Ligand source activities (1 row/activity)





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1218 3614 30 None 177 4 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/acsmedchemlett.9b00050
938 3614 30 None 177 4 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/acsmedchemlett.9b00050
CHEMBL353335 3614 30 None 177 4 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/acsmedchemlett.9b00050
86764103 132435 13 None -2 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 389 5 1 6 3.1 Cc1cc(Oc2ncccc2OC(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C 10.1021/acsmedchemlett.9b00050
CHEMBL3697578 132435 13 None -2 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 389 5 1 6 3.1 Cc1cc(Oc2ncccc2OC(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C 10.1021/acsmedchemlett.9b00050
11938 2410 7 None -69 4 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse D5 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins by HTRF assayAgonist activity at mouse D5 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins by HTRF assay
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
146192952 2410 7 None -69 4 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse D5 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins by HTRF assayAgonist activity at mouse D5 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins by HTRF assay
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
CHEMBL4468760 2410 7 None -69 4 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse D5 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins by HTRF assayAgonist activity at mouse D5 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins by HTRF assay
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
681 1464 72 None 1 15 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
940 1464 72 None 1 15 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
947 1464 72 None 1 15 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
CHEMBL59 1464 72 None 1 15 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
DB00988 1464 72 None 1 15 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
75202022 170808 2 None -1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 363 3 1 6 3.3 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)c(=O)[nH]c(=O)n1C 10.1021/acsmedchemlett.9b00050
CHEMBL4453318 170808 2 None -1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 363 3 1 6 3.3 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)c(=O)[nH]c(=O)n1C 10.1021/acsmedchemlett.9b00050
11681599 75171 0 None - 0 Human 10.3 pKi = 10.3 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2ccc(O)c(Cl)c2CC1 10.1021/jm051237e
CHEMBL203637 75171 0 None - 0 Human 10.3 pKi = 10.3 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2ccc(O)c(Cl)c2CC1 10.1021/jm051237e
11623343 140840 1 None - 0 Human 9.3 pKi = 9.3 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 283 0 2 3 2.7 CN1CCc2cc(O)ccc2Cc2ccc(O)cc2CC1 10.1021/jm051237e
CHEMBL381936 140840 1 None - 0 Human 9.3 pKi = 9.3 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 283 0 2 3 2.7 CN1CCc2cc(O)ccc2Cc2ccc(O)cc2CC1 10.1021/jm051237e
11493746 141321 0 None - 0 Human 8.9 pKi = 8.9 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 335 0 1 2 4.3 CN1CCc2ccccc2Cc2cc(Cl)c(O)c(Cl)c2CC1 10.1021/jm051237e
CHEMBL383451 141321 0 None - 0 Human 8.9 pKi = 8.9 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 335 0 1 2 4.3 CN1CCc2ccccc2Cc2cc(Cl)c(O)c(Cl)c2CC1 10.1021/jm051237e
11595240 140186 0 None - 0 Human 8.8 pKi = 8.8 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2c(ccc(O)c2Cl)CC1 10.1021/jm051237e
CHEMBL380464 140186 0 None - 0 Human 8.8 pKi = 8.8 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2c(ccc(O)c2Cl)CC1 10.1021/jm051237e
11558055 73150 1 None - 0 Human 8.8 pKi = 8.8 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm051237e
CHEMBL1204122 73150 1 None - 0 Human 8.8 pKi = 8.8 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm051237e
CHEMBL201170 73150 1 None - 0 Human 8.8 pKi = 8.8 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm051237e
11558055 73150 1 None - 0 Human 8.8 pKi = 8.8 Functional
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm050846j
CHEMBL1204122 73150 1 None - 0 Human 8.8 pKi = 8.8 Functional
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm050846j
CHEMBL201170 73150 1 None - 0 Human 8.8 pKi = 8.8 Functional
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm050846j
11522339 75250 1 None - 0 Human 8.0 pKi = 8.0 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2c(O)cccc2CC1 10.1021/jm051237e
CHEMBL203689 75250 1 None - 0 Human 8.0 pKi = 8.0 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2c(O)cccc2CC1 10.1021/jm051237e
11500677 140846 1 None - 0 Human 6.0 pKi = 6.0 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)Cc1ccccc1CCN(C)CC2 10.1021/jm051237e
CHEMBL381946 140846 1 None - 0 Human 6.0 pKi = 6.0 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)Cc1ccccc1CCN(C)CC2 10.1021/jm051237e
11573806 75414 0 None - 0 Human 7.9 pKi = 7.9 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 311 2 0 3 3.3 COc1ccc2c(c1)CCN(C)CCc1cc(OC)ccc1C2 10.1021/jm051237e
CHEMBL204065 75414 0 None - 0 Human 7.9 pKi = 7.9 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 311 2 0 3 3.3 COc1ccc2c(c1)CCN(C)CCc1cc(OC)ccc1C2 10.1021/jm051237e
5249952 73406 7 None - 0 Human 7.0 pKi = 7.0 Functional
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 304 1 1 1 4.4 CN1CCc2c([nH]c3ccccc23)CC(c2ccccc2)CC1 10.1021/jm050846j
CHEMBL201584 73406 7 None - 0 Human 7.0 pKi = 7.0 Functional
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 304 1 1 1 4.4 CN1CCc2c([nH]c3ccccc23)CC(c2ccccc2)CC1 10.1021/jm050846j
4350931 169311 44 None - 1 Human 7.9 pKi = 7.9 Functional
Activity at human D5 dopamine receptor expressed in HEK293 cells by calcium fluorescence assayActivity at human D5 dopamine receptor expressed in HEK293 cells by calcium fluorescence assay
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
CHEMBL441618 169311 44 None - 1 Human 7.9 pKi = 7.9 Functional
Activity at human D5 dopamine receptor expressed in HEK293 cells by calcium fluorescence assayActivity at human D5 dopamine receptor expressed in HEK293 cells by calcium fluorescence assay
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
4350931 169311 44 None - 1 Human 7.9 pKi = 7.9 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm051237e
CHEMBL441618 169311 44 None - 1 Human 7.9 pKi = 7.9 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm051237e
42626289 148077 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human Dopamine D5 receptor in HEK293 cells assessed as change in SKF 38393-induced intracellular calcium responseAntagonist activity at human Dopamine D5 receptor in HEK293 cells assessed as change in SKF 38393-induced intracellular calcium response
ChEMBL 379 7 0 4 3.3 COc1ccccc1N1CCN(CCCCN2Cc3ccccc3C2=O)CC1 10.1016/j.bmc.2007.06.002
CHEMBL393492 148077 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human Dopamine D5 receptor in HEK293 cells assessed as change in SKF 38393-induced intracellular calcium responseAntagonist activity at human Dopamine D5 receptor in HEK293 cells assessed as change in SKF 38393-induced intracellular calcium response
ChEMBL 379 7 0 4 3.3 COc1ccccc1N1CCN(CCCCN2Cc3ccccc3C2=O)CC1 10.1016/j.bmc.2007.06.002
11566745 74692 0 None - 0 Human 8.6 pKi = 8.6 Functional
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 283 0 2 3 2.7 CN1CCc2ccccc2Cc2cc(O)c(O)cc2CC1 10.1021/jm050846j
CHEMBL1202298 74692 0 None - 0 Human 8.6 pKi = 8.6 Functional
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 283 0 2 3 2.7 CN1CCc2ccccc2Cc2cc(O)c(O)cc2CC1 10.1021/jm050846j
CHEMBL203029 74692 0 None - 0 Human 8.6 pKi = 8.6 Functional
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 283 0 2 3 2.7 CN1CCc2ccccc2Cc2cc(O)c(O)cc2CC1 10.1021/jm050846j
16090814 81579 0 None - 0 Human 8.6 pKi = 8.6 Functional
Activity at human D5 dopamine receptor expressed in HEK293 cells by calcium fluorescence assayActivity at human D5 dopamine receptor expressed in HEK293 cells by calcium fluorescence assay
ChEMBL 304 0 1 1 4.2 CN1CCCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
CHEMBL216258 81579 0 None - 0 Human 8.6 pKi = 8.6 Functional
Activity at human D5 dopamine receptor expressed in HEK293 cells by calcium fluorescence assayActivity at human D5 dopamine receptor expressed in HEK293 cells by calcium fluorescence assay
ChEMBL 304 0 1 1 4.2 CN1CCCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
11716449 141213 0 None - 0 Human 7.7 pKi = 7.7 Functional
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 304 1 1 1 4.2 CCN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm050846j
CHEMBL382850 141213 0 None - 0 Human 7.7 pKi = 7.7 Functional
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 304 1 1 1 4.2 CCN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm050846j
5249956 73393 1 None - 0 Human 8.5 pKi = 8.5 Functional
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1021/jm050846j
CHEMBL201525 73393 1 None - 0 Human 8.5 pKi = 8.5 Functional
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1021/jm050846j
11573628 74697 0 None - 0 Human 8.5 pKi = 8.5 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2cc(O)c(Cl)cc2CC1 10.1021/jm051237e
CHEMBL203047 74697 0 None - 0 Human 8.5 pKi = 8.5 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2cc(O)c(Cl)cc2CC1 10.1021/jm051237e
11637457 73085 1 None - 0 Human 7.5 pKi = 7.5 Functional
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2ccsc2CC1 10.1021/jm050846j
CHEMBL201093 73085 1 None - 0 Human 7.5 pKi = 7.5 Functional
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2ccsc2CC1 10.1021/jm050846j
9992499 73384 0 None - 0 Human 6.5 pKi = 6.5 Functional
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 254 0 0 2 2.6 CN1CCc2ccccc2Cc2ccn(C)c2CC1 10.1021/jm050846j
CHEMBL201483 73384 0 None - 0 Human 6.5 pKi = 6.5 Functional
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 254 0 0 2 2.6 CN1CCc2ccccc2Cc2ccn(C)c2CC1 10.1021/jm050846j
11716438 140880 1 None - 0 Human 7.4 pKi = 7.4 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2cc(O)ccc2CC1 10.1021/jm051237e
CHEMBL382010 140880 1 None - 0 Human 7.4 pKi = 7.4 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2cc(O)ccc2CC1 10.1021/jm051237e
44436300 148834 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human Dopamine D5 receptor in HEK293 cells assessed as change in SKF 38393-induced intracellular calcium responseAntagonist activity at human Dopamine D5 receptor in HEK293 cells assessed as change in SKF 38393-induced intracellular calcium response
ChEMBL 399 6 0 5 2.4 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2ccccc2)CC1 10.1016/j.bmc.2007.06.002
CHEMBL394110 148834 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human Dopamine D5 receptor in HEK293 cells assessed as change in SKF 38393-induced intracellular calcium responseAntagonist activity at human Dopamine D5 receptor in HEK293 cells assessed as change in SKF 38393-induced intracellular calcium response
ChEMBL 399 6 0 5 2.4 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2ccccc2)CC1 10.1016/j.bmc.2007.06.002
11558247 75420 0 None - 0 Human 7.4 pKi = 7.4 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 282 0 2 3 2.6 CN1CCc2ccccc2Cc2cc(N)c(O)cc2CC1 10.1021/jm051237e
CHEMBL204098 75420 0 None - 0 Human 7.4 pKi = 7.4 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 282 0 2 3 2.6 CN1CCc2ccccc2Cc2cc(N)c(O)cc2CC1 10.1021/jm051237e
75201901 166423 19 None - 4 Human 8.3 pKi = 8.3 Functional
Agonist activity at dopamine D5 receptor (unknown origin)Agonist activity at dopamine D5 receptor (unknown origin)
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b01622
CHEMBL4277264 166423 19 None - 4 Human 8.3 pKi = 8.3 Functional
Agonist activity at dopamine D5 receptor (unknown origin)Agonist activity at dopamine D5 receptor (unknown origin)
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b01622
11536995 139553 1 None - 0 Human 7.3 pKi = 7.3 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 281 1 0 2 3.3 COc1cccc2c1Cc1ccccc1CCN(C)CC2 10.1021/jm051237e
