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm200288r
10098342 137463 0 None -891 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 523 7 1 4 5.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(Br)ccc2o1 10.1021/jm0611152
CHEMBL376445 137463 0 None -891 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 523 7 1 4 5.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(Br)ccc2o1 10.1021/jm0611152
72164300 91723 0 None 2 3 Human 7.5 pKi = 7.5 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 370 3 0 2 5.5 Clc1cccc(N2CCN(Cc3cccc4ccccc34)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
CHEMBL2420782 91723 0 None 2 3 Human 7.5 pKi = 7.5 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 370 3 0 2 5.5 Clc1cccc(N2CCN(Cc3cccc4ccccc34)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
44393415 64899 0 None -12 5 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 499 8 1 5 3.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(I)s2)CC1 10.1016/j.bmcl.2004.05.052
CHEMBL182652 64899 0 None -12 5 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 499 8 1 5 3.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(I)s2)CC1 10.1016/j.bmcl.2004.05.052
44336352 110511 0 None 4 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 425 6 0 3 4.6 CCC1(CC)Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL326250 110511 0 None 4 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 425 6 0 3 4.6 CCC1(CC)Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
9818076 16048 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 308 7 2 4 3.4 O=c1ccc2ccc(CNCCCNc3ccccc3)cc2o1 10.1021/jm990266k
CHEMBL122427 16048 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 308 7 2 4 3.4 O=c1ccc2ccc(CNCCCNc3ccccc3)cc2o1 10.1021/jm990266k
164621627 184901 0 None -13 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 369 5 0 4 3.7 O=C1c2ccc(Cl)cc2CC1CCCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL4862180 184901 0 None -13 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 369 5 0 4 3.7 O=C1c2ccc(Cl)cc2CC1CCCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
60167166 74945 0 None 1 8 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 371 5 0 4 4.7 Clc1ccc(N2CCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL2037430 74945 0 None 1 8 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 371 5 0 4 4.7 Clc1ccc(N2CCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2014.04.026
60167166 74945 0 None 1 8 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 371 5 0 4 4.7 Clc1ccc(N2CCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.ejmech.2012.03.042
CHEMBL2037430 74945 0 None 1 8 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 371 5 0 4 4.7 Clc1ccc(N2CCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.ejmech.2012.03.042
44431487 87646 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 374 5 1 3 4.2 COc1ccc(CN2CCC(NC(=O)c3ccc4ccccc4c3)CC2)cc1 10.1016/j.bmcl.2006.12.106
CHEMBL234646 87646 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 374 5 1 3 4.2 COc1ccc(CN2CCC(NC(=O)c3ccc4ccccc4c3)CC2)cc1 10.1016/j.bmcl.2006.12.106
137632761 156033 0 None -13 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 476 8 3 9 2.7 O=c1ccc2c(N3CCN(CCCCOc4ccn5ncc(/C=N/O)c5c4)CC3)ccc(O)c2[nH]1 10.1016/j.bmc.2017.08.037
CHEMBL4068561 156033 0 None -13 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 476 8 3 9 2.7 O=c1ccc2c(N3CCN(CCCCOc4ccn5ncc(/C=N/O)c5c4)CC3)ccc(O)c2[nH]1 10.1016/j.bmc.2017.08.037
137654675 158088 0 None -8 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 433 7 2 7 2.9 O=c1ccc2c(N3CCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2[nH]1 10.1021/acs.jmedchem.7b00363
CHEMBL4092441 158088 0 None -8 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 433 7 2 7 2.9 O=c1ccc2c(N3CCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2[nH]1 10.1021/acs.jmedchem.7b00363
137633705 156077 0 None -57 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 474 7 2 7 4.0 O=C(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)Nc1ccn2ncc(/C=N\O)c2c1 10.1021/acs.jmedchem.6b01857
CHEMBL4069091 156077 0 None -57 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 474 7 2 7 4.0 O=C(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)Nc1ccn2ncc(/C=N\O)c2c1 10.1021/acs.jmedchem.6b01857
122181331 121358 0 None -15 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 414 9 1 3 5.4 CCCN(CCCCNC(=O)/N=N/c1ccc(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3590082 121358 0 None -15 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 414 9 1 3 5.4 CCCN(CCCCNC(=O)/N=N/c1ccc(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
10691634 100184 0 None 12 2 Human 7.5 pKi = 7.5 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 387 7 0 3 5.7 COc1cc2ccccc2cc1C(=O)CCC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
CHEMBL292186 100184 0 None 12 2 Human 7.5 pKi = 7.5 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 387 7 0 3 5.7 COc1cc2ccccc2cc1C(=O)CCC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
11793892 196374 0 None 31 2 Human 7.5 pKi = 7.5 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 375 7 0 3 5.3 COc1cc2ccccc2cc1COCC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
CHEMBL57407 196374 0 None 31 2 Human 7.5 pKi = 7.5 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 375 7 0 3 5.3 COc1cc2ccccc2cc1COCC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
44273912 77696 0 None 50 2 Human 7.5 pKi = 7.5 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 365 8 1 3 3.8 CCCCC(C)(C)C(=O)NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL20996 77696 0 None 50 2 Human 7.5 pKi = 7.5 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 365 8 1 3 3.8 CCCCC(C)(C)C(=O)NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
44273897 98255 0 None 50 2 Human 7.5 pKi = 7.5 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 395 6 1 3 3.5 CC(C)(C)C(=O)NCCCCN1CCN(c2ccc(Br)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL277669 98255 0 None 50 2 Human 7.5 pKi = 7.5 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 395 6 1 3 3.5 CC(C)(C)C(=O)NCCCCN1CCN(c2ccc(Br)cc2)CC1 10.1016/0960-894X(96)00198-9
2726 906 64 None -8 72 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
621 906 64 None -8 72 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
83 906 64 None -8 72 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
CHEMBL71 906 64 None -8 72 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
DB00477 906 64 None -8 72 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
76325152 105890 0 None -3 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
CHEMBL3115579 105890 0 None -3 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
CHEMBL3139262 105890 0 None -3 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
53248677 66086 0 None -446 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 439 10 1 5 3.9 O=c1ccc2ccc(OCCCCN3CCN(c4ccccc4OCCF)CC3)cc2[nH]1 10.1016/j.bmc.2011.04.021
CHEMBL1813595 66086 0 None -446 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 439 10 1 5 3.9 O=c1ccc2ccc(OCCCCN3CCN(c4ccccc4OCCF)CC3)cc2[nH]1 10.1016/j.bmc.2011.04.021
CHEMBL1851893 66086 0 None -446 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 439 10 1 5 3.9 O=c1ccc2ccc(OCCCCN3CCN(c4ccccc4OCCF)CC3)cc2[nH]1 10.1016/j.bmc.2011.04.021
127053218 138948 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 334 5 0 4 3.5 c1ccc(OC[C@@H]2CN(Cc3ccc4ccccc4n3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3794336 138948 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 334 5 0 4 3.5 c1ccc(OC[C@@H]2CN(Cc3ccc4ccccc4n3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
17469721 77671 6 None 9 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 320 4 0 6 2.0 c1ccc(-n2cc(CN3CCN(c4ncccn4)CC3)cn2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL209832 77671 6 None 9 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 320 4 0 6 2.0 c1ccc(-n2cc(CN3CCN(c4ncccn4)CC3)cn2)cc1 10.1016/j.bmcl.2006.02.075
10359539 58745 6 None 41 4 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity to displace [3H]-spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]-spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 334 4 1 4 2.6 c1ccc(C2=NCC[C@@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(03)00004-0
CHEMBL169459 58745 6 None 41 4 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity to displace [3H]-spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]-spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 334 4 1 4 2.6 c1ccc(C2=NCC[C@@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(03)00004-0
3033769 3229 54 None -562 18 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10.1016/j.bmc.2007.07.017
3299 3229 54 None -562 18 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10.1016/j.bmc.2007.07.017
94 3229 54 None -562 18 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10.1016/j.bmc.2007.07.017
CHEMBL8809 3229 54 None -562 18 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10.1016/j.bmc.2007.07.017
DB12518 3229 54 None -562 18 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10.1016/j.bmc.2007.07.017
25139180 183759 0 None -10 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 490 10 1 2 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CC=C(C#Cc2ccccc2)CC1 10.1021/jm800895v
CHEMBL484357 183759 0 None -10 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 490 10 1 2 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CC=C(C#Cc2ccccc2)CC1 10.1021/jm800895v
114840 69240 55 None 1 2 Human 5.5 pKi = 5.5 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 271 2 4 4 2.2 Oc1ccc(CC2NCCc3cc(O)c(O)cc32)cc1 10.1016/S0960-894X(97)00194-7
CHEMBL19344 69240 55 None 1 2 Human 5.5 pKi = 5.5 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 271 2 4 4 2.2 Oc1ccc(CC2NCCc3cc(O)c(O)cc32)cc1 10.1016/S0960-894X(97)00194-7
CHEMBL5079053 212829 0 None -107 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCc1cc(Cl)c(OC)c(C(=O)NCC2CCCN2CC(=O)N2CCC(c3ccccc3)(c3ccccc3)C2)c1O 10.1021/acs.jmedchem.1c00611
9926141 169689 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 294 6 2 4 3.0 O=c1ccc2cc(CNCCNc3ccccc3)ccc2o1 10.1021/jm990266k
CHEMBL444596 169689 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 294 6 2 4 3.0 O=c1ccc2cc(CNCCNc3ccccc3)ccc2o1 10.1021/jm990266k
11442138 68847 0 None -75 3 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 443 7 1 4 4.5 COc1cccc2c1N1CCN(CCCCNC(=O)c3ccc4ccccc4c3)C[C@H]1CC2 10.1021/jm049031l
CHEMBL192650 68847 0 None -75 3 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 443 7 1 4 4.5 COc1cccc2c1N1CCN(CCCCNC(=O)c3ccc4ccccc4c3)C[C@H]1CC2 10.1021/jm049031l
10470579 205642 0 None -16 4 Human 6.5 pKi = 6.5 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 309 4 3 4 2.8 Oc1nc2c3c(ccc2[nH]1)CC[C@@H](CNCc1ccccc1)O3 10.1016/s0960-894x(01)00778-8
CHEMBL93753 205642 0 None -16 4 Human 6.5 pKi = 6.5 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 309 4 3 4 2.8 Oc1nc2c3c(ccc2[nH]1)CC[C@@H](CNCc1ccccc1)O3 10.1016/s0960-894x(01)00778-8
155195487 172705 0 None -14 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1CC1CC1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
CHEMBL4525362 172705 0 None -14 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1CC1CC1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
9816808 204587 0 None -51 4 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 267 6 2 3 2.7 c1ccc(CNCCOc2cccc3[nH]ncc23)cc1 10.1016/s0960-894x(99)00434-5
CHEMBL87137 204587 0 None -51 4 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 267 6 2 3 2.7 c1ccc(CNCCOc2cccc3[nH]ncc23)cc1 10.1016/s0960-894x(99)00434-5
49783419 17567 0 None -954 13 Rat 6.5 pKi = 6.5 Binding
Binding affinity to rat dopamine D4 receptorBinding affinity to rat dopamine D4 receptor
ChEMBL 366 6 1 6 2.8 CCCCN1CCC(COC(=O)c2cc(F)c(N)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258671 17567 0 None -954 13 Rat 6.5 pKi = 6.5 Binding
Binding affinity to rat dopamine D4 receptorBinding affinity to rat dopamine D4 receptor
ChEMBL 366 6 1 6 2.8 CCCCN1CCC(COC(=O)c2cc(F)c(N)c3c2OCCO3)CC1 10.1021/jm100668r
130431277 169365 0 None -58 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 224 2 1 2 2.3 CCc1cccc(N2CCNCC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4441358 169365 0 None -58 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 224 2 1 2 2.3 CCc1cccc(N2CCNCC2)c1Cl 10.1021/acs.jmedchem.6b00860
44376920 55068 0 None 3 2 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 381 5 1 6 2.4 CC(=O)Nc1ccc(OC[C@@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL161899 55068 0 None 3 2 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 381 5 1 6 2.4 CC(=O)Nc1ccc(OC[C@@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
44273925 76941 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 347 7 1 4 2.8 COc1ccc(N2CCN(CCCCNC(=O)C(C)(C)C)CC2)cc1 10.1016/0960-894X(96)00198-9
CHEMBL20819 76941 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 347 7 1 4 2.8 COc1ccc(N2CCN(CCCCNC(=O)C(C)(C)C)CC2)cc1 10.1016/0960-894X(96)00198-9
44273815 77781 2 None 2 2 Human 6.5 pKi = 6.5 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 317 6 1 3 2.8 CC(C)(C)C(=O)NCCCCN1CCN(c2ccccc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL21035 77781 2 None 2 2 Human 6.5 pKi = 6.5 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 317 6 1 3 2.8 CC(C)(C)C(=O)NCCCCN1CCN(c2ccccc2)CC1 10.1016/0960-894X(96)00198-9
137636308 155661 0 None 8 8 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 329 7 0 3 2.8 CCCCN1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4064222 155661 0 None 8 8 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 329 7 0 3 2.8 CCCCN1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
10430685 54014 0 None -107 5 Human 6.5 pKi = 6.5 Binding
Binding affinity of compound was tested for Dopamine receptor D4Binding affinity of compound was tested for Dopamine receptor D4
ChEMBL 393 8 1 6 4.1 O=C(CCCCCN1CCN(c2noc3ccccc23)CC1)c1ccccc1O 10.1021/jm020994z
CHEMBL160817 54014 0 None -107 5 Human 6.5 pKi = 6.5 Binding
Binding affinity of compound was tested for Dopamine receptor D4Binding affinity of compound was tested for Dopamine receptor D4
ChEMBL 393 8 1 6 4.1 O=C(CCCCCN1CCN(c2noc3ccccc23)CC1)c1ccccc1O 10.1021/jm020994z
6466372 169495 12 None 93 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 311 4 1 5 1.5 Cc1cccc(NC(=O)CN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4443054 169495 12 None 93 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 311 4 1 5 1.5 Cc1cccc(NC(=O)CN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
53248256 61706 0 None -316 4 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 473 8 1 4 4.5 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2ccc3c(c2)Cc2ccccc2-3)CC1 10.1021/jm200288r
CHEMBL1774536 61706 0 None -316 4 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 473 8 1 4 4.5 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2ccc3c(c2)Cc2ccccc2-3)CC1 10.1021/jm200288r
44438239 154395 1 None -13 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 352 4 2 3 4.4 CSc1ccc(C2(O)CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.10.076
CHEMBL401031 154395 1 None -13 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 352 4 2 3 4.4 CSc1ccc(C2(O)CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.10.076
168268918 189414 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 369 5 1 3 4.7 Cc1cccc(CO[C@H]2CCCN(Cc3cc4ccc(Cl)cc4[nH]3)C2)n1 10.1016/j.bmcl.2022.128615
CHEMBL5171398 189414 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 369 5 1 3 4.7 Cc1cccc(CO[C@H]2CCCN(Cc3cc4ccc(Cl)cc4[nH]3)C2)n1 10.1016/j.bmcl.2022.128615
15290395 99437 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 393 7 1 3 4.7 OC(COc1cccc2ccccc12)CN1CCC(Cc2ccc(F)cc2)CC1 10.1016/S0960-894X(97)00233-3
CHEMBL28605 99437 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 393 7 1 3 4.7 OC(COc1cccc2ccccc12)CN1CCC(Cc2ccc(F)cc2)CC1 10.1016/S0960-894X(97)00233-3
44278829 100011 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 393 7 1 4 4.8 OC(COc1cccc2ccccc12)CN1CCC(Sc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
CHEMBL29087 100011 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 393 7 1 4 4.8 OC(COc1cccc2ccccc12)CN1CCC(Sc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
10065188 101133 0 None 3 3 Human 7.5 pKi = 7.5 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 329 4 1 3 2.9 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccccc1 10.1021/jm970021c
CHEMBL298763 101133 0 None 3 3 Human 7.5 pKi = 7.5 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 329 4 1 3 2.9 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccccc1 10.1021/jm970021c
135398737 944 89 None -7 91 Rat 7.5 pKi = 7.5 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
38 944 89 None -7 91 Rat 7.5 pKi = 7.5 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
722 944 89 None -7 91 Rat 7.5 pKi = 7.5 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
CHEMBL42 944 89 None -7 91 Rat 7.5 pKi = 7.5 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
DB00363 944 89 None -7 91 Rat 7.5 pKi = 7.5 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
2865 4079 67 None -66 53 Human 7.5 pKi = 7.5 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmc.2008.06.030
59 4079 67 None -66 53 Human 7.5 pKi = 7.5 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmc.2008.06.030
60854 4079 67 None -66 53 Human 7.5 pKi = 7.5 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmc.2008.06.030
CHEMBL708 4079 67 None -66 53 Human 7.5 pKi = 7.5 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmc.2008.06.030
DB00246 4079 67 None -66 53 Human 7.5 pKi = 7.5 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmc.2008.06.030
9905720 167370 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 3 0 4 3.4 Cc1cccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)c1 10.1021/jm990266k
CHEMBL431479 167370 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 3 0 4 3.4 Cc1cccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)c1 10.1021/jm990266k
10704110 115241 0 None -42 3 Human 7.5 pKi = 7.5 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 219 3 1 2 2.6 CCCN(C)C1CCc2ccc(O)cc2C1 10.1021/jm960345l
CHEMBL335392 115241 0 None -42 3 Human 7.5 pKi = 7.5 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 219 3 1 2 2.6 CCCN(C)C1CCc2ccc(O)cc2C1 10.1021/jm960345l
16094699 81733 4 None 109 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]spiperone from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 309 4 1 3 3.0 Cc1cccc(C(=O)NCN2CCC(c3ccccn3)CC2)c1 10.1021/jm060662k
CHEMBL216794 81733 4 None 109 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]spiperone from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 309 4 1 3 3.0 Cc1cccc(C(=O)NCN2CCC(c3ccccn3)CC2)c1 10.1021/jm060662k
72544787 92698 0 None 6 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 587 12 3 12 1.2 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCCOC4O[C@H](CO)[C@@H](O)[C@H](O)[C@H]4F)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443008 92698 0 None 6 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 587 12 3 12 1.2 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCCOC4O[C@H](CO)[C@@H](O)[C@H](O)[C@H]4F)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
137644966 157948 0 None -45 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 456 6 1 6 4.1 N#Cc1cnn2ccc(NC(=O)CCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/acs.jmedchem.6b01857
CHEMBL4091064 157948 0 None -45 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 456 6 1 6 4.1 N#Cc1cnn2ccc(NC(=O)CCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/acs.jmedchem.6b01857
21219160 91575 0 None 14 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 318 4 0 4 3.8 c1ccc(CN2CCC(n3cc(-c4ccccc4)nn3)CC2)cc1 10.1016/s0960-894x(99)00169-9
CHEMBL24170 91575 0 None 14 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 318 4 0 4 3.8 c1ccc(CN2CCC(n3cc(-c4ccccc4)nn3)CC2)cc1 10.1016/s0960-894x(99)00169-9
10014924 106787 0 None -16 5 Human 7.5 pKi = 7.5 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1 10.1021/jm0503805
CHEMBL316983 106787 0 None -16 5 Human 7.5 pKi = 7.5 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1 10.1021/jm0503805
10014924 106787 0 None -16 5 Human 7.5 pKi = 7.5 Binding
High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsHigh inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1 10.1021/jm049269+
CHEMBL316983 106787 0 None -16 5 Human 7.5 pKi = 7.5 Binding
High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsHigh inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1 10.1021/jm049269+
11383473 4811 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 381 6 0 4 4.3 COc1ccccc1OCC1CN(Cc2ccc(Cl)c(Cl)c2)CCO1 10.1021/jm031111m
CHEMBL104431 4811 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 381 6 0 4 4.3 COc1ccccc1OCC1CN(Cc2ccc(Cl)c(Cl)c2)CCO1 10.1021/jm031111m
11393899 4822 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 347 6 0 4 3.6 COc1ccccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL104485 4822 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 347 6 0 4 3.6 COc1ccccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
11360382 4975 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 359 7 0 3 4.6 CCCc1ccccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL105234 4975 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 359 7 0 3 4.6 CCCc1ccccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
11795245 111212 0 None 25 3 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 399 6 1 4 4.1 COc1cccc2c1CCCC2NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm991138z
CHEMBL2112375 111212 0 None 25 3 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 399 6 1 4 4.1 COc1cccc2c1CCCC2NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm991138z
CHEMBL328681 111212 0 None 25 3 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 399 6 1 4 4.1 COc1cccc2c1CCCC2NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm991138z
57394285 70115 0 None 5 7 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 378 6 0 3 5.2 Fc1ccc(SCCCN2CCCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2012.01.022
CHEMBL1946125 70115 0 None 5 7 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 378 6 0 3 5.2 Fc1ccc(SCCCN2CCCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2012.01.022
11151920 79624 0 None 2 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 338 6 0 5 3.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(C)c1 10.1021/jm060279f
CHEMBL212903 79624 0 None 2 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 338 6 0 5 3.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(C)c1 10.1021/jm060279f
76325152 105890 0 None -3 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
CHEMBL3115579 105890 0 None -3 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
CHEMBL3139262 105890 0 None -3 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
109030343 170293 1 None 15 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 324 5 1 4 2.5 Cc1cccc(NC(=O)CCN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4454068 170293 1 None 15 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 324 5 1 4 2.5 Cc1cccc(NC(=O)CCN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
10065188 101133 0 None 3 3 Human 7.5 pKi = 7.5 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 329 4 1 3 2.9 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccccc1 10.1016/j.bmcl.2005.02.012
CHEMBL298763 101133 0 None 3 3 Human 7.5 pKi = 7.5 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 329 4 1 3 2.9 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccccc1 10.1016/j.bmcl.2005.02.012
49788940 18089 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 352 5 1 4 2.2 N#Cc1ccc(N2CCN(CCNC(=O)c3ccc(F)cc3)CC2)cc1 10.1021/jm100925m
CHEMBL1270422 18089 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 352 5 1 4 2.2 N#Cc1ccc(N2CCN(CCNC(=O)c3ccc(F)cc3)CC2)cc1 10.1021/jm100925m
10424961 205252 0 None -3 3 Human 6.5 pKi = 6.5 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 301 1 0 1 5.0 CC1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00004a016
CHEMBL544184 205252 0 None -3 3 Human 6.5 pKi = 6.5 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 301 1 0 1 5.0 CC1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00004a016
CHEMBL91350 205252 0 None -3 3 Human 6.5 pKi = 6.5 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 301 1 0 1 5.0 CC1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00004a016
10424961 205252 0 None -3 3 Human 6.5 pKi = 6.5 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 301 1 0 1 5.0 CC1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL544184 205252 0 None -3 3 Human 6.5 pKi = 6.5 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 301 1 0 1 5.0 CC1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL91350 205252 0 None -3 3 Human 6.5 pKi = 6.5 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 301 1 0 1 5.0 CC1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
9980998 30819 0 None -1148 8 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in CHO cellsInhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in CHO cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
CHEMBL139926 30819 0 None -1148 8 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in CHO cellsInhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in CHO cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
CHEMBL2112911 30819 0 None -1148 8 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in CHO cellsInhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in CHO cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
44538690 109363 0 None -354 7 Human 6.5 pKi = 6.5 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 380 5 0 4 3.9 O=C(CCCN1CC[C@H]2[C@@H](C1)c1cccc3c1N2CCO3)c1ccc(F)cc1 10.1021/jm401958n
CHEMBL3233432 109363 0 None -354 7 Human 6.5 pKi = 6.5 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 380 5 0 4 3.9 O=C(CCCN1CC[C@H]2[C@@H](C1)c1cccc3c1N2CCO3)c1ccc(F)cc1 10.1021/jm401958n
72737750 114025 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 299 5 0 2 3.7 Fc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
CHEMBL3335543 114025 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 299 5 0 2 3.7 Fc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
137640152 156212 0 None -1995 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 631 15 3 10 4.0 CCCCn1cc(CCCOc2ccc(C(=O)NCCCN3CCCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2OC)nn1 10.1021/acs.jmedchem.7b00363
CHEMBL4070604 156212 0 None -1995 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 631 15 3 10 4.0 CCCCn1cc(CCCOc2ccc(C(=O)NCCCN3CCCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2OC)nn1 10.1021/acs.jmedchem.7b00363
155514430 169297 0 None -14 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 310 6 0 3 3.8 CCCCN1CCN(c2cc(CC)cc(Cl)c2OC)CC1 10.1021/acs.jmedchem.6b00860
CHEMBL4440301 169297 0 None -14 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 310 6 0 3 3.8 CCCCN1CCN(c2cc(CC)cc(Cl)c2OC)CC1 10.1021/acs.jmedchem.6b00860
168270455 189440 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 406 5 1 2 5.8 Fc1cc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
CHEMBL5171772 189440 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 406 5 1 2 5.8 Fc1cc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
155195501 169526 0 None -28 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 410 7 2 6 3.2 C[C@H]1COC(c2ccc(N)nc2)CN1CCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.9b00702
CHEMBL4443441 169526 0 None -28 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 410 7 2 6 3.2 C[C@H]1COC(c2ccc(N)nc2)CN1CCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.9b00702
44355433 21979 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 383 8 0 3 5.9 CCCN(CCc1cccs1)C1CCc2c(cccc2OC2CCCC2)C1 10.1021/jm960345l
CHEMBL132261 21979 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 383 8 0 3 5.9 CCCN(CCc1cccs1)C1CCc2c(cccc2OC2CCCC2)C1 10.1021/jm960345l
10642702 38973 0 None -2 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 366 4 1 3 4.6 OC1(c2ccc(Cl)cc2)CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1021/jm00025a013
CHEMBL147003 38973 0 None -2 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 366 4 1 3 4.6 OC1(c2ccc(Cl)cc2)CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1021/jm00025a013
12997413 7049 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 479 6 1 3 5.5 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1Cc1ccccc1-2 10.1021/jm010146o
CHEMBL108527 7049 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 479 6 1 3 5.5 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1Cc1ccccc1-2 10.1021/jm010146o
44431494 148218 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 345 4 1 3 3.6 O=C(NC1CCN(Cc2cccnc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
CHEMBL394042 148218 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 345 4 1 3 3.6 O=C(NC1CCN(Cc2cccnc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
154725389 176074 1 None -3 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 11 0 6 5.6 COc1ccc(F)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)C(C)C 10.1021/acs.jmedchem.9b01835
CHEMBL4453405 176074 1 None -3 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 11 0 6 5.6 COc1ccc(F)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)C(C)C 10.1021/acs.jmedchem.9b01835
CHEMBL4598003 176074 1 None -3 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 11 0 6 5.6 COc1ccc(F)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)C(C)C 10.1021/acs.jmedchem.9b01835
3198 203802 73 None -26 34 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 203802 73 None -26 34 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 203802 73 None -26 34 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
122180569 121207 0 None -208 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 479 8 0 6 5.0 COc1ccccc1N1CCN(CCCCc2cn(-c3ccc4c(c3)Cc3ccccc3-4)nn2)CC1 10.1016/j.bmc.2015.01.017
CHEMBL3588914 121207 0 None -208 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 479 8 0 6 5.0 COc1ccccc1N1CCN(CCCCc2cn(-c3ccc4c(c3)Cc3ccccc3-4)nn2)CC1 10.1016/j.bmc.2015.01.017
44431459 86894 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 378 4 1 2 4.9 O=C(NC1CCN(Cc2ccccc2Cl)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
CHEMBL233214 86894 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 378 4 1 2 4.9 O=C(NC1CCN(Cc2ccccc2Cl)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
53248361 61753 0 None -213 7 Human 6.5 pKi = 6.5 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 568 7 0 5 3.2 COc1ccccc1N1CCN(CCN(C(=O)C23C4C5C2C2C3C4C52I)c2ccccn2)CC1 10.1021/jm1009956
CHEMBL1774991 61753 0 None -213 7 Human 6.5 pKi = 6.5 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 568 7 0 5 3.2 COc1ccccc1N1CCN(CCN(C(=O)C23C4C5C2C2C3C4C52I)c2ccccn2)CC1 10.1021/jm1009956
10782049 19826 0 None 10 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 321 9 1 3 4.5 Clc1ccc(SCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
CHEMBL130347 19826 0 None 10 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 321 9 1 3 4.5 Clc1ccc(SCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
155515759 169438 0 None 3 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 533 12 2 7 4.1 COc1ccc(N(Cc2cccc(OC)c2)NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1021/acs.jmedchem.9b01085
CHEMBL4442419 169438 0 None 3 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 533 12 2 7 4.1 COc1ccc(N(Cc2cccc(OC)c2)NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1021/acs.jmedchem.9b01085
109030515 175412 1 None 12 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 325 5 1 5 1.9 Cc1cccc(NC(=O)CCN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4588808 175412 1 None 12 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 325 5 1 5 1.9 Cc1cccc(NC(=O)CCN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
25070419 111286 0 None -9 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3cc4ccccn4n3)CC2)c1Cl 10.1021/jm5004039
CHEMBL3287394 111286 0 None -9 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3cc4ccccn4n3)CC2)c1Cl 10.1021/jm5004039
44405414 71476 0 None 1148 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 380 5 1 3 4.6 O=C(N[C@H]1CCN(Cc2ccccc2F)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
CHEMBL196866 71476 0 None 1148 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 380 5 1 3 4.6 O=C(N[C@H]1CCN(Cc2ccccc2F)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
11678172 77678 0 None -72 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 531 8 1 4 5.6 COc1c(Cl)cccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm060138d
CHEMBL209876 77678 0 None -72 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 531 8 1 4 5.6 COc1c(Cl)cccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm060138d
118709160 112907 0 None -2 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 846 18 0 8 10.1 O=C(CCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318832 112907 0 None -2 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 846 18 0 8 10.1 O=C(CCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
118709173 112922 0 None -19 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 944 20 0 10 9.4 O=C(CCN1CCN(CCC(=O)OC2(c3ccc(Cl)cc3)CCN(CCCC(=O)c3ccc(F)cc3)CC2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318846 112922 0 None -19 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 944 20 0 10 9.4 O=C(CCN1CCN(CCC(=O)OC2(c3ccc(Cl)cc3)CCN(CCCC(=O)c3ccc(F)cc3)CC2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
22727324 13317 0 None -1 3 Human 7.5 pKi = 7.5 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 409 8 0 5 4.6 COc1ccccc1N1CCN(CCCCc2cc(-c3ccc(F)cc3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL1192902 13317 0 None -1 3 Human 7.5 pKi = 7.5 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 409 8 0 5 4.6 COc1ccccc1N1CCN(CCCCc2cc(-c3ccc(F)cc3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL544220 13317 0 None -1 3 Human 7.5 pKi = 7.5 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 409 8 0 5 4.6 COc1ccccc1N1CCN(CCCCc2cc(-c3ccc(F)cc3)no2)CC1 10.1016/s0960-894x(02)00179-8
681 1437 65 None -2 38 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
940 1437 65 None -2 38 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
947 1437 65 None -2 38 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
CHEMBL59 1437 65 None -2 38 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
DB00988 1437 65 None -2 38 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
9975465 187068 0 None 109 3 Human 7.5 pKi = 7.5 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL49502 187068 0 None 109 3 Human 7.5 pKi = 7.5 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.02.012
10086123 110996 0 None -9 3 Human 6.5 pKi = 6.5 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 299 1 0 1 4.9 C=C1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL327713 110996 0 None -9 3 Human 6.5 pKi = 6.5 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 299 1 0 1 4.9 C=C1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
72205045 91514 0 None -1 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 380 6 0 4 4.3 Clc1ccc(-n2cc(CCCN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2013.05.027
CHEMBL2414356 91514 0 None -1 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 380 6 0 4 4.3 Clc1ccc(-n2cc(CCCN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2013.05.027
44436606 91565 0 None -102 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 505 7 1 3 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(C#Cc2ccccc2)cc1 10.1016/j.bmc.2007.08.038
CHEMBL241641 91565 0 None -102 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 505 7 1 3 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(C#Cc2ccccc2)cc1 10.1016/j.bmc.2007.08.038
102262219 139529 0 None -6918 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 488 12 4 6 4.1 COc1cc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800400 139529 0 None -6918 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 488 12 4 6 4.1 COc1cc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
15508238 4727 0 None 2 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 340 3 0 2 4.7 C(#Cc1cccn1C1CCN(Cc2ccccc2)CC1)c1ccccc1 10.1016/s0960-894x(99)00540-5
CHEMBL104092 4727 0 None 2 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 340 3 0 2 4.7 C(#Cc1cccn1C1CCN(Cc2ccccc2)CC1)c1ccccc1 10.1016/s0960-894x(99)00540-5
44319370 106564 0 None 1 4 Human 5.5 pKi = 5.5 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 443 5 0 5 3.8 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)[C@@H](C)O1 10.1016/s0960-894x(01)00484-x
CHEMBL315564 106564 0 None 1 4 Human 5.5 pKi = 5.5 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 443 5 0 5 3.8 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)[C@@H](C)O1 10.1016/s0960-894x(01)00484-x
134156222 153817 0 None -50 8 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 334 5 1 3 3.2 O=C1Cc2cc(C(=O)CCCN3CCc4ccccc4C3)ccc2N1 10.1016/j.bmc.2016.09.019
CHEMBL3986927 153817 0 None -50 8 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 334 5 1 3 3.2 O=C1Cc2cc(C(=O)CCCN3CCc4ccccc4C3)ccc2N1 10.1016/j.bmc.2016.09.019
44283889 119616 0 None - 1 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 365 5 0 4 3.0 COc1ccc(N2CCN(CCC3c4ccccc4C(=O)N3C)CC2)cc1 10.1016/s0960-894x(98)00252-2
CHEMBL35114 119616 0 None - 1 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 365 5 0 4 3.0 COc1ccc(N2CCN(CCC3c4ccccc4C(=O)N3C)CC2)cc1 10.1016/s0960-894x(98)00252-2
134156222 153817 0 None -50 8 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 334 5 1 3 3.2 O=C1Cc2cc(C(=O)CCCN3CCc4ccccc4C3)ccc2N1 10.1016/j.bmc.2016.09.019
CHEMBL3986927 153817 0 None -50 8 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 334 5 1 3 3.2 O=C1Cc2cc(C(=O)CCCN3CCc4ccccc4C3)ccc2N1 10.1016/j.bmc.2016.09.019
130431337 173515 0 None -2344 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 438 8 2 3 4.7 CCc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4544583 173515 0 None -2344 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 438 8 2 3 4.7 CCc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
44336052 5362 0 None 19 2 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 4 0 3 3.8 C[C@H]1CN(Cc2ccc(Cl)cc2)[C@H](C)CN1CC(=O)N1CCc2ccccc21 10.1016/s0960-894x(02)00655-8
CHEMBL107351 5362 0 None 19 2 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 4 0 3 3.8 C[C@H]1CN(Cc2ccc(Cl)cc2)[C@H](C)CN1CC(=O)N1CCc2ccccc21 10.1016/s0960-894x(02)00655-8
10801405 26202 1 None -1 3 Human 6.5 pKi = 6.5 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 261 6 0 2 3.7 CCCN(CCC)[C@H]1CCc2ccc(OC)cc2C1 10.1021/jm960345l
CHEMBL135944 26202 1 None -1 3 Human 6.5 pKi = 6.5 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 261 6 0 2 3.7 CCCN(CCC)[C@H]1CCc2ccc(OC)cc2C1 10.1021/jm960345l
44393403 64747 0 None -125 6 Human 6.5 pKi = 6.5 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 533 8 1 5 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(I)ccc3o2)CC1 10.1021/jm900095y
CHEMBL182379 64747 0 None -125 6 Human 6.5 pKi = 6.5 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 533 8 1 5 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(I)ccc3o2)CC1 10.1021/jm900095y
53248213 61705 0 None -851 5 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 462 7 2 3 4.8 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm200288r
CHEMBL1774535 61705 0 None -851 5 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 462 7 2 3 4.8 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm200288r
164627741 185923 0 None -128 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 427 6 2 5 3.8 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1cccc(C#N)c1)CC2 10.1016/j.bmcl.2021.128047
CHEMBL4877460 185923 0 None -128 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 427 6 2 5 3.8 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1cccc(C#N)c1)CC2 10.1016/j.bmcl.2021.128047
71062708 153772 0 None -19 12 Mouse 5.5 pKi = 5.5 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 368 7 0 5 2.8 COc1cccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL3986651 153772 0 None -19 12 Mouse 5.5 pKi = 5.5 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 368 7 0 5 2.8 COc1cccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
168294968 191821 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3cn4ccccc4n3)CC2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5208124 191821 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3cn4ccccc4n3)CC2)cc1F 10.1016/j.bmcl.2022.128615
10276451 198601 33 None -2754 10 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm0611152
CHEMBL2112910 198601 33 None -2754 10 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm0611152
CHEMBL59725 198601 33 None -2754 10 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm0611152
25895957 4775 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 414 5 0 5 3.0 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2cc([N+](=O)[O-])ccc21 10.1016/s0960-894x(02)00655-8
CHEMBL104251 4775 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 414 5 0 5 3.0 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2cc([N+](=O)[O-])ccc21 10.1016/s0960-894x(02)00655-8
10641954 205204 0 None 77 2 Human 7.5 pKi = 7.5 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 355 3 0 4 4.0 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccccc1Cl)CC3 10.1021/jm970170v
CHEMBL91067 205204 0 None 77 2 Human 7.5 pKi = 7.5 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 355 3 0 4 4.0 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccccc1Cl)CC3 10.1021/jm970170v
10335148 78476 0 None -3 3 Human 7.5 pKi = 7.5 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 303 4 1 2 3.9 C1=C(c2ccccc2)CCN(CCc2c[nH]c3ncccc23)C1 10.1016/s0960-894x(99)00025-6
CHEMBL2112912 78476 0 None -3 3 Human 7.5 pKi = 7.5 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 303 4 1 2 3.9 C1=C(c2ccccc2)CCN(CCc2c[nH]c3ncccc23)C1 10.1016/s0960-894x(99)00025-6
21465540 110927 1 None - 1 Human 7.5 pKi = 7.5 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 337 4 2 3 2.8 O=C(NC(=O)c1ccccc1)NC1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL327310 110927 1 None - 1 Human 7.5 pKi = 7.5 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 337 4 2 3 2.8 O=C(NC(=O)c1ccccc1)NC1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
2946349 99272 6 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 325 7 1 3 3.4 OC(COc1ccccc1)CN1CCC(Cc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
CHEMBL284892 99272 6 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 325 7 1 3 3.4 OC(COc1ccccc1)CN1CCC(Cc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
9975465 187068 0 None 109 3 Human 7.5 pKi = 7.5 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1021/jm970021c
CHEMBL49502 187068 0 None 109 3 Human 7.5 pKi = 7.5 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1021/jm970021c
44403210 70199 0 None -7 5 Human 7.5 pKi = 7.5 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 385 8 1 4 3.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2005.07.037
CHEMBL194727 70199 0 None -7 5 Human 7.5 pKi = 7.5 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 385 8 1 4 3.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2005.07.037
10137748 52781 0 None 28 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 433 4 0 4 3.8 COc1cc(C)ccc1CN1CCN(C2CCc3cccc4c3N(C2=O)C(C)(C)C4)CC1 10.1016/s0960-894x(02)01056-9
CHEMBL159742 52781 0 None 28 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 433 4 0 4 3.8 COc1cc(C)ccc1CN1CCN(C2CCc3cccc4c3N(C2=O)C(C)(C)C4)CC1 10.1016/s0960-894x(02)01056-9
71652196 87026 0 None 15 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation counting
ChEMBL 368 4 1 5 3.6 Oc1ccc(N2CCN(Cc3cnn(-c4ccc(Cl)cc4)c3)CC2)cc1 10.1016/j.ejmech.2012.08.011
CHEMBL2333732 87026 0 None 15 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation counting
ChEMBL 368 4 1 5 3.6 Oc1ccc(N2CCN(Cc3cnn(-c4ccc(Cl)cc4)c3)CC2)cc1 10.1016/j.ejmech.2012.08.011
191 399 92 None -8 28 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1021/jm2013419
201 399 92 None -8 28 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1021/jm2013419
2170 399 92 None -8 28 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1021/jm2013419
CHEMBL1113 399 92 None -8 28 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1021/jm2013419
DB00543 399 92 None -8 28 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1021/jm2013419
44431481 87607 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 422 4 1 2 5.0 O=C(NC1CCN(Cc2ccc(Br)cc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
CHEMBL234472 87607 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 422 4 1 2 5.0 O=C(NC1CCN(Cc2ccc(Br)cc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
137643951 157714 0 None -23 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 421 8 1 7 2.7 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(C=O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4088639 157714 0 None -23 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 421 8 1 7 2.7 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(C=O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
16105549 67443 0 None -75 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 462 9 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccc(F)nc3)cc2)CC1 10.1021/jm0611152
CHEMBL1908879 67443 0 None -75 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 462 9 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccc(F)nc3)cc2)CC1 10.1021/jm0611152
CHEMBL221640 67443 0 None -75 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 462 9 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccc(F)nc3)cc2)CC1 10.1021/jm0611152
122181330 121357 0 None -39 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 396 9 1 3 5.3 CCCN(CCCCNC(=O)/N=N/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3590081 121357 0 None -39 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 396 9 1 3 5.3 CCCN(CCCCNC(=O)/N=N/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
56833378 67991 0 None -18 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 1121 39 2 14 10.7 CCCN(CCCCNC(=O)c1ccc(OCCCc2cn(CCCCCCCCn3cc(CCCOc4ccc(C(=O)NCCCCN(CCC)C5Cc6ccccc6C5)cc4OC)nn3)nn2)c(OC)c1)C1Cc2ccccc2C1 10.1021/jm2009919
CHEMBL1916549 67991 0 None -18 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 1121 39 2 14 10.7 CCCN(CCCCNC(=O)c1ccc(OCCCc2cn(CCCCCCCCn3cc(CCCOc4ccc(C(=O)NCCCCN(CCC)C5Cc6ccccc6C5)cc4OC)nn3)nn2)c(OC)c1)C1Cc2ccccc2C1 10.1021/jm2009919
44276050 13169 0 None -3 3 Human 7.5 pKi = 7.5 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 405 9 0 5 4.9 CCOc1ccccc1N1CCN(CCCCc2cc(-c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL1191675 13169 0 None -3 3 Human 7.5 pKi = 7.5 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 405 9 0 5 4.9 CCOc1ccccc1N1CCN(CCCCc2cc(-c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL542809 13169 0 None -3 3 Human 7.5 pKi = 7.5 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 405 9 0 5 4.9 CCOc1ccccc1N1CCN(CCCCc2cc(-c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
22727331 13216 0 None -5 3 Human 7.5 pKi = 7.5 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 451 10 0 7 4.5 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4OC)CC3)on2)c(OC)c1 10.1016/s0960-894x(02)00179-8
CHEMBL1192096 13216 0 None -5 3 Human 7.5 pKi = 7.5 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 451 10 0 7 4.5 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4OC)CC3)on2)c(OC)c1 10.1016/s0960-894x(02)00179-8
CHEMBL543278 13216 0 None -5 3 Human 7.5 pKi = 7.5 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 451 10 0 7 4.5 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4OC)CC3)on2)c(OC)c1 10.1016/s0960-894x(02)00179-8
44438228 93123 0 None 1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 354 4 1 2 5.0 COC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246438 93123 0 None 1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 354 4 1 2 5.0 COC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
19958494 98994 0 None 9 4 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 360 3 1 3 3.9 FC(F)(F)c1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
CHEMBL283036 98994 0 None 9 4 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 360 3 1 3 3.9 FC(F)(F)c1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
127052467 140320 0 None 1 7 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 1 1 4.5 c1ccc2c(c1)CCN(CCCCc1c[nH]c3ccccc13)C2 10.1016/j.bmc.2016.05.053
CHEMBL3819494 140320 0 None 1 7 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 1 1 4.5 c1ccc2c(c1)CCN(CCCCc1c[nH]c3ccccc13)C2 10.1016/j.bmc.2016.05.053
10276451 198601 33 None -2754 10 Human 6.5 pKi = 6.5 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm049612a
CHEMBL2112910 198601 33 None -2754 10 Human 6.5 pKi = 6.5 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm049612a
CHEMBL59725 198601 33 None -2754 10 Human 6.5 pKi = 6.5 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm049612a
10276451 198601 33 None -2754 10 Human 6.5 pKi = 6.5 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm025558r
CHEMBL2112910 198601 33 None -2754 10 Human 6.5 pKi = 6.5 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm025558r
CHEMBL59725 198601 33 None -2754 10 Human 6.5 pKi = 6.5 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm025558r
10276451 198601 33 None -2754 10 Human 6.5 pKi = 6.5 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2005.07.037
CHEMBL2112910 198601 33 None -2754 10 Human 6.5 pKi = 6.5 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2005.07.037
CHEMBL59725 198601 33 None -2754 10 Human 6.5 pKi = 6.5 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2005.07.037
10276451 198601 33 None -2754 10 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2004.05.052
CHEMBL2112910 198601 33 None -2754 10 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2004.05.052
CHEMBL59725 198601 33 None -2754 10 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2004.05.052
44381117 57526 0 None 25 4 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 415 7 2 4 3.6 COc1cc(NC(C)=O)c(Cl)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL167032 57526 0 None 25 4 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 415 7 2 4 3.6 COc1cc(NC(C)=O)c(Cl)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
72545010 92693 0 None 7 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 437 6 3 10 -0.4 COc1ccccc1N1CCN(Cc2cn([C@@H]3O[C@H](CF)[C@@H](O)[C@H](O)[C@H]3O)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443003 92693 0 None 7 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 437 6 3 10 -0.4 COc1ccccc1N1CCN(Cc2cn([C@@H]3O[C@H](CF)[C@@H](O)[C@H](O)[C@H]3O)nn2)CC1 10.1016/j.bmcl.2013.09.026
44319102 204421 0 None 2 4 Human 6.5 pKi = 6.5 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 321 4 0 4 2.7 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CO2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL86060 204421 0 None 2 4 Human 6.5 pKi = 6.5 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 321 4 0 4 2.7 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CO2)cc1 10.1016/s0960-894x(01)00484-x
10276451 198601 33 None -2754 10 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in CHO cellsInhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in CHO cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm040190e
CHEMBL2112910 198601 33 None -2754 10 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in CHO cellsInhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in CHO cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm040190e
CHEMBL59725 198601 33 None -2754 10 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in CHO cellsInhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in CHO cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm040190e
45483654 196441 0 None -14 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 1047 23 2 14 8.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(-c3cn(Cc4ccc(-c5ccc(Cn6cc(-c7cccc(C(=O)NCCCCN8CCN(c9ccccc9OC)CC8)c7)nn6)cc5)cc4)nn3)c2)CC1 10.1021/jm901120h
CHEMBL574569 196441 0 None -14 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 1047 23 2 14 8.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(-c3cn(Cc4ccc(-c5ccc(Cn6cc(-c7cccc(C(=O)NCCCCN8CCN(c9ccccc9OC)CC8)c7)nn6)cc5)cc4)nn3)c2)CC1 10.1021/jm901120h
135545150 38236 0 None - 1 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 341 3 2 5 3.6 Clc1ccc2c(c1)C(NCCN1CCCC1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL146410 38236 0 None - 1 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 341 3 2 5 3.6 Clc1ccc2c(c1)C(NCCN1CCCC1)=Nc1cccnc1N2 10.1021/jm0104825
71658076 89971 0 None -38 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 463 9 1 5 5.1 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(-c3ccccc3)s2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386615 89971 0 None -38 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 463 9 1 5 5.1 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(-c3ccccc3)s2)CC1 10.1016/j.bmc.2013.03.074
60165539 75002 0 None 5 3 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 399 6 0 5 4.7 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL2037524 75002 0 None 5 3 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 399 6 0 5 4.7 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL5075990 212636 0 None -31 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCc1cc(Cl)c(OC)c(C(=O)NCC2CCCN2CCCCNCCC(C(=O)N(C)C)(c2ccccc2)c2ccccc2)c1O 10.1021/acs.jmedchem.1c00611
168291477 191284 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccccc3C)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5199649 191284 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccccc3C)C2)cc1F 10.1016/j.bmcl.2022.128615
42626318 55943 0 None -3090 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 460 7 3 4 3.8 O=C(NCC[C@@H](O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
CHEMBL1627306 55943 0 None -3090 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 460 7 3 4 3.8 O=C(NCC[C@@H](O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
49799693 14280 0 None -25 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 446 6 2 3 4.8 OC1(c2ccc(Br)cc2)CCN(Cc2c[nH]c3ccc(OCCF)cc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1173366 14280 0 None -25 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 446 6 2 3 4.8 OC1(c2ccc(Br)cc2)CCN(Cc2c[nH]c3ccc(OCCF)cc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1200278 14280 0 None -25 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 446 6 2 3 4.8 OC1(c2ccc(Br)cc2)CCN(Cc2c[nH]c3ccc(OCCF)cc23)CC1 10.1016/j.bmc.2010.05.052
11144835 119188 0 None -114 4 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 449 9 1 4 4.7 COc1cccc(C(=O)NCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1021/jm020952a
CHEMBL347290 119188 0 None -114 4 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 449 9 1 4 4.7 COc1cccc(C(=O)NCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1021/jm020952a
127051843 140220 0 None -15 9 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 0 3 3.6 N#Cc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818200 140220 0 None -15 9 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 0 3 3.6 N#Cc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
44395714 12756 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 385 6 0 2 5.9 O=C(CCCN1C2CCC1CC(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
CHEMBL1188714 12756 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 385 6 0 2 5.9 O=C(CCCN1C2CCC1CC(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
CHEMBL537182 12756 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 385 6 0 2 5.9 O=C(CCCN1C2CCC1CC(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
11849181 79650 0 None -2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 372 6 0 5 3.5 CO/N=C(/c1ccc(Cl)cc1)C(C)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
CHEMBL213004 79650 0 None -2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 372 6 0 5 3.5 CO/N=C(/c1ccc(Cl)cc1)C(C)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
60165411 75007 0 None -95 5 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 381 7 0 7 3.3 O=C(CCCCN1CCN(c2ncccn2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL2037529 75007 0 None -95 5 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 381 7 0 7 3.3 O=C(CCCCN1CCN(c2ncccn2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
22727356 13215 0 None -12 3 Human 6.5 pKi = 6.5 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 387 8 0 4 5.0 C(=C/c1cc(CCCCN2CCN(c3ccccc3)CC2)on1)\c1ccccc1 10.1016/s0960-894x(02)00179-8
CHEMBL1192095 13215 0 None -12 3 Human 6.5 pKi = 6.5 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 387 8 0 4 5.0 C(=C/c1cc(CCCCN2CCN(c3ccccc3)CC2)on1)\c1ccccc1 10.1016/s0960-894x(02)00179-8
CHEMBL543277 13215 0 None -12 3 Human 6.5 pKi = 6.5 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 387 8 0 4 5.0 C(=C/c1cc(CCCCN2CCN(c3ccccc3)CC2)on1)\c1ccccc1 10.1016/s0960-894x(02)00179-8
127051843 140220 0 None -15 9 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 0 3 3.6 N#Cc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818200 140220 0 None -15 9 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 0 3 3.6 N#Cc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
44438220 93017 0 None -4 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 381 4 2 2 4.4 CC(=O)NC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246021 93017 0 None -4 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 381 4 2 2 4.4 CC(=O)NC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
12066265 96664 0 None -1 4 Human 6.5 pKi = 6.5 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 487 6 0 2 7.6 Fc1ccc(C(OC2CC3CCC(C2)N3Cc2ccc(Cl)c(Cl)c2)c2ccc(F)cc2)cc1 10.1021/jm010146o
CHEMBL267562 96664 0 None -1 4 Human 6.5 pKi = 6.5 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 487 6 0 2 7.6 Fc1ccc(C(OC2CC3CCC(C2)N3Cc2ccc(Cl)c(Cl)c2)c2ccc(F)cc2)cc1 10.1021/jm010146o
44339953 109212 0 None 3 4 Human 7.5 pKi = 7.5 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 5 2 4 3.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C[C@@H]1C 10.1016/s0960-894x(03)00678-4
CHEMBL322802 109212 0 None 3 4 Human 7.5 pKi = 7.5 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 5 2 4 3.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C[C@@H]1C 10.1016/s0960-894x(03)00678-4
10436653 32573 0 None -51 5 Human 7.5 pKi = 7.5 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 521 8 1 4 3.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3[te]2)CC1 10.1021/jm025558r
CHEMBL141419 32573 0 None -51 5 Human 7.5 pKi = 7.5 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 521 8 1 4 3.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3[te]2)CC1 10.1021/jm025558r
127031500 138820 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 323 5 0 5 2.6 c1ccc(OC[C@@H]2CN(Cc3ncn4ccccc34)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792931 138820 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 323 5 0 5 2.6 c1ccc(OC[C@@H]2CN(Cc3ncn4ccccc34)CCO2)cc1 10.1016/j.bmcl.2016.03.102
71460561 81410 0 None -4 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 435 6 0 5 4.5 O=C(c1cnc2ccccc2n1)N(CCN1CC=C(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL2164346 81410 0 None -4 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 435 6 0 5 4.5 O=C(c1cnc2ccccc2n1)N(CCN1CC=C(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
127052467 140320 0 None 1 7 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 1 1 4.5 c1ccc2c(c1)CCN(CCCCc1c[nH]c3ccccc13)C2 10.1016/j.bmc.2016.05.053
CHEMBL3819494 140320 0 None 1 7 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 1 1 4.5 c1ccc2c(c1)CCN(CCCCc1c[nH]c3ccccc13)C2 10.1016/j.bmc.2016.05.053
57391306 69816 0 None 6 5 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 379 6 0 2 4.9 [O-][S+](CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940407 69816 0 None 6 5 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 379 6 0 2 4.9 [O-][S+](CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2011.12.019
90644227 111288 0 None -26 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 448 8 1 6 4.1 OCc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287396 111288 0 None -26 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 448 8 1 6 4.1 OCc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
44436617 91129 0 None -1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 481 9 1 4 4.8 COc1ccccc1N1CCN(CCCCCNC(=O)c2cccc(C#Cc3ccccc3)c2)CC1 10.1016/j.bmc.2007.08.038
CHEMBL240584 91129 0 None -1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 481 9 1 4 4.8 COc1ccccc1N1CCN(CCCCCNC(=O)c2cccc(C#Cc3ccccc3)c2)CC1 10.1016/j.bmc.2007.08.038
11176211 4723 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 372 8 0 6 3.3 CCOc1ccccc1OCC1CN(Cc2ccc([N+](=O)[O-])cc2)CCO1 10.1021/jm031111m
CHEMBL104079 4723 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 372 8 0 6 3.3 CCOc1ccccc1OCC1CN(Cc2ccc([N+](=O)[O-])cc2)CCO1 10.1021/jm031111m
44283891 119685 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 363 4 0 3 3.6 Cc1ccc(N2CCN(CCC3c4ccccc4C(=O)N3C)CC2)cc1C 10.1016/s0960-894x(98)00252-2
CHEMBL35182 119685 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 363 4 0 3 3.6 Cc1ccc(N2CCN(CCC3c4ccccc4C(=O)N3C)CC2)cc1C 10.1016/s0960-894x(98)00252-2
90644059 111538 0 None 22 3 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 354 4 0 3 3.9 O=C1c2ccccc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
CHEMBL3289643 111538 0 None 22 3 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 354 4 0 3 3.9 O=C1c2ccccc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
10714184 78192 0 None 1 3 Human 6.5 pKi = 6.5 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 369 5 1 3 5.1 CC1(C(=O)/C=C(\O)c2ccc(Cl)cc2)CCN(Cc2ccccc2)CC1 10.1021/jm970111h
CHEMBL2112284 78192 0 None 1 3 Human 6.5 pKi = 6.5 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 369 5 1 3 5.1 CC1(C(=O)/C=C(\O)c2ccc(Cl)cc2)CCN(Cc2ccccc2)CC1 10.1021/jm970111h
10972865 202033 0 None -3 5 Human 6.5 pKi = 6.5 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 479 6 1 3 5.5 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm010146o
CHEMBL67750 202033 0 None -3 5 Human 6.5 pKi = 6.5 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 479 6 1 3 5.5 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm010146o
71657947 89966 0 None -93 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 415 8 1 4 4.1 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386610 89966 0 None -93 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 415 8 1 4 4.1 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2013.03.074
145986441 166619 0 None -102 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 432 7 2 4 3.7 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(Br)cc1)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4291172 166619 0 None -102 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 432 7 2 4 3.7 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(Br)cc1)CC2 10.1021/acsmedchemlett.8b00229
12050198 198570 0 None 17 4 Human 6.5 pKi = 6.5 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 347 6 1 4 4.1 c1ccc(CN2CCC(NCc3coc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
CHEMBL59702 198570 0 None 17 4 Human 6.5 pKi = 6.5 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 347 6 1 4 4.1 c1ccc(CN2CCC(NCc3coc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
92716 71988 20 None 5 2 Human 6.5 pKi = 6.5 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 301 2 4 5 2.3 CN1CCc2cc(O)c(O)cc2C1Cc1ccc(O)c(O)c1 10.1016/S0960-894X(97)00194-7
CHEMBL19844 71988 20 None 5 2 Human 6.5 pKi = 6.5 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 301 2 4 5 2.3 CN1CCc2cc(O)c(O)cc2C1Cc1ccc(O)c(O)c1 10.1016/S0960-894X(97)00194-7
44381286 119861 0 None -1 4 Human 5.5 pKi = 5.5 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 442 5 1 5 3.4 COc1ccc(Br)cc1C1=NCC[C@@H](CN2CCN(c3ccccc3)CC2)N1 10.1016/s0960-894x(03)00004-0
CHEMBL353220 119861 0 None -1 4 Human 5.5 pKi = 5.5 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 442 5 1 5 3.4 COc1ccc(Br)cc1C1=NCC[C@@H](CN2CCN(c3ccccc3)CC2)N1 10.1016/s0960-894x(03)00004-0
380039 14193 4 None -5 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 391 3 0 4 4.2 CN1CN(c2ccccc2)C2(CCN(Cc3csc4ccccc34)CC2)C1=O 10.1016/j.bmc.2010.05.052
CHEMBL1169728 14193 4 None -5 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 391 3 0 4 4.2 CN1CN(c2ccccc2)C2(CCN(Cc3csc4ccccc34)CC2)C1=O 10.1016/j.bmc.2010.05.052
CHEMBL1199909 14193 4 None -5 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 391 3 0 4 4.2 CN1CN(c2ccccc2)C2(CCN(Cc3csc4ccccc34)CC2)C1=O 10.1016/j.bmc.2010.05.052
44438224 154099 0 None -60 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 396 5 1 3 4.9 CCOC(=O)C1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL399396 154099 0 None -60 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 396 5 1 3 4.9 CCOC(=O)C1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
122180570 121208 0 None -114 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 430 8 1 6 3.9 COc1ccccc1N1CCN(CCCCc2cn(-c3ccc4[nH]ccc4c3)nn2)CC1 10.1016/j.bmc.2015.01.017
CHEMBL3588915 121208 0 None -114 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 430 8 1 6 3.9 COc1ccccc1N1CCN(CCCCc2cn(-c3ccc4[nH]ccc4c3)nn2)CC1 10.1016/j.bmc.2015.01.017
44438199 150787 3 None -27 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 340 3 2 2 4.3 OC1(c2cccc(Cl)c2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL396092 150787 3 None -27 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 340 3 2 2 4.3 OC1(c2cccc(Cl)c2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL5091479 213536 1 None -4 2 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CN1CCC(c2ccccc2)(c2ccccc2)C1 10.1021/acs.jmedchem.1c00611
44330585 206567 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 300 2 0 3 4.8 CCCn1ncc2c1-c1c(Cl)sc(Cl)c1CCC2 10.1016/s0960-894x(03)00587-0
CHEMBL99085 206567 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 300 2 0 3 4.8 CCCn1ncc2c1-c1c(Cl)sc(Cl)c1CCC2 10.1016/s0960-894x(03)00587-0
130431325 171846 0 None -2290 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 439 8 1 4 5.0 CCc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4o3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4476699 171846 0 None -2290 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 439 8 1 4 5.0 CCc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4o3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
11809415 120450 0 None - 1 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 321 0 1 5 3.2 Cc1ccc2c(c1)C(N1CCCN(C)CC1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL356171 120450 0 None - 1 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 321 0 1 5 3.2 Cc1ccc2c(c1)C(N1CCCN(C)CC1)=Nc1cccnc1N2 10.1021/jm0104825
11784937 121361 12 None -11220 3 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2C[C@@H]3C[C@]3(c3ccc(C(F)(F)F)cc3F)C2)n1C 10.1021/jm501512b
CHEMBL3590085 121361 12 None -11220 3 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2C[C@@H]3C[C@]3(c3ccc(C(F)(F)F)cc3F)C2)n1C 10.1021/jm501512b
155195496 170149 0 None -72 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 407 7 3 5 3.1 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1CCCCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
CHEMBL4452064 170149 0 None -72 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 407 7 3 5 3.1 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1CCCCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
10063875 101851 0 None -389 5 Human 6.5 pKi = 6.5 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 308 4 2 3 2.7 O=C1Cc2c(ccc3c2O[C@@H](CNCc2ccccc2)CC3)N1 10.1016/s0960-894x(01)00778-8
CHEMBL303556 101851 0 None -389 5 Human 6.5 pKi = 6.5 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 308 4 2 3 2.7 O=C1Cc2c(ccc3c2O[C@@H](CNCc2ccccc2)CC3)N1 10.1016/s0960-894x(01)00778-8
56675269 66077 1 None -3 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 409 8 1 5 3.6 COc1ccc(N2CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)cc1 10.1016/j.bmc.2011.04.021
CHEMBL1813585 66077 1 None -3 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 409 8 1 5 3.6 COc1ccc(N2CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)cc1 10.1016/j.bmc.2011.04.021
CHEMBL1851858 66077 1 None -3 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 409 8 1 5 3.6 COc1ccc(N2CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)cc1 10.1016/j.bmc.2011.04.021
44394599 65902 0 None 85 2 Human 7.4 pKi = 7.4 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 384 6 1 3 4.2 O=Cc1ccccc1-c1ccc(C(=O)NC2CCN(Cc3ccccc3)C2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL184551 65902 0 None 85 2 Human 7.4 pKi = 7.4 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 384 6 1 3 4.2 O=Cc1ccccc1-c1ccc(C(=O)NC2CCN(Cc3ccccc3)C2)cc1 10.1016/j.bmcl.2004.07.045
135398737 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
38 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
722 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
CHEMBL42 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
DB00363 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
44436301 90201 0 None 4 4 Human 7.4 pKi = 7.4 Binding
Binding affinity to human D4RBinding affinity to human D4R
ChEMBL 433 6 0 5 3.1 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2021.128028
CHEMBL238915 90201 0 None 4 4 Human 7.4 pKi = 7.4 Binding
Binding affinity to human D4RBinding affinity to human D4R
ChEMBL 433 6 0 5 3.1 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2021.128028
10472143 118772 0 None -81 16 Human 7.4 pKi = 7.4 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
CHEMBL343755 118772 0 None -81 16 Human 7.4 pKi = 7.4 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
9867004 168702 0 None 5 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 423 4 0 3 4.4 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1c2ccccc2CC12CCCC2 10.1016/s0960-894x(02)00655-8
CHEMBL441274 168702 0 None 5 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 423 4 0 3 4.4 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1c2ccccc2CC12CCCC2 10.1016/s0960-894x(02)00655-8
155529568 170887 0 None 3 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 385 6 1 5 3.5 COc1ccccc1N1CCN(CCNC(=O)/N=N/c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4463276 170887 0 None 3 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 385 6 1 5 3.5 COc1ccccc1N1CCN(CCNC(=O)/N=N/c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
155554837 174064 0 None -2 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 387 4 0 4 3.8 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccc(Cl)cn2)CC1 10.1016/j.bmc.2020.115943
CHEMBL4558031 174064 0 None -2 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 387 4 0 4 3.8 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccc(Cl)cn2)CC1 10.1016/j.bmc.2020.115943
127031201 138845 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 372 6 0 5 3.5 COc1ccc(CN2CCO[C@H](COc3cccc(C#N)c3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3793131 138845 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 372 6 0 5 3.5 COc1ccc(CN2CCO[C@H](COc3cccc(C#N)c3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
127031513 138944 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1cccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)c1 10.1016/j.bmcl.2016.03.102
CHEMBL3794287 138944 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1cccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)c1 10.1016/j.bmcl.2016.03.102
90644059 111538 0 None 22 3 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 354 4 0 3 3.9 O=C1c2ccccc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
CHEMBL3289643 111538 0 None 22 3 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 354 4 0 3 3.9 O=C1c2ccccc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
16725931 150508 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 422 4 1 2 5.0 O=C(NC1CCN(Cc2cccc(Br)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
CHEMBL395867 150508 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 422 4 1 2 5.0 O=C(NC1CCN(Cc2cccc(Br)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
122181327 121354 0 None -50 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 431 8 1 5 4.4 COc1ccccc1N1CCN(CCCCNC(=O)/N=N/c2ccc(F)c(F)c2)CC1 10.1016/j.bmc.2014.12.012
CHEMBL3590078 121354 0 None -50 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 431 8 1 5 4.4 COc1ccccc1N1CCN(CCCCNC(=O)/N=N/c2ccc(F)c(F)c2)CC1 10.1016/j.bmc.2014.12.012
3802 201334 16 None -1 5 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 307 0 1 5 2.8 Cc1ccc2c(c1)C(N1CCN(C)CC1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL63329 201334 16 None -1 5 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 307 0 1 5 2.8 Cc1ccc2c(c1)C(N1CCN(C)CC1)=Nc1cccnc1N2 10.1021/jm0104825
72737723 2541 1 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 315 5 0 2 4.2 Clc1ccc(cc1)CN1CCO[C@@H](C1)CCc1ccccc1 10.1021/ml500267c
8440 2541 1 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 315 5 0 2 4.2 Clc1ccc(cc1)CN1CCO[C@@H](C1)CCc1ccccc1 10.1021/ml500267c
CHEMBL3335556 2541 1 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 315 5 0 2 4.2 Clc1ccc(cc1)CN1CCO[C@@H](C1)CCc1ccccc1 10.1021/ml500267c
155554837 174064 0 None -2 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 387 4 0 4 3.8 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccc(Cl)cn2)CC1 10.1016/j.bmc.2020.115943
CHEMBL4558031 174064 0 None -2 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 387 4 0 4 3.8 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccc(Cl)cn2)CC1 10.1016/j.bmc.2020.115943
76318473 105813 0 None -95 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 510 13 2 6 3.7 COc1ccccc1N1CCN(C/C=C/CNC(=O)c2cc3cc(OCCOCCF)ccc3[nH]2)CC1 10.1039/c3md00098b
CHEMBL3133868 105813 0 None -95 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 510 13 2 6 3.7 COc1ccccc1N1CCN(C/C=C/CNC(=O)c2cc3cc(OCCOCCF)ccc3[nH]2)CC1 10.1039/c3md00098b
CHEMBL3139054 105813 0 None -95 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 510 13 2 6 3.7 COc1ccccc1N1CCN(C/C=C/CNC(=O)c2cc3cc(OCCOCCF)ccc3[nH]2)CC1 10.1039/c3md00098b
57393627 68965 0 None -40 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1101 42 2 17 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928131 68965 0 None -40 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1101 42 2 17 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
118709162 112909 0 None -125 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 874 20 0 8 10.9 O=C(CCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318834 112909 0 None -125 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 874 20 0 8 10.9 O=C(CCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
45270861 193410 0 None 11 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 353 3 0 5 3.1 Cc1cc2nc(C)c(CN3CCN(c4ccc(F)cc4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
CHEMBL549638 193410 0 None 11 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 353 3 0 5 3.1 Cc1cc2nc(C)c(CN3CCN(c4ccc(F)cc4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
11078813 111526 0 None 6 4 Human 5.4 pKi = 5.4 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 356 4 1 5 2.8 OCc1cnn2cccc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1021/jm015522j
CHEMBL328925 111526 0 None 6 4 Human 5.4 pKi = 5.4 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 356 4 1 5 2.8 OCc1cnn2cccc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1021/jm015522j
10973768 107074 0 None -9332 10 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 563 6 1 8 4.4 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCn4c(=O)[nH]c5ccccc5c4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL318901 107074 0 None -9332 10 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 563 6 1 8 4.4 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCn4c(=O)[nH]c5ccccc5c4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
10276451 198601 33 None -2754 10 Human 5.4 pKi = 5.4 Binding
Inhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in CHO cellsInhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in CHO cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm040190e
CHEMBL2112910 198601 33 None -2754 10 Human 5.4 pKi = 5.4 Binding
Inhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in CHO cellsInhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in CHO cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm040190e
CHEMBL59725 198601 33 None -2754 10 Human 5.4 pKi = 5.4 Binding
Inhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in CHO cellsInhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in CHO cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm040190e
71086303 160263 0 None -1 2 Mouse 5.4 pKi = 5.4 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 373 6 0 5 2.9 Clc1cncc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL4114493 160263 0 None -1 2 Mouse 5.4 pKi = 5.4 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 373 6 0 5 2.9 Clc1cncc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
168293874 191581 0 None -83 11 Human 6.4 pKi = 6.4 Binding
Binding affinity to D4 receptor (unknown origin) assessed as inhibition constantBinding affinity to D4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 312 2 3 3 3.3 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5204071 191581 0 None -83 11 Human 6.4 pKi = 6.4 Binding
Binding affinity to D4 receptor (unknown origin) assessed as inhibition constantBinding affinity to D4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 312 2 3 3 3.3 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
44426502 141534 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 386 7 1 2 5.1 O=C(NC1CCN(CCCCc2ccccc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.096
CHEMBL387952 141534 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 386 7 1 2 5.1 O=C(NC1CCN(CCCCc2ccccc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.096
44309688 202294 0 None -19 5 Human 6.4 pKi = 6.4 Binding
Inhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cellsInhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cells
ChEMBL 491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2 10.1021/jm040190e
CHEMBL69571 202294 0 None -19 5 Human 6.4 pKi = 6.4 Binding
Inhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cellsInhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cells
ChEMBL 491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2 10.1021/jm040190e
25132869 102820 0 None -57 6 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptorDisplacement of [125I]IABN from human dopamine D4 receptor
ChEMBL 400 3 2 2 5.5 O[C@]1(c2ccc(Cl)c(Cl)c2)C[C@@H]2CC[C@H](C1)N2Cc1c[nH]c2ccccc12 10.1021/jm800532x
CHEMBL3084503 102820 0 None -57 6 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptorDisplacement of [125I]IABN from human dopamine D4 receptor
ChEMBL 400 3 2 2 5.5 O[C@]1(c2ccc(Cl)c(Cl)c2)C[C@@H]2CC[C@H](C1)N2Cc1c[nH]c2ccccc12 10.1021/jm800532x
44438221 148247 0 None -3 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 342 3 1 1 5.3 FC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL394065 148247 0 None -3 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 342 3 1 1 5.3 FC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
122181007 121282 0 None -15848 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 509 7 2 4 4.9 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)-c1ccccc1C2 10.1016/j.bmc.2015.01.017
CHEMBL3589652 121282 0 None -15848 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 509 7 2 4 4.9 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)-c1ccccc1C2 10.1016/j.bmc.2015.01.017
6674 2777 14 None -3019 8 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 493 7 1 3 5.9 O=C(c1ccc2c(c1)Cc1c2cccc1)NCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm501512b
9891901 2777 14 None -3019 8 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 493 7 1 3 5.9 O=C(c1ccc2c(c1)Cc1c2cccc1)NCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm501512b
CHEMBL300780 2777 14 None -3019 8 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 493 7 1 3 5.9 O=C(c1ccc2c(c1)Cc1c2cccc1)NCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm501512b
11812065 202322 5 None -91 5 Human 6.4 pKi = 6.4 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 431 6 0 4 4.2 O=C1c2ccccc2C(=O)N1CCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/jm010146o
CHEMBL69717 202322 5 None -91 5 Human 6.4 pKi = 6.4 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 431 6 0 4 4.2 O=C1c2ccccc2C(=O)N1CCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/jm010146o
CHEMBL5077645 212738 0 None -97723 4 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None Oc1cccc([C@@]23CCC[C@@H]([C@H]2O)N(C/C=C/c2ccccc2)CC3)c1 10.1021/acs.jmedchem.1c00611
10403435 13339 0 None 1 3 Human 7.4 pKi = 7.4 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 315 3 0 2 5.2 C=CCN1CC=C(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL1193072 13339 0 None 1 3 Human 7.4 pKi = 7.4 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 315 3 0 2 5.2 C=CCN1CC=C(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL544418 13339 0 None 1 3 Human 7.4 pKi = 7.4 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 315 3 0 2 5.2 C=CCN1CC=C(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
9820313 105713 0 None -1 4 Human 7.4 pKi = 7.4 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 361 4 2 3 4.1 FC(F)(F)c1nc2c3c(ccc2[nH]1)CCC(CNCc1ccccc1)O3 10.1016/s0960-894x(01)00778-8
CHEMBL313851 105713 0 None -1 4 Human 7.4 pKi = 7.4 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 361 4 2 3 4.1 FC(F)(F)c1nc2c3c(ccc2[nH]1)CCC(CNCc1ccccc1)O3 10.1016/s0960-894x(01)00778-8
44335896 5304 0 None 45 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 Cc1ccc2c(c1)CCN2C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL106998 5304 0 None 45 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 Cc1ccc2c(c1)CCN2C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
44336005 5370 0 None 60 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 415 4 0 3 4.0 CC1CCc2cc(F)ccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL107391 5370 0 None 60 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 415 4 0 3 4.0 CC1CCc2cc(F)ccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
57399494 70114 0 None 1 8 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 386 4 0 3 4.4 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2020.115943
CHEMBL1946124 70114 0 None 1 8 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 386 4 0 3 4.4 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2020.115943
155564110 174797 0 None -4 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 0 4 4.0 O=C(CCCN1CCCN(c2ccc(Cl)cn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL4574793 174797 0 None -4 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 0 4 4.0 O=C(CCCN1CCCN(c2ccc(Cl)cn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
57399494 70114 0 None -1 8 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 386 4 0 3 4.4 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2012.01.022
CHEMBL1946124 70114 0 None -1 8 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 386 4 0 3 4.4 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2012.01.022
134146195 154054 0 None -3 9 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 362 5 0 3 5.8 Clc1ccc2sc(CCCCN3CCC4CCCCC4C3)nc2c1 10.1016/j.bmc.2016.09.019
CHEMBL3941795 154054 0 None -3 9 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 362 5 0 3 5.8 Clc1ccc2sc(CCCCN3CCC4CCCCC4C3)nc2c1 10.1016/j.bmc.2016.09.019
CHEMBL3991399 154054 0 None -3 9 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 362 5 0 3 5.8 Clc1ccc2sc(CCCCN3CCC4CCCCC4C3)nc2c1 10.1016/j.bmc.2016.09.019
127032084 138811 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 322 5 1 3 3.4 c1ccc(OC[C@@H]2CN(Cc3cccc4cc[nH]c34)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792813 138811 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 322 5 1 3 3.4 c1ccc(OC[C@@H]2CN(Cc3cccc4cc[nH]c34)CCO2)cc1 10.1016/j.bmcl.2016.03.102
127031830 138902 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 356 5 1 3 4.1 Clc1ccc2[nH]cc(CN3CCO[C@H](COc4ccccc4)C3)c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3793906 138902 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 356 5 1 3 4.1 Clc1ccc2[nH]cc(CN3CCO[C@H](COc4ccccc4)C3)c2c1 10.1016/j.bmcl.2016.03.102
10385977 96882 0 None -5 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 394 7 0 4 4.7 COc1ccccc1N1CCN(CCCC2CCCc3c(OC)cccc32)CC1 10.1016/S0960-894X(97)00218-7
CHEMBL26929 96882 0 None -5 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 394 7 0 4 4.7 COc1ccccc1N1CCN(CCCC2CCCc3c(OC)cccc32)CC1 10.1016/S0960-894X(97)00218-7
44431479 87152 2 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 378 4 1 2 4.9 O=C(NC1CCN(Cc2ccc(Cl)cc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
CHEMBL233581 87152 2 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 378 4 1 2 4.9 O=C(NC1CCN(Cc2ccc(Cl)cc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
122189387 122726 0 None 2 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 417 7 0 8 2.7 COc1ccccc1N1CCN(CCCc2cn(-c3ccn4nccc4c3)nn2)CC1 10.1016/j.bmc.2015.07.050
CHEMBL3613873 122726 0 None 2 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 417 7 0 8 2.7 COc1ccccc1N1CCN(CCCc2cn(-c3ccn4nccc4c3)nn2)CC1 10.1016/j.bmc.2015.07.050
71734028 90622 0 None -11 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm400520c
CHEMBL2397390 90622 0 None -11 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm400520c
11079832 164361 0 None 16 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 397 3 1 5 4.4 Cc1ccc2c(c1)C(N1CCN(CCc3ccccc3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL422310 164361 0 None 16 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 397 3 1 5 4.4 Cc1ccc2c(c1)C(N1CCN(CCc3ccccc3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
44372153 119659 0 None 83 4 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 416 4 0 4 5.3 Cc1nn2c(-c3ccccc3)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
CHEMBL351550 119659 0 None 83 4 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 416 4 0 4 5.3 Cc1nn2c(-c3ccccc3)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
57399494 70114 0 None 1 8 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 386 4 0 3 4.4 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2020.115943
CHEMBL1946124 70114 0 None 1 8 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 386 4 0 3 4.4 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2020.115943
155564110 174797 0 None -4 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 0 4 4.0 O=C(CCCN1CCCN(c2ccc(Cl)cn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL4574793 174797 0 None -4 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 0 4 4.0 O=C(CCCN1CCCN(c2ccc(Cl)cn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
134146195 154054 0 None -3 9 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 362 5 0 3 5.8 Clc1ccc2sc(CCCCN3CCC4CCCCC4C3)nc2c1 10.1016/j.bmc.2016.09.019
CHEMBL3941795 154054 0 None -3 9 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 362 5 0 3 5.8 Clc1ccc2sc(CCCCN3CCC4CCCCC4C3)nc2c1 10.1016/j.bmc.2016.09.019
CHEMBL3991399 154054 0 None -3 9 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 362 5 0 3 5.8 Clc1ccc2sc(CCCCN3CCC4CCCCC4C3)nc2c1 10.1016/j.bmc.2016.09.019
139877715 192220 0 None 21 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 321 5 0 4 3.6 c1ccc(N2CCN(CCCc3nc4ccccc4o3)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5179879 192220 0 None 21 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 321 5 0 4 3.6 c1ccc(N2CCN(CCCc3nc4ccccc4o3)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5221531 192220 0 None 21 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 321 5 0 4 3.6 c1ccc(N2CCN(CCCc3nc4ccccc4o3)CC2)cc1 10.1021/acs.jmedchem.2c00840
9906454 137743 0 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 351 5 1 4 2.7 COc1ccc(N2CCN(CCC3NC(=O)c4ccccc43)CC2)cc1 10.1016/s0960-894x(98)00252-2
CHEMBL37706 137743 0 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 351 5 1 4 2.7 COc1ccc(N2CCN(CCC3NC(=O)c4ccccc43)CC2)cc1 10.1016/s0960-894x(98)00252-2
10939408 47159 0 None -645 6 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 455 7 1 3 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2ccccc2c1 10.1021/jm020952a
CHEMBL154508 47159 0 None -645 6 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 455 7 1 3 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2ccccc2c1 10.1021/jm020952a
12050197 100407 0 None -2 4 Human 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 457 6 0 5 4.9 COc1ccc(Br)cc1-c1nc(CN2CCN(Cc3ccccc3)CC2)cs1 10.1016/s0960-894x(00)00405-4
CHEMBL293645 100407 0 None -2 4 Human 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 457 6 0 5 4.9 COc1ccc(Br)cc1-c1nc(CN2CCN(Cc3ccccc3)CC2)cs1 10.1016/s0960-894x(00)00405-4
12049521 201501 0 None 1 4 Human 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 427 5 0 5 4.4 COc1ccc(Br)cc1-c1nc(CN2CCN(c3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL64288 201501 0 None 1 4 Human 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 427 5 0 5 4.4 COc1ccc(Br)cc1-c1nc(CN2CCN(c3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
44381276 58420 0 None 2 4 Human 5.4 pKi = 5.4 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 348 4 1 4 2.1 O=C1C[C@@H](CN2CCN(c3ccccc3)CC2)N=C(c2ccccc2)N1 10.1016/s0960-894x(03)00004-0
CHEMBL168541 58420 0 None 2 4 Human 5.4 pKi = 5.4 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 348 4 1 4 2.1 O=C1C[C@@H](CN2CCN(c3ccccc3)CC2)N=C(c2ccccc2)N1 10.1016/s0960-894x(03)00004-0
3228 3097 17 None -4168 7 Human 5.4 pKi = 5.4 Binding
Displacement of spiperone from human dopamine D4 receptor expressed in CHO cell membrane incubated for 1 hr by competitive radioligand binding assay basedDisplacement of spiperone from human dopamine D4 receptor expressed in CHO cell membrane incubated for 1 hr by competitive radioligand binding assay based
ChEMBL 409 6 1 5 2.9 CNC(=O)c1ccc2c(c1)CCO[C@H]2CCN1CCN(CC1)c1ccc(cc1)OC 10.1016/j.ejmech.2020.113073
9909448 3097 17 None -4168 7 Human 5.4 pKi = 5.4 Binding
Displacement of spiperone from human dopamine D4 receptor expressed in CHO cell membrane incubated for 1 hr by competitive radioligand binding assay basedDisplacement of spiperone from human dopamine D4 receptor expressed in CHO cell membrane incubated for 1 hr by competitive radioligand binding assay based
ChEMBL 409 6 1 5 2.9 CNC(=O)c1ccc2c(c1)CCO[C@H]2CCN1CCN(CC1)c1ccc(cc1)OC 10.1016/j.ejmech.2020.113073
CHEMBL71838 3097 17 None -4168 7 Human 5.4 pKi = 5.4 Binding
Displacement of spiperone from human dopamine D4 receptor expressed in CHO cell membrane incubated for 1 hr by competitive radioligand binding assay basedDisplacement of spiperone from human dopamine D4 receptor expressed in CHO cell membrane incubated for 1 hr by competitive radioligand binding assay based
ChEMBL 409 6 1 5 2.9 CNC(=O)c1ccc2c(c1)CCO[C@H]2CCN1CCN(CC1)c1ccc(cc1)OC 10.1016/j.ejmech.2020.113073
10086348 7969 0 None -144 4 Human 6.4 pKi = 6.4 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 303 3 1 3 3.2 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)nc1 10.1021/jm950721m
CHEMBL109101 7969 0 None -144 4 Human 6.4 pKi = 6.4 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 303 3 1 3 3.2 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)nc1 10.1021/jm950721m
10086348 7969 0 None -144 4 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human dopamine receptor D4 was determinedBinding affinity towards human dopamine receptor D4 was determined
ChEMBL 303 3 1 3 3.2 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)nc1 10.1016/j.bmcl.2005.02.012
CHEMBL109101 7969 0 None -144 4 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human dopamine receptor D4 was determinedBinding affinity towards human dopamine receptor D4 was determined
ChEMBL 303 3 1 3 3.2 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)nc1 10.1016/j.bmcl.2005.02.012
164619127 184943 0 None -32 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 428 10 2 4 4.8 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4862770 184943 0 None -32 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 428 10 2 4 4.8 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
71657943 89962 0 None -128 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 427 9 1 5 4.1 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(SC)cc2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386606 89962 0 None -128 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 427 9 1 5 4.1 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(SC)cc2)CC1 10.1016/j.bmc.2013.03.074
10254390 71344 0 None -2884 8 Rat 6.4 pKi = 6.4 Binding
Binding affinity for rat dopamine D4 receptor using [11C] radiotracerBinding affinity for rat dopamine D4 receptor using [11C] radiotracer
ChEMBL 475 8 1 5 5.1 COc1cccc2cc(C(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)oc12 10.1021/jm050171k
CHEMBL196476 71344 0 None -2884 8 Rat 6.4 pKi = 6.4 Binding
Binding affinity for rat dopamine D4 receptor using [11C] radiotracerBinding affinity for rat dopamine D4 receptor using [11C] radiotracer
ChEMBL 475 8 1 5 5.1 COc1cccc2cc(C(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)oc12 10.1021/jm050171k
