Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
CHEMBL5077128 212712 5 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT5A receptor transfected in HTLA cells assessed as increase in beta-arrestin 2 recruitment at 10 uM incubated for 18 to 20 hrs by bright-Glo reagent based Tango assayAgonist activity at human 5-HT5A receptor transfected in HTLA cells assessed as increase in beta-arrestin 2 recruitment at 10 uM incubated for 18 to 20 hrs by bright-Glo reagent based Tango assay
ChEMBL None None None CS(=O)(=O)C1(CNCc2cccc3cccnc23)CC1 10.1021/acs.jmedchem.1c02031
CHEMBL5082447 213031 2 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human 5-HT5A receptor transfected in HTLA cells assessed as increase in beta-arrestin 2 recruitment at 10 uM incubated for 18 to 20 hrs by bright-Glo reagent based Tango assayAgonist activity at human 5-HT5A receptor transfected in HTLA cells assessed as increase in beta-arrestin 2 recruitment at 10 uM incubated for 18 to 20 hrs by bright-Glo reagent based Tango assay
ChEMBL None None None CS(=O)(=O)C1(CNCc2ccc(Cl)c3cccnc23)CC1 10.1021/acs.jmedchem.1c02031
785909 40807 7 None 1 2 Human 4.3 pEC50 = 4.3 Functional
PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
ChEMBL 336 4 1 3 4.1 COc1ccc(CN2CCc3c([nH]c4ccccc34)C2)c(OC)c1C nan
CHEMBL1487650 40807 7 None 1 2 Human 4.3 pEC50 = 4.3 Functional
PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
ChEMBL 336 4 1 3 4.1 COc1ccc(CN2CCc3c([nH]c4ccccc34)C2)c(OC)c1C nan
1765347 55827 13 None -1 2 Human 4.1 pEC50 = 4.1 Functional
PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
ChEMBL 324 7 2 3 3.8 COc1ccc(CNCCc2c[nH]c3ccccc23)c(OC)c1C nan
CHEMBL1606743 55827 13 None -1 2 Human 4.1 pEC50 = 4.1 Functional
PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
ChEMBL 324 7 2 3 3.8 COc1ccc(CNCCc2c[nH]c3ccccc23)c(OC)c1C nan
CHEMBL1625496 55827 13 None -1 2 Human 4.1 pEC50 = 4.1 Functional
PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
ChEMBL 324 7 2 3 3.8 COc1ccc(CNCCc2c[nH]c3ccccc23)c(OC)c1C nan
253793 10456 44 None -1 2 Human 4.1 pEC50 = 4.1 Functional
PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
ChEMBL 594 2 2 8 6.6 COc1cc2c3cc1Oc1cc(ccc1O)C[C@@H]1c4c(cc(OC)c(O)c4Oc4ccc(cc4)C[C@H]3N(C)CC2)CCN1C nan
CHEMBL1169627 10456 44 None -1 2 Human 4.1 pEC50 = 4.1 Functional
PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
ChEMBL 594 2 2 8 6.6 COc1cc2c3cc1Oc1cc(ccc1O)C[C@@H]1c4c(cc(OC)c(O)c4Oc4ccc(cc4)C[C@H]3N(C)CC2)CCN1C nan
1795 1561 58 None -10 4 Human 4.1 pEC50 = 4.1 Functional
PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
ChEMBL 299 4 3 5 0.4 CCN(c1nc(N)c(nc1Cl)C(=O)N=C(N)N)C(C)C nan
4186 1561 58 None -10 4 Human 4.1 pEC50 = 4.1 Functional
PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
ChEMBL 299 4 3 5 0.4 CCN(c1nc(N)c(nc1Cl)C(=O)N=C(N)N)C(C)C nan
CHEMBL517986 1561 58 None -10 4 Human 4.1 pEC50 = 4.1 Functional
PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
ChEMBL 299 4 3 5 0.4 CCN(c1nc(N)c(nc1Cl)C(=O)N=C(N)N)C(C)C nan
16006492 97020 7 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human recombinant 5HT5A receptor expressed in HEK293-EBNA cells by [35S]GTP-gamma-S binding assayAntagonist activity at human recombinant 5HT5A receptor expressed in HEK293-EBNA cells by [35S]GTP-gamma-S binding assay
ChEMBL 195 0 2 3 2.0 CC1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.080
CHEMBL270177 97020 7 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human recombinant 5HT5A receptor expressed in HEK293-EBNA cells by [35S]GTP-gamma-S binding assayAntagonist activity at human recombinant 5HT5A receptor expressed in HEK293-EBNA cells by [35S]GTP-gamma-S binding assay
ChEMBL 195 0 2 3 2.0 CC1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.080
16006492 97020 7 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human 5HT5A receptor by [35S]GTP-gamma-S binding assayAntagonist activity at human 5HT5A receptor by [35S]GTP-gamma-S binding assay
ChEMBL 195 0 2 3 2.0 CC1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL270177 97020 7 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human 5HT5A receptor by [35S]GTP-gamma-S binding assayAntagonist activity at human 5HT5A receptor by [35S]GTP-gamma-S binding assay
ChEMBL 195 0 2 3 2.0 CC1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
135458393 155056 4 None - 0 Human 7.4 pKd = 7.4 Functional
Antagonist activity at human 5HT5A receptor by [35S]GTP-gamma-S binding assayAntagonist activity at human 5HT5A receptor by [35S]GTP-gamma-S binding assay
ChEMBL 259 2 2 3 2.8 CC1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL404511 155056 4 None - 0 Human 7.4 pKd = 7.4 Functional
Antagonist activity at human 5HT5A receptor by [35S]GTP-gamma-S binding assayAntagonist activity at human 5HT5A receptor by [35S]GTP-gamma-S binding assay
ChEMBL 259 2 2 3 2.8 CC1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
135458392 96976 5 None - 0 Human 8.1 pKd = 8.1 Functional
Antagonist activity at human recombinant 5HT5A receptor expressed in HEK293-EBNA cells by [35S]GTP-gamma-S binding assayAntagonist activity at human recombinant 5HT5A receptor expressed in HEK293-EBNA cells by [35S]GTP-gamma-S binding assay
ChEMBL 209 0 2 3 2.2 CNC1=Nc2cccc(Cl)c2C(C)N1 10.1016/j.bmcl.2007.10.080
CHEMBL269964 96976 5 None - 0 Human 8.1 pKd = 8.1 Functional
Antagonist activity at human recombinant 5HT5A receptor expressed in HEK293-EBNA cells by [35S]GTP-gamma-S binding assayAntagonist activity at human recombinant 5HT5A receptor expressed in HEK293-EBNA cells by [35S]GTP-gamma-S binding assay
ChEMBL 209 0 2 3 2.2 CNC1=Nc2cccc(Cl)c2C(C)N1 10.1016/j.bmcl.2007.10.080




Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Affinity)
# tested GPCRs
(Affinity)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
44469677 15004 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in CHO cells
ChEMBL 336 4 1 4 5.4 C/C(=N\OC(=O)Nc1ccccc1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2010.06.050
CHEMBL1210154 15004 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in CHO cells
ChEMBL 336 4 1 4 5.4 C/C(=N\OC(=O)Nc1ccccc1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2010.06.050
10383252 4519 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 350 5 2 3 1.7 CN(C)CCc1c[nH]c2ccc(CN3C(C)(C)CNS3(=O)=O)cc12 10.1021/jm00045a006
CHEMBL102645 4519 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 350 5 2 3 1.7 CN(C)CCc1c[nH]c2ccc(CN3C(C)(C)CNS3(=O)=O)cc12 10.1021/jm00045a006
72548703 161019 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT5a receptor after 120 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5a receptor after 120 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
CHEMBL4128926 161019 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT5a receptor after 120 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5a receptor after 120 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
10404770 4648 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 336 6 2 3 1.0 CN(C)CCc1c[nH]c2ccc(CCN3CCNS3(=O)=O)cc12 10.1021/jm00045a006
CHEMBL103549 4648 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 336 6 2 3 1.0 CN(C)CCc1c[nH]c2ccc(CCN3CCNS3(=O)=O)cc12 10.1021/jm00045a006
10021702 108904 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 364 7 1 3 1.7 CCN1CCN(CCc2ccc3[nH]cc(CCN(C)C)c3c2)S1(=O)=O 10.1021/jm00045a006
CHEMBL321963 108904 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 364 7 1 3 1.7 CCN1CCN(CCc2ccc3[nH]cc(CCN(C)C)c3c2)S1(=O)=O 10.1021/jm00045a006
10043491 109336 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 350 5 1 3 1.7 CN(C)CCc1c[nH]c2ccc(CN3CCCN(C)S3(=O)=O)cc12 10.1021/jm00045a006
CHEMBL323334 109336 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 350 5 1 3 1.7 CN(C)CCc1c[nH]c2ccc(CN3CCCN(C)S3(=O)=O)cc12 10.1021/jm00045a006
5 139 66 None -323 54 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human 5-HT5a receptor by radioligand displacement assayBinding affinity to human 5-HT5a receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
5202 139 66 None -323 54 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human 5-HT5a receptor by radioligand displacement assayBinding affinity to human 5-HT5a receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
CHEMBL39 139 66 None -323 54 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human 5-HT5a receptor by radioligand displacement assayBinding affinity to human 5-HT5a receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
DB08839 139 66 None -323 54 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human 5-HT5a receptor by radioligand displacement assayBinding affinity to human 5-HT5a receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
5 139 66 None -323 54 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in HEK293 cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.03.006
5202 139 66 None -323 54 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in HEK293 cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.03.006
CHEMBL39 139 66 None -323 54 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in HEK293 cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.03.006
DB08839 139 66 None -323 54 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in HEK293 cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.03.006
5 139 66 None -323 54 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293 cells measured after 120 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.11.014
5202 139 66 None -323 54 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293 cells measured after 120 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.11.014
CHEMBL39 139 66 None -323 54 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293 cells measured after 120 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.11.014
DB08839 139 66 None -323 54 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293 cells measured after 120 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.11.014
5 139 66 None -323 54 Human 6.8 pIC50 = 6.8 Binding
Displacement of radiolabeled serotonin from human 5HT5A receptorDisplacement of radiolabeled serotonin from human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
5202 139 66 None -323 54 Human 6.8 pIC50 = 6.8 Binding
Displacement of radiolabeled serotonin from human 5HT5A receptorDisplacement of radiolabeled serotonin from human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
CHEMBL39 139 66 None -323 54 Human 6.8 pIC50 = 6.8 Binding
Displacement of radiolabeled serotonin from human 5HT5A receptorDisplacement of radiolabeled serotonin from human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
DB08839 139 66 None -323 54 Human 6.8 pIC50 = 6.8 Binding
Displacement of radiolabeled serotonin from human 5HT5A receptorDisplacement of radiolabeled serotonin from human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
5 139 66 None -323 54 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human 5HT5A receptorInhibition of human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm701575k
5202 139 66 None -323 54 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human 5HT5A receptorInhibition of human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm701575k
CHEMBL39 139 66 None -323 54 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human 5HT5A receptorInhibition of human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm701575k
DB08839 139 66 None -323 54 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human 5HT5A receptorInhibition of human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm701575k
10315894 4619 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 350 6 1 3 1.3 CN(C)CCc1c[nH]c2ccc(CCN3CCN(C)S3(=O)=O)cc12 10.1021/jm00045a006
CHEMBL103371 4619 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 350 6 1 3 1.3 CN(C)CCc1c[nH]c2ccc(CCN3CCN(C)S3(=O)=O)cc12 10.1021/jm00045a006
10412397 4620 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 469 8 2 4 2.8 CC(=O)Nc1ccc(CN2CCN(Cc3ccc4[nH]cc(CCN(C)C)c4c3)S2(=O)=O)cc1 10.1021/jm00045a006
CHEMBL103388 4620 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 469 8 2 4 2.8 CC(=O)Nc1ccc(CN2CCN(Cc3ccc4[nH]cc(CCN(C)C)c4c3)S2(=O)=O)cc1 10.1021/jm00045a006
10404070 78039 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 325 4 1 4 1.4 CN1CCN(Cc2ccc3scc(CCN)c3c2)S1(=O)=O 10.1021/jm00045a006
CHEMBL2111620 78039 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 325 4 1 4 1.4 CN1CCN(Cc2ccc3scc(CCN)c3c2)S1(=O)=O 10.1021/jm00045a006
10337965 108104 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 350 5 2 3 1.7 CN(C)CCc1c[nH]c2ccc(CN3CC(C)(C)NS3(=O)=O)cc12 10.1021/jm00045a006
CHEMBL320412 108104 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 350 5 2 3 1.7 CN(C)CCc1c[nH]c2ccc(CN3CC(C)(C)NS3(=O)=O)cc12 10.1021/jm00045a006
5 139 66 None -323 54 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
5202 139 66 None -323 54 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
CHEMBL39 139 66 None -323 54 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
DB08839 139 66 None -323 54 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
5 139 66 None -323 54 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human 5-HT5A receptor by radioligand displacement assayBinding affinity to human 5-HT5A receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2013.03.016
5202 139 66 None -323 54 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human 5-HT5A receptor by radioligand displacement assayBinding affinity to human 5-HT5A receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2013.03.016
CHEMBL39 139 66 None -323 54 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human 5-HT5A receptor by radioligand displacement assayBinding affinity to human 5-HT5A receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2013.03.016
DB08839 139 66 None -323 54 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human 5-HT5A receptor by radioligand displacement assayBinding affinity to human 5-HT5A receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2013.03.016
10885636 110527 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against 5-hydroxytryptamine 5A receptorBinding affinity against 5-hydroxytryptamine 5A receptor
ChEMBL 503 9 0 4 5.7 N#Cc1ccc(CCOC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
CHEMBL326263 110527 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against 5-hydroxytryptamine 5A receptorBinding affinity against 5-hydroxytryptamine 5A receptor
ChEMBL 503 9 0 4 5.7 N#Cc1ccc(CCOC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
2543 3651 66 None -1412 31 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00045a006
5358 3651 66 None -1412 31 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00045a006
54 3651 66 None -1412 31 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00045a006
CHEMBL128 3651 66 None -1412 31 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00045a006
DB00669 3651 66 None -1412 31 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00045a006
9998879 107014 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 364 6 1 3 2.0 CC(C)N1CCN(Cc2ccc3[nH]cc(CCN(C)C)c3c2)S1(=O)=O 10.1021/jm00045a006
CHEMBL318571 107014 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 364 6 1 3 2.0 CC(C)N1CCN(Cc2ccc3[nH]cc(CCN(C)C)c3c2)S1(=O)=O 10.1021/jm00045a006
11730467 10925 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity against 5-hydroxytryptamine 5A receptorBinding affinity against 5-hydroxytryptamine 5A receptor
ChEMBL 476 10 0 2 6.0 O=C(CCCc1ccccc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
CHEMBL117537 10925 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity against 5-hydroxytryptamine 5A receptorBinding affinity against 5-hydroxytryptamine 5A receptor
ChEMBL 476 10 0 2 6.0 O=C(CCCc1ccccc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
11722814 4694 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 308 4 2 3 0.7 CN1CCN(Cc2ccc3[nH]cc(CCN)c3c2)S1(=O)=O 10.1021/jm00045a006
CHEMBL103854 4694 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 308 4 2 3 0.7 CN1CCN(Cc2ccc3[nH]cc(CCN)c3c2)S1(=O)=O 10.1021/jm00045a006
10245588 107341 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 322 4 1 3 1.3 CN(C)CCc1c[nH]c2ccc(N3CCN(C)S3(=O)=O)cc12 10.1021/jm00045a006
CHEMBL319223 107341 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 322 4 1 3 1.3 CN(C)CCc1c[nH]c2ccc(N3CCN(C)S3(=O)=O)cc12 10.1021/jm00045a006
5 139 66 None -323 54 Human 7.1 pIC50 = 7.1 Binding
Percent inhibition against 5-hydroxytryptamine 5A receptor at 1 uMPercent inhibition against 5-hydroxytryptamine 5A receptor at 1 uM
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm058018d
5202 139 66 None -323 54 Human 7.1 pIC50 = 7.1 Binding
Percent inhibition against 5-hydroxytryptamine 5A receptor at 1 uMPercent inhibition against 5-hydroxytryptamine 5A receptor at 1 uM
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm058018d
CHEMBL39 139 66 None -323 54 Human 7.1 pIC50 = 7.1 Binding
Percent inhibition against 5-hydroxytryptamine 5A receptor at 1 uMPercent inhibition against 5-hydroxytryptamine 5A receptor at 1 uM
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm058018d
DB08839 139 66 None -323 54 Human 7.1 pIC50 = 7.1 Binding
Percent inhibition against 5-hydroxytryptamine 5A receptor at 1 uMPercent inhibition against 5-hydroxytryptamine 5A receptor at 1 uM
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm058018d
10340828 4298 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 398 6 1 3 2.8 CN(C)CCc1c[nH]c2ccc(N3CCN(Cc4ccccc4)S3(=O)=O)cc12 10.1021/jm00045a006
CHEMBL101138 4298 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 398 6 1 3 2.8 CN(C)CCc1c[nH]c2ccc(N3CCN(Cc4ccccc4)S3(=O)=O)cc12 10.1021/jm00045a006
10471382 4504 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 322 5 2 3 0.9 CN(C)CCc1c[nH]c2ccc(CN3CCNS3(=O)=O)cc12 10.1021/jm00045a006
CHEMBL102548 4504 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 322 5 2 3 0.9 CN(C)CCc1c[nH]c2ccc(CN3CCNS3(=O)=O)cc12 10.1021/jm00045a006
10471383 4510 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 322 5 2 3 0.9 CNCCc1c[nH]c2ccc(CN3CCN(C)S3(=O)=O)cc12 10.1021/jm00045a006
CHEMBL102586 4510 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 322 5 2 3 0.9 CNCCc1c[nH]c2ccc(CN3CCN(C)S3(=O)=O)cc12 10.1021/jm00045a006
9819150 4600 1 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 336 5 1 3 1.3 CN(C)CCc1c[nH]c2ccc(CN3CCN(C)S3(=O)=O)cc12 10.1021/jm00045a006
CHEMBL103205 4600 1 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 336 5 1 3 1.3 CN(C)CCc1c[nH]c2ccc(CN3CCN(C)S3(=O)=O)cc12 10.1021/jm00045a006
60152964 126269 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 366 1 2 1 2.7 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3c(F)cc(F)cc3F)c2C1 nan
CHEMBL3654198 126269 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 366 1 2 1 2.7 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3c(F)cc(F)cc3F)c2C1 nan
60151043 126277 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 374 1 2 1 3.0 NC(N)=NC(=O)N1Cc2c(-c3c(F)cccc3F)ccc(F)c2C2(CC2)C1 nan
CHEMBL3654206 126277 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 374 1 2 1 3.0 NC(N)=NC(=O)N1Cc2c(-c3c(F)cccc3F)ccc(F)c2C2(CC2)C1 nan
3233 3456 40 None -10 12 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.1c01093
3247 3456 40 None -10 12 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.1c01093
6604889 3456 40 None -10 12 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.1c01093
CHEMBL282199 3456 40 None -10 12 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.1c01093
DB13988 3456 40 None -10 12 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.1c01093
60151044 126283 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 374 1 2 1 3.0 NC(N)=NC(=O)N1Cc2c(-c3ccc(F)cc3F)ccc(F)c2C2(CC2)C1 nan
CHEMBL3654212 126283 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 374 1 2 1 3.0 NC(N)=NC(=O)N1Cc2c(-c3ccc(F)cc3F)ccc(F)c2C2(CC2)C1 nan
60151042 126279 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 392 1 2 1 3.2 NC(N)=NC(=O)N1Cc2c(-c3c(F)cc(F)cc3F)ccc(F)c2C2(CC2)C1 nan
CHEMBL3654208 126279 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 392 1 2 1 3.2 NC(N)=NC(=O)N1Cc2c(-c3c(F)cc(F)cc3F)ccc(F)c2C2(CC2)C1 nan
91819725 126285 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 356 1 2 1 2.9 NC(N)=NC(=O)N1Cc2c(-c3ccccc3F)ccc(F)c2C2(CC2)C1 nan
CHEMBL3654214 126285 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 356 1 2 1 2.9 NC(N)=NC(=O)N1Cc2c(-c3ccccc3F)ccc(F)c2C2(CC2)C1 nan
4106 2466 16 None -14 33 Human 9.0 pKi = 9 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
5358812 2466 16 None -14 33 Human 9.0 pKi = 9 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
89 2466 16 None -14 33 Human 9.0 pKi = 9 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
CHEMBL93240 2466 16 None -14 33 Human 9.0 pKi = 9 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
4106 2466 16 None -14 33 Human 9.0 pKi = 9 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
5358812 2466 16 None -14 33 Human 9.0 pKi = 9 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
89 2466 16 None -14 33 Human 9.0 pKi = 9 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
CHEMBL93240 2466 16 None -14 33 Human 9.0 pKi = 9 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
60150902 126268 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 382 1 2 1 3.2 NC(N)=NC(=O)N1CCc2c(Cl)ccc(-c3c(F)cc(F)cc3F)c2C1 nan
CHEMBL3654197 126268 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 382 1 2 1 3.2 NC(N)=NC(=O)N1CCc2c(Cl)ccc(-c3c(F)cc(F)cc3F)c2C1 nan
60152965 126270 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 348 1 2 1 2.5 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3c(F)cccc3F)c2C1 nan
CHEMBL3654199 126270 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 348 1 2 1 2.5 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3c(F)cccc3F)c2C1 nan
50923586 124640 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 360 2 2 2 3.2 NC(N)=NC(=O)c1ccc2c(Cl)cnc(-c3c(F)cccc3F)c2c1 nan
CHEMBL3644535 124640 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 360 2 2 2 3.2 NC(N)=NC(=O)c1ccc2c(Cl)cnc(-c3c(F)cccc3F)c2c1 nan
60150904 126281 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 392 1 2 1 3.2 NC(N)=NC(=O)N1Cc2c(-c3cc(F)c(F)cc3F)ccc(F)c2C2(CC2)C1 nan
CHEMBL3654210 126281 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 392 1 2 1 3.2 NC(N)=NC(=O)N1Cc2c(-c3cc(F)c(F)cc3F)ccc(F)c2C2(CC2)C1 nan
67961424 124630 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 360 2 2 2 3.2 NC(N)=NC(=O)c1ccc2ncc(Cl)c(-c3ccc(F)cc3F)c2c1 nan
CHEMBL3644525 124630 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 360 2 2 2 3.2 NC(N)=NC(=O)c1ccc2ncc(Cl)c(-c3ccc(F)cc3F)c2c1 nan
50923580 124635 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 358 2 2 2 3.0 Cc1cnc(-c2c(F)cc(F)cc2F)c2cc(C(=O)N=C(N)N)ccc12 nan
CHEMBL3644530 124635 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 358 2 2 2 3.0 Cc1cnc(-c2c(F)cc(F)cc2F)c2cc(C(=O)N=C(N)N)ccc12 nan
44456033 155027 3 None 1 8 Rat 8.9 pKi = 8.9 Binding
Binding affinity to rat 5HT5A receptorBinding affinity to rat 5HT5A receptor
ChEMBL 195 0 2 3 2.0 C[C@@H]1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL404372 155027 3 None 1 8 Rat 8.9 pKi = 8.9 Binding
Binding affinity to rat 5HT5A receptorBinding affinity to rat 5HT5A receptor
ChEMBL 195 0 2 3 2.0 C[C@@H]1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
50923443 124633 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 344 2 2 2 2.7 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3c(F)cccc3F)c2c1 nan
CHEMBL3644528 124633 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 344 2 2 2 2.7 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3c(F)cccc3F)c2c1 nan
CHEMBL5093295 213646 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 32 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 32 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None Clc1ccc(CNC[C@H]2CCn3ccnc3C2)c2ncccc12 10.1021/acs.jmedchem.1c02031
91819723 126278 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 362 1 2 1 3.1 CC1CN(C(=O)N=C(N)N)Cc2c(-c3c(F)cccc3F)ccc(F)c21 nan
CHEMBL3654207 126278 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 362 1 2 1 3.1 CC1CN(C(=O)N=C(N)N)Cc2c(-c3c(F)cccc3F)ccc(F)c21 nan
50923442 124632 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 360 2 2 2 3.2 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3c(F)cccc3Cl)c2c1 nan
CHEMBL3644527 124632 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 360 2 2 2 3.2 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3c(F)cccc3Cl)c2c1 nan
44456033 155027 3 None -1 8 Human 8.8 pKi = 8.8 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 195 0 2 3 2.0 C[C@@H]1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL404372 155027 3 None -1 8 Human 8.8 pKi = 8.8 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 195 0 2 3 2.0 C[C@@H]1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
50923723 124645 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 322 2 2 2 2.8 Cc1cnc(-c2ccccc2F)c2cc(C(=O)N=C(N)N)ccc12 nan
CHEMBL3644540 124645 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 322 2 2 2 2.8 Cc1cnc(-c2ccccc2F)c2cc(C(=O)N=C(N)N)ccc12 nan
136152971 94913 0 None 1 6 Human 8.7 pKi = 8.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 293 2 2 3 3.5 C[C@@H]1NC(NCC(F)F)=Nc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL256694 94913 0 None 1 6 Human 8.7 pKi = 8.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 293 2 2 3 3.5 C[C@@H]1NC(NCC(F)F)=Nc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2007.10.078
60150901 126276 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 381 1 2 2 2.9 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3ncc(Cl)cc3Cl)c2C1 nan
CHEMBL3654205 126276 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 381 1 2 2 2.9 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3ncc(Cl)cc3Cl)c2C1 nan
50923720 124642 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 340 2 2 2 2.9 Cc1cnc(-c2c(F)cccc2F)c2cc(C(=O)N=C(N)N)ccc12 nan
CHEMBL3644537 124642 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 340 2 2 2 2.9 Cc1cnc(-c2c(F)cccc2F)c2cc(C(=O)N=C(N)N)ccc12 nan
16006607 95228 4 None -10 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 219 2 2 4 2.1 CC(C)Oc1cccc2c1N=C(N)NC2C 10.1016/j.bmcl.2007.10.080
CHEMBL258075 95228 4 None -10 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 219 2 2 4 2.1 CC(C)Oc1cccc2c1N=C(N)NC2C 10.1016/j.bmcl.2007.10.080
135458393 155056 4 None 2 5 Human 8.0 pKi = 8 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 259 2 2 3 2.8 CC1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL404511 155056 4 None 2 5 Human 8.0 pKi = 8 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 259 2 2 3 2.8 CC1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
135458392 96976 5 None 1 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 209 0 2 3 2.2 CNC1=Nc2cccc(Cl)c2C(C)N1 10.1016/j.bmcl.2007.10.080
CHEMBL269964 96976 5 None 1 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 209 0 2 3 2.2 CNC1=Nc2cccc(Cl)c2C(C)N1 10.1016/j.bmcl.2007.10.080
135458392 96976 5 None 1 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 209 0 2 3 2.2 CNC1=Nc2cccc(Cl)c2C(C)N1 10.1016/j.bmcl.2007.10.080
CHEMBL269964 96976 5 None 1 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 209 0 2 3 2.2 CNC1=Nc2cccc(Cl)c2C(C)N1 10.1016/j.bmcl.2007.10.080
4106 2466 16 None -14 33 Human 7.0 pKi = 7 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
5358812 2466 16 None -14 33 Human 7.0 pKi = 7 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
89 2466 16 None -14 33 Human 7.0 pKi = 7 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
CHEMBL93240 2466 16 None -14 33 Human 7.0 pKi = 7 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
44351139 18656 0 None -1 3 Human 7.0 pKi = 7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 334 6 0 3 4.5 CCn1c2c(c3ccccc31)CN(CCCOc1ccccc1)CC2 10.1021/jm030080s
CHEMBL128099 18656 0 None -1 3 Human 7.0 pKi = 7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 334 6 0 3 4.5 CCn1c2c(c3ccccc31)CN(CCCOc1ccccc1)CC2 10.1021/jm030080s
44351140 18851 0 None -3 3 Human 7.0 pKi = 7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 320 5 0 3 4.0 Cn1c2c(c3ccccc31)CN(CCCOc1ccccc1)CC2 10.1021/jm030080s
CHEMBL128848 18851 0 None -3 3 Human 7.0 pKi = 7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 320 5 0 3 4.0 Cn1c2c(c3ccccc31)CN(CCCOc1ccccc1)CC2 10.1021/jm030080s
1220 186 46 None -1548 44 Human 6.0 pKi = 6 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030030n
31 186 46 None -1548 44 Human 6.0 pKi = 6 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030030n
7 186 46 None -1548 44 Human 6.0 pKi = 6 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030030n
CHEMBL56 186 46 None -1548 44 Human 6.0 pKi = 6 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030030n
22857296 28937 0 None -123 4 Human 6.0 pKi = 6 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 389 4 2 3 4.1 CN1C[C@H](CNC(=O)OCc2ccccc2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1021/jm030030n
CHEMBL13816 28937 0 None -123 4 Human 6.0 pKi = 6 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 389 4 2 3 4.1 CN1C[C@H](CNC(=O)OCc2ccccc2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1021/jm030030n
CHEMBL5083607 213101 0 None -83 9 Human 6.0 pKi = 6 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None COc1ccccc1-c1cc(C2CCN(C)C2)ccc1Cl 10.1021/acs.jmedchem.1c00110
242 467 117 None -144 51 Human 6.0 pKi = 6 Binding
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
34 467 117 None -144 51 Human 6.0 pKi = 6 Binding
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
60795 467 117 None -144 51 Human 6.0 pKi = 6 Binding
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
CHEMBL1112 467 117 None -144 51 Human 6.0 pKi = 6 Binding
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
DB01238 467 117 None -144 51 Human 6.0 pKi = 6 Binding
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
2389 3279 114 None -331 67 Human 6.0 pKi = 6 Binding
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
5073 3279 114 None -331 67 Human 6.0 pKi = 6 Binding
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
96 3279 114 None -331 67 Human 6.0 pKi = 6 Binding
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
CHEMBL85 3279 114 None -331 67 Human 6.0 pKi = 6 Binding
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
DB00734 3279 114 None -331 67 Human 6.0 pKi = 6 Binding
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A 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
135398737 944 89 None -173 91 Human 6.0 pKi = 6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030030n
38 944 89 None -173 91 Human 6.0 pKi = 6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030030n
722 944 89 None -173 91 Human 6.0 pKi = 6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030030n
CHEMBL42 944 89 None -173 91 Human 6.0 pKi = 6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030030n