CHEMBL379662 139553 1 None - 0 Human 7.3 pKi = 7.3 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 281 1 0 2 3.3 COc1cccc2c1Cc1ccccc1CCN(C)CC2 10.1021/jm051237e
11718008 75289 0 None - 0 Human 7.2 pKi = 7.2 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 349 1 0 2 4.6 COc1c(Cl)cc2c(c1Cl)Cc1ccccc1CCN(C)CC2 10.1021/jm051237e
CHEMBL203734 75289 0 None - 0 Human 7.2 pKi = 7.2 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 349 1 0 2 4.6 COc1c(Cl)cc2c(c1Cl)Cc1ccccc1CCN(C)CC2 10.1021/jm051237e
44408818 140163 1 None - 0 Human 8.1 pKi = 8.1 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)CCN(C)CCc1ccccc1C2 10.1021/jm051237e
CHEMBL380330 140163 1 None - 0 Human 8.1 pKi = 8.1 Functional
Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)CCN(C)CCc1ccccc1C2 10.1021/jm051237e
16090821 81831 0 None - 0 Human 7.1 pKi = 7.1 Functional
Activity at human D5 dopamine receptor expressed in HEK293 cells by calcium fluorescence assayActivity at human D5 dopamine receptor expressed in HEK293 cells by calcium fluorescence assay
ChEMBL 304 0 1 1 4.2 CN1CCCc2c([nH]c3ccccc23)Cc2ccccc2CC1 10.1021/jm060213k
CHEMBL216439 81831 0 None - 0 Human 7.1 pKi = 7.1 Functional
Activity at human D5 dopamine receptor expressed in HEK293 cells by calcium fluorescence assayActivity at human D5 dopamine receptor expressed in HEK293 cells by calcium fluorescence assay
ChEMBL 304 0 1 1 4.2 CN1CCCc2c([nH]c3ccccc23)Cc2ccccc2CC1 10.1021/jm060213k
122324 205 22 None -128 4 Human 6.6 pEC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 16318870
6077 205 22 None -128 4 Human 6.6 pEC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 16318870
CHEMBL86931 205 22 None -128 4 Human 6.6 pEC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 16318870




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3158 56265 27 None - 20 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1628227 56265 27 None - 20 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
1353 1909 93 None -54 86 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3559 1909 93 None -54 86 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
86 1909 93 None -54 86 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
CHEMBL54 1909 93 None -54 86 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
DB00502 1909 93 None -54 86 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
1613 2346 53 None -6 45 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
205 2346 53 None -6 45 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
3964 2346 53 None -6 45 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
CHEMBL831 2346 53 None -6 45 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
DB00408 2346 53 None -6 45 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
135398745 2912 112 None -26 66 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
47 2912 112 None -26 66 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
CHEMBL715 2912 112 None -26 66 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
DB00334 2912 112 None -26 66 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
191 403 98 None - 29 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
201 403 98 None - 29 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
2170 403 98 None - 29 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
CHEMBL1113 403 98 None - 29 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
DB00543 403 98 None - 29 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
2284 3180 33 None - 29 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
4926 3180 33 None - 29 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
7281 3180 33 None - 29 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL564 3180 33 None - 29 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00420 3180 33 None - 29 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
1427 2011 54 None - 27 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
357 2011 54 None - 27 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
3696 2011 54 None - 27 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL11 2011 54 None - 27 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00458 2011 54 None - 27 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
85090335 181112 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 359 3 0 5 3.4 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1ccccc1 10.1016/j.bmcl.2020.127696
CHEMBL4760355 181112 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 359 3 0 5 3.4 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1ccccc1 10.1016/j.bmcl.2020.127696
168295528 193029 0 None -4 20 Human 5.0 pEC50 = 5.0 Binding
Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK 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 193029 0 None -4 20 Human 5.0 pEC50 = 5.0 Binding
Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK 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 193029 0 None -4 20 Human 5.0 pEC50 = 5.0 Binding
Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK 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
85090318 179443 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 413 3 0 5 4.7 Cc1ccc(-n2c(CC3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4740497 179443 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 413 3 0 5 4.7 Cc1ccc(-n2c(CC3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
168290235 192966 0 None -16 20 Human 4.6 pEC50 = 4.6 Binding
Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK 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 192966 0 None -16 20 Human 4.6 pEC50 = 4.6 Binding
Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK 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 192966 0 None -16 20 Human 4.6 pEC50 = 4.6 Binding
Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK 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
85090319 180608 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 401 3 0 6 3.9 COc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4754602 180608 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 401 3 0 6 3.9 COc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
85090328 181033 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 385 2 0 5 4.2 Cc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4759339 181033 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 385 2 0 5 4.2 Cc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
85090333 181299 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 399 2 0 5 4.6 Cc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4762375 181299 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 399 2 0 5 4.6 Cc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
85090332 180717 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 435 3 0 6 4.6 COc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
CHEMBL4755709 180717 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 435 3 0 6 4.6 COc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
2030130 20977 16 None - 0 Human 7.5 pEC50 = 7.5 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 385 2 0 5 4.3 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL1311333 20977 16 None - 0 Human 7.5 pEC50 = 7.5 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 385 2 0 5 4.3 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
85090338 180759 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 389 4 0 6 3.4 COc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4756163 180759 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 389 4 0 6 3.4 COc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
168294767 193017 0 None -4 20 Human 4.5 pEC50 = 4.5 Binding
Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK 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 193017 0 None -4 20 Human 4.5 pEC50 = 4.5 Binding
Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK 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 193017 0 None -4 20 Human 4.5 pEC50 = 4.5 Binding
Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK 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
164612037 185375 0 None -4 20 Human 5.4 pEC50 = 5.4 Binding
Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK 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 185375 0 None -4 20 Human 5.4 pEC50 = 5.4 Binding
Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK 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
85090324 180690 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 405 2 0 5 4.5 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4755481 180690 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 405 2 0 5 4.5 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
85090325 179747 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 405 2 0 5 4.5 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4744261 179747 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 405 2 0 5 4.5 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
85090321 182811 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 373 3 0 5 3.7 Cc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4790909 182811 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 373 3 0 5 3.7 Cc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
85090329 182680 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 419 2 0 5 4.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4789255 182680 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 419 2 0 5 4.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
11938 2410 7 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
Positive allosteric modulation of mouse D5 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assayPositive allosteric modulation of mouse D5 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assay
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
146192952 2410 7 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
Positive allosteric modulation of mouse D5 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assayPositive allosteric modulation of mouse D5 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assay
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
CHEMBL4468760 2410 7 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
Positive allosteric modulation of mouse D5 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assayPositive allosteric modulation of mouse D5 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assay
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
85090334 180623 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 399 3 0 5 4.4 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4754761 180623 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 399 3 0 5 4.4 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
85090323 181920 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 393 3 0 5 4.1 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4779641 181920 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 393 3 0 5 4.1 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2020.127696
85090326 182771 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 423 4 0 6 4.1 COc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
CHEMBL4790277 182771 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 423 4 0 6 4.1 COc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
85090331 181451 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 449 3 0 6 4.9 COc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
CHEMBL4764398 181451 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 449 3 0 6 4.9 COc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
85090322 179457 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 415 3 0 6 4.3 COc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4740678 179457 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 415 3 0 6 4.3 COc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
85090339 182303 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 393 3 0 5 4.1 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1cccc(Cl)c1 10.1016/j.bmcl.2020.127696
