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Ligand source activities (1 row/activity)

Ligand Receptor Assay information Chemical information
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GPCRdb ID #Vendors UniProt IUPHAR Species p-value
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H don H acc LogP Smiles DOI
4106 2350 9 5HT7R 5-HT7 receptor Human 9.2 pEC50 = 9.2 Binding
Displacement of [3H]lysergic acid from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]lysergic acid from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/np058114h
5358812 2350 9 5HT7R 5-HT7 receptor Human 9.2 pEC50 = 9.2 Binding
Displacement of [3H]lysergic acid from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]lysergic acid from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/np058114h
89 2350 9 5HT7R 5-HT7 receptor Human 9.2 pEC50 = 9.2 Binding
Displacement of [3H]lysergic acid from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]lysergic acid from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/np058114h
CHEMBL93240 2350 9 5HT7R 5-HT7 receptor Human 9.2 pEC50 = 9.2 Binding
Displacement of [3H]lysergic acid from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]lysergic acid from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/np058114h
11329254 84554 0 5HT7R 5-HT7 receptor Guinea pig 5.0 pEC50 = 5 Functional
Agonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contractionAgonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contraction
ChEMBL 450 9 1 5 4.5 O=C(CCCCCN1CCN(c2ccccc2[N+](=O)[O-])CC1)NC1CCCc2ccccc21 10.1021/jm070487n
CHEMBL225571 84554 0 5HT7R 5-HT7 receptor Guinea pig 5.0 pEC50 = 5 Functional
Agonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contractionAgonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contraction
ChEMBL 450 9 1 5 4.5 O=C(CCCCCN1CCN(c2ccccc2[N+](=O)[O-])CC1)NC1CCCc2ccccc21 10.1021/jm070487n
135367816 164011 0 5HT7R 5-HT7 receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay
ChEMBL 248 1 1 3 2.7 Clc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4218801 164011 0 5HT7R 5-HT7 receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay
ChEMBL 248 1 1 3 2.7 Clc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
135367816 164011 0 5HT7R 5-HT7 receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay
ChEMBL 248 1 1 3 2.7 Clc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4218801 164011 0 5HT7R 5-HT7 receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay
ChEMBL 248 1 1 3 2.7 Clc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
23643870 92192 0 5HT7R 5-HT7 receptor Guinea pig 5.9 pEC50 = 5.9 Functional
Agonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contractionAgonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contraction
ChEMBL 448 9 1 4 4.6 CN(C)c1ccccc1N1CCN(CCCCCC(=O)NC2CCCc3ccccc32)CC1 10.1021/jm070487n
CHEMBL243955 92192 0 5HT7R 5-HT7 receptor Guinea pig 5.9 pEC50 = 5.9 Functional
Agonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contractionAgonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contraction
ChEMBL 448 9 1 4 4.6 CN(C)c1ccccc1N1CCN(CCCCCC(=O)NC2CCCc3ccccc32)CC1 10.1021/jm070487n
135367820 163997 0 5HT7R 5-HT7 receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay
ChEMBL 232 1 1 3 2.2 Fc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4218672 163997 0 5HT7R 5-HT7 receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay
ChEMBL 232 1 1 3 2.2 Fc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
135367820 163997 0 5HT7R 5-HT7 receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay
ChEMBL 232 1 1 3 2.2 Fc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4218672 163997 0 5HT7R 5-HT7 receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay
ChEMBL 232 1 1 3 2.2 Fc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
5 134 60 5HT7R 5-HT7 receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as increase in cAMP levels by HTRF assayAgonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as increase in cAMP levels by HTRF assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8014553
5202 134 60 5HT7R 5-HT7 receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as increase in cAMP levels by HTRF assayAgonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as increase in cAMP levels by HTRF assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8014553
CHEMBL39 134 60 5HT7R 5-HT7 receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as increase in cAMP levels by HTRF assayAgonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as increase in cAMP levels by HTRF assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8014553
DB08839 134 60 5HT7R 5-HT7 receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as increase in cAMP levels by HTRF assayAgonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as increase in cAMP levels by HTRF assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8014553
67268994 163143 2 5HT7R 5-HT7 receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay
ChEMBL 247 1 2 2 2.4 Clc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4207884 163143 2 5HT7R 5-HT7 receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay
ChEMBL 247 1 2 2 2.4 Clc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
67268994 163143 2 5HT7R 5-HT7 receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay
ChEMBL 247 1 2 2 2.4 Clc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4207884 163143 2 5HT7R 5-HT7 receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay
ChEMBL 247 1 2 2 2.4 Clc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
135367405 163372 0 5HT7R 5-HT7 receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay
ChEMBL 227 1 2 2 2.1 Cc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4210782 163372 0 5HT7R 5-HT7 receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay
ChEMBL 227 1 2 2 2.1 Cc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
135367405 163372 0 5HT7R 5-HT7 receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay
ChEMBL 227 1 2 2 2.1 Cc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4210782 163372 0 5HT7R 5-HT7 receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay
ChEMBL 227 1 2 2 2.1 Cc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
5 134 60 5HT7R 5-HT7 receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human 5-HT7 expressed in HEK-293 cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human 5-HT7 expressed in HEK-293 cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm500880c
5202 134 60 5HT7R 5-HT7 receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human 5-HT7 expressed in HEK-293 cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human 5-HT7 expressed in HEK-293 cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm500880c
CHEMBL39 134 60 5HT7R 5-HT7 receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human 5-HT7 expressed in HEK-293 cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human 5-HT7 expressed in HEK-293 cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm500880c
DB08839 134 60 5HT7R 5-HT7 receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human 5-HT7 expressed in HEK-293 cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human 5-HT7 expressed in HEK-293 cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm500880c
11385992 84008 0 5HT7R 5-HT7 receptor Guinea pig 4.8 pEC50 = 4.8 Functional
Agonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contractionAgonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contraction
ChEMBL 439 8 1 3 5.2 O=C(CCCCCN1CCN(c2ccccc2Cl)CC1)NC1CCCc2ccccc21 10.1021/jm070487n
CHEMBL222477 84008 0 5HT7R 5-HT7 receptor Guinea pig 4.8 pEC50 = 4.8 Functional
Agonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contractionAgonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contraction
ChEMBL 439 8 1 3 5.2 O=C(CCCCCN1CCN(c2ccccc2Cl)CC1)NC1CCCc2ccccc21 10.1021/jm070487n
23643664 2212 5 5HT7R 5-HT7 receptor Guinea pig 5.8 pEC50 = 5.8 Functional
Agonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contractionAgonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contraction
ChEMBL 481 9 1 3 6.2 O=C(NC1CCCc2c1cccc2)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1021/jm070487n
8434 2212 5 5HT7R 5-HT7 receptor Guinea pig 5.8 pEC50 = 5.8 Functional
Agonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contractionAgonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contraction
ChEMBL 481 9 1 3 6.2 O=C(NC1CCCc2c1cccc2)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1021/jm070487n
CHEMBL243954 2212 5 5HT7R 5-HT7 receptor Guinea pig 5.8 pEC50 = 5.8 Functional
Agonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contractionAgonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contraction
ChEMBL 481 9 1 3 6.2 O=C(NC1CCCc2c1cccc2)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1021/jm070487n
11785183 84052 0 5HT7R 5-HT7 receptor Human 5.7 pEC50 = 5.7 Functional
Activity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileumActivity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileum
ChEMBL 419 8 1 3 4.9 Cc1ccccc1N1CCN(CCCCCC(=O)NC2CCCc3ccccc32)CC1 10.1021/jm049702f
CHEMBL222755 84052 0 5HT7R 5-HT7 receptor Human 5.7 pEC50 = 5.7 Functional
Activity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileumActivity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileum
ChEMBL 419 8 1 3 4.9 Cc1ccccc1N1CCN(CCCCCC(=O)NC2CCCc3ccccc32)CC1 10.1021/jm049702f
124247485 163244 4 5HT7R 5-HT7 receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay
ChEMBL 231 1 2 2 1.9 Fc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4209274 163244 4 5HT7R 5-HT7 receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay
ChEMBL 231 1 2 2 1.9 Fc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
124247485 163244 4 5HT7R 5-HT7 receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay
ChEMBL 231 1 2 2 1.9 Fc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4209274 163244 4 5HT7R 5-HT7 receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay
ChEMBL 231 1 2 2 1.9 Fc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
102364516 112804 0 5HT7R 5-HT7 receptor Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT7 expressed in HEK-293 cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human 5-HT7 expressed in HEK-293 cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 346 6 0 2 4.0 O=C1Cc2ccccc2N1CC/C=C/CCN1CCc2ccccc2C1 10.1021/jm500880c