DB00363 944 89 None -173 91 Human 6.0 pKi = 6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030030n
44397431 11652 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 567 11 1 5 7.0 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCc3ccc4c(c3)OCO4)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
CHEMBL1181632 11652 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 567 11 1 5 7.0 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCc3ccc4c(c3)OCO4)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
CHEMBL186261 11652 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 567 11 1 5 7.0 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCc3ccc4c(c3)OCO4)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
33630 178379 94 None -13 27 Human 6.0 pKi = 6 Binding
Displacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO 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 178379 94 None -13 27 Human 6.0 pKi = 6 Binding
Displacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO 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
135514796 92626 0 None 2 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 226 1 4 2 1.2 N=C1NC(=O)/C(=C\c2c[nH]c3ccccc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2442270 92626 0 None 2 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 226 1 4 2 1.2 N=C1NC(=O)/C(=C\c2c[nH]c3ccccc23)N1 10.1016/j.bmc.2013.09.011
136152962 97471 1 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 175 0 2 3 1.6 CNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
CHEMBL272517 97471 1 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 175 0 2 3 1.6 CNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
49756 202609 9 None -138 8 Human 5.0 pKi = 5.0 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 232 4 1 2 2.6 COc1ccc2[nH]c(C)c(CCN(C)C)c2c1 10.1021/jm990550b
CHEMBL7143 202609 9 None -138 8 Human 5.0 pKi = 5.0 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 232 4 1 2 2.6 COc1ccc2[nH]c(C)c(CCN(C)C)c2c1 10.1021/jm990550b
CHEMBL4520788 212225 6 None -48 25 Human 6.0 pKi = 6.0 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a HTR5ASelectivity interaction (GPCR panel (PDSP screen)) EUB0000743a HTR5A
ChEMBL None None None CNCc1ccccc1-c1csc([C@H](C)Nc2nc(C)nc3cc(OC)c(OC)cc23)c1 nan
CHEMBL5078567 212793 1 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor incubated for 2 hr by radioligand binding assay
ChEMBL None None None CN(C)S(=O)(=O)C1(CNCc2ccc(Cl)c3cccnc23)CC1 10.1021/acs.jmedchem.1c02031
11088692 17890 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligandBinding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligand
ChEMBL 326 7 0 3 4.2 CN(CCCOc1ccc(F)cc1)Cc1cn(C)c2ccccc12 10.1021/jm030080s
CHEMBL126666 17890 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligandBinding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligand
ChEMBL 326 7 0 3 4.2 CN(CCCOc1ccc(F)cc1)Cc1cn(C)c2ccccc12 10.1021/jm030080s
5 139 66 None -323 54 Human 7.0 pKi = 7.0 Binding
Displacement of radiolabeled serotonin from human 5HT5A receptorDisplacement of radiolabeled serotonin from human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
5202 139 66 None -323 54 Human 7.0 pKi = 7.0 Binding
Displacement of radiolabeled serotonin from human 5HT5A receptorDisplacement of radiolabeled serotonin from human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
CHEMBL39 139 66 None -323 54 Human 7.0 pKi = 7.0 Binding
Displacement of radiolabeled serotonin from human 5HT5A receptorDisplacement of radiolabeled serotonin from human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
DB08839 139 66 None -323 54 Human 7.0 pKi = 7.0 Binding
Displacement of radiolabeled serotonin from human 5HT5A receptorDisplacement of radiolabeled serotonin from human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
44351116 17768 1 None 1 2 Mouse 6.0 pKi = 6.0 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 244 3 1 3 1.9 Cn1c2c(c3ccccc31)CN(CCCO)CC2 10.1021/jm030080s
CHEMBL126021 17768 1 None 1 2 Mouse 6.0 pKi = 6.0 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 244 3 1 3 1.9 Cn1c2c(c3ccccc31)CN(CCCO)CC2 10.1021/jm030080s
136118729 92630 0 None 4 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2442274 92630 0 None 4 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1 10.1016/j.bmc.2013.09.011
44351116 17768 1 None -1 2 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 244 3 1 3 1.9 Cn1c2c(c3ccccc31)CN(CCCO)CC2 10.1021/jm030080s
CHEMBL126021 17768 1 None -1 2 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 244 3 1 3 1.9 Cn1c2c(c3ccccc31)CN(CCCO)CC2 10.1021/jm030080s
135367857 164052 0 None -69 8 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5-HT5A receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT5A receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 228 1 1 3 2.3 Cc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4215875 164052 0 None -69 8 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5-HT5A receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT5A receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 228 1 1 3 2.3 Cc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
71918568 119049 5 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assay
ChEMBL 317 7 2 3 3.0 O=C(CCCNCc1ccc(Cl)c2cccnc12)NC1CC1 10.1021/acs.jmedchem.1c02031
CHEMBL3459329 119049 5 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assay
ChEMBL 317 7 2 3 3.0 O=C(CCCNCc1ccc(Cl)c2cccnc12)NC1CC1 10.1021/acs.jmedchem.1c02031
44351511 19185 0 None -1 2 Mouse 6.9 pKi = 6.9 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 350 5 0 3 4.3 Cn1c2c(c3ccccc31)CN(CCCC(=O)c1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL129230 19185 0 None -1 2 Mouse 6.9 pKi = 6.9 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 350 5 0 3 4.3 Cn1c2c(c3ccccc31)CN(CCCC(=O)c1ccc(F)cc1)CC2 10.1021/jm030080s
44455980 13869 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 175 0 2 3 1.5 CC1(C)NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.080
CHEMBL1196896 13869 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 175 0 2 3 1.5 CC1(C)NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.080
CHEMBL558579 13869 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 175 0 2 3 1.5 CC1(C)NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.080
72550642 113579 0 None -134 8 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT5A (unknown origin)Binding affinity to 5-HT5A (unknown origin)
ChEMBL 491 10 1 4 5.6 COc1ccccc1N1CCN(CCCCC(=O)NCc2ccccc2-c2ccccc2Cl)CC1 10.1016/j.bmc.2014.07.026
CHEMBL3326982 113579 0 None -134 8 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT5A (unknown origin)Binding affinity to 5-HT5A (unknown origin)
ChEMBL 491 10 1 4 5.6 COc1ccccc1N1CCN(CCCCC(=O)NCc2ccccc2-c2ccccc2Cl)CC1 10.1016/j.bmc.2014.07.026
71918568 119049 5 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assay
ChEMBL 317 7 2 3 3.0 O=C(CCCNCc1ccc(Cl)c2cccnc12)NC1CC1 10.1021/acs.jmedchem.1c02031
CHEMBL3459329 119049 5 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assay
ChEMBL 317 7 2 3 3.0 O=C(CCCNCc1ccc(Cl)c2cccnc12)NC1CC1 10.1021/acs.jmedchem.1c02031
CHEMBL5074821 212565 1 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None Cc1cnn(C[C@H](C)NCc2cccc(OCc3ccccn3)c2)c1 10.1021/acs.jmedchem.1c02031
CHEMBL5087322 213311 7 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None Cc1cnc(NCc2ccccc2-n2ccnc2)nc1N(C)C 10.1021/acs.jmedchem.1c02031
CHEMBL5092728 213610 1 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None CC(C)(C)c1ccc2c(c1)CN(C[C@@H](O)COC1CCOCC1)CC2 10.1021/acs.jmedchem.1c02031
CHEMBL5093652 213662 2 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None N#CC1(c2ccccc2)CCC(NCCc2nnc3ccccn23)CC1 10.1021/acs.jmedchem.1c02031
44397618 67280 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 512 14 1 4 5.9 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cn2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
CHEMBL190382 67280 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 512 14 1 4 5.9 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cn2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
CHEMBL5081379 212974 0 None -18 9 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CCCNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
44351102 16831 0 None 1 3 Mouse 6.9 pKi = 6.9 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 332 6 0 2 4.9 Cn1c2c(c3ccccc31)CN(CCCCCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL125417 16831 0 None 1 3 Mouse 6.9 pKi = 6.9 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 332 6 0 2 4.9 Cn1c2c(c3ccccc31)CN(CCCCCc1ccccc1)CC2 10.1021/jm030080s
9817810 17190 1 None -501 8 Rat 5.9 pKi = 5.9 Binding
Binding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligand
ChEMBL 300 4 1 4 2.4 NCCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL125745 17190 1 None -501 8 Rat 5.9 pKi = 5.9 Binding
Binding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligand
ChEMBL 300 4 1 4 2.4 NCCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
44455963 154647 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 215 1 2 3 2.5 CC1NC(NC2CCC2)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
CHEMBL402400 154647 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 215 1 2 3 2.5 CC1NC(NC2CCC2)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
44351183 18672 0 None -5 3 Mouse 5.9 pKi = 5.9 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 368 6 0 4 4.2 COc1cccc2c3c(n(C)c12)CCN(CCCOc1ccc(F)cc1)C3 10.1021/jm030080s
CHEMBL128184 18672 0 None -5 3 Mouse 5.9 pKi = 5.9 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 368 6 0 4 4.2 COc1cccc2c3c(n(C)c12)CCN(CCCOc1ccc(F)cc1)C3 10.1021/jm030080s
117209962 184286 1 None -46 7 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
ChEMBL 242 2 2 3 1.8 Cc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4852622 184286 1 None -46 7 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
ChEMBL 242 2 2 3 1.8 Cc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
136118716 92627 0 None 3 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2442271 92627 0 None 3 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1 10.1016/j.bmc.2013.09.011
135367820 164269 0 None -23 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT5A receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT5A receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 232 1 1 3 2.2 Fc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4218672 164269 0 None -23 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT5A receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT5A receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 232 1 1 3 2.2 Fc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
136152965 95052 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 271 3 2 3 3.9 CC1NC(NCCC2CCCCC2)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
CHEMBL257302 95052 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 271 3 2 3 3.9 CC1NC(NCCC2CCCCC2)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
11443218 67138 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 489 11 2 3 6.4 c1ccc(CCNCc2ccc(-c3ccc(CNC4CCN(Cc5ccccc5)CC4)cc3)cc2)cc1 10.1016/j.bmcl.2005.06.024
CHEMBL189262 67138 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 489 11 2 3 6.4 c1ccc(CCNCc2ccc(-c3ccc(CNC4CCN(Cc5ccccc5)CC4)cc3)cc2)cc1 10.1016/j.bmcl.2005.06.024
24865725 187501 0 None -2511 12 Human 5.9 pKi = 5.9 Binding
Displacement of radioligand from human cloned 5HT5A receptorDisplacement of radioligand from human cloned 5HT5A receptor
ChEMBL 453 8 1 5 4.2 Cc1ccc2c(OCCN3CCC(Cc4cccc(NS(C)(=O)=O)c4)CC3)cccc2n1 10.1021/jm8001444
CHEMBL497963 187501 0 None -2511 12 Human 5.9 pKi = 5.9 Binding
Displacement of radioligand from human cloned 5HT5A receptorDisplacement of radioligand from human cloned 5HT5A receptor
ChEMBL 453 8 1 5 4.2 Cc1ccc2c(OCCN3CCC(Cc4cccc(NS(C)(=O)=O)c4)CC3)cccc2n1 10.1021/jm8001444
5 139 66 None -323 54 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
5202 139 66 None -323 54 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
CHEMBL39 139 66 None -323 54 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
DB08839 139 66 None -323 54 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
136118613 92631 0 None -5 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3cccc(Br)c23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL2442275 92631 0 None -5 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3cccc(Br)c23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL5087322 213311 7 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None Cc1cnc(NCc2ccccc2-n2ccnc2)nc1N(C)C 10.1021/acs.jmedchem.1c02031
50923441 124629 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 358 2 2 2 3.0 Cc1cc(-c2c(F)cc(F)cc2F)c2cc(C(=O)N=C(N)N)ccc2n1 nan
CHEMBL3644524 124629 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 358 2 2 2 3.0 Cc1cc(-c2c(F)cc(F)cc2F)c2cc(C(=O)N=C(N)N)ccc2n1 nan
11121216 29925 0 None -6 14 Human 7.9 pKi = 7.9 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
ChEMBL 335 1 1 2 3.0 C[C@@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
CHEMBL138989 29925 0 None -6 14 Human 7.9 pKi = 7.9 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
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
10382508 206129 0 None -2 3 Human 7.9 pKi = 7.9 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 338 5 0 3 4.1 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030030n
CHEMBL96504 206129 0 None -2 3 Human 7.9 pKi = 7.9 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 338 5 0 3 4.1 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030030n
10382508 206129 0 None 2 3 Mouse 7.9 pKi = 7.9 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 338 5 0 3 4.1 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL96504 206129 0 None 2 3 Mouse 7.9 pKi = 7.9 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 338 5 0 3 4.1 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030080s
44351059 19231 0 None - 1 Mouse 6.9 pKi = 6.9 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 318 5 0 2 4.6 Cn1c2c(c3ccccc31)CN(CCCCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL129472 19231 0 None - 1 Mouse 6.9 pKi = 6.9 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 318 5 0 2 4.6 Cn1c2c(c3ccccc31)CN(CCCCc1ccccc1)CC2 10.1021/jm030080s
5 139 66 None -323 54 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
5202 139 66 None -323 54 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
CHEMBL39 139 66 None -323 54 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
DB08839 139 66 None -323 54 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
136118732 75893 0 None 1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)NC(=O)/C1=C\c1c[nH]c2c(Br)cccc12 10.1016/j.bmc.2013.09.011
CHEMBL2058409 75893 0 None 1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)NC(=O)/C1=C\c1c[nH]c2c(Br)cccc12 10.1016/j.bmc.2013.09.011
44351342 19233 0 None 1 2 Mouse 6.9 pKi = 6.9 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 332 5 0 3 4.2 Cn1c2c(c3ccccc31)CN(CCCC(=O)c1ccccc1)CC2 10.1021/jm030080s
CHEMBL129476 19233 0 None 1 2 Mouse 6.9 pKi = 6.9 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 332 5 0 3 4.2 Cn1c2c(c3ccccc31)CN(CCCC(=O)c1ccccc1)CC2 10.1021/jm030080s
44456251 12727 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 177 1 2 4 0.7 COc1ccc2c(c1)N=C(N)NC2 10.1016/j.bmcl.2007.10.080
CHEMBL1188516 12727 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 177 1 2 4 0.7 COc1ccc2c(c1)N=C(N)NC2 10.1016/j.bmcl.2007.10.080
CHEMBL536561 12727 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 177 1 2 4 0.7 COc1ccc2c(c1)N=C(N)NC2 10.1016/j.bmcl.2007.10.080
44351183 18672 0 None -6 3 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 368 6 0 4 4.2 COc1cccc2c3c(n(C)c12)CCN(CCCOc1ccc(F)cc1)C3 10.1021/jm030080s
CHEMBL128184 18672 0 None -6 3 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 368 6 0 4 4.2 COc1cccc2c3c(n(C)c12)CCN(CCCOc1ccc(F)cc1)C3 10.1021/jm030080s
1043 1552 13 None -169 28 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation countingDisplacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation counting
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmc.2011.08.033
149 1552 13 None -169 28 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation countingDisplacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation counting
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmc.2011.08.033
8223 1552 13 None -169 28 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation countingDisplacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation counting
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmc.2011.08.033
CHEMBL442 1552 13 None -169 28 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation countingDisplacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation counting
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmc.2011.08.033
DB00696 1552 13 None -169 28 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation countingDisplacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation counting
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmc.2011.08.033
136118619 75898 0 None -2 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 332 1 2 2 2.3 C/N=C1\NC(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058418 75898 0 None -2 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 332 1 2 2 2.3 C/N=C1\NC(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1C 10.1016/j.bmc.2013.09.011
44456487 12764 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 161 0 2 3 1.0 Cc1cccc2c1CNC(N)=N2 10.1016/j.bmcl.2007.10.080
CHEMBL1188759 12764 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 161 0 2 3 1.0 Cc1cccc2c1CNC(N)=N2 10.1016/j.bmcl.2007.10.080
CHEMBL537248 12764 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 161 0 2 3 1.0 Cc1cccc2c1CNC(N)=N2 10.1016/j.bmcl.2007.10.080
136118616 75895 0 None -14 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 332 1 2 2 2.3 C/N=C1\NC(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058415 75895 0 None -14 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 332 1 2 2 2.3 C/N=C1\NC(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1C 10.1016/j.bmc.2013.09.011
136152963 97006 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 259 2 2 3 2.8 C[C@H]1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL270131 97006 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 259 2 2 3 2.8 C[C@H]1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
9888494 97719 0 None -660 13 Human 5.8 pKi = 5.8 Binding
Binding affinity towards cloned human 5-HT5A receptor was determinedBinding affinity towards cloned human 5-HT5A receptor was determined
ChEMBL 422 4 1 5 3.6 O=C1c2ccccc2CCCN1CCN1CCC(n2c(O)nc3cc(F)ccc32)CC1 10.1016/s0960-894x(03)00077-5
CHEMBL273921 97719 0 None -660 13 Human 5.8 pKi = 5.8 Binding
Binding affinity towards cloned human 5-HT5A receptor was determinedBinding affinity towards cloned human 5-HT5A receptor was determined
ChEMBL 422 4 1 5 3.6 O=C1c2ccccc2CCCN1CCN1CCC(n2c(O)nc3cc(F)ccc32)CC1 10.1016/s0960-894x(03)00077-5
1043 1552 13 None -169 28 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2013.12.024
149 1552 13 None -169 28 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2013.12.024
8223 1552 13 None -169 28 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2013.12.024
CHEMBL442 1552 13 None -169 28 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2013.12.024
DB00696 1552 13 None -169 28 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2013.12.024
5 139 66 None -891 54 Mouse 6.8 pKi = 6.8 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptorBinding affinity towards mouse 5-hydroxytryptamine 5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
5202 139 66 None -891 54 Mouse 6.8 pKi = 6.8 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptorBinding affinity towards mouse 5-hydroxytryptamine 5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
CHEMBL39 139 66 None -891 54 Mouse 6.8 pKi = 6.8 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptorBinding affinity towards mouse 5-hydroxytryptamine 5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
DB08839 139 66 None -891 54 Mouse 6.8 pKi = 6.8 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptorBinding affinity towards mouse 5-hydroxytryptamine 5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
53381002 65134 0 None -17 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation countingDisplacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation counting
ChEMBL 240 2 2 4 2.2 COc1cccc2[nH]cc(-c3ccnc(N)n3)c12 10.1016/j.bmc.2011.08.033
CHEMBL1829959 65134 0 None -17 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation countingDisplacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation counting
ChEMBL 240 2 2 4 2.2 COc1cccc2[nH]cc(-c3ccnc(N)n3)c12 10.1016/j.bmc.2011.08.033
136152981 97118 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 203 2 2 3 2.3 CCCNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
CHEMBL270658 97118 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 203 2 2 3 2.3 CCCNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
136118615 92633 0 None -2 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3c(Br)cccc23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL2442277 92633 0 None -2 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3c(Br)cccc23)C1=O 10.1016/j.bmc.2013.09.011
44582676 189187 0 None -12 17 Human 5.8 pKi = 5.8 Binding
Inhibition of human cloned 5HT5A receptor by competitive binding experimentInhibition of human cloned 5HT5A receptor by competitive binding experiment
ChEMBL 403 9 0 4 4.3 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL516088 189187 0 None -12 17 Human 5.8 pKi = 5.8 Binding
Inhibition of human cloned 5HT5A receptor by competitive binding experimentInhibition of human cloned 5HT5A receptor by competitive binding experiment
ChEMBL 403 9 0 4 4.3 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
24865727 192511 0 None -1000 11 Human 5.8 pKi = 5.8 Binding
Displacement of radioligand from human cloned 5HT5A receptorDisplacement of radioligand from human cloned 5HT5A receptor
ChEMBL 479 7 0 5 4.4 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCCS5(=O)=O)c4)CC3)cccc2n1 10.1021/jm8001444
CHEMBL522708 192511 0 None -1000 11 Human 5.8 pKi = 5.8 Binding
Displacement of radioligand from human cloned 5HT5A receptorDisplacement of radioligand from human cloned 5HT5A receptor
ChEMBL 479 7 0 5 4.4 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCCS5(=O)=O)c4)CC3)cccc2n1 10.1021/jm8001444
10947658 28490 0 None -14 16 Human 7.8 pKi = 7.8 Binding
Binding affinities against 5-hydroxytryptamine 5A receptorBinding affinities against 5-hydroxytryptamine 5A receptor
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
CHEMBL137781 28490 0 None -14 16 Human 7.8 pKi = 7.8 Binding
Binding affinities against 5-hydroxytryptamine 5A receptorBinding affinities against 5-hydroxytryptamine 5A receptor
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
1043 1552 13 None -169 28 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2013.12.024
149 1552 13 None -169 28 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2013.12.024
8223 1552 13 None -169 28 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2013.12.024
CHEMBL442 1552 13 None -169 28 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2013.12.024
DB00696 1552 13 None -169 28 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2013.12.024
9867475 17829 0 None -524 9 Rat 5.8 pKi = 5.8 Binding
Binding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligand
ChEMBL 432 7 0 5 4.2 CN(C)CCc1cccc2c1cc(C(=O)c1ccccc1)n2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL126340 17829 0 None -524 9 Rat 5.8 pKi = 5.8 Binding
Binding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligand
ChEMBL 432 7 0 5 4.2 CN(C)CCc1cccc2c1cc(C(=O)c1ccccc1)n2S(=O)(=O)c1ccccc1 10.1021/jm010943m
108182 4068 18 None -51 16 Human 4.8 pKi = 4.8 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl 10.1021/jm030030n
245 4068 18 None -51 16 Human 4.8 pKi = 4.8 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl 10.1021/jm030030n
CHEMBL18041 4068 18 None -51 16 Human 4.8 pKi = 4.8 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl 10.1021/jm030030n
136152968 154785 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 245 2 2 4 2.1 CC1NC(NC[C@H]2CCCO2)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
CHEMBL403102 154785 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 245 2 2 4 2.1 CC1NC(NC[C@H]2CCCO2)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
44351184 18673 0 None -1 3 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 368 6 0 4 4.2 COc1ccc2c(c1)c1c(n2C)CCN(CCCOc2ccc(F)cc2)C1 10.1021/jm030080s
CHEMBL128185 18673 0 None -1 3 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 368 6 0 4 4.2 COc1ccc2c(c1)c1c(n2C)CCN(CCCOc2ccc(F)cc2)C1 10.1021/jm030080s
10028436 3476 3 None -87 12 Human 6.8 pKi = 6.8 Binding
Binding affinity towards 5-hydroxytryptamine 5A receptorBinding affinity towards 5-hydroxytryptamine 5A receptor
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1021/jm030030n
3237 3476 3 None -87 12 Human 6.8 pKi = 6.8 Binding
Binding affinity towards 5-hydroxytryptamine 5A receptorBinding affinity towards 5-hydroxytryptamine 5A receptor
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1021/jm030030n
CHEMBL95104 3476 3 None -87 12 Human 6.8 pKi = 6.8 Binding
Binding affinity towards 5-hydroxytryptamine 5A receptorBinding affinity towards 5-hydroxytryptamine 5A receptor
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1021/jm030030n
44351342 19233 0 None -1 2 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 332 5 0 3 4.2 Cn1c2c(c3ccccc31)CN(CCCC(=O)c1ccccc1)CC2 10.1021/jm030080s
CHEMBL129476 19233 0 None -1 2 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 332 5 0 3 4.2 Cn1c2c(c3ccccc31)CN(CCCC(=O)c1ccccc1)CC2 10.1021/jm030080s
6604756 98375 12 None -28 7 Human 6.8 pKi = 6.8 Binding
Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )
ChEMBL 275 6 0 2 4.2 CCCN(CCC)[C@@H]1CCc2c(OC)cccc2[C@@H]1C 10.1016/S0960-894X(01)80181-5
CHEMBL278751 98375 12 None -28 7 Human 6.8 pKi = 6.8 Binding
Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )
ChEMBL 275 6 0 2 4.2 CCCN(CCC)[C@@H]1CCc2c(OC)cccc2[C@@H]1C 10.1016/S0960-894X(01)80181-5
44582705 186413 0 None -10 13 Human 5.8 pKi = 5.8 Binding
Inhibition of human cloned 5HT5A receptor by competitive binding experimentInhibition of human cloned 5HT5A receptor by competitive binding experiment
ChEMBL 399 9 0 4 4.5 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL490632 186413 0 None -10 13 Human 5.8 pKi = 5.8 Binding
Inhibition of human cloned 5HT5A receptor by competitive binding experimentInhibition of human cloned 5HT5A receptor by competitive binding experiment
ChEMBL 399 9 0 4 4.5 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
13972207 119112 0 None 13 2 Rat 7.8 pKi = 7.8 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 247 7 0 2 3.7 CCCN(CCC)[C@H]1C[C@@H]1c1ccccc1OC 10.1016/0960-894X(96)00045-5
CHEMBL34652 119112 0 None 13 2 Rat 7.8 pKi = 7.8 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 247 7 0 2 3.7 CCCN(CCC)[C@H]1C[C@@H]1c1ccccc1OC 10.1016/0960-894X(96)00045-5
5 139 66 None -323 54 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT5A receptorDisplacement of [3H]LSD from human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm2006782
5202 139 66 None -323 54 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT5A receptorDisplacement of [3H]LSD from human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm2006782
CHEMBL39 139 66 None -323 54 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT5A receptorDisplacement of [3H]LSD from human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm2006782
DB08839 139 66 None -323 54 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT5A receptorDisplacement of [3H]LSD from human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm2006782
71459269 82547 0 None -7413 8 Human 5.8 pKi = 5.8 Binding
Binding affinity to human 5HT5A by Cerep protocol based assayBinding affinity to human 5HT5A by Cerep protocol based assay
ChEMBL 555 7 0 4 6.3 Fc1cccc2c1nc(OCC1CCN(CCCc3ccc(I)cc3)CC1)c1cccnc12 10.1021/jm300943r
CHEMBL2181166 82547 0 None -7413 8 Human 5.8 pKi = 5.8 Binding
Binding affinity to human 5HT5A by Cerep protocol based assayBinding affinity to human 5HT5A by Cerep protocol based assay
ChEMBL 555 7 0 4 6.3 Fc1cccc2c1nc(OCC1CCN(CCCc3ccc(I)cc3)CC1)c1cccnc12 10.1021/jm300943r
44351063 19266 0 None 1 2 Mouse 5.8 pKi = 5.8 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 328 3 0 2 4.2 Cn1c2c(c3ccccc31)CN(CC#CCCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL129774 19266 0 None 1 2 Mouse 5.8 pKi = 5.8 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 328 3 0 2 4.2 Cn1c2c(c3ccccc31)CN(CC#CCCc1ccccc1)CC2 10.1021/jm030080s
44351102 16831 0 None -1 3 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 332 6 0 2 4.9 Cn1c2c(c3ccccc31)CN(CCCCCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL125417 16831 0 None -1 3 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 332 6 0 2 4.9 Cn1c2c(c3ccccc31)CN(CCCCCc1ccccc1)CC2 10.1021/jm030080s
132060776 161852 0 None -5 16 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting method
ChEMBL 419 4 0 4 4.4 O=C(OCc1ccccc1)N1CCc2ccc(N3CCN(C4CCCC4)CC3)cc2C1 10.1016/j.ejmech.2018.02.024
CHEMBL4165863 161852 0 None -5 16 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting method
ChEMBL 419 4 0 4 4.4 O=C(OCc1ccccc1)N1CCc2ccc(N3CCN(C4CCCC4)CC3)cc2C1 10.1016/j.ejmech.2018.02.024
136152974 94782 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 247 5 2 4 2.4 CCOCCCNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
CHEMBL256049 94782 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 247 5 2 4 2.4 CCOCCCNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
168268877 189377 0 None -38 12 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constant
ChEMBL 328 2 3 3 3.8 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5170784 189377 0 None -38 12 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constant
ChEMBL 328 2 3 3 3.8 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
44351063 19266 0 None -1 2 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 328 3 0 2 4.2 Cn1c2c(c3ccccc31)CN(CC#CCCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL129774 19266 0 None -1 2 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 328 3 0 2 4.2 Cn1c2c(c3ccccc31)CN(CC#CCCc1ccccc1)CC2 10.1021/jm030080s
25107716 2319 35 None -309 7 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysis
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1039/C8MD00313K
8436 2319 35 None -309 7 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysis
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1039/C8MD00313K
CHEMBL522691 2319 35 None -309 7 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysis
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1039/C8MD00313K
136100333 94079 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 161 0 2 3 1.0 CNC1=Nc2ccccc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL25163 94079 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 161 0 2 3 1.0 CNC1=Nc2ccccc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL536557 94079 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 161 0 2 3 1.0 CNC1=Nc2ccccc2CN1 10.1016/j.bmcl.2007.10.080
44351193 116352 0 None 1 3 Mouse 6.8 pKi = 6.8 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 372 5 0 3 4.8 Cn1c2c(c3cc(Cl)ccc31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL338095 116352 0 None 1 3 Mouse 6.8 pKi = 6.8 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 372 5 0 3 4.8 Cn1c2c(c3cc(Cl)ccc31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL5074880 212568 0 None -186 9 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CCNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
10028436 3476 3 None -87 12 Human 6.7 pKi = 6.7 Binding
Compound was tested for its binding affinity in 5-hydroxytryptamine 5A receptor (using human cloned receptors in HEK 293 and [3H]5-CTas a radioligand )Compound was tested for its binding affinity in 5-hydroxytryptamine 5A receptor (using human cloned receptors in HEK 293 and [3H]5-CTas a radioligand )
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/s0960-894x(02)00690-x
3237 3476 3 None -87 12 Human 6.7 pKi = 6.7 Binding
Compound was tested for its binding affinity in 5-hydroxytryptamine 5A receptor (using human cloned receptors in HEK 293 and [3H]5-CTas a radioligand )Compound was tested for its binding affinity in 5-hydroxytryptamine 5A receptor (using human cloned receptors in HEK 293 and [3H]5-CTas a radioligand )
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/s0960-894x(02)00690-x
CHEMBL95104 3476 3 None -87 12 Human 6.7 pKi = 6.7 Binding
Compound was tested for its binding affinity in 5-hydroxytryptamine 5A receptor (using human cloned receptors in HEK 293 and [3H]5-CTas a radioligand )Compound was tested for its binding affinity in 5-hydroxytryptamine 5A receptor (using human cloned receptors in HEK 293 and [3H]5-CTas a radioligand )
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/s0960-894x(02)00690-x
136118728 92629 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3cc(Br)ccc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2442273 92629 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3cc(Br)ccc23)N1 10.1016/j.bmc.2013.09.011
44351100 170905 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 330 5 0 2 4.7 Cn1c2c(c3ccccc31)CN(C/C=C/CCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL446356 170905 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 330 5 0 2 4.7 Cn1c2c(c3ccccc31)CN(C/C=C/CCc1ccccc1)CC2 10.1021/jm030080s
44355204 21700 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 247 7 1 2 3.6 CCCN(CCC)C[C@H]1C[C@@H]1c1cccc(O)c1 10.1016/0960-894X(96)00045-5
CHEMBL132019 21700 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 247 7 1 2 3.6 CCCN(CCC)C[C@H]1C[C@@H]1c1cccc(O)c1 10.1016/0960-894X(96)00045-5
136152980 154740 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 217 3 2 3 2.7 CCCCNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
CHEMBL402874 154740 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 217 3 2 3 2.7 CCCCNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
11035049 168013 0 None 1 2 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 335 5 1 4 3.6 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(N)cc1)CC2 10.1021/jm030080s
CHEMBL435814 168013 0 None 1 2 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 335 5 1 4 3.6 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(N)cc1)CC2 10.1021/jm030080s
10924201 117662 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligandBinding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligand
ChEMBL 288 5 0 3 3.0 Cn1ccc2c1CCN(CCCOc1ccc(F)cc1)C2 10.1021/jm030080s
CHEMBL340861 117662 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligandBinding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligand
ChEMBL 288 5 0 3 3.0 Cn1ccc2c1CCN(CCCOc1ccc(F)cc1)C2 10.1021/jm030080s
136179599 12750 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 189 1 2 3 1.9 CCNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
CHEMBL1188681 12750 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 189 1 2 3 1.9 CCNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
CHEMBL537022 12750 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 189 1 2 3 1.9 CCNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
75306277 108767 0 None -99 23 Human 6.7 pKi = 6.7 Binding
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
CHEMBL3217984 108767 0 None -99 23 Human 6.7 pKi = 6.7 Binding
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
11168912 11265 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 555 11 1 5 6.7 O=C(c1ccc2c(c1)OCO2)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
CHEMBL1179769 11265 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 555 11 1 5 6.7 O=C(c1ccc2c(c1)OCO2)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
CHEMBL99071 11265 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 555 11 1 5 6.7 O=C(c1ccc2c(c1)OCO2)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
44397486 66776 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 489 11 2 3 6.4 c1ccc(CCNCc2ccc(-c3cccc(CNC4CCN(Cc5ccccc5)CC4)c3)cc2)cc1 10.1016/j.bmcl.2005.06.024
CHEMBL187415 66776 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 489 11 2 3 6.4 c1ccc(CCNCc2ccc(-c3cccc(CNC4CCN(Cc5ccccc5)CC4)c3)cc2)cc1 10.1016/j.bmcl.2005.06.024
44456170 13040 1 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 165 0 2 3 0.9 NC1=Nc2c(F)cccc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL1190707 13040 1 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 165 0 2 3 0.9 NC1=Nc2c(F)cccc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL541394 13040 1 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 165 0 2 3 0.9 NC1=Nc2c(F)cccc2CN1 10.1016/j.bmcl.2007.10.080
155536080 171548 0 None -13 10 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting method
ChEMBL 219 2 1 2 2.9 CC[C@H]1c2cc(OC)ccc2CC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
CHEMBL4472703 171548 0 None -13 10 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting method
ChEMBL 219 2 1 2 2.9 CC[C@H]1c2cc(OC)ccc2CC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
10171 57 15 None 5 6 Mouse 8.7 pKi = 8.7 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 401 3 1 2 3.7 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)CC 10.1021/jm030030n
272 57 15 None 5 6 Mouse 8.7 pKi = 8.7 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 401 3 1 2 3.7 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)CC 10.1021/jm030030n
CHEMBL274384 57 15 None 5 6 Mouse 8.7 pKi = 8.7 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 401 3 1 2 3.7 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)CC 10.1021/jm030030n
16093484 97610 6 None 3 6 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 229 0 2 3 2.6 CC1NC(N)=Nc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2007.10.080
CHEMBL273170 97610 6 None 3 6 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 229 0 2 3 2.6 CC1NC(N)=Nc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2007.10.080
50923724 124646 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 360 2 2 2 3.2 NC(N)=NC(=O)c1ccc2c(Cl)cnc(-c3ccc(F)cc3F)c2c1 nan
CHEMBL3644541 124646 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 360 2 2 2 3.2 NC(N)=NC(=O)c1ccc2c(Cl)cnc(-c3ccc(F)cc3F)c2c1 nan
CHEMBL5079273 212839 5 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 1 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 1 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None Clc1ccc(CNCCc2cccnc2)c2ncccc12 10.1021/acs.jmedchem.1c02031
91819722 126275 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 365 1 2 2 2.4 NC(N)=NC(=O)N1CCc2c(Cl)ccc(-c3c(F)cncc3F)c2C1 nan
CHEMBL3654204 126275 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 365 1 2 2 2.4 NC(N)=NC(=O)N1CCc2c(Cl)ccc(-c3c(F)cncc3F)c2C1 nan
13972256 119113 1 None 1 2 Rat 8.6 pKi = 8.6 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 233 6 1 2 3.4 CCCN(CCC)[C@H]1C[C@@H]1c1cccc(O)c1 10.1016/0960-894X(96)00045-5
CHEMBL34653 119113 1 None 1 2 Rat 8.6 pKi = 8.6 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 233 6 1 2 3.4 CCCN(CCC)[C@H]1C[C@@H]1c1cccc(O)c1 10.1016/0960-894X(96)00045-5
91819720 126271 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 364 1 2 1 3.0 NC(N)=NC(=O)N1CCc2c(Cl)ccc(-c3ccc(F)cc3F)c2C1 nan
CHEMBL3654200 126271 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 364 1 2 1 3.0 NC(N)=NC(=O)N1CCc2c(Cl)ccc(-c3ccc(F)cc3F)c2C1 nan
60150905 126280 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 302 1 2 1 1.9 NC(N)=NC(=O)N1Cc2c(C3CC3)ccc(F)c2C2(CC2)C1 nan
CHEMBL3654209 126280 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 302 1 2 1 1.9 NC(N)=NC(=O)N1Cc2c(C3CC3)ccc(F)c2C2(CC2)C1 nan
136152964 193270 0 None 2 8 Rat 8.5 pKi = 8.5 Binding
Binding affinity to rat 5HT5A receptorBinding affinity to rat 5HT5A receptor
ChEMBL 259 2 2 3 2.8 C[C@@H]1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL541993 193270 0 None 2 8 Rat 8.5 pKi = 8.5 Binding
Binding affinity to rat 5HT5A receptorBinding affinity to rat 5HT5A receptor
ChEMBL 259 2 2 3 2.8 C[C@@H]1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
1809 134 28 None -229 36 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm030030n
4 134 28 None -229 36 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm030030n
CHEMBL18840 134 28 None -229 36 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm030030n
1809 134 28 None -229 36 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm030030n
4 134 28 None -229 36 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm030030n
CHEMBL18840 134 28 None -229 36 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm030030n
44327952 206304 0 None -3 5 Human 6.7 pKi = 6.7 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 367 5 3 3 2.6 CC[C@@](C)(CO)CNC(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1 10.1021/jm030030n
CHEMBL97518 206304 0 None -3 5 Human 6.7 pKi = 6.7 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 367 5 3 3 2.6 CC[C@@](C)(CO)CNC(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1 10.1021/jm030030n
10872812 17929 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 388 5 0 3 5.3 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(Cl)c(Cl)c1)CC2 10.1021/jm030080s
CHEMBL126897 17929 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 388 5 0 3 5.3 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(Cl)c(Cl)c1)CC2 10.1021/jm030080s
10882775 17930 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 354 5 0 3 4.7 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(Cl)cc1)CC2 10.1021/jm030080s
CHEMBL126898 17930 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 354 5 0 3 4.7 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(Cl)cc1)CC2 10.1021/jm030080s
1524 2150 89 None -1778 51 Human 4.7 pKi = 4.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
197 2150 89 None -1778 51 Human 4.7 pKi = 4.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
3822 2150 89 None -1778 51 Human 4.7 pKi = 4.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
88 2150 89 None -1778 51 Human 4.7 pKi = 4.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
CHEMBL51 2150 89 None -1778 51 Human 4.7 pKi = 4.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
DB12465 2150 89 None -1778 51 Human 4.7 pKi = 4.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
1524 2150 89 None -1778 51 Human 4.7 pKi = 4.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
197 2150 89 None -1778 51 Human 4.7 pKi = 4.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
3822 2150 89 None -1778 51 Human 4.7 pKi = 4.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
88 2150 89 None -1778 51 Human 4.7 pKi = 4.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
CHEMBL51 2150 89 None -1778 51 Human 4.7 pKi = 4.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
DB12465 2150 89 None -1778 51 Human 4.7 pKi = 4.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
71452650 78087 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 330 5 0 2 4.7 Cn1c2c(c3ccccc31)CN(C/C=C\CCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL2111848 78087 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 330 5 0 2 4.7 Cn1c2c(c3ccccc31)CN(C/C=C\CCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL5082151 213016 1 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 1 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 1 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None CN(C)S(=O)(=O)CCNCc1ccc(Cl)c2cccnc12 10.1021/acs.jmedchem.1c02031
127036932 136824 0 None -69 22 Human 5.7 pKi = 5.7 Binding
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
ChEMBL 274 7 1 1 4.0 C=CCN(CC=C)CCc1c[nH]c2ccc(Cl)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3752900 136824 0 None -69 22 Human 5.7 pKi = 5.7 Binding
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
ChEMBL 274 7 1 1 4.0 C=CCN(CC=C)CCc1c[nH]c2ccc(Cl)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL5074821 212565 1 None - 1 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None Cc1cnn(C[C@H](C)NCc2cccc(OCc3ccccn3)c2)c1 10.1021/acs.jmedchem.1c02031
2760172 98353 30 None 1 2 Human 5.7 pKi = 5.7 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 212 1 1 2 2.2 c1ccc2cc(N3CCNCC3)ccc2c1 10.1021/jm030030n
CHEMBL278509 98353 30 None 1 2 Human 5.7 pKi = 5.7 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 212 1 1 2 2.2 c1ccc2cc(N3CCNCC3)ccc2c1 10.1021/jm030030n
CHEMBL5084249 213133 0 None -251 8 Human 5.7 pKi = 5.7 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CCN(CC)CCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
73346042 91402 3 None -21379 17 Human 5.7 pKi = 5.7 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
ChEMBL 405 9 0 8 0.9 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3OCCF)CC2)c1=O 10.1016/j.bmc.2013.05.050
CHEMBL2413153 91402 3 None -21379 17 Human 5.7 pKi = 5.7 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
ChEMBL 405 9 0 8 0.9 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3OCCF)CC2)c1=O 10.1016/j.bmc.2013.05.050
CHEMBL5092728 213610 1 None - 1 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None CC(C)(C)c1ccc2c(c1)CN(C[C@@H](O)COC1CCOCC1)CC2 10.1021/acs.jmedchem.1c02031
70530 96509 96 None -6 3 Mouse 6.7 pKi = 6.7 Binding
Binding affinity towards murine 5-hydroxytryptamine 5A receptorBinding affinity towards murine 5-hydroxytryptamine 5A receptor
ChEMBL 178 1 2 3 0.8 Oc1ccccc1N1CCNCC1 10.1021/jm030030n
CHEMBL266250 96509 96 None -6 3 Mouse 6.7 pKi = 6.7 Binding
Binding affinity towards murine 5-hydroxytryptamine 5A receptorBinding affinity towards murine 5-hydroxytryptamine 5A receptor
ChEMBL 178 1 2 3 0.8 Oc1ccccc1N1CCNCC1 10.1021/jm030030n
1043 1552 13 None -169 28 Human 7.7 pKi = 7.7 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1021/jm990550b
149 1552 13 None -169 28 Human 7.7 pKi = 7.7 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1021/jm990550b
8223 1552 13 None -169 28 Human 7.7 pKi = 7.7 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1021/jm990550b
CHEMBL442 1552 13 None -169 28 Human 7.7 pKi = 7.7 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1021/jm990550b
DB00696 1552 13 None -169 28 Human 7.7 pKi = 7.7 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1021/jm990550b
136152966 95149 0 None -1 5 Human 7.7 pKi = 7.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 289 3 2 4 2.9 COc1c(Cl)ccc2c1C(C)NC(NCC(F)F)=N2 10.1016/j.bmcl.2007.10.078
CHEMBL257744 95149 0 None -1 5 Human 7.7 pKi = 7.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 289 3 2 4 2.9 COc1c(Cl)ccc2c1C(C)NC(NCC(F)F)=N2 10.1016/j.bmcl.2007.10.078
135458427 170987 0 None -5 5 Human 7.7 pKi = 7.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 283 4 2 4 3.0 CC(C)Oc1cccc2c1N=C(NCC(F)F)NC2C 10.1016/j.bmcl.2007.10.078
CHEMBL446459 170987 0 None -5 5 Human 7.7 pKi = 7.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 283 4 2 4 3.0 CC(C)Oc1cccc2c1N=C(NCC(F)F)NC2C 10.1016/j.bmcl.2007.10.078
44456395 95227 0 None -1 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 225 1 2 4 2.0 COc1c(Cl)ccc2c1C(C)NC(N)=N2 10.1016/j.bmcl.2007.10.080
CHEMBL258073 95227 0 None -1 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 225 1 2 4 2.0 COc1c(Cl)ccc2c1C(C)NC(N)=N2 10.1016/j.bmcl.2007.10.080
134138168 147158 0 None -19 10 Human 6.7 pKi = 6.7 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL 275 4 0 2 4.1 COc1ccccc1-c1cc(CN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
CHEMBL3931889 147158 0 None -19 10 Human 6.7 pKi = 6.7 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL 275 4 0 2 4.1 COc1ccccc1-c1cc(CN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
4806 3945 85 None -10 13 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
7351 3945 85 None -10 13 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
9966051 3945 85 None -10 13 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
CHEMBL2104993 3945 85 None -10 13 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
DB09068 3945 85 None -10 13 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
24841480 183317 0 None -1096 20 Human 5.7 pKi = 5.7 Binding
Antagonist activity at serotonin 5HT5A receptor (unknown origin) by PDSP assayAntagonist activity at serotonin 5HT5A receptor (unknown origin) by PDSP assay
ChEMBL 340 3 0 4 4.5 O=C(OCCN1CCCC1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
CHEMBL481153 183317 0 None -1096 20 Human 5.7 pKi = 5.7 Binding
Antagonist activity at serotonin 5HT5A receptor (unknown origin) by PDSP assayAntagonist activity at serotonin 5HT5A receptor (unknown origin) by PDSP assay
ChEMBL 340 3 0 4 4.5 O=C(OCCN1CCCC1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
181743 177997 3 None -1122 22 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5HT5A receptorDisplacement of [3H]LSD from human 5HT5A receptor
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2009.11.053
CHEMBL467094 177997 3 None -1122 22 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5HT5A receptorDisplacement of [3H]LSD from human 5HT5A receptor
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2009.11.053
44351180 17900 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 372 5 0 3 4.8 Cn1c2c(c3cccc(Cl)c31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL126737 17900 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 372 5 0 3 4.8 Cn1c2c(c3cccc(Cl)c31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030080s
44351077 116469 0 None 1 3 Mouse 6.7 pKi = 6.7 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 352 5 1 3 4.2 Cn1c2c(c3ccccc31)CN(CCCC(O)c1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL338696 116469 0 None 1 3 Mouse 6.7 pKi = 6.7 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 352 5 1 3 4.2 Cn1c2c(c3ccccc31)CN(CCCC(O)c1ccc(F)cc1)CC2 10.1021/jm030080s
118464420 137717 0 None -38 8 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 335 1 3 5 2.8 NC1=NC2(CCCCC2)NC(Nc2cccc(Br)c2)=N1 10.1021/acs.jmedchem.5b01631
CHEMBL3770342 137717 0 None -38 8 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 335 1 3 5 2.8 NC1=NC2(CCCCC2)NC(Nc2cccc(Br)c2)=N1 10.1021/acs.jmedchem.5b01631
10324985 76428 7 None -169 17 Human 6.6 pKi = 6.6 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
CHEMBL199824 76428 7 None -169 17 Human 6.6 pKi = 6.6 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
CHEMBL2068762 76428 7 None -169 17 Human 6.6 pKi = 6.6 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
168293874 191581 0 None -52 11 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constant
ChEMBL 312 2 3 3 3.3 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5204071 191581 0 None -52 11 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constant
ChEMBL 312 2 3 3 3.3 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5090584 213497 2 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor incubated for 2 hr by radioligand binding assay
ChEMBL None None None CN(C)S(=O)(=O)CCNCc1cccc2cccnc12 10.1021/acs.jmedchem.1c02031
CHEMBL5071978 212501 0 None -3 6 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CCN(CC)Cc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
117209858 183971 1 None -147 7 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
ChEMBL 262 2 2 3 2.1 Clc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4848305 183971 1 None -147 7 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
ChEMBL 262 2 2 3 2.1 Clc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
122334 319 19 None -51 8 Human 5.6 pKi = 5.6 Binding
Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )
ChEMBL 233 4 1 2 3.1 CCCN[C@@H]1CCc2c([C@@H]1C)cccc2OC 10.1016/S0960-894X(01)80181-5
970 319 19 None -51 8 Human 5.6 pKi = 5.6 Binding
Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )
ChEMBL 233 4 1 2 3.1 CCCN[C@@H]1CCc2c([C@@H]1C)cccc2OC 10.1016/S0960-894X(01)80181-5
CHEMBL27441 319 19 None -51 8 Human 5.6 pKi = 5.6 Binding
Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )
ChEMBL 233 4 1 2 3.1 CCCN[C@@H]1CCc2c([C@@H]1C)cccc2OC 10.1016/S0960-894X(01)80181-5
136118614 92632 0 None -25 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3ccc(Br)cc23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL2442276 92632 0 None -25 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3ccc(Br)cc23)C1=O 10.1016/j.bmc.2013.09.011
155770281 177173 0 None -2 9 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT5A (unknown origin)Binding affinity to 5HT5A (unknown origin)
ChEMBL 517 4 1 2 7.6 CC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.1c00164
CHEMBL4642592 177173 0 None -2 9 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT5A (unknown origin)Binding affinity to 5HT5A (unknown origin)
ChEMBL 517 4 1 2 7.6 CC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.1c00164
44355141 24442 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 261 8 0 2 3.9 CCCN(CCC)C[C@H]1C[C@@H]1c1ccccc1OC 10.1016/0960-894X(96)00045-5
CHEMBL134331 24442 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 261 8 0 2 3.9 CCCN(CCC)C[C@H]1C[C@@H]1c1ccccc1OC 10.1016/0960-894X(96)00045-5
127036953 136990 0 None -239 22 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
ChEMBL 318 7 1 1 4.1 C=CCN(CC=C)CCc1c[nH]c2ccc(Br)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3754166 136990 0 None -239 22 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
ChEMBL 318 7 1 1 4.1 C=CCN(CC=C)CCc1c[nH]c2ccc(Br)cc12 10.1016/j.bmcl.2015.12.053
44455986 97147 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 175 1 2 3 1.7 CCC1NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.080
CHEMBL270841 97147 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 175 1 2 3 1.7 CCC1NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.080
CHEMBL5093342 213788 0 None -28 7 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CCCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5095971 213788 0 None -28 7 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CCCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5090884 213801 0 None -37 7 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CCCCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5096072 213801 0 None -37 7 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CCCCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
136152973 94781 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 247 5 2 4 2.4 CCCOCCNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
CHEMBL256048 94781 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 247 5 2 4 2.4 CCCOCCNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
107838 96874 106 None 1 2 Mouse 5.6 pKi = 5.6 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptorBinding affinity towards mouse 5-hydroxytryptamine 5A receptor
ChEMBL 172 0 2 1 1.8 c1ccc2c3c([nH]c2c1)CNCC3 10.1021/jm030030n
CHEMBL269236 96874 106 None 1 2 Mouse 5.6 pKi = 5.6 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptorBinding affinity towards mouse 5-hydroxytryptamine 5A receptor
ChEMBL 172 0 2 1 1.8 c1ccc2c3c([nH]c2c1)CNCC3 10.1021/jm030030n
CHEMBL4576555 212264 3 None -2 14 Human 5.6 pKi = 5.6 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000705a HTR5ASelectivity interaction (GPCR panel (PDSP screen)) EUB0000705a HTR5A
ChEMBL None None None CN1CCN(C(=O)C(C)(C)c2ccc(C(=O)Nc3cn4cc(-c5cc(C(C)(C)C)cc(C(C)(C)C)c5)ccc4n3)cc2)CC1 nan
44351140 18851 0 None 3 3 Mouse 7.6 pKi = 7.6 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 320 5 0 3 4.0 Cn1c2c(c3ccccc31)CN(CCCOc1ccccc1)CC2 10.1021/jm030080s
CHEMBL128848 18851 0 None 3 3 Mouse 7.6 pKi = 7.6 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 320 5 0 3 4.0 Cn1c2c(c3ccccc31)CN(CCCOc1ccccc1)CC2 10.1021/jm030080s
11444050 11649 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 537 13 2 3 7.1 O=C(CCC1CCCC1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)CC1CCCCN1 10.1016/j.bmcl.2005.06.024
CHEMBL1181620 11649 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 537 13 2 3 7.1 O=C(CCC1CCCC1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)CC1CCCCN1 10.1016/j.bmcl.2005.06.024
CHEMBL185676 11649 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 537 13 2 3 7.1 O=C(CCC1CCCC1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)CC1CCCCN1 10.1016/j.bmcl.2005.06.024
9827938 11666 0 None 6 12 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 517 13 1 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL1181680 11666 0 None 6 12 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 517 13 1 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL188486 11666 0 None 6 12 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 517 13 1 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
11352884 66822 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 518 13 1 4 5.7 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)nc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL187621 66822 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 518 13 1 4 5.7 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)nc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
135966709 154616 4 None -10 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 233 2 2 4 2.3 CNC1=Nc2c(OC(C)C)cccc2C(C)N1 10.1016/j.bmcl.2007.10.080
CHEMBL402179 154616 4 None -10 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 233 2 2 4 2.3 CNC1=Nc2c(OC(C)C)cccc2C(C)N1 10.1016/j.bmcl.2007.10.080
5 139 66 None -323 54 Human 6.6 pKi = 6.6 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
5202 139 66 None -323 54 Human 6.6 pKi = 6.6 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
CHEMBL39 139 66 None -323 54 Human 6.6 pKi = 6.6 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
DB08839 139 66 None -323 54 Human 6.6 pKi = 6.6 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
10893866 20108 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 365 6 0 5 3.9 Cn1c2c(c3ccccc31)CN(CCCOc1ccc([N+](=O)[O-])cc1)CC2 10.1021/jm030080s
CHEMBL130585 20108 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 365 6 0 5 3.9 Cn1c2c(c3ccccc31)CN(CCCOc1ccc([N+](=O)[O-])cc1)CC2 10.1021/jm030080s
44351099 17871 0 None - 1 Mouse 6.6 pKi = 6.6 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 304 4 0 2 4.2 Cn1c2c(c3ccccc31)CN(CCCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL126574 17871 0 None - 1 Mouse 6.6 pKi = 6.6 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 304 4 0 2 4.2 Cn1c2c(c3ccccc31)CN(CCCc1ccccc1)CC2 10.1021/jm030080s
1220 186 46 None -1548 44 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030030n
31 186 46 None -1548 44 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030030n
7 186 46 None -1548 44 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030030n
CHEMBL56 186 46 None -1548 44 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030030n
1220 186 46 None -1548 44 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030030n
31 186 46 None -1548 44 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030030n
7 186 46 None -1548 44 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030030n
CHEMBL56 186 46 None -1548 44 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030030n
44397593 11664 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 553 14 1 4 6.1 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)S(=O)(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL1181677 11664 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 553 14 1 4 6.1 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)S(=O)(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL188440 11664 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 553 14 1 4 6.1 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)S(=O)(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
44397513 12160 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 523 12 1 3 6.5 CN(C)CCN(Cc1ccc(-c2ccc(CNC3Cc4ccccc4C3)cc2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
CHEMBL1184719 12160 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 523 12 1 3 6.5 CN(C)CCN(Cc1ccc(-c2ccc(CNC3Cc4ccccc4C3)cc2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
CHEMBL365422 12160 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 523 12 1 3 6.5 CN(C)CCN(Cc1ccc(-c2ccc(CNC3Cc4ccccc4C3)cc2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
44455943 168436 5 None 2 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 243 1 2 3 3.0 CCC1NC(N)=Nc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2007.10.080
CHEMBL439240 168436 5 None 2 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 243 1 2 3 3.0 CCC1NC(N)=Nc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2007.10.080
10472143 118772 0 None -60 16 Human 7.6 pKi = 7.6 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
CHEMBL343755 118772 0 None -60 16 Human 7.6 pKi = 7.6 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
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
44351193 116352 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 372 5 0 3 4.8 Cn1c2c(c3cc(Cl)ccc31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL338095 116352 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 372 5 0 3 4.8 Cn1c2c(c3cc(Cl)ccc31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL5092524 213601 2 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor incubated for 2 hr by radioligand binding assay
ChEMBL None None None CN(C)S(=O)(=O)CCNCc1ccc(F)c2cccnc12 10.1021/acs.jmedchem.1c02031