CHEMBL4784143 182303 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 393 3 0 5 4.1 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1cccc(Cl)c1 10.1016/j.bmcl.2020.127696
85090320 182561 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 433 3 0 5 5.0 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4787728 182561 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 433 3 0 5 5.0 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
4901726 180797 9 None - 0 Human 7.1 pEC50 = 7.1 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 419 2 0 5 4.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4756486 180797 9 None - 0 Human 7.1 pEC50 = 7.1 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 419 2 0 5 4.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
76284418 182316 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 371 2 0 5 3.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4784295 182316 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 371 2 0 5 3.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
136326241 179426 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 295 1 1 4 2.4 Cn1c2ccccc2c(=O)c2c(=O)[nH]c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4740312 179426 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 295 1 1 4 2.4 Cn1c2ccccc2c(=O)c2c(=O)[nH]c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
85090330 181071 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 463 4 0 6 5.0 COc1ccc(-n2c(CC3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
CHEMBL4759814 181071 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 463 4 0 6 5.0 COc1ccc(-n2c(CC3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
85090337 183279 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 433 3 0 5 5.0 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4796761 183279 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 433 3 0 5 5.0 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
76284419 183246 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 343 2 0 5 3.1 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4796389 183246 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 81.7 nM)
ChEMBL 343 2 0 5 3.1 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CC3)nc21 10.1016/j.bmcl.2020.127696
3036864 202752 19 None -3 28 Human 9.8 pIC50 = 9.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2013.03.016
CHEMBL1256645 202752 19 None -3 28 Human 9.8 pIC50 = 9.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2013.03.016
CHEMBL1814790 202752 19 None -3 28 Human 9.8 pIC50 = 9.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2013.03.016
CHEMBL62 202752 19 None -3 28 Human 9.8 pIC50 = 9.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2013.03.016
3036864 202752 19 None -3 28 Human 9.4 pIC50 = 9.4 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2013.01.044
CHEMBL1256645 202752 19 None -3 28 Human 9.4 pIC50 = 9.4 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2013.01.044
CHEMBL1814790 202752 19 None -3 28 Human 9.4 pIC50 = 9.4 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2013.01.044
CHEMBL62 202752 19 None -3 28 Human 9.4 pIC50 = 9.4 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2013.01.044
5018 3547 13 None -2 10 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]SCH 23390 from human recombinant D5 receptor expressed in GH4 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]SCH 23390 from human recombinant D5 receptor expressed in GH4 cells measured after 60 mins by scintillation counting method
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2016.11.014
943 3547 13 None -2 10 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]SCH 23390 from human recombinant D5 receptor expressed in GH4 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]SCH 23390 from human recombinant D5 receptor expressed in GH4 cells measured after 60 mins by scintillation counting method
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2016.11.014
946 3547 13 None -2 10 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]SCH 23390 from human recombinant D5 receptor expressed in GH4 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]SCH 23390 from human recombinant D5 receptor expressed in GH4 cells measured after 60 mins by scintillation counting method
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2016.11.014
CHEMBL13668 3547 13 None -2 10 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]SCH 23390 from human recombinant D5 receptor expressed in GH4 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]SCH 23390 from human recombinant D5 receptor expressed in GH4 cells measured after 60 mins by scintillation counting method
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2016.11.014
5018 3547 13 None -2 10 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]SCH23390 from human recombinant Dopamine D5 receptor expressed in GH4 cellsDisplacement of [3H]SCH23390 from human recombinant Dopamine D5 receptor expressed in GH4 cells
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2016.03.006
943 3547 13 None -2 10 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]SCH23390 from human recombinant Dopamine D5 receptor expressed in GH4 cellsDisplacement of [3H]SCH23390 from human recombinant Dopamine D5 receptor expressed in GH4 cells
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2016.03.006
946 3547 13 None -2 10 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]SCH23390 from human recombinant Dopamine D5 receptor expressed in GH4 cellsDisplacement of [3H]SCH23390 from human recombinant Dopamine D5 receptor expressed in GH4 cells
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2016.03.006
CHEMBL13668 3547 13 None -2 10 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]SCH23390 from human recombinant Dopamine D5 receptor expressed in GH4 cellsDisplacement of [3H]SCH23390 from human recombinant Dopamine D5 receptor expressed in GH4 cells
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2016.03.006
3036864 202752 19 None -3 28 Human 9.0 pIC50 = 9.0 Binding
Displacement of radiolabeled SCH-23390 from human dopamine D5 receptorDisplacement of radiolabeled SCH-23390 from human dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm8007618
CHEMBL1256645 202752 19 None -3 28 Human 9.0 pIC50 = 9.0 Binding
Displacement of radiolabeled SCH-23390 from human dopamine D5 receptorDisplacement of radiolabeled SCH-23390 from human dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm8007618
CHEMBL1814790 202752 19 None -3 28 Human 9.0 pIC50 = 9.0 Binding
Displacement of radiolabeled SCH-23390 from human dopamine D5 receptorDisplacement of radiolabeled SCH-23390 from human dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm8007618
CHEMBL62 202752 19 None -3 28 Human 9.0 pIC50 = 9.0 Binding
Displacement of radiolabeled SCH-23390 from human dopamine D5 receptorDisplacement of radiolabeled SCH-23390 from human dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm8007618
10907460 9826 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human dopamine receptor D5Inhibition of human dopamine receptor D5
ChEMBL 521 11 1 3 5.8 CCOc1ccc(CCNC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
CHEMBL113956 9826 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human dopamine receptor D5Inhibition of human dopamine receptor D5
ChEMBL 521 11 1 3 5.8 CCOc1ccc(CCNC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
11071079 110591 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human dopamine receptor D5Inhibition of human dopamine receptor D5
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 110591 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human dopamine receptor D5Inhibition of human dopamine receptor D5
ChEMBL 496 9 0 3 6.0 O=C(OCCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
11730467 11026 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human dopamine receptor D5Inhibition of human dopamine receptor D5
ChEMBL 476 10 0 2 6.0 O=C(CCCc1ccccc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
CHEMBL117537 11026 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human dopamine receptor D5Inhibition of human dopamine receptor D5
ChEMBL 476 10 0 2 6.0 O=C(CCCc1ccccc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
11113605 10505 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human dopamine receptor D5Inhibition of human dopamine receptor D5
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 10505 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human dopamine receptor D5Inhibition of human dopamine receptor D5
ChEMBL 480 9 0 2 5.8 O=C(CCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
10918307 9983 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human dopamine receptor D5Inhibition of human dopamine receptor D5
ChEMBL 514 5 1 7 2.6 CNC(=O)CN1CN(c2ccccc2)C2(CCN(C(=O)OCc3cc4c(cc3Cl)OCO4)CC2)C1=O 10.1021/jm010878g
CHEMBL114825 9983 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human dopamine receptor D5Inhibition of human dopamine receptor D5
ChEMBL 514 5 1 7 2.6 CNC(=O)CN1CN(c2ccccc2)C2(CCN(C(=O)OCc3cc4c(cc3Cl)OCO4)CC2)C1=O 10.1021/jm010878g
11059058 10089 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of human dopamine receptor D5Inhibition of human dopamine receptor D5
ChEMBL 429 3 1 7 4.1 O=C(OCc1cc2c(cc1Cl)OCO2)N1CCC(n2c(O)nc3ccccc32)CC1 10.1021/jm010878g
CHEMBL115444 10089 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of human dopamine receptor D5Inhibition of human dopamine receptor D5
ChEMBL 429 3 1 7 4.1 O=C(OCc1cc2c(cc1Cl)OCO2)N1CCC(n2c(O)nc3ccccc32)CC1 10.1021/jm010878g
11005810 10464 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human dopamine receptor D5Inhibition of human dopamine receptor D5
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 10464 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human dopamine receptor D5Inhibition of human dopamine receptor D5
ChEMBL 517 10 1 4 6.2 N#Cc1ccc(CCOC(=O)NC2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
10885636 111014 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of human dopamine receptor D5Inhibition of human dopamine receptor D5
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 111014 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of human dopamine receptor D5Inhibition of human dopamine receptor D5
ChEMBL 503 9 0 4 5.7 N#Cc1ccc(CCOC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
164612037 185375 0 None -4 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK 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 185375 0 None -4 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK 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 192966 0 None -16 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK 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 192966 0 None -16 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK 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 192966 0 None -16 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK 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 193017 0 None -4 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK 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 193017 0 None -4 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK 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 193017 0 None -4 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK 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 193029 0 None -4 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK 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 193029 0 None -4 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK 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 193029 0 None -4 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK 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
11681599 75171 0 None 12 6 Human 10.2 pKi = 10.2 Binding
Binding affinity to D5 dopamine receptor by radioligand binding assayBinding affinity to D5 dopamine receptor by radioligand binding assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2ccc(O)c(Cl)c2CC1 10.1021/jm051237e
CHEMBL203637 75171 0 None 12 6 Human 10.2 pKi = 10.2 Binding