164619127 184943 0 None -32 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 428 10 2 4 4.8 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4862770 184943 0 None -32 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 428 10 2 4 4.8 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
168277394 189807 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5177641 189807 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)cc1F 10.1016/j.bmcl.2022.128615
6917970 3635 54 None -851 34 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2009.08.028
8370 3635 54 None -851 34 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2009.08.028
CHEMBL487387 3635 54 None -851 34 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2009.08.028
11477180 3025 3 None -616 6 Human 6.4 pKi = 6.4 Binding
Binding affinity for human dopamine D4 receptorBinding affinity for human dopamine D4 receptor
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm049465g
6675 3025 3 None -616 6 Human 6.4 pKi = 6.4 Binding
Binding affinity for human dopamine D4 receptorBinding affinity for human dopamine D4 receptor
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm049465g
CHEMBL180010 3025 3 None -616 6 Human 6.4 pKi = 6.4 Binding
Binding affinity for human dopamine D4 receptorBinding affinity for human dopamine D4 receptor
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm049465g
11778580 65796 1 None -645 5 Human 6.4 pKi = 6.4 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 283 0 1 3 2.9 CN1CCOc2cc(O)ccc2Cc2ccccc2CC1 10.1021/jm049720x
CHEMBL184050 65796 1 None -645 5 Human 6.4 pKi = 6.4 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 283 0 1 3 2.9 CN1CCOc2cc(O)ccc2Cc2ccccc2CC1 10.1021/jm049720x
11477180 3025 3 None -616 6 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm200288r
6675 3025 3 None -616 6 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm200288r
CHEMBL180010 3025 3 None -616 6 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm200288r
11477180 3025 3 None -616 6 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm0704200
6675 3025 3 None -616 6 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm0704200
CHEMBL180010 3025 3 None -616 6 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm0704200
11477180 3025 3 None -616 6 Human 6.4 pKi = 6.4 Binding
Inhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cellsInhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cells
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm040190e
6675 3025 3 None -616 6 Human 6.4 pKi = 6.4 Binding
Inhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cellsInhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cells
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm040190e
CHEMBL180010 3025 3 None -616 6 Human 6.4 pKi = 6.4 Binding
Inhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cellsInhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cells
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm040190e
44438203 93222 2 None -34 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 374 3 2 2 4.7 OC1(c2cccc(C(F)(F)F)c2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246848 93222 2 None -34 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 374 3 2 2 4.7 OC1(c2cccc(C(F)(F)F)c2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
17756213 149172 1 None -58 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 281 0 1 2 3.4 CN1CCCc2ccccc2Cc2cc(O)ccc2CC1 10.1021/jm070388+
CHEMBL394779 149172 1 None -58 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 281 0 1 2 3.4 CN1CCCc2ccccc2Cc2cc(O)ccc2CC1 10.1021/jm070388+
11300847 203282 1 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 293 3 1 4 2.3 c1cncc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)c1 10.1021/jm0305669
CHEMBL76653 203282 1 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 293 3 1 4 2.3 c1cncc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)c1 10.1021/jm0305669
154706431 176011 1 None -33 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 451 12 2 3 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4531363 176011 1 None -33 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 451 12 2 3 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4597531 176011 1 None -33 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 451 12 2 3 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
49798833 14245 0 None -8 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 323 3 1 3 4.4 OC1(c2ccccc2)CCN(Cc2cc3ccccc3s2)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1172212 14245 0 None -8 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 323 3 1 3 4.4 OC1(c2ccccc2)CCN(Cc2cc3ccccc3s2)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1200152 14245 0 None -8 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 323 3 1 3 4.4 OC1(c2ccccc2)CCN(Cc2cc3ccccc3s2)CC1 10.1016/j.bmc.2010.05.052
CHEMBL5073754 212534 0 None -15 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CN(C)C(=O)C(CCNCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
11716449 140684 0 None -20 4 Human 6.4 pKi = 6.4 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 304 1 1 1 4.2 CCN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm050846j
CHEMBL382850 140684 0 None -20 4 Human 6.4 pKi = 6.4 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 304 1 1 1 4.2 CCN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm050846j
4420454 55966 6 None 1 5 Human 7.4 pKi = 7.4 Binding
Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4
ChEMBL 205 5 0 1 3.2 C#CC1=CCC(N(CCC)CCC)CC1 10.1021/jm991098z
CHEMBL162762 55966 6 None 1 5 Human 7.4 pKi = 7.4 Binding
Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4
ChEMBL 205 5 0 1 3.2 C#CC1=CCC(N(CCC)CCC)CC1 10.1021/jm991098z
10548105 18682 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 383 9 1 3 4.5 Clc1ccc(OCCNCCCOc2ccc(Br)cc2)cc1 10.1021/jm970422s
CHEMBL128222 18682 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 383 9 1 3 4.5 Clc1ccc(OCCNCCCOc2ccc(Br)cc2)cc1 10.1021/jm970422s
11256262 79591 0 None 3 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 338 7 0 5 3.0 CCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL212782 79591 0 None 3 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 338 7 0 5 3.0 CCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
56837636 68955 0 None -26 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 897 28 2 13 5.1 COc1ccccc1N1CCN(CCCNC(=O)c2cccc(OCCOCCOCCOCCOc3cccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)c3)c2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928121 68955 0 None -26 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 897 28 2 13 5.1 COc1ccccc1N1CCN(CCCNC(=O)c2cccc(OCCOCCOCCOCCOc3cccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)c3)c2)CC1 10.1016/j.bmc.2011.10.063
127046952 139571 0 None -3 6 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 421 12 3 5 4.5 COc1cc(CCNCCc2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800636 139571 0 None -3 6 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 421 12 3 5 4.5 COc1cc(CCNCCc2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
10548105 18682 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 383 9 1 3 4.5 Clc1ccc(OCCNCCCOc2ccc(Br)cc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL128222 18682 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 383 9 1 3 4.5 Clc1ccc(OCCNCCCOc2ccc(Br)cc2)cc1 10.1016/j.bmcl.2005.02.012
11199162 79449 0 None 1 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 358 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL212235 79449 0 None 1 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 358 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
12899499 66290 0 None -7 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 395 7 1 5 3.2 COc1ccccc1N1CCN(CCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1813596 66290 0 None -7 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 395 7 1 5 3.2 COc1ccccc1N1CCN(CCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1852734 66290 0 None -7 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 395 7 1 5 3.2 COc1ccccc1N1CCN(CCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1016/j.bmc.2011.04.021
CHEMBL5083473 213093 0 None 5 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCc1cccc(N2CCN(CCC(c3cccc(O)c3)c3cccc(OC)c3)CC2)c1Cl 10.1021/acs.jmedchem.1c00611
3038495 700 30 None -91 19 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm0611152
7625 700 30 None -91 19 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm0611152
CHEMBL25236 700 30 None -91 19 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm0611152
4420454 55966 6 None 1 5 Human 6.4 pKi = 6.4 Binding
Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4
ChEMBL 205 5 0 1 3.2 C#CC1=CCC(N(CCC)CCC)CC1 10.1021/jm991098z
CHEMBL162762 55966 6 None 1 5 Human 6.4 pKi = 6.4 Binding
Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4
ChEMBL 205 5 0 1 3.2 C#CC1=CCC(N(CCC)CCC)CC1 10.1021/jm991098z
11615489 69100 1 None -3 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 221 5 0 3 2.3 CCCN(CCC)[C@H]1CCn2nccc2C1 10.1021/jm101639t
CHEMBL193337 69100 1 None -3 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 221 5 0 3 2.3 CCCN(CCC)[C@H]1CCn2nccc2C1 10.1021/jm101639t
10039198 56055 0 None -4 4 Human 5.4 pKi = 5.4 Binding
Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4
ChEMBL 277 5 0 1 4.5 CCCN(CCC)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm991098z
CHEMBL163087 56055 0 None -4 4 Human 5.4 pKi = 5.4 Binding
Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4
ChEMBL 277 5 0 1 4.5 CCCN(CCC)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm991098z
CHEMBL5072449 212510 0 None -8 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None O=C(NCCCCN1CC[C@]2(c3cccc(O)c3)CCC[C@H]1[C@H]2O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.1c00611
90389592 147141 0 None -12 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 422 8 1 4 2.8 CC(O)CN1CCN(CC[S+]([O-])C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2020.112674
CHEMBL3931765 147141 0 None -12 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 422 8 1 4 2.8 CC(O)CN1CCN(CC[S+]([O-])C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2020.112674
90389592 147141 0 None -12 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 422 8 1 4 2.8 CC(O)CN1CCN(CC[S+]([O-])C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.6b01373
CHEMBL3931765 147141 0 None -12 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 422 8 1 4 2.8 CC(O)CN1CCN(CC[S+]([O-])C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.6b01373
154705520 175686 1 None -25 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 3 5.6 CCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4452683 175686 1 None -25 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 3 5.6 CCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4594959 175686 1 None -25 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 3 5.6 CCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
71455083 81418 0 None -239 7 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 389 6 0 3 4.8 O=C(C1CCCCC1)N(CCN1CC=C(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL2164354 81418 0 None -239 7 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 389 6 0 3 4.8 O=C(C1CCCCC1)N(CCN1CC=C(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
53325242 56775 0 None -1 17 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
ChEMBL 537 8 1 2 7.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL1644978 56775 0 None -1 17 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
ChEMBL 537 8 1 2 7.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
9907381 4828 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 369 4 0 3 3.0 O=C(CN1CCc2ccccc21)N1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104514 4828 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 369 4 0 3 3.0 O=C(CN1CCc2ccccc21)N1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
72191064 91927 0 None -3 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-spiperone from cloned human dopamine D4 receptorDisplacement of [3H]-spiperone from cloned human dopamine D4 receptor
ChEMBL 469 8 0 6 4.3 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc(Br)cc3)nn2)CC1 10.1016/j.bmcl.2013.08.047
CHEMBL2430442 91927 0 None -3 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-spiperone from cloned human dopamine D4 receptorDisplacement of [3H]-spiperone from cloned human dopamine D4 receptor
ChEMBL 469 8 0 6 4.3 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc(Br)cc3)nn2)CC1 10.1016/j.bmcl.2013.08.047
44438211 146929 2 None -19 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 354 3 2 2 4.7 OC1(c2ccc(Cl)cc2)CCCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL393027 146929 2 None -19 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 354 3 2 2 4.7 OC1(c2ccc(Cl)cc2)CCCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
54477 84230 34 None -14 22 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC 10.1021/jm00025a013
CHEMBL22242 84230 34 None -14 22 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC 10.1021/jm00025a013
3038495 700 30 None -91 19 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm025558r
7625 700 30 None -91 19 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm025558r
CHEMBL25236 700 30 None -91 19 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm025558r
135398737 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9601720
38 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9601720
722 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9601720
CHEMBL42 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9601720
DB00363 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9601720
2865 4079 67 None -66 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm0002432
59 4079 67 None -66 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm0002432
60854 4079 67 None -66 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm0002432
CHEMBL708 4079 67 None -66 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm0002432
DB00246 4079 67 None -66 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm0002432
103 4089 56 None -17 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm0002432
2875 4089 56 None -17 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm0002432
5736 4089 56 None -17 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm0002432
CHEMBL285802 4089 56 None -17 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm0002432
DB09225 4089 56 None -17 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm0002432
2865 4079 67 None -66 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm030480f
59 4079 67 None -66 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm030480f
60854 4079 67 None -66 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm030480f
CHEMBL708 4079 67 None -66 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm030480f
DB00246 4079 67 None -66 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm030480f
103 4089 56 None -17 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
2875 4089 56 None -17 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
5736 4089 56 None -17 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
CHEMBL285802 4089 56 None -17 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
DB09225 4089 56 None -17 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
135398737 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C5MD00258C
38 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C5MD00258C
722 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C5MD00258C
CHEMBL42 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C5MD00258C
DB00363 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C5MD00258C
57394810 69814 0 None 2 5 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 363 6 0 2 5.8 Fc1ccc(SCCCN2CCC(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940405 69814 0 None 2 5 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 363 6 0 2 5.8 Fc1ccc(SCCCN2CCC(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2011.12.019
49782601 17306 0 None -2 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 487 6 1 3 6.2 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
CHEMBL1257810 17306 0 None -2 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 487 6 1 3 6.2 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
45267409 194487 0 None 676 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 351 4 0 6 2.7 COc1ccccc1N1CCN(Cc2c(C)nc3cc(C)ncn23)CC1 10.1016/j.bmc.2009.05.015
CHEMBL561262 194487 0 None 676 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 351 4 0 6 2.7 COc1ccccc1N1CCN(Cc2c(C)nc3cc(C)ncn23)CC1 10.1016/j.bmc.2009.05.015
9906895 119451 1 None 25 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 360 4 0 5 2.7 Fc1ccc(OC[C@@H]2CC[C@@H]3CN(c4ncc(F)cn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL349699 119451 1 None 25 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 360 4 0 5 2.7 Fc1ccc(OC[C@@H]2CC[C@@H]3CN(c4ncc(F)cn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
12050202 201607 0 None 43 4 Human 7.4 pKi = 7.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 441 7 1 5 4.5 COc1ccc(Br)cc1-c1nc(CN[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL64752 201607 0 None 43 4 Human 7.4 pKi = 7.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 441 7 1 5 4.5 COc1ccc(Br)cc1-c1nc(CN[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
45379369 7441 0 None -15 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]radioligand from human recombinant dopamine D4.4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]radioligand from human recombinant dopamine D4.4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2c[nH]c3cccc(c23)CC1 10.1021/jm901291r
CHEMBL1087300 7441 0 None -15 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]radioligand from human recombinant dopamine D4.4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]radioligand from human recombinant dopamine D4.4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2c[nH]c3cccc(c23)CC1 10.1021/jm901291r
8592415 64838 7 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 339 5 1 4 2.8 COc1cccc(N2CCN(CC(=O)Nc3cccc(C)c3)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL182432 64838 7 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 339 5 1 4 2.8 COc1cccc(N2CCN(CC(=O)Nc3cccc(C)c3)CC2)c1 10.1016/j.bmcl.2004.07.068
10477871 82817 0 None -158 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 431 8 2 5 3.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccc(C#N)cc3[nH]2)CC1 10.1021/jm0611152
CHEMBL218638 82817 0 None -158 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 431 8 2 5 3.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccc(C#N)cc3[nH]2)CC1 10.1021/jm0611152
11570589 83833 0 None -18 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 582 13 1 7 4.8 CCCc1c(C(=O)NCCCCCN2CCN(c3ccccc3OC)CC2)nnn1Cc1ccccc1Br 10.1021/jm0611152
CHEMBL221129 83833 0 None -18 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 582 13 1 7 4.8 CCCc1c(C(=O)NCCCCCN2CCN(c3ccccc3OC)CC2)nnn1Cc1ccccc1Br 10.1021/jm0611152
135398737 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
38 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
722 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
CHEMBL42 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
DB00363 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
4064342 205312 29 None -4 3 Human 6.4 pKi = 6.4 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 309 4 2 2 3.5 O=C(Nc1ccccc1)NC1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL91621 205312 29 None -4 3 Human 6.4 pKi = 6.4 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 309 4 2 2 3.5 O=C(Nc1ccccc1)NC1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
12050199 100345 0 None 1 4 Human 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 455 7 1 5 4.9 COc1ccc(Br)cc1-c1nc(CNC2CCN(Cc3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL293225 100345 0 None 1 4 Human 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 455 7 1 5 4.9 COc1ccc(Br)cc1-c1nc(CNC2CCN(Cc3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
44304652 198638 0 None 1 4 Human 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 363 7 1 4 4.4 c1ccc(CN2CC[C@@H](CNCc3csc(-c4ccccc4)n3)C2)cc1 10.1016/s0960-894x(00)00405-4
CHEMBL59749 198638 0 None 1 4 Human 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 363 7 1 4 4.4 c1ccc(CN2CC[C@@H](CNCc3csc(-c4ccccc4)n3)C2)cc1 10.1016/s0960-894x(00)00405-4
44319368 105584 0 None -1 4 Human 6.4 pKi = 6.4 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 429 5 0 5 3.4 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)CO1 10.1016/s0960-894x(01)00484-x
CHEMBL313320 105584 0 None -1 4 Human 6.4 pKi = 6.4 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 429 5 0 5 3.4 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)CO1 10.1016/s0960-894x(01)00484-x
10824155 56944 1 None 1 4 Human 5.4 pKi = 5.4 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 243 5 0 1 3.6 C#CC(C#C)=C1CCC(N(CCC)CCC)CC1 10.1021/jm991098z
CHEMBL165022 56944 1 None 1 4 Human 5.4 pKi = 5.4 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 243 5 0 1 3.6 C#CC(C#C)=C1CCC(N(CCC)CCC)CC1 10.1021/jm991098z
164622629 185014 0 None -20 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 436 6 2 4 4.5 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1ccccc1Cl)CC2 10.1016/j.bmcl.2021.128047
CHEMBL4863748 185014 0 None -20 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 436 6 2 4 4.5 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1ccccc1Cl)CC2 10.1016/j.bmcl.2021.128047
10885524 102651 0 None -38 5 Human 6.4 pKi = 6.4 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 493 7 1 3 5.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)C1c2ccccc2-c2ccccc21 10.1021/jm010146o
CHEMBL307800 102651 0 None -38 5 Human 6.4 pKi = 6.4 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 493 7 1 3 5.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)C1c2ccccc2-c2ccccc21 10.1021/jm010146o
10572985 162930 0 None 1 3 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 398 6 0 3 5.4 COc1ccc2c(c1)C(CCCN1CCN(c3ccc(Cl)cc3)CC1)CCC2 10.1021/jm991138z
CHEMBL420067 162930 0 None 1 3 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 398 6 0 3 5.4 COc1ccc2c(c1)C(CCCN1CCN(c3ccc(Cl)cc3)CC1)CCC2 10.1021/jm991138z
1016 3690 75 None -28 35 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 3690 75 None -28 35 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 3690 75 None -28 35 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
5384 3690 75 None -28 35 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 3690 75 None -28 35 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 3690 75 None -28 35 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
71061611 148528 0 None -10 3 Mouse 5.4 pKi = 5.4 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 356 6 0 4 3.0 Fc1ccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)cc1 nan
CHEMBL3942898 148528 0 None -10 3 Mouse 5.4 pKi = 5.4 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 356 6 0 4 3.0 Fc1ccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)cc1 nan
155522719 170223 0 None - 1 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 298 4 1 6 0.6 O=C(CN1CCN(c2ccccn2)CC1)Nc1cncnc1 10.1021/acs.jmedchem.9b00231
CHEMBL4453069 170223 0 None - 1 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 298 4 1 6 0.6 O=C(CN1CCN(c2ccccn2)CC1)Nc1cncnc1 10.1021/acs.jmedchem.9b00231
135404757 120445 0 None 2 2 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 341 1 2 5 3.6 CN1CCC(NC2=Nc3cccnc3Nc3ccc(Cl)cc32)CC1 10.1021/jm0104825
CHEMBL356149 120445 0 None 2 2 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 341 1 2 5 3.6 CN1CCC(NC2=Nc3cccnc3Nc3ccc(Cl)cc32)CC1 10.1021/jm0104825
44438213 92976 5 None -1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 354 4 2 2 4.4 OC1(Cc2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL245815 92976 5 None -1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 354 4 2 2 4.4 OC1(Cc2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
44438223 93059 0 None -64 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 382 4 1 3 4.5 COC(=O)C1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246231 93059 0 None -64 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 382 4 1 3 4.5 COC(=O)C1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL5077104 212710 0 None -64 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None N#CC(CCNCCCCC(=O)N1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
70788951 26948 1 None -1 5 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL None None None None nan
CHEMBL1366 26948 1 None -1 5 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL None None None None nan
72191065 91926 0 None -10 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-spiperone from cloned human dopamine D4 receptorDisplacement of [3H]-spiperone from cloned human dopamine D4 receptor
ChEMBL 421 9 0 7 3.6 COc1ccc(-c2cn(CCCCN3CCN(c4ccccc4OC)CC3)nn2)cc1 10.1016/j.bmcl.2013.08.047
CHEMBL2430441 91926 0 None -10 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-spiperone from cloned human dopamine D4 receptorDisplacement of [3H]-spiperone from cloned human dopamine D4 receptor
ChEMBL 421 9 0 7 3.6 COc1ccc(-c2cn(CCCCN3CCN(c4ccccc4OC)CC3)nn2)cc1 10.1016/j.bmcl.2013.08.047
118719798 115225 0 None -309 4 Human 6.4 pKi = 6.4 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 473 9 0 7 5.1 COc1ccccc1N1CCN(CCCCc2cn(-c3ccc(-c4ccsc4)cc3)nn2)CC1 10.1016/j.bmcl.2014.12.023
CHEMBL3353901 115225 0 None -309 4 Human 6.4 pKi = 6.4 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 473 9 0 7 5.1 COc1ccccc1N1CCN(CCCCc2cn(-c3ccc(-c4ccsc4)cc3)nn2)CC1 10.1016/j.bmcl.2014.12.023
44356253 11473 0 None -794 5 Human 6.4 pKi = 6.4 Binding
Compound was tested to inhibit Dopa accumulation in Dopamine receptor D4 at 10 mg/kg, scCompound was tested to inhibit Dopa accumulation in Dopamine receptor D4 at 10 mg/kg, sc
ChEMBL 295 2 1 3 3.1 Oc1ccc2c(c1)OC(CN1CCc3ccccc3C1)CC2 10.1021/jm9703653
CHEMBL1180604 11473 0 None -794 5 Human 6.4 pKi = 6.4 Binding
Compound was tested to inhibit Dopa accumulation in Dopamine receptor D4 at 10 mg/kg, scCompound was tested to inhibit Dopa accumulation in Dopamine receptor D4 at 10 mg/kg, sc
ChEMBL 295 2 1 3 3.1 Oc1ccc2c(c1)OC(CN1CCc3ccccc3C1)CC2 10.1021/jm9703653
CHEMBL134808 11473 0 None -794 5 Human 6.4 pKi = 6.4 Binding
Compound was tested to inhibit Dopa accumulation in Dopamine receptor D4 at 10 mg/kg, scCompound was tested to inhibit Dopa accumulation in Dopamine receptor D4 at 10 mg/kg, sc
ChEMBL 295 2 1 3 3.1 Oc1ccc2c(c1)OC(CN1CCc3ccccc3C1)CC2 10.1021/jm9703653
46231784 199653 0 None -6606 4 Human 5.4 pKi = 5.4 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 329 0 2 3 3.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL604314 199653 0 None -6606 4 Human 5.4 pKi = 5.4 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 329 0 2 3 3.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
11762743 103337 0 None -109 5 Human 5.4 pKi = 5.4 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 493 6 1 4 5.1 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2=O 10.1021/jm010146o
CHEMBL309118 103337 0 None -109 5 Human 5.4 pKi = 5.4 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 493 6 1 4 5.1 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2=O 10.1021/jm010146o
44394884 122144 0 None 38 2 Human 8.4 pKi = 8.4 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 356 5 1 2 4.4 O=C(NC1CCN(Cc2ccccc2)C1)c1cccc(-c2ccccc2)c1 10.1016/j.bmcl.2004.07.045
CHEMBL360394 122144 0 None 38 2 Human 8.4 pKi = 8.4 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 356 5 1 2 4.4 O=C(NC1CCN(Cc2ccccc2)C1)c1cccc(-c2ccccc2)c1 10.1016/j.bmcl.2004.07.045
9951233 102317 0 None 33 2 Human 8.4 pKi = 8.4 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 369 3 0 3 3.0 CN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)Cc2ccccc21 10.1016/s0960-894x(00)00421-2
CHEMBL305276 102317 0 None 33 2 Human 8.4 pKi = 8.4 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 369 3 0 3 3.0 CN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)Cc2ccccc21 10.1016/s0960-894x(00)00421-2
10045525 202085 0 None 5 2 Human 8.4 pKi = 8.4 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 383 4 0 3 3.4 CCN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)Cc2ccccc21 10.1016/s0960-894x(00)00421-2
CHEMBL68191 202085 0 None 5 2 Human 8.4 pKi = 8.4 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 383 4 0 3 3.4 CCN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)Cc2ccccc21 10.1016/s0960-894x(00)00421-2
44264682 96869 0 None 141 4 Human 8.4 pKi = 8.4 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1cccc(N2CCN(Cc3cnn4ccccc34)CC2)c1 10.1016/s0960-894x(98)00692-1
CHEMBL269202 96869 0 None 141 4 Human 8.4 pKi = 8.4 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1cccc(N2CCN(Cc3cnn4ccccc34)CC2)c1 10.1016/s0960-894x(98)00692-1
10430183 203916 0 None -39 7 Human 8.4 pKi = 8.4 Binding
Binding affinity to human D4 receptor expressed in CHO cells assessed as inhibition constantBinding affinity to human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 385 5 1 5 2.1 O=C(NCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1 10.1021/acs.jmedchem.2c00633
CHEMBL81728 203916 0 None -39 7 Human 8.4 pKi = 8.4 Binding
Binding affinity to human D4 receptor expressed in CHO cells assessed as inhibition constantBinding affinity to human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 385 5 1 5 2.1 O=C(NCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1 10.1021/acs.jmedchem.2c00633
44335995 107978 0 None 54 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 397 5 0 3 3.8 CC[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL319923 107978 0 None 54 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 397 5 0 3 3.8 CC[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00656-x
44336000 108501 0 None 288 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 383 4 0 3 3.4 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccccc2Cl)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL321201 108501 0 None 288 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 383 4 0 3 3.4 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccccc2Cl)CC1 10.1016/s0960-894x(02)00656-x
44336050 5242 0 None 77 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 376 4 0 2 4.9 Cc1ccc(CN2CCC(CC(=O)N3c4ccccc4CC3C)CC2)cc1C 10.1016/s0960-894x(02)00655-8
CHEMBL106742 5242 0 None 77 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 376 4 0 2 4.9 Cc1ccc(CN2CCC(CC(=O)N3c4ccccc4CC3C)CC2)cc1C 10.1016/s0960-894x(02)00655-8
9800164 4883 0 None 22 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 382 4 0 2 4.9 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104788 4883 0 None 22 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 382 4 0 2 4.9 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
44335796 4896 0 None 15 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 382 4 0 2 4.9 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2cccc(Cl)c2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104832 4896 0 None 15 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 382 4 0 2 4.9 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2cccc(Cl)c2)CC1 10.1016/s0960-894x(02)00655-8
9799781 119699 0 None 52 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 375 3 0 3 3.0 Cc1ccc(CN2CCN(C3CCc4cccc5c4N(CC5)C3=O)CC2)cc1 10.1016/s0960-894x(02)01056-9
CHEMBL351963 119699 0 None 52 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 375 3 0 3 3.0 Cc1ccc(CN2CCN(C3CCc4cccc5c4N(CC5)C3=O)CC2)cc1 10.1016/s0960-894x(02)01056-9
10045525 202085 0 None 5 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 383 4 0 3 3.4 CCN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)Cc2ccccc21 10.1016/s0960-894x(02)01056-9
CHEMBL68191 202085 0 None 5 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 383 4 0 3 3.4 CCN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)Cc2ccccc21 10.1016/s0960-894x(02)01056-9
10543298 39615 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 314 4 0 2 4.8 C1=C(c2ccccc2)CCN(Cc2ccn(-c3ccccc3)c2)C1 10.1021/jm00025a013
CHEMBL147731 39615 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 314 4 0 2 4.8 C1=C(c2ccccc2)CCN(Cc2ccn(-c3ccccc3)c2)C1 10.1021/jm00025a013
10567507 118755 0 None 3 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 317 4 0 3 3.8 c1ccc(N2CCN(Cc3ccn(-c4ccccc4)c3)CC2)cc1 10.1021/jm00025a013
CHEMBL343657 118755 0 None 3 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 317 4 0 3 3.8 c1ccc(N2CCN(Cc3ccn(-c4ccccc4)c3)CC2)cc1 10.1021/jm00025a013
60165416 74946 0 None 7 8 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 385 6 0 4 5.1 Clc1ccc(N2CCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL2037431 74946 0 None 7 8 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 385 6 0 4 5.1 Clc1ccc(N2CCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2014.04.026
60165416 74946 0 None 7 8 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 385 6 0 4 5.1 Clc1ccc(N2CCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.ejmech.2012.03.042
CHEMBL2037431 74946 0 None 7 8 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 385 6 0 4 5.1 Clc1ccc(N2CCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.ejmech.2012.03.042
44405492 139992 0 None 15 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 376 5 1 3 4.7 Cc1ccc(CN2CC[C@H](NC(=O)c3cccc(-c4cccs4)c3)C2)cc1 10.1016/j.bmcl.2005.08.051
CHEMBL381019 139992 0 None 15 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 376 5 1 3 4.7 Cc1ccc(CN2CC[C@H](NC(=O)c3cccc(-c4cccs4)c3)C2)cc1 10.1016/j.bmcl.2005.08.051
11638780 76742 0 None 1412 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 345 3 0 5 2.8 Fc1ccc(N2CCN(Cc3cn4nc(Cl)ccc4n3)CC2)cc1 10.1021/jm060166w
CHEMBL207488 76742 0 None 1412 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 345 3 0 5 2.8 Fc1ccc(N2CCN(Cc3cn4nc(Cl)ccc4n3)CC2)cc1 10.1021/jm060166w
10044835 110918 0 None 45 3 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 372 7 0 4 4.1 COc1cccc(C(=O)CCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
CHEMBL327245 110918 0 None 45 3 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 372 7 0 4 4.1 COc1cccc(C(=O)CCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
9951233 102317 0 None 33 2 Human 8.4 pKi = 8.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 369 3 0 3 3.0 CN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)Cc2ccccc21 10.1021/acs.jmedchem.7b00151
CHEMBL305276 102317 0 None 33 2 Human 8.4 pKi = 8.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 369 3 0 3 3.0 CN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)Cc2ccccc21 10.1021/acs.jmedchem.7b00151
54583898 61282 0 None -8 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 417 7 0 4 3.3 C#Cc1ccc2c(c1)CCN(CCCCN1CCN(c3ccccc3OC)CC1)C2=O 10.1016/j.bmcl.2010.12.083
CHEMBL1771114 61282 0 None -8 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 417 7 0 4 3.3 C#Cc1ccc2c(c1)CCN(CCCCN1CCN(c3ccccc3OC)CC1)C2=O 10.1016/j.bmcl.2010.12.083
44376569 57140 0 None 19 2 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 324 4 0 5 2.5 c1ccc(OC[C@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL165504 57140 0 None 19 2 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 324 4 0 5 2.5 c1ccc(OC[C@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
168286048 192320 0 None 371 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 379 6 0 4 3.2 COc1cccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)c1 10.1021/acs.jmedchem.2c00840
CHEMBL5191408 192320 0 None 371 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 379 6 0 4 3.2 COc1cccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)c1 10.1021/acs.jmedchem.2c00840
CHEMBL5222229 192320 0 None 371 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 379 6 0 4 3.2 COc1cccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)c1 10.1021/acs.jmedchem.2c00840
57396484 69826 2 None 5 6 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 316 6 0 5 2.2 Fc1ccc(OCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940417 69826 2 None 5 6 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 316 6 0 5 2.2 Fc1ccc(OCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
57396484 69826 2 None 5 6 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 316 6 0 5 2.2 Fc1ccc(OCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940417 69826 2 None 5 6 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 316 6 0 5 2.2 Fc1ccc(OCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
56926585 68663 0 None 1000 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 358 4 0 5 2.9 COc1cc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)ccc1F 10.1021/jm200762g
CHEMBL1923293 68663 0 None 1000 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 358 4 0 5 2.9 COc1cc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)ccc1F 10.1021/jm200762g
10090130 192391 0 None 19 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 363 6 0 3 3.6 O=C1CCc2ccccc2N1CCCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5199358 192391 0 None 19 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 363 6 0 3 3.6 O=C1CCc2ccccc2N1CCCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222630 192391 0 None 19 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 363 6 0 3 3.6 O=C1CCc2ccccc2N1CCCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.2c00840
44340097 9349 0 None 8 4 Human 8.4 pKi = 8.4 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL111749 9349 0 None 8 4 Human 8.4 pKi = 8.4 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
10759511 205236 0 None 128 2 Human 8.4 pKi = 8.4 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 339 3 0 4 3.5 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(F)cc1)CC3 10.1021/jm970170v
CHEMBL91273 205236 0 None 128 2 Human 8.4 pKi = 8.4 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 339 3 0 4 3.5 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(F)cc1)CC3 10.1021/jm970170v
4826074 103627 6 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 322 4 1 4 2.9 COc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm0305669
CHEMBL309372 103627 6 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 322 4 1 4 2.9 COc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm0305669
9902381 119006 0 None 114 3 Human 8.4 pKi = 8.4 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 337 3 1 4 2.6 Cc1ccc(N2CCN(Cc3ccc4c(c3)NC(=O)CO4)CC2)cc1 10.1021/jm990277d
CHEMBL345552 119006 0 None 114 3 Human 8.4 pKi = 8.4 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 337 3 1 4 2.6 Cc1ccc(N2CCN(Cc3ccc4c(c3)NC(=O)CO4)CC2)cc1 10.1021/jm990277d
9885114 119099 3 None 47 12 Human 8.4 pKi = 8.4 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 357 3 1 4 3.0 O=C1COc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)ccc2N1 10.1021/jm990277d
CHEMBL346389 119099 3 None 47 12 Human 8.4 pKi = 8.4 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 357 3 1 4 3.0 O=C1COc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)ccc2N1 10.1021/jm990277d
1353 1880 85 None -3 85 Human 8.4 pKi = 8.4 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9810396
3559 1880 85 None -3 85 Human 8.4 pKi = 8.4 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9810396
86 1880 85 None -3 85 Human 8.4 pKi = 8.4 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9810396
CHEMBL54 1880 85 None -3 85 Human 8.4 pKi = 8.4 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9810396
DB00502 1880 85 None -3 85 Human 8.4 pKi = 8.4 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9810396
9887091 106905 0 None 27 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 4 0 3 3.8 CC1(C)Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL317879 106905 0 None 27 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 4 0 3 3.8 CC1(C)Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
10023466 164362 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 392 4 1 3 4.2 Clc1ccccc1CCN1CCN(c2[nH]nc3c2CCc2ccccc2-3)CC1 10.1021/jm0002432
CHEMBL422314 164362 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 392 4 1 3 4.2 Clc1ccccc1CCN1CCN(c2[nH]nc3c2CCc2ccccc2-3)CC1 10.1021/jm0002432
21527771 69813 0 None -1 10 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 363 6 1 3 4.2 OC1(c2ccc(Cl)cc2)CCN(CCCOc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
CHEMBL1940404 69813 0 None -1 10 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 363 6 1 3 4.2 OC1(c2ccc(Cl)cc2)CCN(CCCOc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
25139181 183760 0 None -2 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 414 10 1 2 5.7 C#CC1=CCC(N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm800895v
CHEMBL484358 183760 0 None -2 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 414 10 1 2 5.7 C#CC1=CCC(N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm800895v
25072941 155933 0 None 1 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(C=O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4067439 155933 0 None 1 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(C=O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
10780942 21131 1 None 3 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 305 9 1 3 3.8 Clc1ccccc1OCCNCCCOc1ccccc1 10.1016/j.bmcl.2005.02.012
CHEMBL131396 21131 1 None 3 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 305 9 1 3 3.8 Clc1ccccc1OCCNCCCOc1ccccc1 10.1016/j.bmcl.2005.02.012
10805355 22200 0 None 79 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 316 10 1 5 3.0 O=[N+]([O-])c1ccc(OCCNCCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL132455 22200 0 None 79 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 316 10 1 5 3.0 O=[N+]([O-])c1ccc(OCCNCCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
118719926 115280 0 None 102 8 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL3354073 115280 0 None 102 8 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/acs.jmedchem.8b00265
10719212 205523 0 None -2 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 471 6 2 4 4.3 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(C2C3CC4CC(C3)CC2C4)C1 10.1021/jm9601720
CHEMBL92924 205523 0 None -2 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 471 6 2 4 4.3 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(C2C3CC4CC(C3)CC2C4)C1 10.1021/jm9601720
72164299 91721 4 None 9 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 321 3 0 3 3.7 Clc1cccc(N2CCN(Cc3cccnc3)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
CHEMBL2420780 91721 4 None 9 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 321 3 0 3 3.7 Clc1cccc(N2CCN(Cc3cccnc3)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
10780942 21131 1 None 3 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 305 9 1 3 3.8 Clc1ccccc1OCCNCCCOc1ccccc1 10.1021/jm970422s
CHEMBL131396 21131 1 None 3 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 305 9 1 3 3.8 Clc1ccccc1OCCNCCCOc1ccccc1 10.1021/jm970422s
10805355 22200 0 None 79 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 316 10 1 5 3.0 O=[N+]([O-])c1ccc(OCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
CHEMBL132455 22200 0 None 79 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 316 10 1 5 3.0 O=[N+]([O-])c1ccc(OCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
10519543 112998 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 317 3 0 3 4.1 O=c1ccc2ccc(CN3CC=C(c4ccccc4)CC3)cc2o1 10.1021/jm990266k
CHEMBL332001 112998 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 317 3 0 3 4.1 O=c1ccc2ccc(CN3CC=C(c4ccccc4)CC3)cc2o1 10.1021/jm990266k
155519378 169843 0 None 17 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 505 11 2 5 4.7 COc1ccccc1N1CCN(CCCCNC(=O)NN(Cc2ccccc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4448166 169843 0 None 17 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 505 11 2 5 4.7 COc1ccccc1N1CCN(CCCCNC(=O)NN(Cc2ccccc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
25072632 111284 0 None -1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3ccc4ccnn4c3)CC2)c1Cl 10.1021/jm5004039
CHEMBL3287392 111284 0 None -1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3ccc4ccnn4c3)CC2)c1Cl 10.1021/jm5004039
18403576 6114 0 None - 1 Human 8.4 pKi = 8.4 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 381 6 0 4 4.3 COc1cc(Cl)ccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL108122 6114 0 None - 1 Human 8.4 pKi = 8.4 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 381 6 0 4 4.3 COc1cc(Cl)ccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
71294321 192184 0 None 512 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 351 5 0 5 2.0 O=C1CCc2ccccc2N1CCCN1CCN(c2ncccn2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5172871 192184 0 None 512 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 351 5 0 5 2.0 O=C1CCc2ccccc2N1CCCN1CCN(c2ncccn2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5221357 192184 0 None 512 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 351 5 0 5 2.0 O=C1CCc2ccccc2N1CCCN1CCN(c2ncccn2)CC1 10.1021/acs.jmedchem.2c00840
10593869 205300 0 None 60 3 Human 8.4 pKi = 8.4 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 348 4 1 5 3.8 Cc1c(-c2ccccn2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL91553 205300 0 None 60 3 Human 8.4 pKi = 8.4 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 348 4 1 5 3.8 Cc1c(-c2ccccn2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
10574303 205589 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 423 5 0 4 5.5 Cc1c(-c2ccccc2)n(-c2ccccc2)c(=O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL93432 205589 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 423 5 0 4 5.5 Cc1c(-c2ccccc2)n(-c2ccccc2)c(=O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
11451022 91724 0 None 10 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 352 5 0 4 4.6 CCOc1ccccc1N1CCN(Cc2csc3ccccc23)CC1 10.1016/j.bmcl.2013.07.033
CHEMBL2420890 91724 0 None 10 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 352 5 0 4 4.6 CCOc1ccccc1N1CCN(Cc2csc3ccccc23)CC1 10.1016/j.bmcl.2013.07.033
6603950 201633 9 None -13 9 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 344 1 0 3 4.3 CN1CCN([C@@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm020938y
CHEMBL64875 201633 9 None -13 9 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 344 1 0 3 4.3 CN1CCN([C@@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm020938y
3050372 69823 7 None 5 6 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 296 6 0 3 3.3 c1ccc(OCCCN2CCN(c3ccccc3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940414 69823 7 None 5 6 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 296 6 0 3 3.3 c1ccc(OCCCN2CCN(c3ccccc3)CC2)cc1 10.1016/j.bmc.2011.12.019
127047996 139116 0 None 5 6 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 303 8 3 5 2.3 COc1ccccc1OCCNCCc1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
CHEMBL3797758 139116 0 None 5 6 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 303 8 3 5 2.3 COc1ccccc1OCCNCCc1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
71583848 87303 0 None 6 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 448 4 0 4 5.1 c1ccc(N2CCN(Cc3cnn(-c4cc5ccc4CCc4ccc(cc4)CC5)c3)CC2)cc1 10.1016/j.bmc.2013.01.065
CHEMBL2336892 87303 0 None 6 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 448 4 0 4 5.1 c1ccc(N2CCN(Cc3cnn(-c4cc5ccc4CCc4ccc(cc4)CC5)c3)CC2)cc1 10.1016/j.bmc.2013.01.065
11315028 110155 0 None - 1 Human 8.4 pKi = 8.4 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 380 6 1 4 4.3 COc1ccc(Cl)cc1NCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL325789 110155 0 None - 1 Human 8.4 pKi = 8.4 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 380 6 1 4 4.3 COc1ccc(Cl)cc1NCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
155529592 170881 0 None 10 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 509 10 2 5 4.4 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4463200 170881 0 None 10 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 509 10 2 5 4.4 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
71454294 83663 0 None 23 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 431 6 0 5 4.0 COc1ccccc1N1CCN(Cc2cc(CN3CCOCC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207639 83663 0 None 23 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 431 6 0 5 4.0 COc1ccccc1N1CCN(Cc2cc(CN3CCOCC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
44340084 9000 0 None 6 4 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 401 6 2 4 4.0 CNc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL109912 9000 0 None 6 4 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 401 6 2 4 4.0 CNc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
10549355 203792 0 None 234 2 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 406 5 1 4 5.1 Cc1c(-c2ccc(Cl)cc2)nc(N)nc1C1CCN(CCc2ccccc2)CC1 10.1021/jm970111h
CHEMBL80722 203792 0 None 234 2 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 406 5 1 4 5.1 Cc1c(-c2ccc(Cl)cc2)nc(N)nc1C1CCN(CCc2ccccc2)CC1 10.1021/jm970111h
9948965 114870 0 None 74 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 283 9 1 2 4.0 Cc1ccc(CCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
CHEMBL334989 114870 0 None 74 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 283 9 1 2 4.0 Cc1ccc(CCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
137633863 156084 0 None -2 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(/C=N/O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4069145 156084 0 None -2 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(/C=N/O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
44459463 98702 0 None 19 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 331 4 1 2 4.8 Cc1c(C2CCN(Cc3ccccc3)CC2)n[nH]c1-c1ccccc1 10.1016/s0960-894x(99)00169-9
CHEMBL281195 98702 0 None 19 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 331 4 1 2 4.8 Cc1c(C2CCN(Cc3ccccc3)CC2)n[nH]c1-c1ccccc1 10.1016/s0960-894x(99)00169-9
10020040 99506 0 None 9 3 Rat 8.3 pKi = 8.3 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 338 4 1 4 3.6 CSc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
CHEMBL28651 99506 0 None 9 3 Rat 8.3 pKi = 8.3 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 338 4 1 4 3.6 CSc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
155528865 170823 0 None 1 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 347 6 0 3 4.0 Fc1ccc(CCCCN2CCN(c3ccc(Cl)cn3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4462108 170823 0 None 1 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 347 6 0 3 4.0 Fc1ccc(CCCCN2CCN(c3ccc(Cl)cn3)CC2)cc1 10.1016/j.bmc.2020.115943
155528865 170823 0 None 1 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 347 6 0 3 4.0 Fc1ccc(CCCCN2CCN(c3ccc(Cl)cn3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4462108 170823 0 None 1 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 347 6 0 3 4.0 Fc1ccc(CCCCN2CCN(c3ccc(Cl)cn3)CC2)cc1 10.1016/j.bmc.2020.115943
137660046 158796 0 None -6 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 437 7 2 8 2.4 O=C1COc2c(N3CCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4100183 158796 0 None -6 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 437 7 2 8 2.4 O=C1COc2c(N3CCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2N1 10.1021/acs.jmedchem.7b00363
71734129 90630 0 None -11 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 394 9 1 3 5.2 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm400520c
CHEMBL2397480 90630 0 None -11 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 394 9 1 3 5.2 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm400520c
1613 2316 44 None -2 44 Human 8.3 pKi = 8.3 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm00004a016
205 2316 44 None -2 44 Human 8.3 pKi = 8.3 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm00004a016
3964 2316 44 None -2 44 Human 8.3 pKi = 8.3 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm00004a016
CHEMBL831 2316 44 None -2 44 Human 8.3 pKi = 8.3 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm00004a016
DB00408 2316 44 None -2 44 Human 8.3 pKi = 8.3 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm00004a016
1613 2316 44 None -2 44 Human 8.3 pKi = 8.3 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm00043a008
205 2316 44 None -2 44 Human 8.3 pKi = 8.3 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm00043a008
3964 2316 44 None -2 44 Human 8.3 pKi = 8.3 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm00043a008
CHEMBL831 2316 44 None -2 44 Human 8.3 pKi = 8.3 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm00043a008
DB00408 2316 44 None -2 44 Human 8.3 pKi = 8.3 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm00043a008
9839426 12044 0 None -1 5 Human 8.3 pKi = 8.3 Binding
Binding affinity in humans Dopamine receptor D4 expressed in CHO cells was determined using the agonist [3H]spiperone.Binding affinity in humans Dopamine receptor D4 expressed in CHO cells was determined using the agonist [3H]spiperone.
ChEMBL 303 4 2 3 3.5 Oc1cc2c(cc1Cl)CCC(CNCc1ccccc1)O2 10.1021/jm9703653
CHEMBL1184179 12044 0 None -1 5 Human 8.3 pKi = 8.3 Binding
Binding affinity in humans Dopamine receptor D4 expressed in CHO cells was determined using the agonist [3H]spiperone.Binding affinity in humans Dopamine receptor D4 expressed in CHO cells was determined using the agonist [3H]spiperone.
ChEMBL 303 4 2 3 3.5 Oc1cc2c(cc1Cl)CCC(CNCc1ccccc1)O2 10.1021/jm9703653
CHEMBL337228 12044 0 None -1 5 Human 8.3 pKi = 8.3 Binding
Binding affinity in humans Dopamine receptor D4 expressed in CHO cells was determined using the agonist [3H]spiperone.Binding affinity in humans Dopamine receptor D4 expressed in CHO cells was determined using the agonist [3H]spiperone.
ChEMBL 303 4 2 3 3.5 Oc1cc2c(cc1Cl)CCC(CNCc1ccccc1)O2 10.1021/jm9703653
11153076 4888 0 None - 1 Human 8.3 pKi = 8.3 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 375 7 0 4 4.4 CCOc1ccccc1OCC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/jm031111m
CHEMBL104801 4888 0 None - 1 Human 8.3 pKi = 8.3 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 375 7 0 4 4.4 CCOc1ccccc1OCC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/jm031111m
137631542 155870 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 359 6 0 3 4.6 CCOc1ccccc1CC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/acs.jmedchem.7b00151
CHEMBL4066603 155870 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 359 6 0 3 4.6 CCOc1ccccc1CC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/acs.jmedchem.7b00151
72901200 119272 21 None 154 4 Human 8.3 pKi = 8.3 Binding
Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000539a DRD4Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000539a DRD4
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 nan
CHEMBL3480577 119272 21 None 154 4 Human 8.3 pKi = 8.3 Binding
Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000539a DRD4Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000539a DRD4
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 nan
3626837 205584 8 None -125 4 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 373 6 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm100925m
CHEMBL93403 205584 8 None -125 4 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 373 6 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm100925m
10862425 116133 0 None -9 5 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc3ccnn3c2)CC1 10.1021/jm025558r
CHEMBL336930 116133 0 None -9 5 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc3ccnn3c2)CC1 10.1021/jm025558r
44335678 4742 0 None 35 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 366 4 0 2 4.4 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccccc2F)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104155 4742 0 None 35 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 366 4 0 2 4.4 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccccc2F)CC1 10.1016/s0960-894x(02)00655-8
135398737 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0002432
38 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0002432
722 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0002432
CHEMBL42 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0002432
DB00363 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0002432
135398737 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030480f
38 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030480f
722 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030480f
CHEMBL42 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030480f
DB00363 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030480f
21219166 99610 0 None 11 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 317 4 0 3 4.4 c1ccc(CN2CCC(n3cnc(-c4ccccc4)c3)CC2)cc1 10.1016/s0960-894x(99)00169-9
CHEMBL287217 99610 0 None 11 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 317 4 0 3 4.4 c1ccc(CN2CCC(n3cnc(-c4ccccc4)c3)CC2)cc1 10.1016/s0960-894x(99)00169-9
44436608 146223 0 None -47 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 429 7 1 3 4.3 C#Cc1cccc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmc.2007.08.038
CHEMBL392437 146223 0 None -47 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 429 7 1 3 4.3 C#Cc1cccc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmc.2007.08.038
122181332 121359 0 None -8 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 432 9 1 3 5.6 CCCN(CCCCNC(=O)/N=N/c1cc(F)c(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3590083 121359 0 None -8 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 432 9 1 3 5.6 CCCN(CCCCNC(=O)/N=N/c1cc(F)c(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
56833464 68054 0 None -19 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 1138 38 2 16 9.7 CCCN(CCCCNC(=O)c1ccc(OCCCc2cn(CCCCCCCCn3cc(CCCOc4ccc(C(=O)NCCCCN5CCN(c6ccccc6OC)CC5)cc4OC)nn3)nn2)c(OC)c1)C1Cc2ccccc2C1 10.1021/jm2009919
CHEMBL1916720 68054 0 None -19 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 1138 38 2 16 9.7 CCCN(CCCCNC(=O)c1ccc(OCCCc2cn(CCCCCCCCn3cc(CCCOc4ccc(C(=O)NCCCCN5CCN(c6ccccc6OC)CC5)cc4OC)nn3)nn2)c(OC)c1)C1Cc2ccccc2C1 10.1021/jm2009919
11230330 134664 0 None -19 3 Human 7.4 pKi = 7.4 Binding
High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsHigh inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 245 5 0 3 2.8 CCCN(CCC)[C@H]1CCn2c(C#N)ccc2C1 10.1021/jm049269+
CHEMBL372020 134664 0 None -19 3 Human 7.4 pKi = 7.4 Binding
High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsHigh inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 245 5 0 3 2.8 CCCN(CCC)[C@H]1CCn2c(C#N)ccc2C1 10.1021/jm049269+
11417804 4765 0 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 386 7 0 5 3.9 CCOc1cc(C#N)ccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL104216 4765 0 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 386 7 0 5 3.9 CCOc1cc(C#N)ccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
11750030 4785 0 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 402 5 0 4 4.8 Clc1ccc(CN2CCOC(COc3ccc(Cl)c4cccnc34)C2)cc1 10.1021/jm031111m
CHEMBL104307 4785 0 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 402 5 0 4 4.8 Clc1ccc(CN2CCOC(COc3ccc(Cl)c4cccnc34)C2)cc1 10.1021/jm031111m
11058829 168080 0 None 22 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 417 3 1 5 4.7 Clc1ccc2c(c1)C(N1CCN(CCc3ccccc3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL436274 168080 0 None 22 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 417 3 1 5 4.7 Clc1ccc2c(c1)C(N1CCN(CCc3ccccc3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
135398737 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401958n
38 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401958n
722 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401958n
CHEMBL42 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401958n
DB00363 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401958n
49798837 14229 0 None -16 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 433 3 1 3 4.5 OC1(c2ccc(I)cc2)CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1171249 14229 0 None -16 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 433 3 1 3 4.5 OC1(c2ccc(I)cc2)CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1200077 14229 0 None -16 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 433 3 1 3 4.5 OC1(c2ccc(I)cc2)CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmc.2010.05.052
10761258 100638 1 None 8 3 Human 7.4 pKi = 7.4 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 363 4 1 3 3.5 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1cccc(Cl)c1 10.1016/j.bmcl.2005.02.012
CHEMBL295094 100638 1 None 8 3 Human 7.4 pKi = 7.4 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 363 4 1 3 3.5 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1cccc(Cl)c1 10.1016/j.bmcl.2005.02.012
134130247 154038 0 None -2 8 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 308 4 0 3 4.3 c1ccc2c(c1)CCN(CCCc1nc3ccccc3s1)C2 10.1016/j.bmc.2016.09.019
CHEMBL3890153 154038 0 None -2 8 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 308 4 0 3 4.3 c1ccc2c(c1)CCN(CCCc1nc3ccccc3s1)C2 10.1016/j.bmc.2016.09.019
CHEMBL3991291 154038 0 None -2 8 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 308 4 0 3 4.3 c1ccc2c(c1)CCN(CCCc1nc3ccccc3s1)C2 10.1016/j.bmc.2016.09.019
11036640 120634 0 None 12 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 393 7 1 6 2.3 COc1ccccc1N1CCN(CCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm0611152
CHEMBL357684 120634 0 None 12 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 393 7 1 6 2.3 COc1ccccc1N1CCN(CCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm0611152
10040546 204978 0 None -1 3 Human 6.4 pKi = 6.4 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 301 1 0 1 5.0 C[C@H]1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL89719 204978 0 None -1 3 Human 6.4 pKi = 6.4 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 301 1 0 1 5.0 C[C@H]1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
155552695 173472 0 None -22 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 268 3 0 3 2.7 CCc1cc(Cl)c(OC)c(N2CCN(C)CC2)c1 10.1021/acs.jmedchem.6b00860
CHEMBL4543685 173472 0 None -22 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 268 3 0 3 2.7 CCc1cc(Cl)c(OC)c(N2CCN(C)CC2)c1 10.1021/acs.jmedchem.6b00860
11407122 167250 0 None - 1 Human 6.4 pKi = 6.4 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 406 7 0 6 3.9 COc1ccc([N+](=O)[O-])cc1OCC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/jm031111m
CHEMBL430658 167250 0 None - 1 Human 6.4 pKi = 6.4 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 406 7 0 6 3.9 COc1ccc([N+](=O)[O-])cc1OCC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/jm031111m
12050201 201185 0 None -2 4 Human 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 471 7 1 5 5.3 COc1ccc(Br)cc1-c1nc(CNC2CCN(Cc3ccccc3)CC2)cs1 10.1016/s0960-894x(00)00405-4
CHEMBL62624 201185 0 None -2 4 Human 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 471 7 1 5 5.3 COc1ccc(Br)cc1-c1nc(CNC2CCN(Cc3ccccc3)CC2)cs1 10.1016/s0960-894x(00)00405-4
42626318 55943 0 None -3090 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in human HEK293 cell membrane for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in human HEK293 cell membrane for 1 hr by liquid scintillation counting analysis
ChEMBL 460 7 3 4 3.8 O=C(NCC[C@@H](O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/ml500006v
CHEMBL1627306 55943 0 None -3090 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in human HEK293 cell membrane for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in human HEK293 cell membrane for 1 hr by liquid scintillation counting analysis
ChEMBL 460 7 3 4 3.8 O=C(NCC[C@@H](O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/ml500006v
71658205 89975 0 None -51 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 481 9 1 5 5.3 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(-c3ccc(F)cc3)s2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386619 89975 0 None -51 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 481 9 1 5 5.3 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(-c3ccc(F)cc3)s2)CC1 10.1016/j.bmc.2013.03.074
44438234 93178 2 None -19 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 341 3 1 3 4.6 OC1(c2ccc(Cl)cc2)CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246644 93178 2 None -19 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 341 3 1 3 4.6 OC1(c2ccc(Cl)cc2)CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
16094681 82934 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 343 4 1 3 2.6 Cc1cc(F)ccc1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
CHEMBL219261 82934 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 343 4 1 3 2.6 Cc1cc(F)ccc1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
164609172 183825 0 None -91 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 378 6 1 5 2.8 O=C1CCc2cc(C(=O)CCCN3CCN(c4ccccn4)CC3)ccc2N1 10.1016/j.ejmech.2021.113243
CHEMBL4845947 183825 0 None -91 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 378 6 1 5 2.8 O=C1CCc2cc(C(=O)CCCN3CCN(c4ccccn4)CC3)ccc2N1 10.1016/j.ejmech.2021.113243
127051592 140347 0 None -18 7 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 317 5 0 2 3.4 [O-][S+](CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818710 140347 0 None -18 7 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 317 5 0 2 3.4 [O-][S+](CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819742 140347 0 None -18 7 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 317 5 0 2 3.4 [O-][S+](CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
56594534 70256 0 None -39 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 320 1 2 2 3.2 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2C[C@@H]1CO 10.1021/jm200676f
CHEMBL1949728 70256 0 None -39 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 320 1 2 2 3.2 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2C[C@@H]1CO 10.1021/jm200676f
11036640 120634 0 None 12 5 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 393 7 1 6 2.3 COc1ccccc1N1CCN(CCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
CHEMBL357684 120634 0 None 12 5 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 393 7 1 6 2.3 COc1ccccc1N1CCN(CCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
10761258 100638 1 None 8 3 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 363 4 1 3 3.5 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1cccc(Cl)c1 10.1021/jm970021c
CHEMBL295094 100638 1 None 8 3 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 363 4 1 3 3.5 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1cccc(Cl)c1 10.1021/jm970021c
134130247 154038 0 None -2 8 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 308 4 0 3 4.3 c1ccc2c(c1)CCN(CCCc1nc3ccccc3s1)C2 10.1016/j.bmc.2016.09.019
CHEMBL3890153 154038 0 None -2 8 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 308 4 0 3 4.3 c1ccc2c(c1)CCN(CCCc1nc3ccccc3s1)C2 10.1016/j.bmc.2016.09.019
CHEMBL3991291 154038 0 None -2 8 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 308 4 0 3 4.3 c1ccc2c(c1)CCN(CCCc1nc3ccccc3s1)C2 10.1016/j.bmc.2016.09.019
25070742 111290 0 None -2 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2cccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c12 10.1021/jm5004039
CHEMBL3287398 111290 0 None -2 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2cccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c12 10.1021/jm5004039
118709178 112849 0 None -23 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1154 32 0 17 9.5 O=C(CCc1cn(CCOCCOCCOCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3317465 112849 0 None -23 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1154 32 0 17 9.5 O=C(CCc1cn(CCOCCOCCOCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
118709161 112908 0 None -15 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 860 19 0 8 10.5 O=C(CCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318833 112908 0 None -15 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 860 19 0 8 10.5 O=C(CCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
137657322 159096 0 None -53 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 461 8 2 8 2.7 O=Cc1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc12 10.1016/j.bmc.2017.08.037
CHEMBL4103639 159096 0 None -53 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 461 8 2 8 2.7 O=Cc1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc12 10.1016/j.bmc.2017.08.037
164622487 185540 0 None -3 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 339 4 0 4 2.8 O=C1c2ccc(F)cc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL4871850 185540 0 None -3 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 339 4 0 4 2.8 O=C1c2ccc(F)cc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
11584858 82360 0 None -25 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 554 11 1 7 4.1 COc1ccccc1N1CCN(CCCCCNC(=O)c2nnn(Cc3ccccc3Br)c2C)CC1 10.1021/jm0611152
CHEMBL217981 82360 0 None -25 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 554 11 1 7 4.1 COc1ccccc1N1CCN(CCCCCNC(=O)c2nnn(Cc3ccccc3Br)c2C)CC1 10.1021/jm0611152
155562395 175375 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 323 4 1 3 3.5 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)nc1 10.1021/acs.jmedchem.9b00231
CHEMBL4587925 175375 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 323 4 1 3 3.5 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)nc1 10.1021/acs.jmedchem.9b00231
11545813 180612 0 None 4 7 Human 7.4 pKi = 7.4 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 400 6 0 3 5.2 O=C(CCCN1C2CCC1CN(c1ccc(Cl)cc1)CC2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL476109 180612 0 None 4 7 Human 7.4 pKi = 7.4 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 400 6 0 3 5.2 O=C(CCCN1C2CCC1CN(c1ccc(Cl)cc1)CC2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
10617946 203807 0 None -1 3 Human 6.4 pKi = 6.4 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 351 4 1 2 5.1 Clc1ccc(-c2cc(C3CCCN(Cc4ccccc4)C3)[nH]n2)cc1 10.1021/jm970111h
CHEMBL80833 203807 0 None -1 3 Human 6.4 pKi = 6.4 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 351 4 1 2 5.1 Clc1ccc(-c2cc(C3CCCN(Cc4ccccc4)C3)[nH]n2)cc1 10.1021/jm970111h
10805797 112407 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 322 7 1 4 3.7 CCN(CCNc1ccccc1)Cc1ccc2ccc(=O)oc2c1 10.1021/jm990266k
CHEMBL331045 112407 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 322 7 1 4 3.7 CCN(CCNc1ccccc1)Cc1ccc2ccc(=O)oc2c1 10.1021/jm990266k
145979855 165975 0 None -18 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 405 7 2 5 3.5 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccnc3ccccc13)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4279136 165975 0 None -18 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 405 7 2 5 3.5 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccnc3ccccc13)CC2 10.1021/acsmedchemlett.8b00229
44319102 204421 0 None 2 4 Human 6.4 pKi = 6.4 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 321 4 0 4 2.7 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CO2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL86060 204421 0 None 2 4 Human 6.4 pKi = 6.4 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 321 4 0 4 2.7 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CO2)cc1 10.1016/s0960-894x(01)00484-x
20354789 114026 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 281 5 0 2 3.5 c1ccc(CCC2CN(Cc3ccccc3)CCO2)cc1 10.1021/ml500267c
CHEMBL3335544 114026 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 281 5 0 2 3.5 c1ccc(CCC2CN(Cc3ccccc3)CCO2)cc1 10.1021/ml500267c
142590702 179216 0 None -1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 466 8 1 3 5.7 O=C(c1ccccc1)N1CCC(NCCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2020.112674
CHEMBL4744824 179216 0 None -1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 466 8 1 3 5.7 O=C(c1ccccc1)N1CCC(NCCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2020.112674
22727346 13054 0 None -10 3 Human 6.4 pKi = 6.4 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 435 9 0 6 4.8 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4C)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
CHEMBL1190866 13054 0 None -10 3 Human 6.4 pKi = 6.4 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 435 9 0 6 4.8 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4C)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
CHEMBL541791 13054 0 None -10 3 Human 6.4 pKi = 6.4 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 435 9 0 6 4.8 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4C)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
10597050 108709 0 None -3 3 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 398 6 0 3 5.4 COc1cccc2c1CCCC2CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm991138z
CHEMBL321557 108709 0 None -3 3 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 398 6 0 3 5.4 COc1cccc2c1CCCC2CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm991138z
44393372 65994 0 None -48 5 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 549 8 1 5 4.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(I)ccc3s2)CC1 10.1016/j.bmcl.2004.05.052
CHEMBL184993 65994 0 None -48 5 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 549 8 1 5 4.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(I)ccc3s2)CC1 10.1016/j.bmcl.2004.05.052
127053198 138842 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 317 5 0 3 3.6 Clc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793112 138842 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 317 5 0 3 3.6 Clc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
127029390 138953 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1ccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3794421 138953 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1ccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
56964794 73716 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 418 3 0 5 4.8 Clc1ccc2c(c1)N=C(N1CCN(CCc3ccccc3)CC1)c1cccnc1O2 10.1021/jm2013419
CHEMBL2022272 73716 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 418 3 0 5 4.8 Clc1ccc2c(c1)N=C(N1CCN(CCc3ccccc3)CC1)c1cccnc1O2 10.1021/jm2013419
122189393 122732 0 None -7 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 455 6 0 7 4.0 Clc1cccc(N2CCN(CCCc3cn(-c4ccn5nccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.07.050
CHEMBL3613879 122732 0 None -7 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 455 6 0 7 4.0 Clc1cccc(N2CCN(CCCc3cn(-c4ccn5nccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.07.050
46917563 67993 0 None -58 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 561 18 1 7 5.5 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)C3Cc4ccccc4C3)cc2OC)nn1 10.1021/jm2009919
CHEMBL1916551 67993 0 None -58 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 561 18 1 7 5.5 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)C3Cc4ccccc4C3)cc2OC)nn1 10.1021/jm2009919
1353 1880 85 None -3 85 Human 7.4 pKi = 7.4 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(02)00179-8
3559 1880 85 None -3 85 Human 7.4 pKi = 7.4 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(02)00179-8
86 1880 85 None -3 85 Human 7.4 pKi = 7.4 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(02)00179-8
CHEMBL54 1880 85 None -3 85 Human 7.4 pKi = 7.4 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(02)00179-8
DB00502 1880 85 None -3 85 Human 7.4 pKi = 7.4 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(02)00179-8
10761912 111825 0 None 6 3 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 373 6 1 4 3.5 COc1cccc(NC(=O)CCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
CHEMBL329228 111825 0 None 6 3 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 373 6 1 4 3.5 COc1cccc(NC(=O)CCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
10810976 206186 0 None 10 3 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 399 5 0 4 3.2 COc1cccc2c1CCN(CCN1CCN(c3ccc(Cl)cc3)CC1)C2=O 10.1021/jm991138z
CHEMBL96799 206186 0 None 10 3 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 399 5 0 4 3.2 COc1cccc2c1CCN(CCN1CCN(c3ccc(Cl)cc3)CC1)C2=O 10.1021/jm991138z
9928335 119592 1 None -1 6 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 349 4 1 3 3.3 Cc1ccc(N2CCN(CC[C@H]3NC(=O)c4ccccc43)CC2)cc1C 10.1016/s0960-894x(98)00252-2
CHEMBL35093 119592 1 None -1 6 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 349 4 1 3 3.3 Cc1ccc(N2CCN(CC[C@H]3NC(=O)c4ccccc43)CC2)cc1C 10.1016/s0960-894x(98)00252-2
10520781 205257 0 None - 1 Human 6.4 pKi = 6.4 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 335 2 0 4 3.0 COc1ccc2c3c(c(=O)oc2c1)CN(C(=O)c1ccccc1)CC3 10.1021/jm970170v
CHEMBL91367 205257 0 None - 1 Human 6.4 pKi = 6.4 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 335 2 0 4 3.0 COc1ccc2c3c(c(=O)oc2c1)CN(C(=O)c1ccccc1)CC3 10.1021/jm970170v
16103 202932 37 None -5 4 Human 6.4 pKi = 6.4 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 292 0 1 4 3.1 CN1CCN(C2=Nc3ccccc3Nc3ccccc32)CC1 10.1021/jm00043a008
CHEMBL73538 202932 37 None -5 4 Human 6.4 pKi = 6.4 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 292 0 1 4 3.1 CN1CCN(C2=Nc3ccccc3Nc3ccccc32)CC1 10.1021/jm00043a008
1438298 38383 4 None 26 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in cell membranes incubated for 60 mins by scintillation counting methodDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 328 5 1 3 2.9 Cc1ccc(C(=O)C2CCN(CC(=O)NC3CCCC3)CC2)cc1 10.1021/acs.jmedchem.9b01560
CHEMBL1465169 38383 4 None 26 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in cell membranes incubated for 60 mins by scintillation counting methodDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 328 5 1 3 2.9 Cc1ccc(C(=O)C2CCN(CC(=O)NC3CCCC3)CC2)cc1 10.1021/acs.jmedchem.9b01560
44381146 58199 0 None 1 4 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 429 7 1 4 3.6 COc1cc(N(C)C(C)=O)c(Cl)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL168372 58199 0 None 1 4 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 429 7 1 4 3.6 COc1cc(N(C)C(C)=O)c(Cl)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL5087504 213330 0 None -1 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None Oc1cccc(C(CCNCCCCN2CCN(c3ccccc3)CC2)c2cccc(O)c2)c1 10.1021/acs.jmedchem.1c00611
17755868 142586 1 None -5 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 295 0 1 2 3.8 CN1CCCc2ccccc2Cc2ccc(O)cc2CCC1 10.1021/jm070388+
CHEMBL389559 142586 1 None -5 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 295 0 1 2 3.8 CN1CCCc2ccccc2Cc2ccc(O)cc2CCC1 10.1021/jm070388+
44330650 106918 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 212 0 1 1 3.2 Cc1ccc(C)c2c1CCCc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
CHEMBL317988 106918 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 212 0 1 1 3.2 Cc1ccc(C)c2c1CCCc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
11676873 9105 0 None -1071 6 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 455 8 1 4 4.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc3c(c2)Cc2ccccc2-3)CC1 10.1021/jm0704200
CHEMBL110365 9105 0 None -1071 6 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 455 8 1 4 4.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc3c(c2)Cc2ccccc2-3)CC1 10.1021/jm0704200
122180612 121226 0 None -72 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 467 9 0 6 5.2 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc(-c4ccccc4)cc3)nn2)CC1 10.1016/j.bmc.2015.01.017
CHEMBL3588983 121226 0 None -72 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 467 9 0 6 5.2 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc(-c4ccccc4)cc3)nn2)CC1 10.1016/j.bmc.2015.01.017
17755991 151766 0 None -14 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 267 0 2 2 3.1 Oc1ccc2c(c1)CCCNCCc1ccccc1C2 10.1021/jm070388+
CHEMBL396950 151766 0 None -14 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 267 0 2 2 3.1 Oc1ccc2c(c1)CCCNCCc1ccccc1C2 10.1021/jm070388+
CHEMBL5073904 212536 0 None -6 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None N#CC(CCNCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
16744004 91896 0 None -204 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 535 10 0 6 5.7 COc1ccc(C2=NO[C@H](CCCN3CCN(C(c4ccc(F)cc4)c4ccc(F)cc4)CC3)C2)cc1OC 10.1016/j.ejmech.2006.12.030
CHEMBL243012 91896 0 None -204 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 535 10 0 6 5.7 COc1ccc(C2=NO[C@H](CCCN3CCN(C(c4ccc(F)cc4)c4ccc(F)cc4)CC3)C2)cc1OC 10.1016/j.ejmech.2006.12.030
72191068 91923 0 None -3 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-spiperone from cloned human dopamine D4 receptorDisplacement of [3H]-spiperone from cloned human dopamine D4 receptor
ChEMBL 458 9 0 8 4.2 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc(-c4cnco4)cc3)nn2)CC1 10.1016/j.bmcl.2013.08.047
CHEMBL2430438 91923 0 None -3 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-spiperone from cloned human dopamine D4 receptorDisplacement of [3H]-spiperone from cloned human dopamine D4 receptor
ChEMBL 458 9 0 8 4.2 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc(-c4cnco4)cc3)nn2)CC1 10.1016/j.bmcl.2013.08.047
168270563 189357 0 None -1 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5170381 189357 0 None -1 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)cc1F 10.1016/j.bmcl.2022.128615
9843137 4759 0 None 6 2 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 385 4 0 4 2.9 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCOc2ccccc21 10.1016/s0960-894x(02)00655-8
CHEMBL104196 4759 0 None 6 2 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 385 4 0 4 2.9 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCOc2ccccc21 10.1016/s0960-894x(02)00655-8
71657944 89963 0 None -77 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 421 8 1 5 4.2 COc1ccccc1N1CCCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386607 89963 0 None -77 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 421 8 1 5 4.2 COc1ccccc1N1CCCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1016/j.bmc.2013.03.074
49783209 17427 0 None -74 27 Rat 7.4 pKi = 7.4 Binding
Binding affinity to rat dopamine D4 receptorBinding affinity to rat dopamine D4 receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258223 17427 0 None -74 27 Rat 7.4 pKi = 7.4 Binding
Binding affinity to rat dopamine D4 receptorBinding affinity to rat dopamine D4 receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
44335996 4856 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 417 4 0 3 4.1 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)c(Cl)c2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL104678 4856 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 417 4 0 3 4.1 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)c(Cl)c2)CC1 10.1016/s0960-894x(02)00656-x
9796180 112372 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 295 6 1 4 3.0 O=c1ccc2ccc(CNCCOc3ccccc3)cc2o1 10.1021/jm990266k
CHEMBL330966 112372 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 295 6 1 4 3.0 O=c1ccc2ccc(CNCCOc3ccccc3)cc2o1 10.1021/jm990266k
93601125 138821 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 343 7 0 5 3.0 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1OC 10.1016/j.bmcl.2016.03.102
CHEMBL3792941 138821 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 343 7 0 5 3.0 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1OC 10.1016/j.bmcl.2016.03.102
44276170 95870 0 None -12 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 382 9 0 5 3.9 COc1cccc(C(=O)CCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/S0960-894X(97)00218-7
CHEMBL26135 95870 0 None -12 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 382 9 0 5 3.9 COc1cccc(C(=O)CCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/S0960-894X(97)00218-7
10001519 98852 0 None -8 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 408 8 0 4 5.1 COc1ccccc1N1CCN(CCCCC2CCCc3c(OC)cccc32)CC1 10.1016/S0960-894X(97)00218-7
CHEMBL28209 98852 0 None -8 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 408 8 0 4 5.1 COc1ccccc1N1CCN(CCCCC2CCCc3c(OC)cccc32)CC1 10.1016/S0960-894X(97)00218-7
44431463 87642 2 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 378 4 1 2 4.9 O=C(NC1CCN(Cc2ccc(Cl)cc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
CHEMBL234641 87642 2 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 378 4 1 2 4.9 O=C(NC1CCN(Cc2ccc(Cl)cc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
11761412 116451 0 None -89 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 411 9 1 4 3.6 COc1ccccc1N1CCN(CCCCNC(=O)/C=C/c2ccc(F)cc2)CC1 10.1016/j.bmcl.2010.09.142
CHEMBL338606 116451 0 None -89 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 411 9 1 4 3.6 COc1ccccc1N1CCN(CCCCNC(=O)/C=C/c2ccc(F)cc2)CC1 10.1016/j.bmcl.2010.09.142
72737744 114020 0 None 64 3 Human 7.4 pKi = 7.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 365 6 0 3 4.4 FC(F)(F)Oc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
CHEMBL3335538 114020 0 None 64 3 Human 7.4 pKi = 7.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 365 6 0 3 4.4 FC(F)(F)Oc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
44408818 139635 1 None -21 6 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)CCN(C)CCc1ccccc1C2 10.1016/j.bmc.2009.08.028
CHEMBL380330 139635 1 None -21 6 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)CCN(C)CCc1ccccc1C2 10.1016/j.bmc.2009.08.028
164621388 185154 0 None -7 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 341 4 0 3 3.7 Clc1ccc2c(c1)CC(CCN1CCN(c3ccccn3)CC1)C2 10.1016/j.ejmech.2021.113243
CHEMBL4866058 185154 0 None -7 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 341 4 0 3 3.7 Clc1ccc2c(c1)CC(CCN1CCN(c3ccccn3)CC1)C2 10.1016/j.ejmech.2021.113243
11328099 4781 0 None - 1 Human 6.4 pKi = 6.4 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 439 6 0 4 3.6 COc1cc(I)ccc1OCC1CN(Cc2ccccc2)CCO1 10.1021/jm031111m
CHEMBL104291 4781 0 None - 1 Human 6.4 pKi = 6.4 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 439 6 0 4 3.6 COc1cc(I)ccc1OCC1CN(Cc2ccccc2)CCO1 10.1021/jm031111m
9826801 107451 0 None -18620 12 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 488 6 1 7 3.2 Cn1nnc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL319352 107451 0 None -18620 12 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 488 6 1 7 3.2 Cn1nnc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
57390694 70122 0 None -1 6 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 385 5 0 4 5.1 Clc1ccc(N2CCCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2012.01.022
CHEMBL1946255 70122 0 None -1 6 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 385 5 0 4 5.1 Clc1ccc(N2CCCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2012.01.022
57390694 70122 0 None -1 6 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 385 5 0 4 5.1 Clc1ccc(N2CCCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.ejmech.2012.03.042
CHEMBL1946255 70122 0 None -1 6 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 385 5 0 4 5.1 Clc1ccc(N2CCCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.ejmech.2012.03.042
57403981 70151 0 None -33 6 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 426 6 1 4 5.8 OC1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2CCCCc1nc2ccccc2s1 10.1016/j.bmc.2012.01.022
CHEMBL1946745 70151 0 None -33 6 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 426 6 1 4 5.8 OC1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2CCCCc1nc2ccccc2s1 10.1016/j.bmc.2012.01.022
76524414 140338 0 None -33 8 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 426 6 1 4 5.8 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCCc1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL3819434 140338 0 None -33 8 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 426 6 1 4 5.8 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCCc1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL3819713 140338 0 None -33 8 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 426 6 1 4 5.8 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCCc1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
44330639 206434 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 219 0 0 4 2.4 Cc1sc(C)c2c1CCCc1nncn1-2 10.1016/s0960-894x(03)00587-0
CHEMBL98331 206434 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 219 0 0 4 2.4 Cc1sc(C)c2c1CCCc1nncn1-2 10.1016/s0960-894x(03)00587-0
11488247 198955 0 None -7244 4 Human 5.4 pKi = 5.4 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 470 5 1 4 4.5 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccc(CN(C)S(=O)(=O)c3ccccc3)cc2)C1 10.1016/j.bmcl.2009.12.100
CHEMBL599487 198955 0 None -7244 4 Human 5.4 pKi = 5.4 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 470 5 1 4 4.5 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccc(CN(C)S(=O)(=O)c3ccccc3)cc2)C1 10.1016/j.bmcl.2009.12.100
71062664 146328 0 None - 1 Mouse 6.4 pKi = 6.4 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 6 0 5 2.5 Cc1ncccc1OC[C@@H]1CN(CCN2CCc3ccccc32)CCO1 nan
CHEMBL3925231 146328 0 None - 1 Mouse 6.4 pKi = 6.4 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 6 0 5 2.5 Cc1ncccc1OC[C@@H]1CN(CCN2CCc3ccccc32)CCO1 nan
76524414 140338 0 None -33 8 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 426 6 1 4 5.8 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCCc1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL3819434 140338 0 None -33 8 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 426 6 1 4 5.8 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCCc1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL3819713 140338 0 None -33 8 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 426 6 1 4 5.8 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCCc1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
46231849 199733 0 None -2754 4 Human 5.4 pKi = 5.4 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 356 1 2 4 3.8 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(/C=N/O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL604732 199733 0 None -2754 4 Human 5.4 pKi = 5.4 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 356 1 2 4 3.8 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(/C=N/O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
9950913 102279 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 363 3 0 3 3.1 Cc1ccc(CN2CCN(C3CCc4ccccc4N(C)C3=O)CC2)cc1 10.1016/s0960-894x(00)00421-2
CHEMBL305061 102279 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 363 3 0 3 3.1 Cc1ccc(CN2CCN(C3CCc4ccccc4N(C)C3=O)CC2)cc1 10.1016/s0960-894x(00)00421-2
11794570 197068 0 None 3 3 Human 7.4 pKi = 7.4 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 386 4 0 3 6.0 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)on3)CC2)cc1 10.1021/jm970111h
CHEMBL58296 197068 0 None 3 3 Human 7.4 pKi = 7.4 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 386 4 0 3 6.0 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)on3)CC2)cc1 10.1021/jm970111h
10884046 164817 0 None -3 5 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
CHEMBL423735 164817 0 None -3 5 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
44403213 71443 4 None -83 5 Human 7.4 pKi = 7.4 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 423 7 1 3 4.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2005.07.037
CHEMBL196744 71443 4 None -83 5 Human 7.4 pKi = 7.4 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 423 7 1 3 4.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2005.07.037
155531809 171091 0 None 11 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 555 8 2 4 4.3 O=C(NCCN1CCN(c2ccc(I)cc2)CC1)NN(Cc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
CHEMBL4466114 171091 0 None 11 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 555 8 2 4 4.3 O=C(NCCN1CCN(c2ccc(I)cc2)CC1)NN(Cc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
162648426 179380 0 None 2 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 373 6 0 3 4.6 Fc1ccc(CCCCN2C3CCC2CN(c2ccc(Cl)cn2)C3)cc1 10.1016/j.bmc.2020.115943
CHEMBL4746695 179380 0 None 2 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 373 6 0 3 4.6 Fc1ccc(CCCCN2C3CCC2CN(c2ccc(Cl)cn2)C3)cc1 10.1016/j.bmc.2020.115943
127053215 138894 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 313 6 0 4 3.0 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793858 138894 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 313 6 0 4 3.0 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
164621388 185154 0 None -7 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 341 4 0 3 3.7 Clc1ccc2c(c1)CC(CCN1CCN(c3ccccn3)CC1)C2 10.1016/j.ejmech.2021.113243
CHEMBL4866058 185154 0 None -7 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 341 4 0 3 3.7 Clc1ccc2c(c1)CC(CCN1CCN(c3ccccn3)CC1)C2 10.1016/j.ejmech.2021.113243
44431466 87643 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 422 4 1 2 5.0 O=C(NC1CCN(Cc2ccc(Br)cc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
CHEMBL234643 87643 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 422 4 1 2 5.0 O=C(NC1CCN(Cc2ccc(Br)cc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
3038495 700 30 None -91 19 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm060138d
7625 700 30 None -91 19 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm060138d
CHEMBL25236 700 30 None -91 19 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm060138d
11794570 197068 0 None 3 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 386 4 0 3 6.0 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)on3)CC2)cc1 10.1021/jm960072u
CHEMBL58296 197068 0 None 3 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 386 4 0 3 6.0 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)on3)CC2)cc1 10.1021/jm960072u
1248739 139556 16 None 19 6 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 310 3 0 4 2.8 Fc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1 10.1021/jm060166w