44456284 12736 1 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 161 0 2 3 1.0 Cc1ccc2c(c1)N=C(N)NC2 10.1016/j.bmcl.2007.10.080
CHEMBL1188595 12736 1 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 161 0 2 3 1.0 Cc1ccc2c(c1)N=C(N)NC2 10.1016/j.bmcl.2007.10.080
CHEMBL536789 12736 1 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 161 0 2 3 1.0 Cc1ccc2c(c1)N=C(N)NC2 10.1016/j.bmcl.2007.10.080
136152969 154786 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 286 1 2 4 1.9 CC1NC(NC2CCCCN(C)C2=O)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
CHEMBL403103 154786 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 286 1 2 4 1.9 CC1NC(NC2CCCCN(C)C2=O)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
135458428 154994 0 None 1 5 Human 7.6 pKi = 7.6 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 255 3 2 4 2.2 COc1cccc2c1N=C(NCC(F)F)NC2C 10.1016/j.bmcl.2007.10.078
CHEMBL404248 154994 0 None 1 5 Human 7.6 pKi = 7.6 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 255 3 2 4 2.2 COc1cccc2c1N=C(NCC(F)F)NC2C 10.1016/j.bmcl.2007.10.078
12683497 97071 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 175 0 1 3 1.3 CN(C)C1=Nc2ccccc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL270409 97071 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 175 0 1 3 1.3 CN(C)C1=Nc2ccccc2CN1 10.1016/j.bmcl.2007.10.080
4407909 192264 1 None -50 10 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constant
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5182943 192264 1 None -50 10 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constant
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5221893 192264 1 None -50 10 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constant
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
44351077 116469 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 352 5 1 3 4.2 Cn1c2c(c3ccccc31)CN(CCCC(O)c1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL338696 116469 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 352 5 1 3 4.2 Cn1c2c(c3ccccc31)CN(CCCC(O)c1ccc(F)cc1)CC2 10.1021/jm030080s
44374431 54667 0 None -1 4 Human 6.5 pKi = 6.5 Binding
Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )
ChEMBL 261 4 1 3 2.9 CCCN[C@@H]1CCc2c(C(=O)OC)cccc2[C@@H]1C 10.1016/S0960-894X(01)80181-5
CHEMBL161507 54667 0 None -1 4 Human 6.5 pKi = 6.5 Binding
Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )
ChEMBL 261 4 1 3 2.9 CCCN[C@@H]1CCc2c(C(=O)OC)cccc2[C@@H]1C 10.1016/S0960-894X(01)80181-5
90469115 185260 2 None -954 17 Human 5.5 pKi = 5.5 Binding
Binding affinity to human 5-HT5A receptorBinding affinity to human 5-HT5A receptor
ChEMBL 410 3 1 6 3.0 O=S(=O)(c1cccc(F)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
CHEMBL4867565 185260 2 None -954 17 Human 5.5 pKi = 5.5 Binding
Binding affinity to human 5-HT5A receptorBinding affinity to human 5-HT5A receptor
ChEMBL 410 3 1 6 3.0 O=S(=O)(c1cccc(F)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
CHEMBL5093652 213662 2 None - 1 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None N#CC1(c2ccccc2)CCC(NCCc2nnc3ccccn23)CC1 10.1021/acs.jmedchem.1c02031
CHEMBL5094493 213723 0 None -144 7 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CCCN(CCC)CCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
44351171 116349 0 None 2 2 Mouse 6.5 pKi = 6.5 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 334 6 0 3 4.1 Cn1c2c(c3ccccc31)CN(CCCOCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL338081 116349 0 None 2 2 Mouse 6.5 pKi = 6.5 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 334 6 0 3 4.1 Cn1c2c(c3ccccc31)CN(CCCOCc1ccccc1)CC2 10.1021/jm030080s
44275750 92781 34 None 1 2 Human 8.5 pKi = 8.5 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 228 1 2 3 2.0 Oc1ccc2cccc(N3CCNCC3)c2c1 10.1021/jm030030n
CHEMBL24462 92781 34 None 1 2 Human 8.5 pKi = 8.5 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 228 1 2 3 2.0 Oc1ccc2cccc(N3CCNCC3)c2c1 10.1021/jm030030n
CHEMBL5075486 212605 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 32 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 32 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None O=S1(=O)CCC[C@@H](CNCc2ccc(Cl)c3cccnc23)C1 10.1021/acs.jmedchem.1c02031
50923584 124638 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 326 2 2 2 2.6 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3ccccc3F)c2c1 nan
CHEMBL3644533 124638 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 326 2 2 2 2.6 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3ccccc3F)c2c1 nan
50923585 124639 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 342 2 2 2 3.1 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3ccccc3Cl)c2c1 nan
CHEMBL3644534 124639 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 342 2 2 2 3.1 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3ccccc3Cl)c2c1 nan
91819719 126267 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 348 1 2 1 2.5 NC(N)=NC(=O)N1CCc2cccc(-c3cc(F)c(F)cc3F)c2C1 nan
CHEMBL3654196 126267 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 348 1 2 1 2.5 NC(N)=NC(=O)N1CCc2cccc(-c3cc(F)c(F)cc3F)c2C1 nan
60150903 126282 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 366 1 2 1 2.7 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3cc(F)c(F)cc3F)c2C1 nan
CHEMBL3654211 126282 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 366 1 2 1 2.7 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3cc(F)c(F)cc3F)c2C1 nan
50923581 124631 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 372 2 2 2 3.4 Cc1nc2ccc(C(=O)N=C(N)N)cc2c(-c2c(F)cc(F)cc2F)c1C nan
CHEMBL3644526 124631 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 372 2 2 2 3.4 Cc1nc2ccc(C(=O)N=C(N)N)cc2c(-c2c(F)cc(F)cc2F)c1C nan
60150900 126274 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 345 1 2 2 2.1 Cc1ccc(-c2ncc(F)cc2F)c2c1CCN(C(=O)N=C(N)N)C2 nan
CHEMBL3654203 126274 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 345 1 2 2 2.1 Cc1ccc(-c2ncc(F)cc2F)c2c1CCN(C(=O)N=C(N)N)C2 nan
24936155 94185 0 None -501 7 Human 5.5 pKi = 5.5 Binding
Inhibition of 5HT5A receptorInhibition of 5HT5A receptor
ChEMBL 508 4 2 3 5.1 CC(=O)N1C2C=C(CN3C4CCC3CC(NC(=O)Nc3cc(F)cc(C(F)(F)F)c3)C4)CC1CCC2 10.1016/j.bmcl.2007.10.109
CHEMBL252258 94185 0 None -501 7 Human 5.5 pKi = 5.5 Binding
Inhibition of 5HT5A receptorInhibition of 5HT5A receptor
ChEMBL 508 4 2 3 5.1 CC(=O)N1C2C=C(CN3C4CCC3CC(NC(=O)Nc3cc(F)cc(C(F)(F)F)c3)C4)CC1CCC2 10.1016/j.bmcl.2007.10.109
44374648 119467 0 None -18 4 Human 5.5 pKi = 5.5 Binding
Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )
ChEMBL 351 5 1 4 3.3 CCCN[C@@H]1CCc2c(OS(=O)(=O)C(F)(F)F)cccc2[C@@H]1C 10.1016/S0960-894X(01)80181-5
CHEMBL349843 119467 0 None -18 4 Human 5.5 pKi = 5.5 Binding
Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )
ChEMBL 351 5 1 4 3.3 CCCN[C@@H]1CCc2c(OS(=O)(=O)C(F)(F)F)cccc2[C@@H]1C 10.1016/S0960-894X(01)80181-5
4106 2466 16 None -14 33 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5-HT5A (unknown origin)Binding affinity to 5-HT5A (unknown origin)
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/acs.jnatprod.0c00793
5358812 2466 16 None -14 33 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5-HT5A (unknown origin)Binding affinity to 5-HT5A (unknown origin)
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/acs.jnatprod.0c00793
89 2466 16 None -14 33 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5-HT5A (unknown origin)Binding affinity to 5-HT5A (unknown origin)
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/acs.jnatprod.0c00793
CHEMBL93240 2466 16 None -14 33 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5-HT5A (unknown origin)Binding affinity to 5-HT5A (unknown origin)
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/acs.jnatprod.0c00793
11272242 11657 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 512 14 1 4 5.9 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccn3)cc2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
CHEMBL1181641 11657 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 512 14 1 4 5.9 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccn3)cc2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
CHEMBL186849 11657 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 512 14 1 4 5.9 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccn3)cc2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
11364267 67199 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 512 14 1 4 5.9 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)nc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
CHEMBL189689 67199 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 512 14 1 4 5.9 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)nc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
44355165 115970 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 261 8 0 2 3.9 CCCN(CCC)C[C@H]1C[C@@H]1c1cccc(OC)c1 10.1016/0960-894X(96)00045-5
CHEMBL336124 115970 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 261 8 0 2 3.9 CCCN(CCC)C[C@H]1C[C@@H]1c1cccc(OC)c1 10.1016/0960-894X(96)00045-5
10287730 3480 36 None -3981 12 Human 5.5 pKi = 5.5 Binding
Binding affinity for human 5-hydroxytryptamine 5A receptor Binding affinity for human 5-hydroxytryptamine 5A receptor
ChEMBL 412 6 0 5 4.3 Cc1ccc2c(n1)cccc2OCCN1CCN(CC1)Cc1cccc2c1nccc2 10.1021/jm049039v
77 3480 36 None -3981 12 Human 5.5 pKi = 5.5 Binding
Binding affinity for human 5-hydroxytryptamine 5A receptor Binding affinity for human 5-hydroxytryptamine 5A receptor
ChEMBL 412 6 0 5 4.3 Cc1ccc2c(n1)cccc2OCCN1CCN(CC1)Cc1cccc2c1nccc2 10.1021/jm049039v
CHEMBL425190 3480 36 None -3981 12 Human 5.5 pKi = 5.5 Binding
Binding affinity for human 5-hydroxytryptamine 5A receptor Binding affinity for human 5-hydroxytryptamine 5A receptor
ChEMBL 412 6 0 5 4.3 Cc1ccc2c(n1)cccc2OCCN1CCN(CC1)Cc1cccc2c1nccc2 10.1021/jm049039v
44397511 11663 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 407 10 1 3 4.7 CN(C)CCN(Cc1ccc(-c2ccc(CN)cc2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
CHEMBL1181669 11663 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 407 10 1 3 4.7 CN(C)CCN(Cc1ccc(-c2ccc(CN)cc2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
CHEMBL188050 11663 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 407 10 1 3 4.7 CN(C)CCN(Cc1ccc(-c2ccc(CN)cc2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
107838 96874 106 None -1 2 Human 5.5 pKi = 5.5 Binding
Binding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligandBinding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligand
ChEMBL 172 0 2 1 1.8 c1ccc2c3c([nH]c2c1)CNCC3 10.1021/jm030080s
CHEMBL269236 96874 106 None -1 2 Human 5.5 pKi = 5.5 Binding
Binding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligandBinding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligand
ChEMBL 172 0 2 1 1.8 c1ccc2c3c([nH]c2c1)CNCC3 10.1021/jm030080s
127036186 136889 0 None -102 19 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
ChEMBL 254 7 1 1 3.7 C=CCN(CC=C)CCc1c[nH]c2ccc(C)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3753318 136889 0 None -102 19 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
ChEMBL 254 7 1 1 3.7 C=CCN(CC=C)CCc1c[nH]c2ccc(C)cc12 10.1016/j.bmcl.2015.12.053
216239 23591 114 None -6 7 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from 5HT5A receptor after 1.5 hrs by scintillation counterDisplacement of [3H]LSD from 5HT5A receptor after 1.5 hrs by scintillation counter
ChEMBL 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 10.1021/jm300338m
CHEMBL1200485 23591 114 None -6 7 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from 5HT5A receptor after 1.5 hrs by scintillation counterDisplacement of [3H]LSD from 5HT5A receptor after 1.5 hrs by scintillation counter
ChEMBL 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 10.1021/jm300338m
CHEMBL1336 23591 114 None -6 7 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from 5HT5A receptor after 1.5 hrs by scintillation counterDisplacement of [3H]LSD from 5HT5A receptor after 1.5 hrs by scintillation counter
ChEMBL 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 10.1021/jm300338m
136116062 97231 0 None 2 4 Human 7.5 pKi = 7.5 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 293 2 2 3 3.5 CC1NC(NCC(F)F)=Nc2c(Cl)ccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL271253 97231 0 None 2 4 Human 7.5 pKi = 7.5 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 293 2 2 3 3.5 CC1NC(NCC(F)F)=Nc2c(Cl)ccc(Cl)c21 10.1016/j.bmcl.2007.10.078
71452650 78087 0 None -1 3 Mouse 6.5 pKi = 6.5 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 330 5 0 2 4.7 Cn1c2c(c3ccccc31)CN(C/C=C\CCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL2111848 78087 0 None -1 3 Mouse 6.5 pKi = 6.5 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 330 5 0 2 4.7 Cn1c2c(c3ccccc31)CN(C/C=C\CCc1ccccc1)CC2 10.1021/jm030080s
50878551 90314 60 None -85 18 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL2391541 90314 60 None -85 18 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2015.12.053
136118651 75971 0 None -9 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3c(Br)cccc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2058706 75971 0 None -9 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3c(Br)cccc23)N1 10.1016/j.bmc.2013.09.011
10892139 165035 0 None -1 2 Mouse 6.5 pKi = 6.5 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 306 5 1 2 4.0 c1ccc(OCCCN2CCc3c([nH]c4ccccc34)C2)cc1 10.1021/jm030080s
CHEMBL424258 165035 0 None -1 2 Mouse 6.5 pKi = 6.5 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 306 5 1 2 4.0 c1ccc(OCCCN2CCc3c([nH]c4ccccc34)C2)cc1 10.1021/jm030080s
122483275 137582 0 None -15 8 Human 6.5 pKi = 6.5 Binding
Binding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 427 6 1 5 5.1 O=C(CCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
CHEMBL3764133 137582 0 None -15 8 Human 6.5 pKi = 6.5 Binding
Binding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 427 6 1 5 5.1 O=C(CCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
CHEMBL3765875 137582 0 None -15 8 Human 6.5 pKi = 6.5 Binding
Binding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 427 6 1 5 5.1 O=C(CCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
136118648 75968 0 None -67 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3cccc(Br)c23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2058703 75968 0 None -67 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3cccc(Br)c23)N1 10.1016/j.bmc.2013.09.011
44351361 17785 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 365 5 1 4 4.3 Cn1c2c(c3ccccc31)CN(CCC/C(=N/O)c1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL126138 17785 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 365 5 1 4 4.3 Cn1c2c(c3ccccc31)CN(CCC/C(=N/O)c1ccc(F)cc1)CC2 10.1021/jm030080s
9862256 205391 0 None -2238 9 Rat 5.5 pKi = 5.5 Binding
Binding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligand
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL92139 205391 0 None -2238 9 Rat 5.5 pKi = 5.5 Binding
Binding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligand
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
10035245 29481 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 181 0 2 3 1.4 NC1=Nc2cc(Cl)ccc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL13864 29481 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 181 0 2 3 1.4 NC1=Nc2cc(Cl)ccc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL538340 29481 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 181 0 2 3 1.4 NC1=Nc2cc(Cl)ccc2CN1 10.1016/j.bmcl.2007.10.080
10926167 117590 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 350 6 0 4 4.0 COc1ccc(OCCCN2CCc3c(c4ccccc4n3C)C2)cc1 10.1021/jm030080s
CHEMBL340646 117590 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 350 6 0 4 4.0 COc1ccc(OCCCN2CCc3c(c4ccccc4n3C)C2)cc1 10.1021/jm030080s
44351100 170905 0 None -1 3 Mouse 6.5 pKi = 6.5 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 330 5 0 2 4.7 Cn1c2c(c3ccccc31)CN(C/C=C/CCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL446356 170905 0 None -1 3 Mouse 6.5 pKi = 6.5 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 330 5 0 2 4.7 Cn1c2c(c3ccccc31)CN(C/C=C/CCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL5094680 213734 0 None -23 8 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CCCCNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
11726973 17917 0 None 1 3 Mouse 6.4 pKi = 6.4 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 320 5 0 3 4.0 Cn1c2c(c3ccccc31)CCN(CCCOc1ccccc1)C2 10.1021/jm030080s
CHEMBL126823 17917 0 None 1 3 Mouse 6.4 pKi = 6.4 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 320 5 0 3 4.0 Cn1c2c(c3ccccc31)CCN(CCCOc1ccccc1)C2 10.1021/jm030080s
136152970 94912 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 309 2 2 5 2.8 CC1NC(NCC2COc3ccccc3O2)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
CHEMBL256693 94912 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 309 2 2 5 2.8 CC1NC(NCC2COc3ccccc3O2)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
44355425 23385 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 247 7 1 2 3.6 CCCN(CCC)C[C@@H]1C[C@@H]1c1ccccc1O 10.1016/0960-894X(96)00045-5
CHEMBL133433 23385 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 247 7 1 2 3.6 CCCN(CCC)C[C@@H]1C[C@@H]1c1ccccc1O 10.1016/0960-894X(96)00045-5
44455985 13041 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 161 0 2 3 1.3 CC1NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
CHEMBL1190709 13041 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 161 0 2 3 1.3 CC1NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
CHEMBL541396 13041 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 161 0 2 3 1.3 CC1NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
44455985 13041 1 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 161 0 2 3 1.3 CC1NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.080
CHEMBL1190709 13041 1 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 161 0 2 3 1.3 CC1NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.080
CHEMBL541396 13041 1 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 161 0 2 3 1.3 CC1NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.080
CHEMBL5074190 212543 0 None -151 9 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None COc1ccccc1-c1cc(CCN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
44355426 23975 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 261 8 0 2 3.9 CCCN(CCC)C[C@@H]1C[C@@H]1c1cccc(OC)c1 10.1016/0960-894X(96)00045-5
CHEMBL133935 23975 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 261 8 0 2 3.9 CCCN(CCC)C[C@@H]1C[C@@H]1c1cccc(OC)c1 10.1016/0960-894X(96)00045-5
752521 197060 7 None -19 9 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 295 1 3 5 1.9 CC1(C)N=C(N)N=C(Nc2cccc(Br)c2)N1 10.1021/acs.jmedchem.5b01631
CHEMBL582877 197060 7 None -19 9 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 295 1 3 5 1.9 CC1(C)N=C(N)N=C(Nc2cccc(Br)c2)N1 10.1021/acs.jmedchem.5b01631
136152978 95082 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 207 2 2 3 1.9 CC1NC(NCCF)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
CHEMBL257450 95082 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 207 2 2 3 1.9 CC1NC(NCCF)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
44397435 11658 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 506 12 2 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)Nc1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL1181643 11658 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 506 12 2 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)Nc1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL187029 11658 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 506 12 2 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)Nc1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL5089996 213461 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 32 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 32 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None CN1CC[C@H](CNCc2ccc(Cl)c3cccnc23)CC1=O 10.1021/acs.jmedchem.1c02031
50923444 124634 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 360 2 2 2 3.2 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3ccc(F)cc3Cl)c2c1 nan
CHEMBL3644529 124634 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 360 2 2 2 3.2 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3ccc(F)cc3Cl)c2c1 nan
91819724 126284 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 331 1 2 2 1.8 NC(N)=NC(=O)N1CCc2cccc(-c3ncc(F)cc3F)c2C1 nan
CHEMBL3654213 126284 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 331 1 2 2 1.8 NC(N)=NC(=O)N1CCc2cccc(-c3ncc(F)cc3F)c2C1 nan
91819718 126266 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 365 1 2 2 2.4 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3ncc(Cl)cc3F)c2C1 nan
CHEMBL3654195 126266 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 365 1 2 2 2.4 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3ncc(Cl)cc3F)c2C1 nan
50923722 124644 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 376 3 2 2 3.5 NC(N)=NC(=O)c1ccc2c(C(F)F)cnc(-c3c(F)cccc3F)c2c1 nan
CHEMBL3644539 124644 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 376 3 2 2 3.5 NC(N)=NC(=O)c1ccc2c(C(F)F)cnc(-c3c(F)cccc3F)c2c1 nan
50923719 124641 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 361 2 2 3 2.6 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3c(F)cncc3Cl)c2c1 nan
CHEMBL3644536 124641 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 361 2 2 3 2.6 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3c(F)cncc3Cl)c2c1 nan
16093485 154524 0 None -1 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 239 1 2 4 2.3 COc1cc(Cl)c(C)c2c1N=C(N)NC2C 10.1016/j.bmcl.2007.10.080
CHEMBL401745 154524 0 None -1 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 239 1 2 4 2.3 COc1cc(Cl)c(C)c2c1N=C(N)NC2C 10.1016/j.bmcl.2007.10.080
13972211 138408 1 None 28 2 Rat 8.3 pKi = 8.3 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 233 6 1 2 3.4 CCCN(CCC)[C@H]1C[C@@H]1c1ccccc1O 10.1016/0960-894X(96)00045-5
CHEMBL37844 138408 1 None 28 2 Rat 8.3 pKi = 8.3 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 233 6 1 2 3.4 CCCN(CCC)[C@H]1C[C@@H]1c1ccccc1O 10.1016/0960-894X(96)00045-5
1342 36 42 None -16 18 Human 7.4 pKi = 7.4 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1021/jm030030n
3 36 42 None -16 18 Human 7.4 pKi = 7.4 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1021/jm030030n
CHEMBL277120 36 42 None -16 18 Human 7.4 pKi = 7.4 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1021/jm030030n
1043 1552 13 None -169 28 Human 7.4 pKi = 7.4 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1021/jm030030n
149 1552 13 None -169 28 Human 7.4 pKi = 7.4 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1021/jm030030n
8223 1552 13 None -169 28 Human 7.4 pKi = 7.4 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1021/jm030030n
CHEMBL442 1552 13 None -169 28 Human 7.4 pKi = 7.4 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1021/jm030030n
DB00696 1552 13 None -169 28 Human 7.4 pKi = 7.4 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1021/jm030030n
1342 36 42 None -16 18 Mouse 7.4 pKi = 7.4 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [3H]- LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [3H]- LSD as radioligand
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1021/jm030030n
3 36 42 None -16 18 Mouse 7.4 pKi = 7.4 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [3H]- LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [3H]- LSD as radioligand
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1021/jm030030n
CHEMBL277120 36 42 None -16 18 Mouse 7.4 pKi = 7.4 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [3H]- LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [3H]- LSD as radioligand
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1021/jm030030n
11808247 17891 0 None -4 9 Human 6.4 pKi = 6.4 Binding
Binding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligandBinding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligand
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1021/jm030080s
CHEMBL126667 17891 0 None -4 9 Human 6.4 pKi = 6.4 Binding
Binding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligandBinding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligand
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1021/jm030080s
CHEMBL3819366 17891 0 None -4 9 Human 6.4 pKi = 6.4 Binding
Binding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligandBinding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligand
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1021/jm030080s
9927441 205662 0 None -1174 9 Rat 5.4 pKi = 5.4 Binding
Binding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligand
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm010943m
CHEMBL93868 205662 0 None -1174 9 Rat 5.4 pKi = 5.4 Binding
Binding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligand
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm010943m
44455962 168780 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 195 0 2 3 2.0 C[C@H]1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL441896 168780 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 195 0 2 3 2.0 C[C@H]1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
145980271 165939 0 None -8 16 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells by radioligand binding assay
ChEMBL 538 8 1 3 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL4278465 165939 0 None -8 16 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells by radioligand binding assay
ChEMBL 538 8 1 3 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
92042876 150804 0 None -79 10 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL 261 4 1 2 3.7 CNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL3961059 150804 0 None -79 10 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL 261 4 1 2 3.7 CNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
127026052 137028 0 None -257 19 Human 5.4 pKi = 5.4 Binding
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
ChEMBL 258 7 1 1 3.5 C=CCN(CC=C)CCc1c[nH]c2ccc(F)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3754496 137028 0 None -257 19 Human 5.4 pKi = 5.4 Binding
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
ChEMBL 258 7 1 1 3.5 C=CCN(CC=C)CCc1c[nH]c2ccc(F)cc12 10.1016/j.bmcl.2015.12.053
9904281 47485 24 None 4 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 215 0 2 3 2.0 NC1=Nc2ccc(Cl)c(Cl)c2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL1548 47485 24 None 4 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 215 0 2 3 2.0 NC1=Nc2ccc(Cl)c(Cl)c2CN1 10.1016/j.bmcl.2007.10.080
44355180 164782 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 233 6 0 2 3.1 CCN(CC)C[C@H]1C[C@@H]1c1ccccc1OC 10.1016/0960-894X(96)00045-5
CHEMBL423527 164782 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 233 6 0 2 3.1 CCN(CC)C[C@H]1C[C@@H]1c1ccccc1OC 10.1016/0960-894X(96)00045-5
44351101 16768 0 None 1 2 Mouse 6.4 pKi = 6.4 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 346 7 0 2 5.3 Cn1c2c(c3ccccc31)CN(CCCCCCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL125361 16768 0 None 1 2 Mouse 6.4 pKi = 6.4 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 346 7 0 2 5.3 Cn1c2c(c3ccccc31)CN(CCCCCCc1ccccc1)CC2 10.1021/jm030080s
9796627 96205 0 None -154 7 Rat 5.4 pKi = 5.4 Binding
Binding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligand
ChEMBL 308 4 1 4 3.1 CN(C)CCc1cn(C(=O)c2ccccc2)c2ccc(O)cc12 10.1021/jm010943m
CHEMBL263700 96205 0 None -154 7 Rat 5.4 pKi = 5.4 Binding
Binding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligand
ChEMBL 308 4 1 4 3.1 CN(C)CCc1cn(C(=O)c2ccccc2)c2ccc(O)cc12 10.1021/jm010943m
3649661 137691 6 None -63 8 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 329 3 3 7 2.2 CCOC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL3770106 137691 6 None -63 8 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 329 3 3 7 2.2 CCOC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
12 1524 14 None -208 7 Human 5.3 pKi = 5.3 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm990550b
6918513 1524 14 None -208 7 Human 5.3 pKi = 5.3 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm990550b
CHEMBL267615 1524 14 None -208 7 Human 5.3 pKi = 5.3 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm990550b
44456246 12723 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 161 0 2 3 1.0 Cc1cccc2c1N=C(N)NC2 10.1016/j.bmcl.2007.10.080
CHEMBL1188440 12723 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 161 0 2 3 1.0 Cc1cccc2c1N=C(N)NC2 10.1016/j.bmcl.2007.10.080
CHEMBL536335 12723 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 161 0 2 3 1.0 Cc1cccc2c1N=C(N)NC2 10.1016/j.bmcl.2007.10.080
44456400 12725 0 None -2 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL1188501 12725 0 None -2 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL2436555 12725 0 None -2 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL536539 12725 0 None -2 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
136118660 75903 0 None -3 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3cc(Br)ccc23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058428 75903 0 None -3 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3cc(Br)ccc23)N1C 10.1016/j.bmc.2013.09.011
145963830 163571 0 None -46 7 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 335 4 2 4 4.0 Oc1ccccc1C1=NC(Cc2c[nH]cn2)C(c2ccccc2)S1 10.1021/acs.jnatprod.7b00317
CHEMBL4209942 163571 0 None -46 7 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 335 4 2 4 4.0 Oc1ccccc1C1=NC(Cc2c[nH]cn2)C(c2ccccc2)S1 10.1021/acs.jnatprod.7b00317
136152976 166910 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 243 1 2 3 2.5 CC1NC(NCC(F)(F)F)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
CHEMBL429925 166910 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 243 1 2 3 2.5 CC1NC(NCC(F)(F)F)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
145986752 166723 0 None -12 17 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells by radioligand binding assay
ChEMBL 562 10 1 5 7.3 COc1ccc(N(CCCCN2CCC(O)(c3ccc(Cl)c(C(F)(F)F)c3)CC2)c2ccc(OC)cc2)cc1 10.1016/j.bmcl.2018.10.036
CHEMBL4293307 166723 0 None -12 17 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells by radioligand binding assay
ChEMBL 562 10 1 5 7.3 COc1ccc(N(CCCCN2CCC(O)(c3ccc(Cl)c(C(F)(F)F)c3)CC2)c2ccc(OC)cc2)cc1 10.1016/j.bmcl.2018.10.036
122483281 137580 0 None 6 8 Human 8.3 pKi = 8.3 Binding
Binding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 441 7 0 5 5.4 COc1ccccc1N1CCN(CCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
CHEMBL3763779 137580 0 None 6 8 Human 8.3 pKi = 8.3 Binding
Binding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 441 7 0 5 5.4 COc1ccccc1N1CCN(CCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