Binding affinity to D5 dopamine receptor by radioligand binding assayBinding affinity to D5 dopamine receptor by radioligand binding assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2ccc(O)c(Cl)c2CC1 10.1021/jm051237e
3036864 202752 19 None -3 28 Human 9.8 pKi = 9.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2013.01.044
CHEMBL1256645 202752 19 None -3 28 Human 9.8 pKi = 9.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2013.01.044
CHEMBL1814790 202752 19 None -3 28 Human 9.8 pKi = 9.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2013.01.044
CHEMBL62 202752 19 None -3 28 Human 9.8 pKi = 9.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand displacement assayBinding affinity to human dopamine D5 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2013.01.044
16665071 93399 0 None 7 4 Human 9.6 pKi = 9.6 Binding
Binding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cellsBinding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cells
ChEMBL 334 1 0 3 3.8 COc1ccc2c(c1)c1c(n2C)Cc2ccccc2CCN(C)CC1 10.1016/j.bmcl.2006.11.093
CHEMBL245764 93399 0 None 7 4 Human 9.6 pKi = 9.6 Binding
Binding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cellsBinding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cells
ChEMBL 334 1 0 3 3.8 COc1ccc2c(c1)c1c(n2C)Cc2ccccc2CCN(C)CC1 10.1016/j.bmcl.2006.11.093
3036864 202752 19 None -3 28 Human 9.5 pKi = 9.5 Binding
Antagonist activity at dopamine D5 receptor (unknown origin)Antagonist activity at dopamine D5 receptor (unknown origin)
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2020.127305
CHEMBL1256645 202752 19 None -3 28 Human 9.5 pKi = 9.5 Binding
Antagonist activity at dopamine D5 receptor (unknown origin)Antagonist activity at dopamine D5 receptor (unknown origin)
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2020.127305
CHEMBL1814790 202752 19 None -3 28 Human 9.5 pKi = 9.5 Binding
Antagonist activity at dopamine D5 receptor (unknown origin)Antagonist activity at dopamine D5 receptor (unknown origin)
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2020.127305
CHEMBL62 202752 19 None -3 28 Human 9.5 pKi = 9.5 Binding
Antagonist activity at dopamine D5 receptor (unknown origin)Antagonist activity at dopamine D5 receptor (unknown origin)
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2020.127305
11465618 102396 23 None -1 19 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]SCH 23390 from recombinant human D5 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]SCH 23390 from recombinant human D5 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 102396 23 None -1 19 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]SCH 23390 from recombinant human D5 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]SCH 23390 from recombinant human D5 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 102396 23 None -1 19 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]SCH 23390 from recombinant human D5 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]SCH 23390 from recombinant human D5 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
44439943 93364 0 None 1 4 Human 9.4 pKi = 9.4 Binding
Binding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cellsBinding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cells
ChEMBL 306 0 2 2 3.5 CN1CCc2ccccc2Cc2[nH]c3ccc(O)cc3c2CC1 10.1016/j.bmcl.2006.11.093
CHEMBL245570 93364 0 None 1 4 Human 9.4 pKi = 9.4 Binding
Binding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cellsBinding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cells
ChEMBL 306 0 2 2 3.5 CN1CCc2ccccc2Cc2[nH]c3ccc(O)cc3c2CC1 10.1016/j.bmcl.2006.11.093
3036864 202752 19 None -3 28 Human 9.3 pKi = 9.3 Binding
Displacement of radiolabeled SCH-23390 from human dopamine D5 receptorDisplacement of radiolabeled SCH-23390 from human dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm8007618
CHEMBL1256645 202752 19 None -3 28 Human 9.3 pKi = 9.3 Binding
Displacement of radiolabeled SCH-23390 from human dopamine D5 receptorDisplacement of radiolabeled SCH-23390 from human dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm8007618
CHEMBL1814790 202752 19 None -3 28 Human 9.3 pKi = 9.3 Binding
Displacement of radiolabeled SCH-23390 from human dopamine D5 receptorDisplacement of radiolabeled SCH-23390 from human dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm8007618
CHEMBL62 202752 19 None -3 28 Human 9.3 pKi = 9.3 Binding
Displacement of radiolabeled SCH-23390 from human dopamine D5 receptorDisplacement of radiolabeled SCH-23390 from human dopamine D5 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm8007618
6852376 91597 13 None 3 5 Human 9.3 pKi = 9.3 Binding
Agonist activity at dopamine D5 receptor (unknown origin)Agonist activity at dopamine D5 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmcl.2020.127305
CHEMBL1467585 91597 13 None 3 5 Human 9.3 pKi = 9.3 Binding
Agonist activity at dopamine D5 receptor (unknown origin)Agonist activity at dopamine D5 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmcl.2020.127305
CHEMBL24077 91597 13 None 3 5 Human 9.3 pKi = 9.3 Binding
Agonist activity at dopamine D5 receptor (unknown origin)Agonist activity at dopamine D5 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmcl.2020.127305
CHEMBL503958 91597 13 None 3 5 Human 9.3 pKi = 9.3 Binding
Agonist activity at dopamine D5 receptor (unknown origin)Agonist activity at dopamine D5 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmcl.2020.127305
11778580 66125 1 None 5 5 Human 9.2 pKi = 9.2 Binding
Binding affinity for human recombinant dopamine receptor D5Binding affinity for human recombinant dopamine receptor D5
ChEMBL 283 0 1 3 2.9 CN1CCOc2cc(O)ccc2Cc2ccccc2CC1 10.1021/jm049720x
CHEMBL184050 66125 1 None 5 5 Human 9.2 pKi = 9.2 Binding
Binding affinity for human recombinant dopamine receptor D5Binding affinity for human recombinant dopamine receptor D5
ChEMBL 283 0 1 3 2.9 CN1CCOc2cc(O)ccc2Cc2ccccc2CC1 10.1021/jm049720x
16090814 81579 0 None 1 5 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCH 23390 from human D5 dopamine receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human D5 dopamine receptor expressed in HEK293 cells
ChEMBL 304 0 1 1 4.2 CN1CCCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
CHEMBL216258 81579 0 None 1 5 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCH 23390 from human D5 dopamine receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human D5 dopamine receptor expressed in HEK293 cells
ChEMBL 304 0 1 1 4.2 CN1CCCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
11393666 192984 0 None -1 19 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCH 23390 from recombinant human D5 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]SCH 23390 from recombinant human D5 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 192984 0 None -1 19 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCH 23390 from recombinant human D5 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]SCH 23390 from recombinant human D5 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 192984 0 None -1 19 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCH 23390 from recombinant human D5 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]SCH 23390 from recombinant human D5 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
11595240 140186 0 None -3 4 Human 9.0 pKi = 9.0 Binding
Binding affinity to D5 dopamine receptor by radioligand binding assayBinding affinity to D5 dopamine receptor by radioligand binding assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2c(ccc(O)c2Cl)CC1 10.1021/jm051237e
CHEMBL380464 140186 0 None -3 4 Human 9.0 pKi = 9.0 Binding
Binding affinity to D5 dopamine receptor by radioligand binding assayBinding affinity to D5 dopamine receptor by radioligand binding assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2c(ccc(O)c2Cl)CC1 10.1021/jm051237e
11488247 200637 0 None -1 4 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 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 200637 0 None -1 4 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 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
46231784 201336 0 None -2 4 Human 8.9 pKi = 8.9 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 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 201336 0 None -2 4 Human 8.9 pKi = 8.9 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 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
11558055 73150 1 None -2 6 Human 8.8 pKi = 8.8 Binding
Binding affinity to D5 dopamine receptor by radioligand binding assayBinding affinity to D5 dopamine receptor by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm051237e
CHEMBL1204122 73150 1 None -2 6 Human 8.8 pKi = 8.8 Binding
Binding affinity to D5 dopamine receptor by radioligand binding assayBinding affinity to D5 dopamine receptor by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm051237e
CHEMBL201170 73150 1 None -2 6 Human 8.8 pKi = 8.8 Binding
Binding affinity to D5 dopamine receptor by radioligand binding assayBinding affinity to D5 dopamine receptor by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm051237e
11558055 73150 1 None -2 6 Human 8.8 pKi = 8.8 Binding
Binding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1039/C5MD00258C
CHEMBL1204122 73150 1 None -2 6 Human 8.8 pKi = 8.8 Binding
Binding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1039/C5MD00258C
CHEMBL201170 73150 1 None -2 6 Human 8.8 pKi = 8.8 Binding
Binding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1039/C5MD00258C
11558055 73150 1 None -2 6 Human 8.8 pKi = 8.8 Binding
Binding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cellsBinding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cells
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmcl.2006.11.093
CHEMBL1204122 73150 1 None -2 6 Human 8.8 pKi = 8.8 Binding
Binding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cellsBinding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cells
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmcl.2006.11.093
CHEMBL201170 73150 1 None -2 6 Human 8.8 pKi = 8.8 Binding
Binding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cellsBinding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cells
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmcl.2006.11.093
11558055 73150 1 None -2 6 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cells
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm070388+
CHEMBL1204122 73150 1 None -2 6 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cells
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm070388+
CHEMBL201170 73150 1 None -2 6 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cells
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm070388+
11558055 73150 1 None -2 6 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D5 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 73150 1 None -2 6 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D5 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 73150 1 None -2 6 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D5 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 73150 1 None -2 6 Human 8.8 pKi = 8.8 Binding
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm050846j
CHEMBL1204122 73150 1 None -2 6 Human 8.8 pKi = 8.8 Binding
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm050846j
CHEMBL201170 73150 1 None -2 6 Human 8.8 pKi = 8.8 Binding
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm050846j
11623343 140840 1 None 2 4 Human 8.8 pKi = 8.8 Binding
Binding affinity to D5 dopamine receptor by radioligand binding assayBinding affinity to D5 dopamine receptor by radioligand binding assay
ChEMBL 283 0 2 3 2.7 CN1CCc2cc(O)ccc2Cc2ccc(O)cc2CC1 10.1021/jm051237e
CHEMBL381936 140840 1 None 2 4 Human 8.8 pKi = 8.8 Binding
Binding affinity to D5 dopamine receptor by radioligand binding assayBinding affinity to D5 dopamine receptor by radioligand binding assay
ChEMBL 283 0 2 3 2.7 CN1CCc2cc(O)ccc2Cc2ccc(O)cc2CC1 10.1021/jm051237e
1243 3616 34 None -3 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 10.1016/j.bmcl.2021.128047