CHEMBL380054 139556 16 None 19 6 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 310 3 0 4 2.8 Fc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1 10.1021/jm060166w
22100962 202564 0 None 40 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 340 3 0 3 5.2 Clc1ccc2sc(C3=CCN(Cc4ccccc4)CC3)nc2c1 10.1016/S0960-894X(97)00402-2
CHEMBL71209 202564 0 None 40 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 340 3 0 3 5.2 Clc1ccc2sc(C3=CCN(Cc4ccccc4)CC3)nc2c1 10.1016/S0960-894X(97)00402-2
135398737 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled clozapine from human dopamine D4.4 receptorDisplacement of radiolabeled clozapine from human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm8007618
38 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled clozapine from human dopamine D4.4 receptorDisplacement of radiolabeled clozapine from human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm8007618
722 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled clozapine from human dopamine D4.4 receptorDisplacement of radiolabeled clozapine from human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm8007618
CHEMBL42 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled clozapine from human dopamine D4.4 receptorDisplacement of radiolabeled clozapine from human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm8007618
DB00363 944 89 None -13 91 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled clozapine from human dopamine D4.4 receptorDisplacement of radiolabeled clozapine from human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm8007618
3038495 700 30 None -91 19 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm050170s
7625 700 30 None -91 19 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm050170s
CHEMBL25236 700 30 None -91 19 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm050170s
60165541 74996 0 None 1 5 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 364 6 0 4 5.1 O=C(CCCN1CCC(c2ccccc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL2037518 74996 0 None 1 5 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 364 6 0 4 5.1 O=C(CCCN1CCC(c2ccccc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
44329749 112107 0 None -28 3 Human 7.4 pKi = 7.4 Binding
Tested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cellsTested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cells
ChEMBL 265 2 1 4 2.7 CCCN1CCOC2c3cc(O)ccc3SCC21 10.1021/jm0000113
CHEMBL330216 112107 0 None -28 3 Human 7.4 pKi = 7.4 Binding
Tested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cellsTested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cells
ChEMBL 265 2 1 4 2.7 CCCN1CCOC2c3cc(O)ccc3SCC21 10.1021/jm0000113
164609650 184414 0 None -1 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 389 4 0 4 4.0 O=C1c2cc(Cl)c(Cl)cc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL4854456 184414 0 None -1 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 389 4 0 4 4.0 O=C1c2cc(Cl)c(Cl)cc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
10003809 82752 0 None -97 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 448 8 1 6 4.1 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(C#N)ccc3s2)CC1 10.1021/jm0611152
CHEMBL218318 82752 0 None -97 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 448 8 1 6 4.1 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(C#N)ccc3s2)CC1 10.1021/jm0611152
137653986 158184 0 None -2 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 249 1 3 5 0.1 O=C1COc2c(N3CCNCC3)ccc(O)c2N1 10.1016/j.bmc.2017.08.037
CHEMBL4093493 158184 0 None -2 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 249 1 3 5 0.1 O=C1COc2c(N3CCNCC3)ccc(O)c2N1 10.1016/j.bmc.2017.08.037
44319369 204105 0 None 2 4 Human 6.4 pKi = 6.4 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 335 4 0 4 3.0 C[C@@H]1OC(c2ccccc2)=N[C@H]1CN1CCN(c2ccccc2)CC1 10.1016/s0960-894x(01)00484-x
CHEMBL83306 204105 0 None 2 4 Human 6.4 pKi = 6.4 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 335 4 0 4 3.0 C[C@@H]1OC(c2ccccc2)=N[C@H]1CN1CCN(c2ccccc2)CC1 10.1016/s0960-894x(01)00484-x
168292271 191292 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 424 6 1 3 5.1 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(Cl)c(F)c2)CC1 10.1016/j.bmcl.2022.128615
CHEMBL5199815 191292 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 424 6 1 3 5.1 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(Cl)c(F)c2)CC1 10.1016/j.bmcl.2022.128615
44381432 120206 0 None -1 4 Human 5.4 pKi = 5.4 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 334 3 1 4 2.6 c1ccc(C2=NC[C@@H](N3CCN(c4ccccc4)CC3)CCN2)cc1 10.1016/s0960-894x(03)00004-0
CHEMBL354748 120206 0 None -1 4 Human 5.4 pKi = 5.4 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 334 3 1 4 2.6 c1ccc(C2=NC[C@@H](N3CCN(c4ccccc4)CC3)CCN2)cc1 10.1016/s0960-894x(03)00004-0
71658208 89978 0 None -10 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 441 10 1 6 3.4 COc1ccccc1N1CCCN(CCCCNC(=O)c2cccc(OC)c2OC)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386622 89978 0 None -10 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 441 10 1 6 3.4 COc1ccccc1N1CCCN(CCCCNC(=O)c2cccc(OC)c2OC)CC1 10.1016/j.bmc.2013.03.074
134141355 154048 0 None -3 9 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 327 5 0 2 4.8 O=C(CCCN1CCCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.09.019
CHEMBL3924565 154048 0 None -3 9 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 327 5 0 2 4.8 O=C(CCCN1CCCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.09.019
CHEMBL3991357 154048 0 None -3 9 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 327 5 0 2 4.8 O=C(CCCN1CCCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.09.019
44582675 189109 0 None -7 15 Human 6.4 pKi = 6.4 Binding
Inhibition of human cloned dopamine D4 receptor by competitive binding experimentInhibition of human cloned dopamine D4 receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1[C@H](O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL515472 189109 0 None -7 15 Human 6.4 pKi = 6.4 Binding
Inhibition of human cloned dopamine D4 receptor by competitive binding experimentInhibition of human cloned dopamine D4 receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1[C@H](O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
76318477 105808 0 None -2454 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 422 8 3 5 3.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(O)ccc3[nH]2)CC1 10.1039/c3md00098b
CHEMBL3133875 105808 0 None -2454 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 422 8 3 5 3.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(O)ccc3[nH]2)CC1 10.1039/c3md00098b
CHEMBL3139049 105808 0 None -2454 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 422 8 3 5 3.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(O)ccc3[nH]2)CC1 10.1039/c3md00098b
44438226 154125 0 None -2 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 395 5 2 2 4.5 CC(=O)NCC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL399601 154125 0 None -2 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 395 5 2 2 4.5 CC(=O)NCC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
122180573 121211 0 None -891 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 517 7 0 5 6.3 Clc1cccc(N2CCN(CCCCc3cn(-c4ccc5c(c4)Cc4ccccc4-5)nn3)CC2)c1Cl 10.1016/j.bmc.2015.01.017
CHEMBL3588918 121211 0 None -891 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 517 7 0 5 6.3 Clc1cccc(N2CCN(CCCCc3cn(-c4ccc5c(c4)Cc4ccccc4-5)nn3)CC2)c1Cl 10.1016/j.bmc.2015.01.017
134141355 154048 0 None -3 9 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 327 5 0 2 4.8 O=C(CCCN1CCCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.09.019
CHEMBL3924565 154048 0 None -3 9 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 327 5 0 2 4.8 O=C(CCCN1CCCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.09.019
CHEMBL3991357 154048 0 None -3 9 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 327 5 0 2 4.8 O=C(CCCN1CCCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.09.019
168295019 191901 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(CO[C@H]2CCCN(Cc3ncn4ccccc34)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5209079 191901 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(CO[C@H]2CCCN(Cc3ncn4ccccc34)C2)cc1F 10.1016/j.bmcl.2022.128615
44396220 124903 1 None -177 6 Human 5.4 pKi = 5.4 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 295 6 0 2 4.1 c1ccc(Cc2ccccc2OCCN2CCCCC2)cc1 10.1021/jm049720x
CHEMBL364565 124903 1 None -177 6 Human 5.4 pKi = 5.4 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 295 6 0 2 4.1 c1ccc(Cc2ccccc2OCCN2CCCCC2)cc1 10.1021/jm049720x
133633 2210 46 None -104 8 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1016/j.bmc.2010.05.052
177 2210 46 None -104 8 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1016/j.bmc.2010.05.052
CHEMBL445102 2210 46 None -104 8 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1016/j.bmc.2010.05.052
44278496 99088 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 389 8 0 3 5.2 COC(COc1cccc2ccccc12)CN1CCC(Cc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
CHEMBL28355 99088 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 389 8 0 3 5.2 COC(COc1cccc2ccccc12)CN1CCC(Cc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
44278624 99880 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 409 7 1 3 5.2 OC(COc1cccc2ccccc12)CN1CCC(Cc2ccc(Cl)cc2)CC1 10.1016/S0960-894X(97)00233-3
CHEMBL28953 99880 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 409 7 1 3 5.2 OC(COc1cccc2ccccc12)CN1CCC(Cc2ccc(Cl)cc2)CC1 10.1016/S0960-894X(97)00233-3
52943802 17436 0 None 7 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 363 6 0 2 5.8 Cc1ccc(C)c(C(=O)CCCN2CCC(c3cc(C)ccc3C)CC2)c1 10.1021/jm100899z
CHEMBL1258270 17436 0 None 7 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 363 6 0 2 5.8 Cc1ccc(C)c(C(=O)CCCN2CCC(c3cc(C)ccc3C)CC2)c1 10.1021/jm100899z
57395341 68969 0 None -2 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 495 13 1 8 2.8 CCOCCOCc1ccn2ncc(C(=O)NCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
CHEMBL1928135 68969 0 None -2 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 495 13 1 8 2.8 CCOCCOCc1ccn2ncc(C(=O)NCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
71583849 87304 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 448 4 0 4 5.1 c1ccc(-n2cc(CN3CCN(c4cc5ccc4CCc4ccc(cc4)CC5)CC3)cn2)cc1 10.1016/j.bmc.2013.01.065
CHEMBL2336893 87304 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 448 4 0 4 5.1 c1ccc(-n2cc(CN3CCN(c4cc5ccc4CCc4ccc(cc4)CC5)CC3)cn2)cc1 10.1016/j.bmc.2013.01.065
164609650 184414 0 None -1 7 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 389 4 0 4 4.0 O=C1c2cc(Cl)c(Cl)cc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL4854456 184414 0 None -1 7 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 389 4 0 4 4.0 O=C1c2cc(Cl)c(Cl)cc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
6937303 201517 6 None 3 4 Human 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 335 4 0 4 4.1 c1ccc(-c2nc(CN3CCN(c4ccccc4)CC3)cs2)cc1 10.1016/s0960-894x(00)00405-4
CHEMBL64376 201517 6 None 3 4 Human 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 335 4 0 4 4.1 c1ccc(-c2nc(CN3CCN(c4ccccc4)CC3)cs2)cc1 10.1016/s0960-894x(00)00405-4
44264742 96726 0 None 1 4 Human 5.4 pKi = 5.4 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 298 3 0 4 2.8 c1ccn2ncc(CN3CCN(C4CCCCC4)CC3)c2c1 10.1016/s0960-894x(98)00692-1
CHEMBL268190 96726 0 None 1 4 Human 5.4 pKi = 5.4 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 298 3 0 4 2.8 c1ccn2ncc(CN3CCN(C4CCCCC4)CC3)c2c1 10.1016/s0960-894x(98)00692-1
75201901 165872 14 None -331 24 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4277264 165872 14 None -331 24 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
42626380 55950 0 None -125 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 548 8 3 5 3.1 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3cc(I)ccc3[nH]2)CC1 10.1021/jm900095y
CHEMBL1627313 55950 0 None -125 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 548 8 3 5 3.1 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3cc(I)ccc3[nH]2)CC1 10.1021/jm900095y
3191 102385 93 None -10 25 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 102385 93 None -10 25 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
145986752 166723 0 None -1 17 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
ChEMBL 562 10 1 5 7.3 COc1ccc(N(CCCCN2CCC(O)(c3ccc(Cl)c(C(F)(F)F)c3)CC2)c2ccc(OC)cc2)cc1 10.1016/j.bmcl.2018.10.036
CHEMBL4293307 166723 0 None -1 17 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
ChEMBL 562 10 1 5 7.3 COc1ccc(N(CCCCN2CCC(O)(c3ccc(Cl)c(C(F)(F)F)c3)CC2)c2ccc(OC)cc2)cc1 10.1016/j.bmcl.2018.10.036
44393403 64747 0 None -125 6 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 533 8 1 5 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(I)ccc3o2)CC1 10.1016/j.bmcl.2004.05.052
CHEMBL182379 64747 0 None -125 6 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 533 8 1 5 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(I)ccc3o2)CC1 10.1016/j.bmcl.2004.05.052
10432808 58441 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@H]1CN(Cc2ccccc2)C[C@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
CHEMBL168611 58441 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@H]1CN(Cc2ccccc2)C[C@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
10001207 164769 0 None 38 4 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 402 6 1 3 3.7 COc1ccc(Br)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL423440 164769 0 None 38 4 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 402 6 1 3 3.7 COc1ccc(Br)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
155514137 169261 0 None 15 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 539 9 2 4 5.0 O=C(NCCCN1CCN(c2ccc(Br)cc2)CC1)NN(Cc1ccc(F)cc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
CHEMBL4439728 169261 0 None 15 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 539 9 2 4 5.0 O=C(NCCCN1CCN(c2ccc(Br)cc2)CC1)NN(Cc1ccc(F)cc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
118709179 112927 0 None -18 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1198 35 0 18 9.5 O=C(CCc1cn(CCOCCOCCOCCOCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318851 112927 0 None -18 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1198 35 0 18 9.5 O=C(CCc1cn(CCOCCOCCOCCOCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
44222488 194552 0 None 4 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 382 7 0 4 4.5 Clc1ccc(N2CCN(CCCCCc3cc4ccccn4n3)CC2)cc1 10.1021/jm900690y
CHEMBL561622 194552 0 None 4 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 382 7 0 4 4.5 Clc1ccc(N2CCN(CCCCCc3cc4ccccn4n3)CC2)cc1 10.1021/jm900690y
11303390 4818 0 None - 1 Human 7.3 pKi = 7.3 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 375 7 0 4 4.4 CC(C)Oc1ccccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL104476 4818 0 None - 1 Human 7.3 pKi = 7.3 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 375 7 0 4 4.4 CC(C)Oc1ccccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
8592415 64838 7 None - 1 Human 7.3 pKi = 7.3 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 339 5 1 4 2.8 COc1cccc(N2CCN(CC(=O)Nc3cccc(C)c3)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL182432 64838 7 None - 1 Human 7.3 pKi = 7.3 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 339 5 1 4 2.8 COc1cccc(N2CCN(CC(=O)Nc3cccc(C)c3)CC2)c1 10.1016/j.bmcl.2004.07.068
10763496 111107 0 None 5 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 399 6 1 4 4.1 COc1ccc2c(c1)C(NCCN1CCN(c3ccc(Cl)cc3)CC1)CCC2 10.1021/jm991138z
CHEMBL328283 111107 0 None 5 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 399 6 1 4 4.1 COc1ccc2c(c1)C(NCCN1CCN(c3ccc(Cl)cc3)CC1)CCC2 10.1021/jm991138z
135471592 121168 0 None 3 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 397 3 2 5 4.8 Cc1ccc2c(c1)C(NC1CCN(Cc3ccccc3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL358657 121168 0 None 3 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 397 3 2 5 4.8 Cc1ccc2c(c1)C(NC1CCN(Cc3ccccc3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
72737728 114021 0 None 60 2 Human 7.3 pKi = 7.3 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 311 6 0 3 3.5 COc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
CHEMBL3335539 114021 0 None 60 2 Human 7.3 pKi = 7.3 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 311 6 0 3 3.5 COc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
127051592 140347 0 None -18 7 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 317 5 0 2 3.4 [O-][S+](CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818710 140347 0 None -18 7 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 317 5 0 2 3.4 [O-][S+](CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819742 140347 0 None -18 7 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 317 5 0 2 3.4 [O-][S+](CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
42606339 17749 0 None 19 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptorDisplacement of [3H]Spiperone from human dopamine D4.4 receptor
ChEMBL 397 5 1 4 4.3 Cc1ccc(CNCC2(F)CCN(C(=O)c3csc4ccccc34)CC2)nc1 10.1021/jm100835q
CHEMBL1259241 17749 0 None 19 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptorDisplacement of [3H]Spiperone from human dopamine D4.4 receptor
ChEMBL 397 5 1 4 4.3 Cc1ccc(CNCC2(F)CCN(C(=O)c3csc4ccccc34)CC2)nc1 10.1021/jm100835q
44381279 58431 0 None 10 4 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 348 4 1 4 2.1 O=C1C[C@H](CN2CCN(c3ccccc3)CC2)N=C(c2ccccc2)N1 10.1016/s0960-894x(03)00004-0
CHEMBL168571 58431 0 None 10 4 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 348 4 1 4 2.1 O=C1C[C@H](CN2CCN(c3ccccc3)CC2)N=C(c2ccccc2)N1 10.1016/s0960-894x(03)00004-0
44330638 106793 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 233 0 0 4 2.7 Cc1sc(C)c2c1CCCc1nnc(C)n1-2 10.1016/s0960-894x(03)00587-0
CHEMBL317051 106793 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 233 0 0 4 2.7 Cc1sc(C)c2c1CCCc1nnc(C)n1-2 10.1016/s0960-894x(03)00587-0
44335722 108389 0 None 7 2 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 Cc1cccc2c1CCN2C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL321058 108389 0 None 7 2 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 Cc1cccc2c1CCN2C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
44427827 92843 0 None -1548 6 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 498 8 2 5 4.4 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm0704200
CHEMBL244990 92843 0 None -1548 6 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 498 8 2 5 4.4 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm0704200
44276105 13343 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 381 7 0 5 4.9 Cc1ccccc1N1CCN(CCCCc2cc(-c3cccs3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL1193100 13343 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 381 7 0 5 4.9 Cc1ccccc1N1CCN(CCCCc2cc(-c3cccs3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL544451 13343 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 381 7 0 5 4.9 Cc1ccccc1N1CCN(CCCCc2cc(-c3cccs3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL5093200 213641 0 None -39 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CN(C)CCC(C(=O)NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
10546828 203715 0 None 5 3 Human 7.3 pKi = 7.3 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 365 4 1 2 5.3 CC1(c2cc(-c3ccc(Cl)cc3)[nH]n2)CCN(Cc2ccccc2)CC1 10.1021/jm970111h
CHEMBL80207 203715 0 None 5 3 Human 7.3 pKi = 7.3 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 365 4 1 2 5.3 CC1(c2cc(-c3ccc(Cl)cc3)[nH]n2)CCN(Cc2ccccc2)CC1 10.1021/jm970111h
44323762 204851 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 292 3 1 3 2.9 c1ccc(CN2CCN(c3cccc4[nH]cnc34)CC2)cc1 10.1016/s0960-894x(98)00474-0
CHEMBL88837 204851 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 292 3 1 3 2.9 c1ccc(CN2CCN(c3cccc4[nH]cnc34)CC2)cc1 10.1016/s0960-894x(98)00474-0
44323851 205246 0 None -10 4 Human 7.3 pKi = 7.3 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 302 1 0 2 3.8 C=C1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL91310 205246 0 None -10 4 Human 7.3 pKi = 7.3 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 302 1 0 2 3.8 C=C1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
76309672 85461 0 None 1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 288 3 1 1 2.2 c1ccc(C[n+]2cc[n+](-c3cccc4[nH]cnc34)cc2)cc1 10.1007/s00044-012-0055-5
CHEMBL2298811 85461 0 None 1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 288 3 1 1 2.2 c1ccc(C[n+]2cc[n+](-c3cccc4[nH]cnc34)cc2)cc1 10.1007/s00044-012-0055-5
45482151 196332 0 None -9 4 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D4.4 expressed in CHO cellsBinding affinity to human cloned dopamine D4.4 expressed in CHO cells
ChEMBL 451 8 1 9 1.7 COc1ccccc1N1CCN(CCNC(=O)c2cn(-c3ccc([N+](=O)[O-])cc3)nn2)CC1 10.1016/j.bmc.2009.06.041
CHEMBL573791 196332 0 None -9 4 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D4.4 expressed in CHO cellsBinding affinity to human cloned dopamine D4.4 expressed in CHO cells
ChEMBL 451 8 1 9 1.7 COc1ccccc1N1CCN(CCNC(=O)c2cn(-c3ccc([N+](=O)[O-])cc3)nn2)CC1 10.1016/j.bmc.2009.06.041
9843031 109576 0 None 56 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCCc2ccccc21 10.1016/s0960-894x(02)00655-8
CHEMBL323537 109576 0 None 56 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCCc2ccccc21 10.1016/s0960-894x(02)00655-8
44380815 58701 0 None 2 4 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
CHEMBL169193 58701 0 None 2 4 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
11299620 96835 2 None -87 6 Human 7.3 pKi = 7.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 247 5 1 2 3.4 CCCN(CCC)[C@H]1CCc2c(O)cccc2C1 10.1021/jm960345l
CHEMBL269004 96835 2 None -87 6 Human 7.3 pKi = 7.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 247 5 1 2 3.4 CCCN(CCC)[C@H]1CCc2c(O)cccc2C1 10.1021/jm960345l
127032086 138792 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 337 5 0 5 2.9 Cn1ncc2cc(CN3CCO[C@H](COc4ccccc4)C3)ccc21 10.1016/j.bmcl.2016.03.102
CHEMBL3792637 138792 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 337 5 0 5 2.9 Cn1ncc2cc(CN3CCO[C@H](COc4ccccc4)C3)ccc21 10.1016/j.bmcl.2016.03.102
127030606 138832 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 318 5 0 4 3.0 Clc1ccc(CN2CCO[C@H](COc3cccnc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793033 138832 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 318 5 0 4 3.0 Clc1ccc(CN2CCO[C@H](COc3cccnc3)C2)cc1 10.1016/j.bmcl.2016.03.102
90644226 111287 0 None -22 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 490 9 0 7 4.8 CCOC(=O)c1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287395 111287 0 None -22 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 490 9 0 7 4.8 CCOC(=O)c1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
122181328 121355 0 None -33 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 449 8 1 5 4.5 COc1ccccc1N1CCN(CCCCNC(=O)/N=N/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmc.2014.12.012
CHEMBL3590079 121355 0 None -33 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 449 8 1 5 4.5 COc1ccccc1N1CCN(CCCCNC(=O)/N=N/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmc.2014.12.012
135398737 944 89 None -13 91 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00108-5
38 944 89 None -13 91 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00108-5
722 944 89 None -13 91 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00108-5
CHEMBL42 944 89 None -13 91 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00108-5
DB00363 944 89 None -13 91 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00108-5
11033734 9629 1 None -120 6 Human 7.3 pKi = 7.3 Binding
The binding affinity at the Dopamine receptor D4 determined using [3H]YM-09151-2The binding affinity at the Dopamine receptor D4 determined using [3H]YM-09151-2
ChEMBL 294 1 0 3 3.1 COc1cccc2c1N1CCN(C)C[C@H]1c1ccccc1C2 10.1021/jm010566d
CHEMBL113238 9629 1 None -120 6 Human 7.3 pKi = 7.3 Binding
The binding affinity at the Dopamine receptor D4 determined using [3H]YM-09151-2The binding affinity at the Dopamine receptor D4 determined using [3H]YM-09151-2
ChEMBL 294 1 0 3 3.1 COc1cccc2c1N1CCN(C)C[C@H]1c1ccccc1C2 10.1021/jm010566d
164609529 183882 0 None -64 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 383 5 0 4 4.1 CC1(CCCN2CCN(c3ccccn3)CC2)Cc2cc(Cl)ccc2C1=O 10.1016/j.ejmech.2021.113243
CHEMBL4846823 183882 0 None -64 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 383 5 0 4 4.1 CC1(CCCN2CCN(c3ccccn3)CC2)Cc2cc(Cl)ccc2C1=O 10.1016/j.ejmech.2021.113243
76336022 105898 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 386 6 1 5 3.3 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3115581 105898 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 386 6 1 5 3.3 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139316 105898 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 386 6 1 5 3.3 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
11304676 102333 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Binding affinity for human dopamine receptor D4 using [125I]IABN as radioligandBinding affinity for human dopamine receptor D4 using [125I]IABN as radioligand
ChEMBL 418 6 1 4 3.3 COc1cc(Br)cc(C(=O)NCCN2CCc3ccccc3C2)c1OC 10.1016/j.bmcl.2003.09.083
CHEMBL305366 102333 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Binding affinity for human dopamine receptor D4 using [125I]IABN as radioligandBinding affinity for human dopamine receptor D4 using [125I]IABN as radioligand
ChEMBL 418 6 1 4 3.3 COc1cc(Br)cc(C(=O)NCCN2CCc3ccccc3C2)c1OC 10.1016/j.bmcl.2003.09.083
10587140 203325 1 None 1 3 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 255 3 1 2 3.1 Cc1cc(C2CCN(Cc3ccccc3)CC2)[nH]n1 10.1021/jm970111h
CHEMBL77015 203325 1 None 1 3 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 255 3 1 2 3.1 Cc1cc(C2CCN(Cc3ccccc3)CC2)[nH]n1 10.1021/jm970111h
137643132 157506 0 None -3890 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 503 7 1 7 3.8 CC(C)(C)c1nc(N2CCN(CCCCNC(=O)c3cc4ccccn4n3)CC2)cc(C(F)(F)F)n1 10.1016/j.bmc.2017.04.036
CHEMBL4085920 157506 0 None -3890 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 503 7 1 7 3.8 CC(C)(C)c1nc(N2CCN(CCCCNC(=O)c3cc4ccccn4n3)CC2)cc(C(F)(F)F)n1 10.1016/j.bmc.2017.04.036
164609172 183825 0 None -91 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 378 6 1 5 2.8 O=C1CCc2cc(C(=O)CCCN3CCN(c4ccccn4)CC3)ccc2N1 10.1016/j.ejmech.2021.113243
CHEMBL4845947 183825 0 None -91 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 378 6 1 5 2.8 O=C1CCc2cc(C(=O)CCCN3CCN(c4ccccn4)CC3)ccc2N1 10.1016/j.ejmech.2021.113243
10454026 17725 0 None -1479 9 Human 6.3 pKi = 6.3 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 406 8 2 4 3.5 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm900095y
CHEMBL125916 17725 0 None -1479 9 Human 6.3 pKi = 6.3 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 406 8 2 4 3.5 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm900095y
168275515 189911 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 371 5 0 4 4.1 Cc1nc(CN2CCC(OCc3ccc(F)c(F)c3)CC2)c2ccccn12 10.1016/j.bmcl.2022.128615
CHEMBL5179340 189911 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 371 5 0 4 4.1 Cc1nc(CN2CCC(OCc3ccc(F)c(F)c3)CC2)c2ccccn12 10.1016/j.bmcl.2022.128615
2726 906 64 None -8 72 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 906 64 None -8 72 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 906 64 None -8 72 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 906 64 None -8 72 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 906 64 None -8 72 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
9886340 5342 0 None 97 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 Cc1cccc2c1N(C(=O)CN1CCN(Cc3ccc(Cl)cc3)CC1)CC2 10.1016/s0960-894x(02)00655-8
CHEMBL107229 5342 0 None 97 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 Cc1cccc2c1N(C(=O)CN1CCN(Cc3ccc(Cl)cc3)CC1)CC2 10.1016/s0960-894x(02)00655-8
44380816 119845 0 None 22 4 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 402 6 1 3 3.7 COc1ccc(Br)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL353090 119845 0 None 22 4 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 402 6 1 3 3.7 COc1ccc(Br)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
6604756 98375 12 None -8 7 Human 7.3 pKi = 7.3 Binding
Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)
ChEMBL 275 6 0 2 4.2 CCCN(CCC)[C@@H]1CCc2c(OC)cccc2[C@@H]1C 10.1016/S0960-894X(01)80181-5
CHEMBL278751 98375 12 None -8 7 Human 7.3 pKi = 7.3 Binding
Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)
ChEMBL 275 6 0 2 4.2 CCCN(CCC)[C@@H]1CCc2c(OC)cccc2[C@@H]1C 10.1016/S0960-894X(01)80181-5
6604756 98375 12 None -8 7 Human 7.3 pKi = 7.3 Binding
Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone
ChEMBL 275 6 0 2 4.2 CCCN(CCC)[C@@H]1CCc2c(OC)cccc2[C@@H]1C 10.1021/jm00073a021
CHEMBL278751 98375 12 None -8 7 Human 7.3 pKi = 7.3 Binding
Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone
ChEMBL 275 6 0 2 4.2 CCCN(CCC)[C@@H]1CCc2c(OC)cccc2[C@@H]1C 10.1021/jm00073a021
164609529 183882 0 None -64 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 383 5 0 4 4.1 CC1(CCCN2CCN(c3ccccn3)CC2)Cc2cc(Cl)ccc2C1=O 10.1016/j.ejmech.2021.113243
CHEMBL4846823 183882 0 None -64 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 383 5 0 4 4.1 CC1(CCCN2CCN(c3ccccn3)CC2)Cc2cc(Cl)ccc2C1=O 10.1016/j.ejmech.2021.113243
57390116 68956 0 None -77 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 925 30 2 13 5.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(OCCOCCOCCOCCOc3cccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)c3)c2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928122 68956 0 None -77 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 925 30 2 13 5.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(OCCOCCOCCOCCOc3cccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)c3)c2)CC1 10.1016/j.bmc.2011.10.063
11732013 40568 0 None 12 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 395 1 1 5 4.8 Clc1ccc2c(c1)C(N1CCN(C3CCCCC3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL148559 40568 0 None 12 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 395 1 1 5 4.8 Clc1ccc2c(c1)C(N1CCN(C3CCCCC3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
6604756 98375 12 None -8 7 Human 7.3 pKi = 7.3 Binding
Tested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cellsTested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cells
ChEMBL 275 6 0 2 4.2 CCCN(CCC)[C@@H]1CCc2c(OC)cccc2[C@@H]1C 10.1016/S0960-894X(97)10068-3
CHEMBL278751 98375 12 None -8 7 Human 7.3 pKi = 7.3 Binding
Tested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cellsTested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cells
ChEMBL 275 6 0 2 4.2 CCCN(CCC)[C@@H]1CCc2c(OC)cccc2[C@@H]1C 10.1016/S0960-894X(97)10068-3
72190766 91928 0 None -12 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 391 8 0 6 3.6 COc1ccccc1N1CCN(CCCCn2cc(-c3ccccc3)nn2)CC1 10.1016/j.bmc.2015.01.017
CHEMBL2430443 91928 0 None -12 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 391 8 0 6 3.6 COc1ccccc1N1CCN(CCCCn2cc(-c3ccccc3)nn2)CC1 10.1016/j.bmc.2015.01.017
10831786 203812 0 None -2 3 Human 5.3 pKi = 5.3 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 351 4 1 2 5.5 Clc1ccc(-c2cc(C3CCCCN3Cc3ccccc3)[nH]n2)cc1 10.1021/jm970111h
CHEMBL80863 203812 0 None -2 3 Human 5.3 pKi = 5.3 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 351 4 1 2 5.5 Clc1ccc(-c2cc(C3CCCCN3Cc3ccccc3)[nH]n2)cc1 10.1021/jm970111h
156016177 177080 0 None -47 7 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-Methylspiperone from human dopamine D4 receptor expressed in stable HEK cells incubated for 90 mins by microbeta counting methodDisplacement of [3H]-N-Methylspiperone from human dopamine D4 receptor expressed in stable HEK cells incubated for 90 mins by microbeta counting method
ChEMBL 307 0 1 4 3.6 CN1CCc2cccc3c2C1Cc1ccc2nc(N)sc2c1-3 10.1016/j.bmc.2020.115578
CHEMBL4641502 177080 0 None -47 7 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-Methylspiperone from human dopamine D4 receptor expressed in stable HEK cells incubated for 90 mins by microbeta counting methodDisplacement of [3H]-N-Methylspiperone from human dopamine D4 receptor expressed in stable HEK cells incubated for 90 mins by microbeta counting method
ChEMBL 307 0 1 4 3.6 CN1CCc2cccc3c2C1Cc1ccc2nc(N)sc2c1-3 10.1016/j.bmc.2020.115578
16744005 143346 0 None -23 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 535 10 0 6 5.7 COc1ccc(C2=NO[C@@H](CCCN3CCN(C(c4ccc(F)cc4)c4ccc(F)cc4)CC3)C2)cc1OC 10.1016/j.ejmech.2006.12.030
CHEMBL390181 143346 0 None -23 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 535 10 0 6 5.7 COc1ccc(C2=NO[C@@H](CCCN3CCN(C(c4ccc(F)cc4)c4ccc(F)cc4)CC3)C2)cc1OC 10.1016/j.ejmech.2006.12.030
46231782 198819 0 None -2089 4 Human 5.3 pKi = 5.3 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 371 1 1 4 3.8 COC(=O)c1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.094
CHEMBL598730 198819 0 None -2089 4 Human 5.3 pKi = 5.3 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 371 1 1 4 3.8 COC(=O)c1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.094
44415704 79749 0 None -1659 6 Human 5.3 pKi = 5.3 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 474 2 2 6 4.4 Cc1cccc(N)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
CHEMBL213424 79749 0 None -1659 6 Human 5.3 pKi = 5.3 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 474 2 2 6 4.4 Cc1cccc(N)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
10242548 25400 34 None -3 3 Human 6.3 pKi = 6.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 219 4 1 2 2.6 CCCNC1CCc2c(cccc2OC)C1 10.1021/jm960345l
CHEMBL135152 25400 34 None -3 3 Human 6.3 pKi = 6.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 219 4 1 2 2.6 CCCNC1CCc2c(cccc2OC)C1 10.1021/jm960345l
118719792 115219 0 None -97 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 391 8 0 6 3.4 COc1ccccc1N1CCN(CCCCc2cn(-c3ccccc3)nn2)CC1 10.1016/j.bmc.2015.01.017
CHEMBL3353895 115219 0 None -97 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 391 8 0 6 3.4 COc1ccccc1N1CCN(CCCCc2cn(-c3ccccc3)nn2)CC1 10.1016/j.bmc.2015.01.017
21171 186393 27 None -8 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor after 1 hrDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor after 1 hr
ChEMBL 339 2 0 5 3.1 COc1ccc2c(c1OC)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmcl.2017.01.090
CHEMBL490533 186393 27 None -8 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor after 1 hrDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor after 1 hr
ChEMBL 339 2 0 5 3.1 COc1ccc2c(c1OC)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmcl.2017.01.090
56589561 70257 0 None -53 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 320 1 2 2 3.2 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2C[C@H]1CO 10.1021/jm200676f
CHEMBL1949729 70257 0 None -53 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 320 1 2 2 3.2 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2C[C@H]1CO 10.1021/jm200676f
13091358 70112 0 None -12 6 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 389 6 1 3 4.8 OC1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2CCCOc1ccc(F)cc1 10.1016/j.bmc.2012.01.022
CHEMBL1946122 70112 0 None -12 6 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 389 6 1 3 4.8 OC1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2CCCOc1ccc(F)cc1 10.1016/j.bmc.2012.01.022
9845181 206420 1 None -34 14 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 423 4 0 4 3.3 C[C@H](CN1CCN(c2cc(F)c(F)cc2F)CC1)N1C(=O)CC2(CCCC2)CC1=O 10.1021/jm020938y
CHEMBL98241 206420 1 None -34 14 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 423 4 0 4 3.3 C[C@H](CN1CCN(c2cc(F)c(F)cc2F)CC1)N1C(=O)CC2(CCCC2)CC1=O 10.1021/jm020938y
13091356 113039 0 None -12 8 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 389 6 1 3 4.8 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCOc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
CHEMBL3321789 113039 0 None -12 8 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 389 6 1 3 4.8 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCOc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
44276155 99032 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 437 8 1 5 3.5 COc1ccccc1N1CCN(CCCNC(=O)C2CCCc3cccc(OC)c32)CC1 10.1016/S0960-894X(97)00218-7
CHEMBL283211 99032 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 437 8 1 5 3.5 COc1ccccc1N1CCN(CCCNC(=O)C2CCCc3cccc(OC)c32)CC1 10.1016/S0960-894X(97)00218-7
72164180 91713 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 326 3 0 3 4.4 Clc1cccc(N2CCN(Cc3cccs3)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
CHEMBL2420772 91713 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 326 3 0 3 4.4 Clc1cccc(N2CCN(Cc3cccs3)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
118709165 112912 0 None -22 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 916 23 0 8 12.1 O=C(CCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318837 112912 0 None -22 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 916 23 0 8 12.1 O=C(CCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
118709167 112914 0 None -5 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 972 27 0 8 13.6 O=C(CCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318839 112914 0 None -5 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 972 27 0 8 13.6 O=C(CCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
25141534 55942 0 None -1698 7 Human 5.3 pKi = 5.3 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 460 7 3 4 3.8 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
CHEMBL1627305 55942 0 None -1698 7 Human 5.3 pKi = 5.3 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 460 7 3 4 3.8 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
146025727 171119 0 None -181 27 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4466483 171119 0 None -181 27 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
11016418 105642 0 None -7943 9 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 488 6 0 7 4.2 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCN4CCOC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL313424 105642 0 None -7943 9 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 488 6 0 7 4.2 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCN4CCOC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
137645196 157415 0 None -117 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 277 1 2 5 0.9 CN1CCCN(c2ccc(O)c3c2OCC(=O)N3)CC1 10.1016/j.bmc.2017.08.037
CHEMBL4084712 157415 0 None -117 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 277 1 2 5 0.9 CN1CCCN(c2ccc(O)c3c2OCC(=O)N3)CC1 10.1016/j.bmc.2017.08.037
49798855 14195 0 None -234 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 375 3 0 4 3.7 CN1CN(c2ccccc2)C2(CCN(Cc3coc4ccccc34)CC2)C1=O 10.1016/j.bmc.2010.05.052
CHEMBL1169896 14195 0 None -234 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 375 3 0 4 3.7 CN1CN(c2ccccc2)C2(CCN(Cc3coc4ccccc34)CC2)C1=O 10.1016/j.bmc.2010.05.052
CHEMBL1199933 14195 0 None -234 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 375 3 0 4 3.7 CN1CN(c2ccccc2)C2(CCN(Cc3coc4ccccc34)CC2)C1=O 10.1016/j.bmc.2010.05.052
10597114 171283 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 400 4 1 3 5.0 OC1(c2cccc(C(F)(F)F)c2)CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1021/jm00025a013
CHEMBL446892 171283 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 400 4 1 3 5.0 OC1(c2cccc(C(F)(F)F)c2)CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1021/jm00025a013
71061585 159950 0 None -3 2 Mouse 5.3 pKi = 5.3 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 367 6 0 5 2.8 Cc1ccnc(C)c1OC[C@H]1CN(CCN2CCc3ccccc32)CCO1 nan
CHEMBL4112090 159950 0 None -3 2 Mouse 5.3 pKi = 5.3 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 367 6 0 5 2.8 Cc1ccnc(C)c1OC[C@H]1CN(CCN2CCc3ccccc32)CCO1 nan
CHEMBL4752561 212279 0 None -3 2 Human 5.3 pKi = 5.3 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000739a DRD4Selectivity interaction (GPCR panel (PDSP screen)) EUB0000739a DRD4
ChEMBL None None None COc1cc(-c2cn([C@H]3CCc4ccccc4N(CC(F)(F)F)C3=O)nn2)ccc1-n1ccc(C)n1 nan
164619236 185127 0 None -25 7 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 366 6 1 5 2.6 O=C1CCc2cc(OCCCN3CCN(c4ccccn4)CC3)ccc2N1 10.1016/j.ejmech.2021.113243
CHEMBL4865591 185127 0 None -25 7 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 366 6 1 5 2.6 O=C1CCc2cc(OCCCN3CCN(c4ccccn4)CC3)ccc2N1 10.1016/j.ejmech.2021.113243
10551026 101146 0 None -6 6 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 438 5 1 3 4.6 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL298875 101146 0 None -6 6 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 438 5 1 3 4.6 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
9821803 126944 0 None 524 2 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 390 5 1 2 5.0 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL366043 126944 0 None 524 2 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 390 5 1 2 5.0 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2004.07.045
131396 205008 6 None 1 5 Human 8.3 pKi = 8.3 Binding
Binding affinity against human Dopamine receptor D4.2 in CHO cellsBinding affinity against human Dopamine receptor D4.2 in CHO cells
ChEMBL 435 6 0 5 4.6 CC1SC(C)(C)C(=O)N1CCCCN1CCN(c2csc3cc(F)ccc23)CC1 10.1021/jm960268u
CHEMBL89934 205008 6 None 1 5 Human 8.3 pKi = 8.3 Binding
Binding affinity against human Dopamine receptor D4.2 in CHO cellsBinding affinity against human Dopamine receptor D4.2 in CHO cells
ChEMBL 435 6 0 5 4.6 CC1SC(C)(C)C(=O)N1CCCCN1CCN(c2csc3cc(F)ccc23)CC1 10.1021/jm960268u
10641783 42434 0 None 354 2 Human 8.3 pKi = 8.3 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 353 4 1 5 2.3 COc1ccc(N2CCN(Cc3ccc4c(c3)OCC(=O)N4)CC2)cc1 10.1021/jm990277d
CHEMBL150129 42434 0 None 354 2 Human 8.3 pKi = 8.3 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 353 4 1 5 2.3 COc1ccc(N2CCN(Cc3ccc4c(c3)OCC(=O)N4)CC2)cc1 10.1021/jm990277d
9820304 101599 0 None 12 2 Human 8.3 pKi = 8.3 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(Cl)c1 10.1016/s0960-894x(00)00421-2
CHEMBL1204116 101599 0 None 12 2 Human 8.3 pKi = 8.3 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(Cl)c1 10.1016/s0960-894x(00)00421-2
CHEMBL302075 101599 0 None 12 2 Human 8.3 pKi = 8.3 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(Cl)c1 10.1016/s0960-894x(00)00421-2
1353 1880 85 None -3 85 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(02)00656-x
3559 1880 85 None -3 85 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(02)00656-x
86 1880 85 None -3 85 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(02)00656-x
CHEMBL54 1880 85 None -3 85 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(02)00656-x
DB00502 1880 85 None -3 85 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(02)00656-x
44336047 4717 0 None 57 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 367 4 0 3 2.9 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(F)cc2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL104058 4717 0 None 57 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 367 4 0 3 2.9 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(F)cc2)CC1 10.1016/s0960-894x(02)00656-x
44335925 4876 0 None 5 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 413 5 0 4 3.4 COc1ccc(Cl)cc1CN1CCN(CC(=O)N2c3ccccc3C[C@H]2C)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL104751 4876 0 None 5 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 413 5 0 4 3.4 COc1ccc(Cl)cc1CN1CCN(CC(=O)N2c3ccccc3C[C@H]2C)CC1 10.1016/s0960-894x(02)00656-x
44335835 5006 0 None 1174 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 417 4 0 3 3.8 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL105454 5006 0 None 1174 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 417 4 0 3 3.8 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/s0960-894x(02)00656-x
9867233 5427 0 None 234 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 427 5 0 5 2.6 COC(=O)[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL107631 5427 0 None 234 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 427 5 0 5 2.6 COC(=O)[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00656-x
9865490 167386 0 None 53 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 395 5 0 3 3.6 C=C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL431640 167386 0 None 53 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 395 5 0 3 3.6 C=C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00656-x
44335795 4932 0 None 33 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 362 4 0 2 4.6 Cc1cccc(CN2CCC(CC(=O)N3c4ccccc4CC3C)CC2)c1 10.1016/s0960-894x(02)00655-8
CHEMBL105011 4932 0 None 33 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 362 4 0 2 4.6 Cc1cccc(CN2CCC(CC(=O)N3c4ccccc4CC3C)CC2)c1 10.1016/s0960-894x(02)00655-8
44335816 5146 0 None 758 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 433 5 0 4 3.7 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(OC(F)(F)F)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL106208 5146 0 None 758 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 433 5 0 4 3.7 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(OC(F)(F)F)cc2)CC1 10.1016/s0960-894x(02)00655-8
10157556 119730 0 None 21 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 395 3 0 3 3.4 O=C1C(N2CCN(Cc3ccc(Cl)cc3)CC2)CCc2cccc3c2N1CC3 10.1016/s0960-894x(02)01056-9
CHEMBL352207 119730 0 None 21 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 395 3 0 3 3.4 O=C1C(N2CCN(Cc3ccc(Cl)cc3)CC2)CCc2cccc3c2N1CC3 10.1016/s0960-894x(02)01056-9
1353 1880 85 None -3 85 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cellsDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2011.04.098
3559 1880 85 None -3 85 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cellsDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2011.04.098
86 1880 85 None -3 85 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cellsDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2011.04.098
CHEMBL54 1880 85 None -3 85 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cellsDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2011.04.098
DB00502 1880 85 None -3 85 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cellsDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2011.04.098
11668034 133004 0 None 2 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 380 5 1 3 4.6 O=C(N[C@H]1CCN(Cc2ccc(F)cc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
CHEMBL370823 133004 0 None 2 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 380 5 1 3 4.6 O=C(N[C@H]1CCN(Cc2ccc(F)cc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
22100940 202256 4 None 112 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 306 3 0 3 4.6 C1=C(c2nc3ccccc3s2)CCN(Cc2ccccc2)C1 10.1016/S0960-894X(97)00402-2
CHEMBL69355 202256 4 None 112 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 306 3 0 3 4.6 C1=C(c2nc3ccccc3s2)CCN(Cc2ccccc2)C1 10.1016/S0960-894X(97)00402-2
19958507 98962 0 None 81 5 Rat 8.3 pKi = 8.3 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 320 4 1 3 3.4 CCc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
CHEMBL282829 98962 0 None 81 5 Rat 8.3 pKi = 8.3 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 320 4 1 3 3.4 CCc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
10715375 198019 0 None 630 2 Human 8.3 pKi = 8.3 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 389 6 0 4 4.9 COc1cc2ccccc2cc1C(=O)OCC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
CHEMBL59326 198019 0 None 630 2 Human 8.3 pKi = 8.3 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 389 6 0 4 4.9 COc1cc2ccccc2cc1C(=O)OCC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
10525119 79329 6 None 79 2 Human 8.3 pKi = 8.3 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 401 5 1 3 3.8 O=C(NCCN1CCN(c2ccc(Cl)cc2)CC1)C12CC3CC(CC(C3)C1)C2 10.1016/0960-894X(96)00198-9
CHEMBL21168 79329 6 None 79 2 Human 8.3 pKi = 8.3 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 401 5 1 3 3.8 O=C(NCCN1CCN(c2ccc(Cl)cc2)CC1)C12CC3CC(CC(C3)C1)C2 10.1016/0960-894X(96)00198-9
76325156 105909 1 None -7 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
CHEMBL3115585 105909 1 None -7 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
CHEMBL3139393 105909 1 None -7 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
10049549 82853 0 None 537 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 452 3 0 4 3.9 Clc1ccc(N2CCN(Cc3cnn4c(I)cccc34)CC2)cc1 10.1021/jm0611152
CHEMBL218787 82853 0 None 537 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 452 3 0 4 3.9 Clc1ccc(N2CCN(Cc3cnn4c(I)cccc34)CC2)cc1 10.1021/jm0611152
9968343 42494 0 None 169 3 Human 8.3 pKi = 8.3 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 351 3 1 4 3.0 Cc1ccc(N2CCN(Cc3ccc4c(c3)NC(=O)CO4)CC2)cc1C 10.1021/jm990277d
CHEMBL150181 42494 0 None 169 3 Human 8.3 pKi = 8.3 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 351 3 1 4 3.0 Cc1ccc(N2CCN(Cc3ccc4c(c3)NC(=O)CO4)CC2)cc1C 10.1021/jm990277d
155563452 174737 0 None 6 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 361 6 0 4 3.7 O=C(CCCN1CCN(c2ccc(Cl)cn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL4573441 174737 0 None 6 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 361 6 0 4 3.7 O=C(CCCN1CCN(c2ccc(Cl)cn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
145967572 164381 0 None 1 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 275 8 1 2 4.5 CCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4224763 164381 0 None 1 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 275 8 1 2 4.5 CCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
72545238 92695 0 None 25 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 425 9 0 7 3.3 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443005 92695 0 None 25 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 425 9 0 7 3.3 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
155563452 174737 0 None 6 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 361 6 0 4 3.7 O=C(CCCN1CCN(c2ccc(Cl)cn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL4573441 174737 0 None 6 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 361 6 0 4 3.7 O=C(CCCN1CCN(c2ccc(Cl)cn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
10643589 205735 0 None 13 3 Human 8.3 pKi = 8.3 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 381 4 1 4 5.1 Cc1c(-c2cccc(Cl)c2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL94283 205735 0 None 13 3 Human 8.3 pKi = 8.3 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 381 4 1 4 5.1 Cc1c(-c2cccc(Cl)c2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
3691783 4696 1 None 47 3 Human 8.3 pKi = 8.3 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 318 4 1 3 3.4 c1ccc(-c2nc(CN3CCN(c4ccccc4)CC3)c[nH]2)cc1 10.1021/jm960637m
CHEMBL103871 4696 1 None 47 3 Human 8.3 pKi = 8.3 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 318 4 1 3 3.4 c1ccc(-c2nc(CN3CCN(c4ccccc4)CC3)c[nH]2)cc1 10.1021/jm960637m
11797442 106543 0 None 6 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 441 7 2 4 4.1 COc1cc(NC(=O)C2CCC2)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
CHEMBL315446 106543 0 None 6 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 441 7 2 4 4.1 COc1cc(NC(=O)C2CCC2)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
127031832 138885 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 340 5 1 3 3.6 Fc1ccc2c(CN3CCO[C@H](COc4ccccc4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3793782 138885 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 340 5 1 3 3.6 Fc1ccc2c(CN3CCO[C@H](COc4ccccc4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
137651073 156926 0 None 2 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C#N)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4079301 156926 0 None 2 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C#N)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
10360923 91120 2 None 831 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 356 4 0 4 4.6 Cc1c(-c2ccccc2)cnn1C1CCN(Cc2cccc(C#N)c2)CC1 10.1016/s0960-894x(99)00169-9
CHEMBL24052 91120 2 None 831 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 356 4 0 4 4.6 Cc1c(-c2ccccc2)cnn1C1CCN(Cc2cccc(C#N)c2)CC1 10.1016/s0960-894x(99)00169-9
10737474 100883 0 None 10 3 Human 8.3 pKi = 8.3 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 363 4 1 3 3.5 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL296953 100883 0 None 10 3 Human 8.3 pKi = 8.3 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 363 4 1 3 3.5 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2005.02.012
9975465 187068 0 None 109 3 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL49502 187068 0 None 109 3 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.02.012
137661377 158663 0 None 173 8 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 314 6 0 2 3.9 CCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4098720 158663 0 None 173 8 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 314 6 0 2 3.9 CCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
44412191 137847 0 None 60 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 332 4 0 4 3.5 Cc1c(CN2CCN(c3ccccc3)CC2)cnn1-c1ccccc1 10.1021/jm0611152
CHEMBL377200 137847 0 None 60 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 332 4 0 4 3.5 Cc1c(CN2CCN(c3ccccc3)CC2)cnn1-c1ccccc1 10.1021/jm0611152
10737474 100883 0 None 10 3 Human 8.3 pKi = 8.3 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 363 4 1 3 3.5 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccc(Cl)cc1 10.1021/jm970021c
CHEMBL296953 100883 0 None 10 3 Human 8.3 pKi = 8.3 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 363 4 1 3 3.5 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccc(Cl)cc1 10.1021/jm970021c
13091268 77845 0 None -8 14 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL210578 77845 0 None -8 14 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
13091268 77845 0 None -8 14 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned dopamine D4.4 receptor by radioligand binding assayBinding affinity to human cloned dopamine D4.4 receptor by radioligand binding assay
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2006.03.057
CHEMBL210578 77845 0 None -8 14 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned dopamine D4.4 receptor by radioligand binding assayBinding affinity to human cloned dopamine D4.4 receptor by radioligand binding assay
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2006.03.057
13091268 77845 0 None -8 14 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.12.054
CHEMBL210578 77845 0 None -8 14 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.12.054
25071691 111295 0 None -9 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL3287403 111295 0 None -9 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
44412191 137847 0 None 60 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 332 4 0 4 3.5 Cc1c(CN2CCN(c3ccccc3)CC2)cnn1-c1ccccc1 10.1016/j.bmcl.2006.02.075
CHEMBL377200 137847 0 None 60 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 332 4 0 4 3.5 Cc1c(CN2CCN(c3ccccc3)CC2)cnn1-c1ccccc1 10.1016/j.bmcl.2006.02.075
71734031 90629 0 None -21 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 394 9 1 3 5.2 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm400520c
CHEMBL2397479 90629 0 None -21 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 394 9 1 3 5.2 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm400520c
10133031 57234 0 None 38 2 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 358 4 0 3 3.9 Fc1ccc(OC[C@@H]2CC[C@H]3CN(c4ccc(F)cc4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL166321 57234 0 None 38 2 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 358 4 0 3 3.9 Fc1ccc(OC[C@@H]2CC[C@H]3CN(c4ccc(F)cc4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
10518406 18690 0 None 69 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 301 10 1 4 3.1 COc1ccc(OCCNCCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL128276 18690 0 None 69 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 301 10 1 4 3.1 COc1ccc(OCCNCCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
10518406 18690 0 None 69 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 301 10 1 4 3.1 COc1ccc(OCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
CHEMBL128276 18690 0 None 69 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 301 10 1 4 3.1 COc1ccc(OCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
9952003 5288 0 None -1 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL106916 5288 0 None -1 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
10000302 205491 0 None 109 3 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 387 7 1 4 3.3 COc1cccc(C(=O)NCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm020952a
CHEMBL92713 205491 0 None 109 3 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 387 7 1 4 3.3 COc1cccc(C(=O)NCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm020952a
127031831 138810 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 352 6 1 4 3.5 COc1ccc2c(CN3CCO[C@H](COc4ccccc4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3792805 138810 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 352 6 1 4 3.5 COc1ccc2c(CN3CCO[C@H](COc4ccccc4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
11504230 77840 0 None -12 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 497 8 1 4 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm060138d
CHEMBL210567 77840 0 None -12 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 497 8 1 4 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm060138d
53364153 63510 0 None 3 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 929 25 0 16 7.7 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCc1cn(CCCCCCCCn2cc(COc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803023 63510 0 None 3 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 929 25 0 16 7.7 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCc1cn(CCCCCCCCn2cc(COc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
11233944 4715 0 None - 1 Human 8.3 pKi = 8.3 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 366 5 2 4 4.0 Oc1cc(Cl)ccc1NCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL104041 4715 0 None - 1 Human 8.3 pKi = 8.3 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 366 5 2 4 4.0 Oc1cc(Cl)ccc1NCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
10000302 205491 0 None 109 3 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 387 7 1 4 3.3 COc1cccc(C(=O)NCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
CHEMBL92713 205491 0 None 109 3 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 387 7 1 4 3.3 COc1cccc(C(=O)NCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
10760638 187593 0 None 131 3 Human 8.3 pKi = 8.3 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL49876 187593 0 None 131 3 Human 8.3 pKi = 8.3 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2005.02.012
57396571 69822 0 None 3 5 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 330 6 0 3 3.9 Clc1ccc(N2CCN(CCCOc3ccccc3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940413 69822 0 None 3 5 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 330 6 0 3 3.9 Clc1ccc(N2CCN(CCCOc3ccccc3)CC2)cc1 10.1016/j.bmc.2014.04.026
10618874 201456 0 None 95 2 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 365 5 1 2 5.2 Clc1ccc(-c2cc(C3CCN(CCc4ccccc4)CC3)[nH]n2)cc1 10.1021/jm970111h
CHEMBL6416 201456 0 None 95 2 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 365 5 1 2 5.2 Clc1ccc(-c2cc(C3CCN(CCc4ccccc4)CC3)[nH]n2)cc1 10.1021/jm970111h
10667201 110904 0 None 60 3 Human 8.3 pKi = 8.3 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 375 6 1 4 4.8 Cc1c(-c2ccccc2)nc(O)n1C1CCN(CCCc2ccccc2)CC1 10.1021/jm991029k
CHEMBL327176 110904 0 None 60 3 Human 8.3 pKi = 8.3 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 375 6 1 4 4.8 Cc1c(-c2ccccc2)nc(O)n1C1CCN(CCCc2ccccc2)CC1 10.1021/jm991029k
10546453 111211 0 None 27 3 Human 8.3 pKi = 8.3 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 360 4 2 3 4.0 O=C(Nc1nccc2ccccc12)NC1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL328667 111211 0 None 27 3 Human 8.3 pKi = 8.3 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 360 4 2 3 4.0 O=C(Nc1nccc2ccccc12)NC1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
10760638 187593 0 None 131 3 Human 8.3 pKi = 8.3 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1021/jm970021c
CHEMBL49876 187593 0 None 131 3 Human 8.3 pKi = 8.3 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1021/jm970021c
10618874 201456 0 None 95 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 365 5 1 2 5.2 Clc1ccc(-c2cc(C3CCN(CCc4ccccc4)CC3)[nH]n2)cc1 10.1021/jm0002432
CHEMBL6416 201456 0 None 95 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 365 5 1 2 5.2 Clc1ccc(-c2cc(C3CCN(CCc4ccccc4)CC3)[nH]n2)cc1 10.1021/jm0002432
168280742 190490 0 None -1 4 Human 8.3 pKi = 8.3 Binding
Competitive binding affinity to human D4R in transfected cellsCompetitive binding affinity to human D4R in transfected cells
ChEMBL 230 4 0 2 3.5 O=Cc1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
CHEMBL5187578 190490 0 None -1 4 Human 8.3 pKi = 8.3 Binding
Competitive binding affinity to human D4R in transfected cellsCompetitive binding affinity to human D4R in transfected cells
ChEMBL 230 4 0 2 3.5 O=Cc1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
145969667 164413 0 None -1 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 289 9 1 2 4.9 CCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4225278 164413 0 None -1 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 289 9 1 2 4.9 CCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
10618874 201456 0 None 95 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 365 5 1 2 5.2 Clc1ccc(-c2cc(C3CCN(CCc4ccccc4)CC3)[nH]n2)cc1 10.1021/jm960072u
CHEMBL6416 201456 0 None 95 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 365 5 1 2 5.2 Clc1ccc(-c2cc(C3CCN(CCc4ccccc4)CC3)[nH]n2)cc1 10.1021/jm960072u
11774177 5311 0 None - 1 Human 8.3 pKi = 8.3 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 407 6 0 4 4.9 CC(=O)c1ccc(Cl)cc1OCC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/jm031111m
CHEMBL107068 5311 0 None - 1 Human 8.3 pKi = 8.3 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 407 6 0 4 4.9 CC(=O)c1ccc(Cl)cc1OCC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/jm031111m
CHEMBL4513786 212217 5 None 34 8 Human 8.3 pKi = 8.3 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000289bCl DRD4Selectivity interaction (GPCR panel (PDSP screen)) EUB0000289bCl DRD4
ChEMBL None None None CCCCN(CCCC)C(=O)CN1C[C@@H](c2cc(OC)c3c(c2)OCO3)[C@H](C(=O)O)[C@H]1CC(C)(C)CCC nan
CHEMBL4796803 212217 5 None 34 8 Human 8.3 pKi = 8.3 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000289bCl DRD4Selectivity interaction (GPCR panel (PDSP screen)) EUB0000289bCl DRD4
ChEMBL None None None CCCCN(CCCC)C(=O)CN1C[C@@H](c2cc(OC)c3c(c2)OCO3)[C@H](C(=O)O)[C@H]1CC(C)(C)CCC nan
10693793 107215 0 None 10 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 427 7 2 4 3.7 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
CHEMBL319079 107215 0 None 10 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 427 7 2 4 3.7 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
10758004 21211 0 None 31 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 319 9 1 3 4.1 Cc1ccc(OCCCNCCOc2ccc(Cl)cc2)cc1 10.1021/jm970422s
CHEMBL131484 21211 0 None 31 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 319 9 1 3 4.1 Cc1ccc(OCCCNCCOc2ccc(Cl)cc2)cc1 10.1021/jm970422s
57396571 69822 0 None 3 5 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 330 6 0 3 3.9 Clc1ccc(N2CCN(CCCOc3ccccc3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940413 69822 0 None 3 5 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 330 6 0 3 3.9 Clc1ccc(N2CCN(CCCOc3ccccc3)CC2)cc1 10.1016/j.bmc.2014.04.026
57396571 69822 0 None 3 5 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 330 6 0 3 3.9 Clc1ccc(N2CCN(CCCOc3ccccc3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940413 69822 0 None 3 5 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 330 6 0 3 3.9 Clc1ccc(N2CCN(CCCOc3ccccc3)CC2)cc1 10.1016/j.bmc.2011.12.019
19964410 159151 1 None 70 3 Human 8.3 pKi = 8.3 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 322 5 1 3 3.4 c1ccc(OCC2CN(Cc3c[nH]c4ccccc34)CCO2)cc1 10.1021/acs.jmedchem.7b00151
CHEMBL4104272 159151 1 None 70 3 Human 8.3 pKi = 8.3 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 322 5 1 3 3.4 c1ccc(OCC2CN(Cc3c[nH]c4ccccc34)CCO2)cc1 10.1021/acs.jmedchem.7b00151
10758004 21211 0 None 31 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 319 9 1 3 4.1 Cc1ccc(OCCCNCCOc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL131484 21211 0 None 31 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 319 9 1 3 4.1 Cc1ccc(OCCCNCCOc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2005.02.012
6466372 169495 12 None 93 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 311 4 1 5 1.5 Cc1cccc(NC(=O)CN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4443054 169495 12 None 93 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 311 4 1 5 1.5 Cc1cccc(NC(=O)CN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
15467371 100538 0 None 912 4 Human 8.2 pKi = 8.2 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 351 4 1 4 3.4 N#CC(C#N)=Cc1cc(CN2CCN(c3ccc(Cl)cc3)CC2)c[nH]1 10.1016/s0960-894x(99)00302-9
CHEMBL294458 100538 0 None 912 4 Human 8.2 pKi = 8.2 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 351 4 1 4 3.4 N#CC(C#N)=Cc1cc(CN2CCN(c3ccc(Cl)cc3)CC2)c[nH]1 10.1016/s0960-894x(99)00302-9
45482152 196333 0 None 20 4 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned dopamine D4.4 expressed in CHO cellsBinding affinity to human cloned dopamine D4.4 expressed in CHO cells
ChEMBL 517 9 1 8 3.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cn(-c2ccc([N+](=O)[O-])cc2)nn1 10.1016/j.bmc.2009.06.041
CHEMBL573792 196333 0 None 20 4 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned dopamine D4.4 expressed in CHO cellsBinding affinity to human cloned dopamine D4.4 expressed in CHO cells
ChEMBL 517 9 1 8 3.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cn(-c2ccc([N+](=O)[O-])cc2)nn1 10.1016/j.bmc.2009.06.041
57401706 69828 0 None 1 11 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 331 6 0 4 3.5 Fc1ccc(SCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940419 69828 0 None 1 11 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 331 6 0 4 3.5 Fc1ccc(SCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
57401706 69828 0 None 1 11 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 331 6 0 4 3.5 Fc1ccc(SCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940419 69828 0 None 1 11 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 331 6 0 4 3.5 Fc1ccc(SCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
25071692 111297 0 None -13 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 443 7 0 6 4.5 N#Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL3287405 111297 0 None -13 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 443 7 0 6 4.5 N#Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
76325156 105909 1 None -7 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
CHEMBL3115585 105909 1 None -7 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
CHEMBL3139393 105909 1 None -7 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
44364166 40572 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 280 5 2 4 3.3 O=c1ccc2ccc(NCCNc3ccccc3)cc2o1 10.1021/jm0002432
CHEMBL148561 40572 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 280 5 2 4 3.3 O=c1ccc2ccc(NCCNc3ccccc3)cc2o1 10.1021/jm0002432
9926143 113027 1 None 74 4 Human 8.2 pKi = 8.2 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 294 6 2 4 3.0 O=c1ccc2ccc(CNCCNc3ccccc3)cc2o1 10.1021/jm990266k
CHEMBL332154 113027 1 None 74 4 Human 8.2 pKi = 8.2 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 294 6 2 4 3.0 O=c1ccc2ccc(CNCCNc3ccccc3)cc2o1 10.1021/jm990266k
127031515 138904 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL3793910 138904 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.bmcl.2022.128615
145969667 164413 0 None -1 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 289 9 1 2 4.9 CCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4225278 164413 0 None -1 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 289 9 1 2 4.9 CCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
52919 14317 43 None -3 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 529 15 0 4 8.1 CCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL1200986 14317 43 None -3 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 529 15 0 4 8.1 CCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
71733932 90621 0 None -25 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm400520c
CHEMBL2397389 90621 0 None -25 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm400520c
10378194 196088 0 None 45 6 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 265 3 1 2 2.3 C#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1 10.1016/s0960-894x(02)00316-5
CHEMBL57176 196088 0 None 45 6 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 265 3 1 2 2.3 C#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1 10.1016/s0960-894x(02)00316-5
155523515 170298 0 None 12 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 567 11 2 5 5.9 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(-c3ccccc3)cc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4454096 170298 0 None 12 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 567 11 2 5 5.9 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(-c3ccccc3)cc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
155555060 173753 0 None 14 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 521 11 2 6 4.3 COc1cccc(CN(NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)c2ccc(F)cc2)c1 10.1021/acs.jmedchem.9b01085
CHEMBL4550633 173753 0 None 14 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 521 11 2 6 4.3 COc1cccc(CN(NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)c2ccc(F)cc2)c1 10.1021/acs.jmedchem.9b01085
1353 1880 85 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.06.079
3559 1880 85 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.06.079
86 1880 85 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.06.079
CHEMBL54 1880 85 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.06.079
DB00502 1880 85 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.06.079
44278479 162592 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 359 7 0 2 5.6 c1ccc(CC2CCN(CCCOc3cccc4ccccc34)CC2)cc1 10.1016/S0960-894X(97)00233-3
CHEMBL417858 162592 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 359 7 0 2 5.6 c1ccc(CC2CCN(CCCOc3cccc4ccccc34)CC2)cc1 10.1016/S0960-894X(97)00233-3
135887934 11227 0 None 8 3 Human 7.3 pKi = 7.3 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 379 7 1 6 3.1 c1ccc(N2CCN(CCCCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL1179502 11227 0 None 8 3 Human 7.3 pKi = 7.3 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 379 7 1 6 3.1 c1ccc(N2CCN(CCCCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL80627 11227 0 None 8 3 Human 7.3 pKi = 7.3 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 379 7 1 6 3.1 c1ccc(N2CCN(CCCCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
10084583 104299 3 None -93 6 Human 7.3 pKi = 7.3 Binding
Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 50/2200)Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 50/2200)
ChEMBL 271 5 0 3 3.3 CCCN(CCC)[C@H]1CCc2nn3ccccc3c2C1 10.1016/s0960-894x(02)00390-6
CHEMBL310867 104299 3 None -93 6 Human 7.3 pKi = 7.3 Binding
Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 50/2200)Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 50/2200)
ChEMBL 271 5 0 3 3.3 CCCN(CCC)[C@H]1CCc2nn3ccccc3c2C1 10.1016/s0960-894x(02)00390-6
10639430 168603 1 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 320 4 1 5 2.2 c1ccc(-c2nc(CN3CCN(c4cnccn4)CC3)c[nH]2)cc1 10.1021/jm960637m
CHEMBL440511 168603 1 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 320 4 1 5 2.2 c1ccc(-c2nc(CN3CCN(c4cnccn4)CC3)c[nH]2)cc1 10.1021/jm960637m
135398745 2869 108 None -10 65 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmc.2008.06.030
47 2869 108 None -10 65 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmc.2008.06.030
CHEMBL715 2869 108 None -10 65 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmc.2008.06.030
DB00334 2869 108 None -10 65 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmc.2008.06.030
44454707 97382 0 None 21 5 Human 7.3 pKi = 7.3 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 348 6 0 3 4.0 FCCOc1ccc(CN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmcl.2007.12.026
CHEMBL272073 97382 0 None 21 5 Human 7.3 pKi = 7.3 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 348 6 0 3 4.0 FCCOc1ccc(CN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmcl.2007.12.026
44335987 4745 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 425 4 0 3 4.8 CC1CC(C)(C)N(C(=O)CN2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/s0960-894x(02)00655-8
CHEMBL104160 4745 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 425 4 0 3 4.8 CC1CC(C)(C)N(C(=O)CN2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/s0960-894x(02)00655-8
132578545 154021 0 None -104 9 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 325 3 0 2 4.1 O=C1c2ccc(Cl)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
CHEMBL3898250 154021 0 None -104 9 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 325 3 0 2 4.1 O=C1c2ccc(Cl)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
CHEMBL3991133 154021 0 None -104 9 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 325 3 0 2 4.1 O=C1c2ccc(Cl)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
135398745 2869 108 None -7 65 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2014.07.018
47 2869 108 None -7 65 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2014.07.018
CHEMBL715 2869 108 None -7 65 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2014.07.018
DB00334 2869 108 None -7 65 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2014.07.018
10663221 33491 1 None 60 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]cc(CN3CCN(c4ccccc4)CC3)c2c1 10.1021/jm0009989
CHEMBL142217 33491 1 None 60 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]cc(CN3CCN(c4ccccc4)CC3)c2c1 10.1021/jm0009989
22727323 13030 0 None -8 3 Human 7.3 pKi = 7.3 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 436 9 0 7 4.4 COc1ccccc1N1CCN(CCCCc2cc(-c3cccc([N+](=O)[O-])c3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL1190607 13030 0 None -8 3 Human 7.3 pKi = 7.3 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 436 9 0 7 4.4 COc1ccccc1N1CCN(CCCCc2cc(-c3cccc([N+](=O)[O-])c3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL541270 13030 0 None -8 3 Human 7.3 pKi = 7.3 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 436 9 0 7 4.4 COc1ccccc1N1CCN(CCCCc2cc(-c3cccc([N+](=O)[O-])c3)no2)CC1 10.1016/s0960-894x(02)00179-8
44270444 49059 0 None 138 4 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 340 3 0 4 3.6 Cc1cccn2ncc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1016/s0960-894x(01)00814-9
CHEMBL156369 49059 0 None 138 4 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 340 3 0 4 3.6 Cc1cccn2ncc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1016/s0960-894x(01)00814-9
44273882 77849 0 None 79 2 Human 7.3 pKi = 7.3 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 385 6 1 3 3.8 CC(C)(C)C(=O)NCCCCN1CCN(c2ccc(C(F)(F)F)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL21059 77849 0 None 79 2 Human 7.3 pKi = 7.3 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 385 6 1 3 3.8 CC(C)(C)C(=O)NCCCCN1CCN(c2ccc(C(F)(F)F)cc2)CC1 10.1016/0960-894X(96)00198-9
10939222 202697 1 None -100 5 Human 7.3 pKi = 7.3 Binding
Binding affinity towards Chinese hamster ovary cells transfected with human D4 receptor using [3H]spiperoneBinding affinity towards Chinese hamster ovary cells transfected with human D4 receptor using [3H]spiperone
ChEMBL 445 8 1 4 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(Br)cc2)CC1 10.1016/0960-894X(95)00011-H
CHEMBL71960 202697 1 None -100 5 Human 7.3 pKi = 7.3 Binding
Binding affinity towards Chinese hamster ovary cells transfected with human D4 receptor using [3H]spiperoneBinding affinity towards Chinese hamster ovary cells transfected with human D4 receptor using [3H]spiperone
ChEMBL 445 8 1 4 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(Br)cc2)CC1 10.1016/0960-894X(95)00011-H
132578545 154021 0 None -104 9 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 325 3 0 2 4.1 O=C1c2ccc(Cl)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
CHEMBL3898250 154021 0 None -104 9 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 325 3 0 2 4.1 O=C1c2ccc(Cl)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
CHEMBL3991133 154021 0 None -104 9 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 325 3 0 2 4.1 O=C1c2ccc(Cl)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
2865 4079 67 None -66 53 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm070516u
59 4079 67 None -66 53 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm070516u
60854 4079 67 None -66 53 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm070516u
CHEMBL708 4079 67 None -66 53 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm070516u
DB00246 4079 67 None -66 53 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm070516u
44340415 8492 0 None 1 4 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 460 5 1 3 5.3 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(C#Cc2ccccc2)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL109472 8492 0 None 1 4 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 460 5 1 3 5.3 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(C#Cc2ccccc2)c2ccccc12 10.1016/s0960-894x(03)00678-4
44340302 9660 0 None 1 4 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 466 7 1 3 5.3 COc1c(C(=O)NCC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL113471 9660 0 None 1 4 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 466 7 1 3 5.3 COc1c(C(=O)NCC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
44332686 206682 0 None -44 4 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 320 8 2 4 2.2 CS(=O)(=O)Nc1cccc(OCCNCc2ccccc2)c1 10.1016/s0960-894x(98)00014-6
CHEMBL99849 206682 0 None -44 4 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 320 8 2 4 2.2 CS(=O)(=O)Nc1cccc(OCCNCc2ccccc2)c1 10.1016/s0960-894x(98)00014-6
130431290 173463 0 None -436 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 417 9 2 4 3.5 CCc1c[nH]c(C(=O)NCCCCN2CCN(c3cccc(CC)c3Cl)CC2)n1 10.1021/acs.jmedchem.6b00860
CHEMBL4543524 173463 0 None -436 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 417 9 2 4 3.5 CCc1c[nH]c(C(=O)NCCCCN2CCN(c3cccc(CC)c3Cl)CC2)n1 10.1021/acs.jmedchem.6b00860
72545009 92692 0 None -1 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 437 6 3 10 -0.4 COc1ccccc1N1CCN(Cc2cn([C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3F)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443002 92692 0 None -1 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 437 6 3 10 -0.4 COc1ccccc1N1CCN(Cc2cn([C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3F)nn2)CC1 10.1016/j.bmcl.2013.09.026
11659604 138045 0 None 30 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 311 3 0 5 2.2 Fc1ccc(N2CCN(Cc3cn4ccncc4n3)CC2)cc1 10.1021/jm060166w
CHEMBL377542 138045 0 None 30 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 311 3 0 5 2.2 Fc1ccc(N2CCN(Cc3cn4ccncc4n3)CC2)cc1 10.1021/jm060166w
10034684 69064 63 None 18 2 Human 6.3 pKi = 6.3 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 135 0 2 2 1.4 Oc1ccc2c(c1)CCN2 10.1016/S0960-894X(97)00194-7
CHEMBL19331 69064 63 None 18 2 Human 6.3 pKi = 6.3 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 135 0 2 2 1.4 Oc1ccc2c(c1)CCN2 10.1016/S0960-894X(97)00194-7
155568411 175506 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 331 4 1 5 1.9 O=C(CN1CCN(c2ccc(Cl)cn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
CHEMBL4591118 175506 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 331 4 1 5 1.9 O=C(CN1CCN(c2ccc(Cl)cn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
137647533 157410 0 None -81 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 477 7 2 7 3.8 O=C1CCc2ccc(OCCCCN3CCCN(c4ccc(O)c5oc(=O)ccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4084690 157410 0 None -81 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 477 7 2 7 3.8 O=C1CCc2ccc(OCCCCN3CCCN(c4ccc(O)c5oc(=O)ccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
11154555 788 57 None -501 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
5037 788 57 None -501 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
7671 788 57 None -501 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL2028019 788 57 None -501 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL3085826 788 57 None -501 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
DB06016 788 57 None -501 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
164619236 185127 0 None -25 7 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 366 6 1 5 2.6 O=C1CCc2cc(OCCCN3CCN(c4ccccn4)CC3)ccc2N1 10.1016/j.ejmech.2021.113243
CHEMBL4865591 185127 0 None -25 7 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 366 6 1 5 2.6 O=C1CCc2cc(OCCCN3CCN(c4ccccn4)CC3)ccc2N1 10.1016/j.ejmech.2021.113243
154704705 175751 1 None -2 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 440 11 1 6 4.9 CCOc1ccc(F)cc1C1CC1CNCCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4590356 175751 1 None -2 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 440 11 1 6 4.9 CCOc1ccc(F)cc1C1CC1CNCCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4595409 175751 1 None -2 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 440 11 1 6 4.9 CCOc1ccc(F)cc1C1CC1CNCCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL5074399 212545 0 None -19 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCc1cccc(N2CCN(CCCCNCCC(C(=O)N(C)C)(c3ccccc3)c3ccccc3)CC2)c1Cl 10.1021/acs.jmedchem.1c00611
130431336 174336 0 None -389 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 401 7 2 4 3.0 CCc1cccc(N2CCN(C/C=C/CNC(=O)c3nc(C)c[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4564507 174336 0 None -389 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 401 7 2 4 3.0 CCc1cccc(N2CCN(C/C=C/CNC(=O)c3nc(C)c[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
71062579 147698 0 None - 1 Mouse 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 6 0 5 2.5 Cc1ccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)cn1 nan
CHEMBL3936182 147698 0 None - 1 Mouse 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 6 0 5 2.5 Cc1ccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)cn1 nan
44427970 152078 0 None -9 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 325 2 0 3 3.7 COc1cc2c(cc1OC)Cc1ccccc1CCCN(C)CC2 10.1021/jm070388+
CHEMBL397207 152078 0 None -9 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 325 2 0 3 3.7 COc1cc2c(cc1OC)Cc1ccccc1CCCN(C)CC2 10.1021/jm070388+
11269330 199808 0 None -16595 4 Human 5.3 pKi = 5.3 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 390 1 1 3 5.0 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4ccncc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL605127 199808 0 None -16595 4 Human 5.3 pKi = 5.3 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 390 1 1 3 5.0 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4ccncc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
44330637 206433 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 198 0 0 2 2.6 Cn1cc2c(n1)-c1ccccc1CCC2 10.1016/s0960-894x(03)00587-0
CHEMBL98330 206433 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 198 0 0 2 2.6 Cn1cc2c(n1)-c1ccccc1CCC2 10.1016/s0960-894x(03)00587-0
11154555 788 57 None -501 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
5037 788 57 None -501 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
7671 788 57 None -501 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL2028019 788 57 None -501 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL3085826 788 57 None -501 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
DB06016 788 57 None -501 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
16744171 92125 0 None -245 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 453 10 0 7 4.2 CCOc1ccccc1N1CCN(CCC[C@@H]2CC(c3ccc(OC)c(OC)c3)=NO2)CC1 10.1016/j.ejmech.2006.12.030
CHEMBL243224 92125 0 None -245 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 453 10 0 7 4.2 CCOc1ccccc1N1CCN(CCC[C@@H]2CC(c3ccc(OC)c(OC)c3)=NO2)CC1 10.1016/j.ejmech.2006.12.030
57345620 70150 0 None -32 3 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 454 7 1 5 5.8 O=C(CCCCN1[C@H]2CC[C@@H]1CC(O)(c1ccc(Cl)cc1)C2)c1nc2ccccc2s1 10.1016/j.bmc.2012.01.022
CHEMBL1946744 70150 0 None -32 3 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 454 7 1 5 5.8 O=C(CCCCN1[C@H]2CC[C@@H]1CC(O)(c1ccc(Cl)cc1)C2)c1nc2ccccc2s1 10.1016/j.bmc.2012.01.022
76518515 140339 0 None -31 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 454 7 1 5 5.8 O=C(CCCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL3818881 140339 0 None -31 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 454 7 1 5 5.8 O=C(CCCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL3819714 140339 0 None -31 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 454 7 1 5 5.8 O=C(CCCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
13373172 198101 0 None -125 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 251 0 1 2 3.0 Oc1ccc2c(c1)CCN1Cc3ccccc3CC21 10.1016/j.bmc.2009.08.028
CHEMBL593897 198101 0 None -125 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 251 0 1 2 3.0 Oc1ccc2c(c1)CCN1Cc3ccccc3CC21 10.1016/j.bmc.2009.08.028
44335721 106819 0 None 50 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 387 4 0 3 3.2 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccc(F)cc21 10.1016/s0960-894x(02)00655-8
CHEMBL317266 106819 0 None 50 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 387 4 0 3 3.2 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccc(F)cc21 10.1016/s0960-894x(02)00655-8
127030909 138951 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 367 6 0 4 3.9 FC(F)(F)Oc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3794375 138951 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 367 6 0 4 3.9 FC(F)(F)Oc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
57402787 68853 0 None -14 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 977 28 2 17 4.4 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccc(OCCOCCOCCOCCOc4ccn5ncc(C(=O)NCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1926700 68853 0 None -14 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 977 28 2 17 4.4 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccc(OCCOCCOCCOCCOc4ccn5ncc(C(=O)NCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
44276111 12801 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 450 10 0 7 4.8 CCOc1ccccc1N1CCN(CCCCc2cc(-c3cccc([N+](=O)[O-])c3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL1189040 12801 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 450 10 0 7 4.8 CCOc1ccccc1N1CCN(CCCCc2cc(-c3cccc([N+](=O)[O-])c3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL537975 12801 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 450 10 0 7 4.8 CCOc1ccccc1N1CCN(CCCCc2cc(-c3cccc([N+](=O)[O-])c3)no2)CC1 10.1016/s0960-894x(02)00179-8
10247720 12943 0 None 2 5 Human 7.3 pKi = 7.3 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinityIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinity
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL1190042 12943 0 None 2 5 Human 7.3 pKi = 7.3 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinityIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinity
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL540039 12943 0 None 2 5 Human 7.3 pKi = 7.3 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinityIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinity
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
60165543 74997 0 None 1 5 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 367 6 0 7 2.9 O=C(CCCN1CCN(c2ncccn2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL2037519 74997 0 None 1 5 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 367 6 0 7 2.9 O=C(CCCN1CCN(c2ncccn2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
9881815 204941 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 267 6 2 3 2.7 c1ccc(CNCCOc2cccc3[nH]cnc23)cc1 10.1016/s0960-894x(99)00434-5
CHEMBL89420 204941 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 267 6 2 3 2.7 c1ccc(CNCCOc2cccc3[nH]cnc23)cc1 10.1016/s0960-894x(99)00434-5
242 467 117 None -117 51 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2020.115943
34 467 117 None -117 51 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2020.115943
60795 467 117 None -117 51 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2020.115943
CHEMBL1112 467 117 None -117 51 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2020.115943
DB01238 467 117 None -117 51 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2020.115943
122180574 121212 0 None -512 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 468 7 1 5 5.2 Clc1cccc(N2CCN(CCCCc3cn(-c4ccc5[nH]ccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.01.017
CHEMBL3588919 121212 0 None -512 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 468 7 1 5 5.2 Clc1cccc(N2CCN(CCCCc3cn(-c4ccc5[nH]ccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.01.017
154725277 175858 1 None -19 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 2 5.8 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4472900 175858 1 None -19 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 2 5.8 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4596220 175858 1 None -19 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 2 5.8 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
242 467 117 None -117 51 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2021.113243
34 467 117 None -117 51 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2021.113243
60795 467 117 None -117 51 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2021.113243
CHEMBL1112 467 117 None -117 51 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2021.113243
DB01238 467 117 None -117 51 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2021.113243
242 467 117 None -87 51 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2016.05.053
34 467 117 None -87 51 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2016.05.053
60795 467 117 None -87 51 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2016.05.053
CHEMBL1112 467 117 None -87 51 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2016.05.053
DB01238 467 117 None -87 51 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2016.05.053
135501649 119261 0 None 5 2 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 321 1 2 5 3.2 Cc1ccc2c(c1)C(NC1CCN(C)CC1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL347959 119261 0 None 5 2 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 321 1 2 5 3.2 Cc1ccc2c(c1)C(NC1CCN(C)CC1)=Nc1cccnc1N2 10.1021/jm0104825
71449034 78014 0 None 3 4 Human 6.3 pKi = 6.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 441 7 1 5 4.5 COc1ccc(Br)cc1-c1nc(CNC2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL2111526 78014 0 None 3 4 Human 6.3 pKi = 6.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 441 7 1 5 4.5 COc1ccc(Br)cc1-c1nc(CNC2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
60165545 75005 0 None -2 4 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 336 6 0 4 4.7 O=C(CCCCN1Cc2ccccc2C1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL2037527 75005 0 None -2 4 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 336 6 0 4 4.7 O=C(CCCCN1Cc2ccccc2C1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
76518515 140339 0 None -31 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 454 7 1 5 5.8 O=C(CCCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL3818881 140339 0 None -31 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 454 7 1 5 5.8 O=C(CCCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL3819714 140339 0 None -31 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 454 7 1 5 5.8 O=C(CCCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
44456400 12725 0 None -21 10 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL1188501 12725 0 None -21 10 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL2436555 12725 0 None -21 10 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL536539 12725 0 None -21 10 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
44591088 188991 0 None -3 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 372 6 0 3 4.6 O=C(CCCN1CC2CC1N(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.12.054
CHEMBL514591 188991 0 None -3 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 372 6 0 3 4.6 O=C(CCCN1CC2CC1N(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.12.054
44438236 154361 2 None -173 3 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 354 3 1 3 4.3 Cn1cc(CN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2006.10.076
CHEMBL400827 154361 2 None -173 3 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 354 3 1 3 4.3 Cn1cc(CN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2006.10.076
100 3745 52 None -8 55 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