CHEMBL3321794 112804 0 5HT7R 5-HT7 receptor Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT7 expressed in HEK-293 cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human 5-HT7 expressed in HEK-293 cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 346 6 0 2 4.0 O=C1Cc2ccccc2N1CC/C=C/CCN1CCc2ccccc2C1 10.1021/jm500880c
11282296 142513 0 5HT7R 5-HT7 receptor Human 5.6 pEC50 = 5.6 Functional
Activity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileumActivity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileum
ChEMBL 447 9 1 4 4.8 CC(=O)c1ccccc1N1CCN(CCCCCC(=O)NC2CCCc3ccccc32)CC1 10.1021/jm049702f
CHEMBL389718 142513 0 5HT7R 5-HT7 receptor Human 5.6 pEC50 = 5.6 Functional
Activity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileumActivity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileum
ChEMBL 447 9 1 4 4.8 CC(=O)c1ccccc1N1CCN(CCCCCC(=O)NC2CCCc3ccccc32)CC1 10.1021/jm049702f
11224758 2215 2 5HT7R 5-HT7 receptor Human 5.6 pEC50 = 5.6 Functional
Activity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileumActivity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileum
ChEMBL 451 9 1 4 5.3 CSc1ccccc1N1CCN(CC1)CCCCCC(=O)NC1CCCc2c1cccc2 10.1021/jm049702f
8435 2215 2 5HT7R 5-HT7 receptor Human 5.6 pEC50 = 5.6 Functional
Activity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileumActivity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileum
ChEMBL 451 9 1 4 5.3 CSc1ccccc1N1CCN(CC1)CCCCCC(=O)NC1CCCc2c1cccc2 10.1021/jm049702f
CHEMBL225284 2215 2 5HT7R 5-HT7 receptor Human 5.6 pEC50 = 5.6 Functional
Activity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileumActivity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileum
ChEMBL 451 9 1 4 5.3 CSc1ccccc1N1CCN(CC1)CCCCCC(=O)NC1CCCc2c1cccc2 10.1021/jm049702f
25107520 184916 0 5HT7R 5-HT7 receptor Guinea pig 6.5 pEC50 = 6.5 Functional
Agonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAgonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction
ChEMBL 442 10 1 4 4.7 O=C(CCCCCN1CCN(c2ccccc2-c2ccccc2)CC1)NCc1ccncc1 10.1021/jm800615e
CHEMBL494709 184916 0 5HT7R 5-HT7 receptor Guinea pig 6.5 pEC50 = 6.5 Functional
Agonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAgonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction
ChEMBL 442 10 1 4 4.7 O=C(CCCCCN1CCN(c2ccccc2-c2ccccc2)CC1)NCc1ccncc1 10.1021/jm800615e
42625440 169974 0 5HT7R 5-HT7 receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as increase in cAMP levels by HTRF assayAgonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as increase in cAMP levels by HTRF assay
ChEMBL 320 5 0 2 3.4 O=C1Cc2ccccc2N1CCCCN1CCc2ccccc2C1 10.1021/jm8014553
CHEMBL445334 169974 0 5HT7R 5-HT7 receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as increase in cAMP levels by HTRF assayAgonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as increase in cAMP levels by HTRF assay
ChEMBL 320 5 0 2 3.4 O=C1Cc2ccccc2N1CCCCN1CCc2ccccc2C1 10.1021/jm8014553
92042877 148374 1 5HT7R 5-HT7 receptor Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assayAgonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assay
ChEMBL 241 4 1 2 3.4 CNCc1ccc(C)c(-c2ccccc2OC)c1 10.1016/j.ejmech.2016.07.029
CHEMBL3943658 148374 1 5HT7R 5-HT7 receptor Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assayAgonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assay
ChEMBL 241 4 1 2 3.4 CNCc1ccc(C)c(-c2ccccc2OC)c1 10.1016/j.ejmech.2016.07.029
92042877 148374 1 5HT7R 5-HT7 receptor Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assayAgonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assay
ChEMBL 241 4 1 2 3.4 CNCc1ccc(C)c(-c2ccccc2OC)c1 10.1016/j.ejmech.2016.07.029
CHEMBL3943658 148374 1 5HT7R 5-HT7 receptor Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assayAgonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assay
ChEMBL 241 4 1 2 3.4 CNCc1ccc(C)c(-c2ccccc2OC)c1 10.1016/j.ejmech.2016.07.029
135367857 163780 0 5HT7R 5-HT7 receptor Human 7.4 pEC50 = 7.4 Functional
Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay
ChEMBL 228 1 1 3 2.3 Cc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4215875 163780 0 5HT7R 5-HT7 receptor Human 7.4 pEC50 = 7.4 Functional
Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay
ChEMBL 228 1 1 3 2.3 Cc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
135367857 163780 0 5HT7R 5-HT7 receptor Human 7.4 pEC50 = 7.4 Functional
Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay
ChEMBL 228 1 1 3 2.3 Cc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4215875 163780 0 5HT7R 5-HT7 receptor Human 7.4 pEC50 = 7.4 Functional
Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay
ChEMBL 228 1 1 3 2.3 Cc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
5 134 60 5HT7R 5-HT7 receptor Human 7.3 pEC50 = 7.3 Functional
Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.8b00642
5202 134 60 5HT7R 5-HT7 receptor Human 7.3 pEC50 = 7.3 Functional
Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.8b00642
CHEMBL39 134 60 5HT7R 5-HT7 receptor Human 7.3 pEC50 = 7.3 Functional
Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.8b00642
DB08839 134 60 5HT7R 5-HT7 receptor Human 7.3 pEC50 = 7.3 Functional
Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.8b00642
5 134 60 5HT7R 5-HT7 receptor Human 7.3 pEC50 = 7.3 Functional
Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.8b00642
5202 134 60 5HT7R 5-HT7 receptor Human 7.3 pEC50 = 7.3 Functional
Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.8b00642
CHEMBL39 134 60 5HT7R 5-HT7 receptor Human 7.3 pEC50 = 7.3 Functional
Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.8b00642
DB08839 134 60 5HT7R 5-HT7 receptor Human 7.3 pEC50 = 7.3 Functional
Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.8b00642
25107648 184546 0 5HT7R 5-HT7 receptor Guinea pig 6.3 pEC50 = 6.3 Functional
Agonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAgonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction
ChEMBL 467 8 0 3 5.6 O=C(CCCCCN1CCN(c2ccccc2-c2ccccc2)CC1)N1CCc2ccccc2C1 10.1021/jm800615e
CHEMBL492480 184546 0 5HT7R 5-HT7 receptor Guinea pig 6.3 pEC50 = 6.3 Functional
Agonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAgonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction
ChEMBL 467 8 0 3 5.6 O=C(CCCCCN1CCN(c2ccccc2-c2ccccc2)CC1)N1CCc2ccccc2C1 10.1021/jm800615e
1809 129 22 5HT7R 5-HT7 receptor Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human 5HT7 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assayAgonist activity at human 5HT7 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1016/j.ejmech.2020.112709
4 129 22 5HT7R 5-HT7 receptor Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human 5HT7 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assayAgonist activity at human 5HT7 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1016/j.ejmech.2020.112709
CHEMBL18840 129 22 5HT7R 5-HT7 receptor Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human 5HT7 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assayAgonist activity at human 5HT7 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1016/j.ejmech.2020.112709
5 134 60 5HT7R 5-HT7 receptor Human 8.3 pEC50 = 8.3 Binding
Agonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells by LANCE TR-FRET assayAgonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells by LANCE TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2019.07.046
5202 134 60 5HT7R 5-HT7 receptor Human 8.3 pEC50 = 8.3 Binding
Agonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells by LANCE TR-FRET assayAgonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells by LANCE TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2019.07.046
CHEMBL39 134 60 5HT7R 5-HT7 receptor Human 8.3 pEC50 = 8.3 Binding
Agonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells by LANCE TR-FRET assayAgonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells by LANCE TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2019.07.046
DB08839 134 60 5HT7R 5-HT7 receptor Human 8.3 pEC50 = 8.3 Binding
Agonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells by LANCE TR-FRET assayAgonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells by LANCE TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2019.07.046
5 134 60 5HT7R 5-HT7 receptor Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells by LANCE TR-FRET assayAgonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells by LANCE TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2019.07.046
5202 134 60 5HT7R 5-HT7 receptor Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells by LANCE TR-FRET assayAgonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells by LANCE TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2019.07.046
CHEMBL39 134 60 5HT7R 5-HT7 receptor Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells by LANCE TR-FRET assayAgonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells by LANCE TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2019.07.046
DB08839 134 60 5HT7R 5-HT7 receptor Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells by LANCE TR-FRET assayAgonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells by LANCE TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2019.07.046
5 134 60 5HT7R 5-HT7 receptor Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assayAgonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2016.07.029
5202 134 60 5HT7R 5-HT7 receptor Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assayAgonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2016.07.029
CHEMBL39 134 60 5HT7R 5-HT7 receptor Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assayAgonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2016.07.029
DB08839 134 60 5HT7R 5-HT7 receptor Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assayAgonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2016.07.029
5 134 60 5HT7R 5-HT7 receptor Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assayAgonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2016.07.029
5202 134 60 5HT7R 5-HT7 receptor Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assayAgonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2016.07.029
CHEMBL39 134 60 5HT7R 5-HT7 receptor Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assayAgonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2016.07.029
DB08839 134 60 5HT7R 5-HT7 receptor Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assayAgonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2016.07.029
92042876 150534 0 5HT7R 5-HT7 receptor Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assayAgonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assay