944 3616 34 None -3 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 10.1016/j.bmcl.2021.128047
CHEMBL324017 3616 34 None -3 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin)
ChEMBL 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 10.1016/j.bmcl.2021.128047
10402378 66123 0 None 19 5 Human 8.7 pKi = 8.7 Binding
Binding affinity for human recombinant dopamine receptor D5Binding affinity for human recombinant dopamine receptor D5
ChEMBL 297 1 0 3 3.2 COc1ccc2c(c1)OCCN(C)CCc1ccccc1C2 10.1021/jm049720x
CHEMBL184049 66123 0 None 19 5 Human 8.7 pKi = 8.7 Binding
Binding affinity for human recombinant dopamine receptor D5Binding affinity for human recombinant dopamine receptor D5
ChEMBL 297 1 0 3 3.2 COc1ccc2c(c1)OCCN(C)CCc1ccccc1C2 10.1021/jm049720x
122205438 137398 0 None -1 5 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 307 0 0 2 4.5 CN1CCc2ccccc2Cc2sc3ccccc3c2CC1 10.1039/C5MD00258C
CHEMBL3753266 137398 0 None -1 5 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 307 0 0 2 4.5 CN1CCc2ccccc2Cc2sc3ccccc3c2CC1 10.1039/C5MD00258C
46216855 200376 0 None -2 4 Human 8.7 pKi = 8.7 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 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 200376 0 None -2 4 Human 8.7 pKi = 8.7 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 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
46231925 201376 0 None -5 4 Human 8.0 pKi = 8 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 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 201376 0 None -5 4 Human 8.0 pKi = 8 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 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
45379370 7521 0 None 2 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]radioligand from human recombinant dopamine D5 receptor expressed in HEK293 cells by microplate scintillation countingDisplacement of [3H]radioligand from human recombinant dopamine D5 receptor expressed in HEK293 cells by microplate scintillation counting
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2c([nH]c3ccccc23)CC1 10.1021/jm901291r
CHEMBL1087301 7521 0 None 2 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]radioligand from human recombinant dopamine D5 receptor expressed in HEK293 cells by microplate scintillation countingDisplacement of [3H]radioligand from human recombinant dopamine D5 receptor expressed in HEK293 cells by microplate scintillation counting
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2c([nH]c3ccccc23)CC1 10.1021/jm901291r
11269330 201491 0 None -34 4 Human 8.0 pKi = 8.0 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 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 201491 0 None -34 4 Human 8.0 pKi = 8.0 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 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
135398745 2912 112 None -26 66 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D5 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 2912 112 None -26 66 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D5 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 2912 112 None -26 66 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D5 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 2912 112 None -26 66 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D5 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
10947658 28700 0 None -912 16 Human 6.0 pKi = 6 Binding
Binding affinity against Dopamine receptor D5Binding affinity against Dopamine receptor D5
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 28700 0 None -912 16 Human 6.0 pKi = 6 Binding
Binding affinity against Dopamine receptor D5Binding affinity against Dopamine receptor D5
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
135398737 957 93 None -89 91 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D5 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
38 957 93 None -89 91 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D5 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
722 957 93 None -89 91 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D5 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
CHEMBL42 957 93 None -89 91 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D5 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
DB00363 957 93 None -89 91 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D5 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
2389 3329 118 None -239 67 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D5 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 3329 118 None -239 67 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D5 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 3329 118 None -239 67 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D5 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 3329 118 None -239 67 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D5 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 3329 118 None -239 67 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D5 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
155552185 174059 0 None -1819 16 Human 6.0 pKi = 6 Binding
Displacement of [3H] SCH23390 from D5 receptor (unknown origin)Displacement of [3H] SCH23390 from D5 receptor (unknown origin)
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4544086 174059 0 None -1819 16 Human 6.0 pKi = 6 Binding
Displacement of [3H] SCH23390 from D5 receptor (unknown origin)Displacement of [3H] SCH23390 from D5 receptor (unknown origin)
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
154724609 176597 1 None -11 5 Human 6.0 pKi = 6 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT 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 176597 1 None -11 5 Human 6.0 pKi = 6 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT 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 176597 1 None -11 5 Human 6.0 pKi = 6 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT 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
145969667 164963 0 None -41 6 Human 7.0 pKi = 7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T 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 164963 0 None -41 6 Human 7.0 pKi = 7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T 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
681 1464 72 None -67 39 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 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 1464 72 None -67 39 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 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 1464 72 None -67 39 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 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 1464 72 None -67 39 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 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 1464 72 None -67 39 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 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
21527771 70154 1 None -40 10 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D5 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 70154 1 None -40 10 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D5 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
44415593 80245 0 None -104 6 Human 7.0 pKi = 7.0 Binding
Binding affinity at dopamine D5 receptorBinding affinity at dopamine D5 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 80245 0 None -104 6 Human 7.0 pKi = 7.0 Binding
Binding affinity at dopamine D5 receptorBinding affinity at dopamine D5 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
242 470 124 None -380 52 Human 6.0 pKi = 6.0 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
34 470 124 None -380 52 Human 6.0 pKi = 6.0 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 470 124 None -380 52 Human 6.0 pKi = 6.0 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 470 124 None -380 52 Human 6.0 pKi = 6.0 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 470 124 None -380 52 Human 6.0 pKi = 6.0 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
154704368 176469 1 None -229 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT 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 176469 1 None -229 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT 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 176469 1 None -229 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT 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
126720252 164673 0 None -38 12 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting method
ChEMBL 697 15 2 6 9.2 NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1 10.1021/acs.jmedchem.8b00168
CHEMBL4216870 164673 0 None -38 12 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting method
ChEMBL 697 15 2 6 9.2 NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1 10.1021/acs.jmedchem.8b00168
11566745 74692 0 None 1 4 Human 6.0 pKi = 6.0 Binding
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D5 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 74692 0 None 1 4 Human 6.0 pKi = 6.0 Binding
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D5 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 74692 0 None 1 4 Human 6.0 pKi = 6.0 Binding
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D5 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
154704418 176585 1 None -2 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT 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 176585 1 None -2 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT 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 176585 1 None -2 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT 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
11408135 124186 0 None -245 3 Rat 5.0 pKi = 5.0 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brainInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brain
ChEMBL 443 7 1 4 4.5 COc1ccc2c(c1)N1CCN(CCCCNC(=O)c3ccc4ccccc4c3)C[C@H]1CC2 10.1021/jm049031l
CHEMBL363406 124186 0 None -245 3 Rat 5.0 pKi = 5.0 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brainInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brain
ChEMBL 443 7 1 4 4.5 COc1ccc2c(c1)N1CCN(CCCCNC(=O)c3ccc4ccccc4c3)C[C@H]1CC2 10.1021/jm049031l
5249956 73393 1 None -2 6 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1039/C5MD00258C
CHEMBL201525 73393 1 None -2 6 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1039/C5MD00258C
5249956 73393 1 None -2 6 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cellsBinding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cells
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1016/j.bmcl.2006.11.093
CHEMBL201525 73393 1 None -2 6 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cellsBinding affinity to human cloned dopamine D5 receptor expressed in HEK 293 cells
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1016/j.bmcl.2006.11.093
5249956 73393 1 None -2 6 Human 8.0 pKi = 8.0 Binding
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1021/jm050846j
CHEMBL201525 73393 1 None -2 6 Human 8.0 pKi = 8.0 Binding
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1021/jm050846j
56594534 70598 0 None -1 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in human HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in human HEK293 cells
ChEMBL 320 1 2 2 3.2 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2C[C@@H]1CO 10.1021/jm200676f
CHEMBL1949728 70598 0 None -1 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in human HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in human HEK293 cells
ChEMBL 320 1 2 2 3.2 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2C[C@@H]1CO 10.1021/jm200676f
56597938 3938 3 None -1380 9 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T 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 3938 3 None -1380 9 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T 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 3938 3 None -1380 9 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T 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
164618319 184591 0 None 1 3 Human 6.0 pKi = 6.0 Binding