CHEMBL3765873 137580 0 None 6 8 Human 8.3 pKi = 8.3 Binding
Binding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 441 7 0 5 5.4 COc1ccccc1N1CCN(CCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
16006492 97020 7 None 3 6 Human 8.3 pKi = 8.3 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 195 0 2 3 2.0 CC1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL270177 97020 7 None 3 6 Human 8.3 pKi = 8.3 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 195 0 2 3 2.0 CC1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
44397364 122644 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 518 13 1 4 5.7 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cn2)cc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL361256 122644 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 518 13 1 4 5.7 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cn2)cc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
16006492 97020 7 None 3 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 195 0 2 3 2.0 CC1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.080
CHEMBL270177 97020 7 None 3 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 195 0 2 3 2.0 CC1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.080
16006492 97020 7 None 3 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 195 0 2 3 2.0 CC1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.080
CHEMBL270177 97020 7 None 3 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 195 0 2 3 2.0 CC1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.080
50923582 124636 1 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 345 2 2 3 2.1 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3c(F)cncc3F)c2c1 nan
CHEMBL3644531 124636 1 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 345 2 2 3 2.1 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3c(F)cncc3F)c2c1 nan
135458410 166636 0 None 3 6 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 293 2 2 3 3.5 CC1NC(NCC(F)F)=Nc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL429136 166636 0 None 3 6 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 293 2 2 3 3.5 CC1NC(NCC(F)F)=Nc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2007.10.078
11191906 11662 0 None 6 12 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 537 12 1 3 7.3 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
CHEMBL1181665 11662 0 None 6 12 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 537 12 1 3 7.3 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
CHEMBL187928 11662 0 None 6 12 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 537 12 1 3 7.3 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
4713248 206170 3 None -5 3 Human 5.3 pKi = 5.3 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 281 5 2 3 1.2 CNS(=O)(=O)c1ccc2[nH]cc(CCN(C)C)c2c1 10.1021/jm030030n
CHEMBL96729 206170 3 None -5 3 Human 5.3 pKi = 5.3 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 281 5 2 3 1.2 CNS(=O)(=O)c1ccc2[nH]cc(CCN(C)C)c2c1 10.1021/jm030030n
4713248 206170 3 None -5 3 Human 5.3 pKi = 5.3 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 281 5 2 3 1.2 CNS(=O)(=O)c1ccc2[nH]cc(CCN(C)C)c2c1 10.1021/jm030030n
CHEMBL96729 206170 3 None -5 3 Human 5.3 pKi = 5.3 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 281 5 2 3 1.2 CNS(=O)(=O)c1ccc2[nH]cc(CCN(C)C)c2c1 10.1021/jm030030n
44397427 11651 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 580 14 1 3 8.0 COc1cccc(CCN(Cc2ccc(-c3ccc(CNCCc4ccccc4)cc3)cc2)C(=O)/C=C/c2ccccc2)c1 10.1016/j.bmcl.2005.06.024
CHEMBL1181625 11651 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 580 14 1 3 8.0 COc1cccc(CCN(Cc2ccc(-c3ccc(CNCCc4ccccc4)cc3)cc2)C(=O)/C=C/c2ccccc2)c1 10.1016/j.bmcl.2005.06.024
CHEMBL185996 11651 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 580 14 1 3 8.0 COc1cccc(CCN(Cc2ccc(-c3ccc(CNCCc4ccccc4)cc3)cc2)C(=O)/C=C/c2ccccc2)c1 10.1016/j.bmcl.2005.06.024
44456400 12725 0 None -2 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL1188501 12725 0 None -2 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL2436555 12725 0 None -2 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL536539 12725 0 None -2 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
136152972 94780 0 None -2 4 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 293 2 2 3 3.5 C[C@H]1NC(NCC(F)F)=Nc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL256047 94780 0 None -2 4 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 293 2 2 3 3.5 C[C@H]1NC(NCC(F)F)=Nc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2007.10.078
44355128 117978 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 219 5 1 2 2.8 CCN(CC)C[C@H]1C[C@@H]1c1ccccc1O 10.1016/0960-894X(96)00045-5
CHEMBL341373 117978 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 219 5 1 2 2.8 CCN(CC)C[C@H]1C[C@@H]1c1ccccc1O 10.1016/0960-894X(96)00045-5
136118658 75901 0 None -5 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058426 75901 0 None -5 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1C 10.1016/j.bmc.2013.09.011
379995 116351 2 None - 1 Mouse 6.3 pKi = 6.3 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 336 5 1 2 4.3 O=C(CCCN1CCc2[nH]c3ccccc3c2C1)c1ccc(F)cc1 10.1021/jm030080s
CHEMBL338091 116351 2 None - 1 Mouse 6.3 pKi = 6.3 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 336 5 1 2 4.3 O=C(CCCN1CCc2[nH]c3ccccc3c2C1)c1ccc(F)cc1 10.1021/jm030080s
6918515 2574 33 None -158 6 Human 5.3 pKi = 5.3 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/jm990550b
71 2574 33 None -158 6 Human 5.3 pKi = 5.3 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/jm990550b
CHEMBL7318 2574 33 None -158 6 Human 5.3 pKi = 5.3 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/jm990550b
72550645 113590 0 None -72 8 Human 6.3 pKi = 6.3 Binding
Binding affinity to 5-HT5A (unknown origin)Binding affinity to 5-HT5A (unknown origin)
ChEMBL 505 11 1 4 6.0 COc1ccccc1N1CCN(CCCCCC(=O)NCc2ccccc2-c2ccccc2Cl)CC1 10.1016/j.bmc.2014.07.026
CHEMBL3326993 113590 0 None -72 8 Human 6.3 pKi = 6.3 Binding
Binding affinity to 5-HT5A (unknown origin)Binding affinity to 5-HT5A (unknown origin)
ChEMBL 505 11 1 4 6.0 COc1ccccc1N1CCN(CCCCCC(=O)NCc2ccccc2-c2ccccc2Cl)CC1 10.1016/j.bmc.2014.07.026
18677411 205513 8 None - 1 Mouse 5.3 pKi = 5.3 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 186 0 1 2 1.8 Cn1c2c(c3ccccc31)CNCC2 10.1021/jm030080s
CHEMBL92879 205513 8 None - 1 Mouse 5.3 pKi = 5.3 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 186 0 1 2 1.8 Cn1c2c(c3ccccc31)CNCC2 10.1021/jm030080s
18677411 205513 8 None - 1 Mouse 5.3 pKi = 5.3 Binding
Binding affinity towards murine 5-hydroxytryptamine 5A receptorBinding affinity towards murine 5-hydroxytryptamine 5A receptor
ChEMBL 186 0 1 2 1.8 Cn1c2c(c3ccccc31)CNCC2 10.1021/jm030030n
CHEMBL92879 205513 8 None - 1 Mouse 5.3 pKi = 5.3 Binding
Binding affinity towards murine 5-hydroxytryptamine 5A receptorBinding affinity towards murine 5-hydroxytryptamine 5A receptor
ChEMBL 186 0 1 2 1.8 Cn1c2c(c3ccccc31)CNCC2 10.1021/jm030030n
135474338 188682 0 None -28 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3cc(Br)ccc23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL511879 188682 0 None -28 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3cc(Br)ccc23)C1=O 10.1016/j.bmc.2013.09.011
10382508 206129 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 338 5 0 3 4.1 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030030n
CHEMBL96504 206129 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 338 5 0 3 4.1 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030030n
10382508 206129 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 338 5 0 3 4.1 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL96504 206129 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 338 5 0 3 4.1 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030080s
11045379 19175 0 None -4 2 Mouse 6.3 pKi = 6.3 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 318 5 1 2 4.2 O=C(CCCN1CCc2c([nH]c3ccccc23)C1)c1ccccc1 10.1021/jm030080s
CHEMBL129163 19175 0 None -4 2 Mouse 6.3 pKi = 6.3 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 318 5 1 2 4.2 O=C(CCCN1CCc2c([nH]c3ccccc23)C1)c1ccccc1 10.1021/jm030080s
44456443 12882 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 165 0 2 3 0.9 NC1=Nc2cccc(F)c2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL1189631 12882 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 165 0 2 3 0.9 NC1=Nc2cccc(F)c2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL539103 12882 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 165 0 2 3 0.9 NC1=Nc2cccc(F)c2CN1 10.1016/j.bmcl.2007.10.080
16573 177045 30 None -28 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in Flp-In CHO cell membranes by radioligand binding assayDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in Flp-In CHO cell membranes by radioligand binding assay
ChEMBL 341 3 1 5 3.2 COc1cc2c(cc1O)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/np500893h
CHEMBL464099 177045 30 None -28 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in Flp-In CHO cell membranes by radioligand binding assayDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in Flp-In CHO cell membranes by radioligand binding assay
ChEMBL 341 3 1 5 3.2 COc1cc2c(cc1O)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/np500893h
CHEMBL5085238 213185 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 1 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 1 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None O=S1(=O)CC[C@@H](CNCc2cccc3cccnc23)C1 10.1021/acs.jmedchem.1c02031
44355424 21826 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 247 7 1 2 3.6 CCCN(CCC)C[C@@H]1C[C@@H]1c1cccc(O)c1 10.1016/0960-894X(96)00045-5
CHEMBL132123 21826 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 247 7 1 2 3.6 CCCN(CCC)C[C@@H]1C[C@@H]1c1cccc(O)c1 10.1016/0960-894X(96)00045-5
71462776 82550 0 None -4786 7 Human 5.2 pKi = 5.2 Binding
Binding affinity to human 5HT5A by Cerep protocol based assayBinding affinity to human 5HT5A by Cerep protocol based assay
ChEMBL 460 5 0 3 5.5 CCCN1CCC(COc2nc3c(I)cccc3c3ccccc23)CC1 10.1021/jm300943r
CHEMBL2181169 82550 0 None -4786 7 Human 5.2 pKi = 5.2 Binding
Binding affinity to human 5HT5A by Cerep protocol based assayBinding affinity to human 5HT5A by Cerep protocol based assay
ChEMBL 460 5 0 3 5.5 CCCN1CCC(COc2nc3c(I)cccc3c3ccccc23)CC1 10.1021/jm300943r
44351180 17900 0 None -2 3 Mouse 6.2 pKi = 6.2 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 372 5 0 3 4.8 Cn1c2c(c3cccc(Cl)c31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL126737 17900 0 None -2 3 Mouse 6.2 pKi = 6.2 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 372 5 0 3 4.8 Cn1c2c(c3cccc(Cl)c31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030080s
118464425 137781 0 None -15 9 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 357 3 2 7 2.8 CCOC(=O)c1cccc(NC2=NC(N(C)C)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL3770981 137781 0 None -15 9 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 357 3 2 7 2.8 CCOC(=O)c1cccc(NC2=NC(N(C)C)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
50923721 124643 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 361 2 2 3 2.6 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3ncc(F)cc3Cl)c2c1 nan
CHEMBL3644538 124643 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 361 2 2 3 2.6 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3ncc(F)cc3Cl)c2c1 nan
135458394 97242 5 None 2 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 243 0 2 3 2.9 CNC1=Nc2ccc(Cl)c(Cl)c2C(C)N1 10.1016/j.bmcl.2007.10.080
CHEMBL271298 97242 5 None 2 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 243 0 2 3 2.9 CNC1=Nc2ccc(Cl)c(Cl)c2C(C)N1 10.1016/j.bmcl.2007.10.080
16006606 157119 3 None 1 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 191 1 2 4 1.3 COc1cccc2c1N=C(N)NC2C 10.1016/j.bmcl.2007.10.080
CHEMBL408152 157119 3 None 1 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 191 1 2 4 1.3 COc1cccc2c1N=C(N)NC2C 10.1016/j.bmcl.2007.10.080
135458393 155056 4 None 2 5 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 259 2 2 3 2.8 CC1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL404511 155056 4 None 2 5 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 259 2 2 3 2.8 CC1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
11168182 3478 18 None 50 13 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 10.1016/j.bmcl.2005.06.024
264 3478 18 None 50 13 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 10.1016/j.bmcl.2005.06.024
CHEMBL1181770 3478 18 None 50 13 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 10.1016/j.bmcl.2005.06.024
16006605 97543 3 None -2 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 229 0 2 3 2.6 CC1NC(N)=Nc2c(Cl)ccc(Cl)c21 10.1016/j.bmcl.2007.10.080
CHEMBL272781 97543 3 None -2 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 229 0 2 3 2.6 CC1NC(N)=Nc2c(Cl)ccc(Cl)c21 10.1016/j.bmcl.2007.10.080
91819721 126273 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 382 1 2 1 3.5 NC(N)=NC(=O)N1Cc2c(-c3ccc(F)cc3F)ccc(Cl)c2C(F)C1 nan
CHEMBL3654202 126273 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 382 1 2 1 3.5 NC(N)=NC(=O)N1Cc2c(-c3ccc(F)cc3F)ccc(Cl)c2C(F)C1 nan
CHEMBL5093969 213686 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 32 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 32 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None Clc1ccc(CNCC[C@@H]2CCOC2)c2ncccc12 10.1021/acs.jmedchem.1c02031
CHEMBL5094012 213688 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 32 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 32 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None O=C1C[C@H](CNCc2ccc(Cl)c3cccnc23)CN1C1CC1 10.1021/acs.jmedchem.1c02031
136152964 193270 0 None -2 8 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 259 2 2 3 2.8 C[C@@H]1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL541993 193270 0 None -2 8 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 259 2 2 3 2.8 C[C@@H]1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
60150899 126272 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 349 1 2 2 1.9 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3ncc(F)cc3F)c2C1 nan
CHEMBL3654201 126272 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 349 1 2 2 1.9 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3ncc(F)cc3F)c2C1 nan
22980542 17847 0 None -3 2 Mouse 6.2 pKi = 6.2 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 306 5 1 2 4.0 c1ccc(OCCCN2CCc3[nH]c4ccccc4c3C2)cc1 10.1021/jm030080s
CHEMBL126438 17847 0 None -3 2 Mouse 6.2 pKi = 6.2 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 306 5 1 2 4.0 c1ccc(OCCCN2CCc3[nH]c4ccccc4c3C2)cc1 10.1021/jm030080s
73353884 91890 0 None -5 8 Human 5.2 pKi = 5.2 Binding
Inhibition of 5-HT5A receptor (unknown origin) by PDSP assayInhibition of 5-HT5A receptor (unknown origin) by PDSP assay
ChEMBL 295 3 1 3 2.7 c1cc2c(cc1CN[C@H]1C3C4CC5C6C4CC3C6C51)OCO2 10.1016/j.bmc.2013.07.045
CHEMBL2429890 91890 0 None -5 8 Human 5.2 pKi = 5.2 Binding
Inhibition of 5-HT5A receptor (unknown origin) by PDSP assayInhibition of 5-HT5A receptor (unknown origin) by PDSP assay
ChEMBL 295 3 1 3 2.7 c1cc2c(cc1CN[C@H]1C3C4CC5C6C4CC3C6C51)OCO2 10.1016/j.bmc.2013.07.045
11726973 17917 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 320 5 0 3 4.0 Cn1c2c(c3ccccc31)CCN(CCCOc1ccccc1)C2 10.1021/jm030080s
CHEMBL126823 17917 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 320 5 0 3 4.0 Cn1c2c(c3ccccc31)CCN(CCCOc1ccccc1)C2 10.1021/jm030080s
146025727 171119 0 None -229 27 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT5A receptor stably expressed in Flp-In CHO cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT5A receptor stably expressed in Flp-In CHO cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4466483 171119 0 None -229 27 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT5A receptor stably expressed in Flp-In CHO cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT5A receptor stably expressed in Flp-In CHO cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
44327952 206304 0 None 1 5 Mouse 7.2 pKi = 7.2 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 367 5 3 3 2.6 CC[C@@](C)(CO)CNC(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1 10.1021/jm030030n
CHEMBL97518 206304 0 None 1 5 Mouse 7.2 pKi = 7.2 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 367 5 3 3 2.6 CC[C@@](C)(CO)CNC(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1 10.1021/jm030030n
3233 3456 40 None -10 12 Human 7.2 pKi = 7.2 Binding
Binding affinity towards 5-hydroxytryptamine 5A receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.Binding affinity towards 5-hydroxytryptamine 5A receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
3247 3456 40 None -10 12 Human 7.2 pKi = 7.2 Binding
Binding affinity towards 5-hydroxytryptamine 5A receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.Binding affinity towards 5-hydroxytryptamine 5A receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
6604889 3456 40 None -10 12 Human 7.2 pKi = 7.2 Binding
Binding affinity towards 5-hydroxytryptamine 5A receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.Binding affinity towards 5-hydroxytryptamine 5A receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
CHEMBL282199 3456 40 None -10 12 Human 7.2 pKi = 7.2 Binding
Binding affinity towards 5-hydroxytryptamine 5A receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.Binding affinity towards 5-hydroxytryptamine 5A receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
DB13988 3456 40 None -10 12 Human 7.2 pKi = 7.2 Binding
Binding affinity towards 5-hydroxytryptamine 5A receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.Binding affinity towards 5-hydroxytryptamine 5A receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
22857296 28937 0 None -123 4 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 389 4 2 3 4.1 CN1C[C@H](CNC(=O)OCc2ccccc2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1021/jm030030n
CHEMBL13816 28937 0 None -123 4 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 389 4 2 3 4.1 CN1C[C@H](CNC(=O)OCc2ccccc2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1021/jm030030n
44397433 12159 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 491 12 1 3 5.9 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL1184710 12159 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 491 12 1 3 5.9 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL365084 12159 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 491 12 1 3 5.9 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)c1ccccc1 10.1016/j.bmcl.2005.06.024
2470 3596 46 None -77624 59 Human 4.2 pKi = 4.2 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
3300 3596 46 None -77624 59 Human 4.2 pKi = 4.2 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
5265 3596 46 None -77624 59 Human 4.2 pKi = 4.2 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
99 3596 46 None -77624 59 Human 4.2 pKi = 4.2 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
CHEMBL267930 3596 46 None -77624 59 Human 4.2 pKi = 4.2 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
44397429 11653 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 491 12 1 4 5.7 COCCNCc1ccc(-c2ccc(CN(Cc3cccnc3)C(=O)/C=C/c3ccccc3)cc2)cc1 10.1016/j.bmcl.2005.06.024
CHEMBL1181634 11653 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 491 12 1 4 5.7 COCCNCc1ccc(-c2ccc(CN(Cc3cccnc3)C(=O)/C=C/c3ccccc3)cc2)cc1 10.1016/j.bmcl.2005.06.024
CHEMBL186450 11653 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 491 12 1 4 5.7 COCCNCc1ccc(-c2ccc(CN(Cc3cccnc3)C(=O)/C=C/c3ccccc3)cc2)cc1 10.1016/j.bmcl.2005.06.024
44456253 12728 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 165 0 2 3 0.9 NC1=Nc2cc(F)ccc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL1188517 12728 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 165 0 2 3 0.9 NC1=Nc2cc(F)ccc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL536562 12728 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 165 0 2 3 0.9 NC1=Nc2cc(F)ccc2CN1 10.1016/j.bmcl.2007.10.080
3233 3456 40 None -10 12 Human 7.2 pKi = 7.2 Binding
Binding affinity towards 5-hydroxytryptamine 5 receptorBinding affinity towards 5-hydroxytryptamine 5 receptor
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm030030n
3247 3456 40 None -10 12 Human 7.2 pKi = 7.2 Binding
Binding affinity towards 5-hydroxytryptamine 5 receptorBinding affinity towards 5-hydroxytryptamine 5 receptor
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm030030n
6604889 3456 40 None -10 12 Human 7.2 pKi = 7.2 Binding
Binding affinity towards 5-hydroxytryptamine 5 receptorBinding affinity towards 5-hydroxytryptamine 5 receptor
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm030030n
CHEMBL282199 3456 40 None -10 12 Human 7.2 pKi = 7.2 Binding
Binding affinity towards 5-hydroxytryptamine 5 receptorBinding affinity towards 5-hydroxytryptamine 5 receptor
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm030030n
DB13988 3456 40 None -10 12 Human 7.2 pKi = 7.2 Binding
Binding affinity towards 5-hydroxytryptamine 5 receptorBinding affinity towards 5-hydroxytryptamine 5 receptor
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm030030n
44350898 17797 0 None -1 2 Mouse 6.2 pKi = 6.2 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 370 5 0 3 5.2 Cn1c2c(c3ccccc31)CN(CCCOc1cccc3ccccc13)CC2 10.1021/jm030080s
CHEMBL126188 17797 0 None -1 2 Mouse 6.2 pKi = 6.2 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 370 5 0 3 5.2 Cn1c2c(c3ccccc31)CN(CCCOc1cccc3ccccc13)CC2 10.1021/jm030080s
44350897 117570 0 None -2 2 Mouse 6.2 pKi = 6.2 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 370 5 0 3 5.2 Cn1c2c(c3ccccc31)CN(CCCOc1ccc3ccccc3c1)CC2 10.1021/jm030080s
CHEMBL340511 117570 0 None -2 2 Mouse 6.2 pKi = 6.2 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 370 5 0 3 5.2 Cn1c2c(c3ccccc31)CN(CCCOc1ccc3ccccc3c1)CC2 10.1021/jm030080s
12628906 94159 22 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 147 0 2 3 0.7 NC1=Nc2ccccc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL25212 94159 22 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 147 0 2 3 0.7 NC1=Nc2ccccc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL557381 94159 22 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 147 0 2 3 0.7 NC1=Nc2ccccc2CN1 10.1016/j.bmcl.2007.10.080
135508617 136016503 10530 0 None -12 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 332 1 2 2 2.6 CN1C(=N)N(C)/C(=C/c2c[nH]c3ccc(Br)cc23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL1170237 10530 0 None -12 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 332 1 2 2 2.6 CN1C(=N)N(C)/C(=C/c2c[nH]c3ccc(Br)cc23)C1=O 10.1016/j.bmc.2013.09.011
145977799 163091 0 None -9 6 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 257 3 1 3 2.9 C[C@@H]1SC(c2ccccc2)=N[C@@H]1Cc1c[nH]cn1 10.1021/acs.jnatprod.7b00317
CHEMBL4204036 163091 0 None -9 6 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 257 3 1 3 2.9 C[C@@H]1SC(c2ccccc2)=N[C@@H]1Cc1c[nH]cn1 10.1021/acs.jnatprod.7b00317
44582675 189109 0 None -114 15 Human 5.2 pKi = 5.2 Binding
Inhibition of human cloned 5HT5A receptor by competitive binding experimentInhibition of human cloned 5HT5A receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1[C@H](O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL515472 189109 0 None -114 15 Human 5.2 pKi = 5.2 Binding
Inhibition of human cloned 5HT5A receptor by competitive binding experimentInhibition of human cloned 5HT5A receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1[C@H](O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
117209965 184665 1 None -29 6 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
ChEMBL 262 2 2 3 2.1 Clc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4858338 184665 1 None -29 6 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
ChEMBL 262 2 2 3 2.1 Clc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
4376990 192407 4 None -27 11 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constant
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5207529 192407 4 None -27 11 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constant
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5222754 192407 4 None -27 11 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constant
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
136118661 75904 0 None -7 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058429 75904 0 None -7 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1C 10.1016/j.bmc.2013.09.011
50923583 124637 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 356 3 2 3 2.6 COc1cccc(F)c1-c1ncc(F)c2ccc(C(=O)N=C(N)N)cc12 nan
CHEMBL3644532 124637 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 356 3 2 3 2.6 COc1cccc(F)c1-c1ncc(F)c2ccc(C(=O)N=C(N)N)cc12 nan
CHEMBL5094234 213797 0 None -331 8 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5096019 213797 0 None -331 8 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5091270 213527 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 1 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 1 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None O=S1(=O)CCC[C@@H](CNCc2cccc3cccnc23)C1 10.1021/acs.jmedchem.1c02031
44355201 114719 0 None - 1 Rat 6.1 pKi = 6.1 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 247 7 0 2 3.7 CCCN(CCC)[C@@H]1C[C@@H]1c1cccc(OC)c1 10.1016/0960-894X(96)00045-5
CHEMBL334553 114719 0 None - 1 Rat 6.1 pKi = 6.1 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 247 7 0 2 3.7 CCCN(CCC)[C@@H]1C[C@@H]1c1cccc(OC)c1 10.1016/0960-894X(96)00045-5
130442572 171342 0 None -158 24 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT5A receptor stably expressed in Flp-In CHO cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT5A receptor stably expressed in Flp-In CHO cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4469848 171342 0 None -158 24 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT5A receptor stably expressed in Flp-In CHO cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT5A receptor stably expressed in Flp-In CHO cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
21509921 103979 0 None -74 24 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104091 103979 0 None -74 24 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
44351047 17898 0 None - 1 Mouse 7.1 pKi = 7.1 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 324 5 1 2 4.1 Fc1ccc(OCCCN2CCc3[nH]c4ccccc4c3C2)cc1 10.1021/jm030080s
CHEMBL126724 17898 0 None - 1 Mouse 7.1 pKi = 7.1 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 324 5 1 2 4.1 Fc1ccc(OCCCN2CCc3[nH]c4ccccc4c3C2)cc1 10.1021/jm030080s
44351139 18656 0 None 1 3 Mouse 7.1 pKi = 7.1 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 334 6 0 3 4.5 CCn1c2c(c3ccccc31)CN(CCCOc1ccccc1)CC2 10.1021/jm030080s
CHEMBL128099 18656 0 None 1 3 Mouse 7.1 pKi = 7.1 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 334 6 0 3 4.5 CCn1c2c(c3ccccc31)CN(CCCOc1ccccc1)CC2 10.1021/jm030080s
21509921 103979 0 None -74 24 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104091 103979 0 None -74 24 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
73355415 92101 0 None -38 13 Human 5.1 pKi = 5.1 Binding
Inhibition of 5-HT5A receptor (unknown origin) by PDSP assayInhibition of 5-HT5A receptor (unknown origin) by PDSP assay
ChEMBL 277 3 1 1 2.1 C1C2C3CC4C2C2C1C3[C@H](NCC13C5C6C7C5C1C7C63)C42 10.1016/j.bmc.2013.07.045
CHEMBL2432039 92101 0 None -38 13 Human 5.1 pKi = 5.1 Binding
Inhibition of 5-HT5A receptor (unknown origin) by PDSP assayInhibition of 5-HT5A receptor (unknown origin) by PDSP assay
ChEMBL 277 3 1 1 2.1 C1C2C3CC4C2C2C1C3[C@H](NCC13C5C6C7C5C1C7C63)C42 10.1016/j.bmc.2013.07.045
44355164 22839 0 None - 1 Rat 6.1 pKi = 6.1 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 247 7 1 2 3.6 CCCN(CCC)C[C@H]1C[C@@H]1c1ccccc1O 10.1016/0960-894X(96)00045-5
CHEMBL133020 22839 0 None - 1 Rat 6.1 pKi = 6.1 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 247 7 1 2 3.6 CCCN(CCC)C[C@H]1C[C@@H]1c1ccccc1O 10.1016/0960-894X(96)00045-5
2737389 187003 23 None -53 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysis
ChEMBL 238 2 1 2 2.8 c1ccc(-c2ccccc2N2CCNCC2)cc1 10.1039/C8MD00313K
CHEMBL494675 187003 23 None -53 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysis
ChEMBL 238 2 1 2 2.8 c1ccc(-c2ccccc2N2CCNCC2)cc1 10.1039/C8MD00313K
71459604 83379 0 None -13 14 Human 5.1 pKi = 5.1 Binding
Binding affinity to 5-HT5A receptorBinding affinity to 5-HT5A receptor
ChEMBL 309 4 1 3 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1 10.1016/j.bmcl.2012.08.046
CHEMBL2205811 83379 0 None -13 14 Human 5.1 pKi = 5.1 Binding
Binding affinity to 5-HT5A receptorBinding affinity to 5-HT5A receptor
ChEMBL 309 4 1 3 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1 10.1016/j.bmcl.2012.08.046
136118620 75899 0 None -24 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 332 1 2 2 2.6 CN1C(=N)N(C)/C(=C/c2c[nH]c3cccc(Br)c23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL2058419 75899 0 None -24 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 332 1 2 2 2.6 CN1C(=N)N(C)/C(=C/c2c[nH]c3cccc(Br)c23)C1=O 10.1016/j.bmc.2013.09.011
44397669 11682 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 531 13 1 3 6.4 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)C1CC1c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL1181776 11682 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 531 13 1 3 6.4 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)C1CC1c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL191583 11682 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 531 13 1 3 6.4 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)C1CC1c1ccccc1 10.1016/j.bmcl.2005.06.024
44397362 12153 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 527 15 1 4 6.4 CN(C)CCN(Cc1ccc(-c2ccc(CNCCOc3ccccc3)cc2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
CHEMBL1184673 12153 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 527 15 1 4 6.4 CN(C)CCN(Cc1ccc(-c2ccc(CNCCOc3ccccc3)cc2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
CHEMBL363678 12153 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 527 15 1 4 6.4 CN(C)CCN(Cc1ccc(-c2ccc(CNCCOc3ccccc3)cc2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
44455983 97146 1 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 189 2 2 3 2.1 CCCC1NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.080
CHEMBL270840 97146 1 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 189 2 2 3 2.1 CCCC1NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.080
44456400 12725 0 None -2 10 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL1188501 12725 0 None -2 10 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL2436555 12725 0 None -2 10 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL536539 12725 0 None -2 10 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2007.10.080