ChEMBL 261 4 1 2 3.7 CNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1016/j.ejmech.2016.07.029
CHEMBL3961059 150534 0 5HT7R 5-HT7 receptor Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assayAgonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assay
ChEMBL 261 4 1 2 3.7 CNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1016/j.ejmech.2016.07.029
92042876 150534 0 5HT7R 5-HT7 receptor Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assayAgonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assay
ChEMBL 261 4 1 2 3.7 CNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1016/j.ejmech.2016.07.029
CHEMBL3961059 150534 0 5HT7R 5-HT7 receptor Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assayAgonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assay
ChEMBL 261 4 1 2 3.7 CNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1016/j.ejmech.2016.07.029
135453290 132819 14 5HT7R 5-HT7 receptor Human 5.3 pEC50 = 5.3 Functional
Activity at 5HT7 receptor expressed in human corneal epithelial CEPI-17-CL4 cells by adenylyl cyclase assayActivity at 5HT7 receptor expressed in human corneal epithelial CEPI-17-CL4 cells by adenylyl cyclase assay
ChEMBL 191 2 2 4 1.1 C[C@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
CHEMBL371300 132819 14 5HT7R 5-HT7 receptor Human 5.3 pEC50 = 5.3 Functional
Activity at 5HT7 receptor expressed in human corneal epithelial CEPI-17-CL4 cells by adenylyl cyclase assayActivity at 5HT7 receptor expressed in human corneal epithelial CEPI-17-CL4 cells by adenylyl cyclase assay
ChEMBL 191 2 2 4 1.1 C[C@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
118709756 112808 0 5HT7R 5-HT7 receptor Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5-HT7 expressed in HEK-293 cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human 5-HT7 expressed in HEK-293 cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 352 6 0 2 4.4 O=C1Cc2ccccc2N1CC/C=C/CCN1CC[C@H]2CCCC[C@@H]2C1 10.1021/jm500880c
CHEMBL3321798 112808 0 5HT7R 5-HT7 receptor Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5-HT7 expressed in HEK-293 cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human 5-HT7 expressed in HEK-293 cells assessed as increase in cAMP level after 45 mins by HTRF assay
ChEMBL 352 6 0 2 4.4 O=C1Cc2ccccc2N1CC/C=C/CCN1CC[C@H]2CCCC[C@@H]2C1 10.1021/jm500880c
25107716 2213 30 5HT7R 5-HT7 receptor Guinea pig 6.2 pEC50 = 6.2 Functional
Agonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAgonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1021/jm800615e
8436 2213 30 5HT7R 5-HT7 receptor Guinea pig 6.2 pEC50 = 6.2 Functional
Agonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAgonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1021/jm800615e
CHEMBL522691 2213 30 5HT7R 5-HT7 receptor Guinea pig 6.2 pEC50 = 6.2 Functional
Agonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAgonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1021/jm800615e
1809 129 22 5HT7R 5-HT7 receptor Human 6.2 pEC50 = 6.2 Functional
Activity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileumActivity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileum
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm049702f
4 129 22 5HT7R 5-HT7 receptor Human 6.2 pEC50 = 6.2 Functional
Activity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileumActivity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileum
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm049702f
CHEMBL18840 129 22 5HT7R 5-HT7 receptor Human 6.2 pEC50 = 6.2 Functional
Activity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileumActivity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileum
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm049702f
1809 129 22 5HT7R 5-HT7 receptor Guinea pig 6.2 pEC50 = 6.2 Functional
Agonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAgonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm800615e
4 129 22 5HT7R 5-HT7 receptor Guinea pig 6.2 pEC50 = 6.2 Functional
Agonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAgonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm800615e
CHEMBL18840 129 22 5HT7R 5-HT7 receptor Guinea pig 6.2 pEC50 = 6.2 Functional
Agonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAgonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm800615e
1809 129 22 5HT7R 5-HT7 receptor Guinea pig 6.2 pEC50 = 6.2 Functional
Agonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contractionAgonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contraction
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm070487n
4 129 22 5HT7R 5-HT7 receptor Guinea pig 6.2 pEC50 = 6.2 Functional
Agonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contractionAgonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contraction
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm070487n
CHEMBL18840 129 22 5HT7R 5-HT7 receptor Guinea pig 6.2 pEC50 = 6.2 Functional
Agonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contractionAgonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contraction
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm070487n
11432177 84459 0 5HT7R 5-HT7 receptor Human 5.2 pEC50 = 5.2 Functional
Activity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileumActivity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileum
ChEMBL 435 9 1 4 4.6 COc1ccccc1N1CCN(CCCCCC(=O)NC2CCCc3ccccc32)CC1 10.1021/jm049702f
CHEMBL224820 84459 0 5HT7R 5-HT7 receptor Human 5.2 pEC50 = 5.2 Functional
Activity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileumActivity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileum
ChEMBL 435 9 1 4 4.6 COc1ccccc1N1CCN(CCCCCC(=O)NC2CCCc3ccccc32)CC1 10.1021/jm049702f
5 134 60 5HT7R 5-HT7 receptor Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as increase in serotonin-induced cAMP level after 1 hr by TR-FRET assayAgonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as increase in serotonin-induced cAMP level after 1 hr by TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2018.04.059
5202 134 60 5HT7R 5-HT7 receptor Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as increase in serotonin-induced cAMP level after 1 hr by TR-FRET assayAgonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as increase in serotonin-induced cAMP level after 1 hr by TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2018.04.059
CHEMBL39 134 60 5HT7R 5-HT7 receptor Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as increase in serotonin-induced cAMP level after 1 hr by TR-FRET assayAgonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as increase in serotonin-induced cAMP level after 1 hr by TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2018.04.059
DB08839 134 60 5HT7R 5-HT7 receptor Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as increase in serotonin-induced cAMP level after 1 hr by TR-FRET assayAgonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as increase in serotonin-induced cAMP level after 1 hr by TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2018.04.059
5 134 60 5HT7R 5-HT7 receptor Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell incubated for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysisAgonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell incubated for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysis
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2020.115578
5202 134 60 5HT7R 5-HT7 receptor Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell incubated for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysisAgonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell incubated for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysis
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2020.115578
CHEMBL39 134 60 5HT7R 5-HT7 receptor Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell incubated for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysisAgonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell incubated for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysis
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2020.115578
DB08839 134 60 5HT7R 5-HT7 receptor Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell incubated for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysisAgonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell incubated for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysis
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2020.115578
11431530 83965 0 5HT7R 5-HT7 receptor Guinea pig 5.1 pEC50 = 5.1 Functional
Agonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contractionAgonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contraction
ChEMBL 405 8 1 3 4.6 O=C(CCCCCN1CCN(c2ccccc2)CC1)NC1CCCc2ccccc21 10.1021/jm070487n
CHEMBL222188 83965 0 5HT7R 5-HT7 receptor Guinea pig 5.1 pEC50 = 5.1 Functional
Agonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contractionAgonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contraction
ChEMBL 405 8 1 3 4.6 O=C(CCCCCN1CCN(c2ccccc2)CC1)NC1CCCc2ccccc21 10.1021/jm070487n
23643663 92172 0 5HT7R 5-HT7 receptor Guinea pig 6.1 pEC50 = 6.1 Functional
Agonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contractionAgonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contraction
ChEMBL 447 9 1 3 5.7 CC(C)c1ccccc1N1CCN(CCCCCC(=O)NC2CCCc3ccccc32)CC1 10.1021/jm070487n
CHEMBL243744 92172 0 5HT7R 5-HT7 receptor Guinea pig 6.1 pEC50 = 6.1 Functional
Agonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contractionAgonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contraction
ChEMBL 447 9 1 3 5.7 CC(C)c1ccccc1N1CCN(CCCCCC(=O)NC2CCCc3ccccc32)CC1 10.1021/jm070487n
5 134 60 5HT7R 5-HT7 receptor Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.03.006
5202 134 60 5HT7R 5-HT7 receptor Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.03.006
CHEMBL39 134 60 5HT7R 5-HT7 receptor Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.03.006
DB08839 134 60 5HT7R 5-HT7 receptor Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.03.006
5 134 60 5HT7R 5-HT7 receptor Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO 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 134 60 5HT7R 5-HT7 receptor Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO 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 134 60 5HT7R 5-HT7 receptor Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO 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 134 60 5HT7R 5-HT7 receptor Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO 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