Inhibition of dopamine D5 receptor (unknown origin)Inhibition of dopamine D5 receptor (unknown origin)
ChEMBL 340 2 1 4 2.1 CC(=O)NCC#Cc1ccc2c(c1)C=C([N+](=O)[O-])C(C(F)(F)F)O2 10.1016/j.bmcl.2021.128008
CHEMBL4848838 184591 0 None 1 3 Human 6.0 pKi = 6.0 Binding
Inhibition of dopamine D5 receptor (unknown origin)Inhibition of dopamine D5 receptor (unknown origin)
ChEMBL 340 2 1 4 2.1 CC(=O)NCC#Cc1ccc2c(c1)C=C([N+](=O)[O-])C(C(F)(F)F)O2 10.1016/j.bmcl.2021.128008
122181333 121872 0 None -7762 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293 cell membranesDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293 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 121872 0 None -7762 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293 cell membranesDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293 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
154725276 176288 1 None -40 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT 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 176288 1 None -40 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT 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 176288 1 None -40 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT 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
11335419 67098 1 None -11 6 Human 7.0 pKi = 7.0 Binding
Binding affinity for human recombinant dopamine receptor D5Binding affinity for human recombinant dopamine receptor D5
ChEMBL 295 7 0 2 4.1 c1ccc(Cc2ccccc2OCCCN2CCCC2)cc1 10.1021/jm049720x
CHEMBL187367 67098 1 None -11 6 Human 7.0 pKi = 7.0 Binding
Binding affinity for human recombinant dopamine receptor D5Binding affinity for human recombinant dopamine receptor D5
ChEMBL 295 7 0 2 4.1 c1ccc(Cc2ccccc2OCCCN2CCCC2)cc1 10.1021/jm049720x
21533446 70153 0 None -30 10 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D5 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 70153 0 None -30 10 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D5 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
44436302 90632 0 None -23 4 Human 6.0 pKi = 6.0 Binding
Binding affinity to human D5RBinding affinity to human D5R
ChEMBL 429 7 0 6 2.4 COc1ccccc1N1CCN(CCCCN2C(=O)c3ccccc3S2(=O)=O)CC1 10.1016/j.bmcl.2021.128028
CHEMBL238917 90632 0 None -23 4 Human 6.0 pKi = 6.0 Binding
Binding affinity to human D5RBinding affinity to human D5R
ChEMBL 429 7 0 6 2.4 COc1ccccc1N1CCN(CCCCN2C(=O)c3ccccc3S2(=O)=O)CC1 10.1016/j.bmcl.2021.128028
44436302 90632 0 None -23 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293
ChEMBL 429 7 0 6 2.4 COc1ccccc1N1CCN(CCCCN2C(=O)c3ccccc3S2(=O)=O)CC1 10.1016/j.bmc.2007.06.002
CHEMBL238917 90632 0 None -23 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293
ChEMBL 429 7 0 6 2.4 COc1ccccc1N1CCN(CCCCN2C(=O)c3ccccc3S2(=O)=O)CC1 10.1016/j.bmc.2007.06.002
681 1464 72 None -67 39 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 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 1464 72 None -67 39 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 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 1464 72 None -67 39 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 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 1464 72 None -67 39 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 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 1464 72 None -67 39 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 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
11573806 75414 0 None -6 4 Human 7.9 pKi = 7.9 Binding
Binding affinity to D5 dopamine receptor by radioligand binding assayBinding affinity to D5 dopamine receptor by radioligand binding assay
ChEMBL 311 2 0 3 3.3 COc1ccc2c(c1)CCN(C)CCc1cc(OC)ccc1C2 10.1021/jm051237e
CHEMBL204065 75414 0 None -6 4 Human 7.9 pKi = 7.9 Binding
Binding affinity to D5 dopamine receptor by radioligand binding assayBinding affinity to D5 dopamine receptor by radioligand binding assay
ChEMBL 311 2 0 3 3.3 COc1ccc2c(c1)CCN(C)CCc1cc(OC)ccc1C2 10.1021/jm051237e
11151831 13118 0 None - 1 Human 4.9 pKi = 4.9 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 299 4 1 2 3.9 CCCN(C)[C@@H]1Cc2cc(O)c(F)cc2[C@H]1c1ccccc1 10.1021/jm040889k
CHEMBL1190453 13118 0 None - 1 Human 4.9 pKi = 4.9 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 299 4 1 2 3.9 CCCN(C)[C@@H]1Cc2cc(O)c(F)cc2[C@H]1c1ccccc1 10.1021/jm040889k
CHEMBL540868 13118 0 None - 1 Human 4.9 pKi = 4.9 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 299 4 1 2 3.9 CCCN(C)[C@@H]1Cc2cc(O)c(F)cc2[C@H]1c1ccccc1 10.1021/jm040889k
154706513 176584 1 None -18 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT 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 176584 1 None -18 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT 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 176584 1 None -18 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT 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
53324045 57069 0 None -3 16 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells 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 57069 0 None -3 16 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells 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
3038495 707 37 None -831 19 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT 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 707 37 None -831 19 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT 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 707 37 None -831 19 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT 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
1242 3611 27 None -6 18 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH233930 from dopamine D5 receptor after 1.5 hrs by scintillation countingDisplacement of [3H]SCH233930 from dopamine D5 receptor after 1.5 hrs by scintillation counting
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2011.08.033
935 3611 27 None -6 18 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH233930 from dopamine D5 receptor after 1.5 hrs by scintillation countingDisplacement of [3H]SCH233930 from dopamine D5 receptor after 1.5 hrs by scintillation counting
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2011.08.033
CHEMBL286080 3611 27 None -6 18 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH233930 from dopamine D5 receptor after 1.5 hrs by scintillation countingDisplacement of [3H]SCH233930 from dopamine D5 receptor after 1.5 hrs by scintillation counting
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2011.08.033
33630 178955 99 None -5 28 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells 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 178955 99 None -5 28 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cells 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
164609730 185097 0 None -1 3 Human 5.9 pKi = 5.9 Binding
Inhibition of dopamine D5 receptor (unknown origin)Inhibition of dopamine D5 receptor (unknown origin)
ChEMBL 398 2 1 5 3.5 CC(C)(C)OC(=O)NCC#Cc1ccc2c(c1)C=C([N+](=O)[O-])C(C(F)(F)F)O2 10.1016/j.bmcl.2021.128008
CHEMBL4856060 185097 0 None -1 3 Human 5.9 pKi = 5.9 Binding
Inhibition of dopamine D5 receptor (unknown origin)Inhibition of dopamine D5 receptor (unknown origin)
ChEMBL 398 2 1 5 3.5 CC(C)(C)OC(=O)NCC#Cc1ccc2c(c1)C=C([N+](=O)[O-])C(C(F)(F)F)O2 10.1016/j.bmcl.2021.128008
11154178 200224 0 None -64 3 Human 7.9 pKi = 7.9 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 412 4 1 3 4.6 CC(=O)N(Cc1ccc([C@H]2CN(C)CCc3cc(Cl)c(O)cc32)cc1)C1CCC1 10.1016/j.bmcl.2009.12.100
CHEMBL596824 200224 0 None -64 3 Human 7.9 pKi = 7.9 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 receptor
ChEMBL 412 4 1 3 4.6 CC(=O)N(Cc1ccc([C@H]2CN(C)CCc3cc(Cl)c(O)cc32)cc1)C1CCC1 10.1016/j.bmcl.2009.12.100
122191607 123720 0 None -1778 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 468 9 1 3 5.0 CCCN(CCN1CCN(CCc2c[nH]c3ccccc23)CC1)c1ccc(Br)cc1 10.1021/acsmedchemlett.5b00131
CHEMBL3622099 123720 0 None -1778 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 468 9 1 3 5.0 CCCN(CCN1CCN(CCc2c[nH]c3ccccc23)CC1)c1ccc(Br)cc1 10.1021/acsmedchemlett.5b00131
137654675 158632 0 None -3388 6 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T 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 158632 0 None -3388 6 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T 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
11739113 13095 0 None - 1 Human 4.9 pKi = 4.9 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 297 4 1 2 3.7 C=CCN(C)[C@@H]1Cc2cc(F)c(O)cc2[C@H]1c1ccccc1 10.1021/jm040889k
CHEMBL1190331 13095 0 None - 1 Human 4.9 pKi = 4.9 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 297 4 1 2 3.7 C=CCN(C)[C@@H]1Cc2cc(F)c(O)cc2[C@H]1c1ccccc1 10.1021/jm040889k
CHEMBL540613 13095 0 None - 1 Human 4.9 pKi = 4.9 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 297 4 1 2 3.7 C=CCN(C)[C@@H]1Cc2cc(F)c(O)cc2[C@H]1c1ccccc1 10.1021/jm040889k
57391216 70166 0 None -66 8 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assay
ChEMBL 332 6 0 5 2.9 Fc1ccc(SCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940416 70166 0 None -66 8 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assay
ChEMBL 332 6 0 5 2.9 Fc1ccc(SCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
11716449 141213 0 None 2 4 Human 7.8 pKi = 7.8 Binding
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 304 1 1 1 4.2 CCN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm050846j
CHEMBL382850 141213 0 None 2 4 Human 7.8 pKi = 7.8 Binding
Inhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 304 1 1 1 4.2 CCN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm050846j
164609539 184397 0 None -2 3 Human 5.9 pKi = 5.9 Binding
Inhibition of dopamine D5 receptor (unknown origin)Inhibition of dopamine D5 receptor (unknown origin)
ChEMBL 428 2 0 5 3.3 O=C1c2ccccc2C(=O)N1CC#Cc1ccc2c(c1)C=C([N+](=O)[O-])C(C(F)(F)F)O2 10.1016/j.bmcl.2021.128008
CHEMBL4845850 184397 0 None -2 3 Human 5.9 pKi = 5.9 Binding
Inhibition of dopamine D5 receptor (unknown origin)Inhibition of dopamine D5 receptor (unknown origin)
ChEMBL 428 2 0 5 3.3 O=C1c2ccccc2C(=O)N1CC#Cc1ccc2c(c1)C=C([N+](=O)[O-])C(C(F)(F)F)O2 10.1016/j.bmcl.2021.128008
145988180 165229 0 None -12 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T 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 165229 0 None -12 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T 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
164585473 184560 0 None -2 5 Human 5.8 pKi = 5.8 Binding
Binding affinity to D5 receptor (unknown origin)Binding affinity to D5 receptor (unknown origin)
ChEMBL 503 5 1 2 7.2 O=CN1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.1c00164
CHEMBL4848380 184560 0 None -2 5 Human 5.8 pKi = 5.8 Binding
Binding affinity to D5 receptor (unknown origin)Binding affinity to D5 receptor (unknown origin)
ChEMBL 503 5 1 2 7.2 O=CN1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.1c00164
44209480 70168 0 None -1318 11 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assay
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940418 70168 0 None -1318 11 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assay
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
11637457 73085 1 None -1 5 Human 7.8 pKi = 7.8 Binding
Binding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2ccsc2CC1 10.1039/C5MD00258C
CHEMBL201093 73085 1 None -1 5 Human 7.8 pKi = 7.8 Binding
Binding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D5 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2ccsc2CC1 10.1039/C5MD00258C
228 445 28 None -3 24 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from human D5 receptor expressed in CH4Cl cells incubated for 60 mins by radio ligand binding assayDisplacement of [3H]SCH23390 from human D5 receptor expressed in CH4Cl cells incubated for 60 mins by radio ligand binding assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmcl.2020.127053
33 445 28 None -3 24 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from human D5 receptor expressed in CH4Cl cells incubated for 60 mins by radio ligand binding assayDisplacement of [3H]SCH23390 from human D5 receptor expressed in CH4Cl cells incubated for 60 mins by radio ligand binding assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmcl.2020.127053