5 139 66 None -323 54 Human 7.1 pKi = 7.1 Binding
Binding affinity to human 5-HT5a receptor by radioligand displacement assayBinding affinity to human 5-HT5a receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
5202 139 66 None -323 54 Human 7.1 pKi = 7.1 Binding
Binding affinity to human 5-HT5a receptor by radioligand displacement assayBinding affinity to human 5-HT5a receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
CHEMBL39 139 66 None -323 54 Human 7.1 pKi = 7.1 Binding
Binding affinity to human 5-HT5a receptor by radioligand displacement assayBinding affinity to human 5-HT5a receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
DB08839 139 66 None -323 54 Human 7.1 pKi = 7.1 Binding
Binding affinity to human 5-HT5a receptor by radioligand displacement assayBinding affinity to human 5-HT5a receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
145967795 164271 0 None -5 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 213 2 1 4 2.0 C[C@@H]1SC(c2ccsc2)=N[C@H]1CO 10.1021/acs.jnatprod.7b00317
CHEMBL4218679 164271 0 None -5 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 213 2 1 4 2.0 C[C@@H]1SC(c2ccsc2)=N[C@H]1CO 10.1021/acs.jnatprod.7b00317
44455973 97019 7 None 1 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 209 1 2 3 2.3 CCC1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.080
CHEMBL270176 97019 7 None 1 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 209 1 2 3 2.3 CCC1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.080
160510 100658 36 None -3 4 Human 6.1 pKi = 6.1 Binding
Binding affinity towards 5-HT5A receptorBinding affinity towards 5-HT5A receptor
ChEMBL 184 0 1 1 2.5 CC1=NCCc2c1[nH]c1ccccc21 10.1016/j.bmcl.2003.09.027
CHEMBL1506260 100658 36 None -3 4 Human 6.1 pKi = 6.1 Binding
Binding affinity towards 5-HT5A receptorBinding affinity towards 5-HT5A receptor
ChEMBL 184 0 1 1 2.5 CC1=NCCc2c1[nH]c1ccccc21 10.1016/j.bmcl.2003.09.027
CHEMBL295234 100658 36 None -3 4 Human 6.1 pKi = 6.1 Binding
Binding affinity towards 5-HT5A receptorBinding affinity towards 5-HT5A receptor
ChEMBL 184 0 1 1 2.5 CC1=NCCc2c1[nH]c1ccccc21 10.1016/j.bmcl.2003.09.027
49783209 17427 0 None -14791 27 Human 5.1 pKi = 5.1 Binding
Binding affinity to human 5-HT5A receptorBinding affinity to human 5-HT5A receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258223 17427 0 None -14791 27 Human 5.1 pKi = 5.1 Binding
Binding affinity to human 5-HT5A receptorBinding affinity to human 5-HT5A receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
155551348 173385 0 None -1 2 Human 5.1 pKi = 5.1 Binding
Inhibition of 5HT5A (unknown origin)Inhibition of 5HT5A (unknown origin)
ChEMBL 487 7 1 9 3.7 CCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@@H]1OC(C)(C)O[C@@H]12 10.1021/acs.jmedchem.8b01662
CHEMBL4541409 173385 0 None -1 2 Human 5.1 pKi = 5.1 Binding
Inhibition of 5HT5A (unknown origin)Inhibition of 5HT5A (unknown origin)
ChEMBL 487 7 1 9 3.7 CCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@@H]1OC(C)(C)O[C@@H]12 10.1021/acs.jmedchem.8b01662
136152977 97436 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 225 2 2 3 2.2 CC1NC(NCC(F)F)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
CHEMBL272355 97436 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 225 2 2 3 2.2 CC1NC(NCC(F)F)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
1355 1980 82 None -549 15 Mouse 5.1 pKi = 5.1 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [3H]LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [3H]LSD as radioligand
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm030030n
142 1980 82 None -549 15 Mouse 5.1 pKi = 5.1 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [3H]LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [3H]LSD as radioligand
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm030030n
CHEMBL478 1980 82 None -549 15 Mouse 5.1 pKi = 5.1 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [3H]LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [3H]LSD as radioligand
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm030030n
DB12110 1980 82 None -549 15 Mouse 5.1 pKi = 5.1 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [3H]LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [3H]LSD as radioligand
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm030030n
1355 1980 82 None -549 15 Mouse 5.1 pKi = 5.1 Binding
Binding affinity towards murine 5-hydroxytryptamine 5A receptorBinding affinity towards murine 5-hydroxytryptamine 5A receptor
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm030030n
142 1980 82 None -549 15 Mouse 5.1 pKi = 5.1 Binding
Binding affinity towards murine 5-hydroxytryptamine 5A receptorBinding affinity towards murine 5-hydroxytryptamine 5A receptor
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm030030n
CHEMBL478 1980 82 None -549 15 Mouse 5.1 pKi = 5.1 Binding
Binding affinity towards murine 5-hydroxytryptamine 5A receptorBinding affinity towards murine 5-hydroxytryptamine 5A receptor
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm030030n
DB12110 1980 82 None -549 15 Mouse 5.1 pKi = 5.1 Binding
Binding affinity towards murine 5-hydroxytryptamine 5A receptorBinding affinity towards murine 5-hydroxytryptamine 5A receptor
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm030030n
44351103 20109 0 None -9 2 Mouse 6.1 pKi = 6.1 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 396 7 0 3 5.5 c1ccc(Cn2c3c(c4ccccc42)CN(CCCOc2ccccc2)CC3)cc1 10.1021/jm030080s
CHEMBL130586 20109 0 None -9 2 Mouse 6.1 pKi = 6.1 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 396 7 0 3 5.5 c1ccc(Cn2c3c(c4ccccc42)CN(CCCOc2ccccc2)CC3)cc1 10.1021/jm030080s
132060720 161939 0 None -2 9 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting method
ChEMBL 315 4 0 2 4.9 COc1cccc(-c2ccc3c(c2)CN(Cc2ccccc2)C3)c1 10.1016/j.ejmech.2018.02.024
CHEMBL4167315 161939 0 None -2 9 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting method
ChEMBL 315 4 0 2 4.9 COc1cccc(-c2ccc3c(c2)CN(Cc2ccccc2)C3)c1 10.1016/j.ejmech.2018.02.024
44456398 13837 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 161 0 2 3 1.0 Cc1ccc2c(c1)CNC(N)=N2 10.1016/j.bmcl.2007.10.080
CHEMBL1196644 13837 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 161 0 2 3 1.0 Cc1ccc2c(c1)CNC(N)=N2 10.1016/j.bmcl.2007.10.080
CHEMBL557746 13837 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 161 0 2 3 1.0 Cc1ccc2c(c1)CNC(N)=N2 10.1016/j.bmcl.2007.10.080
135464118 92628 0 None -2 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3ccc(Br)cc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2442272 92628 0 None -2 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3ccc(Br)cc23)N1 10.1016/j.bmc.2013.09.011
44456244 97536 1 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 181 0 2 3 1.4 NC1=Nc2c(Cl)cccc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL272752 97536 1 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 181 0 2 3 1.4 NC1=Nc2c(Cl)cccc2CN1 10.1016/j.bmcl.2007.10.080
53325242 56775 0 None -4 17 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells by radioligand binding assay
ChEMBL 537 8 1 2 7.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL1644978 56775 0 None -4 17 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells by radioligand binding assay
ChEMBL 537 8 1 2 7.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
1621 2396 16 None -27 44 Human 8.1 pKi = 8.1 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
17 2396 16 None -27 44 Human 8.1 pKi = 8.1 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
5761 2396 16 None -27 44 Human 8.1 pKi = 8.1 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
CHEMBL263881 2396 16 None -27 44 Human 8.1 pKi = 8.1 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
DB04829 2396 16 None -27 44 Human 8.1 pKi = 8.1 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
10405482 18950 0 None 11 2 Mouse 7.1 pKi = 7.1 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 348 6 0 3 4.6 COc1ccc(CCCCN2CCc3c(c4ccccc4n3C)C2)cc1 10.1021/jm030080s
CHEMBL128945 18950 0 None 11 2 Mouse 7.1 pKi = 7.1 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 348 6 0 3 4.6 COc1ccc(CCCCN2CCc3c(c4ccccc4n3C)C2)cc1 10.1021/jm030080s
CHEMBL5091373 213791 0 None -436 9 Human 6.0 pKi = 6.0 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5095981 213791 0 None -436 9 Human 6.0 pKi = 6.0 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
44456286 12737 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 165 0 2 3 0.9 NC1=Nc2ccc(F)cc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL1188596 12737 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 165 0 2 3 0.9 NC1=Nc2ccc(F)cc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL536790 12737 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 165 0 2 3 0.9 NC1=Nc2ccc(F)cc2CN1 10.1016/j.bmcl.2007.10.080
136118659 75902 0 None -5 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3ccc(Br)cc23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058427 75902 0 None -5 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3ccc(Br)cc23)N1C 10.1016/j.bmc.2013.09.011
10881882 18008 0 None -3 2 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 324 4 0 3 3.8 Cn1c2c(c3ccccc31)CN(CCOc1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL126994 18008 0 None -3 2 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 324 4 0 3 3.8 Cn1c2c(c3ccccc31)CN(CCOc1ccc(F)cc1)CC2 10.1021/jm030080s
122483292 137583 0 None -33 7 Human 6.0 pKi = 6.0 Binding
Binding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 441 7 1 5 5.5 O=C(CCCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
CHEMBL3764335 137583 0 None -33 7 Human 6.0 pKi = 6.0 Binding
Binding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 441 7 1 5 5.5 O=C(CCCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
CHEMBL3765876 137583 0 None -33 7 Human 6.0 pKi = 6.0 Binding
Binding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 441 7 1 5 5.5 O=C(CCCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
44351499 118048 0 None - 1 Mouse 7.0 pKi = 7.0 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 336 5 0 2 4.7 Cn1c2c(c3ccccc31)CN(CCCCc1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL341506 118048 0 None - 1 Mouse 7.0 pKi = 7.0 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 336 5 0 2 4.7 Cn1c2c(c3ccccc31)CN(CCCCc1ccc(F)cc1)CC2 10.1021/jm030080s
130442480 174698 0 None -117 24 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-LSD from recombinant human 5HT5A receptor stably expressed in Flp-In CHO cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT5A receptor stably expressed in Flp-In CHO cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
CHEMBL4572614 174698 0 None -117 24 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-LSD from recombinant human 5HT5A receptor stably expressed in Flp-In CHO cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT5A receptor stably expressed in Flp-In CHO cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
136152967 155025 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 261 2 2 5 1.3 CC1NC(NCC2COCCO2)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
CHEMBL404365 155025 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 261 2 2 5 1.3 CC1NC(NCC2COCCO2)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
135433933 176464 1 None -8 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 332 1 2 2 2.6 CN1C(=N)N(C)/C(=C/c2c[nH]c3cc(Br)ccc23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL463249 176464 1 None -8 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 332 1 2 2 2.6 CN1C(=N)N(C)/C(=C/c2c[nH]c3cc(Br)ccc23)C1=O 10.1016/j.bmc.2013.09.011
44456207 13535 6 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 177 1 2 4 0.7 COc1cccc2c1N=C(N)NC2 10.1016/j.bmcl.2007.10.080
CHEMBL1194499 13535 6 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 177 1 2 4 0.7 COc1cccc2c1N=C(N)NC2 10.1016/j.bmcl.2007.10.080
CHEMBL552782 13535 6 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 177 1 2 4 0.7 COc1cccc2c1N=C(N)NC2 10.1016/j.bmcl.2007.10.080
CHEMBL5077293 212720 0 None -346 9 Human 6.0 pKi = 6.0 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None COc1ccccc1-c1cc(C2CCNC2)ccc1Cl 10.1021/acs.jmedchem.1c00110
44351184 18673 0 None 1 3 Mouse 7.0 pKi = 7.0 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 368 6 0 4 4.2 COc1ccc2c(c1)c1c(n2C)CCN(CCCOc2ccc(F)cc2)C1 10.1021/jm030080s
CHEMBL128185 18673 0 None 1 3 Mouse 7.0 pKi = 7.0 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 368 6 0 4 4.2 COc1ccc2c(c1)c1c(n2C)CCN(CCCOc2ccc(F)cc2)C1 10.1021/jm030080s
23642275 479 28 None -60 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from recombinant human 5-HT5a receptor after 120 mins by scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5-HT5a receptor after 120 mins by scintillation counting analysis
ChEMBL 283 2 0 3 3.1 CN([C@H]1CCc2c(C1)cccc2c1c(C)nn(c1C)C)C 10.1039/C8MD00313K
8433 479 28 None -60 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from recombinant human 5-HT5a receptor after 120 mins by scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5-HT5a receptor after 120 mins by scintillation counting analysis
ChEMBL 283 2 0 3 3.1 CN([C@H]1CCc2c(C1)cccc2c1c(C)nn(c1C)C)C 10.1039/C8MD00313K
CHEMBL2164327 479 28 None -60 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from recombinant human 5-HT5a receptor after 120 mins by scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5-HT5a receptor after 120 mins by scintillation counting analysis
ChEMBL 283 2 0 3 3.1 CN([C@H]1CCc2c(C1)cccc2c1c(C)nn(c1C)C)C 10.1039/C8MD00313K
13702393 154486 2 None 6 6 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 181 0 2 3 1.4 NC1=Nc2cccc(Cl)c2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL401541 154486 2 None 6 6 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 181 0 2 3 1.4 NC1=Nc2cccc(Cl)c2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL556983 154486 2 None 6 6 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 181 0 2 3 1.4 NC1=Nc2cccc(Cl)c2CN1 10.1016/j.bmcl.2007.10.080
118464427 137806 0 None -36 7 Human 6.0 pKi = 6 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 328 3 4 6 1.8 CCNC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL3771331 137806 0 None -36 7 Human 6.0 pKi = 6 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 328 3 4 6 1.8 CCNC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
44355200 26133 0 None - 1 Rat 6.0 pKi = 6 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 261 8 0 2 3.9 CCCN(CCC)C[C@@H]1C[C@@H]1c1ccccc1OC 10.1016/0960-894X(96)00045-5
CHEMBL135894 26133 0 None - 1 Rat 6.0 pKi = 6 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 261 8 0 2 3.9 CCCN(CCC)C[C@@H]1C[C@@H]1c1ccccc1OC 10.1016/0960-894X(96)00045-5
2543 3651 66 None -1412 31 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3651 66 None -1412 31 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3651 66 None -1412 31 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3651 66 None -1412 31 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3651 66 None -1412 31 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
4106 2466 16 3H-5CT -14 33 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2466 16 3H-5CT -14 33 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2466 16 3H-5CT -14 33 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2466 16 3H-5CT -14 33 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
4106 2466 16 125I-LSD -269 33 Mouse 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2466 16 125I-LSD -269 33 Mouse 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2466 16 125I-LSD -269 33 Mouse 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2466 16 125I-LSD -269 33 Mouse 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
1220 186 46 125I-LSD -794 44 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 186 46 125I-LSD -794 44 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 186 46 125I-LSD -794 44 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 186 46 125I-LSD -794 44 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
10257 728 28 125I-LSD -741 18 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
144 728 28 125I-LSD -741 18 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
CHEMBL416526 728 28 125I-LSD -741 18 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
DB01445 728 28 125I-LSD -741 18 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
135398737 944 89 3H-5CT -173 91 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-5CT -173 91 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-5CT -173 91 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-5CT -173 91 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-5CT -173 91 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
11957541 1430 38 125I-LSD -181 15 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
1229 1430 38 125I-LSD -181 15 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
147 1430 38 125I-LSD -181 15 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
170617 1430 38 125I-LSD -181 15 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
CHEMBL6616 1430 38 125I-LSD -181 15 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
681 1437 65 125I-LSD -199 38 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1437 65 125I-LSD -199 38 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1437 65 125I-LSD -199 38 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1437 65 125I-LSD -199 38 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1437 65 125I-LSD -199 38 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
1357 2450 133 125I-LSD -3311 8 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1672 2450 133 125I-LSD -3311 8 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
224 2450 133 125I-LSD -3311 8 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
896 2450 133 125I-LSD -3311 8 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
CHEMBL45 2450 133 125I-LSD -3311 8 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
DB01065 2450 133 125I-LSD -3311 8 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
206 2457 10 125I-LSD -676 24 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2457 10 125I-LSD -676 24 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2457 10 125I-LSD -676 24 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
133 2460 48 125I-LSD -1862 42 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2460 48 125I-LSD -1862 42 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2460 48 125I-LSD -1862 42 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2460 48 125I-LSD -1862 42 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2460 48 125I-LSD -1862 42 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
134 2478 19 125I-LSD -109 67 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2478 19 125I-LSD -109 67 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2478 19 125I-LSD -109 67 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2478 19 125I-LSD -109 67 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2478 19 125I-LSD -109 67 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
484 2814 45 125I-LSD -31 35 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 2814 45 125I-LSD -31 35 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 2814 45 125I-LSD -31 35 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
1243 3561 26 125I-LSD -3235 5 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O None
944 3561 26 125I-LSD -3235 5 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O None
CHEMBL324017 3561 26 125I-LSD -3235 5 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O None
102 4064 44 125I-LSD -1698 49 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
102 4064 44 125I-LSD -2511 49 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4064 44 125I-LSD -1698 49 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4064 44 125I-LSD -2511 49 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4064 44 125I-LSD -1698 49 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4064 44 125I-LSD -2511 49 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4064 44 125I-LSD -1698 49 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4064 44 125I-LSD -2511 49 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4064 44 125I-LSD -1698 49 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4064 44 125I-LSD -2511 49 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
108182 4068 18 125I-LSD -3 16 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
245 4068 18 125I-LSD -3 16 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
CHEMBL18041 4068 18 125I-LSD -3 16 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
None 214629 0 UNDEFINED -1122 11 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 243 3 1 4 2.7 CCC1=CC2=C(O1)C=CC3=C2N(N=C3)CC(C)N None
179 396 107 3H-LSD -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 396 107 3H-LSD -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 396 107 3H-LSD -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 396 107 3H-LSD -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 396 107 3H-LSD -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
681 1437 65 125I-LSD -1995 38 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1437 65 125I-LSD -1995 38 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1437 65 125I-LSD -1995 38 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1437 65 125I-LSD -1995 38 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1437 65 125I-LSD -1995 38 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
1524 2150 89 125I-LSD -7244 51 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2150 89 125I-LSD -7244 51 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2150 89 125I-LSD -7244 51 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2150 89 125I-LSD -7244 51 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2150 89 125I-LSD -7244 51 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2150 89 125I-LSD -7244 51 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
134 2478 19 3H-LSD -162 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2478 19 3H-LSD -162 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2478 19 3H-LSD -162 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2478 19 3H-LSD -162 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2478 19 3H-LSD -162 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
484 2814 45 125I-LSD -100 35 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
484 2814 45 3H-KETANSERIN -31 35 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 2814 45 125I-LSD -100 35 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 2814 45 3H-KETANSERIN -31 35 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 2814 45 125I-LSD -100 35 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 2814 45 3H-KETANSERIN -31 35 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
15897 2817 0 3H-LSD -354 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2817 0 3H-LSD -354 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2817 0 3H-LSD -354 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
119570 3110 90 3H-LSD -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 3110 90 3H-LSD -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 3110 90 3H-LSD -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 3110 90 3H-LSD -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 3110 90 3H-LSD -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
165193 3138 60 125I-LSD -10000 42 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
2303 3138 60 125I-LSD -10000 42 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
4946 3138 60 125I-LSD -10000 42 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
564 3138 60 125I-LSD -10000 42 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
62882 3138 60 125I-LSD -10000 42 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
63 3138 60 125I-LSD -10000 42 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
66366 3138 60 125I-LSD -10000 42 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
91536 3138 60 125I-LSD -10000 42 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 3138 60 125I-LSD -10000 42 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 3138 60 125I-LSD -10000 42 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
DB00571 3138 60 125I-LSD -10000 42 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
243 3153 85 3H-5CT -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3052762 3153 85 3H-5CT -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3502 3153 85 3H-5CT -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
CHEMBL117287 3153 85 3H-5CT -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
DB06480 3153 85 3H-5CT -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
173 3211 88 3H-LSD -114 22 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 3211 88 3H-LSD -114 22 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 3211 88 3H-LSD -114 22 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
2402 3318 58 3H-LSD -660 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
5095 3318 58 3H-LSD -660 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
7295 3318 58 3H-LSD -660 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
CHEMBL589 3318 58 3H-LSD -660 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
DB00268 3318 58 3H-LSD -660 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
128563 3408 28 3H-LSD -2398 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
1666 3408 28 3H-LSD -2398 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
CHEMBL445332 3408 28 3H-LSD -2398 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
DB12327 3408 28 3H-LSD -2398 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
2543 3651 66 125I-LSD -257 31 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
2543 3651 66 UNDEFINED -257 31 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3651 66 125I-LSD -257 31 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3651 66 UNDEFINED -257 31 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3651 66 125I-LSD -257 31 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3651 66 UNDEFINED -257 31 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3651 66 125I-LSD -257 31 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3651 66 UNDEFINED -257 31 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3651 66 125I-LSD -257 31 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3651 66 UNDEFINED -257 31 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
185 3943 54 3H-LSD -30902 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5311271 3943 54 3H-LSD -30902 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
CHEMBL74355 3943 54 3H-LSD -30902 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
DB16351 3943 54 3H-LSD -30902 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
102 4064 44 3H-LSD -1698 49 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4064 44 3H-LSD -1698 49 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4064 44 3H-LSD -1698 49 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4064 44 3H-LSD -1698 49 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4064 44 3H-LSD -1698 49 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
2662 11279 124 3H-Alpha-Me-histamine -41 31 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 None
CHEMBL118 11279 124 3H-Alpha-Me-histamine -41 31 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 None
10297 26905 29 3H-LSD -38 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
CHEMBL136560 26905 29 3H-LSD -38 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
156391 46537 95 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
CHEMBL1200806 46537 95 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
CHEMBL154 46537 95 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
21830793 91403 5 3H-8-OH-DPAT -66069 46 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
CHEMBL2413154 91403 5 3H-8-OH-DPAT -66069 46 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
2244 93798 96 3H-LSD -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 180 2 1 3 1.3 CC(=O)Oc1ccccc1C(=O)O None
CHEMBL25 93798 96 3H-LSD -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 180 2 1 3 1.3 CC(=O)Oc1ccccc1C(=O)O None
3663 99505 79 3H-LSD -288 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 504 0 6 8 5.1 Cc1cc(O)c2c(=O)c3c(O)cc(O)c4c5c(O)cc(O)c6c(=O)c7c(O)cc(C)c8c1c2c(c34)c(c78)c65 None
CHEMBL286494 99505 79 3H-LSD -288 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 504 0 6 8 5.1 Cc1cc(O)c2c(=O)c3c(O)cc(O)c4c5c(O)cc(O)c6c(=O)c7c(O)cc(C)c8c1c2c(c34)c(c78)c65 None
446220 132998 13 3H-LSD -1778 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
CHEMBL370805 132998 13 3H-LSD -1778 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
1615 167228 22 3H-LSD -26 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
CHEMBL43048 167228 22 3H-LSD -26 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
5280343 187691 119 3H-LSD -147 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL1520590 187691 119 3H-LSD -147 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL50 187691 119 3H-LSD -147 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
54676228 192874 108 3H-LSD -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 2 2 5 1.6 CN1C(C(=O)Nc2ccccn2)=C(O)c2ccccc2S1(=O)=O None
CHEMBL527 192874 108 3H-LSD -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 2 2 5 1.6 CN1C(C(=O)Nc2ccccn2)=C(O)c2ccccc2S1(=O)=O None
4495 194860 87 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 None
CHEMBL56367 194860 87 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 None
54677470 198867 110 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
CHEMBL1256873 198867 110 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
CHEMBL599 198867 110 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
162265 200587 19 3H-LSD -239 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4786 200587 19 3H-LSD -239 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
CHEMBL61006 200587 19 3H-LSD -239 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
5281600 201336 85 3H-LSD -275 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
CHEMBL63354 201336 85 3H-LSD -275 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
1973 201790 12 3H-LSD -3 35 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL1394464 201790 12 3H-LSD -3 35 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL66089 201790 12 3H-LSD -3 35 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
202478 202981 15 3H-LSD -97 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
CHEMBL7393 202981 15 3H-LSD -97 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