5 134 60 5HT7R 5-HT7 receptor Human 9.5 pIC50 = 9.5 Binding
Binding affinity to human 5-HT7 receptor by radioligand displacement assayBinding affinity to human 5-HT7 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 134 60 5HT7R 5-HT7 receptor Human 9.5 pIC50 = 9.5 Binding
Binding affinity to human 5-HT7 receptor by radioligand displacement assayBinding affinity to human 5-HT7 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 134 60 5HT7R 5-HT7 receptor Human 9.5 pIC50 = 9.5 Binding
Binding affinity to human 5-HT7 receptor by radioligand displacement assayBinding affinity to human 5-HT7 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 134 60 5HT7R 5-HT7 receptor Human 9.5 pIC50 = 9.5 Binding
Binding affinity to human 5-HT7 receptor by radioligand displacement assayBinding affinity to human 5-HT7 receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
CHEMBL4128926 160742 0 5HT7R 5-HT7 receptor Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT7 receptor after 120 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 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
5 134 60 5HT7R 5-HT7 receptor Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO 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 134 60 5HT7R 5-HT7 receptor Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO 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 134 60 5HT7R 5-HT7 receptor Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO 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 134 60 5HT7R 5-HT7 receptor Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
5 134 60 5HT7R 5-HT7 receptor Human 9.3 pIC50 = 9.3 Binding
Binding affinity to human 5-HT7 receptor by radioligand displacement assayBinding affinity to human 5-HT7 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 134 60 5HT7R 5-HT7 receptor Human 9.3 pIC50 = 9.3 Binding
Binding affinity to human 5-HT7 receptor by radioligand displacement assayBinding affinity to human 5-HT7 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 134 60 5HT7R 5-HT7 receptor Human 9.3 pIC50 = 9.3 Binding
Binding affinity to human 5-HT7 receptor by radioligand displacement assayBinding affinity to human 5-HT7 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 134 60 5HT7R 5-HT7 receptor Human 9.3 pIC50 = 9.3 Binding
Binding affinity to human 5-HT7 receptor by radioligand displacement assayBinding affinity to human 5-HT7 receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2013.03.016
5 134 60 5HT7R 5-HT7 receptor Human 9.2 pIC50 = 9.2 Binding
Displacement of radiolabeled serotonin from human 5HT7 receptorDisplacement of radiolabeled serotonin from human 5HT7 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
5202 134 60 5HT7R 5-HT7 receptor Human 9.2 pIC50 = 9.2 Binding
Displacement of radiolabeled serotonin from human 5HT7 receptorDisplacement of radiolabeled serotonin from human 5HT7 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
CHEMBL39 134 60 5HT7R 5-HT7 receptor Human 9.2 pIC50 = 9.2 Binding
Displacement of radiolabeled serotonin from human 5HT7 receptorDisplacement of radiolabeled serotonin from human 5HT7 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
DB08839 134 60 5HT7R 5-HT7 receptor Human 9.2 pIC50 = 9.2 Binding
Displacement of radiolabeled serotonin from human 5HT7 receptorDisplacement of radiolabeled serotonin from human 5HT7 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
4106 2350 9 5HT7R 5-HT7 receptor Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at 5HT7R receptor (unknown origin) assessed as forskolin-mediated cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by TR-FRET analysisAntagonist activity at 5HT7R receptor (unknown origin) assessed as forskolin-mediated cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by TR-FRET analysis
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2019.126703
5358812 2350 9 5HT7R 5-HT7 receptor Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at 5HT7R receptor (unknown origin) assessed as forskolin-mediated cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by TR-FRET analysisAntagonist activity at 5HT7R receptor (unknown origin) assessed as forskolin-mediated cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by TR-FRET analysis
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2019.126703
89 2350 9 5HT7R 5-HT7 receptor Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at 5HT7R receptor (unknown origin) assessed as forskolin-mediated cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by TR-FRET analysisAntagonist activity at 5HT7R receptor (unknown origin) assessed as forskolin-mediated cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by TR-FRET analysis
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2019.126703
CHEMBL93240 2350 9 5HT7R 5-HT7 receptor Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at 5HT7R receptor (unknown origin) assessed as forskolin-mediated cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by TR-FRET analysisAntagonist activity at 5HT7R receptor (unknown origin) assessed as forskolin-mediated cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by TR-FRET analysis
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2019.126703
3233 3296 35 5HT7R 5-HT7 receptor Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.8b00642
3247 3296 35 5HT7R 5-HT7 receptor Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.8b00642
6604889 3296 35 5HT7R 5-HT7 receptor Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.8b00642
CHEMBL282199 3296 35 5HT7R 5-HT7 receptor Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.8b00642
DB13988 3296 35 5HT7R 5-HT7 receptor Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.8b00642
3233 3296 35 5HT7R 5-HT7 receptor Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assayAntagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmcl.2018.04.059
3247 3296 35 5HT7R 5-HT7 receptor Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assayAntagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmcl.2018.04.059
6604889 3296 35 5HT7R 5-HT7 receptor Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assayAntagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmcl.2018.04.059
CHEMBL282199 3296 35 5HT7R 5-HT7 receptor Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assayAntagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmcl.2018.04.059
DB13988 3296 35 5HT7R 5-HT7 receptor Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assayAntagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmcl.2018.04.059
3233 3296 35 5HT7R 5-HT7 receptor Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.8b00642
3247 3296 35 5HT7R 5-HT7 receptor Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.8b00642
6604889 3296 35 5HT7R 5-HT7 receptor Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.8b00642
CHEMBL282199 3296 35 5HT7R 5-HT7 receptor Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.8b00642
DB13988 3296 35 5HT7R 5-HT7 receptor Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.8b00642
4106 2350 9 5HT7R 5-HT7 receptor Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human recombinant 5-HT7 receptor assessed as inhibition of serotonin-induced cAMP accumulationAntagonist activity at human recombinant 5-HT7 receptor assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm401895u
5358812 2350 9 5HT7R 5-HT7 receptor Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human recombinant 5-HT7 receptor assessed as inhibition of serotonin-induced cAMP accumulationAntagonist activity at human recombinant 5-HT7 receptor assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm401895u
89 2350 9 5HT7R 5-HT7 receptor Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human recombinant 5-HT7 receptor assessed as inhibition of serotonin-induced cAMP accumulationAntagonist activity at human recombinant 5-HT7 receptor assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm401895u
CHEMBL93240 2350 9 5HT7R 5-HT7 receptor Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human recombinant 5-HT7 receptor assessed as inhibition of serotonin-induced cAMP accumulationAntagonist activity at human recombinant 5-HT7 receptor assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm401895u
5 134 60 5HT7R 5-HT7 receptor Human 8.8 pIC50 = 8.8 Binding
Inhibition of human 5HT7 receptorInhibition of human 5HT7 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm701575k
5202 134 60 5HT7R 5-HT7 receptor Human 8.8 pIC50 = 8.8 Binding
Inhibition of human 5HT7 receptorInhibition of human 5HT7 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm701575k
CHEMBL39 134 60 5HT7R 5-HT7 receptor Human 8.8 pIC50 = 8.8 Binding
Inhibition of human 5HT7 receptorInhibition of human 5HT7 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm701575k
DB08839 134 60 5HT7R 5-HT7 receptor Human 8.8 pIC50 = 8.8 Binding
Inhibition of human 5HT7 receptorInhibition of human 5HT7 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm701575k
11391654 179656 0 5HT7R 5-HT7 receptor Human 7.0 pIC50 = 7 Functional
Inverse agonist activity at 5-HT7 receptor (unknown origin) by cAMP functional assayInverse agonist activity at 5-HT7 receptor (unknown origin) by cAMP functional assay
ChEMBL 273 2 1 3 3.0 CC(C)n1nc2c(c1-c1ccc(F)cc1)CCNCC2 10.1016/j.bmcl.2020.127669
CHEMBL4753511 179656 0 5HT7R 5-HT7 receptor Human 7.0 pIC50 = 7 Functional
Inverse agonist activity at 5-HT7 receptor (unknown origin) by cAMP functional assayInverse agonist activity at 5-HT7 receptor (unknown origin) by cAMP functional assay
ChEMBL 273 2 1 3 3.0 CC(C)n1nc2c(c1-c1ccc(F)cc1)CCNCC2 10.1016/j.bmcl.2020.127669
11430418 18413 8 5HT7R 5-HT7 receptor Human 6.0 pIC50 = 6 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 432 6 1 7 2.5 Nn1c(CCCCN2CCN(c3ccc4ccccc4n3)CC2)nc2c(c1=O)CCCC2 10.1021/jm1002292
CHEMBL1278088 18413 8 5HT7R 5-HT7 receptor Human 6.0 pIC50 = 6 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 432 6 1 7 2.5 Nn1c(CCCCN2CCN(c3ccc4ccccc4n3)CC2)nc2c(c1=O)CCCC2 10.1021/jm1002292
44452114 159978 0 5HT7R 5-HT7 receptor Human 6.0 pIC50 = 6 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 517 8 1 6 3.9 O=C(CCCN1CCN(c2ccccc2F)CC1)NCc1nc2ccc(F)cc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
CHEMBL411442 159978 0 5HT7R 5-HT7 receptor Human 6.0 pIC50 = 6 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 517 8 1 6 3.9 O=C(CCCN1CCN(c2ccccc2F)CC1)NCc1nc2ccc(F)cc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