2637 3745 52 None -8 55 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
5452 3745 52 None -8 55 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
CHEMBL479 3745 52 None -8 55 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
DB00679 3745 52 None -8 55 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
10806501 203572 0 None 24 2 Human 7.3 pKi = 7.3 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 332 5 1 3 3.9 c1ccc(CCN2CCC(c3cc(-c4ccncc4)[nH]n3)CC2)cc1 10.1021/jm970111h
CHEMBL79098 203572 0 None 24 2 Human 7.3 pKi = 7.3 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 332 5 1 3 3.9 c1ccc(CCN2CCC(c3cc(-c4ccncc4)[nH]n3)CC2)cc1 10.1021/jm970111h
9857248 203394 6 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 292 3 1 3 2.9 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)cc1 10.1021/jm0305669
CHEMBL77708 203394 6 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 292 3 1 3 2.9 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)cc1 10.1021/jm0305669
44278458 99229 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 389 7 1 3 4.8 Cc1ccc(CC2CCN(CC(O)COc3cccc4ccccc34)CC2)cc1 10.1016/S0960-894X(97)00233-3
CHEMBL28458 99229 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 389 7 1 3 4.8 Cc1ccc(CC2CCN(CC(O)COc3cccc4ccccc34)CC2)cc1 10.1016/S0960-894X(97)00233-3
136072267 13062 0 None 1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 378 7 1 5 3.7 c1ccc(N2CCN(CCCCCNC3=Nc4ccccc4OC3)CC2)cc1 10.1016/S0960-894X(97)00442-3
CHEMBL1190896 13062 0 None 1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 378 7 1 5 3.7 c1ccc(N2CCN(CCCCCNC3=Nc4ccccc4OC3)CC2)cc1 10.1016/S0960-894X(97)00442-3
CHEMBL541826 13062 0 None 1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 378 7 1 5 3.7 c1ccc(N2CCN(CCCCCNC3=Nc4ccccc4OC3)CC2)cc1 10.1016/S0960-894X(97)00442-3
23992579 91712 5 None 8 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 292 3 0 3 3.7 Clc1ccccc1N1CCN(Cc2cccs2)CC1 10.1016/j.bmcl.2013.07.033
CHEMBL2420771 91712 5 None 8 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 292 3 0 3 3.7 Clc1ccccc1N1CCN(Cc2cccs2)CC1 10.1016/j.bmcl.2013.07.033
3251 4009 50 None -43 12 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
5684 4009 50 None -43 12 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
80 4009 50 None -43 12 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL31354 4009 50 None -43 12 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
44405445 135254 0 None 9 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 446 6 1 4 5.3 O=C(N[C@H]1CCN(Cc2ccc(OC(F)(F)F)cc2)C1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2005.08.051
CHEMBL373032 135254 0 None 9 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 446 6 1 4 5.3 O=C(N[C@H]1CCN(Cc2ccc(OC(F)(F)F)cc2)C1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2005.08.051
11280787 108729 0 None - 1 Human 7.3 pKi = 7.3 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 391 9 0 5 3.6 COCCOc1ccccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL321701 108729 0 None - 1 Human 7.3 pKi = 7.3 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 391 9 0 5 3.6 COCCOc1ccccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
12899569 66291 0 None -20 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 393 7 1 5 3.1 COc1ccccc1N1CCN(CCCOc2ccc3ccc(=O)[nH]c3c2)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1813597 66291 0 None -20 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 393 7 1 5 3.1 COc1ccccc1N1CCN(CCCOc2ccc3ccc(=O)[nH]c3c2)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1852735 66291 0 None -20 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 393 7 1 5 3.1 COc1ccccc1N1CCN(CCCOc2ccc3ccc(=O)[nH]c3c2)CC1 10.1016/j.bmc.2011.04.021
11375068 161309 0 None -588 3 Human 6.3 pKi = 6.3 Binding
Binding affinity for human dopamine D4 receptorBinding affinity for human dopamine D4 receptor
ChEMBL 480 7 1 4 5.2 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2cccnc2)cc1 10.1021/jm049465g
CHEMBL414838 161309 0 None -588 3 Human 6.3 pKi = 6.3 Binding
Binding affinity for human dopamine D4 receptorBinding affinity for human dopamine D4 receptor
ChEMBL 480 7 1 4 5.2 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2cccnc2)cc1 10.1021/jm049465g
44578446 180998 0 None -3 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 372 6 0 3 4.4 O=C(CCCN1CC2CC1CN2c1ccc(Cl)cc1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL476934 180998 0 None -3 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 372 6 0 3 4.4 O=C(CCCN1CC2CC1CN2c1ccc(Cl)cc1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
118709164 112911 0 None -87 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 902 22 0 8 11.7 O=C(CCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318836 112911 0 None -87 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 902 22 0 8 11.7 O=C(CCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
44335998 6387 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 385 5 0 4 2.9 O=C1COc2ccccc2N1CCN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL108261 6387 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 385 5 0 4 2.9 O=C1COc2ccccc2N1CCN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
71657945 89964 0 None -58 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 427 10 1 4 3.9 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(CCF)cc2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386608 89964 0 None -58 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 427 10 1 4 3.9 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(CCF)cc2)CC1 10.1016/j.bmc.2013.03.074
109030515 175412 1 None 12 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 325 5 1 5 1.9 Cc1cccc(NC(=O)CCN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4588808 175412 1 None 12 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 325 5 1 5 1.9 Cc1cccc(NC(=O)CCN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
10803828 11478 1 None -2630 5 Human 6.3 pKi = 6.3 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 295 2 1 3 3.1 Oc1ccc2c(c1)O[C@@H](CN1CCc3ccccc3C1)CC2 10.1021/jm9703653
CHEMBL1180609 11478 1 None -2630 5 Human 6.3 pKi = 6.3 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 295 2 1 3 3.1 Oc1ccc2c(c1)O[C@@H](CN1CCc3ccccc3C1)CC2 10.1021/jm9703653
CHEMBL135044 11478 1 None -2630 5 Human 6.3 pKi = 6.3 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 295 2 1 3 3.1 Oc1ccc2c(c1)O[C@@H](CN1CCc3ccccc3C1)CC2 10.1021/jm9703653
130431340 170779 0 None -851 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 403 8 2 4 3.3 CCc1cccc(N2CCN(CCCCNC(=O)c3nc(C)c[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4461461 170779 0 None -851 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 403 8 2 4 3.3 CCc1cccc(N2CCN(CCCCNC(=O)c3nc(C)c[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
130431342 169017 0 None -144 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 485 9 2 6 4.0 CCc1cc(Cl)c(OC)c(N2CCN(CC(O)CCNC(=O)c3cc4ccccc4o3)CC2)c1 10.1021/acs.jmedchem.6b00860
CHEMBL4436025 169017 0 None -144 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 485 9 2 6 4.0 CCc1cc(Cl)c(OC)c(N2CCN(CC(O)CCNC(=O)c3cc4ccccc4o3)CC2)c1 10.1021/acs.jmedchem.6b00860
12050200 101620 0 None 43 4 Human 7.3 pKi = 7.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 363 6 1 4 4.6 c1ccc(CN2CCC(NCc3csc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
CHEMBL302186 101620 0 None 43 4 Human 7.3 pKi = 7.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 363 6 1 4 4.6 c1ccc(CN2CCC(NCc3csc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
2 3210 19 None -2 28 Human 7.3 pKi = 7.3 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinityIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinity
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(01)00484-x
54562 3210 19 None -2 28 Human 7.3 pKi = 7.3 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinityIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinity
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(01)00484-x
CHEMBL240773 3210 19 None -2 28 Human 7.3 pKi = 7.3 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinityIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinity
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(01)00484-x
2 3210 19 None -2 28 Human 7.3 pKi = 7.3 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0503805
54562 3210 19 None -2 28 Human 7.3 pKi = 7.3 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0503805
CHEMBL240773 3210 19 None -2 28 Human 7.3 pKi = 7.3 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0503805
2 3210 19 None -2 28 Human 7.3 pKi = 7.3 Binding
Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsLow inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm049269+
54562 3210 19 None -2 28 Human 7.3 pKi = 7.3 Binding
Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsLow inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm049269+
CHEMBL240773 3210 19 None -2 28 Human 7.3 pKi = 7.3 Binding
Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsLow inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm049269+
11772242 165734 0 None 4 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 342 6 0 5 2.8 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL427048 165734 0 None 4 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 342 6 0 5 2.8 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
49799687 14276 0 None -14 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 432 3 2 2 4.3 OC1(c2ccc(I)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1173285 14276 0 None -14 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 432 3 2 2 4.3 OC1(c2ccc(I)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1200269 14276 0 None -14 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 432 3 2 2 4.3 OC1(c2ccc(I)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2010.05.052
135398737 944 89 None -13 91 Human 7.3 pKi = 7.3 Binding
Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar testCataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2003.07.015
38 944 89 None -13 91 Human 7.3 pKi = 7.3 Binding
Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar testCataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2003.07.015
722 944 89 None -13 91 Human 7.3 pKi = 7.3 Binding
Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar testCataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2003.07.015
CHEMBL42 944 89 None -13 91 Human 7.3 pKi = 7.3 Binding
Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar testCataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2003.07.015
DB00363 944 89 None -13 91 Human 7.3 pKi = 7.3 Binding
Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar testCataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2003.07.015
44340186 9569 0 None 8 4 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCCN(Cc2ccccc2)C1 10.1016/s0960-894x(03)00678-4
CHEMBL112831 9569 0 None 8 4 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCCN(Cc2ccccc2)C1 10.1016/s0960-894x(03)00678-4
11005852 202170 0 None -263 5 Human 6.3 pKi = 6.3 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 521 8 1 4 5.9 O=C(NCCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2=O 10.1021/jm010146o
CHEMBL68720 202170 0 None -263 5 Human 6.3 pKi = 6.3 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 521 8 1 4 5.9 O=C(NCCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2=O 10.1021/jm010146o
72191066 91925 0 None -199 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-spiperone from cloned human dopamine D4 receptorDisplacement of [3H]-spiperone from cloned human dopamine D4 receptor
ChEMBL 406 8 1 7 3.1 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc(N)cc3)nn2)CC1 10.1016/j.bmcl.2013.08.047
CHEMBL2430440 91925 0 None -199 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-spiperone from cloned human dopamine D4 receptorDisplacement of [3H]-spiperone from cloned human dopamine D4 receptor
ChEMBL 406 8 1 7 3.1 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc(N)cc3)nn2)CC1 10.1016/j.bmcl.2013.08.047
53248209 61662 1 None -3548 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 463 7 1 4 5.0 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm200288r
CHEMBL1774386 61662 1 None -3548 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 463 7 1 4 5.0 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm200288r
4189 205195 91 None -33 34 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 205195 91 None -33 34 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 205195 91 None -33 34 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
71061785 159949 0 None -1 4 Mouse 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 386 5 0 4 3.0 O=C(CN1CCO[C@@H](COc2cccc(Cl)c2)C1)N1CCc2ccccc21 nan
CHEMBL4112056 159949 0 None -1 4 Mouse 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 386 5 0 4 3.0 O=C(CN1CCO[C@@H](COc2cccc(Cl)c2)C1)N1CCc2ccccc21 nan
10039198 56055 0 None -4 4 Human 7.3 pKi = 7.3 Binding
Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4
ChEMBL 277 5 0 1 4.5 CCCN(CCC)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm991098z
CHEMBL163087 56055 0 None -4 4 Human 7.3 pKi = 7.3 Binding
Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4
ChEMBL 277 5 0 1 4.5 CCCN(CCC)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm991098z
135398737 944 89 None -13 91 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2008.06.030
38 944 89 None -13 91 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2008.06.030
722 944 89 None -13 91 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2008.06.030
CHEMBL42 944 89 None -13 91 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2008.06.030
DB00363 944 89 None -13 91 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2008.06.030
1240 8735 15 None -57 4 Human 7.3 pKi = 7.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 309 6 1 2 4.2 CCCN(CCc1ccccc1)C1CCc2c(O)cccc2C1 10.1021/jm960345l
CHEMBL109684 8735 15 None -57 4 Human 7.3 pKi = 7.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 309 6 1 2 4.2 CCCN(CCc1ccccc1)C1CCc2c(O)cccc2C1 10.1021/jm960345l
CHEMBL1256754 8735 15 None -57 4 Human 7.3 pKi = 7.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 309 6 1 2 4.2 CCCN(CCc1ccccc1)C1CCc2c(O)cccc2C1 10.1021/jm960345l
10403092 24928 4 None -26 3 Human 7.3 pKi = 7.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 309 6 1 2 4.2 CCCN(CCc1ccccc1)C1CCc2ccc(O)cc2C1 10.1021/jm960345l
CHEMBL134747 24928 4 None -26 3 Human 7.3 pKi = 7.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 309 6 1 2 4.2 CCCN(CCc1ccccc1)C1CCc2ccc(O)cc2C1 10.1021/jm960345l
145968810 164486 0 None -5 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 381 8 2 4 3.5 CN(C)c1ccc(C(=O)NCCCCN2CCC(c3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2018.03.084
CHEMBL4226226 164486 0 None -5 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 381 8 2 4 3.5 CN(C)c1ccc(C(=O)NCCCCN2CCC(c3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2018.03.084
44431478 87151 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 378 4 1 2 4.9 O=C(NC1CCN(Cc2cccc(Cl)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
CHEMBL233580 87151 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 378 4 1 2 4.9 O=C(NC1CCN(Cc2cccc(Cl)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
137657153 159010 0 None -4 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4102616 159010 0 None -4 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
135398737 944 89 None -13 91 Human 7.3 pKi = 7.3 Binding
In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss miceIn vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2003.07.015
38 944 89 None -13 91 Human 7.3 pKi = 7.3 Binding
In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss miceIn vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2003.07.015
722 944 89 None -13 91 Human 7.3 pKi = 7.3 Binding
In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss miceIn vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2003.07.015
CHEMBL42 944 89 None -13 91 Human 7.3 pKi = 7.3 Binding
In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss miceIn vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2003.07.015
DB00363 944 89 None -13 91 Human 7.3 pKi = 7.3 Binding
In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss miceIn vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2003.07.015
10425450 199 23 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
3301 199 23 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
CHEMBL375596 199 23 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
44393775 65972 0 None - 1 Human 7.3 pKi = 7.3 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 490 4 1 4 4.2 Cc1cc(NC(=O)CN2CCN(c3ccc(Br)cc3C#N)CC2)ccc1Br 10.1016/j.bmcl.2004.07.068
CHEMBL184853 65972 0 None - 1 Human 7.3 pKi = 7.3 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 490 4 1 4 4.2 Cc1cc(NC(=O)CN2CCN(c3ccc(Br)cc3C#N)CC2)ccc1Br 10.1016/j.bmcl.2004.07.068
57393634 68977 0 None -48 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 953 32 2 13 6.2 COc1cc(COCCOCCOCCOCCOCc2ccc(N3CCN(CCCCNC(=O)c4ccccc4)CC3)c(OC)c2)ccc1N1CCN(CCCCNC(=O)c2ccccc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928248 68977 0 None -48 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 953 32 2 13 6.2 COc1cc(COCCOCCOCCOCCOCc2ccc(N3CCN(CCCCNC(=O)c4ccccc4)CC3)c(OC)c2)ccc1N1CCN(CCCCNC(=O)c2ccccc2)CC1 10.1016/j.bmc.2011.10.063
127045854 139034 0 None -416 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 492 12 4 7 3.6 COc1cc(CCNC[C@@H](O)c2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3797205 139034 0 None -416 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 492 12 4 7 3.6 COc1cc(CCNC[C@@H](O)c2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
44337725 108051 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 319 2 0 2 4.3 CN1C2CCC1CC(OC1c3ccccc3Cc3ccccc31)C2 10.1021/jm010146o
CHEMBL320114 108051 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 319 2 0 2 4.3 CN1C2CCC1CC(OC1c3ccccc3Cc3ccccc31)C2 10.1021/jm010146o
22727334 12837 4 None -30 3 Human 6.3 pKi = 6.3 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 361 7 0 4 4.5 c1ccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)cc1 10.1016/s0960-894x(02)00179-8
CHEMBL1189290 12837 4 None -30 3 Human 6.3 pKi = 6.3 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 361 7 0 4 4.5 c1ccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)cc1 10.1016/s0960-894x(02)00179-8
CHEMBL538474 12837 4 None -30 3 Human 6.3 pKi = 6.3 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 361 7 0 4 4.5 c1ccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)cc1 10.1016/s0960-894x(02)00179-8
44455426 154610 0 None -7 12 Human 6.3 pKi = 6.3 Binding
Inhibition of human cloned dopamine D4 receptor by competitive binding experimentInhibition of human cloned dopamine D4 receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL402143 154610 0 None -7 12 Human 6.3 pKi = 6.3 Binding
Inhibition of human cloned dopamine D4 receptor by competitive binding experimentInhibition of human cloned dopamine D4 receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
10402378 65794 0 None -301 5 Human 6.3 pKi = 6.3 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 297 1 0 3 3.2 COc1ccc2c(c1)OCCN(C)CCc1ccccc1C2 10.1021/jm049720x
CHEMBL184049 65794 0 None -301 5 Human 6.3 pKi = 6.3 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 297 1 0 3 3.2 COc1ccc2c(c1)OCCN(C)CCc1ccccc1C2 10.1021/jm049720x
CHEMBL5080654 212926 0 None -8709 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCOC(=O)/C=C1\[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2CCc1ccccc1 10.1021/acs.jmedchem.1c00611
44336127 108793 0 None 4 2 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 411 5 0 3 4.1 CC(C)C1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL321871 108793 0 None 4 2 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 411 5 0 3 4.1 CC(C)C1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
71455083 81418 0 None -239 7 Human 7.3 pKi = 7.3 Binding
Binding affinity to dopamine D4 receptor by radioligand binding assayBinding affinity to dopamine D4 receptor by radioligand binding assay
ChEMBL 389 6 0 3 4.8 O=C(C1CCCCC1)N(CCN1CC=C(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL2164354 81418 0 None -239 7 Human 7.3 pKi = 7.3 Binding
Binding affinity to dopamine D4 receptor by radioligand binding assayBinding affinity to dopamine D4 receptor by radioligand binding assay
ChEMBL 389 6 0 3 4.8 O=C(C1CCCCC1)N(CCN1CC=C(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
10873318 45291 0 None -12 4 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 411 10 1 5 3.4 COc1cccc(C(=O)NCCCCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm020952a
CHEMBL152869 45291 0 None -12 4 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 411 10 1 5 3.4 COc1cccc(C(=O)NCCCCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm020952a
2407 3320 73 None -30 7 Human 7.3 pKi = 7.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1021/jm960345l
59227 3320 73 None -30 7 Human 7.3 pKi = 7.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1021/jm960345l
941 3320 73 None -30 7 Human 7.3 pKi = 7.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1021/jm960345l
CHEMBL1303 3320 73 None -30 7 Human 7.3 pKi = 7.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1021/jm960345l
DB05271 3320 73 None -30 7 Human 7.3 pKi = 7.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1021/jm960345l
127047859 139521 0 None -19 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 476 12 3 6 4.1 COc1cc(CCNCCc2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800341 139521 0 None -19 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 476 12 3 6 4.1 COc1cc(CCNCCc2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
137635685 155464 0 None -1 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 417 7 1 7 3.6 Oc1ccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c2cccnc12 10.1021/acs.jmedchem.7b00363
CHEMBL4061986 155464 0 None -1 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 417 7 1 7 3.6 Oc1ccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c2cccnc12 10.1021/acs.jmedchem.7b00363
44326256 167573 0 None -2 4 Human 7.3 pKi = 7.3 Binding
Tested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cellsTested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cells
ChEMBL 285 5 0 2 5.0 CCCN(CCC)[C@@H]1CCc2c(ccc3ccoc23)[C@@H]1C 10.1016/S0960-894X(97)10068-3
CHEMBL433002 167573 0 None -2 4 Human 7.3 pKi = 7.3 Binding
Tested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cellsTested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cells
ChEMBL 285 5 0 2 5.0 CCCN(CCC)[C@@H]1CCc2c(ccc3ccoc23)[C@@H]1C 10.1016/S0960-894X(97)10068-3
44393411 65762 0 None -123 5 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 587 7 1 4 6.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2s1 10.1016/j.bmcl.2004.05.052
CHEMBL183871 65762 0 None -123 5 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 587 7 1 4 6.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2s1 10.1016/j.bmcl.2004.05.052
71455082 81416 0 None -15 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 436 6 0 4 4.7 O=C(c1cccc2ccccc12)N(CCN1CCN(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL2164352 81416 0 None -15 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 436 6 0 4 4.7 O=C(c1cccc2ccccc12)N(CCN1CCN(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
11477180 3025 3 None -616 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm501512b
6675 3025 3 None -616 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm501512b
CHEMBL180010 3025 3 None -616 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm501512b
857428 31606 29 None 2 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in cell membranes incubated for 60 mins by scintillation counting methodDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 296 4 1 2 4.5 Cc1cccc2cc(CNCc3ccccc3)c(Cl)nc12 10.1021/acs.jmedchem.9b01560
CHEMBL1406529 31606 29 None 2 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in cell membranes incubated for 60 mins by scintillation counting methodDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 296 4 1 2 4.5 Cc1cccc2cc(CNCc3ccccc3)c(Cl)nc12 10.1021/acs.jmedchem.9b01560
107930 1500 20 None -3090 6 Human 5.3 pKi = 5.3 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.100
3304 1500 20 None -3090 6 Human 5.3 pKi = 5.3 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.100
CHEMBL298406 1500 20 None -3090 6 Human 5.3 pKi = 5.3 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.100
DB12273 1500 20 None -3090 6 Human 5.3 pKi = 5.3 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.100
130431316 170114 0 None -13803 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 454 8 3 4 3.7 CCc1cccc(N2CCN(CC(O)CCNC(=O)c3cc4ccccc4[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4451683 170114 0 None -13803 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 454 8 3 4 3.7 CCc1cccc(N2CCN(CC(O)CCNC(=O)c3cc4ccccc4[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
107930 1500 20 None -3090 6 Human 5.3 pKi = 5.3 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.094
3304 1500 20 None -3090 6 Human 5.3 pKi = 5.3 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.094
CHEMBL298406 1500 20 None -3090 6 Human 5.3 pKi = 5.3 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.094
DB12273 1500 20 None -3090 6 Human 5.3 pKi = 5.3 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.094
71062560 152894 0 None 1 2 Mouse 5.3 pKi = 5.3 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 352 5 0 4 2.4 O=C(CN1CCO[C@H](COc2ccccc2)C1)N1CCc2ccccc21 nan
CHEMBL3979116 152894 0 None 1 2 Mouse 5.3 pKi = 5.3 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 352 5 0 4 2.4 O=C(CN1CCO[C@H](COc2ccccc2)C1)N1CCc2ccccc21 nan
154703541 175725 1 None -23 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 464 11 1 3 6.1 CCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4541924 175725 1 None -23 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 464 11 1 3 6.1 CCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4595195 175725 1 None -23 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 464 11 1 3 6.1 CCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
1164 1600 25 None -346 11 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1021/acs.jmedchem.1c00611
1626 1600 25 None -346 11 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1021/acs.jmedchem.1c00611
3345 1600 25 None -346 11 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1021/acs.jmedchem.1c00611
CHEMBL596 1600 25 None -346 11 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1021/acs.jmedchem.1c00611
DB00813 1600 25 None -346 11 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1021/acs.jmedchem.1c00611
9842859 203744 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 380 6 0 7 2.4 CN(CCCCN1CCN(c2ncccn2)CC1)C1=Nc2ccccc2OC1 10.1016/S0960-894X(97)00442-3
CHEMBL80411 203744 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 380 6 0 7 2.4 CN(CCCCN1CCN(c2ncccn2)CC1)C1=Nc2ccccc2OC1 10.1016/S0960-894X(97)00442-3
1621 2396 16 None -64 44 Human 7.3 pKi = 7.3 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
17 2396 16 None -64 44 Human 7.3 pKi = 7.3 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
5761 2396 16 None -64 44 Human 7.3 pKi = 7.3 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
CHEMBL263881 2396 16 None -64 44 Human 7.3 pKi = 7.3 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
DB04829 2396 16 None -64 44 Human 7.3 pKi = 7.3 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
22065962 176222 0 None 20 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 294 3 1 5 1.7 c1cnc(N2CCN(Cc3c[nH]c4ncccc34)CC2)nc1 10.1016/j.bmc.2008.12.054
CHEMBL460644 176222 0 None 20 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 294 3 1 5 1.7 c1cnc(N2CCN(Cc3c[nH]c4ncccc34)CC2)nc1 10.1016/j.bmc.2008.12.054
132075278 162094 0 None 5 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human dopamine D4 expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 308 3 0 3 3.1 c1ccc(CN2CCc3cc(N4CCOCC4)ccc3C2)cc1 10.1016/j.ejmech.2018.02.024
CHEMBL4169752 162094 0 None 5 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human dopamine D4 expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 308 3 0 3 3.1 c1ccc(CN2CCc3cc(N4CCOCC4)ccc3C2)cc1 10.1016/j.ejmech.2018.02.024
11036641 31562 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 393 7 1 6 2.3 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm900690y
CHEMBL140612 31562 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 393 7 1 6 2.3 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm900690y
71462265 81417 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 438 6 0 6 3.5 O=C(c1cnc2ccccc2n1)N(CCN1CCN(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL2164353 81417 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 438 6 0 6 3.5 O=C(c1cnc2ccccc2n1)N(CCN1CCN(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
145989012 166752 0 None -95 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 384 8 2 5 3.0 COc1ccc(C(=O)NCCCCN2CCc3cc(OC)c(O)cc3C2)cc1 10.1021/acsmedchemlett.8b00229
CHEMBL4293886 166752 0 None -95 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 384 8 2 5 3.0 COc1ccc(C(=O)NCCCCN2CCc3cc(OC)c(O)cc3C2)cc1 10.1021/acsmedchemlett.8b00229
137654511 158257 0 None -1 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 259 1 2 4 1.0 CN1CCN(c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmc.2017.08.037
CHEMBL4094407 158257 0 None -1 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 259 1 2 4 1.0 CN1CCN(c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmc.2017.08.037
CHEMBL5075014 212583 0 None -5 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None O=C(NCCCCN1CC[C@]2(c3cccc(O)c3)CCC[C@H]1[C@@H]2O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.1c00611
76311271 105807 0 None -371 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 556 17 2 7 3.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(OCCOCCOCCF)ccc3[nH]2)CC1 10.1039/c3md00098b
CHEMBL3133862 105807 0 None -371 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 556 17 2 7 3.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(OCCOCCOCCF)ccc3[nH]2)CC1 10.1039/c3md00098b
CHEMBL3139046 105807 0 None -371 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 556 17 2 7 3.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(OCCOCCOCCF)ccc3[nH]2)CC1 10.1039/c3md00098b
11646648 93267 5 None -102 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 382 5 2 4 4.4 COc1ccc2[nH]cc(CN3CCC(O)(c4ccc(SC)cc4)CC3)c2c1 10.1016/j.bmcl.2006.10.076
CHEMBL247058 93267 5 None -102 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 382 5 2 4 4.4 COc1ccc2[nH]cc(CN3CCC(O)(c4ccc(SC)cc4)CC3)c2c1 10.1016/j.bmcl.2006.10.076
681 1437 65 None -2 38 Human 7.2 pKi = 7.2 Binding
Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
940 1437 65 None -2 38 Human 7.2 pKi = 7.2 Binding
Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
947 1437 65 None -2 38 Human 7.2 pKi = 7.2 Binding
Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
CHEMBL59 1437 65 None -2 38 Human 7.2 pKi = 7.2 Binding
Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
DB00988 1437 65 None -2 38 Human 7.2 pKi = 7.2 Binding
Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
763194 91711 6 None 33 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 276 3 0 3 3.2 Fc1ccccc1N1CCN(Cc2cccs2)CC1 10.1016/j.bmcl.2013.07.033
CHEMBL2420770 91711 6 None 33 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 276 3 0 3 3.2 Fc1ccccc1N1CCN(Cc2cccs2)CC1 10.1016/j.bmcl.2013.07.033
164609519 183869 0 None -47 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 441 7 1 5 4.1 COc1cc2c(cc1OC)CN(Cc1ccccc1CNC(=O)c1cccc(C#N)c1)CC2 10.1016/j.bmcl.2021.128047
CHEMBL4846574 183869 0 None -47 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 441 7 1 5 4.1 COc1cc2c(cc1OC)CN(Cc1ccccc1CNC(=O)c1cccc(C#N)c1)CC2 10.1016/j.bmcl.2021.128047
25071384 111289 0 None -14 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL3287397 111289 0 None -14 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
242 467 117 None -117 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm501512b
34 467 117 None -117 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm501512b
60795 467 117 None -117 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm501512b
CHEMBL1112 467 117 None -117 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm501512b
DB01238 467 117 None -117 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm501512b
242 467 117 None -117 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm0611152
34 467 117 None -117 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm0611152
60795 467 117 None -117 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm0611152
CHEMBL1112 467 117 None -117 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm0611152
DB01238 467 117 None -117 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm0611152
44419060 137332 0 None -13 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 432 8 1 6 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(C#N)ccc3o2)CC1 10.1021/jm0611152
CHEMBL376020 137332 0 None -13 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 432 8 1 6 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(C#N)ccc3o2)CC1 10.1021/jm0611152
10684789 9122 1 None -89 4 Human 6.2 pKi = 6.2 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 288 3 0 2 3.6 C(#Cc1ccncc1)CCN1CC=C(c2ccccc2)CC1 10.1021/jm950721m
CHEMBL110489 9122 1 None -89 4 Human 6.2 pKi = 6.2 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 288 3 0 2 3.6 C(#Cc1ccncc1)CCN1CC=C(c2ccccc2)CC1 10.1021/jm950721m
30438 196475 30 None 9 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 228 2 1 1 3.4 CC1CCN(Cc2c[nH]c3ccccc23)CC1 10.1021/jm9600712
CHEMBL57478 196475 30 None 9 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 228 2 1 1 3.4 CC1CCN(Cc2c[nH]c3ccccc23)CC1 10.1021/jm9600712
30438 196475 30 None 9 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 228 2 1 1 3.4 CC1CCN(Cc2c[nH]c3ccccc23)CC1 10.1021/jm0002432
CHEMBL57478 196475 30 None 9 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 228 2 1 1 3.4 CC1CCN(Cc2c[nH]c3ccccc23)CC1 10.1021/jm0002432
107995 96678 17 None -1380 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 404 5 2 4 2.2 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(I)c1O 10.1016/j.bmc.2007.07.017
29982233 96678 17 None -1380 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 404 5 2 4 2.2 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(I)c1O 10.1016/j.bmc.2007.07.017
CHEMBL267723 96678 17 None -1380 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 404 5 2 4 2.2 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(I)c1O 10.1016/j.bmc.2007.07.017
118709169 112917 0 None -3 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1029 31 0 8 15.2 O=C(CCCCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318841 112917 0 None -3 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1029 31 0 8 15.2 O=C(CCCCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
10917953 206249 0 None -16595 10 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 489 6 0 8 3.6 Cn1nnc(-c2ccc3c(c2)c(C2CCN(CCN4CCOC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL97242 206249 0 None -16595 10 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 489 6 0 8 3.6 Cn1nnc(-c2ccc3c(c2)c(C2CCN(CCN4CCOC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
134154069 153910 0 None -38 9 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 356 5 0 3 5.3 Clc1ccc2sc(CCCCN3CCc4ccccc4C3)nc2c1 10.1016/j.bmc.2016.09.019
CHEMBL3970299 153910 0 None -38 9 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 356 5 0 3 5.3 Clc1ccc2sc(CCCCN3CCc4ccccc4C3)nc2c1 10.1016/j.bmc.2016.09.019
CHEMBL3990113 153910 0 None -38 9 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 356 5 0 3 5.3 Clc1ccc2sc(CCCCN3CCc4ccccc4C3)nc2c1 10.1016/j.bmc.2016.09.019
9980998 30819 0 None -1148 8 Human 5.2 pKi = 5.2 Binding
Inhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in Sf9 cellsInhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in Sf9 cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
CHEMBL139926 30819 0 None -1148 8 Human 5.2 pKi = 5.2 Binding
Inhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in Sf9 cellsInhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in Sf9 cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
CHEMBL2112911 30819 0 None -1148 8 Human 5.2 pKi = 5.2 Binding
Inhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in Sf9 cellsInhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in Sf9 cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
44335948 167362 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 369 3 0 3 3.4 CC1Cc2ccccc2N1C(=O)CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL431437 167362 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 369 3 0 3 3.4 CC1Cc2ccccc2N1C(=O)CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
154726353 175749 1 None -50 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 467 12 2 3 5.9 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4577162 175749 1 None -50 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 467 12 2 3 5.9 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4595382 175749 1 None -50 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 467 12 2 3 5.9 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
154726792 176010 1 None -141 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4475406 176010 1 None -141 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4597530 176010 1 None -141 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
10684789 9122 1 None -89 4 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human dopamine receptor D4 was determinedBinding affinity towards human dopamine receptor D4 was determined
ChEMBL 288 3 0 2 3.6 C(#Cc1ccncc1)CCN1CC=C(c2ccccc2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL110489 9122 1 None -89 4 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human dopamine receptor D4 was determinedBinding affinity towards human dopamine receptor D4 was determined
ChEMBL 288 3 0 2 3.6 C(#Cc1ccncc1)CCN1CC=C(c2ccccc2)CC1 10.1016/j.bmcl.2005.02.012
134154069 153910 0 None -38 9 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 356 5 0 3 5.3 Clc1ccc2sc(CCCCN3CCc4ccccc4C3)nc2c1 10.1016/j.bmc.2016.09.019
CHEMBL3970299 153910 0 None -38 9 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 356 5 0 3 5.3 Clc1ccc2sc(CCCCN3CCc4ccccc4C3)nc2c1 10.1016/j.bmc.2016.09.019
CHEMBL3990113 153910 0 None -38 9 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 356 5 0 3 5.3 Clc1ccc2sc(CCCCN3CCc4ccccc4C3)nc2c1 10.1016/j.bmc.2016.09.019
164617626 184878 0 None -21 7 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 324 6 1 5 2.4 Nc1ccc(C(=O)CCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
CHEMBL4861794 184878 0 None -21 7 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 324 6 1 5 2.4 Nc1ccc(C(=O)CCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
164617626 184878 0 None -21 7 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 324 6 1 5 2.4 Nc1ccc(C(=O)CCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
CHEMBL4861794 184878 0 None -21 7 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 324 6 1 5 2.4 Nc1ccc(C(=O)CCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
53324045 56776 0 None -1 16 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
ChEMBL 487 7 1 2 7.3 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL1644980 56776 0 None -1 16 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
ChEMBL 487 7 1 2 7.3 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2018.10.036
22727332 13631 0 None -5 3 Human 7.2 pKi = 7.2 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 405 8 0 4 5.1 Fc1ccccc1N1CCN(CCCCc2cc(/C=C/c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL1195194 13631 0 None -5 3 Human 7.2 pKi = 7.2 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 405 8 0 4 5.1 Fc1ccccc1N1CCN(CCCCc2cc(/C=C/c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL554016 13631 0 None -5 3 Human 7.2 pKi = 7.2 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 405 8 0 4 5.1 Fc1ccccc1N1CCN(CCCCc2cc(/C=C/c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
11615489 69100 1 None -3 4 Human 7.2 pKi = 7.2 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 221 5 0 3 2.3 CCCN(CCC)[C@H]1CCn2nccc2C1 10.1021/jm0503805
CHEMBL193337 69100 1 None -3 4 Human 7.2 pKi = 7.2 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 221 5 0 3 2.3 CCCN(CCC)[C@H]1CCn2nccc2C1 10.1021/jm0503805
11356479 71493 0 None -8 3 Human 7.2 pKi = 7.2 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 221 5 0 3 2.3 CCCN(CCC)C1CCn2nccc2C1 10.1021/jm0503805
CHEMBL196928 71493 0 None -8 3 Human 7.2 pKi = 7.2 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 221 5 0 3 2.3 CCCN(CCC)C1CCn2nccc2C1 10.1021/jm0503805
168287735 191208 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
CHEMBL5198353 191208 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
135995891 201271 0 None 9 4 Human 6.2 pKi = 6.2 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 413 4 1 5 4.1 Oc1ccc(Br)cc1-c1nc(CN2CCN(c3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL62996 201271 0 None 9 4 Human 6.2 pKi = 6.2 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 413 4 1 5 4.1 Oc1ccc(Br)cc1-c1nc(CN2CCN(c3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
44456400 12725 0 None -21 10 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL1188501 12725 0 None -21 10 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL2436555 12725 0 None -21 10 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL536539 12725 0 None -21 10 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
16759249 9912 1 None -16 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 385 7 0 2 5.9 CCCCN1C2CCC1CC(OC(c1ccc(F)cc1)c1ccc(F)cc1)C2 10.1021/acs.jmedchem.6b01373
CHEMBL11493 9912 1 None -16 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 385 7 0 2 5.9 CCCCN1C2CCC1CC(OC(c1ccc(F)cc1)c1ccc(F)cc1)C2 10.1021/acs.jmedchem.6b01373
44591087 175177 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 366 3 1 3 4.5 Clc1ccc(N2CCC3CCC(C2)N3Cc2c[nH]c3ncccc23)cc1 10.1016/j.bmc.2008.12.054
CHEMBL458342 175177 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 366 3 1 3 4.5 Clc1ccc(N2CCC3CCC(C2)N3Cc2c[nH]c3ncccc23)cc1 10.1016/j.bmc.2008.12.054
11464115 68292 0 None -30 3 Rat 6.2 pKi = 6.2 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 413 6 1 3 4.5 O=C(NCCCCN1CCN2c3ccccc3CC[C@@H]2C1)c1ccc2ccccc2c1 10.1021/jm049031l
CHEMBL191815 68292 0 None -30 3 Rat 6.2 pKi = 6.2 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 413 6 1 3 4.5 O=C(NCCCCN1CCN2c3ccccc3CC[C@@H]2C1)c1ccc2ccccc2c1 10.1021/jm049031l
122180576 121214 0 None -107 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 479 8 0 6 5.1 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc4c(c3)Cc3ccccc3-4)nn2)CC1 10.1016/j.bmc.2015.01.017
CHEMBL3588921 121214 0 None -107 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 479 8 0 6 5.1 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc4c(c3)Cc3ccccc3-4)nn2)CC1 10.1016/j.bmc.2015.01.017
46231925 199693 0 None -3235 4 Human 5.2 pKi = 5.2 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 384 3 1 4 4.4 CCO/N=C/c1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.094
CHEMBL604525 199693 0 None -3235 4 Human 5.2 pKi = 5.2 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 384 3 1 4 4.4 CCO/N=C/c1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.094
121304441 151852 0 None -11481 5 Human 5.2 pKi = 5.2 Binding
Activity at dopamine D4 receptor (unknown origin)Activity at dopamine D4 receptor (unknown origin)
ChEMBL 515 8 1 6 5.0 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1cccc(C(N)=O)c1 10.1021/acs.jmedchem.6b00972
CHEMBL3970323 151852 0 None -11481 5 Human 5.2 pKi = 5.2 Binding
Activity at dopamine D4 receptor (unknown origin)Activity at dopamine D4 receptor (unknown origin)
ChEMBL 515 8 1 6 5.0 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1cccc(C(N)=O)c1 10.1021/acs.jmedchem.6b00972
CHEMBL5090215 213475 0 None -389 4 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CN(C)C(=O)C(CCNCCCCN1CCc2ccc(C#N)cc2C1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
44339984 167234 0 None 10 4 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL430522 167234 0 None 10 4 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
44370009 49707 0 None 10 3 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 263 2 1 2 3.1 c1c[nH]c2nc(CN3CCc4ccccc4C3)cc-2c1 10.1016/s0960-894x(99)00025-6
CHEMBL156896 49707 0 None 10 3 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 263 2 1 2 3.1 c1c[nH]c2nc(CN3CCc4ccccc4C3)cc-2c1 10.1016/s0960-894x(99)00025-6
3428803 100024 3 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 370 8 1 5 3.3 O=[N+]([O-])c1ccc(OCC(O)CN2CCC(Cc3ccccc3)CC2)cc1 10.1016/S0960-894X(97)00233-3
CHEMBL29098 100024 3 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 370 8 1 5 3.3 O=[N+]([O-])c1ccc(OCC(O)CN2CCC(Cc3ccccc3)CC2)cc1 10.1016/S0960-894X(97)00233-3
44307552 101871 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 357 5 0 3 3.1 CN(C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1)c1ccccc1 10.1016/s0960-894x(00)00421-2
CHEMBL303692 101871 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 357 5 0 3 3.1 CN(C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1)c1ccccc1 10.1016/s0960-894x(00)00421-2
44336085 5108 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 415 4 0 4 4.0 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCCSc2ccccc21 10.1016/s0960-894x(02)00655-8
CHEMBL106007 5108 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 415 4 0 4 4.0 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCCSc2ccccc21 10.1016/s0960-894x(02)00655-8
9840797 15365 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 338 3 0 4 3.3 O=c1ccc2ccc(CN3CCN(c4ccc(F)cc4)CC3)cc2o1 10.1021/jm990266k
CHEMBL121884 15365 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 338 3 0 4 3.3 O=c1ccc2ccc(CN3CCN(c4ccc(F)cc4)CC3)cc2o1 10.1021/jm990266k
127027237 138856 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 314 6 0 5 2.4 COc1ccc(CN2CCO[C@H](COc3cccnc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793264 138856 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 314 6 0 5 2.4 COc1ccc(CN2CCO[C@H](COc3cccnc3)C2)cc1 10.1016/j.bmcl.2016.03.102
137657951 159017 0 None -1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 263 1 2 5 0.5 CN1CCN(c2ccc(O)c3c2OCC(=O)N3)CC1 10.1016/j.bmc.2017.08.037
CHEMBL4102646 159017 0 None -1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 263 1 2 5 0.5 CN1CCN(c2ccc(O)c3c2OCC(=O)N3)CC1 10.1016/j.bmc.2017.08.037
73353534 90627 0 None -13 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 549 18 1 7 5.4 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cnn(CCCC)n3)c(OC)c2)CC1 10.1021/jm400520c
CHEMBL2397477 90627 0 None -13 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 549 18 1 7 5.4 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cnn(CCCC)n3)c(OC)c2)CC1 10.1021/jm400520c
52937776 60842 0 None -83 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 430 10 1 4 4.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCn2nccc2C1 10.1021/jm101639t
CHEMBL1765629 60842 0 None -83 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 430 10 1 4 4.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCn2nccc2C1 10.1021/jm101639t
44307552 101871 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 357 5 0 3 3.1 CN(C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1)c1ccccc1 10.1021/acs.jmedchem.7b00151
CHEMBL303692 101871 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 357 5 0 3 3.1 CN(C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1)c1ccccc1 10.1021/acs.jmedchem.7b00151
42606573 17664 0 None 20 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptorDisplacement of [3H]Spiperone from human dopamine D4.4 receptor
ChEMBL 381 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3coc4ccccc34)CC2)nc1 10.1021/jm100835q
CHEMBL1258999 17664 0 None 20 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptorDisplacement of [3H]Spiperone from human dopamine D4.4 receptor
ChEMBL 381 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3coc4ccccc34)CC2)nc1 10.1021/jm100835q
12050196 201428 5 None 8 4 Human 6.2 pKi = 6.2 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 349 5 0 4 4.1 c1ccc(CN2CCN(Cc3csc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
CHEMBL64043 201428 5 None 8 4 Human 6.2 pKi = 6.2 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 349 5 0 4 4.1 c1ccc(CN2CCN(Cc3csc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
12050193 201506 0 None -1 4 Human 6.2 pKi = 6.2 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 443 5 0 5 4.9 COc1ccc(Br)cc1-c1nc(CN2CCN(c3ccccc3)CC2)cs1 10.1016/s0960-894x(00)00405-4
CHEMBL64325 201506 0 None -1 4 Human 6.2 pKi = 6.2 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 443 5 0 5 4.9 COc1ccc(Br)cc1-c1nc(CN2CCN(c3ccccc3)CC2)cs1 10.1016/s0960-894x(00)00405-4
46231846 199654 0 None -2344 4 Human 5.2 pKi = 5.2 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 341 1 1 3 3.8 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(C=O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL604316 199654 0 None -2344 4 Human 5.2 pKi = 5.2 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 341 1 1 3 3.8 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(C=O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
10735463 161328 0 None 239 3 Human 8.2 pKi = 8.2 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 334 4 1 5 2.5 Cc1[nH]c(-c2ccccc2)nc1CN1CCN(c2ncccn2)CC1 10.1021/jm960637m
CHEMBL415014 161328 0 None 239 3 Human 8.2 pKi = 8.2 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 334 4 1 5 2.5 Cc1[nH]c(-c2ccccc2)nc1CN1CCN(c2ncccn2)CC1 10.1021/jm960637m
44335877 4791 0 None 426 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 419 4 0 3 3.7 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2cc(F)c(Cl)cc2F)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL104323 4791 0 None 426 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 419 4 0 3 3.7 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2cc(F)c(Cl)cc2F)CC1 10.1016/s0960-894x(02)00656-x
44336027 5037 0 None 165 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 367 4 0 3 2.9 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2cccc(F)c2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL105601 5037 0 None 165 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 367 4 0 3 2.9 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2cccc(F)c2)CC1 10.1016/s0960-894x(02)00656-x
44335960 6450 0 None 31 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 383 4 0 3 3.4 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL108282 6450 0 None 31 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 383 4 0 3 3.4 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00656-x
44336108 5608 0 None 85 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 5 0 3 3.8 CCC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL107793 5608 0 None 85 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 5 0 3 3.8 CCC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
44335923 108706 0 None 125 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 377 5 0 3 3.3 CCc1ccc(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
CHEMBL321538 108706 0 None 125 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 377 5 0 3 3.3 CCc1ccc(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
44335884 162825 0 None 11 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 366 4 0 2 4.4 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccc(F)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL419356 162825 0 None 11 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 366 4 0 2 4.4 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccc(F)cc2)CC1 10.1016/s0960-894x(02)00655-8
44335799 162902 0 None 102 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 433 5 0 4 3.7 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2cccc(OC(F)(F)F)c2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL419908 162902 0 None 102 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 433 5 0 4 3.7 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2cccc(OC(F)(F)F)c2)CC1 10.1016/s0960-894x(02)00655-8
1353 1880 85 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm100899z
3559 1880 85 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm100899z
86 1880 85 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm100899z
CHEMBL54 1880 85 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm100899z
DB00502 1880 85 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm100899z
25071691 111295 0 None -9 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL3287403 111295 0 None -9 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL4547253 212243 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysis
ChEMBL None None None Fc1ccc(CN2CCC(n3cc(Cc4ccc(Br)cc4)nn3)CC2)cc1 10.1016/j.bmc.2022.116851
CHEMBL4567314 212262 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysis
ChEMBL None None None Brc1ccc(Cc2cn(C3CCN(Cc4ccccc4)CC3)nn2)cc1 10.1016/j.bmc.2022.116851
71459761 83666 0 None 14 7 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 540 7 0 5 6.1 COc1ccccc1N1CCN(Cc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207642 83666 0 None 14 7 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 540 7 0 5 6.1 COc1ccccc1N1CCN(Cc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
10570563 17846 0 None 15 2 Human 8.2 pKi = 8.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1Cl 10.1021/acs.jmedchem.7b00151
CHEMBL1202212 17846 0 None 15 2 Human 8.2 pKi = 8.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1Cl 10.1021/acs.jmedchem.7b00151
CHEMBL126429 17846 0 None 15 2 Human 8.2 pKi = 8.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1Cl 10.1021/acs.jmedchem.7b00151
1353 1880 85 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0611152
3559 1880 85 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0611152
86 1880 85 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0611152
CHEMBL54 1880 85 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0611152
DB00502 1880 85 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0611152
9836900 41458 1 None 1 3 Human 8.2 pKi = 8.2 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 323 3 1 4 2.3 O=C1COc2cc(CN3CCN(c4ccccc4)CC3)ccc2N1 10.1021/jm990277d
CHEMBL149233 41458 1 None 1 3 Human 8.2 pKi = 8.2 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 323 3 1 4 2.3 O=C1COc2cc(CN3CCN(c4ccccc4)CC3)ccc2N1 10.1021/jm990277d
44336012 108727 0 None 120 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 383 4 0 3 3.4 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2cccc(Cl)c2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL321698 108727 0 None 120 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 383 4 0 3 3.4 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2cccc(Cl)c2)CC1 10.1016/s0960-894x(02)00656-x
90644058 111537 0 None 104 4 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 372 4 0 3 4.0 O=C1c2ccc(F)cc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
CHEMBL3289642 111537 0 None 104 4 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 372 4 0 3 4.0 O=C1c2ccc(F)cc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
54585811 61281 0 None -4 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 418 7 0 5 3.2 COc1ccccc1N1CCN(CCCCN2CCc3cc(C#N)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771113 61281 0 None -4 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 418 7 0 5 3.2 COc1ccccc1N1CCN(CCCCN2CCc3cc(C#N)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
90644058 111537 0 None 104 4 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 372 4 0 3 4.0 O=C1c2ccc(F)cc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
CHEMBL3289642 111537 0 None 104 4 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 372 4 0 3 4.0 O=C1c2ccc(F)cc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
2389 3279 114 None -21 67 Human 8.2 pKi = 8.2 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
5073 3279 114 None -21 67 Human 8.2 pKi = 8.2 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
96 3279 114 None -21 67 Human 8.2 pKi = 8.2 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
CHEMBL85 3279 114 None -21 67 Human 8.2 pKi = 8.2 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
DB00734 3279 114 None -21 67 Human 8.2 pKi = 8.2 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
72164302 91729 0 None 19 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 359 3 1 2 4.8 Clc1cccc(N2CCN(Cc3c[nH]c4ccccc34)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
CHEMBL2420895 91729 0 None 19 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 359 3 1 2 4.8 Clc1cccc(N2CCN(Cc3c[nH]c4ccccc34)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
155562328 175270 0 None 7 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 521 11 2 6 4.3 COc1ccc(N(Cc2cccc(F)c2)NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1021/acs.jmedchem.9b01085
CHEMBL4585384 175270 0 None 7 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 521 11 2 6 4.3 COc1ccc(N(Cc2cccc(F)c2)NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1021/acs.jmedchem.9b01085
57393083 69824 0 None 1 7 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 314 6 0 4 2.8 Fc1ccc(CCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940415 69824 0 None 1 7 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 314 6 0 4 2.8 Fc1ccc(CCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
57393083 69824 0 None 1 7 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 314 6 0 4 2.8 Fc1ccc(CCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940415 69824 0 None 1 7 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 314 6 0 4 2.8 Fc1ccc(CCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
681 1437 65 None -2 38 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm800895v
940 1437 65 None -2 38 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm800895v
947 1437 65 None -2 38 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm800895v
CHEMBL59 1437 65 None -2 38 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm800895v
DB00988 1437 65 None -2 38 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm800895v
19964401 156105 0 None 208 3 Human 8.2 pKi = 8.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 320 5 1 2 4.0 c1ccc(CCC2CN(Cc3c[nH]c4ccccc34)CCO2)cc1 10.1021/acs.jmedchem.7b00151
CHEMBL4069306 156105 0 None 208 3 Human 8.2 pKi = 8.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 320 5 1 2 4.0 c1ccc(CCC2CN(Cc3c[nH]c4ccccc34)CCO2)cc1 10.1021/acs.jmedchem.7b00151
11849778 80730 0 None 35 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 360 6 0 5 2.9 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cc(F)cc(F)c1 10.1021/jm060279f
CHEMBL215705 80730 0 None 35 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 360 6 0 5 2.9 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cc(F)cc(F)c1 10.1021/jm060279f
1353 1880 85 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2004859
3559 1880 85 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2004859
86 1880 85 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2004859
CHEMBL54 1880 85 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2004859
DB00502 1880 85 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2004859
1353 1880 85 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2009919
3559 1880 85 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2009919
86 1880 85 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2009919
CHEMBL54 1880 85 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2009919
DB00502 1880 85 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2009919
9817253 106073 0 None -6 4 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 283 6 3 4 2.4 Oc1nc2c(OCCNCc3ccccc3)cccc2[nH]1 10.1016/s0960-894x(99)00434-5
CHEMBL314174 106073 0 None -6 4 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 283 6 3 4 2.4 Oc1nc2c(OCCNCc3ccccc3)cccc2[nH]1 10.1016/s0960-894x(99)00434-5
10249755 167621 0 None 1258 2 Human 8.2 pKi = 8.2 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 389 6 0 4 5.1 COc1cc2ccccc2cc1OC(=O)CC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
CHEMBL433255 167621 0 None 1258 2 Human 8.2 pKi = 8.2 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 389 6 0 4 5.1 COc1cc2ccccc2cc1OC(=O)CC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
15443 117307 91 None 1 9 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL340211 117307 91 None 1 9 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
15443 117307 91 None 1 9 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.ejmech.2021.113243
CHEMBL340211 117307 91 None 1 9 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.ejmech.2021.113243
1353 1880 85 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm070516u
3559 1880 85 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm070516u
86 1880 85 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm070516u
CHEMBL54 1880 85 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm070516u
DB00502 1880 85 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm070516u
11336814 79691 0 None 7 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 342 6 0 5 2.8 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(F)c1 10.1021/jm060279f
CHEMBL213164 79691 0 None 7 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 342 6 0 5 2.8 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(F)c1 10.1021/jm060279f
11200205 138382 0 None 9 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 392 6 0 5 4.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm060279f
CHEMBL378324 138382 0 None 9 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 392 6 0 5 4.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm060279f
53363200 63522 0 None 2 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 509 14 0 9 3.7 CCOCCn1cc(CCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
CHEMBL1803052 63522 0 None 2 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 509 14 0 9 3.7 CCOCCn1cc(CCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
16121920 194202 0 None 426 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 380 5 1 6 2.7 COc1ccccc1N1CCN(Cc2c(C)[nH]c3nc(N(C)C)ncc23)CC1 10.1016/j.bmc.2009.05.015
CHEMBL558838 194202 0 None 426 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 380 5 1 6 2.7 COc1ccccc1N1CCN(Cc2c(C)[nH]c3nc(N(C)C)ncc23)CC1 10.1016/j.bmc.2009.05.015
45267435 194317 0 None 426 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 3 1 3 3.5 Clc1nccc2c(CN3CCN(c4ccccc4)CC3)c[nH]c12 10.1016/j.bmc.2009.05.015
CHEMBL559868 194317 0 None 426 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 3 1 3 3.5 Clc1nccc2c(CN3CCN(c4ccccc4)CC3)c[nH]c12 10.1016/j.bmc.2009.05.015
10088259 101443 3 None 134 3 Human 8.2 pKi = 8.2 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 334 4 1 4 2.4 Cc1ccc(C(=O)NCN2CCN(c3ccccc3C#N)CC2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL300956 101443 3 None 134 3 Human 8.2 pKi = 8.2 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 334 4 1 4 2.4 Cc1ccc(C(=O)NCN2CCN(c3ccccc3C#N)CC2)cc1 10.1016/j.bmcl.2005.02.012
71458040 78477 0 None 27 3 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 329 5 1 2 4.5 C1=C(/C=C/c2ccccc2)CCN(CCc2c[nH]c3ncccc23)C1 10.1016/s0960-894x(99)00025-6
CHEMBL2112913 78477 0 None 27 3 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 329 5 1 2 4.5 C1=C(/C=C/c2ccccc2)CCN(CCc2c[nH]c3ncccc23)C1 10.1016/s0960-894x(99)00025-6
10088259 101443 3 None 134 3 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 334 4 1 4 2.4 Cc1ccc(C(=O)NCN2CCN(c3ccccc3C#N)CC2)cc1 10.1021/jm970021c
CHEMBL300956 101443 3 None 134 3 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 334 4 1 4 2.4 Cc1ccc(C(=O)NCN2CCN(c3ccccc3C#N)CC2)cc1 10.1021/jm970021c
155561496 175099 0 None -5 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-N-methylspiperone from dopamine D4 receptor (unknown origin) expressed in HEK293 cell membranesDisplacement of [3H]-N-methylspiperone from dopamine D4 receptor (unknown origin) expressed in HEK293 cell membranes
ChEMBL 438 8 0 6 3.1 COc1cc2c(cc1OC)C(=O)N(CCCCN1CCN(c3ccccn3)CC1)CCC2 10.1021/acs.jmedchem.8b00760
CHEMBL4581645 175099 0 None -5 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-N-methylspiperone from dopamine D4 receptor (unknown origin) expressed in HEK293 cell membranesDisplacement of [3H]-N-methylspiperone from dopamine D4 receptor (unknown origin) expressed in HEK293 cell membranes
ChEMBL 438 8 0 6 3.1 COc1cc2c(cc1OC)C(=O)N(CCCCN1CCN(c3ccccn3)CC1)CCC2 10.1021/acs.jmedchem.8b00760
10065083 31887 1 None -1 10 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 328 6 0 5 2.4 O=C(CCCN1CCN(c2ncccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2011.12.019
CHEMBL140872 31887 1 None -1 10 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 328 6 0 5 2.4 O=C(CCCN1CCN(c2ncccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2011.12.019
137638973 156332 0 None -15 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccc2c(/C=N/O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4071868 156332 0 None -15 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccc2c(/C=N/O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
10065083 31887 1 None 1 10 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 328 6 0 5 2.4 O=C(CCCN1CCN(c2ncccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL140872 31887 1 None 1 10 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 328 6 0 5 2.4 O=C(CCCN1CCN(c2ncccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
11653679 180609 1 None 3 11 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 374 6 0 3 4.7 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL476108 180609 1 None 3 11 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 374 6 0 3 4.7 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
168273039 192194 0 None 1659 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 394 6 0 5 3.1 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc([N+](=O)[O-])cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5175009 192194 0 None 1659 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 394 6 0 5 3.1 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc([N+](=O)[O-])cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5221414 192194 0 None 1659 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 394 6 0 5 3.1 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc([N+](=O)[O-])cc2)CC1 10.1021/acs.jmedchem.2c00840
10498196 41738 0 None 63 3 Human 8.2 pKi = 8.2 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 352 4 1 4 3.4 COc1ccc(C2CCN(Cc3ccc4c(c3)OCC(=O)N4)CC2)cc1 10.1021/jm990277d
CHEMBL149497 41738 0 None 63 3 Human 8.2 pKi = 8.2 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 352 4 1 4 3.4 COc1ccc(C2CCN(Cc3ccc4c(c3)OCC(=O)N4)CC2)cc1 10.1021/jm990277d
10382581 100828 0 None 151 3 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2cccc(C)c2)CC1 10.1021/jm970021c
CHEMBL296506 100828 0 None 151 3 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2cccc(C)c2)CC1 10.1021/jm970021c
15443 117307 91 None 1 9 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL340211 117307 91 None 1 9 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
15443 117307 91 None 1 9 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.ejmech.2021.113243
CHEMBL340211 117307 91 None 1 9 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.ejmech.2021.113243
44278114 99742 0 None 104 4 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 334 5 1 3 3.8 CCCc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
CHEMBL28833 99742 0 None 104 4 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 334 5 1 3 3.8 CCCc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
10382581 100828 0 None 151 3 Human 8.2 pKi = 8.2 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2cccc(C)c2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL296506 100828 0 None 151 3 Human 8.2 pKi = 8.2 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2cccc(C)c2)CC1 10.1016/j.bmcl.2005.02.012
133079 3581 33 None 1 4 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 10.1021/jm0002432
980 3581 33 None 1 4 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 10.1021/jm0002432
CHEMBL69759 3581 33 None 1 4 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 10.1021/jm0002432
11465618 101926 18 None -25 19 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
CHEMBL3039528 101926 18 None -25 19 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
CHEMBL5191141 101926 18 None -25 19 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
53364225 63514 0 None -2 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 932 25 0 18 5.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCc1cn(CCOCCOCCn2cc(COc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803027 63514 0 None -2 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 932 25 0 18 5.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCc1cn(CCOCCOCCn2cc(COc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
10336538 1595 44 None -3 8 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm900690y
974 1595 44 None -3 8 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm900690y
CHEMBL310843 1595 44 None -3 8 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm900690y
155562395 175375 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 323 4 1 3 3.5 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)nc1 10.1021/acs.jmedchem.9b00231
CHEMBL4587925 175375 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 323 4 1 3 3.5 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)nc1 10.1021/acs.jmedchem.9b00231
9946469 43872 0 None 11 3 Human 8.2 pKi = 8.2 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 351 3 1 4 3.0 Cc1ccc(N2CCN(Cc3ccc4c(c3)OCC(=O)N4)CC2)cc1C 10.1021/jm990277d
CHEMBL151533 43872 0 None 11 3 Human 8.2 pKi = 8.2 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 351 3 1 4 3.0 Cc1ccc(N2CCN(Cc3ccc4c(c3)OCC(=O)N4)CC2)cc1C 10.1021/jm990277d
9907332 16219 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 368 3 0 4 4.1 Cc1ccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)cc1Cl 10.1021/jm990266k
CHEMBL123031 16219 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 368 3 0 4 4.1 Cc1ccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)cc1Cl 10.1021/jm990266k
57391307 69820 0 None 8 7 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 348 6 0 3 4.1 Fc1ccc(OCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940411 69820 0 None 8 7 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 348 6 0 3 4.1 Fc1ccc(OCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
57391307 69820 0 None 8 7 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 348 6 0 3 4.1 Fc1ccc(OCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940411 69820 0 None 8 7 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 348 6 0 3 4.1 Fc1ccc(OCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2011.12.019
168277064 192236 0 None 1202 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 379 6 0 4 3.2 COc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5178868 192236 0 None 1202 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 379 6 0 4 3.2 COc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5221670 192236 0 None 1202 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 379 6 0 4 3.2 COc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
10786367 203465 0 None 9 3 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 385 4 1 2 5.8 Clc1ccc(-c2cc(C3CCN(Cc4cccc(Cl)c4)CC3)[nH]n2)cc1 10.1021/jm970111h
CHEMBL78287 203465 0 None 9 3 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 385 4 1 2 5.8 Clc1ccc(-c2cc(C3CCN(Cc4cccc(Cl)c4)CC3)[nH]n2)cc1 10.1021/jm970111h
10018480 13718 0 None -1 3 Human 7.2 pKi = 7.2 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 313 3 0 1 5.0 C=CCN1CC=C(C2=Cc3ccccc3Cc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL1195797 13718 0 None -1 3 Human 7.2 pKi = 7.2 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 313 3 0 1 5.0 C=CCN1CC=C(C2=Cc3ccccc3Cc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL555362 13718 0 None -1 3 Human 7.2 pKi = 7.2 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 313 3 0 1 5.0 C=CCN1CC=C(C2=Cc3ccccc3Cc3ccccc32)CC1 10.1021/jm00004a016
135398737 944 89 None -13 91 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2012.08.011
38 944 89 None -13 91 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2012.08.011
722 944 89 None -13 91 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2012.08.011
CHEMBL42 944 89 None -13 91 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2012.08.011
DB00363 944 89 None -13 91 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2012.08.011
135398737 944 89 None -13 91 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.05.027
38 944 89 None -13 91 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.05.027
722 944 89 None -13 91 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.05.027
CHEMBL42 944 89 None -13 91 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.05.027
DB00363 944 89 None -13 91 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.05.027
137636066 155692 0 None -38 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 480 7 3 7 3.0 O=C1CCc2ccc(OCCCCN3CCCN(c4ccc(O)c5c4OCC(=O)N5)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4064742 155692 0 None -38 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 480 7 3 7 3.0 O=C1CCc2ccc(OCCCCN3CCCN(c4ccc(O)c5c4OCC(=O)N5)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
71733932 90621 0 None -25 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm501889t
CHEMBL2397389 90621 0 None -25 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm501889t
13457126 99362 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 392 6 1 4 3.9 O=C(CCN1CCN(c2ccc(CO)c(Cl)c2)CC1)c1ccc(Cl)cc1 10.1016/s0960-894x(98)00252-2
CHEMBL285543 99362 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 392 6 1 4 3.9 O=C(CCN1CCN(c2ccc(CO)c(Cl)c2)CC1)c1ccc(Cl)cc1 10.1016/s0960-894x(98)00252-2
69432471 109358 0 None -60 5 Human 7.2 pKi = 7.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 378 5 0 3 4.4 O=C(CCCN1CC[C@H]2[C@@H](C1)c1cccc3c1N2CCC3)c1ccc(F)cc1 10.1021/jm401958n
CHEMBL3233427 109358 0 None -60 5 Human 7.2 pKi = 7.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 378 5 0 3 4.4 O=C(CCCN1CC[C@H]2[C@@H](C1)c1cccc3c1N2CCC3)c1ccc(F)cc1 10.1021/jm401958n
17755867 85682 1 None -28 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 281 0 1 2 3.4 CN1CCCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm070388+
CHEMBL231070 85682 1 None -28 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 281 0 1 2 3.4 CN1CCCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm070388+
46912547 14277 0 None -67 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 462 4 2 3 4.3 COc1cccc2[nH]cc(CN3CCC(O)(c4ccc(I)cc4)CC3)c12 10.1016/j.bmc.2010.05.052
CHEMBL1173287 14277 0 None -67 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 462 4 2 3 4.3 COc1cccc2[nH]cc(CN3CCC(O)(c4ccc(I)cc4)CC3)c12 10.1016/j.bmc.2010.05.052
CHEMBL1200270 14277 0 None -67 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 462 4 2 3 4.3 COc1cccc2[nH]cc(CN3CCC(O)(c4ccc(I)cc4)CC3)c12 10.1016/j.bmc.2010.05.052
164628178 185765 0 None -46 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4875081 185765 0 None -46 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
10007017 82615 0 None -812 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 522 7 2 3 5.6 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(Br)ccc2[nH]1 10.1021/jm0611152
CHEMBL218150 82615 0 None -812 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 522 7 2 3 5.6 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(Br)ccc2[nH]1 10.1021/jm0611152
12581154 25275 10 None -4 3 Human 6.2 pKi = 6.2 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 191 2 1 2 1.8 CNC1CCc2c(cccc2OC)C1 10.1021/jm960345l
CHEMBL135048 25275 10 None -4 3 Human 6.2 pKi = 6.2 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 191 2 1 2 1.8 CNC1CCc2c(cccc2OC)C1 10.1021/jm960345l
10184153 13193 0 None -15 3 Human 6.2 pKi = 6.2 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 477 10 0 4 6.6 C(=C/c1cc(CCCCN2CCN(C(c3ccccc3)c3ccccc3)CC2)on1)\c1ccccc1 10.1016/s0960-894x(02)00179-8
CHEMBL1191883 13193 0 None -15 3 Human 6.2 pKi = 6.2 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 477 10 0 4 6.6 C(=C/c1cc(CCCCN2CCN(C(c3ccccc3)c3ccccc3)CC2)on1)\c1ccccc1 10.1016/s0960-894x(02)00179-8
CHEMBL543041 13193 0 None -15 3 Human 6.2 pKi = 6.2 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 477 10 0 4 6.6 C(=C/c1cc(CCCCN2CCN(C(c3ccccc3)c3ccccc3)CC2)on1)\c1ccccc1 10.1016/s0960-894x(02)00179-8
10994141 44670 0 None -831 4 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 456 7 1 4 4.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccnc2ccccc12 10.1021/jm020952a
CHEMBL152304 44670 0 None -831 4 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 456 7 1 4 4.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccnc2ccccc12 10.1021/jm020952a
164628178 185765 0 None -46 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4875081 185765 0 None -46 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
71657942 89961 0 None -154 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 424 9 1 5 3.5 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(N(C)C)cc2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386605 89961 0 None -154 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 424 9 1 5 3.5 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(N(C)C)cc2)CC1 10.1016/j.bmc.2013.03.074
168268877 189377 0 None -134 12 Human 6.2 pKi = 6.2 Binding
Binding affinity to D4 receptor (unknown origin) assessed as inhibition constantBinding affinity to D4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 328 2 3 3 3.8 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5170784 189377 0 None -134 12 Human 6.2 pKi = 6.2 Binding
Binding affinity to D4 receptor (unknown origin) assessed as inhibition constantBinding affinity to D4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 328 2 3 3 3.8 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
44438204 93223 2 None -48 3 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 324 3 2 2 3.8 OC1(c2ccc(F)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246849 93223 2 None -48 3 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 324 3 2 2 3.8 OC1(c2ccc(F)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
10786591 205002 0 None - 1 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 389 3 0 4 4.7 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(Cl)c(Cl)c1)CC3 10.1021/jm970170v
CHEMBL89913 205002 0 None - 1 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 389 3 0 4 4.7 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(Cl)c(Cl)c1)CC3 10.1021/jm970170v
3746693 200715 12 None 3 3 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 385 4 1 2 5.8 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)[nH]n3)CC2)cc1 10.1021/jm970111h
CHEMBL61080 200715 12 None 3 3 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 385 4 1 2 5.8 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)[nH]n3)CC2)cc1 10.1021/jm970111h
3746693 200715 12 None 3 3 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 385 4 1 2 5.8 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)[nH]n3)CC2)cc1 10.1021/jm0002432
CHEMBL61080 200715 12 None 3 3 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 385 4 1 2 5.8 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)[nH]n3)CC2)cc1 10.1021/jm0002432
155538028 171793 0 None 3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 453 11 2 6 3.1 C=CCN(NC(=O)NCCCN1CCN(c2ccccc2OC)CC1)c1ccc(OC)cc1 10.1021/acs.jmedchem.9b01085
CHEMBL4475978 171793 0 None 3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 453 11 2 6 3.1 C=CCN(NC(=O)NCCCN1CCN(c2ccccc2OC)CC1)c1ccc(OC)cc1 10.1021/acs.jmedchem.9b01085
49782603 17307 0 None -2 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 385 6 1 3 4.9 Cc1ccc(C)c(C(=O)CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)c1 10.1021/jm100899z
CHEMBL1257811 17307 0 None -2 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 385 6 1 3 4.9 Cc1ccc(C)c(C(=O)CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)c1 10.1021/jm100899z
3746693 200715 12 None 3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 385 4 1 2 5.8 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)[nH]n3)CC2)cc1 10.1021/jm960072u
CHEMBL61080 200715 12 None 3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 385 4 1 2 5.8 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)[nH]n3)CC2)cc1 10.1021/jm960072u
11187628 4803 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 363 6 0 4 4.3 COc1ccccc1SCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL104378 4803 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 363 6 0 4 4.3 COc1ccccc1SCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
11164922 5306 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 381 6 0 4 4.0 COc1ccccc1OCC1CN(Cc2ccc(C(F)(F)F)cc2)CCO1 10.1021/jm031111m
CHEMBL107019 5306 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 381 6 0 4 4.0 COc1ccccc1OCC1CN(Cc2ccc(C(F)(F)F)cc2)CCO1 10.1021/jm031111m
9925730 204575 0 None -5 4 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 281 6 2 3 3.0 Cc1nc2c(OCCNCc3ccccc3)cccc2[nH]1 10.1016/s0960-894x(99)00434-5
CHEMBL87067 204575 0 None -5 4 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 281 6 2 3 3.0 Cc1nc2c(OCCNCc3ccccc3)cccc2[nH]1 10.1016/s0960-894x(99)00434-5
178078 120604 3 None -117 3 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human Dopamine receptor D4.2 evaluated using [3H]spiperoneBinding affinity towards human Dopamine receptor D4.2 evaluated using [3H]spiperone
ChEMBL 345 4 1 2 5.4 Oc1ccc(C2=CCC[C@@H](CN3CC=C(c4ccccc4)CC3)C2)cc1 10.1021/jm00026a007
CHEMBL357416 120604 3 None -117 3 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human Dopamine receptor D4.2 evaluated using [3H]spiperoneBinding affinity towards human Dopamine receptor D4.2 evaluated using [3H]spiperone
ChEMBL 345 4 1 2 5.4 Oc1ccc(C2=CCC[C@@H](CN3CC=C(c4ccccc4)CC3)C2)cc1 10.1021/jm00026a007
8704110 66268 9 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 327 4 1 3 2.9 Cc1cccc(NC(=O)CN2CCN(c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL185263 66268 9 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 327 4 1 3 2.9 Cc1cccc(NC(=O)CN2CCN(c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2004.07.068
44340302 9660 0 None 1 4 Human 6.2 pKi = 6.2 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 466 7 1 3 5.3 COc1c(C(=O)NCC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL113471 9660 0 None 1 4 Human 6.2 pKi = 6.2 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 466 7 1 3 5.3 COc1c(C(=O)NCC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
25139331 169361 0 None 1 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 310 9 2 2 3.9 CCCNCCCCNC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800895v
CHEMBL444128 169361 0 None 1 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 310 9 2 2 3.9 CCCNCCCCNC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800895v
137636298 155657 0 None -3 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 245 1 3 4 0.6 O=c1ccc2c(N3CCNCC3)ccc(O)c2[nH]1 10.1016/j.bmc.2017.08.037
CHEMBL4064191 155657 0 None -3 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 245 1 3 4 0.6 O=c1ccc2c(N3CCNCC3)ccc(O)c2[nH]1 10.1016/j.bmc.2017.08.037
681 1437 65 None -2 38 Human 7.2 pKi = 7.2 Binding
Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
940 1437 65 None -2 38 Human 7.2 pKi = 7.2 Binding
Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
947 1437 65 None -2 38 Human 7.2 pKi = 7.2 Binding
Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
CHEMBL59 1437 65 None -2 38 Human 7.2 pKi = 7.2 Binding
Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
DB00988 1437 65 None -2 38 Human 7.2 pKi = 7.2 Binding
Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
137643122 157491 0 None -17 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 467 8 2 10 2.6 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCCO5)CC3)cc12 10.1016/j.bmc.2017.08.037
CHEMBL4085752 157491 0 None -17 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 467 8 2 10 2.6 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCCO5)CC3)cc12 10.1016/j.bmc.2017.08.037
10642106 38986 2 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 357 3 1 4 3.0 O=C1COc2ccc(CN3CCN(c4ccc(Cl)cc4)CC3)cc2N1 10.1021/jm990277d
CHEMBL147011 38986 2 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 357 3 1 4 3.0 O=C1COc2ccc(CN3CCN(c4ccc(Cl)cc4)CC3)cc2N1 10.1021/jm990277d
49799715 14218 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 385 3 2 3 3.8 OC1(c2ccc(Br)cc2)CCN(Cc2c[nH]c3ncccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1170879 14218 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 385 3 2 3 3.8 OC1(c2ccc(Br)cc2)CCN(Cc2c[nH]c3ncccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1200020 14218 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 385 3 2 3 3.8 OC1(c2ccc(Br)cc2)CCN(Cc2c[nH]c3ncccc23)CC1 10.1016/j.bmc.2010.05.052
44374648 119467 0 None -3 4 Human 6.2 pKi = 6.2 Binding
Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)
ChEMBL 351 5 1 4 3.3 CCCN[C@@H]1CCc2c(OS(=O)(=O)C(F)(F)F)cccc2[C@@H]1C 10.1016/S0960-894X(01)80181-5
CHEMBL349843 119467 0 None -3 4 Human 6.2 pKi = 6.2 Binding
Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)
ChEMBL 351 5 1 4 3.3 CCCN[C@@H]1CCc2c(OS(=O)(=O)C(F)(F)F)cccc2[C@@H]1C 10.1016/S0960-894X(01)80181-5
176 394 63 None -4 31 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 394 63 None -4 31 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 394 63 None -4 31 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 394 63 None -4 31 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 394 63 None -4 31 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
44336105 4867 0 None -1 2 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 425 6 0 3 4.5 CC(C)CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104713 4867 0 None -1 2 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 425 6 0 3 4.5 CC(C)CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
155195486 169120 0 None -14 3 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1C[C@@H]1C[C@H]1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
CHEMBL4437740 169120 0 None -14 3 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1C[C@@H]1C[C@H]1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
46231847 198890 0 None -3162 4 Human 5.2 pKi = 5.2 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 343 1 2 3 3.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(CO)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL599116 198890 0 None -3162 4 Human 5.2 pKi = 5.2 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 343 1 2 3 3.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(CO)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
10544707 16125 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 3 0 4 3.4 Cc1ccccc1N1CCN(Cc2ccc3oc(=O)ccc3c2)CC1 10.1021/jm990266k
CHEMBL122531 16125 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 3 0 4 3.4 Cc1ccccc1N1CCN(Cc2ccc3oc(=O)ccc3c2)CC1 10.1021/jm990266k
44426509 85316 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 372 6 1 2 4.7 O=C(NC1CCN(CCCc2ccccc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.096
CHEMBL229024 85316 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 372 6 1 2 4.7 O=C(NC1CCN(CCCc2ccccc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.096
242 467 117 None -117 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.08.037
34 467 117 None -117 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.08.037
60795 467 117 None -117 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.08.037
CHEMBL1112 467 117 None -117 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.08.037
DB01238 467 117 None -117 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.08.037
242 467 117 None -117 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
34 467 117 None -117 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
60795 467 117 None -117 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
CHEMBL1112 467 117 None -117 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
DB01238 467 117 None -117 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
10357869 4815 0 None 6 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 307 4 0 4 4.0 c1ccc(CN2CCC(n3cccc3-c3cnco3)CC2)cc1 10.1016/s0960-894x(99)00540-5
CHEMBL104453 4815 0 None 6 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 307 4 0 4 4.0 c1ccc(CN2CCC(n3cccc3-c3cnco3)CC2)cc1 10.1016/s0960-894x(99)00540-5
44273920 73576 0 None 6 2 Human 7.2 pKi = 7.2 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 377 5 1 3 3.7 CC(C)(C)C(=O)NCCCCN1CCN2c3ccc(Cl)cc3CCC2C1 10.1016/0960-894X(96)00198-9
CHEMBL20204 73576 0 None 6 2 Human 7.2 pKi = 7.2 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 377 5 1 3 3.7 CC(C)(C)C(=O)NCCCCN1CCN2c3ccc(Cl)cc3CCC2C1 10.1016/0960-894X(96)00198-9
44273921 77009 0 None 25 2 Human 7.2 pKi = 7.2 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 365 6 1 3 3.8 CC1CN(CCCCNC(=O)C(C)(C)C)CCN1c1ccc(Cl)cc1 10.1016/0960-894X(96)00198-9
CHEMBL20854 77009 0 None 25 2 Human 7.2 pKi = 7.2 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 365 6 1 3 3.8 CC1CN(CCCCNC(=O)C(C)(C)C)CCN1c1ccc(Cl)cc1 10.1016/0960-894X(96)00198-9
4302960 100592 57 None -199 6 Human 7.2 pKi = 7.2 Binding
Binding affinity towards Dopamine D4 receptorBinding affinity towards Dopamine D4 receptor
ChEMBL 485 10 1 5 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccc(C(C)=O)cc3)cc2)CC1 10.1016/0960-894X(95)00011-H
CHEMBL294747 100592 57 None -199 6 Human 7.2 pKi = 7.2 Binding
Binding affinity towards Dopamine D4 receptorBinding affinity towards Dopamine D4 receptor
ChEMBL 485 10 1 5 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccc(C(C)=O)cc3)cc2)CC1 10.1016/0960-894X(95)00011-H
168268735 192167 0 None 16 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 335 4 0 3 2.8 O=C1CCc2ccccc2N1CCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5171721 192167 0 None 16 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 335 4 0 3 2.8 O=C1CCc2ccccc2N1CCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5221227 192167 0 None 16 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 335 4 0 3 2.8 O=C1CCc2ccccc2N1CCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5092243 213580 0 None 1 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCc1cccc(N2CCN(CCC(c3cccc(OC)c3)c3cccc(OC)c3)CC2)c1Cl 10.1021/acs.jmedchem.1c00611
10430816 167684 1 None -371 4 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 395 8 1 4 3.6 COc1cccc(C(=O)NCCCCN2CCN(c3cccc(C)c3C)CC2)c1 10.1021/jm020952a
CHEMBL433741 167684 1 None -371 4 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 395 8 1 4 3.6 COc1cccc(C(=O)NCCCCN2CCN(c3cccc(C)c3C)CC2)c1 10.1021/jm020952a
49788868 18039 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 364 6 1 5 2.1 COc1cccc(C(=O)NCCN2CCN(c3ccc(C#N)cc3)CC2)c1 10.1021/jm100925m
CHEMBL1270120 18039 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 364 6 1 5 2.1 COc1cccc(C(=O)NCCN2CCN(c3ccc(C#N)cc3)CC2)c1 10.1021/jm100925m
44437896 151936 0 None -57 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 400 6 1 3 2.7 C=CCN1CCC[C@H]1CNC(=O)c1cc(I)ccc1OC 10.1016/j.bmc.2007.07.017
CHEMBL397103 151936 0 None -57 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 400 6 1 3 2.7 C=CCN1CCC[C@H]1CNC(=O)c1cc(I)ccc1OC 10.1016/j.bmc.2007.07.017
10479822 82616 0 None -1778 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 469 7 2 4 4.7 N#Cc1ccc2cc(C(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)[nH]c2c1 10.1021/jm0611152
CHEMBL218151 82616 0 None -1778 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 469 7 2 4 4.7 N#Cc1ccc2cc(C(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)[nH]c2c1 10.1021/jm0611152
90389439 145166 0 None -14 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 406 8 1 4 3.8 CC(O)CN1CCN(CCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2020.112674
CHEMBL3916231 145166 0 None -14 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 406 8 1 4 3.8 CC(O)CN1CCN(CCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2020.112674
90389439 145166 0 None -14 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 406 8 1 4 3.8 CC(O)CN1CCN(CCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.6b01373
CHEMBL3916231 145166 0 None -14 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 406 8 1 4 3.8 CC(O)CN1CCN(CCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.6b01373
52937871 60844 0 None -162 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 458 11 1 5 4.6 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCn2ncc(C=O)c2C1 10.1021/jm101639t
CHEMBL1765631 60844 0 None -162 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 458 11 1 5 4.6 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCn2ncc(C=O)c2C1 10.1021/jm101639t
12280575 10190 2 None -6 5 Human 6.2 pKi = 6.2 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 261 6 0 2 3.7 CCCN(CCC)C1CCc2c(cccc2OC)C1 10.1021/jm960345l
CHEMBL11615 10190 2 None -6 5 Human 6.2 pKi = 6.2 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 261 6 0 2 3.7 CCCN(CCC)C1CCc2c(cccc2OC)C1 10.1021/jm960345l