5311189 203133 4 3H-LSD -194 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 None
CHEMBL7549 203133 4 3H-LSD -194 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 None
4158 203630 21 3H-LSD -141 20 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
CHEMBL1722 203630 21 3H-LSD -141 20 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
CHEMBL796 203630 21 3H-LSD -141 20 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
None 214217 0 3H-LSD -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 2 0 4 3.6 CC1=NC=CN1CC2CCC3=C(C2=O)C4=CC=CC=C4N3C.Cl None
25137849 214425 0 3H-LSD -4 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
71290 214425 0 3H-LSD -4 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
3337 214441 0 3H-LSD -1513 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
65801 214441 0 3H-LSD -1513 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
66264 214441 0 3H-LSD -1513 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
91452 214441 0 3H-LSD -1513 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
None 214486 0 3H-LSD -95499 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 316 7 3 3 3.0 CC(CF)NCC(COC1=CC=CC2=C1C3=CC=CC=C3N2)O None
3821 214549 0 3H-LSD -1 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 237 2 1 2 2.9 CNC1(CCCCC1=O)C2=CC=CC=C2Cl None
None 214560 0 3H-LSD -1 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 240 7 4 6 -0.8 C(C(C(=O)O)N)SSCC(C(=O)O)N None
None 214561 0 3H-LSD -1 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 4 2 3 0.2 CSCCC(C(=O)O)N None
None 214562 0 3H-LSD -1 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 3 3 3 -0.3 C(CS)C(C(=O)O)N None
None 214563 0 3H-LSD -1 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 121 2 3 3 -0.7 C(C(C(=O)O)N)S None
None 214564 0 3H-LSD -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 117 0 1 3 -0.0 C1CSC(=O)C1N None
None 214565 0 3H-LSD -1 39 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 3 3 3 -1.4 C(C(C(=O)O)N)S(=O)O None
None 214566 0 3H-LSD -1 38 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 3 3 4 -1.7 C(C(C(=O)O)N)S(=O)(=O)O None
None 214567 0 3H-LSD -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 183 4 3 4 -1.3 C(CS(=O)(=O)O)C(C(=O)O)N None
None 214574 0 3H-LSD -13 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 2 1 2 1.2 CC(C(=O)C1=CC=CC=C1)N None
1576 214575 0 3H-LSD -16 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 163 3 1 2 1.5 CC(C(=O)C1=CC=CC=C1)NC None
None 214576 0 3H-LSD -16 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 536 11 1 4 9.0 CC(C)C(=O)C12C(=O)C(=C(C(C1=O)(CC(C2(C)CCC=C(C)C)CC=C(C)C)CC=C(C)C)O)CC=C(C)C None
4978 214577 0 3H-LSD -16 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 520 1 7 9 4.3 CC1=CC(=C2C3=C1C4=C5C(=C(C=C4CO)O)C(=O)C6=C(C=C(C7=C6C5=C3C8=C7C(=CC(=C8C2=O)O)O)O)O)O None
None 214578 0 3H-LSD -3 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 464 4 8 12 -0.6 C1=CC(=C(C=C1C2=C(C(=C3C(=CC(=O)C=C3O2)O)O)OC4C(C(C(C(O4)CO)O)O)O)O)O None
None 214579 0 3H-LSD -281 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 610 6 10 16 -1.7 CC1C(C(C(C(O1)OCC2C(C(C(C(O2)OC3=C(OC4=CC(=CC(=C4C3=O)O)O)C5=CC(=C(C=C5)O)O)O)O)O)O)O)O None
None 214580 0 3H-LSD -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 448 3 7 11 0.4 CC1C(C(C(C(O1)OC2=C(OC3=CC(=O)C=C(C3=C2O)O)C4=CC(=C(C=C4)O)O)O)O)O None
135269 214639 0 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 222 5 1 3 2.5 CCCCC(=O)OC1=CC=CC=C1C(=O)O None
23681059 214640 0 3H-LSD -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 CC(C1=CC2=C(C=C1)C=C(C=C2)OC)C(=O)O None
5018304 214641 0 3H-LSD -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 317 4 1 3 0.0 C1=CC=C(C(=C1)CC(=O)[O-])NC2=C(C=CC=C2Cl)Cl.[Na+] None
84003 214643 0 3H-LSD -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 376 6 5 7 -0.0 C1CN2C(=CC=C2C(=O)C3=CC=CC=C3)C1C(=O)O.C(C(CO)(CO)N)O None
123619 214644 0 3H-Alpha-Me-histamine -1412 27 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 358 3 0 4 4.2 CC1=NC=C(C=C1)C2=NC=C(C=C2C3=CC=C(C=C3)S(=O)(=O)C)Cl None
119828 214645 0 3H-Alpha-Me-histamine -1 30 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 5 1 5 3.5 CCC(=O)NS(=O)(=O)C1=CC=C(C=C1)C2=C(ON=C2C3=CC=CC=C3)C None
5090 214646 0 3H-Alpha-Me-histamine -1348 31 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)C1=CC=C(C=C1)C2=C(C(=O)OC2)C3=CC=CC=C3 None
119607 214647 0 3H-Alpha-Me-histamine -97 28 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 1 4 3.0 CC1=C(C(=NO1)C2=CC=CC=C2)C3=CC=C(C=C3)S(=O)(=O)N None
None 214648 0 3H-Alpha-Me-histamine -7 29 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 517 8 2 5 5.2 CC1=C(C2=C(N1C(=O)C3=CC=C(C=C3)Cl)C=CC(=C2)OC)CC(=O)NCCC4=CC=C(C=C4)NC(=O)C None
5 139 66 3H-LSD -891 54 Mouse 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 3H-LSD -891 54 Mouse 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 3H-LSD -891 54 Mouse 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 3H-LSD -891 54 Mouse 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
2726 906 64 3H-LSD -16 72 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 3H-LSD -16 72 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 3H-LSD -16 72 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 3H-LSD -16 72 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 3H-LSD -16 72 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1809 134 28 UNDEFINED -257 36 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
1809 134 28 125I-LSD -363 36 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 28 UNDEFINED -257 36 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 28 125I-LSD -363 36 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 28 UNDEFINED -257 36 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 28 125I-LSD -363 36 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
135398745 2869 108 3H-LSD -109 65 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-LSD -109 65 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-LSD -109 65 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-LSD -109 65 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
242 467 117 3H-LSD -144 51 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 467 117 3H-LSD -144 51 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 467 117 3H-LSD -144 51 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 467 117 3H-LSD -144 51 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 467 117 3H-LSD -144 51 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
242 467 117 3H-LSD -144 51 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 467 117 3H-LSD -144 51 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 467 117 3H-LSD -144 51 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 467 117 3H-LSD -144 51 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 467 117 3H-LSD -144 51 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
4106 2466 16 UNDEFINED -269 33 Mouse 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2466 16 UNDEFINED -269 33 Mouse 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2466 16 UNDEFINED -269 33 Mouse 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2466 16 UNDEFINED -269 33 Mouse 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
1220 186 46 125I-LSD -1071 44 Mouse 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 186 46 125I-LSD -1071 44 Mouse 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 186 46 125I-LSD -1071 44 Mouse 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 186 46 125I-LSD -1071 44 Mouse 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
5 139 66 3H-5CT -323 54 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 3H-5CT -323 54 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 3H-5CT -323 54 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 3H-5CT -323 54 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 139 66 125I-LSD -999 54 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 125I-LSD -999 54 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 125I-LSD -999 54 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 125I-LSD -999 54 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
103 4089 56 3H-LSD -25 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4089 56 3H-LSD -25 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4089 56 3H-LSD -25 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4089 56 3H-LSD -25 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4089 56 3H-LSD -25 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
7153 97570 74 3H-LSD -70 33 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97570 74 3H-LSD -70 33 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
135398745 2869 108 3H-LSD -109 65 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-LSD -109 65 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-LSD -109 65 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-LSD -109 65 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
11954224 214174 0 3H-LSD -147 59 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
1212 1632 45 3H-LSD -63 65 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1632 45 3H-LSD -63 65 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1632 45 3H-LSD -63 65 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1632 45 3H-LSD -63 65 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1632 45 3H-LSD -63 65 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
4106 2466 16 125I-LSD -128 33 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2466 16 125I-LSD -128 33 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2466 16 125I-LSD -128 33 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2466 16 125I-LSD -128 33 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
11954224 214174 0 125I-LSD -131 59 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
1809 134 28 125I-LSD -257 36 Mouse 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 28 125I-LSD -257 36 Mouse 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 28 125I-LSD -257 36 Mouse 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4452 2721 18 3H-LSD -52480 18 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
983 2721 18 3H-LSD -52480 18 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
CHEMBL20734 2721 18 3H-LSD -52480 18 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
1220 186 46 UNDEFINED -1071 44 Mouse 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 186 46 UNDEFINED -1071 44 Mouse 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 186 46 UNDEFINED -1071 44 Mouse 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 186 46 UNDEFINED -1071 44 Mouse 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
None 214366 0 3H-LSD -1737 23 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 772 16 4 10 5.5 CN(C)CCONC(=CC=C1C=CC(=O)C=C1)C2=CC=CC=C2F.CN(C)CCONC(=CC=C1C=CC(=O)C=C1)C2=CC=CC=C2F.C(=CC(=O)O)C(=O)O None
134 2478 19 125I-LSD -109 67 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2478 19 125I-LSD -109 67 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2478 19 125I-LSD -109 67 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2478 19 125I-LSD -109 67 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2478 19 125I-LSD -109 67 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
2389 3279 114 3H-LSD -331 67 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 3H-LSD -331 67 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 3H-LSD -331 67 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 3H-LSD -331 67 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 3H-LSD -331 67 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
1809 134 28 3H-5CT -229 36 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 28 3H-5CT -229 36 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 28 3H-5CT -229 36 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
6971132 214235 0 3H-LSD -512 14 Mouse 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 268 1 2 2 2.1 CN1CC(C=C2C1CC3=CNC4=CC=CC2=C34)C(=O)O None
1524 2150 89 3H-5CT -1778 51 Human 4.7 pKi = 4.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2150 89 3H-5CT -1778 51 Human 4.7 pKi = 4.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2150 89 3H-5CT -1778 51 Human 4.7 pKi = 4.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2150 89 3H-5CT -1778 51 Human 4.7 pKi = 4.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2150 89 3H-5CT -1778 51 Human 4.7 pKi = 4.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2150 89 3H-5CT -1778 51 Human 4.7 pKi = 4.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
2389 3279 114 3H-LSD -331 67 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 3H-LSD -331 67 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 3H-LSD -331 67 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 3H-LSD -331 67 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 3H-LSD -331 67 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
1353 1880 85 3H-LSD -77 85 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-LSD -77 85 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-LSD -77 85 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-LSD -77 85 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-LSD -77 85 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
242 467 117 3H-LSD -144 51 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 467 117 3H-LSD -144 51 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 467 117 3H-LSD -144 51 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 467 117 3H-LSD -144 51 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 467 117 3H-LSD -144 51 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
2337 3205 72 3H-LSD -38 62 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 3H-LSD -38 62 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 3H-LSD -38 62 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 3H-LSD -38 62 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 3H-LSD -38 62 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
1809 134 28 125I-LSD -363 36 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 28 125I-LSD -363 36 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 28 125I-LSD -363 36 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
5 139 66 125I-LSD -999 54 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 125I-LSD -999 54 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 125I-LSD -999 54 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 125I-LSD -999 54 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
1220 186 46 3H-5CT -1548 44 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 186 46 3H-5CT -1548 44 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 186 46 3H-5CT -1548 44 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 186 46 3H-5CT -1548 44 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
5 139 66 125I-LSD -891 54 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 139 66 UNDEFINED -891 54 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 125I-LSD -891 54 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 UNDEFINED -891 54 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 125I-LSD -891 54 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 UNDEFINED -891 54 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 125I-LSD -891 54 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 UNDEFINED -891 54 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
115 3732 78 125I-LSD -61 26 Mouse 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 3732 78 125I-LSD -61 26 Mouse 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 3732 78 125I-LSD -61 26 Mouse 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
145 140 48 3H-LSD -53 29 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
1832 140 48 3H-LSD -53 29 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL7257 140 48 3H-LSD -53 29 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB14010 140 48 3H-LSD -53 29 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
115237 55296 113 3H-LSD -33 54 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55296 113 3H-LSD -33 54 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
4106 2466 16 125I-LSD -128 33 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2466 16 125I-LSD -128 33 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2466 16 125I-LSD -128 33 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2466 16 125I-LSD -128 33 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
103 4089 56 3H-LSD -25 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4089 56 3H-LSD -25 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4089 56 3H-LSD -25 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4089 56 3H-LSD -25 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4089 56 3H-LSD -25 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
10257 728 28 3H-LSD -741 18 Mouse 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
144 728 28 3H-LSD -741 18 Mouse 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
CHEMBL416526 728 28 3H-LSD -741 18 Mouse 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
DB01445 728 28 3H-LSD -741 18 Mouse 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
2865 4079 67 3H-LSD -169 53 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4079 67 3H-LSD -169 53 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4079 67 3H-LSD -169 53 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4079 67 3H-LSD -169 53 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4079 67 3H-LSD -169 53 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
1588 2294 24 3H-LSD -12 43 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2294 24 3H-LSD -12 43 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2294 24 3H-LSD -12 43 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2294 24 3H-LSD -12 43 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2294 24 3H-LSD -12 43 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
11954224 214174 0 125I-LSD -131 59 Mouse 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
2865 4079 67 3H-LSD -169 53 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4079 67 3H-LSD -169 53 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4079 67 3H-LSD -169 53 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4079 67 3H-LSD -169 53 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4079 67 3H-LSD -169 53 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
2337 3205 72 3H-LSD -38 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 3H-LSD -38 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 3H-LSD -38 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 3H-LSD -38 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 3H-LSD -38 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
None 214168 0 125I-LSD -223 23 Mouse 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
None 214526 0 3H-LSD -3630 11 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 426 6 0 6 3.4 C1CCC2C(C1)C(=O)N(C2=O)CCCCN3CCN(CC3)C4=NSC5=CC=CC=C54 None
11954259 214201 0 3H-LSD -1202 43 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
100 3745 52 3H-LSD -23 55 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3745 52 3H-LSD -23 55 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3745 52 3H-LSD -23 55 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3745 52 3H-LSD -23 55 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3745 52 3H-LSD -23 55 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
11954224 214174 0 3H-LSD -131 59 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
135398737 944 89 3H-LSD -173 91 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-LSD -173 91 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-LSD -173 91 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-LSD -173 91 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-LSD -173 91 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
3294 1975 106 3H-LSD -676 44 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 1975 106 3H-LSD -676 44 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 1975 106 3H-LSD -676 44 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 1975 106 3H-LSD -676 44 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 1975 106 3H-LSD -676 44 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
2470 3596 46 None -77624 59 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3596 46 None -77624 59 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3596 46 None -77624 59 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3596 46 None -77624 59 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3596 46 None -77624 59 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
1524 2150 89 None -1778 51 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2150 89 None -1778 51 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2150 89 None -1778 51 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2150 89 None -1778 51 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2150 89 None -1778 51 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2150 89 None -1778 51 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
2543 3651 66 None -257 31 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3651 66 None -257 31 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3651 66 None -257 31 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3651 66 None -257 31 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3651 66 None -257 31 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
1342 36 42 3H-LSD -16 18 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 36 42 3H-LSD -16 18 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 36 42 3H-LSD -16 18 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
135398737 944 89 None -67 91 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 None -67 91 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 None -67 91 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 None -67 91 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 None -67 91 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
102 4064 44 None -407 49 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4064 44 None -407 49 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4064 44 None -407 49 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4064 44 None -407 49 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4064 44 None -407 49 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
216239 23591 114 None -6 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from 5HT5A receptor after 1.5 hrs by scintillation counterDisplacement of [3H]LSD from 5HT5A receptor after 1.5 hrs by scintillation counter
Drug Central 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 None
CHEMBL1200485 23591 114 None -6 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from 5HT5A receptor after 1.5 hrs by scintillation counterDisplacement of [3H]LSD from 5HT5A receptor after 1.5 hrs by scintillation counter
Drug Central 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 None
CHEMBL1336 23591 114 None -6 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from 5HT5A receptor after 1.5 hrs by scintillation counterDisplacement of [3H]LSD from 5HT5A receptor after 1.5 hrs by scintillation counter
Drug Central 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 None
2337 3205 72 None -38 62 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 None -38 62 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 None -38 62 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 None -38 62 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 None -38 62 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
1353 1880 85 None -77 85 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 None -77 85 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 None -77 85 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 None -77 85 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 None -77 85 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
242 467 117 None -144 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 467 117 None -144 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 467 117 None -144 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 467 117 None -144 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 467 117 None -144 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
134 2478 19 3H-LSD -67 67 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2478 19 3H-LSD -67 67 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2478 19 3H-LSD -67 67 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2478 19 3H-LSD -67 67 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2478 19 3H-LSD -67 67 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
2543 3651 66 3H-5CT -1412 31 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3651 66 3H-5CT -1412 31 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3651 66 3H-5CT -1412 31 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3651 66 3H-5CT -1412 31 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3651 66 3H-5CT -1412 31 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
2435 3533 78 3H-LSD -999 48 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3533 78 3H-LSD -999 48 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3533 78 3H-LSD -999 48 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3533 78 3H-LSD -999 48 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3533 78 3H-LSD -999 48 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
1809 134 28 3H-LSD -257 36 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 28 3H-LSD -257 36 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 28 3H-LSD -257 36 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
3294 1975 106 3H-LSD -676 44 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 1975 106 3H-LSD -676 44 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 1975 106 3H-LSD -676 44 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 1975 106 3H-LSD -676 44 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 1975 106 3H-LSD -676 44 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
135398737 944 89 None -173 91 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 None -173 91 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 None -173 91 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 None -173 91 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 None -173 91 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
33630 178379 94 None -13 27 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells by radioligand binding assay
Drug Central 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
CHEMBL47050 178379 94 None -13 27 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells by radioligand binding assay
Drug Central 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
102 4064 44 None -1698 49 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4064 44 None -1698 49 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4064 44 None -1698 49 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4064 44 None -1698 49 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4064 44 None -1698 49 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
5022 1621 67 None -1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 None
6918248 1621 67 None -1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 None
8182 1621 67 None -1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 None
CHEMBL231068 1621 67 None -1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 None
DB04908 1621 67 None -1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 None
1613 2316 44 None -15 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2316 44 None -15 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2316 44 None -15 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2316 44 None -15 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2316 44 None -15 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
133 2460 48 None -251 42 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2460 48 None -251 42 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2460 48 None -251 42 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2460 48 None -251 42 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2460 48 None -251 42 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
11954224 214174 0 UNDEFINED -131 59 Mouse 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
11954224 214174 0 125I-LSD -131 59 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
100 3745 52 None -23 55 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3745 52 None -23 55 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3745 52 None -23 55 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3745 52 None -23 55 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3745 52 None -23 55 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
212 3746 43 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
2639 3746 43 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
941651 3746 43 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
CHEMBL1201 3746 43 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
DB01623 3746 43 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
2865 4079 67 None -169 53 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4079 67 None -169 53 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4079 67 None -169 53 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4079 67 None -169 53 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4079 67 None -169 53 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
115237 55296 113 None -33 54 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55296 113 None -33 54 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
4806 3945 85 None -10 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
7351 3945 85 None -10 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
9966051 3945 85 None -10 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
CHEMBL2104993 3945 85 None -10 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
DB09068 3945 85 None -10 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
2389 3279 114 None -331 67 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 None -331 67 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 None -331 67 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 None -331 67 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 None -331 67 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