44452114 159978 0 5HT7R 5-HT7 receptor Human 6.0 pIC50 = 6 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 517 8 1 6 3.9 O=C(CCCN1CCN(c2ccccc2F)CC1)NCc1nc2ccc(F)cc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
CHEMBL411442 159978 0 5HT7R 5-HT7 receptor Human 6.0 pIC50 = 6 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 517 8 1 6 3.9 O=C(CCCN1CCN(c2ccccc2F)CC1)NCc1nc2ccc(F)cc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
72197486 101791 0 5HT7R 5-HT7 receptor Human 6.0 pIC50 = 6 Binding
Displacement of [3H]-LSD from human recombinant 5HT-7 receptor expressed in CHOK1 cell membranes after 120 minsDisplacement of [3H]-LSD from human recombinant 5HT-7 receptor expressed in CHOK1 cell membranes after 120 mins
ChEMBL 364 4 2 4 4.2 Clc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
CHEMBL2393245 101791 0 5HT7R 5-HT7 receptor Human 6.0 pIC50 = 6 Binding
Displacement of [3H]-LSD from human recombinant 5HT-7 receptor expressed in CHOK1 cell membranes after 120 minsDisplacement of [3H]-LSD from human recombinant 5HT-7 receptor expressed in CHOK1 cell membranes after 120 mins
ChEMBL 364 4 2 4 4.2 Clc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
CHEMBL3040361 101791 0 5HT7R 5-HT7 receptor Human 6.0 pIC50 = 6 Binding
Displacement of [3H]-LSD from human recombinant 5HT-7 receptor expressed in CHOK1 cell membranes after 120 minsDisplacement of [3H]-LSD from human recombinant 5HT-7 receptor expressed in CHOK1 cell membranes after 120 mins
ChEMBL 364 4 2 4 4.2 Clc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
49864602 15305 0 5HT7R 5-HT7 receptor Human 6.0 pIC50 = 6 Binding
Displacement of [3H]LSD from human 5HT7 expressed in CHOKI cellsDisplacement of [3H]LSD from human 5HT7 expressed in CHOKI cells
ChEMBL 373 5 0 4 3.0 CC(C)N(c1cccc(N2CCN(C)CC2)c1)S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2010.06.150
CHEMBL1222138 15305 0 5HT7R 5-HT7 receptor Human 6.0 pIC50 = 6 Binding
Displacement of [3H]LSD from human 5HT7 expressed in CHOKI cellsDisplacement of [3H]LSD from human 5HT7 expressed in CHOKI cells
ChEMBL 373 5 0 4 3.0 CC(C)N(c1cccc(N2CCN(C)CC2)c1)S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2010.06.150
127028798 137392 0 5HT7R 5-HT7 receptor Human 6.0 pIC50 = 6 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay
ChEMBL 454 6 2 5 2.4 Cc1ccc(C)c(N2CCN(CC(O)CN3C(=O)NC(C)(c4ccc(F)cc4)C3=O)CC2)c1 10.1016/j.ejmech.2016.02.024
CHEMBL3769612 137392 0 5HT7R 5-HT7 receptor Human 6.0 pIC50 = 6 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay
ChEMBL 454 6 2 5 2.4 Cc1ccc(C)c(N2CCN(CC(O)CN3C(=O)NC(C)(c4ccc(F)cc4)C3=O)CC2)c1 10.1016/j.ejmech.2016.02.024
44576978 184595 0 5HT7R 5-HT7 receptor Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membraneDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membrane
ChEMBL 457 8 1 5 3.5 COc1ccc(S(=O)(=O)NCCCN2CCN(c3ccc(Cl)c(Cl)c3)CC2)cc1 10.1016/j.bmc.2008.04.023
CHEMBL492793 184595 0 5HT7R 5-HT7 receptor Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membraneDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membrane
ChEMBL 457 8 1 5 3.5 COc1ccc(S(=O)(=O)NCCCN2CCN(c3ccc(Cl)c(Cl)c3)CC2)cc1 10.1016/j.bmc.2008.04.023
145946966 166762 0 5HT7R 5-HT7 receptor Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assayAntagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assay
ChEMBL 354 7 0 4 3.9 COc1ccccc1N1CCN(CCCOc2ccc(C)cc2C)CC1 10.1016/j.bmcl.2018.04.059
CHEMBL4209888 166762 0 5HT7R 5-HT7 receptor Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assayAntagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assay
ChEMBL 354 7 0 4 3.9 COc1ccccc1N1CCN(CCCOc2ccc(C)cc2C)CC1 10.1016/j.bmcl.2018.04.059
CHEMBL4300899 166762 0 5HT7R 5-HT7 receptor Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assayAntagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assay
ChEMBL 354 7 0 4 3.9 COc1ccccc1N1CCN(CCCOc2ccc(C)cc2C)CC1 10.1016/j.bmcl.2018.04.059
72197485 101777 0 5HT7R 5-HT7 receptor Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-LSD from human recombinant 5HT-7 receptor expressed in CHOK1 cell membranes after 120 minsDisplacement of [3H]-LSD from human recombinant 5HT-7 receptor expressed in CHOK1 cell membranes after 120 mins
ChEMBL 348 4 2 4 3.6 Fc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
CHEMBL2393244 101777 0 5HT7R 5-HT7 receptor Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-LSD from human recombinant 5HT-7 receptor expressed in CHOK1 cell membranes after 120 minsDisplacement of [3H]-LSD from human recombinant 5HT-7 receptor expressed in CHOK1 cell membranes after 120 mins
ChEMBL 348 4 2 4 3.6 Fc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
CHEMBL3040288 101777 0 5HT7R 5-HT7 receptor Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-LSD from human recombinant 5HT-7 receptor expressed in CHOK1 cell membranes after 120 minsDisplacement of [3H]-LSD from human recombinant 5HT-7 receptor expressed in CHOK1 cell membranes after 120 mins
ChEMBL 348 4 2 4 3.6 Fc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
42635388 185020 0 5HT7R 5-HT7 receptor Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membraneDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membrane
ChEMBL 471 8 1 5 3.6 COc1ccc(S(=O)(=O)NC(C)CCN2CCN(c3cccc(C(F)(F)F)c3)CC2)cc1 10.1016/j.bmc.2008.04.023
CHEMBL495250 185020 0 5HT7R 5-HT7 receptor Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membraneDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membrane
ChEMBL 471 8 1 5 3.6 COc1ccc(S(=O)(=O)NC(C)CCN2CCN(c3cccc(C(F)(F)F)c3)CC2)cc1 10.1016/j.bmc.2008.04.023
44452277 95393 0 5HT7R 5-HT7 receptor Human 7.0 pIC50 = 7.0 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 515 8 1 6 4.3 O=C(CCCN1CCN(c2cccc(Cl)c2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
CHEMBL260073 95393 0 5HT7R 5-HT7 receptor Human 7.0 pIC50 = 7.0 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 515 8 1 6 4.3 O=C(CCCN1CCN(c2cccc(Cl)c2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
44452245 95460 0 5HT7R 5-HT7 receptor Human 7.0 pIC50 = 7.0 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 573 11 1 8 4.2 CCOc1ccccc1N1CCN(CCCC(=O)NCc2nc3cc(F)ccc3c(=O)n2-c2ccccc2OC)CC1 10.1016/j.ejmech.2008.09.050
CHEMBL260514 95460 0 5HT7R 5-HT7 receptor Human 7.0 pIC50 = 7.0 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 573 11 1 8 4.2 CCOc1ccccc1N1CCN(CCCC(=O)NCc2nc3cc(F)ccc3c(=O)n2-c2ccccc2OC)CC1 10.1016/j.ejmech.2008.09.050
44452251 95548 0 5HT7R 5-HT7 receptor Human 6.0 pIC50 = 6.0 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 495 7 1 6 3.8 Cc1ccc(N2CCN(CCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)cc1C 10.1016/j.ejmech.2008.09.050
CHEMBL260901 95548 0 5HT7R 5-HT7 receptor Human 6.0 pIC50 = 6.0 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 495 7 1 6 3.8 Cc1ccc(N2CCN(CCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)cc1C 10.1016/j.ejmech.2008.09.050
44452219 160412 0 5HT7R 5-HT7 receptor Human 6.0 pIC50 = 6.0 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 529 9 1 7 3.8 COc1ccc(N2CCN(CCCC(=O)NCc3nc4cc(F)ccc4c(=O)n3-c3ccccc3)CC2)cc1 10.1016/j.ejmech.2008.09.050
CHEMBL411868 160412 0 5HT7R 5-HT7 receptor Human 6.0 pIC50 = 6.0 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 529 9 1 7 3.8 COc1ccc(N2CCN(CCCC(=O)NCc3nc4cc(F)ccc4c(=O)n3-c3ccccc3)CC2)cc1 10.1016/j.ejmech.2008.09.050
54576142 65934 0 5HT7R 5-HT7 receptor Human 8.0 pIC50 = 8.0 Binding
Inhibition of 5HT7 receptor by competition binding assayInhibition of 5HT7 receptor by competition binding assay
ChEMBL 485 7 1 5 4.7 Cc1nc(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c(C)n1-c1ccccc1 10.1021/jm200682b
CHEMBL1852341 65934 0 5HT7R 5-HT7 receptor Human 8.0 pIC50 = 8.0 Binding
Inhibition of 5HT7 receptor by competition binding assayInhibition of 5HT7 receptor by competition binding assay
ChEMBL 485 7 1 5 4.7 Cc1nc(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c(C)n1-c1ccccc1 10.1021/jm200682b
CHEMBL3216098 65934 0 5HT7R 5-HT7 receptor Human 8.0 pIC50 = 8.0 Binding
Inhibition of 5HT7 receptor by competition binding assayInhibition of 5HT7 receptor by competition binding assay
ChEMBL 485 7 1 5 4.7 Cc1nc(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c(C)n1-c1ccccc1 10.1021/jm200682b
4106 2350 9 5HT7R 5-HT7 receptor Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human 5HT7 receptor expressed in CHO-K1 cells assessed as inhibition of 5CT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5CT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT7 receptor expressed in CHO-K1 cells assessed as inhibition of 5CT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5CT addition by calcium 4 dye based FLIPR assay
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2020.112709
5358812 2350 9 5HT7R 5-HT7 receptor Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human 5HT7 receptor expressed in CHO-K1 cells assessed as inhibition of 5CT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5CT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT7 receptor expressed in CHO-K1 cells assessed as inhibition of 5CT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5CT addition by calcium 4 dye based FLIPR assay
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2020.112709
89 2350 9 5HT7R 5-HT7 receptor Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human 5HT7 receptor expressed in CHO-K1 cells assessed as inhibition of 5CT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5CT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT7 receptor expressed in CHO-K1 cells assessed as inhibition of 5CT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5CT addition by calcium 4 dye based FLIPR assay
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2020.112709
CHEMBL93240 2350 9 5HT7R 5-HT7 receptor Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human 5HT7 receptor expressed in CHO-K1 cells assessed as inhibition of 5CT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5CT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT7 receptor expressed in CHO-K1 cells assessed as inhibition of 5CT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5CT addition by calcium 4 dye based FLIPR assay
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2020.112709
24882509 95552 0 5HT7R 5-HT7 receptor Human 7.9 pIC50 = 7.9 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 543 10 1 7 4.1 CCOc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccc(F)cc3c(=O)n2-c2ccccc2)CC1 10.1016/j.ejmech.2008.09.050