6005 445 28 None -3 24 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from human D5 receptor expressed in CH4Cl cells incubated for 60 mins by radio ligand binding assayDisplacement of [3H]SCH23390 from human D5 receptor expressed in CH4Cl cells incubated for 60 mins by radio ligand binding assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmcl.2020.127053
CHEMBL53 445 28 None -3 24 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from human D5 receptor expressed in CH4Cl cells incubated for 60 mins by radio ligand binding assayDisplacement of [3H]SCH23390 from human D5 receptor expressed in CH4Cl cells incubated for 60 mins by radio ligand binding assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmcl.2020.127053
DB00714 445 28 None -3 24 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from human D5 receptor expressed in CH4Cl cells incubated for 60 mins by radio ligand binding assayDisplacement of [3H]SCH23390 from human D5 receptor expressed in CH4Cl cells incubated for 60 mins by radio ligand binding assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmcl.2020.127053
3246443 37684 2 None -2 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor after 1 hrDisplacement of [3H]SCH23390 from human dopamine D5 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 37684 2 None -2 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor after 1 hrDisplacement of [3H]SCH23390 from human dopamine D5 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
137636066 156231 0 None -9549 6 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T 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 156231 0 None -9549 6 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T 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
11439436 12792 0 None - 1 Human 4.8 pKi = 4.8 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 311 5 0 2 4.0 C=CCN(C)[C@@H]1Cc2cc(OC)c(F)cc2[C@H]1c1ccccc1 10.1021/jm040889k
CHEMBL1188091 12792 0 None - 1 Human 4.8 pKi = 4.8 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 311 5 0 2 4.0 C=CCN(C)[C@@H]1Cc2cc(OC)c(F)cc2[C@H]1c1ccccc1 10.1021/jm040889k
CHEMBL535151 12792 0 None - 1 Human 4.8 pKi = 4.8 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 311 5 0 2 4.0 C=CCN(C)[C@@H]1Cc2cc(OC)c(F)cc2[C@H]1c1ccccc1 10.1021/jm040889k
46227284 199713 0 None 1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation counting
ChEMBL 281 1 0 2 3.5 COc1ccc2c(c1)CCN(C)Cc1ccccc1CC2 10.1016/j.bmc.2009.08.028
CHEMBL593394 199713 0 None 1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation counting
ChEMBL 281 1 0 2 3.5 COc1ccc2c(c1)CCN(C)Cc1ccccc1CC2 10.1016/j.bmc.2009.08.028
90644071 112040 0 None -8 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assay
ChEMBL 368 5 0 3 5.2 Clc1ccc(N2CCCN(CCCc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289655 112040 0 None -8 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assay
ChEMBL 368 5 0 3 5.2 Clc1ccc(N2CCCN(CCCc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
45379377 7455 0 None 1 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]radioligand from human recombinant dopamine D5 receptor expressed in HEK293 cells by microplate scintillation countingDisplacement of [3H]radioligand from human recombinant dopamine D5 receptor expressed in HEK293 cells by microplate scintillation counting
ChEMBL 274 0 1 1 3.7 c1ccc2c(c1)CCN1CCc3cccc4[nH]cc(c34)C21 10.1021/jm901291r
CHEMBL1086790 7455 0 None 1 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]radioligand from human recombinant dopamine D5 receptor expressed in HEK293 cells by microplate scintillation countingDisplacement of [3H]radioligand from human recombinant dopamine D5 receptor expressed in HEK293 cells by microplate scintillation counting
ChEMBL 274 0 1 1 3.7 c1ccc2c(c1)CCN1CCc3cccc4[nH]cc(c34)C21 10.1021/jm901291r
44591134 176198 0 None -125 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 535 11 0 5 7.7 CN(CCCN1c2ccccc2Sc2ccc(Cl)cc21)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
CHEMBL459373 176198 0 None -125 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 535 11 0 5 7.7 CN(CCCN1c2ccccc2Sc2ccc(Cl)cc21)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
72164182 92148 0 None -25 5 Human 5.8 pKi = 5.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand binding assayBinding affinity to human dopamine D5 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 92148 0 None -25 5 Human 5.8 pKi = 5.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand binding assayBinding affinity to human dopamine D5 receptor by radioligand binding assay
ChEMBL 326 3 0 3 4.4 Clc1ccc(N2CCN(Cc3cccs3)CC2)cc1Cl 10.1016/j.bmcl.2013.07.033
154703647 176363 1 None -28 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT 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 176363 1 None -28 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT 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 176363 1 None -28 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT 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
6603820 95772 19 None -1 13 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from rat dopamine D5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from rat dopamine D5 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 95772 19 None -1 13 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from rat dopamine D5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from rat dopamine D5 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
10200496 83591 0 None -30 5 Human 7.8 pKi = 7.8 Binding
Inhibition of human dopamine D5 receptorInhibition of human dopamine D5 receptor
ChEMBL 391 6 1 3 3.6 O=C(CCCN1CC[Si](O)(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1021/jm1013693
CHEMBL2204343 83591 0 None -30 5 Human 7.8 pKi = 7.8 Binding
Inhibition of human dopamine D5 receptorInhibition of human dopamine D5 receptor
ChEMBL 391 6 1 3 3.6 O=C(CCCN1CC[Si](O)(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1021/jm1013693
242 470 124 None -380 52 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T 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
34 470 124 None -380 52 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T 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 470 124 None -380 52 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T 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 470 124 None -380 52 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T 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 470 124 None -380 52 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T 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
242 470 124 None -380 52 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T 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
34 470 124 None -380 52 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T 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 470 124 None -380 52 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T 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 470 124 None -380 52 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T 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 470 124 None -380 52 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T 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
163198500 186396 3 None 3 2 Human 5.8 pKi = 5.8 Binding
Inhibition of dopamine D5 receptor (unknown origin)Inhibition of dopamine D5 receptor (unknown origin)
ChEMBL 371 1 0 3 3.2 O=[N+]([O-])C1=Cc2cc(I)ccc2OC1C(F)(F)F 10.1016/j.bmcl.2021.128008
CHEMBL4875858 186396 3 None 3 2 Human 5.8 pKi = 5.8 Binding
Inhibition of dopamine D5 receptor (unknown origin)Inhibition of dopamine D5 receptor (unknown origin)
ChEMBL 371 1 0 3 3.2 O=[N+]([O-])C1=Cc2cc(I)ccc2OC1C(F)(F)F 10.1016/j.bmcl.2021.128008
137655795 158580 0 None -6309 6 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T 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 158580 0 None -6309 6 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T 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
137660046 159341 0 None -22387 6 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T 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 159341 0 None -22387 6 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T 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
11324023 12809 0 None - 1 Human 4.8 pKi = 4.8 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 299 4 1 2 3.9 CCCN(C)[C@@H]1Cc2cc(F)c(O)cc2[C@H]1c1ccccc1 10.1021/jm040889k
CHEMBL1188254 12809 0 None - 1 Human 4.8 pKi = 4.8 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 299 4 1 2 3.9 CCCN(C)[C@@H]1Cc2cc(F)c(O)cc2[C@H]1c1ccccc1 10.1021/jm040889k
CHEMBL535823 12809 0 None - 1 Human 4.8 pKi = 4.8 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 299 4 1 2 3.9 CCCN(C)[C@@H]1Cc2cc(F)c(O)cc2[C@H]1c1ccccc1 10.1021/jm040889k
11416811 12823 0 None - 1 Human 4.8 pKi = 4.8 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 313 5 0 2 4.2 CCCN(C)[C@@H]1Cc2cc(OC)c(F)cc2[C@H]1c1ccccc1 10.1021/jm040889k
CHEMBL1188384 12823 0 None - 1 Human 4.8 pKi = 4.8 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 313 5 0 2 4.2 CCCN(C)[C@@H]1Cc2cc(OC)c(F)cc2[C@H]1c1ccccc1 10.1021/jm040889k
CHEMBL536271 12823 0 None - 1 Human 4.8 pKi = 4.8 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 313 5 0 2 4.2 CCCN(C)[C@@H]1Cc2cc(OC)c(F)cc2[C@H]1c1ccccc1 10.1021/jm040889k
11438636 13117 0 None - 1 Human 4.8 pKi = 4.8 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 285 3 0 2 3.5 COc1cc2c(cc1F)C[C@@H](N(C)C)[C@@H]2c1ccccc1 10.1021/jm040889k
CHEMBL1190452 13117 0 None - 1 Human 4.8 pKi = 4.8 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 285 3 0 2 3.5 COc1cc2c(cc1F)C[C@@H](N(C)C)[C@@H]2c1ccccc1 10.1021/jm040889k
CHEMBL540867 13117 0 None - 1 Human 4.8 pKi = 4.8 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 285 3 0 2 3.5 COc1cc2c(cc1F)C[C@@H](N(C)C)[C@@H]2c1ccccc1 10.1021/jm040889k
11818686 13895 0 None - 1 Human 4.8 pKi = 4.8 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 257 2 1 2 2.9 COc1cc2c(cc1F)[C@@H](c1ccccc1)[C@H](N)C2 10.1021/jm040889k
CHEMBL1196231 13895 0 None - 1 Human 4.8 pKi = 4.8 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 257 2 1 2 2.9 COc1cc2c(cc1F)[C@@H](c1ccccc1)[C@H](N)C2 10.1021/jm040889k
CHEMBL556194 13895 0 None - 1 Human 4.8 pKi = 4.8 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 257 2 1 2 2.9 COc1cc2c(cc1F)[C@@H](c1ccccc1)[C@H](N)C2 10.1021/jm040889k
85658088 165001 0 None -5 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T 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 165001 0 None -5 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293T 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
44436300 148834 0 None -64 4 Human 5.8 pKi = 5.8 Binding
Binding affinity to human D5RBinding affinity to human D5R
ChEMBL 399 6 0 5 2.4 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2ccccc2)CC1 10.1016/j.bmcl.2021.128028
CHEMBL394110 148834 0 None -64 4 Human 5.8 pKi = 5.8 Binding
Binding affinity to human D5RBinding affinity to human D5R
ChEMBL 399 6 0 5 2.4 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2ccccc2)CC1 10.1016/j.bmcl.2021.128028
44436300 148834 0 None -64 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293
ChEMBL 399 6 0 5 2.4 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2ccccc2)CC1 10.1016/j.bmc.2007.06.002
CHEMBL394110 148834 0 None -64 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293
ChEMBL 399 6 0 5 2.4 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2ccccc2)CC1 10.1016/j.bmc.2007.06.002
17755866 142882 1 None -1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cells
ChEMBL 281 0 1 2 3.4 CN1CCCc2cc(O)ccc2Cc2ccccc2CC1 10.1021/jm070388+
CHEMBL389356 142882 1 None -1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human dopamine D5 receptor expressed in HEK293 cells
ChEMBL 281 0 1 2 3.4 CN1CCCc2cc(O)ccc2Cc2ccccc2CC1 10.1021/jm070388+