49798797 14241 0 None -10 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 433 3 2 3 3.7 OC1(c2ccc(I)cc2)CCN(Cc2c[nH]c3ncccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1172208 14241 0 None -10 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 433 3 2 3 3.7 OC1(c2ccc(I)cc2)CCN(Cc2c[nH]c3ncccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1200149 14241 0 None -10 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 433 3 2 3 3.7 OC1(c2ccc(I)cc2)CCN(Cc2c[nH]c3ncccc23)CC1 10.1016/j.bmc.2010.05.052
3038495 700 30 None -91 19 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/acs.jmedchem.9b01835
7625 700 30 None -91 19 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/acs.jmedchem.9b01835
CHEMBL25236 700 30 None -91 19 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/acs.jmedchem.9b01835
72190766 91928 0 None -12 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-spiperone from cloned human dopamine D4 receptorDisplacement of [3H]-spiperone from cloned human dopamine D4 receptor
ChEMBL 391 8 0 6 3.6 COc1ccccc1N1CCN(CCCCn2cc(-c3ccccc3)nn2)CC1 10.1016/j.bmcl.2013.08.047
CHEMBL2430443 91928 0 None -12 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-spiperone from cloned human dopamine D4 receptorDisplacement of [3H]-spiperone from cloned human dopamine D4 receptor
ChEMBL 391 8 0 6 3.6 COc1ccccc1N1CCN(CCCCn2cc(-c3ccccc3)nn2)CC1 10.1016/j.bmcl.2013.08.047
44336175 107711 0 None -13 2 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 399 5 0 4 3.1 COc1cccc2c1CCN2C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL319650 107711 0 None -13 2 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 399 5 0 4 3.1 COc1cccc2c1CCN2C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
44339879 171716 0 None 4 4 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.8 CNc1cc(OC)c(C(=O)N[C@H]2CCCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL447476 171716 0 None 4 4 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.8 CNc1cc(OC)c(C(=O)N[C@H]2CCCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(03)00678-4
10871118 205080 0 None 186 4 Human 7.2 pKi = 7.2 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cccn4nccc34)CC2)cc1 10.1021/jm015522j
CHEMBL90374 205080 0 None 186 4 Human 7.2 pKi = 7.2 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cccn4nccc34)CC2)cc1 10.1021/jm015522j
44335847 4992 0 None 36 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@@H]3C)CC2)cc1 10.1016/s0960-894x(02)00656-x
CHEMBL105354 4992 0 None 36 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@@H]3C)CC2)cc1 10.1016/s0960-894x(02)00656-x
155536022 171537 0 None 3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 467 11 2 6 3.5 C=C(C)CN(NC(=O)NCCCN1CCN(c2ccccc2OC)CC1)c1ccc(OC)cc1 10.1021/acs.jmedchem.9b01085
CHEMBL4472580 171537 0 None 3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 467 11 2 6 3.5 C=C(C)CN(NC(=O)NCCCN1CCN(c2ccccc2OC)CC1)c1ccc(OC)cc1 10.1021/acs.jmedchem.9b01085
164614709 184626 0 None -15 7 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 383 6 0 4 4.1 O=C1c2ccc(Cl)cc2CC1CCCCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL4857665 184626 0 None -15 7 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 383 6 0 4 4.1 O=C1c2ccc(Cl)cc2CC1CCCCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
57400556 68968 0 None -97 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 495 13 1 8 3.1 CCOCCOc1ccn2ncc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
CHEMBL1928134 68968 0 None -97 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 495 13 1 8 3.1 CCOCCOc1ccn2ncc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
56589560 70253 0 None -14 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 304 0 1 1 4.2 C[C@H]1Cc2c([nH]c3ccccc23)Cc2ccccc2CCN1C 10.1021/jm200676f
CHEMBL1949725 70253 0 None -14 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 304 0 1 1 4.2 C[C@H]1Cc2c([nH]c3ccccc23)Cc2ccccc2CCN1C 10.1021/jm200676f
164614709 184626 0 None -15 7 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 383 6 0 4 4.1 O=C1c2ccc(Cl)cc2CC1CCCCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL4857665 184626 0 None -15 7 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 383 6 0 4 4.1 O=C1c2ccc(Cl)cc2CC1CCCCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
164621610 185609 0 None -4 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 355 4 0 4 3.3 O=C1c2ccc(Cl)cc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL4872800 185609 0 None -4 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 355 4 0 4 3.3 O=C1c2ccc(Cl)cc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL5088070 213362 0 None -75 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCc1cccc(N2CCN(CCC(C(=O)N(C)C)(c3ccccc3)c3ccccc3)CC2)c1Cl 10.1021/acs.jmedchem.1c00611
24810004 16373 0 None -10 4 Human 6.2 pKi = 6.2 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 419 6 0 2 6.3 Fc1ccc(C(OC2CC3CCC(C2)N3Cc2ccccc2)c2ccc(F)cc2)cc1 10.1021/jm010146o
CHEMBL12375 16373 0 None -10 4 Human 6.2 pKi = 6.2 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 419 6 0 2 6.3 Fc1ccc(C(OC2CC3CCC(C2)N3Cc2ccccc2)c2ccc(F)cc2)cc1 10.1021/jm010146o
42626103 55960 0 None -1479 4 Human 6.2 pKi = 6.2 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 442 6 2 3 4.6 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
CHEMBL1627323 55960 0 None -1479 4 Human 6.2 pKi = 6.2 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 442 6 2 3 4.6 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
168274755 190048 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 403 5 0 4 4.8 Cn1cnc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
CHEMBL5181334 190048 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 403 5 0 4 4.8 Cn1cnc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
10039198 56055 0 None -4 4 Human 6.2 pKi = 6.2 Binding
Dissociation constant of compound on one-site model Dopamine receptor D4.4Dissociation constant of compound on one-site model Dopamine receptor D4.4
ChEMBL 277 5 0 1 4.5 CCCN(CCC)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm991098z
CHEMBL163087 56055 0 None -4 4 Human 6.2 pKi = 6.2 Binding
Dissociation constant of compound on one-site model Dopamine receptor D4.4Dissociation constant of compound on one-site model Dopamine receptor D4.4
ChEMBL 277 5 0 1 4.5 CCCN(CCC)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm991098z
11049209 205672 0 None -13182 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 486 6 1 5 4.4 Cn1ccc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL93923 205672 0 None -13182 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 486 6 1 5 4.4 Cn1ccc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
11658914 69897 0 None -30 3 Human 5.2 pKi = 5.2 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 255 5 0 3 3.0 CCCN(CCC)C1CCn2ncc(Cl)c2C1 10.1021/jm0503805
CHEMBL194099 69897 0 None -30 3 Human 5.2 pKi = 5.2 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 255 5 0 3 3.0 CCCN(CCC)C1CCn2ncc(Cl)c2C1 10.1021/jm0503805
54456 161940 27 None -1 2 Human 5.2 pKi = 5.2 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 179 0 3 3 1.3 CC1NCCc2cc(O)c(O)cc21 10.1016/S0960-894X(97)00194-7
CHEMBL416732 161940 27 None -1 2 Human 5.2 pKi = 5.2 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 179 0 3 3 1.3 CC1NCCc2cc(O)c(O)cc21 10.1016/S0960-894X(97)00194-7
155568867 175580 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 297 4 1 5 1.2 O=C(CN1CCN(c2ccccn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
CHEMBL4592753 175580 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 297 4 1 5 1.2 O=C(CN1CCN(c2ccccn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
71658206 89976 0 None -42 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 416 8 1 5 3.5 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(Cl)nc2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386620 89976 0 None -42 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 416 8 1 5 3.5 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(Cl)nc2)CC1 10.1016/j.bmc.2013.03.074
11316709 167806 0 None -77 3 Rat 6.2 pKi = 6.2 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 443 7 1 4 4.5 COc1cccc2c1CC[C@@H]1CN(CCCCNC(=O)c3ccc4ccccc4c3)CCN21 10.1021/jm049031l
CHEMBL434532 167806 0 None -77 3 Rat 6.2 pKi = 6.2 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 443 7 1 4 4.5 COc1cccc2c1CC[C@@H]1CN(CCCCNC(=O)c3ccc4ccccc4c3)CCN21 10.1021/jm049031l
10761828 38439 0 None -3 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 372 4 1 5 4.4 Oc1nc2ccccc2n1C1CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1021/jm00025a013
CHEMBL146557 38439 0 None -3 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 372 4 1 5 4.4 Oc1nc2ccccc2n1C1CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1021/jm00025a013
168274850 189562 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 405 6 0 5 4.4 FC(F)(F)Oc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5173767 189562 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 405 6 0 5 4.4 FC(F)(F)Oc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.bmcl.2022.128615
2993172 126646 3 None -32 3 Human 5.2 pKi = 5.2 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 297 6 0 3 3.0 c1ccc(Cc2ccccc2OCCN2CCOCC2)cc1 10.1021/jm049720x
CHEMBL365697 126646 3 None -32 3 Human 5.2 pKi = 5.2 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 297 6 0 3 3.0 c1ccc(Cc2ccccc2OCCN2CCOCC2)cc1 10.1021/jm049720x
9828632 99608 0 None -8 3 Human 7.2 pKi = 7.2 Binding
Affinity against D4 receptor was evaluatedAffinity against D4 receptor was evaluated
ChEMBL 535 6 1 4 5.5 COc1c(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(Br)c2ccccc12 10.1016/s0960-894x(98)00469-7
CHEMBL287198 99608 0 None -8 3 Human 7.2 pKi = 7.2 Binding
Affinity against D4 receptor was evaluatedAffinity against D4 receptor was evaluated
ChEMBL 535 6 1 4 5.5 COc1c(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(Br)c2ccccc12 10.1016/s0960-894x(98)00469-7
763343 91709 8 None 25 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 258 3 0 3 3.1 c1ccc(N2CCN(Cc3cccs3)CC2)cc1 10.1016/j.bmcl.2013.07.033
CHEMBL2420769 91709 8 None 25 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 258 3 0 3 3.1 c1ccc(N2CCN(Cc3cccs3)CC2)cc1 10.1016/j.bmcl.2013.07.033
10137747 119668 0 None 4 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 433 4 0 4 3.8 COc1ccc(C)cc1CN1CCN(C2CCc3cccc4c3N(C2=O)C(C)(C)C4)CC1 10.1016/s0960-894x(02)01056-9
CHEMBL351612 119668 0 None 4 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 433 4 0 4 3.8 COc1ccc(C)cc1CN1CCN(C2CCc3cccc4c3N(C2=O)C(C)(C)C4)CC1 10.1016/s0960-894x(02)01056-9
164621610 185609 0 None -4 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 355 4 0 4 3.3 O=C1c2ccc(Cl)cc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL4872800 185609 0 None -4 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 355 4 0 4 3.3 O=C1c2ccc(Cl)cc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
11676195 193478 0 None 1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 423 8 1 6 3.4 CSc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm900690y
CHEMBL550222 193478 0 None 1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 423 8 1 6 3.4 CSc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm900690y
72737730 114028 0 None 42 3 Human 7.2 pKi = 7.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 365 6 0 3 4.4 FC(F)(F)Oc1ccc(CN2CCO[C@H](CCc3ccccc3)C2)cc1 10.1021/ml500267c
CHEMBL3335554 114028 0 None 42 3 Human 7.2 pKi = 7.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 365 6 0 3 4.4 FC(F)(F)Oc1ccc(CN2CCO[C@H](CCc3ccccc3)C2)cc1 10.1021/ml500267c
155535272 171465 0 None -177 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 280 5 0 2 3.8 CCCCN1CCN(c2cccc(CC)c2Cl)CC1 10.1021/acs.jmedchem.6b00860
CHEMBL4471669 171465 0 None -177 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 280 5 0 2 3.8 CCCCN1CCN(c2cccc(CC)c2Cl)CC1 10.1021/acs.jmedchem.6b00860
60165535 75000 0 None -12 6 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 322 5 0 3 4.7 c1ccc2c(c1)CCN(CCCCc1nc3ccccc3s1)C2 10.1016/j.ejmech.2012.03.042
CHEMBL2037522 75000 0 None -12 6 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 322 5 0 3 4.7 c1ccc2c(c1)CCN(CCCCc1nc3ccccc3s1)C2 10.1016/j.ejmech.2012.03.042
11428005 4988 0 None - 1 Human 6.2 pKi = 6.2 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 347 6 0 4 3.6 COc1ccccc1OCC1CN(Cc2cccc(Cl)c2)CCO1 10.1021/jm031111m
CHEMBL105312 4988 0 None - 1 Human 6.2 pKi = 6.2 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 347 6 0 4 3.6 COc1ccccc1OCC1CN(Cc2cccc(Cl)c2)CCO1 10.1021/jm031111m
44304643 201584 0 None 1 4 Human 6.2 pKi = 6.2 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 469 8 0 5 5.1 COc1ccc(Br)cc1-c1nc(CN(C)C[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL64668 201584 0 None 1 4 Human 6.2 pKi = 6.2 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 469 8 0 5 5.1 COc1ccc(Br)cc1-c1nc(CN(C)C[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
11028157 201033 0 None -128 4 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 563 8 1 4 6.3 COc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(Br)c2ccccc12 10.1021/jm020952a
CHEMBL61789 201033 0 None -128 4 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 563 8 1 4 6.3 COc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(Br)c2ccccc12 10.1021/jm020952a
30982708 10582 5 None -134 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 384 3 2 2 4.4 OC1(c2ccc(Br)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1170683 10582 5 None -134 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 384 3 2 2 4.4 OC1(c2ccc(Br)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2010.05.052
71658203 89973 0 None -57 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 483 8 1 5 4.6 COc1ccccc1N1CCCN(CCCCNC(=O)c2cccc3c2-c2ccccc2C3=O)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386617 89973 0 None -57 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 483 8 1 5 4.6 COc1ccccc1N1CCCN(CCCCNC(=O)c2cccc3c2-c2ccccc2C3=O)CC1 10.1016/j.bmc.2013.03.074
11247757 133056 0 None -70 3 Rat 6.2 pKi = 6.2 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 443 7 1 4 4.5 COc1cccc2c1CC[C@H]1CN(CCCCNC(=O)c3ccc4ccccc4c3)CCN21 10.1021/jm049031l
CHEMBL371200 133056 0 None -70 3 Rat 6.2 pKi = 6.2 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 443 7 1 4 4.5 COc1cccc2c1CC[C@H]1CN(CCCCNC(=O)c3ccc4ccccc4c3)CCN21 10.1021/jm049031l
44431465 150204 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 422 4 1 2 5.0 O=C(NC1CCN(Cc2cccc(Br)c2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
CHEMBL395631 150204 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 422 4 1 2 5.0 O=C(NC1CCN(Cc2cccc(Br)c2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
137645574 157261 0 None -70 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 462 7 3 6 3.1 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4083239 157261 0 None -70 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 462 7 3 6 3.1 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
45271691 193880 0 None 46 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 369 3 0 5 3.6 Cc1cc2nc(C)c(CN3CCN(c4ccc(Cl)cc4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
CHEMBL554692 193880 0 None 46 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 369 3 0 5 3.6 Cc1cc2nc(C)c(CN3CCN(c4ccc(Cl)cc4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
45272580 194782 0 None 13 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 351 4 0 6 2.7 COc1ccccc1N1CCN(Cc2cnc3cc(C)nc(C)n23)CC1 10.1016/j.bmc.2009.05.015
CHEMBL563109 194782 0 None 13 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 351 4 0 6 2.7 COc1ccccc1N1CCN(Cc2cnc3cc(C)nc(C)n23)CC1 10.1016/j.bmc.2009.05.015
145993700 166776 0 None -75 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 370 7 3 5 2.7 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(O)cc1)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4294279 166776 0 None -75 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 370 7 3 5 2.7 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(O)cc1)CC2 10.1021/acsmedchemlett.8b00229
56833379 67992 0 None -54 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 1155 37 2 18 8.6 COc1cc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2009919
CHEMBL1916550 67992 0 None -54 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 1155 37 2 18 8.6 COc1cc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2009919
CHEMBL5089932 213459 0 None -25 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCc1cc(Cl)c(OC)c(C(=O)NC[C@@H]2CCCN2CCCCNCCC(C(=O)N(C)C)(c2ccccc2)c2ccccc2)c1O 10.1021/acs.jmedchem.1c00611
46227273 198129 0 None -2 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 281 3 0 2 3.8 COc1ccc2c(c1)CCN(C)C2Cc1ccccc1C 10.1016/j.bmc.2009.08.028
CHEMBL594127 198129 0 None -2 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 281 3 0 2 3.8 COc1ccc2c(c1)CCN(C)C2Cc1ccccc1C 10.1016/j.bmc.2009.08.028
155195487 172705 0 None -14 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1CC1CC1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
CHEMBL4525362 172705 0 None -14 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1CC1CC1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
49799709 14291 0 None -24 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 446 6 2 3 4.8 OC1(c2ccc(Br)cc2)CCN(Cc2c[nH]c3cccc(OCCF)c23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1173711 14291 0 None -24 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 446 6 2 3 4.8 OC1(c2ccc(Br)cc2)CCN(Cc2c[nH]c3cccc(OCCF)c23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1200302 14291 0 None -24 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 446 6 2 3 4.8 OC1(c2ccc(Br)cc2)CCN(Cc2c[nH]c3cccc(OCCF)c23)CC1 10.1016/j.bmc.2010.05.052
44361021 118281 0 None -23 6 Human 7.2 pKi = 7.2 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccn3nccc3c2)CC1 10.1021/jm025558r
CHEMBL342060 118281 0 None -23 6 Human 7.2 pKi = 7.2 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccn3nccc3c2)CC1 10.1021/jm025558r
44335971 5245 0 None 18 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 4 0 3 4.0 CC(c1ccc(Cl)cc1)N1CCN(CC(=O)N2c3ccccc3CC2C)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL106751 5245 0 None 18 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 4 0 3 4.0 CC(c1ccc(Cl)cc1)N1CCN(CC(=O)N2c3ccccc3CC2C)CC1 10.1016/s0960-894x(02)00655-8
10740969 98629 0 None 3 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 423 7 1 5 3.4 COc1ccccc1N1CCN(CCC(=O)NC2CCCc3c(OC)cccc32)CC1 10.1016/S0960-894X(97)00218-7
CHEMBL28063 98629 0 None 3 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 423 7 1 5 3.4 COc1ccccc1N1CCN(CCC(=O)NC2CCCc3c(OC)cccc32)CC1 10.1016/S0960-894X(97)00218-7
11849267 79462 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 372 6 0 5 3.7 CO/N=C(\CCN1CCN(c2ccccn2)CC1C)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL212292 79462 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 372 6 0 5 3.7 CO/N=C(\CCN1CCN(c2ccccn2)CC1C)c1ccc(Cl)cc1 10.1021/jm060279f
127052488 140268 0 None -2 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 477 8 0 4 6.3 Fc1ccc(C(c2ccc(F)cc2)N2CCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2016.06.011
CHEMBL3818799 140268 0 None -2 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 477 8 0 4 6.3 Fc1ccc(C(c2ccc(F)cc2)N2CCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2016.06.011
11133602 30559 0 None -3 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 421 9 1 6 3.1 COc1ccccc1N1CCN(CCCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm0611152
CHEMBL139600 30559 0 None -3 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 421 9 1 6 3.1 COc1ccccc1N1CCN(CCCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm0611152
44361021 118281 0 None -23 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccn3nccc3c2)CC1 10.1021/jm0611152
CHEMBL342060 118281 0 None -23 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccn3nccc3c2)CC1 10.1021/jm0611152
45361874 169454 2 None 48 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 324 5 1 4 2.4 CCc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4442548 169454 2 None 48 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 324 5 1 4 2.4 CCc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
25139481 184257 0 None -4 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 392 10 1 2 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCCCC1 10.1021/jm800895v
CHEMBL485227 184257 0 None -4 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 392 10 1 2 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCCCC1 10.1021/jm800895v
154706590 175735 1 None -36 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 421 11 2 2 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4590839 175735 1 None -36 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 421 11 2 2 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4595264 175735 1 None -36 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 421 11 2 2 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
127049061 140236 0 None -4 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 440 6 1 5 5.3 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
CHEMBL3818398 140236 0 None -4 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 440 6 1 5 5.3 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
CHEMBL5081136 212953 0 None -309 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCc1cc(Cl)c(OC)c(C(=O)NC[C@@H]2C[C@@H](OCCCCNCCC(C(=O)N(C)C)(c3ccccc3)c3ccccc3)CN2)c1O 10.1021/acs.jmedchem.1c00611
155516042 175719 0 None -446 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4443039 175719 0 None -446 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4595150 175719 0 None -446 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
154703875 175874 1 None -52 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4586582 175874 1 None -52 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4596341 175874 1 None -52 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
10827222 6907 1 None -61 5 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human dopamine receptor D4 was determinedBinding affinity towards human dopamine receptor D4 was determined
ChEMBL 288 3 0 2 3.6 C(#Cc1cccnc1)CCN1CC=C(c2ccccc2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL108463 6907 1 None -61 5 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human dopamine receptor D4 was determinedBinding affinity towards human dopamine receptor D4 was determined
ChEMBL 288 3 0 2 3.6 C(#Cc1cccnc1)CCN1CC=C(c2ccccc2)CC1 10.1016/j.bmcl.2005.02.012
127049061 140236 0 None -4 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 440 6 1 5 5.3 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
CHEMBL3818398 140236 0 None -4 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 440 6 1 5 5.3 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
44438231 93176 3 None -4 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 375 3 2 3 4.4 OC1(c2ccc(Cl)c(Cl)c2)CCN(Cc2n[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246642 93176 3 None -4 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 375 3 2 3 4.4 OC1(c2ccc(Cl)c(Cl)c2)CCN(Cc2n[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
10927750 7297 0 None 1 3 Human 6.2 pKi = 6.2 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 411 6 1 3 4.2 O=C(NCCCN1CCN(c2ccccc2)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm010146o
CHEMBL108637 7297 0 None 1 3 Human 6.2 pKi = 6.2 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 411 6 1 3 4.2 O=C(NCCCN1CCN(c2ccccc2)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm010146o
44438208 92938 2 None -3 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 336 4 2 3 3.7 COc1ccc(C2(O)CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.10.076
CHEMBL245614 92938 2 None -3 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 336 4 2 3 3.7 COc1ccc(C2(O)CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.10.076
11133602 30559 0 None -3 5 Human 7.2 pKi = 7.2 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 421 9 1 6 3.1 COc1ccccc1N1CCN(CCCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
CHEMBL139600 30559 0 None -3 5 Human 7.2 pKi = 7.2 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 421 9 1 6 3.1 COc1ccccc1N1CCN(CCCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
10713620 39156 0 None -19 3 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human Dopamine receptor D4.2 evaluated using [3H]spiperoneBinding affinity towards human Dopamine receptor D4.2 evaluated using [3H]spiperone
ChEMBL 361 4 2 3 5.1 Oc1ccc(C2=CCN(C[C@@H]3CCC=C(c4ccc(O)cc4)C3)CC2)cc1 10.1021/jm00026a007
CHEMBL147159 39156 0 None -19 3 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human Dopamine receptor D4.2 evaluated using [3H]spiperoneBinding affinity towards human Dopamine receptor D4.2 evaluated using [3H]spiperone
ChEMBL 361 4 2 3 5.1 Oc1ccc(C2=CCN(C[C@@H]3CCC=C(c4ccc(O)cc4)C3)CC2)cc1 10.1021/jm00026a007
127052488 140268 0 None -2 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 477 8 0 4 6.3 Fc1ccc(C(c2ccc(F)cc2)N2CCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2016.06.011
CHEMBL3818799 140268 0 None -2 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 477 8 0 4 6.3 Fc1ccc(C(c2ccc(F)cc2)N2CCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2016.06.011
57390118 68960 0 None -77 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 953 32 2 13 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928126 68960 0 None -77 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 953 32 2 13 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
22100970 102352 4 None 10 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 323 3 1 2 4.5 Clc1ccc(CN2CC=C(c3nc4ccccc4[nH]3)CC2)cc1 10.1016/S0960-894X(97)00402-2
CHEMBL305481 102352 4 None 10 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 323 3 1 2 4.5 Clc1ccc(CN2CC=C(c3nc4ccccc4[nH]3)CC2)cc1 10.1016/S0960-894X(97)00402-2
10073022 85631 0 None -4 4 Human 7.2 pKi = 7.2 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 461 9 0 2 7.1 Fc1ccc(C(O[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCc2ccccc2)c2ccc(F)cc2)cc1 10.1021/jm010146o
CHEMBL2308105 85631 0 None -4 4 Human 7.2 pKi = 7.2 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 461 9 0 2 7.1 Fc1ccc(C(O[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCc2ccccc2)c2ccc(F)cc2)cc1 10.1021/jm010146o
72545008 92691 0 None 1 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 451 15 0 9 1.6 COc1ccccc1N1CCN(Cc2cn(CCOCCOCCOCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443001 92691 0 None 1 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 451 15 0 9 1.6 COc1ccccc1N1CCN(Cc2cn(CCOCCOCCOCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
10960333 205256 0 None 1 4 Human 5.2 pKi = 5.2 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 398 5 0 6 3.5 CCOC(=O)c1cnn2cccc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1021/jm015522j
CHEMBL91362 205256 0 None 1 4 Human 5.2 pKi = 5.2 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 398 5 0 6 3.5 CCOC(=O)c1cnn2cccc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1021/jm015522j
10827222 6907 1 None -61 5 Human 6.2 pKi = 6.2 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 288 3 0 2 3.6 C(#Cc1cccnc1)CCN1CC=C(c2ccccc2)CC1 10.1021/jm950721m
CHEMBL108463 6907 1 None -61 5 Human 6.2 pKi = 6.2 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 288 3 0 2 3.6 C(#Cc1cccnc1)CCN1CC=C(c2ccccc2)CC1 10.1021/jm950721m
44275820 13854 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 375 7 0 4 4.8 Cc1ccccc1N1CCN(CCCCc2cc(-c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL1196753 13854 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 375 7 0 4 4.8 Cc1ccccc1N1CCN(CCCCc2cc(-c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL558036 13854 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 375 7 0 4 4.8 Cc1ccccc1N1CCN(CCCCc2cc(-c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
44123782 189009 0 None -6 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 338 3 1 3 3.7 Clc1ccc(N2CC3CC2CN3Cc2c[nH]c3ncccc23)cc1 10.1016/j.bmc.2008.12.054
CHEMBL514747 189009 0 None -6 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 338 3 1 3 3.7 Clc1ccc(N2CC3CC2CN3Cc2c[nH]c3ncccc23)cc1 10.1016/j.bmc.2008.12.054
71456889 81412 0 None -36 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 466 7 0 5 4.7 COc1ccccc1N1CCN(CCN(C(=O)c2cccc3ccccc23)c2ccccn2)CC1 10.1016/j.bmcl.2012.05.119
CHEMBL2164348 81412 0 None -36 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 466 7 0 5 4.7 COc1ccccc1N1CCN(CCN(C(=O)c2cccc3ccccc23)c2ccccn2)CC1 10.1016/j.bmcl.2012.05.119
44431476 87149 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.5 Cc1ccc(CN2CCC(NC(=O)c3cccc4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.12.106
CHEMBL233578 87149 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.5 Cc1ccc(CN2CCC(NC(=O)c3cccc4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.12.106
25139477 183663 0 None -15 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 486 10 1 2 6.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm800895v
CHEMBL483593 183663 0 None -15 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 486 10 1 2 6.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm800895v
44436618 147390 0 None -45 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 443 8 1 3 4.7 C#Cc1ccc(C(=O)NCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.bmc.2007.08.038
CHEMBL393365 147390 0 None -45 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 443 8 1 3 4.7 C#Cc1ccc(C(=O)NCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.bmc.2007.08.038
130442572 171342 0 None -147 24 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4469848 171342 0 None -147 24 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
130442480 174698 0 None -85 24 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
CHEMBL4572614 174698 0 None -85 24 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
2812 4711 96 None -39 34 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 4711 96 None -39 34 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
44340333 9571 0 None 19 4 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 384 5 1 3 3.8 C#Cc1cc(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)c(OC)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL112833 9571 0 None 19 4 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 384 5 1 3 3.8 C#Cc1cc(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)c(OC)c2ccccc12 10.1016/s0960-894x(03)00678-4
21462980 46871 0 None 23 3 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 263 2 1 2 3.1 c1ccc2c(c1)CCN(Cc1c[nH]c3ncccc13)C2 10.1016/s0960-894x(99)00025-6
CHEMBL154286 46871 0 None 23 3 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 263 2 1 2 3.1 c1ccc2c(c1)CCN(Cc1c[nH]c3ncccc13)C2 10.1016/s0960-894x(99)00025-6
2389 3279 114 None -21 67 Human 8.2 pKi = 8.2 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm00004a016
5073 3279 114 None -21 67 Human 8.2 pKi = 8.2 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm00004a016
96 3279 114 None -21 67 Human 8.2 pKi = 8.2 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm00004a016
CHEMBL85 3279 114 None -21 67 Human 8.2 pKi = 8.2 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm00004a016
DB00734 3279 114 None -21 67 Human 8.2 pKi = 8.2 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm00004a016
9861459 163566 0 None -17 4 Human 8.2 pKi = 8.2 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 309 4 3 4 2.8 Oc1nc2c3c(ccc2[nH]1)CC[C@H](CNCc1ccccc1)O3 10.1016/s0960-894x(01)00778-8
CHEMBL420986 163566 0 None -17 4 Human 8.2 pKi = 8.2 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 309 4 3 4 2.8 Oc1nc2c3c(ccc2[nH]1)CC[C@H](CNCc1ccccc1)O3 10.1016/s0960-894x(01)00778-8
6469918 79481 13 None 169 6 Human 8.2 pKi = 8.2 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1 10.1016/j.ejmech.2019.111569
CHEMBL212370 79481 13 None 169 6 Human 8.2 pKi = 8.2 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1 10.1016/j.ejmech.2019.111569
10646834 106680 0 None 14 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 441 7 2 4 4.1 COc1cc(NC(=O)C2CCC2)c(Cl)cc1C(=O)N[C@@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
CHEMBL316317 106680 0 None 14 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 441 7 2 4 4.1 COc1cc(NC(=O)C2CCC2)c(Cl)cc1C(=O)N[C@@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
44336099 110199 0 None 38 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 417 4 0 3 4.1 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2cc(Cl)cc(Cl)c2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL326010 110199 0 None 38 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 417 4 0 3 4.1 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2cc(Cl)cc(Cl)c2)CC1 10.1016/s0960-894x(02)00656-x
44336051 110818 0 None 16 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 4 0 3 4.0 C[C@@H]1c2ccccc2N(C(=O)CN2CCN(Cc3ccc(Cl)cc3)CC2)[C@@H]1C 10.1016/s0960-894x(02)00655-8
CHEMBL326670 110818 0 None 16 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 4 0 3 4.0 C[C@@H]1c2ccccc2N(C(=O)CN2CCN(Cc3ccc(Cl)cc3)CC2)[C@@H]1C 10.1016/s0960-894x(02)00655-8
44335798 4776 0 None 213 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 363 4 0 3 3.1 Cc1ccccc1CN1CCN(CC(=O)N2c3ccccc3CC2C)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104256 4776 0 None 213 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 363 4 0 3 3.1 Cc1ccccc1CN1CCN(CC(=O)N2c3ccccc3CC2C)CC1 10.1016/s0960-894x(02)00655-8
44335924 4846 0 None 125 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 367 4 0 3 2.9 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(F)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104614 4846 0 None 125 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 367 4 0 3 2.9 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(F)cc2)CC1 10.1016/s0960-894x(02)00655-8
44335886 4871 0 None 7 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 366 4 0 2 4.4 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2cccc(F)c2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104719 4871 0 None 7 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 366 4 0 2 4.4 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2cccc(F)c2)CC1 10.1016/s0960-894x(02)00655-8
44335991 4887 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 405 5 0 4 2.8 O=S1(=O)Cc2ccccc2N1CCN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104800 4887 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 405 5 0 4 2.8 O=S1(=O)Cc2ccccc2N1CCN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
1353 1880 85 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00025a013
3559 1880 85 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00025a013
86 1880 85 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00025a013
CHEMBL54 1880 85 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00025a013
DB00502 1880 85 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00025a013
44405522 71585 0 None 251 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 406 5 1 5 4.1 O=C(N[C@H]1CCN(Cc2ccc3c(c2)OCO3)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
CHEMBL197225 71585 0 None 251 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 406 5 1 5 4.1 O=C(N[C@H]1CCN(Cc2ccc3c(c2)OCO3)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
6469918 79481 13 None 169 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1 10.1021/jm060166w
CHEMBL212370 79481 13 None 169 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1 10.1021/jm060166w
11338828 4966 0 None - 1 Human 8.2 pKi = 8.2 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 409 7 0 4 5.1 CCOc1cc(Cl)ccc1OCC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/jm031111m
CHEMBL105181 4966 0 None - 1 Human 8.2 pKi = 8.2 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 409 7 0 4 5.1 CCOc1cc(Cl)ccc1OCC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/jm031111m
9820680 204482 0 None -2 4 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 369 6 2 3 4.4 FC(F)(F)c1nc2c(OCCNCc3ccccc3)cc(Cl)cc2[nH]1 10.1016/s0960-894x(99)00434-5
CHEMBL86504 204482 0 None -2 4 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 369 6 2 3 4.4 FC(F)(F)c1nc2c(OCCNCc3ccccc3)cc(Cl)cc2[nH]1 10.1016/s0960-894x(99)00434-5
681 1437 65 None -2 38 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
940 1437 65 None -2 38 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
947 1437 65 None -2 38 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
CHEMBL59 1437 65 None -2 38 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
DB00988 1437 65 None -2 38 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
71151588 117755 0 None -70 10 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cells
ChEMBL 518 9 1 7 3.6 NC(=O)c1ccccc1OCCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2014.12.045
CHEMBL3409256 117755 0 None -70 10 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cells
ChEMBL 518 9 1 7 3.6 NC(=O)c1ccccc1OCCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2014.12.045
25071385 158611 0 None -3 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C=O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4098236 158611 0 None -3 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C=O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
133079 3581 33 None -1 4 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 10.1021/jm960084f
980 3581 33 None -1 4 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 10.1021/jm960084f
CHEMBL69759 3581 33 None -1 4 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 10.1021/jm960084f
2563 3694 55 None 1 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 383 6 0 6 1.4 O=C1N(CCCCN2CCN(CC2)c2ncccn2)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1016/s0960-894x(01)00167-6
55 3694 55 None 1 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 383 6 0 6 1.4 O=C1N(CCCCN2CCN(CC2)c2ncccn2)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1016/s0960-894x(01)00167-6
91273 3694 55 None 1 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 383 6 0 6 1.4 O=C1N(CCCCN2CCN(CC2)c2ncccn2)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1016/s0960-894x(01)00167-6
CHEMBL274047 3694 55 None 1 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 383 6 0 6 1.4 O=C1N(CCCCN2CCN(CC2)c2ncccn2)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1016/s0960-894x(01)00167-6
DB12833 3694 55 None 1 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 383 6 0 6 1.4 O=C1N(CCCCN2CCN(CC2)c2ncccn2)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1016/s0960-894x(01)00167-6
53361302 63519 0 None 4 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 493 13 0 8 4.4 CCCCn1cc(CCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
CHEMBL1803049 63519 0 None 4 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 493 13 0 8 4.4 CCCCn1cc(CCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
53361302 63519 0 None 4 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 493 13 0 8 4.4 CCCCn1cc(CCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2009919
CHEMBL1803049 63519 0 None 4 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 493 13 0 8 4.4 CCCCn1cc(CCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2009919
1353 1880 85 None -3 85 Human 8.1 pKi = 8.1 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049612a
3559 1880 85 None -3 85 Human 8.1 pKi = 8.1 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049612a
86 1880 85 None -3 85 Human 8.1 pKi = 8.1 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049612a
CHEMBL54 1880 85 None -3 85 Human 8.1 pKi = 8.1 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049612a
DB00502 1880 85 None -3 85 Human 8.1 pKi = 8.1 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049612a
1353 1880 85 None -3 85 Human 8.1 pKi = 8.1 Binding
Binding affinity for human recombinant dopamine receptor D4.2Binding affinity for human recombinant dopamine receptor D4.2
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049720x
3559 1880 85 None -3 85 Human 8.1 pKi = 8.1 Binding
Binding affinity for human recombinant dopamine receptor D4.2Binding affinity for human recombinant dopamine receptor D4.2
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049720x
86 1880 85 None -3 85 Human 8.1 pKi = 8.1 Binding
Binding affinity for human recombinant dopamine receptor D4.2Binding affinity for human recombinant dopamine receptor D4.2
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049720x
CHEMBL54 1880 85 None -3 85 Human 8.1 pKi = 8.1 Binding
Binding affinity for human recombinant dopamine receptor D4.2Binding affinity for human recombinant dopamine receptor D4.2
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049720x
DB00502 1880 85 None -3 85 Human 8.1 pKi = 8.1 Binding
Binding affinity for human recombinant dopamine receptor D4.2Binding affinity for human recombinant dopamine receptor D4.2
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049720x
1353 1880 85 None -3 85 Human 8.1 pKi = 8.1 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960637m
3559 1880 85 None -3 85 Human 8.1 pKi = 8.1 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960637m
86 1880 85 None -3 85 Human 8.1 pKi = 8.1 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960637m
CHEMBL54 1880 85 None -3 85 Human 8.1 pKi = 8.1 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960637m
DB00502 1880 85 None -3 85 Human 8.1 pKi = 8.1 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960637m
10905940 44947 0 None -3 4 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 421 7 1 4 3.9 COc1cccc(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1021/jm020952a
CHEMBL152576 44947 0 None -3 4 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 421 7 1 4 3.9 COc1cccc(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1021/jm020952a
56926586 68667 0 None 316 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 344 3 1 5 2.6 Oc1cc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)ccc1F 10.1021/jm200762g
CHEMBL1923415 68667 0 None 316 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 344 3 1 5 2.6 Oc1cc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)ccc1F 10.1021/jm200762g
44339953 109212 0 None 3 4 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 5 2 4 3.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C[C@@H]1C 10.1016/s0960-894x(03)00678-4
CHEMBL322802 109212 0 None 3 4 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 5 2 4 3.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C[C@@H]1C 10.1016/s0960-894x(03)00678-4
72164181 91715 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 274 3 1 4 2.8 Oc1ccccc1N1CCN(Cc2cccs2)CC1 10.1016/j.bmcl.2013.07.033
CHEMBL2420774 91715 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 274 3 1 4 2.8 Oc1ccccc1N1CCN(Cc2cccs2)CC1 10.1016/j.bmcl.2013.07.033
127027905 138926 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 327 5 0 3 4.3 Cc1ccc(CN2CCO[C@H](CSc3ccccc3)C2)cc1C 10.1016/j.bmcl.2016.03.102
CHEMBL3794079 138926 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 327 5 0 3 4.3 Cc1ccc(CN2CCO[C@H](CSc3ccccc3)C2)cc1C 10.1016/j.bmcl.2016.03.102
3069135 69821 2 None 3 6 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 314 6 0 3 3.4 Fc1ccc(OCCCN2CCN(c3ccccc3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940412 69821 2 None 3 6 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 314 6 0 3 3.4 Fc1ccc(OCCCN2CCN(c3ccccc3)CC2)cc1 10.1016/j.bmc.2011.12.019
10687362 106125 0 None 288 2 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 323 2 0 3 3.8 Cc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(F)cc1)CC3 10.1021/jm970170v
CHEMBL314285 106125 0 None 288 2 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 323 2 0 3 3.8 Cc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(F)cc1)CC3 10.1021/jm970170v
10570898 204769 0 None - 1 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 366 4 0 6 3.3 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc([N+](=O)[O-])cc1)CC3 10.1021/jm970170v
CHEMBL88296 204769 0 None - 1 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 366 4 0 6 3.3 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc([N+](=O)[O-])cc1)CC3 10.1021/jm970170v
10833953 30909 0 None 1445 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 384 3 1 3 4.7 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)cc2c1 10.1021/jm0009989
CHEMBL140006 30909 0 None 1445 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 384 3 1 3 4.7 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)cc2c1 10.1021/jm0009989
11811640 164714 0 None 6 4 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 408 8 1 6 3.2 COc1cccc(C(=O)NCCCCN2CCN(c3noc4ccccc34)CC2)c1 10.1021/jm020952a
CHEMBL423040 164714 0 None 6 4 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 408 8 1 6 3.2 COc1cccc(C(=O)NCCCCN2CCN(c3noc4ccccc34)CC2)c1 10.1021/jm020952a
44395741 180999 0 None 1 10 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1021/jm100899z
CHEMBL476935 180999 0 None 1 10 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1021/jm100899z
CHEMBL558392 180999 0 None 1 10 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1021/jm100899z
44372009 48575 0 None 109 4 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 402 4 0 4 5.0 Clc1ccc(N2CCN(Cc3cnn4c(-c5ccccc5)cccc34)CC2)cc1 10.1016/s0960-894x(01)00814-9
CHEMBL155913 48575 0 None 109 4 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 402 4 0 4 5.0 Clc1ccc(N2CCN(Cc3cnn4c(-c5ccccc5)cccc34)CC2)cc1 10.1016/s0960-894x(01)00814-9
10593191 188519 0 None 33 3 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2ccc(C)cc2)CC1 10.1021/jm970021c
CHEMBL51023 188519 0 None 33 3 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2ccc(C)cc2)CC1 10.1021/jm970021c
10593191 188519 0 None 33 3 Human 8.1 pKi = 8.1 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2ccc(C)cc2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL51023 188519 0 None 33 3 Human 8.1 pKi = 8.1 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2ccc(C)cc2)CC1 10.1016/j.bmcl.2005.02.012
2402 3318 58 None -2 25 Human 8.1 pKi = 8.1 Binding
Binding affinity to human dopamine D4 receptorBinding affinity to human dopamine D4 receptor
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1039/C4MD00066H
5095 3318 58 None -2 25 Human 8.1 pKi = 8.1 Binding
Binding affinity to human dopamine D4 receptorBinding affinity to human dopamine D4 receptor
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1039/C4MD00066H
7295 3318 58 None -2 25 Human 8.1 pKi = 8.1 Binding
Binding affinity to human dopamine D4 receptorBinding affinity to human dopamine D4 receptor
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1039/C4MD00066H
CHEMBL589 3318 58 None -2 25 Human 8.1 pKi = 8.1 Binding
Binding affinity to human dopamine D4 receptorBinding affinity to human dopamine D4 receptor
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1039/C4MD00066H
DB00268 3318 58 None -2 25 Human 8.1 pKi = 8.1 Binding
Binding affinity to human dopamine D4 receptorBinding affinity to human dopamine D4 receptor
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1039/C4MD00066H
9798466 133755 1 None 1 6 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 349 4 1 3 3.3 Cc1ccc(N2CCN(CC[C@@H]3NC(=O)c4ccccc43)CC2)cc1C 10.1021/jm0002432
CHEMBL37170 133755 1 None 1 6 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 349 4 1 3 3.3 Cc1ccc(N2CCN(CC[C@@H]3NC(=O)c4ccccc43)CC2)cc1C 10.1021/jm0002432
57401819 69817 0 None 10 7 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 346 6 0 2 4.6 Fc1ccc(CCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940408 69817 0 None 10 7 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 346 6 0 2 4.6 Fc1ccc(CCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
57401819 69817 0 None 10 7 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 346 6 0 2 4.6 Fc1ccc(CCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940408 69817 0 None 10 7 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 346 6 0 2 4.6 Fc1ccc(CCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2011.12.019
137657115 159208 0 None -3 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(/C=N/O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4105030 159208 0 None -3 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(/C=N/O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
9798466 133755 1 None 1 6 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 349 4 1 3 3.3 Cc1ccc(N2CCN(CC[C@@H]3NC(=O)c4ccccc43)CC2)cc1C 10.1016/s0960-894x(98)00252-2
CHEMBL37170 133755 1 None 1 6 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 349 4 1 3 3.3 Cc1ccc(N2CCN(CC[C@@H]3NC(=O)c4ccccc43)CC2)cc1C 10.1016/s0960-894x(98)00252-2
10568805 168601 0 None 74 2 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 335 4 0 4 3.4 COc1ccc2c3c(c(=O)oc2c1)CN(CCc1ccccc1)CC3 10.1021/jm970170v
CHEMBL440506 168601 0 None 74 2 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 335 4 0 4 3.4 COc1ccc2c3c(c(=O)oc2c1)CN(CCc1ccccc1)CC3 10.1021/jm970170v
164620912 185153 0 None -1 6 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 341 4 1 4 2.6 OC1c2ccc(F)cc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL4866053 185153 0 None -1 6 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 341 4 1 4 2.6 OC1c2ccc(F)cc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
137640371 156273 0 None -5 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccc2c(C=O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4071185 156273 0 None -5 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccc2c(C=O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
1353 1880 85 None -3 85 Human 8.1 pKi = 8.1 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm1013693
3559 1880 85 None -3 85 Human 8.1 pKi = 8.1 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm1013693
86 1880 85 None -3 85 Human 8.1 pKi = 8.1 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm1013693
CHEMBL54 1880 85 None -3 85 Human 8.1 pKi = 8.1 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm1013693
DB00502 1880 85 None -3 85 Human 8.1 pKi = 8.1 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm1013693
44273908 76363 0 None 100 2 Human 8.1 pKi = 8.1 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 363 5 1 3 3.5 CC1(C(=O)NCCN2CCN(c3ccc(Cl)cc3)CC2)CCCCC1 10.1016/0960-894X(96)00198-9
CHEMBL20655 76363 0 None 100 2 Human 8.1 pKi = 8.1 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 363 5 1 3 3.5 CC1(C(=O)NCCN2CCN(c3ccc(Cl)cc3)CC2)CCCCC1 10.1016/0960-894X(96)00198-9
44273887 76698 0 None 316 2 Human 8.1 pKi = 8.1 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 351 7 1 3 3.4 CCCC(C)(C)C(=O)NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL20725 76698 0 None 316 2 Human 8.1 pKi = 8.1 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 351 7 1 3 3.4 CCCC(C)(C)C(=O)NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
10359736 99053 0 None 316 2 Human 8.1 pKi = 8.1 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 337 6 1 3 3.0 CCC(C)(C)C(=O)NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL283353 99053 0 None 316 2 Human 8.1 pKi = 8.1 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 337 6 1 3 3.0 CCC(C)(C)C(=O)NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
44394675 165819 0 None 53 2 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 384 6 1 3 4.2 O=Cc1ccc(-c2ccc(C(=O)NC3CCN(Cc4ccccc4)C3)cc2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL427522 165819 0 None 53 2 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 384 6 1 3 4.2 O=Cc1ccc(-c2ccc(C(=O)NC3CCN(Cc4ccccc4)C3)cc2)cc1 10.1016/j.bmcl.2004.07.045
135398737 944 89 None -13 91 Human 7.2 pKi = 7.2 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960637m
38 944 89 None -13 91 Human 7.2 pKi = 7.2 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960637m
722 944 89 None -13 91 Human 7.2 pKi = 7.2 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960637m
CHEMBL42 944 89 None -13 91 Human 7.2 pKi = 7.2 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960637m
DB00363 944 89 None -13 91 Human 7.2 pKi = 7.2 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960637m
57391897 68967 0 None -7 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 481 12 1 8 2.7 CCOCCOc1ccn2ncc(C(=O)NCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
CHEMBL1928133 68967 0 None -7 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 481 12 1 8 2.7 CCOCCOc1ccn2ncc(C(=O)NCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
45270021 193494 0 None 60 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 335 3 0 5 3.0 Cc1cc2nc(C)c(CN3CCN(c4ccccc4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
CHEMBL550392 193494 0 None 60 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 335 3 0 5 3.0 Cc1cc2nc(C)c(CN3CCN(c4ccccc4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
11382447 109178 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 347 6 0 4 3.6 COc1ccc(Cl)cc1OCC1CN(Cc2ccccc2)CCO1 10.1021/jm031111m
CHEMBL322519 109178 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 347 6 0 4 3.6 COc1ccc(Cl)cc1OCC1CN(Cc2ccccc2)CCO1 10.1021/jm031111m
60149678 114019 0 None 229 2 Human 7.2 pKi = 7.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 321 5 1 3 3.4 c1ccc(CC[C@@H]2CN(Cc3nc4ccccc4[nH]3)CCO2)cc1 10.1021/ml500267c
CHEMBL3335537 114019 0 None 229 2 Human 7.2 pKi = 7.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 321 5 1 3 3.4 c1ccc(CC[C@@H]2CN(Cc3nc4ccccc4[nH]3)CCO2)cc1 10.1021/ml500267c
57267 1563 11 None -416 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 340 6 2 4 2.8 CCN1CCC[C@H]1CNC(=O)c1c(O)c(CC)cc(c1OC)Cl 10.1021/acs.jmedchem.6b01373
966 1563 11 None -416 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 340 6 2 4 2.8 CCN1CCC[C@H]1CNC(=O)c1c(O)c(CC)cc(c1OC)Cl 10.1021/acs.jmedchem.6b01373
CHEMBL8946 1563 11 None -416 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 340 6 2 4 2.8 CCN1CCC[C@H]1CNC(=O)c1c(O)c(CC)cc(c1OC)Cl 10.1021/acs.jmedchem.6b01373
DB15492 1563 11 None -416 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 340 6 2 4 2.8 CCN1CCC[C@H]1CNC(=O)c1c(O)c(CC)cc(c1OC)Cl 10.1021/acs.jmedchem.6b01373
9865858 162754 0 None -44 8 Human 7.2 pKi = 7.2 Binding
The compound was tested for binding affinity against Dopamine receptor D4The compound was tested for binding affinity against Dopamine receptor D4
ChEMBL 402 6 1 5 4.0 COc1ccccc1N1CCC(CNCC2COc3ccc(Cl)cc3O2)CC1 10.1021/jm9910122
CHEMBL418854 162754 0 None -44 8 Human 7.2 pKi = 7.2 Binding
The compound was tested for binding affinity against Dopamine receptor D4The compound was tested for binding affinity against Dopamine receptor D4
ChEMBL 402 6 1 5 4.0 COc1ccccc1N1CCC(CNCC2COc3ccc(Cl)cc3O2)CC1 10.1021/jm9910122
49798879 10511 4 None -275 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 414 4 2 3 4.4 COc1ccc2[nH]cc(CN3CCC(O)(c4ccc(Br)cc4)CC3)c2c1 10.1016/j.bmc.2010.05.052
CHEMBL1170096 10511 4 None -275 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 414 4 2 3 4.4 COc1ccc2[nH]cc(CN3CCC(O)(c4ccc(Br)cc4)CC3)c2c1 10.1016/j.bmc.2010.05.052
44319369 204105 0 None 2 4 Human 6.2 pKi = 6.2 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 335 4 0 4 3.0 C[C@@H]1OC(c2ccccc2)=N[C@H]1CN1CCN(c2ccccc2)CC1 10.1016/s0960-894x(01)00484-x
CHEMBL83306 204105 0 None 2 4 Human 6.2 pKi = 6.2 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 335 4 0 4 3.0 C[C@@H]1OC(c2ccccc2)=N[C@H]1CN1CCN(c2ccccc2)CC1 10.1016/s0960-894x(01)00484-x
44380716 58778 0 None 1 4 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 429 7 1 4 3.6 COc1cc(N(C)C(C)=O)c(Cl)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL169631 58778 0 None 1 4 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 429 7 1 4 3.6 COc1cc(N(C)C(C)=O)c(Cl)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
44324980 205688 0 None -1318 3 Human 5.2 pKi = 5.2 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 249 2 1 4 1.9 CCCN1COC[C@@H]2c3cc(O)ccc3OC[C@H]21 10.1021/jm960345l
CHEMBL94015 205688 0 None -1318 3 Human 5.2 pKi = 5.2 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 249 2 1 4 1.9 CCCN1COC[C@@H]2c3cc(O)ccc3OC[C@H]21 10.1021/jm960345l
10310103 106828 0 None -1778 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 425 5 0 5 5.3 N#CCCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ncccn4)cc23)CC1 10.1021/jm020938y
CHEMBL317333 106828 0 None -1778 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 425 5 0 5 5.3 N#CCCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ncccn4)cc23)CC1 10.1021/jm020938y
9865920 107047 0 None -1 2 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 403 4 0 3 3.7 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccc(Cl)cc21 10.1016/s0960-894x(02)00655-8
CHEMBL318739 107047 0 None -1 2 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 403 4 0 3 3.7 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccc(Cl)cc21 10.1016/s0960-894x(02)00655-8
9887092 102201 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 397 5 0 3 4.1 CCN1C(=O)C(CC)(N2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/s0960-894x(00)00421-2
CHEMBL304584 102201 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 397 5 0 3 4.1 CCN1C(=O)C(CC)(N2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/s0960-894x(00)00421-2
71658338 89979 0 None -97 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 410 9 2 5 3.5 CNc1ccc(C(=O)NCCCCN2CCCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2013.03.074
CHEMBL2386623 89979 0 None -97 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 410 9 2 5 3.5 CNc1ccc(C(=O)NCCCCN2CCCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2013.03.074
10569690 205344 10 None 3 3 Human 7.2 pKi = 7.2 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 347 4 1 4 4.4 Cc1nc(O)n(C2CCN(Cc3ccccc3)CC2)c1-c1ccccc1 10.1021/jm991029k
CHEMBL91821 205344 10 None 3 3 Human 7.2 pKi = 7.2 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 347 4 1 4 4.4 Cc1nc(O)n(C2CCN(Cc3ccccc3)CC2)c1-c1ccccc1 10.1021/jm991029k
73346042 91402 3 None -707 17 Human 7.2 pKi = 7.2 Binding
Binding affinity to dopamine 4 receptor (unknown origin)Binding affinity to dopamine 4 receptor (unknown origin)
ChEMBL 405 9 0 8 0.9 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3OCCF)CC2)c1=O 10.1016/j.bmc.2013.05.050
CHEMBL2413153 91402 3 None -707 17 Human 7.2 pKi = 7.2 Binding
Binding affinity to dopamine 4 receptor (unknown origin)Binding affinity to dopamine 4 receptor (unknown origin)
ChEMBL 405 9 0 8 0.9 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3OCCF)CC2)c1=O 10.1016/j.bmc.2013.05.050
135398737 944 89 None -13 91 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00025a013
38 944 89 None -13 91 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00025a013
722 944 89 None -13 91 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00025a013
CHEMBL42 944 89 None -13 91 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00025a013
DB00363 944 89 None -13 91 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00025a013
56649648 67513 0 None -213 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 474 8 0 5 3.0 COc1ccccc1N1CCN(CCN(C(=O)C23C4C5C2C2C3C4C52CF)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
CHEMBL1910139 67513 0 None -213 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 474 8 0 5 3.0 COc1ccccc1N1CCN(CCN(C(=O)C23C4C5C2C2C3C4C52CF)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
44426499 141533 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 372 6 1 2 4.7 O=C(NC1CCN(CCCc2ccccc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.096
CHEMBL387951 141533 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 372 6 1 2 4.7 O=C(NC1CCN(CCCc2ccccc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.096
11451703 138489 0 None 2 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 376 6 0 5 3.4 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(F)c(Cl)c1 10.1021/jm060279f
CHEMBL378576 138489 0 None 2 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 376 6 0 5 3.4 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(F)c(Cl)c1 10.1021/jm060279f
12050195 201593 0 None 1 4 Human 6.2 pKi = 6.2 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 441 6 0 5 4.4 COc1ccc(Br)cc1-c1nc(CN2CCN(Cc3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL64696 201593 0 None 1 4 Human 6.2 pKi = 6.2 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 441 6 0 5 4.4 COc1ccc(Br)cc1-c1nc(CN2CCN(Cc3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
130431287 170651 0 None -223 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 469 9 1 5 5.0 CCc1cc(Cl)c(OC)c(N2CCN(CCCCNC(=O)c3cc4ccccc4o3)CC2)c1 10.1021/acs.jmedchem.6b00860
CHEMBL4459533 170651 0 None -223 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 469 9 1 5 5.0 CCc1cc(Cl)c(OC)c(N2CCN(CCCCNC(=O)c3cc4ccccc4o3)CC2)c1 10.1021/acs.jmedchem.6b00860
44315403 203760 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 327 3 1 4 2.9 Clc1ccccc1N1CCN(Cc2nc3ccc[nH]c-3n2)CC1 10.1021/jm0305669
CHEMBL80469 203760 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 327 3 1 4 2.9 Clc1ccccc1N1CCN(Cc2nc3ccc[nH]c-3n2)CC1 10.1021/jm0305669
44278456 99424 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 373 7 0 2 5.8 CC(COc1cccc2ccccc12)CN1CCC(Cc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
CHEMBL28596 99424 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 373 7 0 2 5.8 CC(COc1cccc2ccccc12)CN1CCC(Cc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
122205438 136875 0 None -47 5 Human 7.1 pKi = 7.1 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 307 0 0 2 4.5 CN1CCc2ccccc2Cc2sc3ccccc3c2CC1 10.1039/C5MD00258C
CHEMBL3753266 136875 0 None -47 5 Human 7.1 pKi = 7.1 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 307 0 0 2 4.5 CN1CCc2ccccc2Cc2sc3ccccc3c2CC1 10.1039/C5MD00258C
11121216 29925 0 None -36 14 Human 7.1 pKi = 7.1 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
ChEMBL 335 1 1 2 3.0 C[C@@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
CHEMBL138989 29925 0 None -36 14 Human 7.1 pKi = 7.1 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
ChEMBL 335 1 1 2 3.0 C[C@@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
128054 203431 5 None -39 3 Human 7.1 pKi = 7.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 315 6 1 3 4.3 CCCN(CCc1ccsc1)C1CCc2c(O)cccc2C1 10.1021/jm960345l
CHEMBL7806 203431 5 None -39 3 Human 7.1 pKi = 7.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 315 6 1 3 4.3 CCCN(CCc1ccsc1)C1CCc2c(O)cccc2C1 10.1021/jm960345l
127032085 138858 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 363 5 0 5 3.3 FC1(F)Oc2ccc(CN3CCO[C@H](COc4ccccc4)C3)cc2O1 10.1016/j.bmcl.2016.03.102
CHEMBL3793266 138858 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 363 5 0 5 3.3 FC1(F)Oc2ccc(CN3CCO[C@H](COc4ccccc4)C3)cc2O1 10.1016/j.bmcl.2016.03.102
10247720 12943 0 None 2 5 Human 7.1 pKi = 7.1 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL1190042 12943 0 None 2 5 Human 7.1 pKi = 7.1 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL540039 12943 0 None 2 5 Human 7.1 pKi = 7.1 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
135398737 944 89 None -13 91 Human 7.1 pKi = 7.1 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/S0960-894X(97)00194-7
38 944 89 None -13 91 Human 7.1 pKi = 7.1 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/S0960-894X(97)00194-7
722 944 89 None -13 91 Human 7.1 pKi = 7.1 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/S0960-894X(97)00194-7
CHEMBL42 944 89 None -13 91 Human 7.1 pKi = 7.1 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/S0960-894X(97)00194-7
DB00363 944 89 None -13 91 Human 7.1 pKi = 7.1 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/S0960-894X(97)00194-7
49798853 14194 0 None -1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 363 3 1 4 4.4 O=c1[nH]c2ccccc2n1C1CCN(Cc2csc3ccccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1169895 14194 0 None -1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 363 3 1 4 4.4 O=c1[nH]c2ccccc2n1C1CCN(Cc2csc3ccccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1199932 14194 0 None -1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 363 3 1 4 4.4 O=c1[nH]c2ccccc2n1C1CCN(Cc2csc3ccccc23)CC1 10.1016/j.bmc.2010.05.052
10254390 71344 0 None -5623 8 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 475 8 1 5 5.1 COc1cccc2cc(C(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)oc12 10.1021/jm020952a
CHEMBL196476 71344 0 None -5623 8 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 475 8 1 5 5.1 COc1cccc2cc(C(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)oc12 10.1021/jm020952a
10961938 119034 0 None -1202 8 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 485 8 1 4 5.5 COc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc2ccccc12 10.1021/jm020952a
CHEMBL345820 119034 0 None -1202 8 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 485 8 1 4 5.5 COc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc2ccccc12 10.1021/jm020952a
145993377 166415 0 None -269 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 430 8 2 4 4.6 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(-c3ccccc3)cc1)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4287471 166415 0 None -269 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 430 8 2 4 4.6 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(-c3ccccc3)cc1)CC2 10.1021/acsmedchemlett.8b00229
11071135 206268 0 None -3311 8 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 500 6 0 6 4.6 CN1CCC(CCN2CCC(c3cn(-c4ccc(F)cc4)c4ccc(-c5ncn(C)n5)cc34)CC2)C1=O 10.1021/jm020938y
CHEMBL97333 206268 0 None -3311 8 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 500 6 0 6 4.6 CN1CCC(CCN2CCC(c3cn(-c4ccc(F)cc4)c4ccc(-c5ncn(C)n5)cc34)CC2)C1=O 10.1021/jm020938y
137646281 157264 0 None -1659 17 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 423 8 0 7 3.8 COc1ccccc1N1CCN(CCCSc2nnc(-c3ccccc3)n2C)CC1 10.1021/acs.jmedchem.9b00412
CHEMBL4083252 157264 0 None -1659 17 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 423 8 0 7 3.8 COc1ccccc1N1CCN(CCCSc2nnc(-c3ccccc3)n2C)CC1 10.1021/acs.jmedchem.9b00412
44336003 5547 0 None 8 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 389 4 0 3 3.6 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCCC2CCCCC21 10.1016/s0960-894x(02)00655-8
CHEMBL107755 5547 0 None 8 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 389 4 0 3 3.6 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCCC2CCCCC21 10.1016/s0960-894x(02)00655-8
44336100 109288 0 None -1 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 423 4 0 3 4.5 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1c2ccccc2[C@H]2CCCC[C@H]21 10.1016/s0960-894x(02)00655-8
CHEMBL323213 109288 0 None -1 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 423 4 0 3 4.5 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1c2ccccc2[C@H]2CCCC[C@H]21 10.1016/s0960-894x(02)00655-8
30743524 4826 0 None 8 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 5 0 3 3.4 O=C(CCN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccccc21 10.1016/s0960-894x(02)00655-8
CHEMBL104498 4826 0 None 8 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 5 0 3 3.4 O=C(CCN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccccc21 10.1016/s0960-894x(02)00655-8
44336031 5141 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 382 4 0 2 4.6 CC1Cc2ccccc2N1C(=O)CN1CCC(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL106170 5141 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 382 4 0 2 4.6 CC1Cc2ccccc2N1C(=O)CN1CCC(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
71657946 89965 0 None -398 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 407 9 1 4 4.1 C=Cc1ccc(C(=O)NCCCCN2CCCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2013.03.074
CHEMBL2386609 89965 0 None -398 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 407 9 1 4 4.1 C=Cc1ccc(C(=O)NCCCCN2CCCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2013.03.074
10559624 26184 2 None -512 3 Human 6.1 pKi = 6.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 191 1 1 2 1.8 CN(C)C1CCc2ccc(O)cc2C1 10.1021/jm960345l
CHEMBL135932 26184 2 None -512 3 Human 6.1 pKi = 6.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 191 1 1 2 1.8 CN(C)C1CCc2ccc(O)cc2C1 10.1021/jm960345l
10494689 11462 1 None -3 5 Human 7.1 pKi = 7.1 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 303 4 2 3 3.5 Oc1cc2c(cc1Cl)CC[C@@H](CNCc1ccccc1)O2 10.1021/jm9703653
CHEMBL1180589 11462 1 None -3 5 Human 7.1 pKi = 7.1 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 303 4 2 3 3.5 Oc1cc2c(cc1Cl)CC[C@@H](CNCc1ccccc1)O2 10.1021/jm9703653
CHEMBL134343 11462 1 None -3 5 Human 7.1 pKi = 7.1 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 303 4 2 3 3.5 Oc1cc2c(cc1Cl)CC[C@@H](CNCc1ccccc1)O2 10.1021/jm9703653
10495881 108701 0 None 3 3 Human 7.1 pKi = 7.1 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 319 4 1 4 2.8 c1ccc(-c2nc(CN3CCN(c4cccnc4)CC3)c[nH]2)cc1 10.1021/jm960637m
CHEMBL321513 108701 0 None 3 3 Human 7.1 pKi = 7.1 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 319 4 1 4 2.8 c1ccc(-c2nc(CN3CCN(c4cccnc4)CC3)c[nH]2)cc1 10.1021/jm960637m
30616772 4720 0 None 112 2 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 371 5 0 5 3.1 O=c1oc2ccccc2n1CCN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104063 4720 0 None 112 2 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 371 5 0 5 3.1 O=c1oc2ccccc2n1CCN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
127028183 138786 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 366 6 0 5 3.2 COc1ccc(CN2CCO[C@H](COc3cccc(F)n3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3792532 138786 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 366 6 0 5 3.2 COc1ccc(CN2CCO[C@H](COc3cccc(F)n3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
9886609 164777 0 None -6 3 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards human recombinant Dopamine receptor D4 expressed in CHO-K1 cells was determined using [3H]spiperone as radioligandIn vitro binding affinity towards human recombinant Dopamine receptor D4 expressed in CHO-K1 cells was determined using [3H]spiperone as radioligand
ChEMBL 388 5 1 3 5.0 c1ccc(N2CCN(CC[C@H]3CC[C@H](c4c[nH]c5ccccc54)CC3)CC2)nc1 10.1021/jm960597m
CHEMBL423499 164777 0 None -6 3 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards human recombinant Dopamine receptor D4 expressed in CHO-K1 cells was determined using [3H]spiperone as radioligandIn vitro binding affinity towards human recombinant Dopamine receptor D4 expressed in CHO-K1 cells was determined using [3H]spiperone as radioligand
ChEMBL 388 5 1 3 5.0 c1ccc(N2CCN(CC[C@H]3CC[C@H](c4c[nH]c5ccccc54)CC3)CC2)nc1 10.1021/jm960597m
127027238 138881 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 318 5 0 4 3.0 Clc1ccc(CN2CCO[C@H](COc3ccccn3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793709 138881 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 318 5 0 4 3.0 Clc1ccc(CN2CCO[C@H](COc3ccccn3)C2)cc1 10.1016/j.bmcl.2016.03.102
44264641 203094 1 None 4 3 Human 5.1 pKi = 5.1 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 230 2 0 4 1.1 CN1CCN(Cc2cnn3ccccc23)CC1 10.1016/s0960-894x(98)00692-1
CHEMBL7505 203094 1 None 4 3 Human 5.1 pKi = 5.1 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 230 2 0 4 1.1 CN1CCN(Cc2cnn3ccccc23)CC1 10.1016/s0960-894x(98)00692-1
12581219 25058 2 None -4 3 Human 6.1 pKi = 6.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 205 2 0 2 2.1 COc1cccc2c1CCC(N(C)C)C2 10.1021/jm960345l
CHEMBL134866 25058 2 None -4 3 Human 6.1 pKi = 6.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 205 2 0 2 2.1 COc1cccc2c1CCC(N(C)C)C2 10.1021/jm960345l
CHEMBL4560038 212258 0 None - 1 Human 6.1 pKi = 6.1 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000587a DRD4Selectivity interaction (GPCR panel (PDSP screen)) EUB0000587a DRD4
ChEMBL None None None CCNC(=O)c1cc2c(N3CCOC[C@H]3C)ccnc2n1C nan
10567839 205305 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 322 3 0 5 2.8 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccncc1)CC3 10.1021/jm970170v
CHEMBL91585 205305 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 322 3 0 5 2.8 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccncc1)CC3 10.1021/jm970170v
44278853 105317 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 405 8 1 4 4.5 COc1ccc(CC2CCN(CC(O)COc3cccc4ccccc34)CC2)cc1 10.1016/S0960-894X(97)00233-3
CHEMBL31269 105317 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 405 8 1 4 4.5 COc1ccc(CC2CCN(CC(O)COc3cccc4ccccc34)CC2)cc1 10.1016/S0960-894X(97)00233-3
10636896 18696 1 None -3 2 Human 7.1 pKi = 7.1 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 285 9 1 3 3.4 Cc1ccccc1OCCNCCCOc1ccccc1 10.1021/jm970422s
CHEMBL128313 18696 1 None -3 2 Human 7.1 pKi = 7.1 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 285 9 1 3 3.4 Cc1ccccc1OCCNCCCOc1ccccc1 10.1021/jm970422s
10688157 15405 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 3 0 4 3.4 Cc1cccc(N2CCN(Cc3ccc4oc(=O)ccc4c3)CC2)c1 10.1021/jm990266k
CHEMBL122116 15405 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 3 0 4 3.4 Cc1cccc(N2CCN(Cc3ccc4oc(=O)ccc4c3)CC2)c1 10.1021/jm990266k
10636896 18696 1 None -3 2 Human 7.1 pKi = 7.1 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 285 9 1 3 3.4 Cc1ccccc1OCCNCCCOc1ccccc1 10.1016/j.bmcl.2005.02.012
CHEMBL128313 18696 1 None -3 2 Human 7.1 pKi = 7.1 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 285 9 1 3 3.4 Cc1ccccc1OCCNCCCOc1ccccc1 10.1016/j.bmcl.2005.02.012
118719925 115279 0 None 7 8 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 330 7 1 3 2.8 O=C1CCc2ccccc2N1CCCN1CCC(CCCO)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL3354072 115279 0 None 7 8 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 330 7 1 3 2.8 O=C1CCc2ccccc2N1CCCN1CCC(CCCO)CC1 10.1021/acs.jmedchem.8b00265
71658077 89972 0 None -56 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 425 10 2 5 3.0 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(CCO)cc2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386616 89972 0 None -56 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 425 10 2 5 3.0 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(CCO)cc2)CC1 10.1016/j.bmc.2013.03.074
9884771 16421 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 350 4 0 5 3.1 COc1ccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)cc1 10.1021/jm990266k
CHEMBL124050 16421 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 350 4 0 5 3.1 COc1ccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)cc1 10.1021/jm990266k
137657427 159012 0 None -67 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 476 7 3 6 3.5 O=C1CCc2ccc(OCCCCN3CCCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4102628 159012 0 None -67 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 476 7 3 6 3.5 O=C1CCc2ccc(OCCCCN3CCCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
11570471 141385 0 None -21 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 568 12 1 7 4.4 CCCc1c(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)nnn1Cc1ccccc1Br 10.1021/jm0611152
CHEMBL386986 141385 0 None -21 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 568 12 1 7 4.4 CCCc1c(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)nnn1Cc1ccccc1Br 10.1021/jm0611152
CHEMBL4579981 212265 8 None - 1 Human 5.1 pKi = 5.1 Binding
Affinity Biochemical interaction (Radioligand binding assay) EUB0000338a DRD4Affinity Biochemical interaction (Radioligand binding assay) EUB0000338a DRD4
ChEMBL None None None Cc1ccc2[nH]c(CNCCCc3ccncc3)cc(=O)c2c1 nan
11092112 205894 0 None -13489 9 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 485 6 0 6 4.9 O=C1OCCN1CCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ncccn4)cc23)CC1 10.1021/jm020938y
CHEMBL95175 205894 0 None -13489 9 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 485 6 0 6 4.9 O=C1OCCN1CCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ncccn4)cc23)CC1 10.1021/jm020938y
46231924 198894 0 None -1737 4 Human 5.1 pKi = 5.1 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 370 2 1 4 4.0 CO/N=C/c1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.094
CHEMBL599134 198894 0 None -1737 4 Human 5.1 pKi = 5.1 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 370 2 1 4 4.0 CO/N=C/c1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.094
118719807 115234 0 None -81 4 Human 6.1 pKi = 6.1 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 434 9 0 7 3.5 COc1ccccc1N1CCN(CCCCc2cn(-c3ccc(N(C)C)cc3)nn2)CC1 10.1016/j.bmcl.2014.12.023
CHEMBL3353910 115234 0 None -81 4 Human 6.1 pKi = 6.1 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 434 9 0 7 3.5 COc1ccccc1N1CCN(CCCCc2cn(-c3ccc(N(C)C)cc3)nn2)CC1 10.1016/j.bmcl.2014.12.023
44403220 71582 0 None -3 5 Human 7.1 pKi = 7.1 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 386 8 1 5 2.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(F)n2)CC1 10.1016/j.bmcl.2005.07.037
CHEMBL197214 71582 0 None -3 5 Human 7.1 pKi = 7.1 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 386 8 1 5 2.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(F)n2)CC1 10.1016/j.bmcl.2005.07.037
10375676 114705 30 None -99 3 Human 7.1 pKi = 7.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 205 3 2 2 2.2 CCCNC1CCc2c(O)cccc2C1 10.1021/jm960345l
CHEMBL334472 114705 30 None -99 3 Human 7.1 pKi = 7.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 205 3 2 2 2.2 CCCNC1CCc2c(O)cccc2C1 10.1021/jm960345l
56597938 3877 1 None -204 9 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
7651 3877 1 None -204 9 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
CHEMBL2165126 3877 1 None -204 9 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
122189394 122733 0 None -245 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 469 7 0 7 4.4 Clc1cccc(N2CCN(CCCCc3cn(-c4ccn5nccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.07.050
CHEMBL3613880 122733 0 None -245 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 469 7 0 7 4.4 Clc1cccc(N2CCN(CCCCc3cn(-c4ccn5nccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.07.050
22727361 13146 0 None -4 3 Human 7.1 pKi = 7.1 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 421 9 0 6 4.5 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)c(OC)c1 10.1016/s0960-894x(02)00179-8
CHEMBL1191469 13146 0 None -4 3 Human 7.1 pKi = 7.1 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 421 9 0 6 4.5 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)c(OC)c1 10.1016/s0960-894x(02)00179-8
CHEMBL542573 13146 0 None -4 3 Human 7.1 pKi = 7.1 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 421 9 0 6 4.5 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)c(OC)c1 10.1016/s0960-894x(02)00179-8
155530763 171003 0 None 9 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 323 5 1 3 3.6 Cc1cccc(NC(=O)CCN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4464861 171003 0 None 9 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 323 5 1 3 3.6 Cc1cccc(NC(=O)CCN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
137655594 158094 0 None -18 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 287 3 2 4 1.8 CCCN1CCN(c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmc.2017.08.037
CHEMBL4092462 158094 0 None -18 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 287 3 2 4 1.8 CCCN1CCN(c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmc.2017.08.037
142590721 179694 0 None -6 3 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 486 9 1 3 5.2 [O-][S+](CCNC1CCN(Cc2ccc(F)cc2)CC1)C(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.ejmech.2020.112674
CHEMBL4750660 179694 0 None -6 3 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 486 9 1 3 5.2 [O-][S+](CCNC1CCN(Cc2ccc(F)cc2)CC1)C(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.ejmech.2020.112674
44431474 87055 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.5 Cc1cccc(CN2CCC(NC(=O)c3cccc4ccccc34)CC2)c1 10.1016/j.bmcl.2006.12.106
CHEMBL233404 87055 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.5 Cc1cccc(CN2CCC(NC(=O)c3cccc4ccccc34)CC2)c1 10.1016/j.bmcl.2006.12.106
57393628 68971 0 None -229 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1005 30 2 17 5.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cnn3ccc(OCCOCCOCCOCCOc4ccn5ncc(C(=O)NCCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928137 68971 0 None -229 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1005 30 2 17 5.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cnn3ccc(OCCOCCOCCOCCOc4ccn5ncc(C(=O)NCCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
440229 87083 48 None -14 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human dopamine D4 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]SCH23390 from human dopamine D4 receptor expressed in HEK293 cells after 1 hr
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)[C@@H]1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmcl.2017.01.090
CHEMBL2334891 87083 48 None -14 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human dopamine D4 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]SCH23390 from human dopamine D4 receptor expressed in HEK293 cells after 1 hr
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)[C@@H]1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmcl.2017.01.090
10895106 32011 0 None -1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 421 9 1 6 3.1 COc1ccccc1N1CCN(CCCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm0611152
CHEMBL140968 32011 0 None -1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 421 9 1 6 3.1 COc1ccccc1N1CCN(CCCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm0611152
44335979 5035 0 None 8 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 Cc1ccc2c(c1)N(C(=O)CN1CCN(Cc3ccc(Cl)cc3)CC1)CC2 10.1016/s0960-894x(02)00655-8
CHEMBL105595 5035 0 None 8 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 Cc1ccc2c(c1)N(C(=O)CN1CCN(Cc3ccc(Cl)cc3)CC1)CC2 10.1016/s0960-894x(02)00655-8
127052458 140209 0 None -77 7 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 5 1 3 3.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(O)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818056 140209 0 None -77 7 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 5 1 3 3.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(O)cc1 10.1016/j.bmc.2016.05.053
22727322 13825 0 None -32 3 Human 6.1 pKi = 6.1 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 421 9 0 6 4.5 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
CHEMBL1196566 13825 0 None -32 3 Human 6.1 pKi = 6.1 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 421 9 0 6 4.5 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
CHEMBL557409 13825 0 None -32 3 Human 6.1 pKi = 6.1 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 421 9 0 6 4.5 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
154706030 175971 1 None -37 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4580817 175971 1 None -37 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4597188 175971 1 None -37 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
127052458 140209 0 None -77 7 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 5 1 3 3.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(O)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818056 140209 0 None -77 7 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 5 1 3 3.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(O)cc1 10.1016/j.bmc.2016.05.053
44340376 110157 0 None 6 4 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 452 6 1 3 4.9 COc1c(C(=O)NC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL325818 110157 0 None 6 4 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 452 6 1 3 4.9 COc1c(C(=O)NC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
10895106 32011 0 None -1 5 Human 7.1 pKi = 7.1 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 421 9 1 6 3.1 COc1ccccc1N1CCN(CCCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
CHEMBL140968 32011 0 None -1 5 Human 7.1 pKi = 7.1 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 421 9 1 6 3.1 COc1ccccc1N1CCN(CCCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
72164182 91718 0 None -1 5 Human 7.1 pKi = 7.1 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 326 3 0 3 4.4 Clc1ccc(N2CCN(Cc3cccs3)CC2)cc1Cl 10.1016/j.bmcl.2013.07.033
CHEMBL2420777 91718 0 None -1 5 Human 7.1 pKi = 7.1 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 326 3 0 3 4.4 Clc1ccc(N2CCN(Cc3cccs3)CC2)cc1Cl 10.1016/j.bmcl.2013.07.033
25072946 111292 0 None -12 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2c(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cccc12 10.1021/jm5004039
CHEMBL3287400 111292 0 None -12 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2c(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cccc12 10.1021/jm5004039
44405530 140781 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 446 6 1 4 5.3 O=C(N[C@H]1CCN(Cc2ccc(OC(F)(F)F)cc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
CHEMBL383383 140781 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 446 6 1 4 5.3 O=C(N[C@H]1CCN(Cc2ccc(OC(F)(F)F)cc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
56837419 68962 0 None -338 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 997 35 2 14 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928128 68962 0 None -338 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 997 35 2 14 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
15888352 123594 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 369 4 0 3 3.7 CN1C(=O)c2ccccc2C1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(98)00252-2
CHEMBL36337 123594 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 369 4 0 3 3.7 CN1C(=O)c2ccccc2C1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(98)00252-2
90644066 111548 0 None 17 4 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 354 5 0 3 4.8 Clc1ccc(N2CCN(CCCc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289653 111548 0 None 17 4 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 354 5 0 3 4.8 Clc1ccc(N2CCN(CCCc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
5280343 187691 119 None 1 32 Human 5.1 pKi = 5.1 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/np1000329
CHEMBL1520590 187691 119 None 1 32 Human 5.1 pKi = 5.1 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/np1000329
CHEMBL50 187691 119 None 1 32 Human 5.1 pKi = 5.1 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/np1000329
44591086 188990 0 None -61 3 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 367 3 2 3 4.2 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1c[nH]c2ncccc12 10.1016/j.bmc.2008.12.054
CHEMBL514590 188990 0 None -61 3 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 367 3 2 3 4.2 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1c[nH]c2ncccc12 10.1016/j.bmc.2008.12.054
44395709 174326 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 373 4 1 3 4.2 O=C(CN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
CHEMBL456429 174326 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 373 4 1 3 4.2 O=C(CN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
CHEMBL556361 174326 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 373 4 1 3 4.2 O=C(CN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
44395709 174326 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 373 4 1 3 4.2 O=C(CN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.12.054
CHEMBL456429 174326 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 373 4 1 3 4.2 O=C(CN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.12.054
CHEMBL556361 174326 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 373 4 1 3 4.2 O=C(CN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.12.054
44436302 90203 0 None -1 4 Human 7.1 pKi = 7.1 Binding
Binding affinity to human D4RBinding affinity to human D4R
ChEMBL 429 7 0 6 2.4 COc1ccccc1N1CCN(CCCCN2C(=O)c3ccccc3S2(=O)=O)CC1 10.1016/j.bmcl.2021.128028
CHEMBL238917 90203 0 None -1 4 Human 7.1 pKi = 7.1 Binding
Binding affinity to human D4RBinding affinity to human D4R
ChEMBL 429 7 0 6 2.4 COc1ccccc1N1CCN(CCCCN2C(=O)c3ccccc3S2(=O)=O)CC1 10.1016/j.bmcl.2021.128028
44273896 99015 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 351 6 1 3 3.4 CC(C)(C)C(=O)NCCCCN1CCN(c2ccccc2Cl)CC1 10.1016/0960-894X(96)00198-9
CHEMBL283142 99015 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 351 6 1 3 3.4 CC(C)(C)C(=O)NCCCCN1CCN(c2ccccc2Cl)CC1 10.1016/0960-894X(96)00198-9
9888211 21216 9 None -100 10 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 417 6 1 3 4.5 O=C1c2ccccc2C(=O)N1CCCCN1CC=C(c2c[nH]c3ccc(F)cc23)CC1 10.1021/jm070516u
CHEMBL131495 21216 9 None -100 10 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 417 6 1 3 4.5 O=C1c2ccccc2C(=O)N1CCCCN1CC=C(c2c[nH]c3ccc(F)cc23)CC1 10.1021/jm070516u
11347425 203409 3 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 310 3 1 3 3.0 Fc1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)cc1 10.1021/jm0305669
CHEMBL77850 203409 3 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 310 3 1 3 3.0 Fc1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)cc1 10.1021/jm0305669
12997412 9102 0 None -1 3 Human 6.1 pKi = 6.1 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 411 6 1 3 4.2 O=C(NCCCN1CCN(c2ccccc2)CC1)c1cccc2c1Cc1ccccc1-2 10.1021/jm010146o
CHEMBL110349 9102 0 None -1 3 Human 6.1 pKi = 6.1 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 411 6 1 3 4.2 O=C(NCCCN1CCN(c2ccccc2)CC1)c1cccc2c1Cc1ccccc1-2 10.1021/jm010146o
11168182 3478 18 None -125 13 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpirideBinding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpiride
ChEMBL 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 10.1016/j.bmcl.2005.06.024
264 3478 18 None -125 13 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpirideBinding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpiride
ChEMBL 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 10.1016/j.bmcl.2005.06.024
CHEMBL1181770 3478 18 None -125 13 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpirideBinding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpiride
ChEMBL 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 10.1016/j.bmcl.2005.06.024
57326584 73717 0 None -8 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 396 1 0 5 4.9 Clc1ccc2c(c1)N=C(N1CCN(C3CCCCC3)CC1)c1cccnc1O2 10.1021/jm2013419
CHEMBL2022273 73717 0 None -8 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 396 1 0 5 4.9 Clc1ccc2c(c1)N=C(N1CCN(C3CCCCC3)CC1)c1cccnc1O2 10.1021/jm2013419
44394618 65860 0 None 15 2 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 374 5 1 2 4.5 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL184388 65860 0 None 15 2 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 374 5 1 2 4.5 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2004.07.045
44335918 5068 0 None 61 2 Human 8.1 pKi = 8.1 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 407 5 0 5 2.2 COC(=O)[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(C)cc2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL105745 5068 0 None 61 2 Human 8.1 pKi = 8.1 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 407 5 0 5 2.2 COC(=O)[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(C)cc2)CC1 10.1016/s0960-894x(02)00656-x
233952 198017 14 None 15 3 Human 8.1 pKi = 8.1 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 291 3 1 2 3.5 c1ccc(N2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1021/jm9600712
CHEMBL59324 198017 14 None 15 3 Human 8.1 pKi = 8.1 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 291 3 1 2 3.5 c1ccc(N2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1021/jm9600712
44335876 4987 0 None 15 2 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 377 4 0 3 3.4 Cc1ccc(C)c(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)c1 10.1016/s0960-894x(02)00655-8
CHEMBL105304 4987 0 None 15 2 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 377 4 0 3 3.4 Cc1ccc(C)c(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)c1 10.1016/s0960-894x(02)00655-8
44336314 109153 0 None 204 2 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 369 5 0 3 3.0 O=C1Cc2ccccc2N1CCN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL322326 109153 0 None 204 2 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 369 5 0 3 3.0 O=C1Cc2ccccc2N1CCN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
233952 198017 14 None 15 3 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 291 3 1 2 3.5 c1ccc(N2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1021/jm0002432
CHEMBL59324 198017 14 None 15 3 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 291 3 1 2 3.5 c1ccc(N2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1021/jm0002432
11739255 79608 0 None 8 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 338 6 0 5 3.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(C)c1 10.1021/jm060279f
CHEMBL212861 79608 0 None 8 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 338 6 0 5 3.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(C)c1 10.1021/jm060279f
10425450 199 23 None -1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/jm060662k
3301 199 23 None -1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/jm060662k
CHEMBL375596 199 23 None -1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/jm060662k
15840856 99368 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 358 5 0 3 4.7 COc1ccccc1N1CCN(Cc2cccc(-c3ccccc3)c2)CC1 10.1016/S0960-894X(97)00218-7
CHEMBL285577 99368 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 358 5 0 3 4.7 COc1ccccc1N1CCN(Cc2cccc(-c3ccccc3)c2)CC1 10.1016/S0960-894X(97)00218-7
44436596 91564 0 None 3 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 401 5 1 3 3.5 C#Cc1ccc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.bmc.2007.08.038
CHEMBL241631 91564 0 None 3 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 401 5 1 3 3.5 C#Cc1ccc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.bmc.2007.08.038
10359736 99053 0 None 316 2 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.