CHEMBL260907 95552 0 5HT7R 5-HT7 receptor Human 7.9 pIC50 = 7.9 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 543 10 1 7 4.1 CCOc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccc(F)cc3c(=O)n2-c2ccccc2)CC1 10.1016/j.ejmech.2008.09.050
44452277 95393 0 5HT7R 5-HT7 receptor Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 515 8 1 6 4.3 O=C(CCCN1CCN(c2cccc(Cl)c2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
CHEMBL260073 95393 0 5HT7R 5-HT7 receptor Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 515 8 1 6 4.3 O=C(CCCN1CCN(c2cccc(Cl)c2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
44452245 95460 0 5HT7R 5-HT7 receptor Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 573 11 1 8 4.2 CCOc1ccccc1N1CCN(CCCC(=O)NCc2nc3cc(F)ccc3c(=O)n2-c2ccccc2OC)CC1 10.1016/j.bmc.2007.11.049
CHEMBL260514 95460 0 5HT7R 5-HT7 receptor Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 573 11 1 8 4.2 CCOc1ccccc1N1CCN(CCCC(=O)NCc2nc3cc(F)ccc3c(=O)n2-c2ccccc2OC)CC1 10.1016/j.bmc.2007.11.049
46232586 194507 0 5HT7R 5-HT7 receptor Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 473 9 0 4 4.6 O=S(=O)(c1ccc(F)cc1)N(CCCN1CCN(c2ccccc2)CC1)CC1CCCCC1 10.1016/j.bmc.2009.12.067
CHEMBL601659 194507 0 5HT7R 5-HT7 receptor Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 473 9 0 4 4.6 O=S(=O)(c1ccc(F)cc1)N(CCCN1CCN(c2ccccc2)CC1)CC1CCCCC1 10.1016/j.bmc.2009.12.067
44452251 95548 0 5HT7R 5-HT7 receptor Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 495 7 1 6 3.8 Cc1ccc(N2CCN(CCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)cc1C 10.1016/j.bmc.2007.11.049
CHEMBL260901 95548 0 5HT7R 5-HT7 receptor Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 495 7 1 6 3.8 Cc1ccc(N2CCN(CCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)cc1C 10.1016/j.bmc.2007.11.049
44452219 160412 0 5HT7R 5-HT7 receptor Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 529 9 1 7 3.8 COc1ccc(N2CCN(CCCC(=O)NCc3nc4cc(F)ccc4c(=O)n3-c3ccccc3)CC2)cc1 10.1016/j.bmc.2007.11.049
CHEMBL411868 160412 0 5HT7R 5-HT7 receptor Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 529 9 1 7 3.8 COc1ccc(N2CCN(CCCC(=O)NCc3nc4cc(F)ccc4c(=O)n3-c3ccccc3)CC2)cc1 10.1016/j.bmc.2007.11.049
135 2377 31 5HT7R 5-HT7 receptor Human 6.9 pIC50 = 6.9 Binding
Binding affinity for human cloned 5-hydroxytryptamine 7 receptorBinding affinity for human cloned 5-hydroxytryptamine 7 receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
1796 2377 31 5HT7R 5-HT7 receptor Human 6.9 pIC50 = 6.9 Binding
Binding affinity for human cloned 5-hydroxytryptamine 7 receptorBinding affinity for human cloned 5-hydroxytryptamine 7 receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
4184 2377 31 5HT7R 5-HT7 receptor Human 6.9 pIC50 = 6.9 Binding
Binding affinity for human cloned 5-hydroxytryptamine 7 receptorBinding affinity for human cloned 5-hydroxytryptamine 7 receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
CHEMBL6437 2377 31 5HT7R 5-HT7 receptor Human 6.9 pIC50 = 6.9 Binding
Binding affinity for human cloned 5-hydroxytryptamine 7 receptorBinding affinity for human cloned 5-hydroxytryptamine 7 receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
DB06148 2377 31 5HT7R 5-HT7 receptor Human 6.9 pIC50 = 6.9 Binding
Binding affinity for human cloned 5-hydroxytryptamine 7 receptorBinding affinity for human cloned 5-hydroxytryptamine 7 receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
46232818 194565 0 5HT7R 5-HT7 receptor Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 463 9 0 4 4.5 O=S(=O)(c1ccc2ccccc2c1)N(CCCN1CCN(c2ccccc2)CC1)CC1CC1 10.1016/j.bmc.2009.12.067
CHEMBL602060 194565 0 5HT7R 5-HT7 receptor Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 463 9 0 4 4.5 O=S(=O)(c1ccc2ccccc2c1)N(CCCN1CCN(c2ccccc2)CC1)CC1CC1 10.1016/j.bmc.2009.12.067
11113605 10227 0 5HT7R 5-HT7 receptor Human 5.9 pIC50 = 5.9 Binding
Inhibition of human 5-hydroxytryptamine 7 receptorInhibition of human 5-hydroxytryptamine 7 receptor
ChEMBL 480 9 0 2 5.8 O=C(CCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
CHEMBL116735 10227 0 5HT7R 5-HT7 receptor Human 5.9 pIC50 = 5.9 Binding
Inhibition of human 5-hydroxytryptamine 7 receptorInhibition of human 5-hydroxytryptamine 7 receptor
ChEMBL 480 9 0 2 5.8 O=C(CCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
44451927 95341 0 5HT7R 5-HT7 receptor Human 6.9 pIC50 = 6.9 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 529 9 1 7 3.8 COc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccc(F)cc3c(=O)n2-c2ccccc2)CC1 10.1016/j.ejmech.2008.09.050
CHEMBL259776 95341 0 5HT7R 5-HT7 receptor Human 6.9 pIC50 = 6.9 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 529 9 1 7 3.8 COc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccc(F)cc3c(=O)n2-c2ccccc2)CC1 10.1016/j.ejmech.2008.09.050
44452038 95554 0 5HT7R 5-HT7 receptor Human 5.9 pIC50 = 5.9 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 533 8 1 6 4.4 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)NCc1nc2ccc(F)cc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
CHEMBL260969 95554 0 5HT7R 5-HT7 receptor Human 5.9 pIC50 = 5.9 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 533 8 1 6 4.4 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)NCc1nc2ccc(F)cc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
155561990 174864 0 5HT7R 5-HT7 receptor Human 7.9 pIC50 = 7.9 Binding
Antagonist activity at 5-HT7 receptor (unknown origin)Antagonist activity at 5-HT7 receptor (unknown origin)
ChEMBL 557 11 1 7 4.5 CCOc1ccccc1N1CCN(CCCCC(=O)NCc2nc3cc(F)ccc3c(=O)n2-c2ccccc2)CC1 10.1016/j.ejmech.2019.111705
CHEMBL4582321 174864 0 5HT7R 5-HT7 receptor Human 7.9 pIC50 = 7.9 Binding
Antagonist activity at 5-HT7 receptor (unknown origin)Antagonist activity at 5-HT7 receptor (unknown origin)
ChEMBL 557 11 1 7 4.5 CCOc1ccccc1N1CCN(CCCCC(=O)NCc2nc3cc(F)ccc3c(=O)n2-c2ccccc2)CC1 10.1016/j.ejmech.2019.111705
24882509 95552 0 5HT7R 5-HT7 receptor Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 543 10 1 7 4.1 CCOc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccc(F)cc3c(=O)n2-c2ccccc2)CC1 10.1016/j.bmc.2007.11.049
CHEMBL260907 95552 0 5HT7R 5-HT7 receptor Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 543 10 1 7 4.1 CCOc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccc(F)cc3c(=O)n2-c2ccccc2)CC1 10.1016/j.bmc.2007.11.049
42635204 185081 0 5HT7R 5-HT7 receptor Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membraneDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membrane
ChEMBL 477 7 1 4 4.3 O=S(=O)(NCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmc.2008.04.023
CHEMBL495678 185081 0 5HT7R 5-HT7 receptor Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membraneDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membrane
ChEMBL 477 7 1 4 4.3 O=S(=O)(NCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmc.2008.04.023
46232860 194645 0 5HT7R 5-HT7 receptor Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 494 10 0 6 3.9 COc1ccccc1N1CCN(CCCN(CC2CC2)S(=O)(=O)c2cccc3cccnc23)CC1 10.1016/j.bmc.2009.12.067
CHEMBL602677 194645 0 5HT7R 5-HT7 receptor Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 494 10 0 6 3.9 COc1ccccc1N1CCN(CCCN(CC2CC2)S(=O)(=O)c2cccc3cccnc23)CC1 10.1016/j.bmc.2009.12.067
135339817 180609 0 5HT7R 5-HT7 receptor Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human 5HT7 receptor expressed in CHO-K1 cells assessed as inhibition of 5CT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5CT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT7 receptor expressed in CHO-K1 cells assessed as inhibition of 5CT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5CT addition by calcium 4 dye based FLIPR assay
ChEMBL 437 6 0 5 4.2 CN1CCc2ccc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc2C1=O 10.1016/j.ejmech.2020.112709
CHEMBL4764679 180609 0 5HT7R 5-HT7 receptor Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human 5HT7 receptor expressed in CHO-K1 cells assessed as inhibition of 5CT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5CT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT7 receptor expressed in CHO-K1 cells assessed as inhibition of 5CT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5CT addition by calcium 4 dye based FLIPR assay
ChEMBL 437 6 0 5 4.2 CN1CCc2ccc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc2C1=O 10.1016/j.ejmech.2020.112709
206 2342 7 5HT7R 5-HT7 receptor Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as inhibition of serotonon-induced increase in cAMP levels by HTRF assay relative to untreated controlAntagonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as inhibition of serotonon-induced increase in cAMP levels by HTRF assay relative to untreated control
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1021/jm8014553
68848 2342 7 5HT7R 5-HT7 receptor Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as inhibition of serotonon-induced increase in cAMP levels by HTRF assay relative to untreated controlAntagonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as inhibition of serotonon-induced increase in cAMP levels by HTRF assay relative to untreated control
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1021/jm8014553
CHEMBL12314 2342 7 5HT7R 5-HT7 receptor Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as inhibition of serotonon-induced increase in cAMP levels by HTRF assay relative to untreated controlAntagonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as inhibition of serotonon-induced increase in cAMP levels by HTRF assay relative to untreated control
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1021/jm8014553
44451927 95341 0 5HT7R 5-HT7 receptor Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 529 9 1 7 3.8 COc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccc(F)cc3c(=O)n2-c2ccccc2)CC1 10.1016/j.bmc.2007.11.049
CHEMBL259776 95341 0 5HT7R 5-HT7 receptor Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 529 9 1 7 3.8 COc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccc(F)cc3c(=O)n2-c2ccccc2)CC1 10.1016/j.bmc.2007.11.049
44452038 95554 0 5HT7R 5-HT7 receptor Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 533 8 1 6 4.4 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)NCc1nc2ccc(F)cc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
CHEMBL260969 95554 0 5HT7R 5-HT7 receptor Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 533 8 1 6 4.4 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)NCc1nc2ccc(F)cc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
46232771 194440 0 5HT7R 5-HT7 receptor Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 443 10 0 5 3.3 COc1ccc(S(=O)(=O)N(CCCN2CCN(c3ccccc3)CC2)CC2CC2)cc1 10.1016/j.bmc.2009.12.067