180 401 56 None -112 40 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1016/j.bmcl.2008.09.012
200 401 56 None -112 40 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1016/j.bmcl.2008.09.012
2160 401 56 None -112 40 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1016/j.bmcl.2008.09.012
CHEMBL629 401 56 None -112 40 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1016/j.bmcl.2008.09.012
DB00321 401 56 None -112 40 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1016/j.bmcl.2008.09.012
44436305 154402 0 None -23 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293
ChEMBL 430 6 0 5 4.0 O=c1c2ccccc2ncn1CCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2007.06.002
CHEMBL398813 154402 0 None -23 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293
ChEMBL 430 6 0 5 4.0 O=c1c2ccccc2ncn1CCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2007.06.002
11464115 68632 0 None -89 3 Rat 5.8 pKi = 5.8 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brainInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brain
ChEMBL 413 6 1 3 4.5 O=C(NCCCCN1CCN2c3ccccc3CC[C@@H]2C1)c1ccc2ccccc2c1 10.1021/jm049031l
CHEMBL191815 68632 0 None -89 3 Rat 5.8 pKi = 5.8 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brainInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brain
ChEMBL 413 6 1 3 4.5 O=C(NCCCCN1CCN2c3ccccc3CC[C@@H]2C1)c1ccc2ccccc2c1 10.1021/jm049031l
2726 918 68 None -47 73 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2008.09.012
621 918 68 None -47 73 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2008.09.012
83 918 68 None -47 73 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2008.09.012
CHEMBL71 918 68 None -47 73 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2008.09.012
DB00477 918 68 None -47 73 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2008.09.012
154705520 176258 1 None -114 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT 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 176258 1 None -114 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT 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 176258 1 None -114 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT 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
76314268 106432 0 None -1230 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 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 106432 0 None -1230 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 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 106432 0 None -1230 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 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
72164180 92143 0 None -38 4 Human 5.8 pKi = 5.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand binding assayBinding affinity to human dopamine D5 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 92143 0 None -38 4 Human 5.8 pKi = 5.8 Binding
Binding affinity to human dopamine D5 receptor by radioligand binding assayBinding affinity to human dopamine D5 receptor by radioligand binding assay
ChEMBL 326 3 0 3 4.4 Clc1cccc(N2CCN(Cc3cccs3)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
11134444 90631 0 None -17 7 Human 5.8 pKi = 5.8 Binding
Binding affinity to human D5RBinding affinity to human D5R
ChEMBL 467 6 0 5 3.5 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2021.128028
CHEMBL238916 90631 0 None -17 7 Human 5.8 pKi = 5.8 Binding
Binding affinity to human D5RBinding affinity to human D5R
ChEMBL 467 6 0 5 3.5 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2021.128028
11134444 90631 0 None -17 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293
ChEMBL 467 6 0 5 3.5 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2007.06.002
CHEMBL238916 90631 0 None -17 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293
ChEMBL 467 6 0 5 3.5 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2007.06.002
57401819 70158 0 None -229 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 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 70158 0 None -229 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 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
76314268 106432 0 None -1230 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 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 106432 0 None -1230 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 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 106432 0 None -1230 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 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
46227325 200125 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 1 2 3.4 CN1CCCc2cc(O)ccc2Cc2ccccc2C1 10.1016/j.bmc.2009.08.028
CHEMBL596179 200125 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 1 2 3.4 CN1CCCc2cc(O)ccc2Cc2ccccc2C1 10.1016/j.bmc.2009.08.028
11358377 202337 0 None 2 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation counting
ChEMBL 295 0 0 3 3.5 CN1CCCc2cc3c(cc2-c2ccccc2CC1)OCO3 10.1016/j.bmc.2009.08.028
CHEMBL610449 202337 0 None 2 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation counting
ChEMBL 295 0 0 3 3.5 CN1CCCc2cc3c(cc2-c2ccccc2CC1)OCO3 10.1016/j.bmc.2009.08.028
154726793 176231 1 None -61 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT 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 176231 1 None -61 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT 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 176231 1 None -61 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT 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
46227317 200161 0 None -1 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D5 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 200161 0 None -1 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D5 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
44436306 97198 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293
ChEMBL 417 6 0 3 4.2 O=C1Cc2ccccc2N1CCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2007.06.002
CHEMBL268371 97198 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293Displacement of [3H]SCH 23390 from human Dopamine D5 receptor expressed in HEK293
ChEMBL 417 6 0 3 4.2 O=C1Cc2ccccc2N1CCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2007.06.002
137645830 157850 0 None -478 6 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 424 7 1 8 2.8 Oc1ccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c2c1OCCO2 10.1021/acs.jmedchem.7b00363
CHEMBL4083727 157850 0 None -478 6 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D5R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 424 7 1 8 2.8 Oc1ccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c2c1OCCO2 10.1021/acs.jmedchem.7b00363
11449266 13949 0 None - 1 Human 4.7 pKi = 4.7 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 257 2 1 2 2.9 COc1cc2c(cc1F)C[C@@H](N)[C@@H]2c1ccccc1 10.1021/jm040889k
CHEMBL1196658 13949 0 None - 1 Human 4.7 pKi = 4.7 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 257 2 1 2 2.9 COc1cc2c(cc1F)C[C@@H](N)[C@@H]2c1ccccc1 10.1021/jm040889k
CHEMBL557781 13949 0 None - 1 Human 4.7 pKi = 4.7 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 257 2 1 2 2.9 COc1cc2c(cc1F)C[C@@H](N)[C@@H]2c1ccccc1 10.1021/jm040889k
11449669 13950 0 None - 1 Human 4.7 pKi = 4.7 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 271 3 1 2 3.1 CN[C@@H]1Cc2cc(F)c(OC)cc2[C@H]1c1ccccc1 10.1021/jm040889k
CHEMBL1196659 13950 0 None - 1 Human 4.7 pKi = 4.7 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 271 3 1 2 3.1 CN[C@@H]1Cc2cc(F)c(OC)cc2[C@H]1c1ccccc1 10.1021/jm040889k
CHEMBL557782 13950 0 None - 1 Human 4.7 pKi = 4.7 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 271 3 1 2 3.1 CN[C@@H]1Cc2cc(F)c(OC)cc2[C@H]1c1ccccc1 10.1021/jm040889k
11210215 14001 0 None - 1 Human 4.7 pKi = 4.7 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 311 5 0 2 4.0 C=CCN(C)[C@@H]1Cc2cc(F)c(OC)cc2[C@H]1c1ccccc1 10.1021/jm040889k
CHEMBL1197038 14001 0 None - 1 Human 4.7 pKi = 4.7 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 311 5 0 2 4.0 C=CCN(C)[C@@H]1Cc2cc(F)c(OC)cc2[C@H]1c1ccccc1 10.1021/jm040889k
CHEMBL559164 14001 0 None - 1 Human 4.7 pKi = 4.7 Binding
Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranesInhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes
ChEMBL 311 5 0 2 4.0 C=CCN(C)[C@@H]1Cc2cc(F)c(OC)cc2[C@H]1c1ccccc1 10.1021/jm040889k
76336022 106377 0 None -512 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 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 106377 0 None -512 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 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 106377 0 None -512 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 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
11775107 166214 0 None -588 3 Rat 5.7 pKi = 5.7 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brainInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brain
ChEMBL 443 7 1 4 4.5 COc1cccc2c1N1CCN(CCCCNC(=O)c3ccc4ccccc4c3)C[C@@H]1CC2 10.1021/jm049031l
CHEMBL426629 166214 0 None -588 3 Rat 5.7 pKi = 5.7 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brainInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1-like in rat brain
ChEMBL 443 7 1 4 4.5 COc1cccc2c1N1CCN(CCCCNC(=O)c3ccc4ccccc4c3)C[C@@H]1CC2 10.1021/jm049031l
76336022 106377 0 None -512 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 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 106377 0 None -512 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 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 106377 0 None -512 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D5 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
135398737 957 93 None -89 91 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2008.09.012
38 957 93 None -89 91 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2008.09.012
722 957 93 None -89 91 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2008.09.012
CHEMBL42 957 93 None -89 91 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2008.09.012
DB00363 957 93 None -89 91 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2008.09.012
75306277 109252 0 None -99 23 Human 6.7 pKi = 6.7 Binding
Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D5 receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
CHEMBL3217984 109252 0 None -99 23 Human 6.7 pKi = 6.7 Binding
Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D5 receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
90644062 112032 0 None -104 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 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 112032 0 None -104 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D5 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D5 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
154727843 176431 1 None -17 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT 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 176431 1 None -17 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT 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 176431 1 None -17 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D5 receptor transiently expressed in HEKT 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
107930 1528 26 None -1 6 Human 8.7 pKi = 8.7 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 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 1528 26 None -1 6 Human 8.7 pKi = 8.7 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 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 1528 26 None -1 6 Human 8.7 pKi = 8.7 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 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 1528 26 None -1 6 Human 8.7 pKi = 8.7 Binding
Binding affinity to dopamine D5 receptorBinding affinity to dopamine D5 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
107930 1528 26 None -1 6 Human 8.7 pKi = 8.7 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 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 1528 26 None -1 6 Human 8.7 pKi = 8.7 Binding
Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D5 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 1528 26