ChEMBL 337 6 1 3 3.0 CCC(C)(C)C(=O)NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm981041x
CHEMBL283353 99053 0 None 316 2 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.
ChEMBL 337 6 1 3 3.0 CCC(C)(C)C(=O)NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm981041x
137655735 158446 0 None -11 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 436 8 2 8 2.7 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(/C=N\O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4096353 158446 0 None -11 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 436 8 2 8 2.7 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(/C=N\O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
22100943 102660 0 None 41 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 340 3 0 3 5.2 Clc1cccc(CN2CC=C(c3nc4ccccc4s3)CC2)c1 10.1016/S0960-894X(97)00402-2
CHEMBL307869 102660 0 None 41 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 340 3 0 3 5.2 Clc1cccc(CN2CC=C(c3nc4ccccc4s3)CC2)c1 10.1016/S0960-894X(97)00402-2
119570 3110 90 None -10 40 Human 8.1 pKi = 8.1 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm0503805
2233 3110 90 None -10 40 Human 8.1 pKi = 8.1 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm0503805
953 3110 90 None -10 40 Human 8.1 pKi = 8.1 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm0503805
CHEMBL301265 3110 90 None -10 40 Human 8.1 pKi = 8.1 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm0503805
DB00413 3110 90 None -10 40 Human 8.1 pKi = 8.1 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm0503805
119570 3110 90 None -10 40 Human 8.1 pKi = 8.1 Binding
High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsHigh inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
2233 3110 90 None -10 40 Human 8.1 pKi = 8.1 Binding
High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsHigh inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
953 3110 90 None -10 40 Human 8.1 pKi = 8.1 Binding
High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsHigh inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
CHEMBL301265 3110 90 None -10 40 Human 8.1 pKi = 8.1 Binding
High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsHigh inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
DB00413 3110 90 None -10 40 Human 8.1 pKi = 8.1 Binding
High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsHigh inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
91864602 140207 0 None -7 8 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 313 5 0 2 4.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818047 140207 0 None -7 8 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 313 5 0 2 4.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.05.053
10318141 205361 0 None 120 3 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 389 3 0 4 4.4 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(C(F)(F)F)cc1)CC3 10.1021/jm970170v
CHEMBL91938 205361 0 None 120 3 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 389 3 0 4 4.4 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(C(F)(F)F)cc1)CC3 10.1021/jm970170v
12888943 9478 0 None 2 4 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.8 CNc1cc(OC)c(C(=O)NC2CCN(Cc3ccccc3)CC2)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL112395 9478 0 None 2 4 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.8 CNc1cc(OC)c(C(=O)NC2CCN(Cc3ccccc3)CC2)cc1Cl 10.1016/s0960-894x(03)00678-4
137640189 156411 0 None -10 6 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 466 7 3 7 2.6 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCC(=O)N5)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4072780 156411 0 None -10 6 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 466 7 3 7 2.6 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCC(=O)N5)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
10737474 100883 0 None 10 3 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 363 4 1 3 3.5 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL296953 100883 0 None 10 3 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 363 4 1 3 3.5 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2005.02.012
53363199 63521 0 None 10 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 481 12 0 9 3.2 CCOCCn1cc(COc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
CHEMBL1803051 63521 0 None 10 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 481 12 0 9 3.2 CCOCCn1cc(COc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
22100957 202563 4 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 358 3 0 3 5.4 Clc1ccc(CN2CC=C(c3nc4cc(Cl)ccc4o3)CC2)cc1 10.1016/S0960-894X(97)00402-2
CHEMBL71208 202563 4 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 358 3 0 3 5.4 Clc1ccc(CN2CC=C(c3nc4cc(Cl)ccc4o3)CC2)cc1 10.1016/S0960-894X(97)00402-2
10620139 205047 0 None - 1 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 385 4 0 5 4.0 COc1cc2oc(=O)c3c(c2cc1OC)CCN(Cc1ccc(Cl)cc1)C3 10.1021/jm970170v
CHEMBL90173 205047 0 None - 1 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 385 4 0 5 4.0 COc1cc2oc(=O)c3c(c2cc1OC)CCN(Cc1ccc(Cl)cc1)C3 10.1021/jm970170v
9945233 203383 1 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm0305669
CHEMBL77563 203383 1 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm0305669
119570 3110 90 None -10 40 Human 8.1 pKi = 8.1 Binding
Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 8.5/130)Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 8.5/130)
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
2233 3110 90 None -10 40 Human 8.1 pKi = 8.1 Binding
Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 8.5/130)Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 8.5/130)
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
953 3110 90 None -10 40 Human 8.1 pKi = 8.1 Binding
Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 8.5/130)Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 8.5/130)
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
CHEMBL301265 3110 90 None -10 40 Human 8.1 pKi = 8.1 Binding
Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 8.5/130)Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 8.5/130)
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
DB00413 3110 90 None -10 40 Human 8.1 pKi = 8.1 Binding
Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 8.5/130)Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 8.5/130)
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
2812861 206699 5 None 177 3 Human 8.1 pKi = 8.1 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 319 4 1 4 2.8 c1ccc(-c2nc(CN3CCN(c4ccccn4)CC3)c[nH]2)cc1 10.1021/jm960637m
CHEMBL99967 206699 5 None 177 3 Human 8.1 pKi = 8.1 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 319 4 1 4 2.8 c1ccc(-c2nc(CN3CCN(c4ccccn4)CC3)c[nH]2)cc1 10.1021/jm960637m
10324985 76428 7 None -6 17 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
CHEMBL199824 76428 7 None -6 17 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
CHEMBL2068762 76428 7 None -6 17 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
2389 3279 114 None -21 67 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmc.2008.06.030
5073 3279 114 None -21 67 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmc.2008.06.030
96 3279 114 None -21 67 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmc.2008.06.030
CHEMBL85 3279 114 None -21 67 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmc.2008.06.030
DB00734 3279 114 None -21 67 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmc.2008.06.030
2 3210 19 None -2 28 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm5004039
54562 3210 19 None -2 28 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm5004039
CHEMBL240773 3210 19 None -2 28 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm5004039
2 3210 19 None -2 28 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2016.04.028
54562 3210 19 None -2 28 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2016.04.028
CHEMBL240773 3210 19 None -2 28 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2016.04.028
2 3210 19 None -2 28 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm400520c
54562 3210 19 None -2 28 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm400520c
CHEMBL240773 3210 19 None -2 28 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm400520c
2 3210 19 None -2 28 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm501889t
54562 3210 19 None -2 28 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm501889t
CHEMBL240773 3210 19 None -2 28 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm501889t
44284013 138700 0 None - 1 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 394 6 2 4 3.7 OCc1ccc(N2CCN(CC[C@H](O)c3ccc(Cl)cc3)CC2)cc1Cl 10.1016/s0960-894x(98)00252-2
CHEMBL37885 138700 0 None - 1 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 394 6 2 4 3.7 OCc1ccc(N2CCN(CC[C@H](O)c3ccc(Cl)cc3)CC2)cc1Cl 10.1016/s0960-894x(98)00252-2
10450880 205435 0 None 316 2 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 355 3 0 4 4.0 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(Cl)cc1)CC3 10.1021/jm970170v
CHEMBL92373 205435 0 None 316 2 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 355 3 0 4 4.0 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(Cl)cc1)CC3 10.1021/jm970170v
10685891 11492 1 None -7 5 Human 8.1 pKi = 8.1 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 303 4 2 3 3.5 Oc1cc2c(cc1Cl)CC[C@H](CNCc1ccccc1)O2 10.1021/jm9703653
CHEMBL1180627 11492 1 None -7 5 Human 8.1 pKi = 8.1 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 303 4 2 3 3.5 Oc1cc2c(cc1Cl)CC[C@H](CNCc1ccccc1)O2 10.1021/jm9703653
CHEMBL135357 11492 1 None -7 5 Human 8.1 pKi = 8.1 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 303 4 2 3 3.5 Oc1cc2c(cc1Cl)CC[C@H](CNCc1ccccc1)O2 10.1021/jm9703653
3645619 2985 13 None -4 9 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm970021c
975 2985 13 None -4 9 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm970021c
CHEMBL45244 2985 13 None -4 9 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm970021c
57401820 69818 0 None 6 7 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 364 6 0 3 4.8 Fc1ccc(SCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940409 69818 0 None 6 7 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 364 6 0 3 4.8 Fc1ccc(SCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
57401820 69818 0 None 6 7 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 364 6 0 3 4.8 Fc1ccc(SCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940409 69818 0 None 6 7 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 364 6 0 3 4.8 Fc1ccc(SCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2011.12.019
118709175 112924 0 None -4 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 474 10 0 5 4.9 CN(C)CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318848 112924 0 None -4 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 474 10 0 5 4.9 CN(C)CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
3645619 2985 13 None -4 9 Human 8.1 pKi = 8.1 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/j.bmcl.2005.02.012
975 2985 13 None -4 9 Human 8.1 pKi = 8.1 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/j.bmcl.2005.02.012
CHEMBL45244 2985 13 None -4 9 Human 8.1 pKi = 8.1 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/j.bmcl.2005.02.012
44323780 112083 0 None 20 4 Human 8.1 pKi = 8.1 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 341 3 1 3 3.2 O=C1Cc2c(ccc(Cl)c2N2CCN(Cc3ccccc3)CC2)N1 10.1016/s0960-894x(98)00474-0
CHEMBL330108 112083 0 None 20 4 Human 8.1 pKi = 8.1 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 341 3 1 3 3.2 O=C1Cc2c(ccc(Cl)c2N2CCN(Cc3ccccc3)CC2)N1 10.1016/s0960-894x(98)00474-0
44323780 112083 0 None 20 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 341 3 1 3 3.2 O=C1Cc2c(ccc(Cl)c2N2CCN(Cc3ccccc3)CC2)N1 10.1007/s00044-012-0055-5
CHEMBL330108 112083 0 None 20 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 341 3 1 3 3.2 O=C1Cc2c(ccc(Cl)c2N2CCN(Cc3ccccc3)CC2)N1 10.1007/s00044-012-0055-5
44222483 194577 0 None -2 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 409 7 1 6 3.0 CSc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm900690y
CHEMBL561763 194577 0 None -2 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 409 7 1 6 3.0 CSc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm900690y
9819770 140554 6 None 208 3 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 349 4 1 3 3.3 Cc1ccc(N2CCN(CCC3NC(=O)c4ccccc43)CC2)cc1C 10.1016/s0960-894x(98)00252-2
CHEMBL38262 140554 6 None 208 3 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 349 4 1 3 3.3 Cc1ccc(N2CCN(CCC3NC(=O)c4ccccc43)CC2)cc1C 10.1016/s0960-894x(98)00252-2
137653577 158327 0 None 208 3 Human 8.1 pKi = 8.1 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 349 4 1 3 3.6 Cc1ccc(N2CCN(CCC3C(=O)Nc4ccccc43)CC2)cc1C 10.1021/acs.jmedchem.7b00151
CHEMBL4095082 158327 0 None 208 3 Human 8.1 pKi = 8.1 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 349 4 1 3 3.6 Cc1ccc(N2CCN(CCC3C(=O)Nc4ccccc43)CC2)cc1C 10.1021/acs.jmedchem.7b00151
44360992 118899 0 None 2 6 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc3ccnn23)CC1 10.1021/jm025558r
CHEMBL344677 118899 0 None 2 6 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc3ccnn23)CC1 10.1021/jm025558r
228 441 26 None -1 24 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
33 441 26 None -1 24 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
6005 441 26 None -1 24 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
CHEMBL53 441 26 None -1 24 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
DB00714 441 26 None -1 24 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
13091359 113040 0 None -12 10 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
CHEMBL3321790 113040 0 None -12 10 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
681 1437 65 None -2 38 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.01.065
940 1437 65 None -2 38 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.01.065
947 1437 65 None -2 38 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.01.065
CHEMBL59 1437 65 None -2 38 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.01.065
DB00988 1437 65 None -2 38 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.01.065
44360992 118899 0 None 2 6 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc3ccnn23)CC1 10.1021/jm0611152
CHEMBL344677 118899 0 None 2 6 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc3ccnn23)CC1 10.1021/jm0611152
11776546 201545 1 None -7 6 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 243 6 2 3 2.6 Oc1cccc(OCCNCc2ccccc2)c1 10.1016/s0960-894x(98)00014-6
CHEMBL64508 201545 1 None -7 6 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 243 6 2 3 2.6 Oc1cccc(OCCNCc2ccccc2)c1 10.1016/s0960-894x(98)00014-6
11776546 201545 1 None -7 6 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 243 6 2 3 2.6 Oc1cccc(OCCNCc2ccccc2)c1 10.1016/s0960-894x(99)00434-5
CHEMBL64508 201545 1 None -7 6 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 243 6 2 3 2.6 Oc1cccc(OCCNCc2ccccc2)c1 10.1016/s0960-894x(99)00434-5
10392655 198581 0 None -389 5 Human 6.1 pKi = 6.1 Binding
Binding affinity for human dopamine receptor D4 using [125I]IABN as radioligandBinding affinity for human dopamine receptor D4 using [125I]IABN as radioligand
ChEMBL 543 9 1 5 5.1 COc1cc(Br)cc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1OC 10.1016/j.bmcl.2003.09.083
CHEMBL59713 198581 0 None -389 5 Human 6.1 pKi = 6.1 Binding
Binding affinity for human dopamine receptor D4 using [125I]IABN as radioligandBinding affinity for human dopamine receptor D4 using [125I]IABN as radioligand
ChEMBL 543 9 1 5 5.1 COc1cc(Br)cc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1OC 10.1016/j.bmcl.2003.09.083
10392655 198581 0 None -389 5 Human 6.1 pKi = 6.1 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by radioligand binding assayBinding affinity to dopamine D4 receptor (unknown origin) by radioligand binding assay
ChEMBL 543 9 1 5 5.1 COc1cc(Br)cc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1OC 10.1021/jm301545c
CHEMBL59713 198581 0 None -389 5 Human 6.1 pKi = 6.1 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by radioligand binding assayBinding affinity to dopamine D4 receptor (unknown origin) by radioligand binding assay
ChEMBL 543 9 1 5 5.1 COc1cc(Br)cc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1OC 10.1021/jm301545c
72205046 91515 0 None -8 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 394 7 0 4 4.7 Clc1ccc(-n2cc(CCCCN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2013.05.027
CHEMBL2414357 91515 0 None -8 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 394 7 0 4 4.7 Clc1ccc(-n2cc(CCCCN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2013.05.027
122177643 120698 0 None -501 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 632 20 3 9 5.1 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)CCc3ccc(O)c4[nH]c(=O)ccc34)cc2OC)nn1 10.1021/jm501889t
CHEMBL3577344 120698 0 None -501 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 632 20 3 9 5.1 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)CCc3ccc(O)c4[nH]c(=O)ccc34)cc2OC)nn1 10.1021/jm501889t
11452692 58604 0 None -338 4 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 413 10 1 4 3.5 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(CCF)cc2)CC1 10.1021/jm101323b
CHEMBL1688991 58604 0 None -338 4 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 413 10 1 4 3.5 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(CCF)cc2)CC1 10.1021/jm101323b
11452692 58604 0 None -338 4 Human 6.1 pKi = 6.1 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 413 10 1 4 3.5 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(CCF)cc2)CC1 10.1016/j.bmcl.2014.12.023
CHEMBL1688991 58604 0 None -338 4 Human 6.1 pKi = 6.1 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 413 10 1 4 3.5 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(CCF)cc2)CC1 10.1016/j.bmcl.2014.12.023
155512662 169088 2 None -1621 3 Human 6.1 pKi = 6.1 Binding
Displacement of 2,3-dimethoxy-5-[125I]-iodo-N-[9-benzyl-9-azabicyclo[3.3.1]nonan-3beta-yl]benzamide from dopamine human D4 receptor expressed in HEK293 cells measured after 60 mins by gamma counting analysisDisplacement of 2,3-dimethoxy-5-[125I]-iodo-N-[9-benzyl-9-azabicyclo[3.3.1]nonan-3beta-yl]benzamide from dopamine human D4 receptor expressed in HEK293 cells measured after 60 mins by gamma counting analysis
ChEMBL 444 8 1 5 4.6 N#Cc1cccc(N2CCN(CCCCNC(=O)c3ccc(-c4ccsc4)cc3)CC2)c1 10.1016/j.bmcl.2019.07.020
CHEMBL4437341 169088 2 None -1621 3 Human 6.1 pKi = 6.1 Binding
Displacement of 2,3-dimethoxy-5-[125I]-iodo-N-[9-benzyl-9-azabicyclo[3.3.1]nonan-3beta-yl]benzamide from dopamine human D4 receptor expressed in HEK293 cells measured after 60 mins by gamma counting analysisDisplacement of 2,3-dimethoxy-5-[125I]-iodo-N-[9-benzyl-9-azabicyclo[3.3.1]nonan-3beta-yl]benzamide from dopamine human D4 receptor expressed in HEK293 cells measured after 60 mins by gamma counting analysis
ChEMBL 444 8 1 5 4.6 N#Cc1cccc(N2CCN(CCCCNC(=O)c3ccc(-c4ccsc4)cc3)CC2)c1 10.1016/j.bmcl.2019.07.020
71456890 81415 0 None -50 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 436 6 0 4 4.7 O=C(c1ccc2ccccc2c1)N(CCN1CCN(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL2164351 81415 0 None -50 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 436 6 0 4 4.7 O=C(c1ccc2ccccc2c1)N(CCN1CCN(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
44415689 138579 0 None -912 6 Human 6.1 pKi = 6.1 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 494 2 2 6 4.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3c(N)cccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL378669 138579 0 None -912 6 Human 6.1 pKi = 6.1 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 494 2 2 6 4.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3c(N)cccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
44336004 5361 0 None 23 2 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 439 4 0 3 5.1 Cc1ccc2c(c1)N(C(=O)CN1CCN(Cc3ccc(Cl)cc3)CC1)C(C)(C)CC2C 10.1016/s0960-894x(02)00655-8
CHEMBL107338 5361 0 None 23 2 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 439 4 0 3 5.1 Cc1ccc2c(c1)N(C(=O)CN1CCN(Cc3ccc(Cl)cc3)CC1)C(C)(C)CC2C 10.1016/s0960-894x(02)00655-8
242 467 117 None -117 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
34 467 117 None -117 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
60795 467 117 None -117 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
CHEMBL1112 467 117 None -117 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
DB01238 467 117 None -117 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
242 467 117 None -117 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
34 467 117 None -117 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
60795 467 117 None -117 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
CHEMBL1112 467 117 None -117 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
DB01238 467 117 None -117 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
72737767 114022 4 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 315 5 0 2 4.2 Clc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
CHEMBL3335540 114022 4 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 315 5 0 2 4.2 Clc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
134144304 153956 0 None 1 9 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 327 5 0 2 4.4 O=C(CCCN1CCc2ccccc2CC1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.09.019
CHEMBL3952251 153956 0 None 1 9 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 327 5 0 2 4.4 O=C(CCCN1CCc2ccccc2CC1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.09.019
CHEMBL3990525 153956 0 None 1 9 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 327 5 0 2 4.4 O=C(CCCN1CCc2ccccc2CC1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.09.019
44283963 139657 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 394 6 2 4 3.7 OCc1ccc(N2CCN(CC[C@@H](O)c3ccc(Cl)cc3)CC2)cc1Cl 10.1016/s0960-894x(98)00252-2
CHEMBL38046 139657 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 394 6 2 4 3.7 OCc1ccc(N2CCN(CC[C@@H](O)c3ccc(Cl)cc3)CC2)cc1Cl 10.1016/s0960-894x(98)00252-2
2274 3124 53 None -56 32 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 3124 53 None -56 32 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 3124 53 None -56 32 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 3124 53 None -56 32 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 3124 53 None -56 32 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
154705015 175940 1 None -186 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4454380 175940 1 None -186 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4596929 175940 1 None -186 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
71062829 159587 0 None -1 3 Mouse 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 339 6 0 5 2.2 c1ccc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)nc1 nan
CHEMBL4108986 159587 0 None -1 3 Mouse 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 339 6 0 5 2.2 c1ccc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)nc1 nan
44591043 176238 0 None 3 2 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 326 3 2 2 3.9 OC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2008.12.054
CHEMBL460855 176238 0 None 3 2 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 326 3 2 2 3.9 OC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2008.12.054
130431343 173944 0 None -2454 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 439 8 1 5 3.9 CCc1cccc(N2CCN(CCCCNC(=O)c3cn4ccccc4n3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4555307 173944 0 None -2454 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 439 8 1 5 3.9 CCc1cccc(N2CCN(CCCCNC(=O)c3cn4ccccc4n3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
44454685 94610 0 None 7 5 Human 7.1 pKi = 7.1 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 348 6 0 3 4.0 FCCOc1cccc(CN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2007.12.026
CHEMBL255163 94610 0 None 7 5 Human 7.1 pKi = 7.1 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 348 6 0 3 4.0 FCCOc1cccc(CN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2007.12.026
134144304 153956 0 None 1 9 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 327 5 0 2 4.4 O=C(CCCN1CCc2ccccc2CC1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.09.019
CHEMBL3952251 153956 0 None 1 9 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 327 5 0 2 4.4 O=C(CCCN1CCc2ccccc2CC1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.09.019
CHEMBL3990525 153956 0 None 1 9 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 327 5 0 2 4.4 O=C(CCCN1CCc2ccccc2CC1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.09.019
57391895 68959 0 None -42 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 925 30 2 13 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928125 68959 0 None -42 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 925 30 2 13 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
155513053 169131 0 None 6 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 323 5 1 3 3.5 CCc1cccc(NC(=O)CN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4437912 169131 0 None 6 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 323 5 1 3 3.5 CCc1cccc(NC(=O)CN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
11405107 197385 0 None 7 4 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 341 3 1 2 3.7 C(#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1)c1ccccc1 10.1016/s0960-894x(02)00316-5
CHEMBL58662 197385 0 None 7 4 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 341 3 1 2 3.7 C(#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1)c1ccccc1 10.1016/s0960-894x(02)00316-5
11808247 17891 0 None 1 9 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL126667 17891 0 None 1 9 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819366 17891 0 None 1 9 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
11314005 109045 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 346 5 0 4 3.7 Cc1ncccc1OCC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/jm031111m
CHEMBL322175 109045 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 346 5 0 4 3.7 Cc1ncccc1OCC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/jm031111m
162645252 183043 0 None -1 7 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 389 7 0 3 5.0 Fc1ccc(CCCCN2CCN(c3cccc(-c4ccccc4)n3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4743284 183043 0 None -1 7 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 389 7 0 3 5.0 Fc1ccc(CCCCN2CCN(c3cccc(-c4ccccc4)n3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4802393 183043 0 None -1 7 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 389 7 0 3 5.0 Fc1ccc(CCCCN2CCN(c3cccc(-c4ccccc4)n3)CC2)cc1 10.1016/j.bmc.2020.115943
11808247 17891 0 None 1 9 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL126667 17891 0 None 1 9 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819366 17891 0 None 1 9 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
10961938 119034 0 None -1380 8 Rat 6.1 pKi = 6.1 Binding
Binding affinity for rat dopamine D4 receptor using [11C] radiotracerBinding affinity for rat dopamine D4 receptor using [11C] radiotracer
ChEMBL 485 8 1 4 5.5 COc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc2ccccc12 10.1021/jm050171k
CHEMBL345820 119034 0 None -1380 8 Rat 6.1 pKi = 6.1 Binding
Binding affinity for rat dopamine D4 receptor using [11C] radiotracerBinding affinity for rat dopamine D4 receptor using [11C] radiotracer
ChEMBL 485 8 1 4 5.5 COc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc2ccccc12 10.1021/jm050171k
71658207 89977 0 None -46 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 460 8 1 5 3.6 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(Br)nc2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386621 89977 0 None -46 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 460 8 1 5 3.6 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(Br)nc2)CC1 10.1016/j.bmc.2013.03.074
4209 3114 71 None -1318 33 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm020938y
4893 3114 71 None -1318 33 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm020938y
503 3114 71 None -1318 33 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm020938y
5385 3114 71 None -1318 33 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm020938y
CHEMBL2 3114 71 None -1318 33 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm020938y
DB00457 3114 71 None -1318 33 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm020938y
127052486 140292 0 None -8 8 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 424 6 1 5 4.8 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2nc3ccccc3o2)CC1 10.1016/j.bmc.2016.06.011
CHEMBL3819153 140292 0 None -8 8 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 424 6 1 5 4.8 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2nc3ccccc3o2)CC1 10.1016/j.bmc.2016.06.011
46231926 198895 0 None -41686 4 Human 5.1 pKi = 5.1 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 446 4 1 4 5.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(/C=N/OCc4ccccc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL599135 198895 0 None -41686 4 Human 5.1 pKi = 5.1 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 446 4 1 4 5.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(/C=N/OCc4ccccc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
10689266 205315 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 351 4 0 5 3.4 COc1ccc(CN2CCc3c(c(=O)oc4cc(OC)ccc34)C2)cc1 10.1021/jm970170v
CHEMBL91658 205315 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 351 4 0 5 3.4 COc1ccc(CN2CCc3c(c(=O)oc4cc(OC)ccc34)C2)cc1 10.1021/jm970170v
162645252 183043 0 None -1 7 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 389 7 0 3 5.0 Fc1ccc(CCCCN2CCN(c3cccc(-c4ccccc4)n3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4743284 183043 0 None -1 7 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 389 7 0 3 5.0 Fc1ccc(CCCCN2CCN(c3cccc(-c4ccccc4)n3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4802393 183043 0 None -1 7 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 389 7 0 3 5.0 Fc1ccc(CCCCN2CCN(c3cccc(-c4ccccc4)n3)CC2)cc1 10.1016/j.bmc.2020.115943
56649649 67515 0 None -97 8 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 480 8 0 5 4.6 COc1ccccc1N1CCN(CCN(C(=O)C23CCC(CF)(CC2)CC3)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
CHEMBL1910140 67515 0 None -97 8 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 480 8 0 5 4.6 COc1ccccc1N1CCN(CCN(C(=O)C23CCC(CF)(CC2)CC3)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
44431483 167084 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 412 4 1 2 5.3 O=C(NC1CCN(Cc2ccc(C(F)(F)F)cc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
CHEMBL430167 167084 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 412 4 1 2 5.3 O=C(NC1CCN(Cc2ccc(C(F)(F)F)cc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
137655451 158307 0 None -6 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4094869 158307 0 None -6 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
56833463 67994 0 None -41 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 578 17 1 9 4.4 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2009919
CHEMBL1916552 67994 0 None -41 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 578 17 1 9 4.4 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2009919
11783703 40793 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 375 1 1 5 4.5 Cc1ccc2c(c1)C(N1CCN(C3CCCCC3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL148752 40793 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 375 1 1 5 4.5 Cc1ccc2c(c1)C(N1CCN(C3CCCCC3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
11560697 10510 0 None -363 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 414 4 2 3 4.4 COc1cccc2[nH]cc(CN3CCC(O)(c4ccc(Br)cc4)CC3)c12 10.1016/j.bmc.2010.05.052
CHEMBL1170095 10510 0 None -363 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 414 4 2 3 4.4 COc1cccc2[nH]cc(CN3CCC(O)(c4ccc(Br)cc4)CC3)c12 10.1016/j.bmc.2010.05.052
127052486 140292 0 None -8 8 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 424 6 1 5 4.8 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2nc3ccccc3o2)CC1 10.1016/j.bmc.2016.06.011
CHEMBL3819153 140292 0 None -8 8 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 424 6 1 5 4.8 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2nc3ccccc3o2)CC1 10.1016/j.bmc.2016.06.011
154705128 175717 1 None -58 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 462 12 1 3 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4454872 175717 1 None -58 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 462 12 1 3 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4595148 175717 1 None -58 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 462 12 1 3 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL5079903 212879 0 None -32 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None N#CC(CCN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
154724609 176025 1 None -1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 440 10 0 6 4.8 COc1ccc(F)cc1C1CC1CN(C)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4514800 176025 1 None -1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 440 10 0 6 4.8 COc1ccc(F)cc1C1CC1CN(C)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4597637 176025 1 None -1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 440 10 0 6 4.8 COc1ccc(F)cc1C1CC1CN(C)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
154726922 175967 1 None 1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 12 0 6 5.6 CCCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4442936 175967 1 None 1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 12 0 6 5.6 CCCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4597157 175967 1 None 1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 12 0 6 5.6 CCCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
118709171 112919 0 None -2 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1085 35 0 8 16.8 O=C(CCCCCCCCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318843 112919 0 None -2 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1085 35 0 8 16.8 O=C(CCCCCCCCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
45483655 196438 0 None -12 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 1047 23 2 14 8.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3cn(Cc4ccc(-c5ccc(Cn6cc(-c7ccc(C(=O)NCCCCN8CCN(c9ccccc9OC)CC8)cc7)nn6)cc5)cc4)nn3)cc2)CC1 10.1021/jm901120h
CHEMBL574534 196438 0 None -12 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 1047 23 2 14 8.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3cn(Cc4ccc(-c5ccc(Cn6cc(-c7ccc(C(=O)NCCCCN8CCN(c9ccccc9OC)CC8)cc7)nn6)cc5)cc4)nn3)cc2)CC1 10.1021/jm901120h
11151135 108929 0 None - 1 Human 6.1 pKi = 6.1 Binding
In vitro ability to inhibit binding of [3H]spiperone to human recombinant Dopamine receptor D4.2 expressed on CHO cellsIn vitro ability to inhibit binding of [3H]spiperone to human recombinant Dopamine receptor D4.2 expressed on CHO cells
ChEMBL 313 6 0 4 3.0 COc1ccccc1OCC1CN(Cc2ccccc2)CCO1 10.1021/jm031111m
CHEMBL322002 108929 0 None - 1 Human 6.1 pKi = 6.1 Binding
In vitro ability to inhibit binding of [3H]spiperone to human recombinant Dopamine receptor D4.2 expressed on CHO cellsIn vitro ability to inhibit binding of [3H]spiperone to human recombinant Dopamine receptor D4.2 expressed on CHO cells
ChEMBL 313 6 0 4 3.0 COc1ccccc1OCC1CN(Cc2ccccc2)CCO1 10.1021/jm031111m
154706123 175714 1 None -107 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4593394 175714 1 None -107 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4595145 175714 1 None -107 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
127035062 135928 0 None -29 19 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor after 90 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor after 90 mins by scintillation counting method
ChEMBL 447 12 0 5 5.2 COc1ccc(CCN(CCCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
CHEMBL3735756 135928 0 None -29 19 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor after 90 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor after 90 mins by scintillation counting method
ChEMBL 447 12 0 5 5.2 COc1ccc(CCN(CCCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
91864602 140207 0 None -7 8 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 313 5 0 2 4.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818047 140207 0 None -7 8 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 313 5 0 2 4.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.05.053
168286314 191063 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5196213 191063 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)c1 10.1016/j.bmcl.2022.128615
56681925 66034 0 None -2 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 462 7 1 5 3.5 CN1CN(c2ccccc2)C2(CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)C1=O 10.1016/j.bmc.2011.04.021
CHEMBL1813589 66034 0 None -2 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 462 7 1 5 3.5 CN1CN(c2ccccc2)C2(CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)C1=O 10.1016/j.bmc.2011.04.021
CHEMBL1851628 66034 0 None -2 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 462 7 1 5 3.5 CN1CN(c2ccccc2)C2(CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)C1=O 10.1016/j.bmc.2011.04.021
44338149 109848 0 None -4 3 Human 6.1 pKi = 6.1 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 575 10 0 3 8.2 Fc1ccc(C(OCCN2C3CCC2CC(OC(c2ccc(F)cc2)c2ccc(F)cc2)C3)c2ccc(F)cc2)cc1 10.1021/jm010146o
CHEMBL323997 109848 0 None -4 3 Human 6.1 pKi = 6.1 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 575 10 0 3 8.2 Fc1ccc(C(OCCN2C3CCC2CC(OC(c2ccc(F)cc2)c2ccc(F)cc2)C3)c2ccc(F)cc2)cc1 10.1021/jm010146o
44360984 34855 0 None -7 6 Human 7.1 pKi = 7.1 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cccn3nccc23)CC1 10.1021/jm025558r
CHEMBL143352 34855 0 None -7 6 Human 7.1 pKi = 7.1 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cccn3nccc23)CC1 10.1021/jm025558r
44316315 203808 0 None -5 5 Human 7.1 pKi = 7.1 Binding
Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 87/23000)Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 87/23000)
ChEMBL 215 2 0 3 2.1 CCCN1CCc2nn3ccccc3c2C1 10.1016/s0960-894x(02)00390-6
CHEMBL80845 203808 0 None -5 5 Human 7.1 pKi = 7.1 Binding
Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 87/23000)Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 87/23000)
ChEMBL 215 2 0 3 2.1 CCCN1CCc2nn3ccccc3c2C1 10.1016/s0960-894x(02)00390-6
10623982 205323 0 None 2 3 Human 7.1 pKi = 7.1 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 463 7 2 4 4.6 COc1cc(NC(=O)c2ccccc2)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
CHEMBL91693 205323 0 None 2 3 Human 7.1 pKi = 7.1 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 463 7 2 4 4.6 COc1cc(NC(=O)c2ccccc2)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
22100965 202065 4 None 16 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 340 3 0 3 5.2 Clc1ccccc1CN1CC=C(c2nc3ccccc3s2)CC1 10.1016/S0960-894X(97)00402-2
CHEMBL67982 202065 4 None 16 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 340 3 0 3 5.2 Clc1ccccc1CN1CC=C(c2nc3ccccc3s2)CC1 10.1016/S0960-894X(97)00402-2
44372154 53940 0 None 11 4 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 434 4 0 4 5.4 Cc1nn2c(-c3ccc(F)cc3)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
CHEMBL160749 53940 0 None 11 4 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 434 4 0 4 5.4 Cc1nn2c(-c3ccc(F)cc3)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
44360984 34855 0 None -7 6 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cccn3nccc23)CC1 10.1021/jm0611152
CHEMBL143352 34855 0 None -7 6 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cccn3nccc23)CC1 10.1021/jm0611152
16007117 79626 0 None -870 6 Human 6.1 pKi = 6.1 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 479 2 1 5 5.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL212912 79626 0 None -870 6 Human 6.1 pKi = 6.1 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 479 2 1 5 5.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
137660707 158752 0 None -281 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 463 7 2 7 3.4 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5oc(=O)ccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4099666 158752 0 None -281 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 463 7 2 7 3.4 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5oc(=O)ccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
118719795 115222 0 None -234 4 Human 6.1 pKi = 6.1 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 442 8 0 7 4.0 COc1ccccc1N1CCN(CCCCc2cn(-c3cccc4cnccc34)nn2)CC1 10.1016/j.bmcl.2014.12.023
CHEMBL3353898 115222 0 None -234 4 Human 6.1 pKi = 6.1 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 442 8 0 7 4.0 COc1ccccc1N1CCN(CCCCc2cn(-c3cccc4cnccc34)nn2)CC1 10.1016/j.bmcl.2014.12.023
154725749 176114 1 None -79 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 2 5.8 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4453478 176114 1 None -79 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 2 5.8 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4598388 176114 1 None -79 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 2 5.8 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
11849229 137646 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 349 7 0 6 2.5 N#CCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL376955 137646 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 349 7 0 6 2.5 N#CCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
22727347 12920 0 None -5 3 Human 7.1 pKi = 7.1 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 417 9 0 5 5.0 COc1ccccc1N1CCN(CCCCc2cc(/C=C/c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL1189897 12920 0 None -5 3 Human 7.1 pKi = 7.1 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 417 9 0 5 5.0 COc1ccccc1N1CCN(CCCCc2cc(/C=C/c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL539744 12920 0 None -5 3 Human 7.1 pKi = 7.1 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 417 9 0 5 5.0 COc1ccccc1N1CCN(CCCCc2cc(/C=C/c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
11775107 165663 0 None -26 3 Rat 7.1 pKi = 7.1 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 443 7 1 4 4.5 COc1cccc2c1N1CCN(CCCCNC(=O)c3ccc4ccccc4c3)C[C@@H]1CC2 10.1021/jm049031l
CHEMBL426629 165663 0 None -26 3 Rat 7.1 pKi = 7.1 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 443 7 1 4 4.5 COc1cccc2c1N1CCN(CCCCNC(=O)c3ccc4ccccc4c3)C[C@@H]1CC2 10.1021/jm049031l
863787 65959 13 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 339 5 1 4 2.8 COc1ccc(N2CCN(CC(=O)Nc3cccc(C)c3)CC2)cc1 10.1016/j.bmcl.2004.07.068
CHEMBL184772 65959 13 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 339 5 1 4 2.8 COc1ccc(N2CCN(CC(=O)Nc3cccc(C)c3)CC2)cc1 10.1016/j.bmcl.2004.07.068
164610259 184524 0 None -2 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 480 6 2 4 4.7 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1ccccc1Br)CC2 10.1016/j.bmcl.2021.128047
CHEMBL4856161 184524 0 None -2 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 480 6 2 4 4.7 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1ccccc1Br)CC2 10.1016/j.bmcl.2021.128047
49782841 17470 0 None -549 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 523 7 1 4 6.1 O=C(NCCCCN1CCN(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccccc2s1 10.1021/jm100899z
CHEMBL1258382 17470 0 None -549 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 523 7 1 4 6.1 O=C(NCCCCN1CCN(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccccc2s1 10.1021/jm100899z
137642033 157599 0 None -147 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 291 3 2 5 1.3 CCCN1CCN(c2ccc(O)c3c2OCC(=O)N3)CC1 10.1016/j.bmc.2017.08.037
CHEMBL4087217 157599 0 None -147 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 291 3 2 5 1.3 CCCN1CCN(c2ccc(O)c3c2OCC(=O)N3)CC1 10.1016/j.bmc.2017.08.037
44438237 93226 2 None -47 3 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 424 8 1 3 6.4 CCCCCCn1cc(CN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2006.10.076
CHEMBL246855 93226 2 None -47 3 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 424 8 1 3 6.4 CCCCCCn1cc(CN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2006.10.076
127053222 138839 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 369 5 0 3 4.1 Fc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1C(F)(F)F 10.1016/j.bmcl.2016.03.102
CHEMBL3793072 138839 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 369 5 0 3 4.1 Fc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1C(F)(F)F 10.1016/j.bmcl.2016.03.102
57398352 69819 0 None 6 5 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 398 6 0 3 5.1 Fc1ccc(SCCCN2CCN(c3ccc(C(F)(F)F)cc3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940410 69819 0 None 6 5 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 398 6 0 3 5.1 Fc1ccc(SCCCN2CCN(c3ccc(C(F)(F)F)cc3)CC2)cc1 10.1016/j.bmc.2011.12.019
90644228 111294 0 None -14 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287402 111294 0 None -14 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
118709177 112926 0 None -17 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1135 31 0 14 12.5 O=C(CCc1cn(CCCCCCCCCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318850 112926 0 None -17 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1135 31 0 14 12.5 O=C(CCc1cn(CCCCCCCCCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
135442113 118487 0 None 2 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 417 3 2 5 5.1 Clc1ccc2c(c1)C(NC1CCN(Cc3ccccc3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL342536 118487 0 None 2 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 417 3 2 5 5.1 Clc1ccc2c(c1)C(NC1CCN(Cc3ccccc3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
155533824 171332 0 None -27 6 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 238 2 0 2 2.7 CCc1cccc(N2CCN(C)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4469777 171332 0 None -27 6 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 238 2 0 2 2.7 CCc1cccc(N2CCN(C)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
51353676 59865 0 None -1380 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 442 11 1 5 3.4 CN(C)c1ccc(C(=O)NCCCCN2CCN(c3ccccc3OCCF)CC2)cc1 10.1021/jm101323b
CHEMBL1689002 59865 0 None -1380 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 442 11 1 5 3.4 CN(C)c1ccc(C(=O)NCCCCN2CCN(c3ccccc3OCCF)CC2)cc1 10.1021/jm101323b
CHEMBL1739784 59865 0 None -1380 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 442 11 1 5 3.4 CN(C)c1ccc(C(=O)NCCCCN2CCN(c3ccccc3OCCF)CC2)cc1 10.1021/jm101323b
51353992 59895 0 None -812 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 443 11 1 4 3.7 O=C(NC/C=C/CN1CCN(c2ccccc2OCCF)CC1)c1ccc(CCF)cc1 10.1021/jm101323b
CHEMBL1689009 59895 0 None -812 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 443 11 1 4 3.7 O=C(NC/C=C/CN1CCN(c2ccccc2OCCF)CC1)c1ccc(CCF)cc1 10.1021/jm101323b
CHEMBL1739965 59895 0 None -812 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 443 11 1 4 3.7 O=C(NC/C=C/CN1CCN(c2ccccc2OCCF)CC1)c1ccc(CCF)cc1 10.1021/jm101323b
9980998 30819 0 None -1148 8 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm020952a
CHEMBL139926 30819 0 None -1148 8 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm020952a
CHEMBL2112911 30819 0 None -1148 8 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm020952a
9980998 30819 0 None -1148 8 Human 6.1 pKi = 6.1 Binding
Inhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in Sf9 cellsInhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in Sf9 cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
CHEMBL139926 30819 0 None -1148 8 Human 6.1 pKi = 6.1 Binding
Inhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in Sf9 cellsInhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in Sf9 cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
CHEMBL2112911 30819 0 None -1148 8 Human 6.1 pKi = 6.1 Binding
Inhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in Sf9 cellsInhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in Sf9 cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
53248365 61757 0 None -933 7 Human 6.1 pKi = 6.1 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 554 6 1 5 2.9 O=C(N(CCN1CCN(c2ccccc2O)CC1)c1ccccn1)C12C3C4C1C1C2C3C41I 10.1021/jm1009956
CHEMBL1774995 61757 0 None -933 7 Human 6.1 pKi = 6.1 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 554 6 1 5 2.9 O=C(N(CCN1CCN(c2ccccc2O)CC1)c1ccccn1)C12C3C4C1C1C2C3C41I 10.1021/jm1009956
53326601 58603 0 None -1122 4 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 410 9 1 5 3.1 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(N(C)C)cc2)CC1 10.1021/jm101323b
CHEMBL1688990 58603 0 None -1122 4 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 410 9 1 5 3.1 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(N(C)C)cc2)CC1 10.1021/jm101323b
53326601 58603 0 None -1122 4 Human 6.1 pKi = 6.1 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 410 9 1 5 3.1 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(N(C)C)cc2)CC1 10.1016/j.bmcl.2014.12.023
CHEMBL1688990 58603 0 None -1122 4 Human 6.1 pKi = 6.1 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 410 9 1 5 3.1 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(N(C)C)cc2)CC1 10.1016/j.bmcl.2014.12.023
135398737 944 89 None -7 91 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
38 944 89 None -7 91 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
722 944 89 None -7 91 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
CHEMBL42 944 89 None -7 91 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
DB00363 944 89 None -7 91 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
3645619 2985 13 None -4 9 Human 8.1 pKi = 8.1 Binding
Binding affinity towards cloned human Dopamine receptor D4Binding affinity towards cloned human Dopamine receptor D4
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/s0960-894x(00)00633-8
975 2985 13 None -4 9 Human 8.1 pKi = 8.1 Binding
Binding affinity towards cloned human Dopamine receptor D4Binding affinity towards cloned human Dopamine receptor D4
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/s0960-894x(00)00633-8
CHEMBL45244 2985 13 None -4 9 Human 8.1 pKi = 8.1 Binding
Binding affinity towards cloned human Dopamine receptor D4Binding affinity towards cloned human Dopamine receptor D4
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/s0960-894x(00)00633-8
10950176 44758 1 None -33 4 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 435 8 1 4 4.3 COc1cccc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1021/jm020952a
CHEMBL152391 44758 1 None -33 4 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 435 8 1 4 4.3 COc1cccc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1021/jm020952a
135398737 944 89 None -13 91 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00655-8
38 944 89 None -13 91 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00655-8
722 944 89 None -13 91 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00655-8
CHEMBL42 944 89 None -13 91 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00655-8
DB00363 944 89 None -13 91 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00655-8
155530733 171013 0 None 9 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 477 9 2 5 3.9 COc1ccccc1N1CCN(CCNC(=O)NN(Cc2ccccc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4465002 171013 0 None 9 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 477 9 2 5 3.9 COc1ccccc1N1CCN(CCNC(=O)NN(Cc2ccccc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
10158455 119465 0 None 15 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 409 3 0 3 3.8 CC1Cc2cccc3c2N1C(=O)C(N1CCN(Cc2ccc(Cl)cc2)CC1)CC3 10.1016/s0960-894x(02)01056-9
CHEMBL349833 119465 0 None 15 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 409 3 0 3 3.8 CC1Cc2cccc3c2N1C(=O)C(N1CCN(Cc2ccc(Cl)cc2)CC1)CC3 10.1016/s0960-894x(02)01056-9
10495652 36345 0 None 2 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 316 4 0 2 4.9 c1ccc(C2CCN(Cc3ccn(-c4ccccc4)c3)CC2)cc1 10.1021/jm00025a013
CHEMBL144835 36345 0 None 2 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 316 4 0 2 4.9 c1ccc(C2CCN(Cc3ccn(-c4ccccc4)c3)CC2)cc1 10.1021/jm00025a013
1613 2316 44 None -2 44 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm2013419
205 2316 44 None -2 44 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm2013419
3964 2316 44 None -2 44 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm2013419
CHEMBL831 2316 44 None -2 44 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm2013419
DB00408 2316 44 None -2 44 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm2013419
163091 491 30 None -147 10 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 285 0 0 2 4.3 Clc1ccc2c(c1)[C@H]1CN(C[C@@H]1c1c(O2)cccc1)C 10.1039/C5MD00258C
22 491 30 None -147 10 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 285 0 0 2 4.3 Clc1ccc2c(c1)[C@H]1CN(C[C@@H]1c1c(O2)cccc1)C 10.1039/C5MD00258C
CHEMBL504548 491 30 None -147 10 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 285 0 0 2 4.3 Clc1ccc2c(c1)[C@H]1CN(C[C@@H]1c1c(O2)cccc1)C 10.1039/C5MD00258C
10643780 118890 0 None 97 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 384 3 1 3 4.7 N#Cc1ccc2cc(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)[nH]c2c1 10.1021/jm0009989
CHEMBL344602 118890 0 None 97 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 384 3 1 3 4.7 N#Cc1ccc2cc(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)[nH]c2c1 10.1021/jm0009989
10594113 203202 1 None 13 3 Human 8.0 pKi = 8.0 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 351 4 1 2 5.1 Clc1ccc(-c2cc(C3CCN(Cc4ccccc4)CC3)[nH]n2)cc1 10.1021/jm970111h
CHEMBL76090 203202 1 None 13 3 Human 8.0 pKi = 8.0 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 351 4 1 2 5.1 Clc1ccc(-c2cc(C3CCN(Cc4ccccc4)CC3)[nH]n2)cc1 10.1021/jm970111h
11131951 49651 1 None -363 4 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 353 6 1 4 2.6 COc1cccc(C(=O)NCCN2CCN(c3ccc(C)cc3)CC2)c1 10.1021/jm100925m
CHEMBL156845 49651 1 None -363 4 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 353 6 1 4 2.6 COc1cccc(C(=O)NCCN2CCN(c3ccc(C)cc3)CC2)c1 10.1021/jm100925m
15467369 100461 0 None 562 3 Human 8.0 pKi = 8.0 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 317 4 1 4 2.8 N#CC(C#N)=Cc1ccc(CN2CCN(c3ccccc3)CC2)[nH]1 10.1016/s0960-894x(99)00302-9
CHEMBL293956 100461 0 None 562 3 Human 8.0 pKi = 8.0 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 317 4 1 4 2.8 N#CC(C#N)=Cc1ccc(CN2CCN(c3ccccc3)CC2)[nH]1 10.1016/s0960-894x(99)00302-9
90644230 111298 0 None -4 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 443 7 0 6 4.5 N#Cc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287406 111298 0 None -4 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 443 7 0 6 4.5 N#Cc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
23364995 112921 0 None -2 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 417 7 0 4 5.0 CC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318845 112921 0 None -2 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 417 7 0 4 5.0 CC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
11292776 5510 0 None - 1 Human 8.0 pKi = 8.0 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 409 7 0 4 5.1 CCOc1ccc(Cl)cc1OCC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/jm031111m
CHEMBL107691 5510 0 None - 1 Human 8.0 pKi = 8.0 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 409 7 0 4 5.1 CCOc1ccc(Cl)cc1OCC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/jm031111m
44283757 137337 0 None 128 2 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 348 4 1 2 4.4 Cc1ccc(C2CCN(CCC3NC(=O)c4ccccc43)CC2)cc1C 10.1016/s0960-894x(98)00252-2
CHEMBL37604 137337 0 None 128 2 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 348 4 1 2 4.4 Cc1ccc(C2CCN(CCC3NC(=O)c4ccccc43)CC2)cc1C 10.1016/s0960-894x(98)00252-2
57345617 70113 0 None 1 7 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 387 6 1 2 5.3 OC1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2CCCCc1ccc(F)cc1 10.1016/j.bmc.2012.01.022
CHEMBL1946123 70113 0 None 1 7 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 387 6 1 2 5.3 OC1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2CCCCc1ccc(F)cc1 10.1016/j.bmc.2012.01.022
127028505 138803 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 333 5 0 3 4.3 Clc1ccc(CN2CCO[C@H](CSc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792731 138803 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 333 5 0 3 4.3 Clc1ccc(CN2CCO[C@H](CSc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
76518514 113038 0 None 1 9 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 387 6 1 2 5.3 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCCc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
CHEMBL3321788 113038 0 None 1 9 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 387 6 1 2 5.3 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCCc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
122177645 120700 0 None -44 6 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 591 18 2 8 5.6 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)[C@H]3CCc4c(O)cccc4C3)cc2OC)nn1 10.1021/jm501889t
CHEMBL3577346 120700 0 None -44 6 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 591 18 2 8 5.6 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)[C@H]3CCc4c(O)cccc4C3)cc2OC)nn1 10.1021/jm501889t
10356955 12879 0 None -1 3 Human 8.0 pKi = 8.0 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 291 1 0 2 4.7 CN1CCC(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL1189601 12879 0 None -1 3 Human 8.0 pKi = 8.0 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 291 1 0 2 4.7 CN1CCC(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL539057 12879 0 None -1 3 Human 8.0 pKi = 8.0 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 291 1 0 2 4.7 CN1CCC(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
57398351 69815 0 None 4 7 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 347 6 0 2 5.1 Fc1ccc(OCCCN2CCC(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940406 69815 0 None 4 7 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 347 6 0 2 5.1 Fc1ccc(OCCCN2CCC(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
57398351 69815 0 None 4 7 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 347 6 0 2 5.1 Fc1ccc(OCCCN2CCC(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940406 69815 0 None 4 7 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 347 6 0 2 5.1 Fc1ccc(OCCCN2CCC(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2011.12.019
11504230 77840 0 None -12 7 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 497 8 1 4 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm060138d
CHEMBL210567 77840 0 None -12 7 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 497 8 1 4 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm060138d
71461481 83656 0 None 8 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 356 4 0 3 4.1 C#Cc1cc(CN2CCN(c3ccccc3OC)CC2)c2cccccc1-2 10.1016/j.bmcl.2012.09.064
CHEMBL2207632 83656 0 None 8 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 356 4 0 3 4.1 C#Cc1cc(CN2CCN(c3ccccc3OC)CC2)c2cccccc1-2 10.1016/j.bmcl.2012.09.064
76321556 105896 0 None 2 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3115578 105896 0 None 2 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139302 105896 0 None 2 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
2099556 203344 6 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1cccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)c1 10.1021/jm0305669
CHEMBL77151 203344 6 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1cccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)c1 10.1021/jm0305669
155566403 175363 0 None 52 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 477 9 2 4 4.8 O=C(NCCCN1CCN(c2ccc(Cl)cc2)CC1)NN(Cc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
CHEMBL4587645 175363 0 None 52 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 477 9 2 4 4.8 O=C(NCCCN1CCN(c2ccc(Cl)cc2)CC1)NN(Cc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
76321556 105896 0 None 2 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3115578 105896 0 None 2 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139302 105896 0 None 2 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
54585810 61275 0 None 1 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 469 8 0 4 5.0 COc1ccccc1N1CCN(CCCCN2CCc3c(cccc3-c3ccccc3)C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771108 61275 0 None 1 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 469 8 0 4 5.0 COc1ccccc1N1CCN(CCCCN2CCc3c(cccc3-c3ccccc3)C2=O)CC1 10.1016/j.bmcl.2010.12.083
44403225 70204 0 None 5 5 Human 8.0 pKi = 8 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 421 9 1 5 2.7 COc1ccccc1N1CCN(CCCCNS(=O)(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2005.07.037
CHEMBL194755 70204 0 None 5 5 Human 8.0 pKi = 8 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 421 9 1 5 2.7 COc1ccccc1N1CCN(CCCCNS(=O)(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2005.07.037
9129986 4989 1 None 67 2 Human 8.0 pKi = 8 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 379 5 0 4 2.8 COc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1016/s0960-894x(02)00656-x
CHEMBL105317 4989 1 None 67 2 Human 8.0 pKi = 8 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 379 5 0 4 2.8 COc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1016/s0960-894x(02)00656-x
44412268 77964 8 None 47 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 319 4 0 5 2.6 c1ccc(N2CCN(Cc3cn(-c4ccccc4)nn3)CC2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL211026 77964 8 None 47 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 319 4 0 5 2.6 c1ccc(N2CCN(Cc3cn(-c4ccccc4)nn3)CC2)cc1 10.1016/j.bmcl.2006.02.075
25142456 81994 2 None -44 9 Human 7.1 pKi = 7.1 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)C1c3ccccc3CNC1CO2 10.1021/jm0604979
CHEMBL217299 81994 2 None -44 9 Human 7.1 pKi = 7.1 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)C1c3ccccc3CNC1CO2 10.1021/jm0604979
11849268 168232 0 None -4 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 357 6 0 4 4.4 CO/N=C(/CCN1CCC(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL437532 168232 0 None -4 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 357 6 0 4 4.4 CO/N=C(/CCN1CCC(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
118719797 115224 0 None -12 4 Human 7.1 pKi = 7.1 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 459 8 0 7 4.8 COc1ccccc1N1CCN(CCCc2cn(-c3ccc(-c4ccsc4)cc3)nn2)CC1 10.1016/j.bmcl.2014.12.023
CHEMBL3353900 115224 0 None -12 4 Human 7.1 pKi = 7.1 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 459 8 0 7 4.8 COc1ccccc1N1CCN(CCCc2cn(-c3ccc(-c4ccsc4)cc3)nn2)CC1 10.1016/j.bmcl.2014.12.023
71086428 151021 0 None 66 2 Mouse 7.1 pKi = 7.1 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 373 6 0 5 2.9 Clc1cncc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL3963122 151021 0 None 66 2 Mouse 7.1 pKi = 7.1 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 373 6 0 5 2.9 Clc1cncc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
8704110 66268 9 None - 1 Human 7.0 pKi = 7.0 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 327 4 1 3 2.9 Cc1cccc(NC(=O)CN2CCN(c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL185263 66268 9 None - 1 Human 7.0 pKi = 7.0 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 327 4 1 3 2.9 Cc1cccc(NC(=O)CN2CCN(c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2004.07.068
127698 115500 6 None -6 4 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Dopamine receptor D4.2 evaluated using [3H]spiperoneBinding affinity towards human Dopamine receptor D4.2 evaluated using [3H]spiperone
ChEMBL 329 4 0 1 5.7 C1=C(c2ccccc2)CCN(C[C@@H]2CCC=C(c3ccccc3)C2)C1 10.1021/jm00026a007
CHEMBL335545 115500 6 None -6 4 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Dopamine receptor D4.2 evaluated using [3H]spiperoneBinding affinity towards human Dopamine receptor D4.2 evaluated using [3H]spiperone
ChEMBL 329 4 0 1 5.7 C1=C(c2ccccc2)CCN(C[C@@H]2CCC=C(c3ccccc3)C2)C1 10.1021/jm00026a007
127698 115500 6 None -6 4 Human 7.0 pKi = 7.0 Binding
Tested for binding affinity towards human Dopamine receptor D4.2 using [3H]spiperone as radioligandTested for binding affinity towards human Dopamine receptor D4.2 using [3H]spiperone as radioligand
ChEMBL 329 4 0 1 5.7 C1=C(c2ccccc2)CCN(C[C@@H]2CCC=C(c3ccccc3)C2)C1 10.1021/jm00047a010
CHEMBL335545 115500 6 None -6 4 Human 7.0 pKi = 7.0 Binding
Tested for binding affinity towards human Dopamine receptor D4.2 using [3H]spiperone as radioligandTested for binding affinity towards human Dopamine receptor D4.2 using [3H]spiperone as radioligand
ChEMBL 329 4 0 1 5.7 C1=C(c2ccccc2)CCN(C[C@@H]2CCC=C(c3ccccc3)C2)C1 10.1021/jm00047a010
127046949 139379 0 None -141 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 472 12 3 5 4.6 COc1cc(CCNCCc2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3799455 139379 0 None -141 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 472 12 3 5 4.6 COc1cc(CCNCCc2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
135398737 944 89 None -13 91 Human 5.1 pKi = 5.1 Binding
Binding affinity towards Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00656-x
38 944 89 None -13 91 Human 5.1 pKi = 5.1 Binding
Binding affinity towards Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00656-x
722 944 89 None -13 91 Human 5.1 pKi = 5.1 Binding
Binding affinity towards Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00656-x
CHEMBL42 944 89 None -13 91 Human 5.1 pKi = 5.1 Binding
Binding affinity towards Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00656-x
DB00363 944 89 None -13 91 Human 5.1 pKi = 5.1 Binding
Binding affinity towards Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00656-x
11630058 140843 0 None -7 2 Human 4.1 pKi = 4.1 Binding
Binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandBinding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 237 4 1 5 1.0 CCCNC1CCn2ncc(C(=O)OC)c2C1 10.1021/jm0503805
CHEMBL383805 140843 0 None -7 2 Human 4.1 pKi = 4.1 Binding
Binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandBinding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 237 4 1 5 1.0 CCCNC1CCn2ncc(C(=O)OC)c2C1 10.1021/jm0503805
142590701 178941 0 None -1 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 484 8 1 3 5.8 O=C(c1ccc(F)cc1)N1CCC(NCCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2020.112674
CHEMBL4741279 178941 0 None -1 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 484 8 1 3 5.8 O=C(c1ccc(F)cc1)N1CCC(NCCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2020.112674
132060720 161939 0 None -2 9 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human dopamine D4 expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 315 4 0 2 4.9 COc1cccc(-c2ccc3c(c2)CN(Cc2ccccc2)C3)c1 10.1016/j.ejmech.2018.02.024
CHEMBL4167315 161939 0 None -2 9 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human dopamine D4 expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 315 4 0 2 4.9 COc1cccc(-c2ccc3c(c2)CN(Cc2ccccc2)C3)c1 10.1016/j.ejmech.2018.02.024
11699516 141102 0 None -2 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 540 10 1 7 3.7 COc1ccccc1N1CCN(CCCCNC(=O)c2nnn(Cc3ccccc3Br)c2C)CC1 10.1021/jm0611152
CHEMBL385289 141102 0 None -2 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 540 10 1 7 3.7 COc1ccccc1N1CCN(CCCCNC(=O)c2nnn(Cc3ccccc3Br)c2C)CC1 10.1021/jm0611152
8690650 4699 4 None 1 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 268 3 1 3 2.7 Oc1ccc(N2CCN(Cc3ccccc3)CC2)cc1 10.1016/s0960-894x(98)00014-6
CHEMBL103900 4699 4 None 1 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 268 3 1 3 2.7 Oc1ccc(N2CCN(Cc3ccccc3)CC2)cc1 10.1016/s0960-894x(98)00014-6
154726381 175953 1 None -173 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4522558 175953 1 None -173 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4597048 175953 1 None -173 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
44269820 44787 0 None -2 3 Human 7.0 pKi = 7.0 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 369 3 0 4 4.8 CN1CCN(c2nc3ccccc3c(Cl)c2Sc2ccccc2)CC1 10.1016/s0960-894x(01)00167-6
CHEMBL15242 44787 0 None -2 3 Human 7.0 pKi = 7.0 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 369 3 0 4 4.8 CN1CCN(c2nc3ccccc3c(Cl)c2Sc2ccccc2)CC1 10.1016/s0960-894x(01)00167-6
56649650 67516 0 None -104 8 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 466 8 0 5 4.2 COc1ccccc1N1CCN(CCN(C(=O)C23CCC(CF)(CC2)C3)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
CHEMBL1910141 67516 0 None -104 8 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 466 8 0 5 4.2 COc1ccccc1N1CCN(CCN(C(=O)C23CCC(CF)(CC2)C3)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
9882594 109894 0 None -436 5 Human 7.0 pKi = 7.0 Binding
The binding affinity at the Dopamine receptor D4 determined using [3H]YM-09151-2The binding affinity at the Dopamine receptor D4 determined using [3H]YM-09151-2
ChEMBL 294 1 0 3 3.1 COc1cccc2c1N1CCN(C)CC1c1ccccc1C2 10.1021/jm010566d
CHEMBL324270 109894 0 None -436 5 Human 7.0 pKi = 7.0 Binding
The binding affinity at the Dopamine receptor D4 determined using [3H]YM-09151-2The binding affinity at the Dopamine receptor D4 determined using [3H]YM-09151-2
ChEMBL 294 1 0 3 3.1 COc1cccc2c1N1CCN(C)CC1c1ccccc1C2 10.1021/jm010566d
9910451 163578 0 None -912 7 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 428 5 0 6 4.7 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCC#N)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL420997 163578 0 None -912 7 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 428 5 0 6 4.7 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCC#N)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
11152225 5058 0 None - 1 Human 6.0 pKi = 6.0 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 347 6 0 4 3.6 COc1cc(Cl)cc(OCC2CN(Cc3ccccc3)CCO2)c1 10.1021/jm031111m
CHEMBL105690 5058 0 None - 1 Human 6.0 pKi = 6.0 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 347 6 0 4 3.6 COc1cc(Cl)cc(OCC2CN(Cc3ccccc3)CCO2)c1 10.1021/jm031111m
127046948 139540 0 None -398 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 488 12 4 6 4.1 COc1cc(CCNC[C@@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800468 139540 0 None -398 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 488 12 4 6 4.1 COc1cc(CCNC[C@@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
44582705 186413 0 None -5 13 Human 6.0 pKi = 6.0 Binding
Inhibition of human cloned dopamine D4 receptor by competitive binding experimentInhibition of human cloned dopamine D4 receptor by competitive binding experiment
ChEMBL 399 9 0 4 4.5 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL490632 186413 0 None -5 13 Human 6.0 pKi = 6.0 Binding
Inhibition of human cloned dopamine D4 receptor by competitive binding experimentInhibition of human cloned dopamine D4 receptor by competitive binding experiment
ChEMBL 399 9 0 4 4.5 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
9980998 30819 0 None -1148 8 Human 7.0 pKi = 7.0 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm025558r
CHEMBL139926 30819 0 None -1148 8 Human 7.0 pKi = 7.0 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm025558r
CHEMBL2112911 30819 0 None -1148 8 Human 7.0 pKi = 7.0 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm025558r
9928553 17258 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 354 3 0 4 3.8 O=c1ccc2ccc(CN3CCN(c4ccc(Cl)cc4)CC3)cc2o1 10.1021/jm990266k
CHEMBL125763 17258 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 354 3 0 4 3.8 O=c1ccc2ccc(CN3CCN(c4ccc(Cl)cc4)CC3)cc2o1 10.1021/jm990266k
53359025 62024 0 None 2 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cellsDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cells
ChEMBL 339 5 1 3 2.5 O=C(CCCN1C2C3C4CC5C6C4C2C6C1(O)C53)c1ccc(F)cc1 10.1016/j.bmcl.2011.04.098
CHEMBL1779058 62024 0 None 2 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cellsDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cells
ChEMBL 339 5 1 3 2.5 O=C(CCCN1C2C3C4CC5C6C4C2C6C1(O)C53)c1ccc(F)cc1 10.1016/j.bmcl.2011.04.098
9980998 30819 0 None -1148 8 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in CHO cellsInhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in CHO cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
CHEMBL139926 30819 0 None -1148 8 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in CHO cellsInhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in CHO cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
CHEMBL2112911 30819 0 None -1148 8 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in CHO cellsInhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in CHO cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
9980998 30819 0 None -1148 8 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm0611152
CHEMBL139926 30819 0 None -1148 8 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm0611152
CHEMBL2112911 30819 0 None -1148 8 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm0611152
10522334 104933 0 None -1 3 Human 6.0 pKi = 6.0 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 357 4 1 2 4.6 c1ccc(CCN2CCC3(CCc4c3n[nH]c4-c3ccccc3)CC2)cc1 10.1021/jm970111h
CHEMBL311832 104933 0 None -1 3 Human 6.0 pKi = 6.0 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 357 4 1 2 4.6 c1ccc(CCN2CCC3(CCc4c3n[nH]c4-c3ccccc3)CC2)cc1 10.1021/jm970111h
44323870 111102 0 None -9 4 Human 6.0 pKi = 6.0 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 364 1 0 2 5.2 CC(C)=C1c2ccc(Cl)cc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL328246 111102 0 None -9 4 Human 6.0 pKi = 6.0 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 364 1 0 2 5.2 CC(C)=C1c2ccc(Cl)cc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
44393737 65430 0 None - 1 Human 6.0 pKi = 6.0 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 646 4 1 4 5.7 Cc1c(Br)cc(Br)c(NC(=O)CN2CCN(c3ccc(Br)cc3C#N)CC2)c1Br 10.1016/j.bmcl.2004.07.068
CHEMBL183466 65430 0 None - 1 Human 6.0 pKi = 6.0 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 646 4 1 4 5.7 Cc1c(Br)cc(Br)c(NC(=O)CN2CCN(c3ccc(Br)cc3C#N)CC2)c1Br 10.1016/j.bmcl.2004.07.068
49798799 14243 0 None -3 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 353 4 2 4 3.8 CSc1ccc(C2(O)CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/j.bmc.2010.05.052
CHEMBL1172209 14243 0 None -3 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 353 4 2 4 3.8 CSc1ccc(C2(O)CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/j.bmc.2010.05.052
CHEMBL1200150 14243 0 None -3 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 353 4 2 4 3.8 CSc1ccc(C2(O)CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/j.bmc.2010.05.052
20256387 4704 1 None 1 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 227 6 1 2 2.9 c1ccc(CNCCOc2ccccc2)cc1 10.1016/s0960-894x(98)00014-6
CHEMBL103951 4704 1 None 1 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 227 6 1 2 2.9 c1ccc(CNCCOc2ccccc2)cc1 10.1016/s0960-894x(98)00014-6
122181326 121353 0 None -30 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 413 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)/N=N/c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL3590077 121353 0 None -30 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 413 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)/N=N/c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
137636498 155655 0 None -40 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 446 7 2 6 3.8 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5ncccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4064186 155655 0 None -40 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 446 7 2 6 3.8 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5ncccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
122181326 121353 0 None -30 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 413 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)/N=N/c2ccc(F)cc2)CC1 10.1016/j.bmc.2014.12.012
CHEMBL3590077 121353 0 None -30 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 413 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)/N=N/c2ccc(F)cc2)CC1 10.1016/j.bmc.2014.12.012
749986 202560 10 None 15 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 289 3 1 2 3.9 C1=C(c2nc3ccccc3[nH]2)CCN(Cc2ccccc2)C1 10.1016/S0960-894X(97)00402-2
CHEMBL71173 202560 10 None 15 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 289 3 1 2 3.9 C1=C(c2nc3ccccc3[nH]2)CCN(Cc2ccccc2)C1 10.1016/S0960-894X(97)00402-2
49798835 14246 0 None -14 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 385 3 1 3 4.7 OC1(c2ccc(Br)cc2)CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1172213 14246 0 None -14 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 385 3 1 3 4.7 OC1(c2ccc(Br)cc2)CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1200153 14246 0 None -14 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 385 3 1 3 4.7 OC1(c2ccc(Br)cc2)CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmc.2010.05.052
15508240 110038 0 None 6 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 264 3 0 2 3.3 C#Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
CHEMBL325104 110038 0 None 6 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 264 3 0 2 3.3 C#Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
49798857 14200 0 None -117 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 407 5 0 4 4.0 O=C1N(CCF)CN(c2ccccc2)C12CCN(Cc1coc3ccccc13)CC2 10.1016/j.bmc.2010.05.052
CHEMBL1170085 14200 0 None -117 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 407 5 0 4 4.0 O=C1N(CCF)CN(c2ccccc2)C12CCN(Cc1coc3ccccc13)CC2 10.1016/j.bmc.2010.05.052
CHEMBL1199947 14200 0 None -117 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 407 5 0 4 4.0 O=C1N(CCF)CN(c2ccccc2)C12CCN(Cc1coc3ccccc13)CC2 10.1016/j.bmc.2010.05.052
154725276 175716 1 None -34 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 478 12 1 3 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4456964 175716 1 None -34 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 478 12 1 3 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4595147 175716 1 None -34 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 478 12 1 3 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
23290944 81414 0 None -323 7 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 392 6 0 4 3.8 O=C(C1CCCCC1)N(CCN1CCN(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL2164350 81414 0 None -323 7 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 392 6 0 4 3.8 O=C(C1CCCCC1)N(CCN1CCN(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
44336055 5278 0 None 43 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 4 0 3 3.8 CC1CCc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL106897 5278 0 None 43 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 4 0 3 3.8 CC1CCc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
145993990 166800 0 None -21 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 372 7 2 4 3.1 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(F)cc1)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4294577 166800 0 None -21 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 372 7 2 4 3.1 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(F)cc1)CC2 10.1021/acsmedchemlett.8b00229
155563301 174678 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 344 4 1 4 2.8 Cc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4572245 174678 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 344 4 1 4 2.8 Cc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
168284020 190659 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 387 5 0 4 4.6 Cc1nc(CN2CCC(OCc3ccc(Cl)c(F)c3)CC2)c2ccccn12 10.1016/j.bmcl.2022.128615
CHEMBL5190239 190659 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 387 5 0 4 4.6 Cc1nc(CN2CCC(OCc3ccc(Cl)c(F)c3)CC2)c2ccccn12 10.1016/j.bmcl.2022.128615
137651576 156946 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 308 7 0 3 3.6 COc1cccc(CCC2=NCCN2CCc2ccccc2)c1 10.1021/acs.jmedchem.8b00265
CHEMBL4079495 156946 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 308 7 0 3 3.6 COc1cccc(CCC2=NCCN2CCc2ccccc2)c1 10.1021/acs.jmedchem.8b00265
164612933 184417 0 None -9 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 436 6 2 4 4.5 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1cccc(Cl)c1)CC2 10.1016/j.bmcl.2021.128047
CHEMBL4854512 184417 0 None -9 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 436 6 2 4 4.5 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1cccc(Cl)c1)CC2 10.1016/j.bmcl.2021.128047
164627090 185976 0 None -12 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 432 7 2 5 3.9 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1ccccc1OC)CC2 10.1016/j.bmcl.2021.128047
CHEMBL4878121 185976 0 None -12 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 432 7 2 5 3.9 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1ccccc1OC)CC2 10.1016/j.bmcl.2021.128047
9843032 108046 0 None 45 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.6 CC1CN(C(=O)CN2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/s0960-894x(02)00655-8
CHEMBL320067 108046 0 None 45 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.6 CC1CN(C(=O)CN2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/s0960-894x(02)00655-8
44431468 87842 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 412 4 1 2 5.3 O=C(NC1CCN(Cc2ccc(C(F)(F)F)cc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
CHEMBL234824 87842 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 412 4 1 2 5.3 O=C(NC1CCN(Cc2ccc(C(F)(F)F)cc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
10110263 12883 1 None -7 3 Human 7.0 pKi = 7.0 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 379 7 0 4 4.6 Fc1ccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)cc1 10.1016/s0960-894x(02)00179-8
CHEMBL1189648 12883 1 None -7 3 Human 7.0 pKi = 7.0 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 379 7 0 4 4.6 Fc1ccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)cc1 10.1016/s0960-894x(02)00179-8
CHEMBL539235 12883 1 None -7 3 Human 7.0 pKi = 7.0 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 379 7 0 4 4.6 Fc1ccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)cc1 10.1016/s0960-894x(02)00179-8
15508242 164697 0 None 32 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 268 4 0 3 3.1 O=Cc1ccn(C2CCN(Cc3ccccc3)CC2)c1 10.1016/s0960-894x(99)00540-5
CHEMBL422959 164697 0 None 32 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 268 4 0 3 3.1 O=Cc1ccn(C2CCN(Cc3ccccc3)CC2)c1 10.1016/s0960-894x(99)00540-5
45270813 195014 0 None -112 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 365 4 0 6 3.0 COc1ccc(N2CCN(Cc3c(C)nc4cc(C)nc(C)n34)CC2)cc1 10.1016/j.bmc.2009.05.015
CHEMBL564709 195014 0 None -112 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 365 4 0 6 3.0 COc1ccc(N2CCN(Cc3c(C)nc4cc(C)nc(C)n34)CC2)cc1 10.1016/j.bmc.2009.05.015
154704418 176013 1 None -2 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 458 12 1 6 4.8 Cn1c(SCCCNCC2CC2c2cc(F)ccc2OCCF)nnc1-c1ccccc1 10.1021/acs.jmedchem.9b01835
CHEMBL4546749 176013 1 None -2 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 458 12 1 6 4.8 Cn1c(SCCCNCC2CC2c2cc(F)ccc2OCCF)nnc1-c1ccccc1 10.1021/acs.jmedchem.9b01835
CHEMBL4597533 176013 1 None -2 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 458 12 1 6 4.8 Cn1c(SCCCNCC2CC2c2cc(F)ccc2OCCF)nnc1-c1ccccc1 10.1021/acs.jmedchem.9b01835
12581203 24869 0 None -7 3 Human 6.0 pKi = 6.0 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 233 4 0 2 2.9 CCN(CC)C1CCc2c(cccc2OC)C1 10.1021/jm960345l
CHEMBL134701 24869 0 None -7 3 Human 6.0 pKi = 6.0 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 233 4 0 2 2.9 CCN(CC)C1CCc2c(cccc2OC)C1 10.1021/jm960345l
25141538 55948 0 None -407 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 440 8 3 5 2.6 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3cc(F)ccc3[nH]2)CC1 10.1021/jm900095y
CHEMBL1627311 55948 0 None -407 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 440 8 3 5 2.6 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3cc(F)ccc3[nH]2)CC1 10.1021/jm900095y
681 1437 65 None -2 38 Human 7.0 pKi = 7.0 Binding
Binding Affinity was determined in the presence of 100 micro M Gpp(NH)p for decoupling of the ternary complex of Compound to Dopamine receptor D4.4Binding Affinity was determined in the presence of 100 micro M Gpp(NH)p for decoupling of the ternary complex of Compound to Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
940 1437 65 None -2 38 Human 7.0 pKi = 7.0 Binding
Binding Affinity was determined in the presence of 100 micro M Gpp(NH)p for decoupling of the ternary complex of Compound to Dopamine receptor D4.4Binding Affinity was determined in the presence of 100 micro M Gpp(NH)p for decoupling of the ternary complex of Compound to Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
947 1437 65 None -2 38 Human 7.0 pKi = 7.0 Binding
Binding Affinity was determined in the presence of 100 micro M Gpp(NH)p for decoupling of the ternary complex of Compound to Dopamine receptor D4.4Binding Affinity was determined in the presence of 100 micro M Gpp(NH)p for decoupling of the ternary complex of Compound to Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
CHEMBL59 1437 65 None -2 38 Human 7.0 pKi = 7.0 Binding
Binding Affinity was determined in the presence of 100 micro M Gpp(NH)p for decoupling of the ternary complex of Compound to Dopamine receptor D4.4Binding Affinity was determined in the presence of 100 micro M Gpp(NH)p for decoupling of the ternary complex of Compound to Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
DB00988 1437 65 None -2 38 Human 7.0 pKi = 7.0 Binding
Binding Affinity was determined in the presence of 100 micro M Gpp(NH)p for decoupling of the ternary complex of Compound to Dopamine receptor D4.4Binding Affinity was determined in the presence of 100 micro M Gpp(NH)p for decoupling of the ternary complex of Compound to Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
44330694 107102 0 None 9 2 Human 7.0 pKi = 7.0 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 260 2 0 3 4.1 CCCn1ncc2c1-c1c(C)sc(C)c1CCC2 10.1016/s0960-894x(03)00587-0
CHEMBL318949 107102 0 None 9 2 Human 7.0 pKi = 7.0 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 260 2 0 3 4.1 CCCn1ncc2c1-c1c(C)sc(C)c1CCC2 10.1016/s0960-894x(03)00587-0
44403224 71571 0 None -10 5 Human 7.0 pKi = 7.0 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 424 7 1 4 3.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc(F)n1 10.1016/j.bmcl.2005.07.037
CHEMBL197195 71571 0 None -10 5 Human 7.0 pKi = 7.0 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 424 7 1 4 3.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc(F)n1 10.1016/j.bmcl.2005.07.037
22100968 202405 4 None 2 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 290 3 0 3 4.1 C1=C(c2nc3ccccc3o2)CCN(Cc2ccccc2)C1 10.1016/S0960-894X(97)00402-2
CHEMBL70267 202405 4 None 2 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 290 3 0 3 4.1 C1=C(c2nc3ccccc3o2)CCN(Cc2ccccc2)C1 10.1016/S0960-894X(97)00402-2
11230330 134664 0 None -19 3 Human 5.0 pKi = 5.0 Binding
Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsLow inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 245 5 0 3 2.8 CCCN(CCC)[C@H]1CCn2c(C#N)ccc2C1 10.1021/jm049269+
CHEMBL372020 134664 0 None -19 3 Human 5.0 pKi = 5.0 Binding
Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsLow inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 245 5 0 3 2.8 CCCN(CCC)[C@H]1CCn2c(C#N)ccc2C1 10.1021/jm049269+
44415593 79837 0 None -977 6 Human 6.0 pKi = 6.0 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 495 2 1 5 5.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc4ccccc34)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL213834 79837 0 None -977 6 Human 6.0 pKi = 6.0 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 495 2 1 5 5.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc4ccccc34)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
154725234 175718 1 None -1 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 472 12 0 6 5.2 CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.9b01835
CHEMBL4585289 175718 1 None -1 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 472 12 0 6 5.2 CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.9b01835
CHEMBL4595149 175718 1 None -1 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 472 12 0 6 5.2 CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.9b01835
11547151 83947 0 None -14 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 462 10 1 7 3.0 COc1ccccc1N1CCN(CCCCNC(=O)c2nnn(Cc3ccccc3)c2C)CC1 10.1021/jm0611152
CHEMBL221843 83947 0 None -14 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 462 10 1 7 3.0 COc1ccccc1N1CCN(CCCCNC(=O)c2nnn(Cc3ccccc3)c2C)CC1 10.1021/jm0611152
44275807 98513 0 None -8912 10 Human 5.0 pKi = 5.0 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 422 7 0 4 4.5 C[C@H]1CC[C@H](C)N1CCCOc1ccc(-c2ccc(C(=O)N3CCOCC3)cc2)cc1 10.1016/s0960-894x(03)00118-5
CHEMBL27979 98513 0 None -8912 10 Human 5.0 pKi = 5.0 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 422 7 0 4 4.5 C[C@H]1CC[C@H](C)N1CCCOc1ccc(-c2ccc(C(=O)N3CCOCC3)cc2)cc1 10.1016/s0960-894x(03)00118-5
155515301 169400 0 None -812 7 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting
ChEMBL 444 6 0 5 4.2 COc1ccccc1N1CCN(C[C@H]2OCCOC2(c2ccccc2)c2ccccc2)CC1 10.1016/j.ejmech.2019.02.056
CHEMBL4441888 169400 0 None -812 7 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting
ChEMBL 444 6 0 5 4.2 COc1ccccc1N1CCN(C[C@H]2OCCOC2(c2ccccc2)c2ccccc2)CC1 10.1016/j.ejmech.2019.02.056
49798874 14236 0 None -1096 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 488 7 0 7 3.8 O=C1N(Cc2cn(CCF)nn2)CN(c2ccccc2)C12CCN(Cc1coc3ccccc13)CC2 10.1016/j.bmc.2010.05.052
CHEMBL1171630 14236 0 None -1096 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 488 7 0 7 3.8 O=C1N(Cc2cn(CCF)nn2)CN(c2ccccc2)C12CCN(Cc1coc3ccccc13)CC2 10.1016/j.bmc.2010.05.052
CHEMBL1200106 14236 0 None -1096 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 488 7 0 7 3.8 O=C1N(Cc2cn(CCF)nn2)CN(c2ccccc2)C12CCN(Cc1coc3ccccc13)CC2 10.1016/j.bmc.2010.05.052
122189391 122730 0 None -11 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 431 7 0 9 2.1 COc1ccccc1N1CCN(CCc2cn(-c3ccn4ncc(C=O)c4c3)nn2)CC1 10.1016/j.bmc.2015.07.050
CHEMBL3613877 122730 0 None -11 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 431 7 0 9 2.1 COc1ccccc1N1CCN(CCc2cn(-c3ccn4ncc(C=O)c4c3)nn2)CC1 10.1016/j.bmc.2015.07.050
16090814 81169 0 None -74 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human D4 dopamine receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 dopamine receptor expressed in CHO cells
ChEMBL 304 0 1 1 4.2 CN1CCCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
CHEMBL216258 81169 0 None -74 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human D4 dopamine receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 dopamine receptor expressed in CHO cells
ChEMBL 304 0 1 1 4.2 CN1CCCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
142590731 182500 0 None -1 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 470 9 1 3 6.2 Fc1ccc(CN2CCC(NCCSC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1016/j.ejmech.2020.112674
CHEMBL4794406 182500 0 None -1 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 470 9 1 3 6.2 Fc1ccc(CN2CCC(NCCSC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1016/j.ejmech.2020.112674
154704536 175873 1 None -1 3 Human 6.0 pKi = 6 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 454 11 0 6 5.2 CCOc1ccc(F)cc1C1CC1CN(C)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4467528 175873 1 None -1 3 Human 6.0 pKi = 6 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 454 11 0 6 5.2 CCOc1ccc(F)cc1C1CC1CN(C)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4596340 175873 1 None -1 3 Human 6.0 pKi = 6 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 454 11 0 6 5.2 CCOc1ccc(F)cc1C1CC1CN(C)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
11637457 72740 1 None -8 5 Human 7.0 pKi = 7 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2ccsc2CC1 10.1039/C5MD00258C
CHEMBL201093 72740 1 None -8 5 Human 7.0 pKi = 7 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2ccsc2CC1 10.1039/C5MD00258C
51353678 59871 0 None -1905 3 Human 6.0 pKi = 6 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 461 13 1 5 3.7 O=C(NCCCCN1CCN(c2ccccc2OCCF)CC1)c1ccc(OCCF)cc1 10.1021/jm101323b
CHEMBL1689004 59871 0 None -1905 3 Human 6.0 pKi = 6 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 461 13 1 5 3.7 O=C(NCCCCN1CCN(c2ccccc2OCCF)CC1)c1ccc(OCCF)cc1 10.1021/jm101323b
CHEMBL1739810 59871 0 None -1905 3 Human 6.0 pKi = 6 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 461 13 1 5 3.7 O=C(NCCCCN1CCN(c2ccccc2OCCF)CC1)c1ccc(OCCF)cc1 10.1021/jm101323b
44380921 58021 0 None -2 4 Human 6.0 pKi = 6 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@H]1CN(Cc2ccccc2)C[C@@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
CHEMBL168274 58021 0 None -2 4 Human 6.0 pKi = 6 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@H]1CN(Cc2ccccc2)C[C@@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
11212939 68818 0 None -10 3 Rat 6.0 pKi = 6 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 443 7 1 4 4.5 COc1ccc2c(c1)N1CCN(CCCCNC(=O)c3ccc4ccccc4c3)C[C@@H]1CC2 10.1021/jm049031l
CHEMBL192439 68818 0 None -10 3 Rat 6.0 pKi = 6 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 443 7 1 4 4.5 COc1ccc2c(c1)N1CCN(CCCCNC(=O)c3ccc4ccccc4c3)C[C@@H]1CC2 10.1021/jm049031l
44336035 5222 0 None 2 2 Human 6.0 pKi = 6 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 403 4 0 3 3.7 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2c(Cl)cccc21 10.1016/s0960-894x(02)00655-8
CHEMBL106598 5222 0 None 2 2 Human 6.0 pKi = 6 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 403 4 0 3 3.7 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2c(Cl)cccc21 10.1016/s0960-894x(02)00655-8
135 2496 38 None - 57 Human 8.3 pIC50 = 8.3 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2496 38 None - 57 Human 8.3 pIC50 = 8.3 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2496 38 None - 57 Human 8.3 pIC50 = 8.3 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2496 38 None - 57 Human 8.3 pIC50 = 8.3 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2496 38 None - 57 Human 8.3 pIC50 = 8.3 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1353 1880 85 None -3 85 Human 8.0 pKd = 8.0 Binding
radioligand [3H]spiperone 0.5nM competition binding; human recombinant dopaminereceptors in CHO cellsradioligand [3H]spiperone 0.5nM competition binding; human recombinant dopaminereceptors in CHO cells
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 None -3 85 Human 8.0 pKd = 8.0 Binding
radioligand [3H]spiperone 0.5nM competition binding; human recombinant dopaminereceptors in CHO cellsradioligand [3H]spiperone 0.5nM competition binding; human recombinant dopaminereceptors in CHO cells
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 None -3 85 Human 8.0 pKd = 8.0 Binding
radioligand [3H]spiperone 0.5nM competition binding; human recombinant dopaminereceptors in CHO cellsradioligand [3H]spiperone 0.5nM competition binding; human recombinant dopaminereceptors in CHO cells
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 None -3 85 Human 8.0 pKd = 8.0 Binding