CHEMBL601249 194440 0 5HT7R 5-HT7 receptor Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 443 10 0 5 3.3 COc1ccc(S(=O)(=O)N(CCCN2CCN(c3ccccc3)CC2)CC2CC2)cc1 10.1016/j.bmc.2009.12.067
10067306 192457 0 5HT7R 5-HT7 receptor Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]LSD from human cloned 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human cloned 5HT7 receptor expressed in CHO cells
ChEMBL 363 5 0 5 3.1 CN(C)CCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL584046 192457 0 5HT7R 5-HT7 receptor Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]LSD from human cloned 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human cloned 5HT7 receptor expressed in CHO cells
ChEMBL 363 5 0 5 3.1 CN(C)CCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
46232622 194302 0 5HT7R 5-HT7 receptor Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 505 9 0 4 5.6 O=S(=O)(c1ccc2ccccc2c1)N(CCCN1CCN(c2ccccc2)CC1)CC1CCCCC1 10.1016/j.bmc.2009.12.067
CHEMBL600012 194302 0 5HT7R 5-HT7 receptor Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 505 9 0 4 5.6 O=S(=O)(c1ccc2ccccc2c1)N(CCCN1CCN(c2ccccc2)CC1)CC1CCCCC1 10.1016/j.bmc.2009.12.067
42635387 185014 0 5HT7R 5-HT7 receptor Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membraneDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membrane
ChEMBL 477 7 1 4 4.6 O=S(=O)(NCCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmc.2008.04.023
CHEMBL495212 185014 0 5HT7R 5-HT7 receptor Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membraneDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membrane
ChEMBL 477 7 1 4 4.6 O=S(=O)(NCCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmc.2008.04.023
46232773 194535 0 5HT7R 5-HT7 receptor Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 511 10 0 5 4.3 COc1ccc(S(=O)(=O)N(CCCN2CCN(c3cccc(C(F)(F)F)c3)CC2)CC2CC2)cc1 10.1016/j.bmc.2009.12.067
CHEMBL601855 194535 0 5HT7R 5-HT7 receptor Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 511 10 0 5 4.3 COc1ccc(S(=O)(=O)N(CCCN2CCN(c3cccc(C(F)(F)F)c3)CC2)CC2CC2)cc1 10.1016/j.bmc.2009.12.067
CHEMBL4636148 176410 0 5HT7R 5-HT7 receptor Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell preincubated for 30 mins followed by incubation with agonist for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysisAntagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell preincubated for 30 mins followed by incubation with agonist for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysis
ChEMBL 293 1 2 2 2.9 CN1CCc2cccc3c2C1Cc1ccc(NC(N)=O)cc1-3 10.1016/j.bmc.2020.115578
44452278 95394 0 5HT7R 5-HT7 receptor Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 515 8 1 6 4.3 O=C(CCCN1CCN(c2ccccc2Cl)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
CHEMBL260074 95394 0 5HT7R 5-HT7 receptor Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 515 8 1 6 4.3 O=C(CCCN1CCN(c2ccccc2Cl)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
44452039 95555 0 5HT7R 5-HT7 receptor Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 533 8 1 6 4.4 O=C(CCCN1CCN(c2cccc(Cl)c2)CC1)NCc1nc2ccc(F)cc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
CHEMBL260970 95555 0 5HT7R 5-HT7 receptor Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 533 8 1 6 4.4 O=C(CCCN1CCN(c2cccc(Cl)c2)CC1)NCc1nc2ccc(F)cc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
44452278 95394 0 5HT7R 5-HT7 receptor Human 6.9 pIC50 = 6.9 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 515 8 1 6 4.3 O=C(CCCN1CCN(c2ccccc2Cl)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
CHEMBL260074 95394 0 5HT7R 5-HT7 receptor Human 6.9 pIC50 = 6.9 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 515 8 1 6 4.3 O=C(CCCN1CCN(c2ccccc2Cl)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
44452039 95555 0 5HT7R 5-HT7 receptor Human 6.9 pIC50 = 6.9 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 533 8 1 6 4.4 O=C(CCCN1CCN(c2cccc(Cl)c2)CC1)NCc1nc2ccc(F)cc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
CHEMBL260970 95555 0 5HT7R 5-HT7 receptor Human 6.9 pIC50 = 6.9 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 533 8 1 6 4.4 O=C(CCCN1CCN(c2cccc(Cl)c2)CC1)NCc1nc2ccc(F)cc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
44451930 95079 0 5HT7R 5-HT7 receptor Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 529 9 1 7 3.8 CCOc1ccccc1N1CCN(CCC(=O)NCc2nc3ccccc3c(=O)n2-c2ccc(F)cc2)CC1 10.1016/j.bmc.2007.11.049
CHEMBL258524 95079 0 5HT7R 5-HT7 receptor Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 529 9 1 7 3.8 CCOc1ccccc1N1CCN(CCC(=O)NCc2nc3ccccc3c(=O)n2-c2ccc(F)cc2)CC1 10.1016/j.bmc.2007.11.049
44451930 95079 0 5HT7R 5-HT7 receptor Human 5.9 pIC50 = 5.9 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 529 9 1 7 3.8 CCOc1ccccc1N1CCN(CCC(=O)NCc2nc3ccccc3c(=O)n2-c2ccc(F)cc2)CC1 10.1016/j.ejmech.2008.09.050
CHEMBL258524 95079 0 5HT7R 5-HT7 receptor Human 5.9 pIC50 = 5.9 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 529 9 1 7 3.8 CCOc1ccccc1N1CCN(CCC(=O)NCc2nc3ccccc3c(=O)n2-c2ccc(F)cc2)CC1 10.1016/j.ejmech.2008.09.050
10472158 190418 0 5HT7R 5-HT7 receptor Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]LSD from human cloned 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human cloned 5HT7 receptor expressed in CHO cells
ChEMBL 335 4 1 5 2.5 NCCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565745 190418 0 5HT7R 5-HT7 receptor Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]LSD from human cloned 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human cloned 5HT7 receptor expressed in CHO cells
ChEMBL 335 4 1 5 2.5 NCCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
127028797 137541 0 5HT7R 5-HT7 receptor Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay
ChEMBL 494 6 2 5 3.1 CC1(c2ccc(F)cc2)NC(=O)N(CC(O)CN2CCN(c3cccc(Cl)c3Cl)CC2)C1=O 10.1016/j.ejmech.2016.02.024
CHEMBL3771309 137541 0 5HT7R 5-HT7 receptor Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay
ChEMBL 494 6 2 5 3.1 CC1(c2ccc(F)cc2)NC(=O)N(CC(O)CN2CCN(c3cccc(Cl)c3Cl)CC2)C1=O 10.1016/j.ejmech.2016.02.024
44452223 95305 0 5HT7R 5-HT7 receptor Human 5.9 pIC50 = 5.9 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 497 8 1 7 3.2 COc1cccc(N2CCN(CCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)c1 10.1016/j.ejmech.2008.09.050
CHEMBL259625 95305 0 5HT7R 5-HT7 receptor Human 5.9 pIC50 = 5.9 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 497 8 1 7 3.2 COc1cccc(N2CCN(CCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)c1 10.1016/j.ejmech.2008.09.050
42388965 184858 0 5HT7R 5-HT7 receptor Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membraneDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membrane
ChEMBL 427 7 1 4 3.5 O=S(=O)(NCCCN1CCN(c2ccccc2F)CC1)c1ccc2ccccc2c1 10.1016/j.bmc.2008.04.023
CHEMBL494428 184858 0 5HT7R 5-HT7 receptor Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membraneDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membrane
ChEMBL 427 7 1 4 3.5 O=S(=O)(NCCCN1CCN(c2ccccc2F)CC1)c1ccc2ccccc2c1 10.1016/j.bmc.2008.04.023
44452223 95305 0 5HT7R 5-HT7 receptor Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 497 8 1 7 3.2 COc1cccc(N2CCN(CCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)c1 10.1016/j.bmc.2007.11.049
CHEMBL259625 95305 0 5HT7R 5-HT7 receptor Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 497 8 1 7 3.2 COc1cccc(N2CCN(CCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)c1 10.1016/j.bmc.2007.11.049
53320009 56149 0 5HT7R 5-HT7 receptor Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]LSD from human 5HT7 receptor expressed in cellsDisplacement of [3H]LSD from human 5HT7 receptor expressed in cells
ChEMBL 435 3 0 5 3.4 CN1CCN(c2ccc3c(c2)N(S(=O)(=O)c2ccc4ccccc4c2)CCC3=O)CC1 10.1016/j.bmcl.2010.12.007
CHEMBL1642116 56149 0 5HT7R 5-HT7 receptor Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]LSD from human 5HT7 receptor expressed in cellsDisplacement of [3H]LSD from human 5HT7 receptor expressed in cells
ChEMBL 435 3 0 5 3.4 CN1CCN(c2ccc3c(c2)N(S(=O)(=O)c2ccc4ccccc4c2)CCC3=O)CC1 10.1016/j.bmcl.2010.12.007
169713 79515 13 5HT7R 5-HT7 receptor Human 6.8 pIC50 = 6.8 Binding
Inhibition of 5HT7 receptorInhibition of 5HT7 receptor
ChEMBL 309 3 2 2 2.6 CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2NC1 10.1016/j.bmcl.2009.09.002
CHEMBL21343 79515 13 5HT7R 5-HT7 receptor Human 6.8 pIC50 = 6.8 Binding
Inhibition of 5HT7 receptorInhibition of 5HT7 receptor
ChEMBL 309 3 2 2 2.6 CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2NC1 10.1016/j.bmcl.2009.09.002
11047568 9781 0 5HT7R 5-HT7 receptor Human 5.8 pIC50 = 5.8 Binding
Inhibition of human 5-hydroxytryptamine 7 receptorInhibition of human 5-hydroxytryptamine 7 receptor
ChEMBL 396 9 0 4 4.0 CCOc1ccc(CCOC(=O)N2CCN(CCCc3ccccc3)CC2)cc1 10.1021/jm010878g
CHEMBL115249 9781 0 5HT7R 5-HT7 receptor Human 5.8 pIC50 = 5.8 Binding
Inhibition of human 5-hydroxytryptamine 7 receptorInhibition of human 5-hydroxytryptamine 7 receptor
ChEMBL 396 9 0 4 4.0 CCOc1ccc(CCOC(=O)N2CCN(CCCc3ccccc3)CC2)cc1 10.1021/jm010878g
10885636 110289 0 5HT7R 5-HT7 receptor Human 5.8 pIC50 = 5.8 Binding
Inhibition of human 5-hydroxytryptamine 7 receptorInhibition of human 5-hydroxytryptamine 7 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 110289 0 5HT7R 5-HT7 receptor Human 5.8 pIC50 = 5.8 Binding
Inhibition of human 5-hydroxytryptamine 7 receptorInhibition of human 5-hydroxytryptamine 7 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
46232732 194510 0 5HT7R 5-HT7 receptor Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 431 9 0 4 3.4 O=S(=O)(c1ccc(F)cc1)N(CCCN1CCN(c2ccccc2)CC1)CC1CC1 10.1016/j.bmc.2009.12.067
CHEMBL601673 194510 0 5HT7R 5-HT7 receptor Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 431 9 0 4 3.4 O=S(=O)(c1ccc(F)cc1)N(CCCN1CCN(c2ccccc2)CC1)CC1CC1 10.1016/j.bmc.2009.12.067
44452276 159109 0 5HT7R 5-HT7 receptor Human 5.8 pIC50 = 5.8 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 527 8 1 6 4.4 Cc1ccc(C)c(N2CCN(CCCC(=O)NCc3nc4cc(F)ccc4c(=O)n3-c3ccccc3)CC2)c1 10.1016/j.ejmech.2008.09.050
CHEMBL410722 159109 0 5HT7R 5-HT7 receptor Human 5.8 pIC50 = 5.8 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 527 8 1 6 4.4 Cc1ccc(C)c(N2CCN(CCCC(=O)NCc3nc4cc(F)ccc4c(=O)n3-c3ccccc3)CC2)c1 10.1016/j.ejmech.2008.09.050
11536844 114381 0 5HT7R 5-HT7 receptor Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human 5-HT7 receptor expressed in CHO cells assessed as cAMP production by EIA systemAntagonist activity at human 5-HT7 receptor expressed in CHO cells assessed as cAMP production by EIA system