134 2478 19 None -109 67 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2478 19 None -109 67 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2478 19 None -109 67 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2478 19 None -109 67 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2478 19 None -109 67 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1212 1632 45 None -63 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1632 45 None -63 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1632 45 None -63 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1632 45 None -63 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1632 45 None -63 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3389 215982 0 None -1 26 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 549 12 0 6 6.8 CCCCCCC(=O)OCCN1CCN(CCCN2C3=CC=CC=C3SC3=C2C=C(C=C3)C(F)(F)F)CC1 None
11978813 713 72 None -8 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
5014 713 72 None -8 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
7672 713 72 None -8 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
CHEMBL2105760 713 72 None -8 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
DB09128 713 72 None -8 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
22530 55838 54 None -1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 2 0 2 3.7 CN1CCc2c(c3ccccc3n2Cc2ccccc2)C1 None
CHEMBL1600878 55838 54 None -1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 2 0 2 3.7 CN1CCc2c(c3ccccc3n2Cc2ccccc2)C1 None
CHEMBL1625607 55838 54 None -1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 2 0 2 3.7 CN1CCc2c(c3ccccc3n2Cc2ccccc2)C1 None
2726 906 64 None -16 72 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 None -16 72 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 None -16 72 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 None -16 72 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 None -16 72 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
141 1399 32 3H-LSD -7 21 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
6089 1399 32 3H-LSD -7 21 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
CHEMBL12420 1399 32 3H-LSD -7 21 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
DB01488 1399 32 3H-LSD -7 21 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
134 2478 19 I125-2-iodo LSD -67 67 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2478 19 I125-2-iodo LSD -67 67 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2478 19 I125-2-iodo LSD -67 67 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2478 19 I125-2-iodo LSD -67 67 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2478 19 I125-2-iodo LSD -67 67 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
134 2478 19 125I-LSD -67 67 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2478 19 125I-LSD -67 67 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2478 19 125I-LSD -67 67 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2478 19 125I-LSD -67 67 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2478 19 125I-LSD -67 67 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
133 2460 48 3H-5CT -251 42 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2460 48 3H-5CT -251 42 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2460 48 3H-5CT -251 42 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2460 48 3H-5CT -251 42 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2460 48 3H-5CT -251 42 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
102 4064 44 UNDEFINED -1698 49 Mouse 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4064 44 UNDEFINED -1698 49 Mouse 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4064 44 UNDEFINED -1698 49 Mouse 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4064 44 UNDEFINED -1698 49 Mouse 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4064 44 UNDEFINED -1698 49 Mouse 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
2470 3596 46 3H-5CT -77624 59 Human 4.2 pKi = 4.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3596 46 3H-5CT -77624 59 Human 4.2 pKi = 4.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3596 46 3H-5CT -77624 59 Human 4.2 pKi = 4.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3596 46 3H-5CT -77624 59 Human 4.2 pKi = 4.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3596 46 3H-5CT -77624 59 Human 4.2 pKi = 4.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
107780 1814 50 3H-5HT -6760 17 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
14 1814 50 3H-5HT -6760 17 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL15928 1814 50 3H-5HT -6760 17 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
134 2478 19 None -162 67 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2478 19 None -162 67 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2478 19 None -162 67 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2478 19 None -162 67 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2478 19 None -162 67 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
134 2478 19 None -67 67 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2478 19 None -67 67 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2478 19 None -67 67 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2478 19 None -67 67 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2478 19 None -67 67 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
103 4089 56 None -25 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4089 56 None -25 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4089 56 None -25 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4089 56 None -25 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4089 56 None -25 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
11954224 214174 0 None -147 59 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation countingDisplacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation counting
Drug Central 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
1613 2316 44 3H-LSD -15 44 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2316 44 3H-LSD -15 44 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2316 44 3H-LSD -15 44 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2316 44 3H-LSD -15 44 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2316 44 3H-LSD -15 44 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
134 2478 19 UNDEFINED -67 67 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2478 19 UNDEFINED -67 67 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2478 19 UNDEFINED -67 67 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2478 19 UNDEFINED -67 67 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2478 19 UNDEFINED -67 67 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1621 2396 16 None -27 44 Human 8.1 pKi = 8.1 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2396 16 None -27 44 Human 8.1 pKi = 8.1 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2396 16 None -27 44 Human 8.1 pKi = 8.1 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2396 16 None -27 44 Human 8.1 pKi = 8.1 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2396 16 None -27 44 Human 8.1 pKi = 8.1 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
11954224 214174 0 None -131 59 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
11954224 214174 0 None -131 59 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
46780481 107045 18 None -50 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107045 18 None -50 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107045 18 None -50 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107045 18 None -50 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
1621 2396 16 3H-LSD -28 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2396 16 3H-LSD -28 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2396 16 3H-LSD -28 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2396 16 3H-LSD -28 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2396 16 3H-LSD -28 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
6971132 214235 0 3H-LSD -2 14 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 268 1 2 2 2.1 CN1CC(C=C2C1CC3=CNC4=CC=CC2=C34)C(=O)O None
4806 3945 85 None -10 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 21486038
7351 3945 85 None -10 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 21486038
9966051 3945 85 None -10 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 21486038
CHEMBL2104993 3945 85 None -10 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 21486038
DB09068 3945 85 None -10 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 21486038
11168182 3478 18 None 50 13 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 16002289
264 3478 18 None 50 13 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 16002289
CHEMBL1181770 3478 18 None 50 13 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 16002289
135398745 2869 108 None -109 65 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 None -109 65 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 None -109 65 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 None -109 65 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
1524 2150 89 None -1778 51 Human 4.7 pKi None 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 7988681
197 2150 89 None -1778 51 Human 4.7 pKi None 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 7988681
3822 2150 89 None -1778 51 Human 4.7 pKi None 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 7988681
88 2150 89 None -1778 51 Human 4.7 pKi None 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 7988681
CHEMBL51 2150 89 None -1778 51 Human 4.7 pKi None 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 7988681
DB12465 2150 89 None -1778 51 Human 4.7 pKi None 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 7988681
2543 3651 66 None -257 31 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11343685
2543 3651 66 None -257 31 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8450829
5358 3651 66 None -257 31 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11343685
5358 3651 66 None -257 31 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8450829
54 3651 66 None -257 31 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11343685
54 3651 66 None -257 31 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8450829
CHEMBL128 3651 66 None -257 31 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11343685
CHEMBL128 3651 66 None -257 31 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8450829
DB00669 3651 66 None -257 31 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11343685
DB00669 3651 66 None -257 31 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8450829
165193 3138 60 None -7943 42 Human 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 7988681
2303 3138 60 None -7943 42 Human 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 7988681
4946 3138 60 None -7943 42 Human 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 7988681
564 3138 60 None -7943 42 Human 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 7988681
62882 3138 60 None -7943 42 Human 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 7988681
63 3138 60 None -7943 42 Human 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 7988681
66366 3138 60 None -7943 42 Human 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 7988681
91536 3138 60 None -7943 42 Human 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 7988681
CHEMBL27 3138 60 None -7943 42 Human 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 7988681
CHEMBL452861 3138 60 None -7943 42 Human 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 7988681
DB00571 3138 60 None -7943 42 Human 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 7988681
135398737 944 89 None -67 91 Mouse 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11343685
38 944 89 None -67 91 Mouse 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11343685
722 944 89 None -67 91 Mouse 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11343685
CHEMBL42 944 89 None -67 91 Mouse 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11343685
DB00363 944 89 None -67 91 Mouse 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11343685
12 1524 14 None -208 7 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10715164
6918513 1524 14 None -208 7 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10715164
CHEMBL267615 1524 14 None -208 7 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10715164
6918515 2574 33 None -158 6 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10715164
71 2574 33 None -158 6 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10715164
CHEMBL7318 2574 33 None -158 6 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10715164
2543 3651 66 None -1412 31 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11343685
2543 3651 66 None -1412 31 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 7988681
5358 3651 66 None -1412 31 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11343685
5358 3651 66 None -1412 31 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 7988681
54 3651 66 None -1412 31 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11343685
54 3651 66 None -1412 31 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 7988681
CHEMBL128 3651 66 None -1412 31 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11343685
CHEMBL128 3651 66 None -1412 31 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 7988681
DB00669 3651 66 None -1412 31 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11343685
DB00669 3651 66 None -1412 31 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 7988681
102 4064 44 None -407 49 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 7988681
3659 4064 44 None -407 49 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 7988681
8969 4064 44 None -407 49 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 7988681
CHEMBL15245 4064 44 None -407 49 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 7988681
DB01392 4064 44 None -407 49 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 7988681
102 4064 44 None -1698 49 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8450829
102 4064 44 None -1698 49 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8549774
3659 4064 44 None -1698 49 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8450829
3659 4064 44 None -1698 49 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8549774
8969 4064 44 None -1698 49 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8450829
8969 4064 44 None -1698 49 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8549774
CHEMBL15245 4064 44 None -1698 49 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8450829
CHEMBL15245 4064 44 None -1698 49 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8549774
DB01392 4064 44 None -1698 49 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8450829
DB01392 4064 44 None -1698 49 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8549774
115 3732 78 None -61 26 Mouse 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 8450829
4296 3732 78 None -61 26 Mouse 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 8450829
CHEMBL274866 3732 78 None -61 26 Mouse 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 8450829
10257 728 28 None -741 18 Mouse 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 8450829
10257 728 28 None -741 18 Mouse 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 8549774
144 728 28 None -741 18 Mouse 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 8450829
144 728 28 None -741 18 Mouse 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 8549774
CHEMBL416526 728 28 None -741 18 Mouse 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 8450829
CHEMBL416526 728 28 None -741 18 Mouse 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 8549774
DB01445 728 28 None -741 18 Mouse 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 8450829
DB01445 728 28 None -741 18 Mouse 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 8549774
1220 186 46 None -1548 44 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 11343685
1220 186 46 None -1548 44 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 7988681
31 186 46 None -1548 44 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 11343685
31 186 46 None -1548 44 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 7988681
7 186 46 None -1548 44 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 11343685
7 186 46 None -1548 44 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 7988681
CHEMBL56 186 46 None -1548 44 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 11343685
CHEMBL56 186 46 None -1548 44 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 7988681
122130461 2395 0 None -1584 2 Mouse 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 268 1 2 2 2.1 CN1C[C@@H](C=C2C1Cc1c[nH]c3c1c2ccc3)C(=O)O 8549774
139 2395 0 None -1584 2 Mouse 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 268 1 2 2 2.1 CN1C[C@@H](C=C2C1Cc1c[nH]c3c1c2ccc3)C(=O)O 8549774
6717 2395 0 None -1584 2 Mouse 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 268 1 2 2 2.1 CN1C[C@@H](C=C2C1Cc1c[nH]c3c1c2ccc3)C(=O)O 8549774
1220 186 46 None -1071 44 Mouse 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 11343685
1220 186 46 None -1071 44 Mouse 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 8450829
31 186 46 None -1071 44 Mouse 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 11343685
31 186 46 None -1071 44 Mouse 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 8450829
7 186 46 None -1071 44 Mouse 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 11343685
7 186 46 None -1071 44 Mouse 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 8450829
CHEMBL56 186 46 None -1071 44 Mouse 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 11343685
CHEMBL56 186 46 None -1071 44 Mouse 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 8450829
108029 3361 50 None -1000 13 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 7988681
23 3361 50 None -1000 13 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 7988681
CHEMBL18785 3361 50 None -1000 13 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 7988681
197706 1436 0 None -3981 10 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 2 5 2.3 NCCc1c[nH]c2c1cc(OCC(=O)N1CCN(CC1)c1ccc(cc1)C#N)cc2 10381763
39 1436 0 None -3981 10 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 2 5 2.3 NCCc1c[nH]c2c1cc(OCC(=O)N1CCN(CC1)c1ccc(cc1)C#N)cc2 10381763
CHEMBL1742428 1436 0 None -3981 10 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 2 5 2.3 NCCc1c[nH]c2c1cc(OCC(=O)N1CCN(CC1)c1ccc(cc1)C#N)cc2 10381763
133 2460 48 None -251 42 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 7988681
1723 2460 48 None -251 42 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 7988681
28693 2460 48 None -251 42 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 7988681
CHEMBL19215 2460 48 None -251 42 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 7988681
DB13520 2460 48 None -251 42 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 7988681
135398737 944 89 None -173 91 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11343685
135398737 944 89 None -173 91 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 7988681
38 944 89 None -173 91 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11343685
38 944 89 None -173 91 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 7988681
722 944 89 None -173 91 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11343685
722 944 89 None -173 91 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 7988681
CHEMBL42 944 89 None -173 91 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11343685
CHEMBL42 944 89 None -173 91 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 7988681
DB00363 944 89 None -173 91 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11343685
DB00363 944 89 None -173 91 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 7988681
5 139 66 None -891 54 Mouse 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11343685
5 139 66 None -891 54 Mouse 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8450829
5 139 66 None -891 54 Mouse 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8549774
5202 139 66 None -891 54 Mouse 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11343685
5202 139 66 None -891 54 Mouse 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8450829
5202 139 66 None -891 54 Mouse 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8549774
CHEMBL39 139 66 None -891 54 Mouse 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11343685
CHEMBL39 139 66 None -891 54 Mouse 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8450829
CHEMBL39 139 66 None -891 54 Mouse 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8549774
DB08839 139 66 None -891 54 Mouse 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11343685
DB08839 139 66 None -891 54 Mouse 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8450829
DB08839 139 66 None -891 54 Mouse 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8549774
108029 3361 50 None -316 13 Mouse 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 8450829
23 3361 50 None -316 13 Mouse 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 8450829
CHEMBL18785 3361 50 None -316 13 Mouse 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 8450829
5 139 66 None -999 54 Rat 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 7682702
5202 139 66 None -999 54 Rat 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 7682702
CHEMBL39 139 66 None -999 54 Rat 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 7682702
DB08839 139 66 None -999 54 Rat 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 7682702
134 2478 19 None -109 67 Rat 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7682702
1775 2478 19 None -109 67 Rat 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7682702
9681 2478 19 None -109 67 Rat 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7682702
CHEMBL1065 2478 19 None -109 67 Rat 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7682702
DB00247 2478 19 None -109 67 Rat 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7682702
134 2478 19 None -67 67 Mouse 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8450829
134 2478 19 None -67 67 Mouse 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8549774
1775 2478 19 None -67 67 Mouse 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8450829
1775 2478 19 None -67 67 Mouse 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8549774
9681 2478 19 None -67 67 Mouse 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8450829
9681 2478 19 None -67 67 Mouse 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8549774
CHEMBL1065 2478 19 None -67 67 Mouse 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8450829
CHEMBL1065 2478 19 None -67 67 Mouse 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8549774
DB00247 2478 19 None -67 67 Mouse 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8450829
DB00247 2478 19 None -67 67 Mouse 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8549774
5 139 66 None -323 54 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11343685
5 139 66 None -323 54 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 7988681
5202 139 66 None -323 54 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11343685
5202 139 66 None -323 54 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 7988681
CHEMBL39 139 66 None -323 54 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11343685
CHEMBL39 139 66 None -323 54 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 7988681
DB08839 139 66 None -323 54 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11343685
DB08839 139 66 None -323 54 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 7988681
4106 2466 16 None -269 33 Mouse 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 11343685
4106 2466 16 None -269 33 Mouse 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 8450829
5358812 2466 16 None -269 33 Mouse 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 11343685
5358812 2466 16 None -269 33 Mouse 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 8450829
89 2466 16 None -269 33 Mouse 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 11343685
89 2466 16 None -269 33 Mouse 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 8450829
CHEMBL93240 2466 16 None -269 33 Mouse 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 11343685
CHEMBL93240 2466 16 None -269 33 Mouse 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 8450829
134 2478 19 None -162 67 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7988681
1775 2478 19 None -162 67 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7988681
9681 2478 19 None -162 67 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7988681
CHEMBL1065 2478 19 None -162 67 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7988681
DB00247 2478 19 None -162 67 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7988681
5074 3280 75 None -74 29 Mouse 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 11343685
97 3280 75 None -74 29 Mouse 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 11343685
CHEMBL267777 3280 75 None -74 29 Mouse 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 11343685
DB12693 3280 75 None -74 29 Mouse 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 11343685
4106 2466 16 None -128 33 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 7682702
5358812 2466 16 None -128 33 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 7682702
89 2466 16 None -128 33 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 7682702
CHEMBL93240 2466 16 None -128 33 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 7682702
1809 134 28 None -257 36 Mouse 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 11343685
1809 134 28 None -257 36 Mouse 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8450829
1809 134 28 None -257 36 Mouse 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8549774
4 134 28 None -257 36 Mouse 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 11343685
4 134 28 None -257 36 Mouse 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8450829
4 134 28 None -257 36 Mouse 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8549774
CHEMBL18840 134 28 None -257 36 Mouse 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 11343685
CHEMBL18840 134 28 None -257 36 Mouse 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8450829
CHEMBL18840 134 28 None -257 36 Mouse 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8549774
5074 3280 75 None -46 29 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 11343685
97 3280 75 None -46 29 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 11343685
CHEMBL267777 3280 75 None -46 29 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 11343685
DB12693 3280 75 None -46 29 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 11343685
1809 134 28 None -229 36 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 11343685
1809 134 28 None -229 36 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 7988681
4 134 28 None -229 36 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 11343685
4 134 28 None -229 36 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 7988681
CHEMBL18840 134 28 None -229 36 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 11343685
CHEMBL18840 134 28 None -229 36 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 7988681
1043 1552 13 None -138 28 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 11343685
1043 1552 13 None -138 28 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 8450829
1043 1552 13 None -138 28 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 8549774
149 1552 13 None -138 28 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 11343685
149 1552 13 None -138 28 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 8450829
149 1552 13 None -138 28 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 8549774
8223 1552 13 None -138 28 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 11343685
8223 1552 13 None -138 28 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 8450829
8223 1552 13 None -138 28 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 8549774
CHEMBL442 1552 13 None -138 28 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 11343685
CHEMBL442 1552 13 None -138 28 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 8450829
CHEMBL442 1552 13 None -138 28 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 8549774
DB00696 1552 13 None -138 28 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 11343685
DB00696 1552 13 None -138 28 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 8450829
DB00696 1552 13 None -138 28 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 8549774
1809 134 28 None -363 36 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 7682702
4 134 28 None -363 36 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 7682702
CHEMBL18840 134 28 None -363 36 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 7682702
1043 1552 13 None -69 28 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 7682702
149 1552 13 None -69 28 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 7682702
8223 1552 13 None -69 28 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 7682702
CHEMBL442 1552 13 None -69 28 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 7682702
DB00696 1552 13 None -69 28 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 7682702
1043 1552 13 None -169 28 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 11343685
1043 1552 13 None -169 28 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 7988681
149 1552 13 None -169 28 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 11343685
149 1552 13 None -169 28 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 7988681
8223 1552 13 None -169 28 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 11343685
8223 1552 13 None -169 28 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 7988681
CHEMBL442 1552 13 None -169 28 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 11343685
CHEMBL442 1552 13 None -169 28 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 7988681
DB00696 1552 13 None -169 28 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 11343685
DB00696 1552 13 None -169 28 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 7988681
4106 2466 16 None -14 33 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 11343685
4106 2466 16 None -14 33 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 7988681
5358812 2466 16 None -14 33 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 11343685
5358812 2466 16 None -14 33 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 7988681
89 2466 16 None -14 33 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 11343685
89 2466 16 None -14 33 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 7988681
CHEMBL93240 2466 16 None -14 33 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 11343685
CHEMBL93240 2466 16 None -14 33 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 7988681