radioligand [3H]spiperone 0.5nM competition binding; human recombinant dopaminereceptors in CHO cellsradioligand [3H]spiperone 0.5nM competition binding; human recombinant dopaminereceptors in CHO cells
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 None -3 85 Human 8.0 pKd = 8.0 Binding
radioligand [3H]spiperone 0.5nM competition binding; human recombinant dopaminereceptors in CHO cellsradioligand [3H]spiperone 0.5nM competition binding; human recombinant dopaminereceptors in CHO cells
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
9952220 97804 5 None -8 4 Human 8.0 pKd = 8.0 Binding
Binding Affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding Affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
Drug Central 387 6 2 4 3.8 CNc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)[C@H]2C)cc1Cl None
CHEMBL274491 97804 5 None -8 4 Human 8.0 pKd = 8.0 Binding
Binding Affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding Affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
Drug Central 387 6 2 4 3.8 CNc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)[C@H]2C)cc1Cl None
188942 2778 38 None -12 4 Human 8.3 pKd = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 9262371
3297 2778 38 None -12 4 Human 8.3 pKd = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 9262371
979 2778 38 None -12 4 Human 8.3 pKd = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 9262371
CHEMBL103772 2778 38 None -12 4 Human 8.3 pKd = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 9262371
2470 3596 46 None -20 59 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1840645
2470 3596 46 None -20 59 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7777184
3300 3596 46 None -20 59 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1840645
3300 3596 46 None -20 59 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7777184
5265 3596 46 None -20 59 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1840645
5265 3596 46 None -20 59 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7777184
99 3596 46 None -20 59 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1840645
99 3596 46 None -20 59 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7777184
CHEMBL267930 3596 46 None -20 59 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1840645
CHEMBL267930 3596 46 None -20 59 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7777184
4452 2721 18 None -7 18 Human 10.0 pKd None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 8248849
983 2721 18 None -7 18 Human 10.0 pKd None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 8248849
CHEMBL20734 2721 18 None -7 18 Human 10.0 pKd None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 8248849
4452 2721 18 3H-YM 09151-2 -7 18 Human 10.5 pKi = 10.5 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
983 2721 18 3H-YM 09151-2 -7 18 Human 10.5 pKi = 10.5 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
CHEMBL20734 2721 18 3H-YM 09151-2 -7 18 Human 10.5 pKi = 10.5 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
2470 3596 46 3H-SPIPERONE -4 59 Rat 10.3 pKi = 10.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3596 46 3H-SPIPERONE -4 59 Rat 10.3 pKi = 10.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3596 46 3H-SPIPERONE -4 59 Rat 10.3 pKi = 10.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3596 46 3H-SPIPERONE -4 59 Rat 10.3 pKi = 10.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3596 46 3H-SPIPERONE -4 59 Rat 10.3 pKi = 10.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
16363 589 48 UNDEFINED -1 6 Human 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
312 589 48 UNDEFINED -1 6 Human 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
9215 589 48 UNDEFINED -1 6 Human 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL297302 589 48 UNDEFINED -1 6 Human 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB12867 589 48 UNDEFINED -1 6 Human 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2470 3596 46 3H-SPIPERONE -20 59 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3596 46 3H-SPIPERONE -20 59 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3596 46 3H-SPIPERONE -20 59 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3596 46 3H-SPIPERONE -20 59 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3596 46 3H-SPIPERONE -20 59 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
2470 3596 46 3H-SPIPERONE -20 59 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3596 46 3H-SPIPERONE -20 59 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3596 46 3H-SPIPERONE -20 59 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3596 46 3H-SPIPERONE -20 59 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3596 46 3H-SPIPERONE -20 59 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
None 214526 0 UNDEFINED 4 11 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 426 6 0 6 3.4 C1CCC2C(C1)C(=O)N(C2=O)CCCCN3CCN(CC3)C4=NSC5=CC=CC=C54 None
2 3210 19 3H-SPIPERONE -2 28 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
54562 3210 19 3H-SPIPERONE -2 28 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
CHEMBL240773 3210 19 3H-SPIPERONE -2 28 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
2389 3279 114 3H-SPIPERONE -21 67 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2389 3279 114 UNDEFINED -21 67 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 3H-SPIPERONE -21 67 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 UNDEFINED -21 67 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 3H-SPIPERONE -21 67 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 UNDEFINED -21 67 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 3H-SPIPERONE -21 67 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 UNDEFINED -21 67 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 3H-SPIPERONE -21 67 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 UNDEFINED -21 67 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
1353 1880 85 3H-SPIPERONE -3 85 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-SPIPERONE -3 85 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-SPIPERONE -3 85 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-SPIPERONE -3 85 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-SPIPERONE -3 85 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
5567 42556 24 UNDEFINED -11 7 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 409 6 1 3 4.8 O=C(CCCN1CCC(O)(c2cccc(C(F)(F)F)c2)CC1)c1ccc(F)cc1 None
CHEMBL15023 42556 24 UNDEFINED -11 7 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 409 6 1 3 4.8 O=C(CCCN1CCC(O)(c2cccc(C(F)(F)F)c2)CC1)c1ccc(F)cc1 None
2470 3596 46 3H-SPIPERONE -4 59 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3596 46 3H-SPIPERONE -4 59 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3596 46 3H-SPIPERONE -4 59 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3596 46 3H-SPIPERONE -4 59 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3596 46 3H-SPIPERONE -4 59 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
1238 201484 21 R-SAT -2 16 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL64249 201484 21 R-SAT -2 16 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
3303 2213 41 UNDEFINED 1 15 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 None
5311200 2213 41 UNDEFINED 1 15 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 None
CHEMBL267014 2213 41 UNDEFINED 1 15 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 None
11976 907 54 UNDEFINED -2 23 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
667467 907 54 UNDEFINED -2 23 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
CHEMBL908 907 54 UNDEFINED -2 23 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
DB01239 907 54 UNDEFINED -2 23 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
1353 1880 85 3H-SPIROPERIDOL -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-SPIROPERIDOL -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-SPIROPERIDOL -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-SPIROPERIDOL -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-SPIROPERIDOL -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
2865 4079 67 UNDEFINED -66 53 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4079 67 UNDEFINED -66 53 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4079 67 UNDEFINED -66 53 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4079 67 UNDEFINED -66 53 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4079 67 UNDEFINED -66 53 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
1353 1880 85 3H-Haloperidol -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 1880 85 3H-SPIPERONE -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 1880 85 UNDEFINED -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-Haloperidol -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-SPIPERONE -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 UNDEFINED -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-Haloperidol -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-SPIPERONE -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 UNDEFINED -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-Haloperidol -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-SPIPERONE -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 UNDEFINED -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-Haloperidol -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-SPIPERONE -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 UNDEFINED -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3168 9172 84 UNDEFINED -4 21 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
CHEMBL1108 9172 84 UNDEFINED -4 21 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
2435 3533 78 3H-SPIPERONE -10 48 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3533 78 3H-SPIPERONE -10 48 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3533 78 3H-SPIPERONE -10 48 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3533 78 3H-SPIPERONE -10 48 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3533 78 3H-SPIPERONE -10 48 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
2435 3533 78 UNDEFINED -10 48 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3533 78 UNDEFINED -10 48 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3533 78 UNDEFINED -10 48 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3533 78 UNDEFINED -10 48 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3533 78 UNDEFINED -10 48 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
2435 3533 78 3H-Sertindole -10 48 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3533 78 3H-Sertindole -10 48 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3533 78 3H-Sertindole -10 48 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3533 78 3H-Sertindole -10 48 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3533 78 3H-Sertindole -10 48 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
2726 906 64 3H-SPIPERONE -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 3H-SPIPERONE -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 3H-SPIPERONE -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 3H-SPIPERONE -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 3H-SPIPERONE -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
2726 906 64 3H-Chlorpromazine -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
2726 906 64 UNDEFINED -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 3H-Chlorpromazine -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 UNDEFINED -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 3H-Chlorpromazine -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 UNDEFINED -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 3H-Chlorpromazine -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 UNDEFINED -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 3H-Chlorpromazine -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 UNDEFINED -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
2470 3596 46 3H-SPIPERONE -20 59 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3596 46 3H-SPIPERONE -20 59 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3596 46 3H-SPIPERONE -20 59 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3596 46 3H-SPIPERONE -20 59 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3596 46 3H-SPIPERONE -20 59 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
100 3745 52 3H-SPIPERONE -8 55 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
100 3745 52 UNDEFINED -8 55 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3745 52 3H-SPIPERONE -8 55 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3745 52 UNDEFINED -8 55 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3745 52 3H-SPIPERONE -8 55 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3745 52 UNDEFINED -8 55 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3745 52 3H-SPIPERONE -8 55 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3745 52 UNDEFINED -8 55 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3745 52 3H-SPIPERONE -8 55 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3745 52 UNDEFINED -8 55 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
135398737 944 89 3H-Clozapine -13 91 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 944 89 3H-SPIPERONE -13 91 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 944 89 UNDEFINED -13 91 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-Clozapine -13 91 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-SPIPERONE -13 91 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 UNDEFINED -13 91 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-Clozapine -13 91 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-SPIPERONE -13 91 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 UNDEFINED -13 91 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-Clozapine -13 91 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-SPIPERONE -13 91 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 UNDEFINED -13 91 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-Clozapine -13 91 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-SPIPERONE -13 91 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 UNDEFINED -13 91 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
5281878 1630 33 UNDEFINED -14 16 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 1630 33 UNDEFINED -14 16 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 1630 33 UNDEFINED -14 16 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 1630 33 UNDEFINED -14 16 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 1630 33 UNDEFINED -14 16 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 1630 33 UNDEFINED -14 16 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 1630 33 UNDEFINED -14 16 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
135398745 2869 108 3H-Olanzapine -10 65 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745 2869 108 UNDEFINED -10 65 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-Olanzapine -10 65 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 UNDEFINED -10 65 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-Olanzapine -10 65 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 UNDEFINED -10 65 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-Olanzapine -10 65 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 UNDEFINED -10 65 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
3303 2213 41 R-SAT 1 15 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 None
5311200 2213 41 R-SAT 1 15 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 None
CHEMBL267014 2213 41 R-SAT 1 15 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 None
16362 3076 67 R-SAT -20 29 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 3076 67 R-SAT -20 29 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 3076 67 R-SAT -20 29 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 3076 67 R-SAT -20 29 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 3076 67 R-SAT -20 29 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
46780481 107045 18 3H-NMSP -23 53 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107045 18 3H-NMSP -23 53 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107045 18 3H-NMSP -23 53 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107045 18 3H-NMSP -23 53 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
1613 2316 44 3H-NEMONAPRIDE -2 44 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2316 44 3H-NEMONAPRIDE -2 44 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2316 44 3H-NEMONAPRIDE -2 44 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2316 44 3H-NEMONAPRIDE -2 44 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2316 44 3H-NEMONAPRIDE -2 44 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
100 3745 52 3H-SPIPERONE -3 55 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3745 52 3H-SPIPERONE -3 55 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3745 52 3H-SPIPERONE -3 55 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3745 52 3H-SPIPERONE -3 55 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3745 52 3H-SPIPERONE -3 55 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
115368 3007 0 None 1 3 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 None
2112 3007 0 None 1 3 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 None
7556 3007 0 None 1 3 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 None
CHEMBL1472975 3007 0 None 1 3 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 None
DB08922 3007 0 None 1 3 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 None
2435 3533 78 3H-SPIPERONE -19 48 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3533 78 3H-SPIPERONE -19 48 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3533 78 3H-SPIPERONE -19 48 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3533 78 3H-SPIPERONE -19 48 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3533 78 3H-SPIPERONE -19 48 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
1353 1880 85 3H-SPIPERONE -4 85 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-SPIPERONE -4 85 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-SPIPERONE -4 85 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-SPIPERONE -4 85 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-SPIPERONE -4 85 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
100 3745 52 3H-SPIPERONE -8 55 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3745 52 3H-SPIPERONE -8 55 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3745 52 3H-SPIPERONE -8 55 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3745 52 3H-SPIPERONE -8 55 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3745 52 3H-SPIPERONE -8 55 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
4257 77868 26 None - 1 Human 8.0 pKi = 8.0 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
Drug Central 478 4 1 4 4.7 O=C1NC2CCCCN2C12CCN(CCCN1c3ccccc3CCc3ccc(Cl)cc31)CC2 None
CHEMBL2106650 77868 26 None - 1 Human 8.0 pKi = 8.0 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
Drug Central 478 4 1 4 4.7 O=C1NC2CCCCN2C12CCN(CCCN1c3ccccc3CCc3ccc(Cl)cc31)CC2 None
25139335 183736 0 UNDEFINED 2 3 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 314 8 0 4 3.6 CC#CC1=CCC(N(CCC)CCCCn2cc(C)nn2)CC1 None
CHEMBL484203 183736 0 UNDEFINED 2 3 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 314 8 0 4 3.6 CC#CC1=CCC(N(CCC)CCCCn2cc(C)nn2)CC1 None
242 467 117 R-SAT -117 51 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 467 117 R-SAT -117 51 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 467 117 R-SAT -117 51 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 467 117 R-SAT -117 51 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 467 117 R-SAT -117 51 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
5281878 1630 33 R-SAT -14 16 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 1630 33 R-SAT -14 16 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 1630 33 R-SAT -14 16 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 1630 33 R-SAT -14 16 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 1630 33 R-SAT -14 16 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 1630 33 R-SAT -14 16 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 1630 33 R-SAT -14 16 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1577 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
164512405 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2537 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5355 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5501 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
643497 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
688272 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
958 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
960 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL196677 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL26 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL267044 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB00391 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB16021 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2865 4079 67 R-SAT -66 53 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4079 67 R-SAT -66 53 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4079 67 R-SAT -66 53 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4079 67 R-SAT -66 53 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4079 67 R-SAT -66 53 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
54477 84230 34 R-SAT -14 22 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
CHEMBL22242 84230 34 R-SAT -14 22 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
15387 214209 0 R-SAT -35 23 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CC1)CCCC(=O)C2=CC=C(C=C2)F None
119192 2446 48 3H-N-Methylspiporone -2818 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 586 7 2 7 5.8 COc1cccc(c1c1cc(nn1c1ccnc2c1ccc(c2)Cl)C(=O)NC1(C(=O)O)C2CC3CC1CC(C2)C3)OC None
1582 2446 48 3H-N-Methylspiporone -2818 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 586 7 2 7 5.8 COc1cccc(c1c1cc(nn1c1ccnc2c1ccc(c2)Cl)C(=O)NC1(C(=O)O)C2CC3CC1CC(C2)C3)OC None
CHEMBL506981 2446 48 3H-N-Methylspiporone -2818 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 586 7 2 7 5.8 COc1cccc(c1c1cc(nn1c1ccnc2c1ccc(c2)Cl)C(=O)NC1(C(=O)O)C2CC3CC1CC(C2)C3)OC None
DB06455 2446 48 3H-N-Methylspiporone -2818 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 586 7 2 7 5.8 COc1cccc(c1c1cc(nn1c1ccnc2c1ccc(c2)Cl)C(=O)NC1(C(=O)O)C2CC3CC1CC(C2)C3)OC None
134 2478 19 3H-NMSP -8511 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2478 19 3H-NMSP -8511 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2478 19 3H-NMSP -8511 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2478 19 3H-NMSP -8511 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2478 19 3H-NMSP -8511 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
15897 2817 0 3H-NMSP -354 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2817 0 3H-NMSP -354 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2817 0 3H-NMSP -354 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
128563 3408 28 3H-NMSP -2398 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
1666 3408 28 3H-NMSP -2398 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
CHEMBL445332 3408 28 3H-NMSP -2398 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
DB12327 3408 28 3H-NMSP -2398 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
189 3436 31 3H-YM 09151-1 -4168 17 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 None
5163 3436 31 3H-YM 09151-1 -4168 17 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 None
CHEMBL297784 3436 31 3H-YM 09151-1 -4168 17 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 None
1577 3647 104 3H-SPIPERONE -28 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
164512405 3647 104 3H-SPIPERONE -28 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2537 3647 104 3H-SPIPERONE -28 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5355 3647 104 3H-SPIPERONE -28 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5501 3647 104 3H-SPIPERONE -28 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
643497 3647 104 3H-SPIPERONE -28 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
688272 3647 104 3H-SPIPERONE -28 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
958 3647 104 3H-SPIPERONE -28 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
960 3647 104 3H-SPIPERONE -28 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL196677 3647 104 3H-SPIPERONE -28 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL26 3647 104 3H-SPIPERONE -28 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL267044 3647 104 3H-SPIPERONE -28 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB00391 3647 104 3H-SPIPERONE -28 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB16021 3647 104 3H-SPIPERONE -28 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
185 3943 54 3H-NMSP -7244 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5311271 3943 54 3H-NMSP -7244 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
CHEMBL74355 3943 54 3H-NMSP -7244 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
DB16351 3943 54 3H-NMSP -7244 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
2662 11279 124 3H-NMSP -41 31 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 None
CHEMBL118 11279 124 3H-NMSP -41 31 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 None
10297 26905 29 3H-NMSP -38 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
CHEMBL136560 26905 29 3H-NMSP -38 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
156391 46537 95 3H-NMSP -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
CHEMBL1200806 46537 95 3H-NMSP -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
CHEMBL154 46537 95 3H-NMSP -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
10624 69957 17 3H-NMSP -102 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
138543650 69957 17 3H-NMSP -102 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
CHEMBL194378 69957 17 3H-NMSP -102 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
2244 93798 96 3H-NMSP -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 180 2 1 3 1.3 CC(=O)Oc1ccccc1C(=O)O None
CHEMBL25 93798 96 3H-NMSP -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 180 2 1 3 1.3 CC(=O)Oc1ccccc1C(=O)O None
24840389 114714 3 3H-SPIPERONE -7413 15 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 415 9 0 4 4.6 CCCN(CCC)C1CCc2cc(CS(=O)(=O)c3ccc(OC)cc3)ccc2C1 None
CHEMBL334529 114714 3 3H-SPIPERONE -7413 15 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 415 9 0 4 4.6 CCCN(CCC)C1CCc2cc(CS(=O)(=O)c3ccc(OC)cc3)ccc2C1 None
446220 132998 13 3H-NMSP -1778 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
CHEMBL370805 132998 13 3H-NMSP -1778 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
1615 167228 22 3H-NMSP -26 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
1615 167228 22 3H-NMSP -26 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
CHEMBL43048 167228 22 3H-NMSP -26 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
CHEMBL43048 167228 22 3H-NMSP -26 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
54676228 192874 108 3H-NMSP -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 2 2 5 1.6 CN1C(C(=O)Nc2ccccn2)=C(O)c2ccccc2S1(=O)=O None
CHEMBL527 192874 108 3H-NMSP -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 2 2 5 1.6 CN1C(C(=O)Nc2ccccn2)=C(O)c2ccccc2S1(=O)=O None
4495 194860 87 3H-NMSP -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 None
CHEMBL56367 194860 87 3H-NMSP -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 None
54677470 198867 110 3H-NMSP -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
CHEMBL1256873 198867 110 3H-NMSP -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
CHEMBL599 198867 110 3H-NMSP -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
162265 200587 19 3H-NMSP -239 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4786 200587 19 3H-NMSP -239 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
CHEMBL61006 200587 19 3H-NMSP -239 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
5281600 201336 85 3H-Methylspiperone -275 33 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
CHEMBL63354 201336 85 3H-Methylspiperone -275 33 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
4054 203790 64 3H-NMSP -1 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL1699 203790 64 3H-NMSP -1 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL807 203790 64 3H-NMSP -1 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
11954224 214174 0 3H-NMSP -141253 59 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
None 214217 0 3H-N-Methylspiperone -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 2 0 4 3.6 CC1=NC=CN1CC2CCC3=C(C2=O)C4=CC=CC=C4N3C.Cl None
25137849 214425 0 3H-NMSP -4 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
71290 214425 0 3H-NMSP -4 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
3337 214441 0 3H-NMSP -1513 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
65801 214441 0 3H-NMSP -1513 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
66264 214441 0 3H-NMSP -1513 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
91452 214441 0 3H-NMSP -1513 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
None 214486 0 3H-NMSP -95499 29 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 316 7 3 3 3.0 CC(CF)NCC(COC1=CC=CC2=C1C3=CC=CC=C3N2)O None
3821 214549 0 3H-N-Methylspiperone -1 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 237 2 1 2 2.9 CNC1(CCCCC1=O)C2=CC=CC=C2Cl None
None 214560 0 3H-NMSP -1 33 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 240 7 4 6 -0.8 C(C(C(=O)O)N)SSCC(C(=O)O)N None
None 214561 0 3H-NMSP -1 33 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 4 2 3 0.2 CSCCC(C(=O)O)N None
None 214562 0 3H-NMSP -1 33 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 3 3 3 -0.3 C(CS)C(C(=O)O)N None
None 214563 0 3H-NMSP -1 33 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 121 2 3 3 -0.7 C(C(C(=O)O)N)S None
None 214564 0 3H-NMSP -1 28 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 117 0 1 3 -0.0 C1CSC(=O)C1N None
None 214565 0 3H-NMSP -1 39 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 3 3 3 -1.4 C(C(C(=O)O)N)S(=O)O None
None 214566 0 3H-NMSP -1 38 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 3 3 4 -1.7 C(C(C(=O)O)N)S(=O)(=O)O None
None 214567 0 3H-NMSP -1 29 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 183 4 3 4 -1.3 C(CS(=O)(=O)O)C(C(=O)O)N None
None 214574 0 3H-NMSP -13 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 2 1 2 1.2 CC(C(=O)C1=CC=CC=C1)N None
1576 214575 0 3H-NMSP -16 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 163 3 1 2 1.5 CC(C(=O)C1=CC=CC=C1)NC None
None 214576 0 3H-Methylspiperone -16 28 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 536 11 1 4 9.0 CC(C)C(=O)C12C(=O)C(=C(C(C1=O)(CC(C2(C)CCC=C(C)C)CC=C(C)C)CC=C(C)C)O)CC=C(C)C None
None 214578 0 3H-Methylspiperone -3 28 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 464 4 8 12 -0.6 C1=CC(=C(C=C1C2=C(C(=C3C(=CC(=O)C=C3O2)O)O)OC4C(C(C(C(O4)CO)O)O)O)O)O None
None 214579 0 3H-Methylspiperone -281 28 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 610 6 10 16 -1.7 CC1C(C(C(C(O1)OCC2C(C(C(C(O2)OC3=C(OC4=CC(=CC(=C4C3=O)O)O)C5=CC(=C(C=C5)O)O)O)O)O)O)O)O None
None 214580 0 3H-Methylspiperone -1 28 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 448 3 7 11 0.4 CC1C(C(C(C(O1)OC2=C(OC3=CC(=O)C=C(C3=C2O)O)C4=CC(=C(C=C4)O)O)O)O)O None
135269 214639 0 3H-NMSP -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 222 5 1 3 2.5 CCCCC(=O)OC1=CC=CC=C1C(=O)O None
23681059 214640 0 3H-NMSP -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 CC(C1=CC2=C(C=C1)C=C(C=C2)OC)C(=O)O None
5018304 214641 0 3H-NMSP -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 317 4 1 3 0.0 C1=CC=C(C(=C1)CC(=O)[O-])NC2=C(C=CC=C2Cl)Cl.[Na+] None
3672 214642 0 3H-NMSP -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 206 4 1 1 3.1 CC(C)CC1=CC=C(C=C1)C(C)C(=O)O None
84003 214643 0 3H-NMSP -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 376 6 5 7 -0.0 C1CN2C(=CC=C2C(=O)C3=CC=CC=C3)C1C(=O)O.C(C(CO)(CO)N)O None
119828 214645 0 3H-NMSP -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 5 1 5 3.5 CCC(=O)NS(=O)(=O)C1=CC=C(C=C1)C2=C(ON=C2C3=CC=CC=C3)C None
None 214703 0 3H-SPIPERONE -660 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
None 214703 0 UNDEFINED -660 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
None 214747 0 3H-NMSP -4570 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 347 6 0 3 5.0 CC(=O)N(CC1=CC=CC=C1OC)C2=CC=CC=C2OC3=CC=CC=C3 None
1577 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
164512405 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2537 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5355 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5501 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
643497 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
688272 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
958 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
960 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL196677 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL26 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL267044 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB00391 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB16021 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
135409468 2004 63 3H-NMSP -18 40 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
333 2004 63 3H-NMSP -18 40 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
CHEMBL845 2004 63 3H-NMSP -18 40 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
44395711 174327 0 UNDEFINED -5 3 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 345 3 1 2 4.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1ccc(F)cc1 None
CHEMBL456430 174327 0 UNDEFINED -5 3 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 345 3 1 2 4.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1ccc(F)cc1 None
CHEMBL537183 174327 0 UNDEFINED -5 3 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 345 3 1 2 4.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1ccc(F)cc1 None
1353 1880 85 UNDEFINED -3 85 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 UNDEFINED -3 85 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 UNDEFINED -3 85 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 UNDEFINED -3 85 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 UNDEFINED -3 85 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
2865 4079 67 3H-NMSP -66 53 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4079 67 3H-NMSP -66 53 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4079 67 3H-NMSP -66 53 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4079 67 3H-NMSP -66 53 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4079 67 3H-NMSP -66 53 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
2337 3205 72 3H-SPIPERONE -114 62 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 3H-SPIPERONE -114 62 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 3H-SPIPERONE -114 62 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 3H-SPIPERONE -114 62 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 3H-SPIPERONE -114 62 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
9906978 42466 1 UNDEFINED 1 12 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 None
CHEMBL150161 42466 1 UNDEFINED 1 12 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 None
25139329 186520 0 UNDEFINED -7 4 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 514 10 0 4 7.6 CCCN(CCCCn1cc(-c2ccc(-c3ccccc3)cc2)nn1)C1CC=C(C#Cc2ccccc2)CC1 None
CHEMBL491466 186520 0 UNDEFINED -7 4 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 514 10 0 4 7.6 CCCN(CCCCn1cc(-c2ccc(-c3ccccc3)cc2)nn1)C1CC=C(C#Cc2ccccc2)CC1 None
2274 3124 53 R-SAT -56 32 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 3124 53 R-SAT -56 32 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 3124 53 R-SAT -56 32 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 3124 53 R-SAT -56 32 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 3124 53 R-SAT -56 32 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2337 3205 72 3H-SPIPERONE -173 62 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 3H-SPIPERONE -173 62 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 3H-SPIPERONE -173 62 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 3H-SPIPERONE -173 62 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 3H-SPIPERONE -173 62 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
37459 735 10 3H-SPIPERONE -123 24 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
62 735 10 3H-SPIPERONE -123 24 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
CHEMBL8514 735 10 3H-SPIPERONE -123 24 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
1613 2316 44 3H-NMSP -2 44 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
1613 2316 44 3H-SPIPERONE -2 44 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2316 44 3H-NMSP -2 44 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2316 44 3H-SPIPERONE -2 44 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2316 44 3H-NMSP -2 44 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2316 44 3H-SPIPERONE -2 44 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2316 44 3H-NMSP -2 44 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2316 44 3H-SPIPERONE -2 44 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2316 44 3H-NMSP -2 44 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2316 44 3H-SPIPERONE -2 44 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
100 3745 52 3H-SPIPERONE -3 55 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3745 52 3H-SPIPERONE -3 55 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3745 52 3H-SPIPERONE -3 55 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3745 52 3H-SPIPERONE -3 55 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3745 52 3H-SPIPERONE -3 55 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2726 906 64 3H-SPIPERONE -10 72 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 3H-SPIPERONE -10 72 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 3H-SPIPERONE -10 72 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 3H-SPIPERONE -10 72 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 3H-SPIPERONE -10 72 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1353 1880 85 UNDEFINED -3 85 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 UNDEFINED -3 85 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 UNDEFINED -3 85 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 UNDEFINED -3 85 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 UNDEFINED -3 85 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
None 214476 0 3H-YM 09151-2 15 2 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 291 3 2 2 3.8 C1=CC=C2C(=C1)C=CC=C2NC(=O)C3=CC=CC=C3C(=O)O None
2337 3205 72 3H-NMSP -114 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 3H-NMSP -114 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 3H-NMSP -114 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 3H-NMSP -114 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 3H-NMSP -114 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
44591089 188892 0 UNDEFINED - 1 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 327 3 2 3 3.3 OC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ncccc23)C1 None
CHEMBL513776 188892 0 UNDEFINED - 1 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 327 3 2 3 3.3 OC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ncccc23)C1 None
2 3210 19 3H-SPIPERONE -2 28 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
54562 3210 19 3H-SPIPERONE -2 28 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
CHEMBL240773 3210 19 3H-SPIPERONE -2 28 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
4978 214577 0 3H-Methylspiperone -2 28 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 520 1 7 9 4.3 CC1=CC(=C2C3=C1C4=C5C(=C(C=C4CO)O)C(=O)C6=C(C=C(C7=C6C5=C3C8=C7C(=CC(=C8C2=O)O)O)O)O)O None
119570 3110 90 3H-SPIPERONE -10 40 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 3110 90 3H-SPIPERONE -10 40 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 3110 90 3H-SPIPERONE -10 40 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 3110 90 3H-SPIPERONE -10 40 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 3110 90 3H-SPIPERONE -10 40 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
6603820 95330 13 3H-SCH23390 -1 13 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
CHEMBL25856 95330 13 3H-SCH23390 -1 13 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
None 214476 0 3H-SPIPERONE 15 2 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 291 3 2 2 3.8 C1=CC=C2C(=C1)C=CC=C2NC(=O)C3=CC=CC=C3C(=O)O None
1712 2456 0 3H-SPIPERONE -3 21 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
4078 2456 0 3H-SPIPERONE -3 21 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
7227 2456 0 3H-SPIPERONE -3 21 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
CHEMBL1088 2456 0 3H-SPIPERONE -3 21 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
DB00933 2456 0 3H-SPIPERONE -3 21 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
101 3762 18 3H-SPIPERONE -21 13 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 None
55752 3762 18 3H-SPIPERONE -21 13 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL35057 3762 18 3H-SPIPERONE -21 13 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 None
279 1631 26 3H-SPIPERONE -26 17 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
49381 1631 26 3H-SPIPERONE -26 17 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
CHEMBL63756 1631 26 3H-SPIPERONE -26 17 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
5281878 1630 33 R-SAT -14 16 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 1630 33 R-SAT -14 16 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 1630 33 R-SAT -14 16 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 1630 33 R-SAT -14 16 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 1630 33 R-SAT -14 16 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 1630 33 R-SAT -14 16 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 1630 33 R-SAT -14 16 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
None 214399 0 3H-YM 09151-2 -1 4 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 233 4 1 2 3.1 CCCNC1CCC2=C(C1C)C=CC=C2OC None
3033769 3229 54 3H-YM 09151-2 -562 18 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3299 3229 54 3H-YM 09151-2 -562 18 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
94 3229 54 3H-YM 09151-2 -562 18 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
CHEMBL8809 3229 54 3H-YM 09151-2 -562 18 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
DB12518 3229 54 3H-YM 09151-2 -562 18 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
15387 214209 0 3H-YM 09151-2 -35 23 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CC1)CCCC(=O)C2=CC=C(C=C2)F None
135398745 2869 108 3H-SPIPERONE -10 65 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-SPIPERONE -10 65 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-SPIPERONE -10 65 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-SPIPERONE -10 65 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
5467 204212 40 R-SAT 6 5 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 328 8 1 5 1.2 CCN(CC)CCNC(=O)c1cc(S(C)(=O)=O)ccc1OC None
CHEMBL84158 204212 40 R-SAT 6 5 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 328 8 1 5 1.2 CCN(CC)CCNC(=O)c1cc(S(C)(=O)=O)ccc1OC None
2274 3124 53 3H-NEMONAPRIDE -56 32 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 3124 53 3H-NEMONAPRIDE -56 32 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 3124 53 3H-NEMONAPRIDE -56 32 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 3124 53 3H-NEMONAPRIDE -56 32 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 3124 53 3H-NEMONAPRIDE -56 32 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
25139332 183737 0 UNDEFINED -1 4 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 352 11 1 2 5.0 CCCN(CCC)CCCCNC(=O)c1ccc(-c2ccccc2)cc1 None
CHEMBL484204 183737 0 UNDEFINED -1 4 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 352 11 1 2 5.0 CCCN(CCC)CCCCNC(=O)c1ccc(-c2ccccc2)cc1 None
None 215619 0 UNDEFINED -380 4 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 451 3 0 7 3.9 CC1=NC2=C(C=C1)C3=C(C=C2)OCC(O3)CN4CCN(CC4)C5=NC6=C(C=C5)C=C(C=C6)C#N None
3663 99505 79 3H-Methylspiperone -42 29 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 504 0 6 8 5.1 Cc1cc(O)c2c(=O)c3c(O)cc(O)c4c5c(O)cc(O)c6c(=O)c7c(O)cc(C)c8c1c2c(c34)c(c78)c65 None
CHEMBL286494 99505 79 3H-Methylspiperone -42 29 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 504 0 6 8 5.1 Cc1cc(O)c2c(=O)c3c(O)cc(O)c4c5c(O)cc(O)c6c(=O)c7c(O)cc(C)c8c1c2c(c34)c(c78)c65 None
1353 1880 85 3H-NMSP -3 85 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-NMSP -3 85 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-NMSP -3 85 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-NMSP -3 85 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-NMSP -3 85 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
135398745 2869 108 3H-SPIPERONE -7 65 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-SPIPERONE -7 65 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-SPIPERONE -7 65 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-SPIPERONE -7 65 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
2726 906 64 3H-YM 09151-2 -8 72 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 3H-YM 09151-2 -8 72 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 3H-YM 09151-2 -8 72 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 3H-YM 09151-2 -8 72 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 3H-YM 09151-2 -8 72 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
133633 2210 46 UNDEFINED -104 8 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 None
177 2210 46 UNDEFINED -104 8 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 None
CHEMBL445102 2210 46 UNDEFINED -104 8 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 None
2435 3533 78 3H-NEMONAPRIDE -10 48 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3533 78 3H-NEMONAPRIDE -10 48 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3533 78 3H-NEMONAPRIDE -10 48 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3533 78 3H-NEMONAPRIDE -10 48 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3533 78 3H-NEMONAPRIDE -10 48 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
104911 214249 0 3H-NMSP -67 36 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 530 7 0 5 5.1 COC1=CC=CC=C1N2CCN(CC2)CCN(C3=CC=CC=N3)C(=O)C4CCCCC4.Cl.Cl.Cl None
2389 3279 114 3H-SPIPERONE -28 67 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 3H-SPIPERONE -28 67 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 3H-SPIPERONE -28 67 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 3H-SPIPERONE -28 67 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 3H-SPIPERONE -28 67 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2337 3205 72 3H-NEMONAPRIDE -114 62 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 3H-NEMONAPRIDE -114 62 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 3H-NEMONAPRIDE -114 62 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 3H-NEMONAPRIDE -114 62 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 3H-NEMONAPRIDE -114 62 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
6852400 214160 0 R-SAT -794 21 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
73759726 214160 0 R-SAT -794 21 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
209 3008 94 UNDEFINED -30 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 3008 94 UNDEFINED -30 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 3008 94 UNDEFINED -30 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 3008 94 UNDEFINED -30 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 3008 94 UNDEFINED -30 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
100 3745 52 3H-NMSP -8 55 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3745 52 3H-NMSP -8 55 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3745 52 3H-NMSP -8 55 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3745 52 3H-NMSP -8 55 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3745 52 3H-NMSP -8 55 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
44395741 180999 0 UNDEFINED 1 10 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
CHEMBL476935 180999 0 UNDEFINED 1 10 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
CHEMBL558392 180999 0 UNDEFINED 1 10 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
44395741 180999 0 UNDEFINED 1 10 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
CHEMBL476935 180999 0 UNDEFINED 1 10 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
CHEMBL558392 180999 0 UNDEFINED 1 10 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
44350664 117646 0 UNDEFINED -1 6 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 6 0 2 5.2 O=C(CCCN1C2CCC1CC(c1ccccc1)C2)c1ccc(F)cc1 None
CHEMBL340816 117646 0 UNDEFINED -1 6 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 6 0 2 5.2 O=C(CCCN1C2CCC1CC(c1ccccc1)C2)c1ccc(F)cc1 None
CHEMBL553417 117646 0 UNDEFINED -1 6 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 6 0 2 5.2 O=C(CCCN1C2CCC1CC(c1ccccc1)C2)c1ccc(F)cc1 None
2389 3279 114 3H-NEMONAPRIDE -21 67 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2389 3279 114 R-SAT -21 67 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 3H-NEMONAPRIDE -21 67 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 R-SAT -21 67 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 3H-NEMONAPRIDE -21 67 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 R-SAT -21 67 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 3H-NEMONAPRIDE -21 67 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 R-SAT -21 67 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 3H-NEMONAPRIDE -21 67 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 R-SAT -21 67 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
103 4089 56 3H-NMSP -17 53 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4089 56 3H-NMSP -17 53 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4089 56 3H-NMSP -17 53 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4089 56 3H-NMSP -17 53 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4089 56 3H-NMSP -17 53 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2389 3279 114 3H-NMSP -21 67 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 3H-NMSP -21 67 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 3H-NMSP -21 67 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 3H-NMSP -21 67 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 3H-NMSP -21 67 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
44591045 176163 0 UNDEFINED 19 3 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 340 3 1 3 3.9 Clc1ccc(N2CCCN(Cc3c[nH]c4ncccc34)CC2)cc1 None
CHEMBL460223 176163 0 UNDEFINED 19 3 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 340 3 1 3 3.9 Clc1ccc(N2CCCN(Cc3c[nH]c4ncccc34)CC2)cc1 None
25139478 184373 0 UNDEFINED -138 4 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 510 10 0 4 7.5 CCCN(CCCCn1cc(-c2ccc(-c3ccccc3)cc2)nn1)C1CC=C(C#C[Si](C)(C)C)CC1 None
CHEMBL485384 184373 0 UNDEFINED -138 4 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 510 10 0 4 7.5 CCCN(CCCCn1cc(-c2ccc(-c3ccccc3)cc2)nn1)C1CC=C(C#C[Si](C)(C)C)CC1 None
135398745 2869 108 3H-NMSP -10 65 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-NMSP -10 65 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-NMSP -10 65 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-NMSP -10 65 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
214 3799 52 3H-SPIPERONE -22 29 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 3799 52 3H-SPIPERONE -22 29 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 3799 52 3H-SPIPERONE -22 29 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 3799 52 3H-SPIPERONE -22 29 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 3799 52 3H-SPIPERONE -22 29 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 3799 52 3H-SPIPERONE -22 29 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
None 214591 0 3H-SPIPERONE -3 19 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 246 2 1 4 1.6 CCCN1CCCC2C1CC3=CN=C(N=C3C2)N None
13091273 181856 0 UNDEFINED -8 6 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 367 6 1 3 4.3 O=C(CCCN1C2CCC1CC(O)(c1ccccc1)C2)c1ccc(F)cc1 None
CHEMBL478617 181856 0 UNDEFINED -8 6 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 367 6 1 3 4.3 O=C(CCCN1C2CCC1CC(O)(c1ccccc1)C2)c1ccc(F)cc1 None
CHEMBL553327 181856 0 UNDEFINED -8 6 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 367 6 1 3 4.3 O=C(CCCN1C2CCC1CC(O)(c1ccccc1)C2)c1ccc(F)cc1 None
25139479 183735 0 UNDEFINED -21 4 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 438 10 0 4 6.2 C#CC1=CCC(N(CCC)CCCCn2cc(-c3ccc(-c4ccccc4)cc3)nn2)CC1 None
CHEMBL484202 183735 0 UNDEFINED -21 4 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 438 10 0 4 6.2 C#CC1=CCC(N(CCC)CCCCn2cc(-c3ccc(-c4ccccc4)cc3)nn2)CC1 None
191 399 92 UNDEFINED -8 28 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
201 399 92 UNDEFINED -8 28 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2170 399 92 UNDEFINED -8 28 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
CHEMBL1113 399 92 UNDEFINED -8 28 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
DB00543 399 92 UNDEFINED -8 28 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
1353 1880 85 3H-SPIPERONE -3 85 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-SPIPERONE -3 85 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-SPIPERONE -3 85 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-SPIPERONE -3 85 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-SPIPERONE -3 85 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
135398745 2869 108 3H-SPIPERONE -10 65 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-SPIPERONE -10 65 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-SPIPERONE -10 65 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-SPIPERONE -10 65 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
4249 77814 30 UNDEFINED -7 5 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 355 6 1 3 4.1 Cc1ccc(C2(O)CCN(CCCC(=O)c3ccc(F)cc3)CC2)cc1 None
CHEMBL2104700 77814 30 UNDEFINED -7 5 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 355 6 1 3 4.1 Cc1ccc(C2(O)CCN(CCCC(=O)c3ccc(F)cc3)CC2)cc1 None
1353 1880 85 3H-SPIPERONE -4 85 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-SPIPERONE -4 85 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-SPIPERONE -4 85 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-SPIPERONE -4 85 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-SPIPERONE -4 85 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3294 1975 106 UNDEFINED -11 44 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 1975 106 UNDEFINED -11 44 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 1975 106 UNDEFINED -11 44 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 1975 106 UNDEFINED -11 44 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 1975 106 UNDEFINED -11 44 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
1353 1880 85 3H-NEMONAPRIDE -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 1880 85 3H-YM 09151-2 -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-NEMONAPRIDE -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-YM 09151-2 -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-NEMONAPRIDE -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-YM 09151-2 -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-NEMONAPRIDE -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-YM 09151-2 -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-NEMONAPRIDE -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-YM 09151-2 -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
2726 906 64 3H-SCH23390 -10 72 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 3H-SCH23390 -10 72 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 3H-SCH23390 -10 72 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 3H-SCH23390 -10 72 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 3H-SCH23390 -10 72 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
135409468 2004 63 UNDEFINED -18 40 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
333 2004 63 UNDEFINED -18 40 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
CHEMBL845 2004 63 UNDEFINED -18 40 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
1577 3647 104 3H-SPIPERONE -8 25 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
164512405 3647 104 3H-SPIPERONE -8 25 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2537 3647 104 3H-SPIPERONE -8 25 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5355 3647 104 3H-SPIPERONE -8 25 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5501 3647 104 3H-SPIPERONE -8 25 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
643497 3647 104 3H-SPIPERONE -8 25 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
688272 3647 104 3H-SPIPERONE -8 25 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
958 3647 104 3H-SPIPERONE -8 25 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
960 3647 104 3H-SPIPERONE -8 25 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL196677 3647 104 3H-SPIPERONE -8 25 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL26 3647 104 3H-SPIPERONE -8 25 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL267044 3647 104 3H-SPIPERONE -8 25 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB00391 3647 104 3H-SPIPERONE -8 25 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB16021 3647 104 3H-SPIPERONE -8 25 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
None 214240 0 3H-SPIPERONE 3 2 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 310 3 0 2 4.8 CN(C)CCC=C1C2=CC=CC=C2C=NC3=C1C=C(C=C3)Cl None
1577 3647 104 UNDEFINED -8 25 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
164512405 3647 104 UNDEFINED -8 25 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2537 3647 104 UNDEFINED -8 25 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5355 3647 104 UNDEFINED -8 25 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5501 3647 104 UNDEFINED -8 25 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
643497 3647 104 UNDEFINED -8 25 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
688272 3647 104 UNDEFINED -8 25 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
958 3647 104 UNDEFINED -8 25 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
960 3647 104 UNDEFINED -8 25 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL196677 3647 104 UNDEFINED -8 25 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL26 3647 104 UNDEFINED -8 25 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL267044 3647 104 UNDEFINED -8 25 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB00391 3647 104 UNDEFINED -8 25 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB16021 3647 104 UNDEFINED -8 25 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2337 3205 72 3H-SPIPERONE -114 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2337 3205 72 3H-SPIPERONE -173 62 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 3H-SPIPERONE -114 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 3H-SPIPERONE -173 62 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 3H-SPIPERONE -114 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 3H-SPIPERONE -173 62 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 3H-SPIPERONE -114 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 3H-SPIPERONE -173 62 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 3H-SPIPERONE -114 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 3H-SPIPERONE -173 62 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
1577 3647 104 3H-NEMONAPRIDE -8 25 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
164512405 3647 104 3H-NEMONAPRIDE -8 25 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2537 3647 104 3H-NEMONAPRIDE -8 25 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5355 3647 104 3H-NEMONAPRIDE -8 25 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5501 3647 104 3H-NEMONAPRIDE -8 25 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
643497 3647 104 3H-NEMONAPRIDE -8 25 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
688272 3647 104 3H-NEMONAPRIDE -8 25 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
958 3647 104 3H-NEMONAPRIDE -8 25 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
960 3647 104 3H-NEMONAPRIDE -8 25 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL196677 3647 104 3H-NEMONAPRIDE -8 25 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL26 3647 104 3H-NEMONAPRIDE -8 25 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL267044 3647 104 3H-NEMONAPRIDE -8 25 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB00391 3647 104 3H-NEMONAPRIDE -8 25 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB16021 3647 104 3H-NEMONAPRIDE -8 25 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
11954259 214201 0 3H-NMSP -676 43 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
135398737 944 89 3H-SPIPERONE -13 91 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 944 89 3H-SPIROPERIDOL -13 91 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-SPIPERONE -13 91 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-SPIROPERIDOL -13 91 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-SPIPERONE -13 91 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-SPIROPERIDOL -13 91 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-SPIPERONE -13 91 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-SPIROPERIDOL -13 91 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-SPIPERONE -13 91 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-SPIROPERIDOL -13 91 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
279 1631 26 UNDEFINED -4 17 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
49381 1631 26 UNDEFINED -4 17 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
CHEMBL63756 1631 26 UNDEFINED -4 17 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
1577 3647 104 3H-SPIPERONE -8 25 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
164512405 3647 104 3H-SPIPERONE -8 25 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2537 3647 104 3H-SPIPERONE -8 25 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5355 3647 104 3H-SPIPERONE -8 25 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5501 3647 104 3H-SPIPERONE -8 25 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
643497 3647 104 3H-SPIPERONE -8 25 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
688272 3647 104 3H-SPIPERONE -8 25 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
958 3647 104 3H-SPIPERONE -8 25 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
960 3647 104 3H-SPIPERONE -8 25 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL196677 3647 104 3H-SPIPERONE -8 25 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL26 3647 104 3H-SPIPERONE -8 25 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL267044 3647 104 3H-SPIPERONE -8 25 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB00391 3647 104 3H-SPIPERONE -8 25 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB16021 3647 104 3H-SPIPERONE -8 25 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
21830793 91403 5 3H-8-OH-DPAT -144 46 Bovine 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
CHEMBL2413154 91403 5 3H-8-OH-DPAT -144 46 Bovine 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
44578445 180997 0 UNDEFINED -13 3 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 352 6 0 3 4.1 O=C(CCCN1CC2CCC(C1)N2c1ccccc1)c1ccc(F)cc1 None
CHEMBL476933 180997 0 UNDEFINED -13 3 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 352 6 0 3 4.1 O=C(CCCN1CC2CCC(C1)N2c1ccccc1)c1ccc(F)cc1 None
135398737 944 89 3H-SPIPERONE -13 91 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 944 89 3H-SPIPERONE -7 91 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-SPIPERONE -13 91 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-SPIPERONE -7 91 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-SPIPERONE -13 91 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-SPIPERONE -7 91 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-SPIPERONE -13 91 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-SPIPERONE -7 91 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-SPIPERONE -13 91 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-SPIPERONE -7 91 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1353 1880 85 R-SAT -3 85 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 R-SAT -3 85 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 R-SAT -3 85 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 R-SAT -3 85 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 R-SAT -3 85 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
44134711 214215 0 3H-SPIPERONE -275 13 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 340 6 2 4 2.8 CCC1=CC(=C(C(=C1O)C(=O)NCC2CCCN2CC)OC)Cl None
100 3745 52 3H-YM 09151-2 -8 55 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3745 52 3H-YM 09151-2 -8 55 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3745 52 3H-YM 09151-2 -8 55 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3745 52 3H-YM 09151-2 -8 55 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3745 52 3H-YM 09151-2 -8 55 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2337 3205 72 UNDEFINED -114 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 UNDEFINED -114 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 UNDEFINED -114 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 UNDEFINED -114 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 UNDEFINED -114 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
54477 84230 34 3H-NEMONAPRIDE -14 22 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
CHEMBL22242 84230 34 3H-NEMONAPRIDE -14 22 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
2337 3205 72 3H-N-Methylspiperone -114 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 3H-N-Methylspiperone -114 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 3H-N-Methylspiperone -114 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 3H-N-Methylspiperone -114 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 3H-N-Methylspiperone -114 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
None 214880 0 UNDEFINED -102 3 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 453 10 0 7 4.2 CCOC1=CC=CC=C1N2CCN(CC2)CCCC3CC(=NO3)C4=CC(=C(C=C4)OC)OC None
2726 906 64 3H-NEMONAPRIDE -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 3H-NEMONAPRIDE -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 3H-NEMONAPRIDE -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 3H-NEMONAPRIDE -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 3H-NEMONAPRIDE -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1212 1632 45 3H-NEMONAPRIDE -77 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1632 45 3H-NEMONAPRIDE -77 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1632 45 3H-NEMONAPRIDE -77 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1632 45 3H-NEMONAPRIDE -77 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1632 45 3H-NEMONAPRIDE -77 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
65750 214699 0 R-SAT -1 3 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 346 6 0 3 5.7 CCN(CC)CCCN1C2=CC=CC=C2SC3=C1C=C(C=C3)Cl None
15387 214209 0 3H-SPIPERONE -33 23 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CC1)CCCC(=O)C2=CC=C(C=C2)F None
243 3153 85 3H-SPIPERONE -12 34 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3052762 3153 85 3H-SPIPERONE -12 34 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3502 3153 85 3H-SPIPERONE -12 34 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
CHEMBL117287 3153 85 3H-SPIPERONE -12 34 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
DB06480 3153 85 3H-SPIPERONE -12 34 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
179 396 107 3H-NMSP -50 50 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 396 107 3H-NMSP -50 50 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 396 107 3H-NMSP -50 50 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 396 107 3H-NMSP -50 50 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 396 107 3H-NMSP -50 50 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
3033769 3229 54 3H-SPIPERONE -288 18 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3299 3229 54 3H-SPIPERONE -288 18 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
94 3229 54 3H-SPIPERONE -288 18 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
CHEMBL8809 3229 54 3H-SPIPERONE -288 18 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
DB12518 3229 54 3H-SPIPERONE -288 18 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
2726 906 64 3H-NMSP -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
2726 906 64 R-SAT -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 3H-NMSP -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 R-SAT -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 3H-NMSP -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 R-SAT -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 3H-NMSP -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 R-SAT -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 3H-NMSP -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 R-SAT -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1830 2552 39 3H-SPIPERONE -120 27 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
1830 2552 39 UNDEFINED -120 27 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 2552 39 3H-SPIPERONE -120 27 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 2552 39 UNDEFINED -120 27 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 2552 39 3H-SPIPERONE -120 27 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 2552 39 UNDEFINED -120 27 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 2552 39 3H-SPIPERONE -120 27 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 2552 39 UNDEFINED -120 27 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 2552 39 3H-SPIPERONE -120 27 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 2552 39 UNDEFINED -120 27 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
3033769 3229 54 3H-SPIPERONE -562 18 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3033769 3229 54 3H-SPIPERONE -288 18 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3299 3229 54 3H-SPIPERONE -562 18 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3299 3229 54 3H-SPIPERONE -288 18 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
94 3229 54 3H-SPIPERONE -562 18 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
94 3229 54 3H-SPIPERONE -288 18 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
CHEMBL8809 3229 54 3H-SPIPERONE -562 18 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
CHEMBL8809 3229 54 3H-SPIPERONE -288 18 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
DB12518 3229 54 3H-SPIPERONE -562 18 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
DB12518 3229 54 3H-SPIPERONE -288 18 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
54477 84230 34 3H-SPIPERONE -14 22 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
CHEMBL22242 84230 34 3H-SPIPERONE -14 22 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
9906978 42466 1 UNDEFINED 1 12 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 None
CHEMBL150161 42466 1 UNDEFINED 1 12 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 None
3294 1975 106 3H-SPIPERONE -11 44 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 1975 106 3H-SPIPERONE -11 44 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 1975 106 3H-SPIPERONE -11 44 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 1975 106 3H-SPIPERONE -11 44 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 1975 106 3H-SPIPERONE -11 44 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
100 3745 52 3H-NEMONAPRIDE -8 55 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3745 52 3H-NEMONAPRIDE -8 55 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3745 52 3H-NEMONAPRIDE -8 55 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3745 52 3H-NEMONAPRIDE -8 55 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3745 52 3H-NEMONAPRIDE -8 55 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
242 467 117 3H-Methylspiperone -87 51 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 467 117 3H-Methylspiperone -87 51 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 467 117 3H-Methylspiperone -87 51 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 467 117 3H-Methylspiperone -87 51 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 467 117 3H-Methylspiperone -87 51 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
135398745 2869 108 3H-SPIPERONE -10 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-SPIPERONE -10 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-SPIPERONE -10 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-SPIPERONE -10 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
4249 77814 30 R-SAT -7 5 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 355 6 1 3 4.1 Cc1ccc(C2(O)CCN(CCCC(=O)c3ccc(F)cc3)CC2)cc1 None
CHEMBL2104700 77814 30 R-SAT -7 5 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 355 6 1 3 4.1 Cc1ccc(C2(O)CCN(CCCC(=O)c3ccc(F)cc3)CC2)cc1 None
44134711 214215 0 3H-SPIPERONE -275 13 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 340 6 2 4 2.8 CCC1=CC(=C(C(=C1O)C(=O)NCC2CCCN2CC)OC)Cl None
44591042 176237 0 UNDEFINED -15 3 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 380 4 2 2 4.9 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCc1c[nH]c2ccccc12 None
CHEMBL460854 176237 0 UNDEFINED -15 3 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 380 4 2 2 4.9 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCc1c[nH]c2ccccc12 None
2435 3533 78 R-SAT -10 48 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3533 78 R-SAT -10 48 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3533 78 R-SAT -10 48 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3533 78 R-SAT -10 48 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3533 78 R-SAT -10 48 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
135398737 944 89 3H-YM 09151-2 -13 91 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-YM 09151-2 -13 91 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-YM 09151-2 -13 91 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-YM 09151-2 -13 91 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-YM 09151-2 -13 91 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
163839 2910 0 3H-Methylspiperone -15 7 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 391 6 1 4 3.7 Cc1cccc(c1C)N1CCN(CC1)CCCOc1ccc2c(c1)[nH]c(=O)cc2 None
268 2910 0 3H-Methylspiperone -15 7 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 391 6 1 4 3.7 Cc1cccc(c1C)N1CCN(CC1)CCCOc1ccc2c(c1)[nH]c(=O)cc2 None
CHEMBL55171 2910 0 3H-Methylspiperone -15 7 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 391 6 1 4 3.7 Cc1cccc(c1C)N1CCN(CC1)CCCOc1ccc2c(c1)[nH]c(=O)cc2 None
54477 84230 34 3H-SPIPERONE -14 22 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
54477 84230 34 UNDEFINED -14 22 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
54477 84230 34 3H-SPIPERONE -38 22 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
CHEMBL22242 84230 34 3H-SPIPERONE -14 22 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
CHEMBL22242 84230 34 UNDEFINED -14 22 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
CHEMBL22242 84230 34 3H-SPIPERONE -38 22 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
31101 720 39 3H-SPIPERONE -186 35 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 720 39 3H-SPIPERONE -186 35 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 720 39 3H-SPIPERONE -186 35 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 720 39 3H-SPIPERONE -186 35 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 720 39 3H-SPIPERONE -186 35 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
135398737 944 89 3H-Methylspiperone -7 91 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-Methylspiperone -7 91 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-Methylspiperone -7 91 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-Methylspiperone -7 91 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-Methylspiperone -7 91 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1613 2316 44 3H-YM 09151-2 -2 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2316 44 3H-YM 09151-2 -2 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2316 44 3H-YM 09151-2 -2 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2316 44 3H-YM 09151-2 -2 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2316 44 3H-YM 09151-2 -2 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
119570 3110 90 3H-NMSP -10 40 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 3110 90 3H-NMSP -10 40 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 3110 90 3H-NMSP -10 40 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 3110 90 3H-NMSP -10 40 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 3110 90 3H-NMSP -10 40 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
135398745 2869 108 3H-SCH23390 -10 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-SCH23390 -10 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-SCH23390 -10 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-SCH23390 -10 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
3033769 3229 54 3H-SPIPERONE -562 18 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3299 3229 54 3H-SPIPERONE -562 18 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
94 3229 54 3H-SPIPERONE -562 18 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
CHEMBL8809 3229 54 3H-SPIPERONE -562 18 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
DB12518 3229 54 3H-SPIPERONE -562 18 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
1353 1880 85 3H-SPIPERONE -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-SPIPERONE -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-SPIPERONE -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-SPIPERONE -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-SPIPERONE -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 1880 85 UNDEFINED -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 UNDEFINED -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 UNDEFINED -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 UNDEFINED -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 UNDEFINED -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 1880 85 3H-N-Methylspiperone -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-N-Methylspiperone -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-N-Methylspiperone -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-N-Methylspiperone -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-N-Methylspiperone -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
None 214477 0 3H-YM 09151-2 -3 2 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 359 1 2 2 3.7 CC(C)(C)C(=O)NC1CC2C(CC3=C(NC4=CC=CC2=C34)Cl)N(C1)C None
3691783 4696 1 UNDEFINED 47 3 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 318 4 1 3 3.4 c1ccc(-c2nc(CN3CCN(c4ccccc4)CC3)c[nH]2)cc1 None
CHEMBL103871 4696 1 UNDEFINED 47 3 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 318 4 1 3 3.4 c1ccc(-c2nc(CN3CCN(c4ccccc4)CC3)c[nH]2)cc1 None
9906978 42466 1 UNDEFINED 1 12 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 None
CHEMBL150161 42466 1 UNDEFINED 1 12 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 None
None 214360 0 3H-SPIPERONE 758 7 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 401 5 1 5 2.2 C1COC(C2=CC=CC=C21)CCN3CCN(CC3)C4=CC=C(C=C4)S(=O)(=O)N None
2470 3596 46 R-SAT -20 59 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3596 46 R-SAT -20 59 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3596 46 R-SAT -20 59 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3596 46 R-SAT -20 59 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3596 46 R-SAT -20 59 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
100 3745 52 3H-SPIPERONE -3 55 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3745 52 3H-SPIPERONE -3 55 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3745 52 3H-SPIPERONE -3 55 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3745 52 3H-SPIPERONE -3 55 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3745 52 3H-SPIPERONE -3 55 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
135398737 944 89 3H-SPIROPERIDOL -13 91 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-SPIROPERIDOL -13 91 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-SPIROPERIDOL -13 91 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-SPIROPERIDOL -13 91 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-SPIROPERIDOL -13 91 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1212 1632 45 3H-SPIPERONE -77 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1632 45 3H-SPIPERONE -77 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1632 45 3H-SPIPERONE -77 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1632 45 3H-SPIPERONE -77 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1632 45 3H-SPIPERONE -77 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
135398745 2869 108 3H-NEMONAPRIDE -10 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-NEMONAPRIDE -10 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-NEMONAPRIDE -10 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-NEMONAPRIDE -10 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
16362 3076 67 3H-SPIPERONE -186 29 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 3076 67 3H-SPIPERONE -186 29 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 3076 67 3H-SPIPERONE -186 29 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 3076 67 3H-SPIPERONE -186 29 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 3076 67 3H-SPIPERONE -186 29 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
5074 3280 75 UNDEFINED -56 29 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3280 75 UNDEFINED -56 29 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3280 75 UNDEFINED -56 29 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3280 75 UNDEFINED -56 29 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
16106 117643 28 3H-SPIPERONE -1 11 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
16106 117643 28 UNDEFINED -1 11 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
CHEMBL340801 117643 28 3H-SPIPERONE -1 11 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
CHEMBL340801 117643 28 UNDEFINED -1 11 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
None 214668 0 3H-SPIPERONE -100 6 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 453 8 1 4 4.6 COC1=CC=CC=C1N2CCN(CC2)CCCCNC(=O)C3=CC4=CC=CC=C4C=C3.Cl None
2337 3205 72 3H-SPIPERONE -114 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2337 3205 72 UNDEFINED -114 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 3H-SPIPERONE -114 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 UNDEFINED -114 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 3H-SPIPERONE -114 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 UNDEFINED -114 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 3H-SPIPERONE -114 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 UNDEFINED -114 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 3H-SPIPERONE -114 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 UNDEFINED -114 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
None 215425 0 UNDEFINED -120 3 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 366 3 2 2 4.8 C1CC2CC(CC1N2CC3=CNC4=CC=CC=C43)(C5=CC=C(C=C5)Cl)O None
2202 3083 91 3H-SPIPERONE -2 21 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
4850 3083 91 3H-SPIPERONE -2 21 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
49 3083 91 3H-SPIPERONE -2 21 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
CHEMBL1371770 3083 91 3H-SPIPERONE -2 21 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
DB12478 3083 91 3H-SPIPERONE -2 21 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
135398745 2869 108 R-SAT -10 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 R-SAT -10 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 R-SAT -10 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 R-SAT -10 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
33630 178379 94 3H-SPIPERONE -5 27 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
CHEMBL47050 178379 94 3H-SPIPERONE -5 27 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
25139180 183759 0 UNDEFINED -10 4 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 490 10 1 2 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CC=C(C#Cc2ccccc2)CC1 None
CHEMBL484357 183759 0 UNDEFINED -10 4 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 490 10 1 2 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CC=C(C#Cc2ccccc2)CC1 None
135398737 944 89 3H-SPIPERONE -7 91 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-SPIPERONE -7 91 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-SPIPERONE -7 91 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-SPIPERONE -7 91 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-SPIPERONE -7 91 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
209 3008 94 3H-SPIPERONE -30 23 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 3008 94 3H-SPIPERONE -30 23 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 3008 94 3H-SPIPERONE -30 23 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 3008 94 3H-SPIPERONE -30 23 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 3008 94 3H-SPIPERONE -30 23 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2865 4079 67 UNDEFINED -66 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4079 67 UNDEFINED -66 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4079 67 UNDEFINED -66 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4079 67 UNDEFINED -66 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4079 67 UNDEFINED -66 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
214 3799 52 3H-YM 09151-2 -33 29 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 3799 52 3H-YM 09151-2 -33 29 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 3799 52 3H-YM 09151-2 -33 29 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 3799 52 3H-YM 09151-2 -33 29 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 3799 52 3H-YM 09151-2 -33 29 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 3799 52 3H-YM 09151-2 -33 29 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2865 4079 67 3H-N-Methylspiperone -66 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4079 67 3H-N-Methylspiperone -66 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4079 67 3H-N-Methylspiperone -66 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4079 67 3H-N-Methylspiperone -66 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4079 67 3H-N-Methylspiperone -66 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
5567 42556 24 R-SAT -11 7 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 409 6 1 3 4.8 O=C(CCCN1CCC(O)(c2cccc(C(F)(F)F)c2)CC1)c1ccc(F)cc1 None
CHEMBL15023 42556 24 R-SAT -11 7 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 409 6 1 3 4.8 O=C(CCCN1CCC(O)(c2cccc(C(F)(F)F)c2)CC1)c1ccc(F)cc1 None
2 3210 19 3H-SPIPERONE -2 28 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
54562 3210 19 3H-SPIPERONE -2 28 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
CHEMBL240773 3210 19 3H-SPIPERONE -2 28 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
104870 98423 39 3H-SPIPERONE -2 21 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
5374 98423 39 3H-SPIPERONE -2 21 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
CHEMBL279085 98423 39 3H-SPIPERONE -2 21 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
2 3210 19 3H-SPIPERONE -2 28 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
54562 3210 19 3H-SPIPERONE -2 28 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
CHEMBL240773 3210 19 3H-SPIPERONE -2 28 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
135398737 944 89 3H-SPIPERONE -13 91 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-SPIPERONE -13 91 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-SPIPERONE -13 91 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-SPIPERONE -13 91 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-SPIPERONE -13 91 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
31101 720 39 3H-SPIPERONE -489 35 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 720 39 3H-SPIPERONE -489 35 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 720 39 3H-SPIPERONE -489 35 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 720 39 3H-SPIPERONE -489 35 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 720 39 3H-SPIPERONE -489 35 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
1830 2552 39 3H-SPIPERONE -120 27 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 2552 39 3H-SPIPERONE -120 27 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 2552 39 3H-SPIPERONE -120 27 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 2552 39 3H-SPIPERONE -120 27 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 2552 39 3H-SPIPERONE -120 27 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
3036864 201066 16 3H-SPIPERONE -14791 27 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 201066 16 3H-SPIPERONE -14791 27 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 201066 16 3H-SPIPERONE -14791 27 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 201066 16 3H-SPIPERONE -14791 27 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
1212 1632 45 3H-NMSP -77 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1632 45 3H-NMSP -77 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1632 45 3H-NMSP -77 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1632 45 3H-NMSP -77 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1632 45 3H-NMSP -77 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
54477 84230 34 3H-SPIPERONE -14 22 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
CHEMBL22242 84230 34 3H-SPIPERONE -14 22 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
2726 906 64 3H-SPIPERONE -10 72 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 3H-SPIPERONE -10 72 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 3H-SPIPERONE -10 72 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 3H-SPIPERONE -10 72 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 3H-SPIPERONE -10 72 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
31101 720 39 3H-SPIPERONE -186 35 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 720 39 3H-SPIPERONE -186 35 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 720 39 3H-SPIPERONE -186 35 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 720 39 3H-SPIPERONE -186 35 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 720 39 3H-SPIPERONE -186 35 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
6917970 3635 54 3H-NMSP -851 34 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
8370 3635 54 3H-NMSP -851 34 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
CHEMBL487387 3635 54 3H-NMSP -851 34 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
37459 735 10 3H-SPIPERONE -123 24 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
62 735 10 3H-SPIPERONE -123 24 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
CHEMBL8514 735 10 3H-SPIPERONE -123 24 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
135398737 944 89 3H-NMSP -13 91 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-NMSP -13 91 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-NMSP -13 91 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-NMSP -13 91 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-NMSP -13 91 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
214 3799 52 3H-SPIPERONE -33 29 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 3799 52 3H-SPIPERONE -33 29 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 3799 52 3H-SPIPERONE -33 29 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 3799 52 3H-SPIPERONE -33 29 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 3799 52 3H-SPIPERONE -33 29 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 3799 52 3H-SPIPERONE -33 29 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
None 214668 0 3H-SPIPERONE -100 6 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 453 8 1 4 4.6 COC1=CC=CC=C1N2CCN(CC2)CCCCNC(=O)C3=CC4=CC=CC=C4C=C3.Cl None
None 214479 0 3H-SPIPERONE 1 4 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 226 0 2 2 1.4 C1CCC(=O)NCCCCCC(=O)NCC1 None
186 1777 47 3H-NMSP -512 16 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
71781 1777 47 3H-NMSP -512 16 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
CHEMBL18972 1777 47 3H-NMSP -512 16 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
30137 2833 0 3H-SPIPERONE -10 10 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
8594 2833 0 3H-SPIPERONE -10 10 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
934 2833 0 3H-SPIPERONE -10 10 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
2470 3596 46 3H-SPIPERONE -20 59 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3596 46 3H-SPIPERONE -20 59 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3596 46 3H-SPIPERONE -20 59 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3596 46 3H-SPIPERONE -20 59 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3596 46 3H-SPIPERONE -20 59 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
25139181 183760 0 UNDEFINED -2 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 414 10 1 2 5.7 C#CC1=CCC(N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 None
CHEMBL484358 183760 0 UNDEFINED -2 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 414 10 1 2 5.7 C#CC1=CCC(N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 None
25058166 214181 0 3H-SPIPERONE -8 26 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 214181 0 3H-SPIPERONE -8 26 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
2389 3279 114 3H-SPIPERONE -21 67 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 3H-SPIPERONE -21 67 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 3H-SPIPERONE -21 67 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 3H-SPIPERONE -21 67 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 3H-SPIPERONE -21 67 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
37459 735 10 UNDEFINED -123 24 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
62 735 10 UNDEFINED -123 24 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
CHEMBL8514 735 10 UNDEFINED -123 24 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
71240 205983 10 R-SAT -9 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 408 4 1 3 4.0 OCCN1CCN([C@@H]2C[C@@H](c3ccc(F)cc3)c3ccc(C(F)(F)F)cc32)CC1 None
CHEMBL95636 205983 10 R-SAT -9 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 408 4 1 3 4.0 OCCN1CCN([C@@H]2C[C@@H](c3ccc(F)cc3)c3ccc(C(F)(F)F)cc32)CC1 None
1588 2294 24 3H-SPIPERONE -23 43 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2294 24 3H-SPIPERONE -23 43 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2294 24 3H-SPIPERONE -23 43 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2294 24 3H-SPIPERONE -23 43 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2294 24 3H-SPIPERONE -23 43 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
1613 2316 44 3H-SPIROPERIDOL -2 44 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2316 44 3H-SPIROPERIDOL -2 44 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2316 44 3H-SPIROPERIDOL -2 44 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2316 44 3H-SPIROPERIDOL -2 44 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2316 44 3H-SPIROPERIDOL -2 44 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
191 399 92 R-SAT -8 28 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
201 399 92 R-SAT -8 28 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2170 399 92 R-SAT -8 28 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
CHEMBL1113 399 92 R-SAT -8 28 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
DB00543 399 92 R-SAT -8 28 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
37459 735 10 3H-SPIPERONE -123 24 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
62 735 10 3H-SPIPERONE -123 24 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
CHEMBL8514 735 10 3H-SPIPERONE -123 24 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
135398737 944 89 3H-NEMONAPRIDE -13 91 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-NEMONAPRIDE -13 91 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-NEMONAPRIDE -13 91 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-NEMONAPRIDE -13 91 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-NEMONAPRIDE -13 91 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
214 3799 52 3H-NEMONAPRIDE -33 29 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 3799 52 3H-NEMONAPRIDE -33 29 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 3799 52 3H-NEMONAPRIDE -33 29 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 3799 52 3H-NEMONAPRIDE -33 29 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 3799 52 3H-NEMONAPRIDE -33 29 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 3799 52 3H-NEMONAPRIDE -33 29 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
135398737 944 89 3H-SPIPERONE -13 91 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-SPIPERONE -13 91 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-SPIPERONE -13 91 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-SPIPERONE -13 91 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-SPIPERONE -13 91 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
11545813 180612 0 UNDEFINED 4 7 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 400 6 0 3 5.2 O=C(CCCN1C2CCC1CN(c1ccc(Cl)cc1)CC2)c1ccc(F)cc1 None
CHEMBL476109 180612 0 UNDEFINED 4 7 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 400 6 0 3 5.2 O=C(CCCN1C2CCC1CN(c1ccc(Cl)cc1)CC2)c1ccc(F)cc1 None
15387 214209 0 3H-SPIPERONE -35 23 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CC1)CCCC(=O)C2=CC=C(C=C2)F None
15387 214209 0 UNDEFINED -35 23 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CC1)CCCC(=O)C2=CC=C(C=C2)F None
3033769 3229 54 3H-NEMONAPRIDE -562 18 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3299 3229 54 3H-NEMONAPRIDE -562 18 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
94 3229 54 3H-NEMONAPRIDE -562 18 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
CHEMBL8809 3229 54 3H-NEMONAPRIDE -562 18 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
DB12518 3229 54 3H-NEMONAPRIDE -562 18 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
25058166 214181 0 3H-SPIPERONE -8 26 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 214181 0 3H-SPIPERONE -8 26 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
None 214879 0 UNDEFINED -69 3 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 535 10 0 6 5.7 COC1=C(C=C(C=C1)C2=NOC(C2)CCCN3CCN(CC3)C(C4=CC=C(C=C4)F)C5=CC=C(C=C5)F)OC None
16362 3076 67 3H-SPIPERONE -186 29 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 3076 67 3H-SPIPERONE -186 29 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 3076 67 3H-SPIPERONE -186 29 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 3076 67 3H-SPIPERONE -186 29 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 3076 67 3H-SPIPERONE -186 29 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
1830 2552 39 3H-NEMONAPRIDE -120 27 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 2552 39 3H-NEMONAPRIDE -120 27 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 2552 39 3H-NEMONAPRIDE -120 27 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 2552 39 3H-NEMONAPRIDE -120 27 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 2552 39 3H-NEMONAPRIDE -120 27 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
214 3799 52 3H-SPIPERONE -33 29 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
214 3799 52 UNDEFINED -33 29 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 3799 52 3H-SPIPERONE -33 29 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 3799 52 UNDEFINED -33 29 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 3799 52 3H-SPIPERONE -33 29 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 3799 52 UNDEFINED -33 29 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 3799 52 3H-SPIPERONE -33 29 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 3799 52 UNDEFINED -33 29 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 3799 52 3H-SPIPERONE -33 29 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 3799 52 UNDEFINED -33 29 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 3799 52 3H-SPIPERONE -33 29 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 3799 52 UNDEFINED -33 29 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
25058166 214181 0 3H-YM 09151-2 -8 26 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 214181 0 3H-YM 09151-2 -8 26 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
1257 214628 0 3H-SPIPERONE 1 2 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCCC2C1CC3=C(C2)NN=C3 None
209 3008 94 3H-NEMONAPRIDE -30 23 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 3008 94 3H-NEMONAPRIDE -30 23 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 3008 94 3H-NEMONAPRIDE -30 23 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 3008 94 3H-NEMONAPRIDE -30 23 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 3008 94 3H-NEMONAPRIDE -30 23 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2448 214184 0 R-SAT -13 17 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 419 6 1 3 4.5 C1CN(CCC1(C2=CC=C(C=C2)Br)O)CCCC(=O)C3=CC=C(C=C3)F None
None 214879 0 UNDEFINED -69 3 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 535 10 0 6 5.7 COC1=C(C=C(C=C1)C2=NOC(C2)CCCN3CCN(CC3)C(C4=CC=C(C=C4)F)C5=CC=C(C=C5)F)OC None
1353 1880 85 3H-SPIPERONE -3 85 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-SPIPERONE -3 85 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-SPIPERONE -3 85 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-SPIPERONE -3 85 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-SPIPERONE -3 85 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
4209 3114 71 None -1318 33 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
4893 3114 71 None -1318 33 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
503 3114 71 None -1318 33 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
5385 3114 71 None -1318 33 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
CHEMBL2 3114 71 None -1318 33 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
DB00457 3114 71 None -1318 33 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
1353 1880 85 3H-SPIPERONE -3 85 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 1880 85 3H-SPIPERONE -4 85 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-SPIPERONE -3 85 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-SPIPERONE -4 85 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-SPIPERONE -3 85 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-SPIPERONE -4 85 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-SPIPERONE -3 85 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-SPIPERONE -4 85 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-SPIPERONE -3 85 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-SPIPERONE -4 85 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
5280343 187691 119 None 1 32 Human 8.3 pKi = 8.3 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
Drug Central 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL1520590 187691 119 None 1 32 Human 8.3 pKi = 8.3 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
Drug Central 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL50 187691 119 None 1 32 Human 8.3 pKi = 8.3 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
Drug Central 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
2812 4711 96 None -39 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
CHEMBL104 4711 96 None -39 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
2601 3721 30 3H-YM 09151-2 -7 21 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
443951 3721 30 3H-YM 09151-2 -7 21 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
56 3721 30 3H-YM 09151-2 -7 21 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL73151 3721 30 3H-YM 09151-2 -7 21 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
DB13399 3721 30 3H-YM 09151-2 -7 21 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
176 394 63 None -4 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2157 394 63 None -4 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2566 394 63 None -4 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
CHEMBL633 394 63 None -4 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
DB01118 394 63 None -4 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
4189 205195 91 None -33 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL1559 205195 91 None -33 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL91 205195 91 None -33 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
13091268 77845 0 UNDEFINED -8 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 None
CHEMBL210578 77845 0 UNDEFINED -8 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 None
2274 3124 53 UNDEFINED -56 32 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 3124 53 UNDEFINED -56 32 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 3124 53 UNDEFINED -56 32 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 3124 53 UNDEFINED -56 32 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 3124 53 UNDEFINED -56 32 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
1016 3690 75 None -28 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2561 3690 75 None -28 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2733526 3690 75 None -28 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
5384 3690 75 None -28 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
CHEMBL83 3690 75 None -28 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
DB00675 3690 75 None -28 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
54477 84230 34 None -14 22 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
Drug Central 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
CHEMBL22242 84230 34 None -14 22 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
Drug Central 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
3198 203802 73 None -26 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL1201049 203802 73 None -26 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL808 203802 73 None -26 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
1499 2060 43 None -18 17 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
3779 2060 43 None -18 17 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
536 2060 43 None -18 17 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
CHEMBL434 2060 43 None -18 17 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
DB01064 2060 43 None -18 17 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
7077 66625 24 None -10 5 Human 8.3 pKi = 8.3 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
Drug Central 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 None
CHEMBL186720 66625 24 None -10 5 Human 8.3 pKi = 8.3 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
Drug Central 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 None
CHEMBL3925724 66625 24 None -10 5 Human 8.3 pKi = 8.3 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
Drug Central 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 None
1830 2552 39 R-SAT -120 27 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 2552 39 R-SAT -120 27 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 2552 39 R-SAT -120 27 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 2552 39 R-SAT -120 27 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 2552 39 R-SAT -120 27 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
1830 2552 39 None -120 27 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 2552 39 None -120 27 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 2552 39 None -120 27 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 2552 39 None -120 27 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 2552 39 None -120 27 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
2247 502 77 None -63 41 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
249 502 77 None -63 41 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
2603 502 77 None -63 41 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
CHEMBL296419 502 77 None -63 41 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
DB00637 502 77 None -63 41 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
1577 3647 104 None -8 25 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
164512405 3647 104 None -8 25 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2537 3647 104 None -8 25 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5355 3647 104 None -8 25 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5501 3647 104 None -8 25 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
643497 3647 104 None -8 25 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
688272 3647 104 None -8 25 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
958 3647 104 None -8 25 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
960 3647 104 None -8 25 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL196677 3647 104 None -8 25 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL26 3647 104 None -8 25 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL267044 3647 104 None -8 25 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB00391 3647 104 None -8 25 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB16021 3647 104 None -8 25 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
1577 3647 104 None -8 25 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
164512405 3647 104 None -8 25 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2537 3647 104 None -8 25 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5355 3647 104 None -8 25 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5501 3647 104 None -8 25 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
643497 3647 104 None -8 25 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
688272 3647 104 None -8 25 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
958 3647 104 None -8 25 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
960 3647 104 None -8 25 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL196677 3647 104 None -8 25 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL26 3647 104 None -8 25 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL267044 3647 104 None -8 25 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB00391 3647 104 None -8 25 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB16021 3647 104 None -8 25 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2337 3205 72 None -114 62 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 None -114 62 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 None -114 62 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 None -114 62 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 None -114 62 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
103 4089 56 3H-SPIPERONE -4 53 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4089 56 3H-SPIPERONE -4 53 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4089 56 3H-SPIPERONE -4 53 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4089 56 3H-SPIPERONE -4 53 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4089 56 3H-SPIPERONE -4 53 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
219050 3321 21 3H-SPIPERONE -58 21 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 None
52 3321 21 3H-SPIPERONE -58 21 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 None
CHEMBL431367 3321 21 3H-SPIPERONE -58 21 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 None
3117 206106 100 None -2 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC None
CHEMBL964 206106 100 None -2 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC None
1212 1632 45 3H-SPIPERONE -77 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1212 1632 45 UNDEFINED -77 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1632 45 3H-SPIPERONE -77 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1632 45 UNDEFINED -77 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1632 45 3H-SPIPERONE -77 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1632 45 UNDEFINED -77 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1632 45 3H-SPIPERONE -77 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1632 45 UNDEFINED -77 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1632 45 3H-SPIPERONE -77 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1632 45 UNDEFINED -77 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
135398745 2869 108 UNDEFINED -10 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 UNDEFINED -10 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 UNDEFINED -10 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 UNDEFINED -10 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
None 214880 0 UNDEFINED -102 3 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 453 10 0 7 4.2 CCOC1=CC=CC=C1N2CCN(CC2)CCCC3CC(=NO3)C4=CC(=C(C=C4)OC)OC None
37459 735 10 3H-SPIPERONE -123 24 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
62 735 10 3H-SPIPERONE -123 24 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
CHEMBL8514 735 10 3H-SPIPERONE -123 24 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
242 467 117 3H-NMSP -87 51 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 467 117 3H-NMSP -87 51 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 467 117 3H-NMSP -87 51 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 467 117 3H-NMSP -87 51 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 467 117 3H-NMSP -87 51 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
44591088 188991 0 UNDEFINED -3 3 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 372 6 0 3 4.6 O=C(CCCN1CC2CC1N(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 None
CHEMBL514591 188991 0 UNDEFINED -3 3 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 372 6 0 3 4.6 O=C(CCCN1CC2CC1N(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 None
242 467 117 3H-NMSP -117 51 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 467 117 3H-NMSP -117 51 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 467 117 3H-NMSP -117 51 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 467 117 3H-NMSP -117 51 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 467 117 3H-NMSP -117 51 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
1577 3647 104 3H-SPIPERONE -28 25 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
164512405 3647 104 3H-SPIPERONE -28 25 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2537 3647 104 3H-SPIPERONE -28 25 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5355 3647 104 3H-SPIPERONE -28 25 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5501 3647 104 3H-SPIPERONE -28 25 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
643497 3647 104 3H-SPIPERONE -28 25 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
688272 3647 104 3H-SPIPERONE -28 25 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
958 3647 104 3H-SPIPERONE -28 25 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
960 3647 104 3H-SPIPERONE -28 25 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL196677 3647 104 3H-SPIPERONE -28 25 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL26 3647 104 3H-SPIPERONE -28 25 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL267044 3647 104 3H-SPIPERONE -28 25 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB00391 3647 104 3H-SPIPERONE -28 25 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB16021 3647 104 3H-SPIPERONE -28 25 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
44578446 180998 0 UNDEFINED -3 3 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 372 6 0 3 4.4 O=C(CCCN1CC2CC1CN2c1ccc(Cl)cc1)c1ccc(F)cc1 None
CHEMBL476934 180998 0 UNDEFINED -3 3 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 372 6 0 3 4.4 O=C(CCCN1CC2CC1CN2c1ccc(Cl)cc1)c1ccc(F)cc1 None
9429 214381 0 3H-SPIPERONE -251 5 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 638 6 2 10 2.2 CN1CCN(CC1)CCCN2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C.CS(=O)(=O)O.CS(=O)(=O)O None
135398737 944 89 3H-N-Methylspiperone -13 91 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-N-Methylspiperone -13 91 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-N-Methylspiperone -13 91 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-N-Methylspiperone -13 91 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-N-Methylspiperone -13 91 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
5311189 203133 4 3H-NMSP -1 27 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 None
CHEMBL7549 203133 4 3H-NMSP -1 27 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 None
135398737 944 89 UNDEFINED -13 91 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 UNDEFINED -13 91 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 UNDEFINED -13 91 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 UNDEFINED -13 91 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 UNDEFINED -13 91 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1577 3647 104 R-SAT -8 25 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
164512405 3647 104 R-SAT -8 25 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2537 3647 104 R-SAT -8 25 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5355 3647 104 R-SAT -8 25 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5501 3647 104 R-SAT -8 25 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
643497 3647 104 R-SAT -8 25 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
688272 3647 104 R-SAT -8 25 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
958 3647 104 R-SAT -8 25 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
960 3647 104 R-SAT -8 25 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL196677 3647 104 R-SAT -8 25 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL26 3647 104 R-SAT -8 25 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL267044 3647 104 R-SAT -8 25 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB00391 3647 104 R-SAT -8 25 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB16021 3647 104 R-SAT -8 25 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
115237 55296 113 3H-NMSP -15 54 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55296 113 3H-NMSP -15 54 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
135398737 944 89 3H-SPIPERONE -13 91 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-SPIPERONE -13 91 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-SPIPERONE -13 91 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-SPIPERONE -13 91 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-SPIPERONE -13 91 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
185 3943 54 3H-SPIPERONE -7244 37 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5311271 3943 54 3H-SPIPERONE -7244 37 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
CHEMBL74355 3943 54 3H-SPIPERONE -7244 37 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
DB16351 3943 54 3H-SPIPERONE -7244 37 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
202478 202981 15 3H-YM 09151-2 -7 25 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
CHEMBL7393 202981 15 3H-YM 09151-2 -7 25 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
1621 2396 16 3H-NMSP -181 44 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2396 16 3H-NMSP -181 44 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2396 16 3H-NMSP -181 44 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2396 16 3H-NMSP -181 44 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2396 16 3H-NMSP -181 44 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
22065962 176222 0 UNDEFINED 20 3 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 294 3 1 5 1.7 c1cnc(N2CCN(Cc3c[nH]c4ncccc34)CC2)nc1 None
CHEMBL460644 176222 0 UNDEFINED 20 3 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 294 3 1 5 1.7 c1cnc(N2CCN(Cc3c[nH]c4ncccc34)CC2)nc1 None
None 214590 0 3H-SPIPERONE -74 19 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 451 8 2 4 3.2 CCNC(=O)N(CCCN(C)C)C(=O)C1CC2C(CC3=CNC4=CC=CC2=C34)N(C1)CC=C None
10060538 4508 6 3H-SPIPERONE -3890 4 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 247 2 1 3 2.5 CCCN1CCOC2c3cc(O)ccc3CCC21 None
CHEMBL102582 4508 6 3H-SPIPERONE -3890 4 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 247 2 1 3 2.5 CCCN1CCOC2c3cc(O)ccc3CCC21 None
2105 3005 34 3H-SPIPERONE -48 33 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 3005 34 3H-SPIPERONE -48 33 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 3005 34 3H-SPIPERONE -48 33 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 3005 34 3H-SPIPERONE -48 33 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 3005 34 3H-SPIPERONE -48 33 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
44591087 175177 0 UNDEFINED -1 3 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 366 3 1 3 4.5 Clc1ccc(N2CCC3CCC(C2)N3Cc2c[nH]c3ncccc23)cc1 None
CHEMBL458342 175177 0 UNDEFINED -1 3 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 366 3 1 3 4.5 Clc1ccc(N2CCC3CCC(C2)N3Cc2c[nH]c3ncccc23)cc1 None
33630 178379 94 None -13 27 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
Drug Central 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
CHEMBL47050 178379 94 None -13 27 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
Drug Central 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
2402 3318 58 None -2 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
5095 3318 58 None -2 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
7295 3318 58 None -2 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
CHEMBL589 3318 58 None -2 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
DB00268 3318 58 None -2 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
681 1437 65 UNDEFINED -2 38 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1437 65 UNDEFINED -2 38 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1437 65 UNDEFINED -2 38 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1437 65 UNDEFINED -2 38 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1437 65 UNDEFINED -2 38 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
3191 102385 93 None -10 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
CHEMBL305660 102385 93 None -10 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
15387 214209 0 None -35 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 263 5 0 2 3.5 CC1CCN(CC1)CCCC(=O)C2=CC=C(C=C2)F None
31101 720 39 None -186 35 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 720 39 None -186 35 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 720 39 None -186 35 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 720 39 None -186 35 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 720 39 None -186 35 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
212 3746 43 UNDEFINED -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
2639 3746 43 UNDEFINED -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
941651 3746 43 UNDEFINED -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
CHEMBL1201 3746 43 UNDEFINED -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
DB01623 3746 43 UNDEFINED -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
104870 98423 39 None -2 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
5374 98423 39 None -2 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
CHEMBL279085 98423 39 None -2 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
1153 1598 53 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
12668023 1598 53 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
30026874 1598 53 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
30026875 1598 53 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
3341 1598 53 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
6603851 1598 53 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
933 1598 53 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
939 1598 53 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
985 1598 53 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
CHEMBL1160786 1598 53 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
CHEMBL1161520 1598 53 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
CHEMBL588 1598 53 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
DB00800 1598 53 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
2202 3083 91 None -2 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
4850 3083 91 None -2 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
49 3083 91 None -2 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
CHEMBL1371770 3083 91 None -2 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
DB12478 3083 91 None -2 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
10065083 31887 1 UNDEFINED 1 10 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 328 6 0 5 2.4 O=C(CCCN1CCN(c2ncccn2)CC1)c1ccc(F)cc1 None
CHEMBL140872 31887 1 UNDEFINED 1 10 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 328 6 0 5 2.4 O=C(CCCN1CCN(c2ncccn2)CC1)c1ccc(F)cc1 None
46 2861 0 R-SAT -33 5 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 420 4 0 6 4.0 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2C None
71351 2861 0 R-SAT -33 5 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 420 4 0 6 4.0 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2C None
CHEMBL2104619 2861 0 R-SAT -33 5 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 420 4 0 6 4.0 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2C None
DB06229 2861 0 R-SAT -33 5 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 420 4 0 6 4.0 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2C None
11653679 180609 1 UNDEFINED 3 11 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 374 6 0 3 4.7 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
CHEMBL476108 180609 1 UNDEFINED 3 11 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 374 6 0 3 4.7 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
242 467 117 None -117 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 467 117 None -117 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 467 117 None -117 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 467 117 None -117 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 467 117 None -117 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
212 3746 43 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
2639 3746 43 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
941651 3746 43 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
CHEMBL1201 3746 43 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
DB01623 3746 43 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
11154555 788 57 None -501 12 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
5037 788 57 None -501 12 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
7671 788 57 None -501 12 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL2028019 788 57 None -501 12 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL3085826 788 57 None -501 12 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB06016 788 57 None -501 12 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
21302490 112308 26 None -12 9 Human 8.2 pKi = 8.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
Drug Central 393 5 0 4 3.9 CN1CCN2c3c(cccc31)[C@@H]1CN(CCCC(=O)c3ccc(F)cc3)CC[C@@H]12 None
CHEMBL3233142 112308 26 None -12 9 Human 8.2 pKi = 8.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
Drug Central 393 5 0 4 3.9 CN1CCN2c3c(cccc31)[C@@H]1CN(CCCC(=O)c3ccc(F)cc3)CC[C@@H]12 None
CHEMBL3306803 112308 26 None -12 9 Human 8.2 pKi = 8.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
Drug Central 393 5 0 4 3.9 CN1CCN2c3c(cccc31)[C@@H]1CN(CCCC(=O)c3ccc(F)cc3)CC[C@@H]12 None
135398745 2869 108 3H-N-Methylspiperone -10 65 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-N-Methylspiperone -10 65 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-N-Methylspiperone -10 65 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-N-Methylspiperone -10 65 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
6852400 214160 0 3H-SPIPERONE -794 21 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
73759726 214160 0 3H-SPIPERONE -794 21 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
25139331 169361 0 UNDEFINED 1 4 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 310 9 2 2 3.9 CCCNCCCCNC(=O)c1ccc(-c2ccccc2)cc1 None
CHEMBL444128 169361 0 UNDEFINED 1 4 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 310 9 2 2 3.9 CCCNCCCCNC(=O)c1ccc(-c2ccccc2)cc1 None
3033769 3229 54 3H-RACLOPRIDE -562 18 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3033769 3229 54 3H-SPIPERONE -562 18 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3033769 3229 54 UNDEFINED -562 18 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3299 3229 54 3H-RACLOPRIDE -562 18 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3299 3229 54 3H-SPIPERONE -562 18 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3299 3229 54 UNDEFINED -562 18 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
94 3229 54 3H-RACLOPRIDE -562 18 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
94 3229 54 3H-SPIPERONE -562 18 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
94 3229 54 UNDEFINED -562 18 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
CHEMBL8809 3229 54 3H-RACLOPRIDE -562 18 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
CHEMBL8809 3229 54 3H-SPIPERONE -562 18 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
CHEMBL8809 3229 54 UNDEFINED -562 18 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
DB12518 3229 54 3H-RACLOPRIDE -562 18 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
DB12518 3229 54 3H-SPIPERONE -562 18 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
DB12518 3229 54 UNDEFINED -562 18 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
44134711 214215 0 3H-Methylspiperone -724 13 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 340 6 2 4 2.8 CCC1=CC(=C(C(=C1O)C(=O)NCC2CCCN2CC)OC)Cl None
None 214361 0 3H-YM 09151-2 -8 5 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 273 6 0 2 4.3 CCCN(CCC)C1C=CC2=C(C1C)C=CC=C2OC None
25139481 184257 0 UNDEFINED -4 4 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 392 10 1 2 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCCCC1 None
CHEMBL485227 184257 0 UNDEFINED -4 4 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 392 10 1 2 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCCCC1 None
25139477 183663 0 UNDEFINED -15 4 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 486 10 1 2 6.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CC=C(C#C[Si](C)(C)C)CC1 None
CHEMBL483593 183663 0 UNDEFINED -15 4 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 486 10 1 2 6.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CC=C(C#C[Si](C)(C)C)CC1 None
44123782 189009 0 UNDEFINED -6 3 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 338 3 1 3 3.7 Clc1ccc(N2CC3CC2CN3Cc2c[nH]c3ncccc23)cc1 None
CHEMBL514747 189009 0 UNDEFINED -6 3 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 338 3 1 3 3.7 Clc1ccc(N2CC3CC2CN3Cc2c[nH]c3ncccc23)cc1 None
2477 734 54 None -1 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
36 734 54 None -1 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
437 734 54 None -1 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
CHEMBL49 734 54 None -1 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
DB00490 734 54 None -1 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
2389 3279 114 3H-SPIPERONE -21 67 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2389 3279 114 3H-SPIROPERIDOL -21 67 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 3H-SPIPERONE -21 67 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 3H-SPIROPERIDOL -21 67 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 3H-SPIPERONE -21 67 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 3H-SPIROPERIDOL -21 67 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 3H-SPIPERONE -21 67 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 3H-SPIROPERIDOL -21 67 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 3H-SPIPERONE -21 67 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 3H-SPIROPERIDOL -21 67 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
1212 1632 45 R-SAT -77 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1632 45 R-SAT -77 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1632 45 R-SAT -77 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1632 45 R-SAT -77 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1632 45 R-SAT -77 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2274 3124 53 None -56 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 3124 53 None -56 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 3124 53 None -56 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 3124 53 None -56 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 3124 53 None -56 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
1621 2396 16 None -64 44 Human 8.1 pKi = 8.1 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2396 16 None -64 44 Human 8.1 pKi = 8.1 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2396 16 None -64 44 Human 8.1 pKi = 8.1 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2396 16 None -64 44 Human 8.1 pKi = 8.1 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2396 16 None -64 44 Human 8.1 pKi = 8.1 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
2105 3005 34 None -48 33 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 3005 34 None -48 33 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 3005 34 None -48 33 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 3005 34 None -48 33 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 3005 34 None -48 33 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
2407 3320 73 None -30 7 Human 8.1 pKi = 8.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
59227 3320 73 None -30 7 Human 8.1 pKi = 8.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
941 3320 73 None -30 7 Human 8.1 pKi = 8.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
CHEMBL1303 3320 73 None -30 7 Human 8.1 pKi = 8.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
DB05271 3320 73 None -30 7 Human 8.1 pKi = 8.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
115237 55296 113 None -15 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55296 113 None -15 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
242 467 117 None -87 51 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 467 117 None -87 51 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 467 117 None -87 51 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 467 117 None -87 51 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 467 117 None -87 51 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
37 766 56 None -7 17 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
460 766 56 None -7 17 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
54746 766 56 None -7 17 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
CHEMBL1201087 766 56 None -7 17 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
DB00248 766 56 None -7 17 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
135398745 2869 108 None -7 65 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 None -7 65 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 None -7 65 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 None -7 65 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
2865 4079 67 None -66 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4079 67 None -66 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4079 67 None -66 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4079 67 None -66 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4079 67 None -66 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
49831411 216027 0 None -1 14 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 659 19 0 6 8.7 CCCCCCCCCCCC(=O)OCN1C(=O)CCC2=CC=C(OCCCCN3CCN(CC3)C3=C(Cl)C(Cl)=CC=C3)C=C12 None
49831411 216027 0 None -1 14 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 659 19 0 6 8.7 CCCCCCCCCCCC(=O)OCN1C(=O)CCC2=CC=C(OCCCCN3CCN(CC3)C3=C(Cl)C(Cl)=CC=C3)C=C12 None
214 3799 52 None -33 29 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 3799 52 None -33 29 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 3799 52 None -33 29 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 3799 52 None -33 29 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 3799 52 None -33 29 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 3799 52 None -33 29 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
103 4089 56 None -17 53 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4089 56 None -17 53 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4089 56 None -17 53 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4089 56 None -17 53 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4089 56 None -17 53 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
3389 215982 0 None -1 26 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 549 12 0 6 6.8 CCCCCCC(=O)OCCN1CCN(CCCN2C3=CC=CC=C3SC3=C2C=C(C=C3)C(F)(F)F)CC1 None
191 399 92 None -8 28 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
201 399 92 None -8 28 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2170 399 92 None -8 28 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
CHEMBL1113 399 92 None -8 28 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
DB00543 399 92 None -8 28 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2389 3279 114 3H-SPIPERONE -28 67 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 3H-SPIPERONE -28 67 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 3H-SPIPERONE -28 67 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 3H-SPIPERONE -28 67 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 3H-SPIPERONE -28 67 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
135398737 944 89 None -13 91 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 None -13 91 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 None -13 91 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 None -13 91 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 None -13 91 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
16106 117643 28 None -1 11 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
CHEMBL340801 117643 28 None -1 11 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
1212 1632 45 None -77 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1632 45 None -77 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1632 45 None -77 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1632 45 None -77 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1632 45 None -77 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
209 3008 94 None -30 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 3008 94 None -30 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 3008 94 None -30 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 3008 94 None -30 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 3008 94 None -30 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
3294 1975 106 None -11 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 1975 106 None -11 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 1975 106 None -11 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 1975 106 None -11 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 1975 106 None -11 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
135398737 944 89 R-SAT -13 91 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 R-SAT -13 91 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 R-SAT -13 91 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 R-SAT -13 91 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 R-SAT -13 91 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
65750 214699 0 None -1 3 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 346 6 0 3 5.7 CCN(CC)CCCN1C2=CC=CC=C2SC3=C1C=C(C=C3)Cl None
2726 906 64 None -8 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 None -8 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 None -8 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 None -8 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 None -8 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1443 1997 30 None -1 10 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 None
33625 1997 30 None -1 10 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 None
501 1997 30 None -1 10 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 None
CHEMBL279516 1997 30 None -1 10 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 None
DB08950 1997 30 None -1 10 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 None
2448 214184 0 None -13 17 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 419 6 1 3 4.5 C1CN(CCC1(C2=CC=C(C=C2)Br)O)CCCC(=O)C3=CC=C(C=C3)F None
1613 2316 44 3H-SPIPERONE -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
1613 2316 44 UNDEFINED -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2316 44 3H-SPIPERONE -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2316 44 UNDEFINED -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2316 44 3H-SPIPERONE -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2316 44 UNDEFINED -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2316 44 3H-SPIPERONE -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2316 44 UNDEFINED -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2316 44 3H-SPIPERONE -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2316 44 UNDEFINED -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
5280343 187691 119 UNDEFINED 1 32 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL1520590 187691 119 UNDEFINED 1 32 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL50 187691 119 UNDEFINED 1 32 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
5467 204212 40 None 6 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 328 8 1 5 1.2 CCN(CC)CCNC(=O)c1cc(S(C)(=O)=O)ccc1OC None
CHEMBL84158 204212 40 None 6 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 328 8 1 5 1.2 CCN(CC)CCNC(=O)c1cc(S(C)(=O)=O)ccc1OC None
16106 117643 28 3H-SPIPERONE 1 11 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
CHEMBL340801 117643 28 3H-SPIPERONE 1 11 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
2435 3533 78 None -10 48 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3533 78 None -10 48 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3533 78 None -10 48 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3533 78 None -10 48 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3533 78 None -10 48 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
100 3745 52 None -8 55 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3745 52 None -8 55 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3745 52 None -8 55 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3745 52 None -8 55 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3745 52 None -8 55 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
135409468 2004 63 R-SAT -18 40 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
333 2004 63 R-SAT -18 40 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
CHEMBL845 2004 63 R-SAT -18 40 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
2274 3124 53 3H-SPIPERONE -56 32 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 3124 53 3H-SPIPERONE -56 32 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 3124 53 3H-SPIPERONE -56 32 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 3124 53 3H-SPIPERONE -56 32 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 3124 53 3H-SPIPERONE -56 32 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
15387 214209 0 3H-SPIPERONE -35 23 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CC1)CCCC(=O)C2=CC=C(C=C2)F None
213 3792 50 3H-NMSP -3 43 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 3792 50 3H-NMSP -3 43 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 3792 50 3H-NMSP -3 43 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 3792 50 3H-NMSP -3 43 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 3792 50 3H-NMSP -3 43 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
6450478 214238 0 3H-SPIPERONE -14 11 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 340 0 0 6 3.4 CN1CCN(CC1)C2=NC3=CSC=C3C(=CC#N)C4=CSC=C42 None
11954259 214201 0 3H-SPIPERONE -257 43 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
5280343 187691 119 3H-Methylspiperone -114 32 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL1520590 187691 119 3H-Methylspiperone -114 32 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL50 187691 119 3H-Methylspiperone -114 32 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
44591086 188990 0 UNDEFINED -61 3 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 367 3 2 3 4.2 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1c[nH]c2ncccc12 None
CHEMBL514590 188990 0 UNDEFINED -61 3 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 367 3 2 3 4.2 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1c[nH]c2ncccc12 None
44395709 174326 0 UNDEFINED 1 3 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 373 4 1 3 4.2 O=C(CN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 None
CHEMBL456429 174326 0 UNDEFINED 1 3 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 373 4 1 3 4.2 O=C(CN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 None
CHEMBL556361 174326 0 UNDEFINED 1 3 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 373 4 1 3 4.2 O=C(CN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 None
2389 3279 114 None -21 67 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 None -21 67 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 None -21 67 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 None -21 67 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 None -21 67 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
1712 2456 0 None -2 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
4078 2456 0 None -2 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
7227 2456 0 None -2 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
CHEMBL1088 2456 0 None -2 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
DB00933 2456 0 None -2 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
135398737 944 89 None -7 91 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 None -7 91 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 None -7 91 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 None -7 91 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 None -7 91 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
228 441 26 None -1 24 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
33 441 26 None -1 24 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
6005 441 26 None -1 24 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
CHEMBL53 441 26 None -1 24 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
DB00714 441 26 None -1 24 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
1222 1634 44 None -14 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3396 1634 44 None -14 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
85 1634 44 None -14 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL46516 1634 44 None -14 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
DB04842 1634 44 None -14 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
2601 3721 30 None -7 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
443951 3721 30 None -7 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
56 3721 30 None -7 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL73151 3721 30 None -7 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
DB13399 3721 30 None -7 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
4249 77814 30 None -7 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 355 6 1 3 4.1 Cc1ccc(C2(O)CCN(CCCC(=O)c3ccc(F)cc3)CC2)cc1 None
CHEMBL2104700 77814 30 None -7 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 355 6 1 3 4.1 Cc1ccc(C2(O)CCN(CCCC(=O)c3ccc(F)cc3)CC2)cc1 None
2601 3721 30 3H-SPIPERONE -7 21 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
443951 3721 30 3H-SPIPERONE -7 21 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
56 3721 30 3H-SPIPERONE -7 21 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL73151 3721 30 3H-SPIPERONE -7 21 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
DB13399 3721 30 3H-SPIPERONE -7 21 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
2563 3694 55 None 1 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
Drug Central 383 6 0 6 1.4 O=C1N(CCCCN2CCN(CC2)c2ncccn2)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 None
55 3694 55 None 1 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
Drug Central 383 6 0 6 1.4 O=C1N(CCCCN2CCN(CC2)c2ncccn2)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 None
91273 3694 55 None 1 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
Drug Central 383 6 0 6 1.4 O=C1N(CCCCN2CCN(CC2)c2ncccn2)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 None
CHEMBL274047 3694 55 None 1 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
Drug Central 383 6 0 6 1.4 O=C1N(CCCCN2CCN(CC2)c2ncccn2)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 None
DB12833 3694 55 None 1 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
Drug Central 383 6 0 6 1.4 O=C1N(CCCCN2CCN(CC2)c2ncccn2)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 None
11978813 713 72 None -10 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
5014 713 72 None -10 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
7672 713 72 None -10 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
CHEMBL2105760 713 72 None -10 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
DB09128 713 72 None -10 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
52919 14317 43 None -3 4 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 529 15 0 4 8.1 CCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
CHEMBL1200986 14317 43 None -3 4 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 529 15 0 4 8.1 CCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
1588 2294 24 None -23 43 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2294 24 None -23 43 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2294 24 None -23 43 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2294 24 None -23 43 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2294 24 None -23 43 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
1613 2316 44 None -2 44 Human 8.1 pKi = 8.1 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2316 44 None -2 44 Human 8.1 pKi = 8.1 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2316 44 None -2 44 Human 8.1 pKi = 8.1 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2316 44 None -2 44 Human 8.1 pKi = 8.1 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2316 44 None -2 44 Human 8.1 pKi = 8.1 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
5022 1621 67 None -1 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 None
6918248 1621 67 None -1 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 None
8182 1621 67 None -1 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 None
CHEMBL231068 1621 67 None -1 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 None
DB04908 1621 67 None -1 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 None
1524 2150 89 None -3 51 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2150 89 None -3 51 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2150 89 None -3 51 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2150 89 None -3 51 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2150 89 None -3 51 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2150 89 None -3 51 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
2780 110040 32 None -4 11 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
Drug Central 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 None
CHEMBL325109 110040 32 None -4 11 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
Drug Central 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 None
2389 3279 114 UNDEFINED -21 67 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 UNDEFINED -21 67 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 UNDEFINED -21 67 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 UNDEFINED -21 67 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 UNDEFINED -21 67 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
25058166 214181 0 3H-SPIPERONE -8 26 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 214181 0 3H-SPIPERONE -8 26 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
2389 3279 114 3H-N-Methylspiperone -21 67 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 3H-N-Methylspiperone -21 67 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 3H-N-Methylspiperone -21 67 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 3H-N-Methylspiperone -21 67 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 3H-N-Methylspiperone -21 67 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
16363 589 48 None -1 6 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
312 589 48 None -1 6 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
9215 589 48 None -1 6 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL297302 589 48 None -1 6 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB12867 589 48 None -1 6 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
46780481 107045 18 None -23 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107045 18 None -23 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107045 18 None -23 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107045 18 None -23 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
16362 3076 67 None -20 29 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 3076 67 None -20 29 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 3076 67 None -20 29 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 3076 67 None -20 29 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 3076 67 None -20 29 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
135398745 2869 108 None -10 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 None -10 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 None -10 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 None -10 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
1222 1634 44 R-SAT -14 32 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3396 1634 44 R-SAT -14 32 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
85 1634 44 R-SAT -14 32 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL46516 1634 44 R-SAT -14 32 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
DB04842 1634 44 R-SAT -14 32 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
15387 214209 0 3H-NEMONAPRIDE -35 23 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CC1)CCCC(=O)C2=CC=C(C=C2)F None
44591043 176238 0 UNDEFINED 3 2 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 3 2 2 3.9 OC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)C1 None
CHEMBL460855 176238 0 UNDEFINED 3 2 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 3 2 2 3.9 OC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)C1 None
None 214241 0 3H-SPIPERONE -1 2 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 411 6 1 3 3.9 C1CCC(CC1)NC(=O)N2CCN(CC2)CCCC(=O)C3=CC=C(C=C3)F.Cl None
2402 3318 58 3H-SPIPERONE -2 25 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
5095 3318 58 3H-SPIPERONE -2 25 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
7295 3318 58 3H-SPIPERONE -2 25 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
CHEMBL589 3318 58 3H-SPIPERONE -2 25 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
DB00268 3318 58 3H-SPIPERONE -2 25 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
10060538 4508 6 3H-SPIPERONE -3890 4 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 247 2 1 3 2.5 CCCN1CCOC2c3cc(O)ccc3CCC21 None
CHEMBL102582 4508 6 3H-SPIPERONE -3890 4 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 247 2 1 3 2.5 CCCN1CCOC2c3cc(O)ccc3CCC21 None
None 214684 0 3H-SPIPERONE -467 4 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 160 1 0 2 2.6 CC(=O)C1=CC2=CC=CC=C2O1 None
681 1437 65 None -2 38 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1437 65 None -2 38 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1437 65 None -2 38 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1437 65 None -2 38 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1437 65 None -2 38 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
135398737 944 89 3H-SPIPERONE -13 91 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-SPIPERONE -13 91 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-SPIPERONE -13 91 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-SPIPERONE -13 91 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-SPIPERONE -13 91 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1613 2316 44 3H-SPIPERONE -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2316 44 3H-SPIPERONE -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2316 44 3H-SPIPERONE -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2316 44 3H-SPIPERONE -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2316 44 3H-SPIPERONE -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
2389 3279 114 3H-SCH23390 -21 67 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 3H-SCH23390 -21 67 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 3H-SCH23390 -21 67 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 3H-SCH23390 -21 67 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 3H-SCH23390 -21 67 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2435 3533 78 3H-SPIPERONE -10 48 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3533 78 3H-SPIPERONE -10 48 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3533 78 3H-SPIPERONE -10 48 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3533 78 3H-SPIPERONE -10 48 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3533 78 3H-SPIPERONE -10 48 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
3168 9172 84 None -4 21 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
CHEMBL1108 9172 84 None -4 21 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
1712 2456 0 R-SAT -2 21 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
4078 2456 0 R-SAT -2 21 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
7227 2456 0 R-SAT -2 21 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
CHEMBL1088 2456 0 R-SAT -2 21 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
DB00933 2456 0 R-SAT -2 21 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
1212 1632 45 3H-SPIPERONE -18 65 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1632 45 3H-SPIPERONE -18 65 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1632 45 3H-SPIPERONE -18 65 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1632 45 3H-SPIPERONE -18 65 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1632 45 3H-SPIPERONE -18 65 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
119570 3110 90 None -10 40 Human 8.0 pKi = 8.0 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 3110 90 None -10 40 Human 8.0 pKi = 8.0 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 3110 90 None -10 40 Human 8.0 pKi = 8.0 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 3110 90 None -10 40 Human 8.0 pKi = 8.0 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 3110 90 None -10 40 Human 8.0 pKi = 8.0 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
1238 201484 21 None -2 16 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL64249 201484 21 None -2 16 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
2726 906 64 3H-SPIPERONE -8 72 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 3H-SPIPERONE -8 72 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 3H-SPIPERONE -8 72 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 3H-SPIPERONE -8 72 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 3H-SPIPERONE -8 72 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
135398737 944 89 3H-SPIPERONE -7 91 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-SPIPERONE -7 91 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-SPIPERONE -7 91 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-SPIPERONE -7 91 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-SPIPERONE -7 91 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398745 2869 108 3H-SPIPERONE -7 65 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-SPIPERONE -7 65 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-SPIPERONE -7 65 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-SPIPERONE -7 65 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
2470 3596 46 None -20 59 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3596 46 None -20 59 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3596 46 None -20 59 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3596 46 None -20 59 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3596 46 None -20 59 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
2726 906 64 3H-SPIPERONE -10 72 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 3H-SPIPERONE -10 72 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 3H-SPIPERONE -10 72 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 3H-SPIPERONE -10 72 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 3H-SPIPERONE -10 72 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
191 399 92 3H-SPIPERONE -67 28 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
201 399 92 3H-SPIPERONE -67 28 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2170 399 92 3H-SPIPERONE -67 28 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
CHEMBL1113 399 92 3H-SPIPERONE -67 28 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
DB00543 399 92 3H-SPIPERONE -67 28 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
None 214684 0 3H-SPIPERONE -467 4 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 160 1 0 2 2.6 CC(=O)C1=CC2=CC=CC=C2O1 None
1577 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
164512405 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2537 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5355 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5501 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
643497 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
688272 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
958 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
960 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL196677 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL26 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL267044 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB00391 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB16021 3647 104 3H-SPIPERONE -8 25 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
202478 202981 15 3H-NMSP -7 25 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
CHEMBL7393 202981 15 3H-NMSP -7 25 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
115368 3007 0 None 1 3 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 9577836
2112 3007 0 None 1 3 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 9577836
7556 3007 0 None 1 3 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 9577836
CHEMBL1472975 3007 0 None 1 3 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 9577836
DB08922 3007 0 None 1 3 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 9577836
16363 589 48 None -1 6 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 9577836
312 589 48 None -1 6 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 9577836
9215 589 48 None -1 6 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 9577836
CHEMBL297302 589 48 None -1 6 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 9577836
DB12867 589 48 None -1 6 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 9577836
1577 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
164512405 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
2537 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
5355 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
5501 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
643497 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
688272 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
958 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
960 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
CHEMBL196677 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
CHEMBL26 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
CHEMBL267044 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
DB00391 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
DB16021 3647 104 None -8 25 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
3033769 3229 54 None -288 18 Rat 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10617689
3299 3229 54 None -288 18 Rat 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10617689
94 3229 54 None -288 18 Rat 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10617689
CHEMBL8809 3229 54 None -288 18 Rat 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10617689
DB12518 3229 54 None -288 18 Rat 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10617689
16094676 230 17 None - 1 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 4 1 3 2.2 Cc1cccc(c1)C(=O)NCN1CCC(CC1)c1cccc[n+]1[O-] 17149874
8439 230 17 None - 1 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 4 1 3 2.2 Cc1cccc(c1)C(=O)NCN1CCC(CC1)c1cccc[n+]1[O-] 17149874
CHEMBL219182 230 17 None - 1 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 4 1 3 2.2 Cc1cccc(c1)C(=O)NCN1CCC(CC1)c1cccc[n+]1[O-] 17149874
2274 3124 53 None -56 32 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 3124 53 None -56 32 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 3124 53 None -56 32 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 3124 53 None -56 32 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 3124 53 None -56 32 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
31101 720 39 None -186 35 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
35 720 39 None -186 35 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
403 720 39 None -186 35 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
CHEMBL493 720 39 None -186 35 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
DB01200 720 39 None -186 35 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
1577 3647 104 None -8 25 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
1577 3647 104 None -8 25 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
164512405 3647 104 None -8 25 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
164512405 3647 104 None -8 25 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
2537 3647 104 None -8 25 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
2537 3647 104 None -8 25 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
5355 3647 104 None -8 25 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
5355 3647 104 None -8 25 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
5501 3647 104 None -8 25 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
5501 3647 104 None -8 25 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
643497 3647 104 None -8 25 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
643497 3647 104 None -8 25 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
688272 3647 104 None -8 25 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
688272 3647 104 None -8 25 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
958 3647 104 None -8 25 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
958 3647 104 None -8 25 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
960 3647 104 None -8 25 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
960 3647 104 None -8 25 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
CHEMBL196677 3647 104 None -8 25 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
CHEMBL196677 3647 104 None -8 25 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
CHEMBL26 3647 104 None -8 25 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
CHEMBL26 3647 104 None -8 25 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
CHEMBL267044 3647 104 None -8 25 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
CHEMBL267044 3647 104 None -8 25 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
DB00391 3647 104 None -8 25 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
DB00391 3647 104 None -8 25 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
DB16021 3647 104 None -8 25 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
DB16021 3647 104 None -8 25 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
2407 3320 73 None -30 7 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 8863800
59227 3320 73 None -30 7 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 8863800
941 3320 73 None -30 7 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 8863800
CHEMBL1303 3320 73 None -30 7 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 8863800
DB05271 3320 73 None -30 7 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 8863800
214 3799 52 None -33 29 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 9015795
2740 3799 52 None -33 29 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 9015795
5566 3799 52 None -33 29 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 9015795
66064 3799 52 None -33 29 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 9015795
CHEMBL422 3799 52 None -33 29 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 9015795
DB00831 3799 52 None -33 29 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 9015795
103 4089 56 None -17 53 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 8935801
2875 4089 56 None -17 53 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 8935801
5736 4089 56 None -17 53 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 8935801
CHEMBL285802 4089 56 None -17 53 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 8935801
DB09225 4089 56 None -17 53 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 8935801
72737723 2541 1 None - 1 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 5 0 2 4.2 Clc1ccc(cc1)CN1CCO[C@@H](C1)CCc1ccccc1 25221667
8440 2541 1 None - 1 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 5 0 2 4.2 Clc1ccc(cc1)CN1CCO[C@@H](C1)CCc1ccccc1 25221667
CHEMBL3335556 2541 1 None - 1 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 5 0 2 4.2 Clc1ccc(cc1)CN1CCO[C@@H](C1)CCc1ccccc1 25221667
2 3210 19 None -2 28 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 12388666
2 3210 19 None -2 28 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 1840645
2 3210 19 None -2 28 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 8967990
54562 3210 19 None -2 28 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 12388666
54562 3210 19 None -2 28 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 1840645
54562 3210 19 None -2 28 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 8967990
CHEMBL240773 3210 19 None -2 28 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 12388666
CHEMBL240773 3210 19 None -2 28 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 1840645
CHEMBL240773 3210 19 None -2 28 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 8967990
681 1437 65 None -2 38 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 1840645
940 1437 65 None -2 38 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 1840645
947 1437 65 None -2 38 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 1840645
CHEMBL59 1437 65 None -2 38 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 1840645
DB00988 1437 65 None -2 38 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 1840645
3251 4009 50 None -43 12 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 21520940
5684 4009 50 None -43 12 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 21520940
80 4009 50 None -43 12 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 21520940
CHEMBL31354 4009 50 None -43 12 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 21520940
10425450 199 23 None -1 4 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 16153699
10425450 199 23 None 1 4 Rat 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 16153699
3301 199 23 None -1 4 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 16153699
3301 199 23 None 1 4 Rat 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 16153699
CHEMBL375596 199 23 None -1 4 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 16153699
CHEMBL375596 199 23 None 1 4 Rat 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 16153699
1613 2316 44 None -2 44 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 9015795
205 2316 44 None -2 44 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 9015795
3964 2316 44 None -2 44 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 9015795
CHEMBL831 2316 44 None -2 44 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 9015795
DB00408 2316 44 None -2 44 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 9015795
228 441 26 None -1 24 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
33 441 26 None -1 24 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
6005 441 26 None -1 24 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
CHEMBL53 441 26 None -1 24 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
DB00714 441 26 None -1 24 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
2435 3533 78 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 16135699
2435 3533 78 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 9015795
2435 3533 78 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 9577836
60149 3533 78 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 16135699
60149 3533 78 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 9015795
60149 3533 78 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 9577836
98 3533 78 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 16135699
98 3533 78 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 9015795
98 3533 78 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 9577836
CHEMBL12713 3533 78 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 16135699
CHEMBL12713 3533 78 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 9015795
CHEMBL12713 3533 78 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 9577836
DB06144 3533 78 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 16135699
DB06144 3533 78 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 9015795
DB06144 3533 78 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 9577836
133008 2211 16 None 204 2 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 8642551
3302 2211 16 None 204 2 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 8642551
CHEMBL444309 2211 16 None 204 2 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 8642551
1353 1880 85 None -3 85 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 18308814
1353 1880 85 None -3 85 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 7862709
1353 1880 85 None -3 85 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 8102973
3559 1880 85 None -3 85 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 18308814
3559 1880 85 None -3 85 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 7862709
3559 1880 85 None -3 85 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 8102973
86 1880 85 None -3 85 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 18308814
86 1880 85 None -3 85 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 7862709
86 1880 85 None -3 85 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 8102973
CHEMBL54 1880 85 None -3 85 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 18308814
CHEMBL54 1880 85 None -3 85 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 7862709
CHEMBL54 1880 85 None -3 85 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 8102973
DB00502 1880 85 None -3 85 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 18308814
DB00502 1880 85 None -3 85 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 7862709
DB00502 1880 85 None -3 85 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 8102973
3645619 2985 13 None 4 9 Rat 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 15448188
975 2985 13 None 4 9 Rat 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 15448188
CHEMBL45244 2985 13 None 4 9 Rat 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 15448188
11301655 198 31 None 245 4 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 15992586
8441 198 31 None 245 4 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 15992586
CHEMBL127257 198 31 None 245 4 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 15992586
133079 3581 33 None 1 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 9098699
980 3581 33 None 1 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 9098699
CHEMBL69759 3581 33 None 1 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 9098699
5615 3836 4 None - 1 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 339 6 0 4 4.0 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccccc1)C)C 9098699
5781 3836 4 None - 1 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 339 6 0 4 4.0 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccccc1)C)C 9098699
CHEMBL1179189 3836 4 None - 1 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 339 6 0 4 4.0 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccccc1)C)C 9098699
3303 2213 41 None 1 15 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 8642550
5311200 2213 41 None 1 15 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 8642550
CHEMBL267014 2213 41 None 1 15 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 8642550
179 396 107 None -50 50 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 396 107 None -50 50 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 396 107 None -50 50 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 396 107 None -50 50 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 396 107 None -50 50 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
243 3153 85 None -12 34 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3052762 3153 85 None -12 34 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3502 3153 85 None -12 34 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
CHEMBL117287 3153 85 None -12 34 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
DB06480 3153 85 None -12 34 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
213 3792 50 None -3 43 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 3792 50 None -3 43 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 3792 50 None -3 43 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 3792 50 None -3 43 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 3792 50 None -3 43 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2342 592 0 None -1 6 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 404 6 0 6 2.4 CCN(C(=O)C1CN2CCc3c(C2CC1OC(=O)C)cc(c(c3)OC)OC)CC None
331 592 0 None -1 6 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 404 6 0 6 2.4 CCN(C(=O)C1CN2CCc3c(C2CC1OC(=O)C)cc(c(c3)OC)OC)CC None
7124 592 0 None -1 6 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 404 6 0 6 2.4 CCN(C(=O)C1CN2CCc3c(C2CC1OC(=O)C)cc(c(c3)OC)OC)CC None
CHEMBL1201250 592 0 None -1 6 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 404 6 0 6 2.4 CCN(C(=O)C1CN2CCc3c(C2CC1OC(=O)C)cc(c(c3)OC)OC)CC None
DB00767 592 0 None -1 6 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 404 6 0 6 2.4 CCN(C(=O)C1CN2CCc3c(C2CC1OC(=O)C)cc(c(c3)OC)OC)CC None
5281878 1630 33 None -14 16 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 1630 33 None -14 16 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 1630 33 None -14 16 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 1630 33 None -14 16 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 1630 33 None -14 16 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 1630 33 None -14 16 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 1630 33 None -14 16 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
11976 907 54 None -2 23 Human 8.0 pKi None 8.0 Binding
NoneNone
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
667467 907 54 None -2 23 Human 8.0 pKi None 8.0 Binding
NoneNone
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
CHEMBL908 907 54 None -2 23 Human 8.0 pKi None 8.0 Binding
NoneNone
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
DB01239 907 54 None -2 23 Human 8.0 pKi None 8.0 Binding
NoneNone
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
5567 42556 24 None -11 7 Human 8.0 pKi None 8.0 Binding
NoneNone
Drug Central 409 6 1 3 4.8 O=C(CCCN1CCC(O)(c2cccc(C(F)(F)F)c2)CC1)c1ccc(F)cc1 None
CHEMBL15023 42556 24 None -11 7 Human 8.0 pKi None 8.0 Binding
NoneNone
Drug Central 409 6 1 3 4.8 O=C(CCCN1CCC(O)(c2cccc(C(F)(F)F)c2)CC1)c1ccc(F)cc1 None
6603897 2216 19 None 5 2 Rat 10.0 pKi None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 418 3 1 3 3.5 Ic1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10617689
978 2216 19 None 5 2 Rat 10.0 pKi None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 418 3 1 3 3.5 Ic1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10617689
CHEMBL60518 2216 19 None 5 2 Rat 10.0 pKi None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 418 3 1 3 3.5 Ic1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10617689
37459 735 10 None -123 24 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 8967990
62 735 10 None -123 24 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 8967990
CHEMBL8514 735 10 None -123 24 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 8967990
3408722 2674 41 None -1318 5 Rat 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 365 7 1 4 3.7 CCCCN1CCCC1CNC(=O)c1cc(C#N)c2c(c1OC)cccc2 10617689
44 2674 41 None -1318 5 Rat 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 365 7 1 4 3.7 CCCCN1CCCC1CNC(=O)c1cc(C#N)c2c(c1OC)cccc2 10617689
CHEMBL286252 2674 41 None -1318 5 Rat 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 365 7 1 4 3.7 CCCCN1CCCC1CNC(=O)c1cc(C#N)c2c(c1OC)cccc2 10617689
1153 1598 53 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
12668023 1598 53 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
30026874 1598 53 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
30026875 1598 53 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
3341 1598 53 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
6603851 1598 53 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
933 1598 53 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
939 1598 53 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
985 1598 53 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
CHEMBL1160786 1598 53 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
CHEMBL1161520 1598 53 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
CHEMBL588 1598 53 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
DB00800 1598 53 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
2202 3083 91 None -2 21 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
4850 3083 91 None -2 21 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
49 3083 91 None -2 21 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
CHEMBL1371770 3083 91 None -2 21 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
DB12478 3083 91 None -2 21 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
57267 1563 11 None -416 4 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 6 2 4 2.8 CCN1CCC[C@H]1CNC(=O)c1c(O)c(CC)cc(c1OC)Cl 7475902
966 1563 11 None -416 4 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 6 2 4 2.8 CCN1CCC[C@H]1CNC(=O)c1c(O)c(CC)cc(c1OC)Cl 7475902
CHEMBL8946 1563 11 None -416 4 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 6 2 4 2.8 CCN1CCC[C@H]1CNC(=O)c1c(O)c(CC)cc(c1OC)Cl 7475902
DB15492 1563 11 None -416 4 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 6 2 4 2.8 CCN1CCC[C@H]1CNC(=O)c1c(O)c(CC)cc(c1OC)Cl 7475902
2105 3005 34 None -48 33 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
47811 3005 34 None -48 33 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
48 3005 34 None -48 33 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
CHEMBL531 3005 34 None -48 33 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
DB01186 3005 34 None -48 33 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
242 467 117 None -87 51 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10617689
34 467 117 None -87 51 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10617689
60795 467 117 None -87 51 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10617689
CHEMBL1112 467 117 None -87 51 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10617689
DB01238 467 117 None -87 51 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10617689
37 766 56 None -7 17 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
460 766 56 None -7 17 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
54746 766 56 None -7 17 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
CHEMBL1201087 766 56 None -7 17 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
DB00248 766 56 None -7 17 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
681 1437 65 None -7 38 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10617689
940 1437 65 None -7 38 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10617689
947 1437 65 None -7 38 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10617689
CHEMBL59 1437 65 None -7 38 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10617689
DB00988 1437 65 None -7 38 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10617689
135398737 944 89 None -13 91 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8102973
38 944 89 None -13 91 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8102973
722 944 89 None -13 91 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8102973
CHEMBL42 944 89 None -13 91 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8102973
DB00363 944 89 None -13 91 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8102973
2726 906 64 None -8 72 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 8102973
621 906 64 None -8 72 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 8102973
83 906 64 None -8 72 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 8102973
CHEMBL71 906 64 None -8 72 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 8102973
DB00477 906 64 None -8 72 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 8102973
11429930 3289 0 None - 1 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 415 8 3 7 1.9 COc1cc(ccc1O)N1CCN(CC1)CC(COc1ccccc1NC(=O)C)O 15448188
982 3289 0 None - 1 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 415 8 3 7 1.9 COc1cc(ccc1O)N1CCN(CC1)CC(COc1ccccc1NC(=O)C)O 15448188
2601 3721 30 None -7 21 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
443951 3721 30 None -7 21 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
56 3721 30 None -7 21 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
CHEMBL73151 3721 30 None -7 21 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
DB13399 3721 30 None -7 21 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
219050 3321 21 None -58 21 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 12388666
52 3321 21 None -58 21 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 12388666
CHEMBL431367 3321 21 None -58 21 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 12388666
1588 2294 24 None -23 43 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
28864 2294 24 None -23 43 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
43 2294 24 None -23 43 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
CHEMBL157138 2294 24 None -23 43 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
DB00589 2294 24 None -23 43 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
133079 3581 33 None -1 4 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 15448188
980 3581 33 None -1 4 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 15448188
CHEMBL69759 3581 33 None -1 4 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 15448188
10336538 1595 44 None 3 8 Rat 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 15448188
974 1595 44 None 3 8 Rat 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 15448188
CHEMBL310843 1595 44 None 3 8 Rat 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 15448188
2470 3596 46 None -20 59 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7475902
3300 3596 46 None -20 59 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7475902
5265 3596 46 None -20 59 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7475902
99 3596 46 None -20 59 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7475902
CHEMBL267930 3596 46 None -20 59 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7475902
973 1154 33 None 9 6 Rat 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 15448188
9796720 1154 33 None 9 6 Rat 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 15448188
CHEMBL77395 1154 33 None 9 6 Rat 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 15448188
977 1155 3 None 10 4 Rat 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 4 0 5 2.7 Fc1ccc(cc1)OC[C@@H]1CC[C@@H]2N(C1)CCN(C2)c1ncc(cn1)F 15448188
9820261 1155 3 None 10 4 Rat 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 4 0 5 2.7 Fc1ccc(cc1)OC[C@@H]1CC[C@@H]2N(C1)CCN(C2)c1ncc(cn1)F 15448188
CHEMBL66227 1155 3 None 10 4 Rat 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 4 0 5 2.7 Fc1ccc(cc1)OC[C@@H]1CC[C@@H]2N(C1)CCN(C2)c1ncc(cn1)F 15448188
188942 2778 38 None 12 4 Rat 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 15448188
3297 2778 38 None 12 4 Rat 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 15448188
979 2778 38 None 12 4 Rat 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 15448188
CHEMBL103772 2778 38 None 12 4 Rat 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 15448188
5041 3242 5 None 1 5 Rat 9.6 pKi None 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 15448188
981 3242 5 None 1 5 Rat 9.6 pKi None 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 15448188
CHEMBL4096543 3242 5 None 1 5 Rat 9.6 pKi None 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 15448188