ChEMBL 307 1 2 2 2.1 NC(N)=NC(=O)c1ccc2c(c1)[C@]1(CCCO1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
CHEMBL3343672 114381 0 5HT7R 5-HT7 receptor Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human 5-HT7 receptor expressed in CHO cells assessed as cAMP production by EIA systemAntagonist activity at human 5-HT7 receptor expressed in CHO cells assessed as cAMP production by EIA system
ChEMBL 307 1 2 2 2.1 NC(N)=NC(=O)c1ccc2c(c1)[C@]1(CCCO1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
44452276 159109 0 5HT7R 5-HT7 receptor Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 527 8 1 6 4.4 Cc1ccc(C)c(N2CCN(CCCC(=O)NCc3nc4cc(F)ccc4c(=O)n3-c3ccccc3)CC2)c1 10.1016/j.bmc.2007.11.049
CHEMBL410722 159109 0 5HT7R 5-HT7 receptor Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 527 8 1 6 4.4 Cc1ccc(C)c(N2CCN(CCCC(=O)NCc3nc4cc(F)ccc4c(=O)n3-c3ccccc3)CC2)c1 10.1016/j.bmc.2007.11.049
12 1450 13 5HT7R 5-HT7 receptor Human 5.8 pIC50 = 5.8 Binding
Inhibitory activity against 5-hydroxytryptamine 7 receptor in humanInhibitory activity against 5-hydroxytryptamine 7 receptor in human
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1016/j.bmcl.2005.06.067
6918513 1450 13 5HT7R 5-HT7 receptor Human 5.8 pIC50 = 5.8 Binding
Inhibitory activity against 5-hydroxytryptamine 7 receptor in humanInhibitory activity against 5-hydroxytryptamine 7 receptor in human
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1016/j.bmcl.2005.06.067
CHEMBL267615 1450 13 5HT7R 5-HT7 receptor Human 5.8 pIC50 = 5.8 Binding
Inhibitory activity against 5-hydroxytryptamine 7 receptor in humanInhibitory activity against 5-hydroxytryptamine 7 receptor in human
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1016/j.bmcl.2005.06.067
46232653 194603 0 5HT7R 5-HT7 receptor Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 523 9 0 4 5.8 O=S(=O)(c1ccc2ccccc2c1)N(CCCN1CCN(c2ccc(F)cc2)CC1)CC1CCCCC1 10.1016/j.bmc.2009.12.067
CHEMBL602284 194603 0 5HT7R 5-HT7 receptor Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 523 9 0 4 5.8 O=S(=O)(c1ccc2ccccc2c1)N(CCCN1CCN(c2ccc(F)cc2)CC1)CC1CCCCC1 10.1016/j.bmc.2009.12.067
46232730 194476 0 5HT7R 5-HT7 receptor Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 463 9 0 4 4.5 O=S(=O)(c1cccc2ccccc12)N(CCCN1CCN(c2ccccc2)CC1)CC1CC1 10.1016/j.bmc.2009.12.067
CHEMBL601457 194476 0 5HT7R 5-HT7 receptor Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 463 9 0 4 4.5 O=S(=O)(c1cccc2ccccc12)N(CCCN1CCN(c2ccccc2)CC1)CC1CC1 10.1016/j.bmc.2009.12.067
72197484 101782 0 5HT7R 5-HT7 receptor Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-LSD from human recombinant 5HT-7 receptor expressed in CHOK1 cell membranes after 120 minsDisplacement of [3H]-LSD from human recombinant 5HT-7 receptor expressed in CHOK1 cell membranes after 120 mins
ChEMBL 330 4 2 4 3.5 c1ccc(Cc2nc3c(c(Nc4ccccc4)n2)CCNCC3)cc1 10.1016/j.ejmech.2013.02.020
CHEMBL2393243 101782 0 5HT7R 5-HT7 receptor Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-LSD from human recombinant 5HT-7 receptor expressed in CHOK1 cell membranes after 120 minsDisplacement of [3H]-LSD from human recombinant 5HT-7 receptor expressed in CHOK1 cell membranes after 120 mins
ChEMBL 330 4 2 4 3.5 c1ccc(Cc2nc3c(c(Nc4ccccc4)n2)CCNCC3)cc1 10.1016/j.ejmech.2013.02.020
CHEMBL3040324 101782 0 5HT7R 5-HT7 receptor Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-LSD from human recombinant 5HT-7 receptor expressed in CHOK1 cell membranes after 120 minsDisplacement of [3H]-LSD from human recombinant 5HT-7 receptor expressed in CHOK1 cell membranes after 120 mins
ChEMBL 330 4 2 4 3.5 c1ccc(Cc2nc3c(c(Nc4ccccc4)n2)CCNCC3)cc1 10.1016/j.ejmech.2013.02.020
18180076 15242 0 5HT7R 5-HT7 receptor Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]LSD from human 5HT7 expressed in CHOKI cellsDisplacement of [3H]LSD from human 5HT7 expressed in CHOKI cells
ChEMBL 381 4 1 4 3.4 CN1CCN(c2cccc(NS(=O)(=O)c3ccc4ccccc4c3)c2)CC1 10.1016/j.bmcl.2010.06.150
CHEMBL1221497 15242 0 5HT7R 5-HT7 receptor Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]LSD from human 5HT7 expressed in CHOKI cellsDisplacement of [3H]LSD from human 5HT7 expressed in CHOKI cells
ChEMBL 381 4 1 4 3.4 CN1CCN(c2cccc(NS(=O)(=O)c3ccc4ccccc4c3)c2)CC1 10.1016/j.bmcl.2010.06.150
44452247 95500 0 5HT7R 5-HT7 receptor Human 6.8 pIC50 = 6.8 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 549 8 1 6 4.9 O=C(CCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
CHEMBL260706 95500 0 5HT7R 5-HT7 receptor Human 6.8 pIC50 = 6.8 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 549 8 1 6 4.9 O=C(CCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
11500509 119814 0 5HT7R 5-HT7 receptor Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human 5-HT7 receptor expressed in CHO cells assessed as cAMP production by EIA systemAntagonist activity at human 5-HT7 receptor expressed in CHO cells assessed as cAMP production by EIA system
ChEMBL 307 1 2 2 2.1 NC(N)=NC(=O)c1ccc2c(c1)C1(CCCO1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
CHEMBL3343670 119814 0 5HT7R 5-HT7 receptor Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human 5-HT7 receptor expressed in CHO cells assessed as cAMP production by EIA systemAntagonist activity at human 5-HT7 receptor expressed in CHO cells assessed as cAMP production by EIA system
ChEMBL 307 1 2 2 2.1 NC(N)=NC(=O)c1ccc2c(c1)C1(CCCO1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
CHEMBL3545812 119814 0 5HT7R 5-HT7 receptor Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human 5-HT7 receptor expressed in CHO cells assessed as cAMP production by EIA systemAntagonist activity at human 5-HT7 receptor expressed in CHO cells assessed as cAMP production by EIA system
ChEMBL 307 1 2 2 2.1 NC(N)=NC(=O)c1ccc2c(c1)C1(CCCO1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
44452115 95691 0 5HT7R 5-HT7 receptor Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 573 11 1 8 4.2 CCOc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccc(F)cc3c(=O)n2-c2cccc(OC)c2)CC1 10.1016/j.bmc.2007.11.049
CHEMBL261742 95691 0 5HT7R 5-HT7 receptor Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 573 11 1 8 4.2 CCOc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccc(F)cc3c(=O)n2-c2cccc(OC)c2)CC1 10.1016/j.bmc.2007.11.049
44451980 155212 0 5HT7R 5-HT7 receptor Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 573 11 1 8 4.2 CCOc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccc(F)cc3c(=O)n2-c2ccc(OC)cc2)CC1 10.1016/j.bmc.2007.11.049
CHEMBL406221 155212 0 5HT7R 5-HT7 receptor Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 573 11 1 8 4.2 CCOc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccc(F)cc3c(=O)n2-c2ccc(OC)cc2)CC1 10.1016/j.bmc.2007.11.049
44452115 95691 0 5HT7R 5-HT7 receptor Human 7.8 pIC50 = 7.8 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 573 11 1 8 4.2 CCOc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccc(F)cc3c(=O)n2-c2cccc(OC)c2)CC1 10.1016/j.ejmech.2008.09.050
CHEMBL261742 95691 0 5HT7R 5-HT7 receptor Human 7.8 pIC50 = 7.8 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 573 11 1 8 4.2 CCOc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccc(F)cc3c(=O)n2-c2cccc(OC)c2)CC1 10.1016/j.ejmech.2008.09.050
44451980 155212 0 5HT7R 5-HT7 receptor Human 7.8 pIC50 = 7.8 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 573 11 1 8 4.2 CCOc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccc(F)cc3c(=O)n2-c2ccc(OC)cc2)CC1 10.1016/j.ejmech.2008.09.050
CHEMBL406221 155212 0 5HT7R 5-HT7 receptor Human 7.8 pIC50 = 7.8 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 573 11 1 8 4.2 CCOc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccc(F)cc3c(=O)n2-c2ccc(OC)cc2)CC1 10.1016/j.ejmech.2008.09.050
44452247 95500 0 5HT7R 5-HT7 receptor Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 549 8 1 6 4.9 O=C(CCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
CHEMBL260706 95500 0 5HT7R 5-HT7 receptor Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 549 8 1 6 4.9 O=C(CCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
46232690 194544 0 5HT7R 5-HT7 receptor Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 574 9 0 5 6.0 O=S(=O)(c1cccc2cccnc12)N(CCCN1CCN(c2cccc(C(F)(F)F)c2)CC1)CC1CCCCC1 10.1016/j.bmc.2009.12.067
CHEMBL601886 194544 0 5HT7R 5-HT7 receptor Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 574 9 0 5 6.0 O=S(=O)(c1cccc2cccnc12)N(CCCN1CCN(c2cccc(C(F)(F)F)c2)CC1)CC1CCCCC1 10.1016/j.bmc.2009.12.067
155568606 175260 0 5HT7R 5-HT7 receptor Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assayAntagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assay
ChEMBL 532 9 1 6 4.5 COc1ccc(/C=C2\NC(=O)N(CCCCN3CCN(c4cccc(Cl)c4Cl)CC3)C2=O)cc1OC 10.1016/j.bmc.2019.07.046
CHEMBL4591601 175260 0 5HT7R 5-HT7 receptor Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assayAntagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assay
ChEMBL 532 9 1 6 4.5 COc1ccc(/C=C2\NC(=O)N(CCCCN3CCN(c4cccc(Cl)c4Cl)CC3)C2=O)cc1OC 10.1016/j.bmc.2019.07.046
155568606 175260 0 5HT7R 5-HT7 receptor Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assayAntagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assay
ChEMBL 532 9 1 6 4.5 COc1ccc(/C=C2\NC(=O)N(CCCCN3CCN(c4cccc(Cl)c4Cl)CC3)C2=O)cc1OC 10.1016/j.bmc.2019.07.046
CHEMBL4591601 175260 0 5HT7R 5-HT7 receptor Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assayAntagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assay
ChEMBL 532 9 1 6 4.5 COc1ccc(/C=C2\NC(=O)N(CCCCN3CCN(c4cccc(Cl)c4Cl)CC3)C2=O)cc1OC 10.1016/j.bmc.2019.07.046
11957735 193607 0 5HT7R 5-HT7 receptor Human 5.8 pIC50 = 5.8 Binding
Inhibition of 5HT7 receptorInhibition of 5HT7 receptor
ChEMBL 350 4 1 5 4.0 CN(C)Cc1nc(-c2ccc(C(C)(C)C)cc2)n(-c2cccc(O)c2)n1 10.1016/j.bmc.2009.07.007
CHEMBL595449 193607 0 5HT7R 5-HT7 receptor Human 5.8 pIC50 = 5.8 Binding
Inhibition of 5HT7 receptorInhibition of 5HT7 receptor
ChEMBL 350 4 1 5 4.0 CN(C)Cc1nc(-c2ccc(C(C)(C)C)cc2)n(-c2cccc(O)c2)n1 10.1016/j.bmc.2009.07.007
46232589 194398 0 5HT7R 5-HT7 receptor Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 515 11 0 6 4.5 COc1ccc(S(=O)(=O)N(CCCN2CCN(c3ccccc3OC)CC2)CC2CCCCC2)cc1 10.1016/j.bmc.2009.12.067
CHEMBL600822 194398 0 5HT7R 5-HT7 receptor Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 515 11 0 6 4.5 COc1ccc(S(=O)(=O)N(CCCN2CCN(c3ccccc3OC)CC2)CC2CCCCC2)cc1 10.1016/j.bmc.2009.12.067
19426635 199151 0 5HT7R 5-HT7 receptor Human 7.7 pIC50 = 7.7 Binding
Binding affinity for human cloned 5-hydroxytryptamine 7 receptorBinding affinity for human cloned 5-hydroxytryptamine 7 receptor
ChEMBL 280 2 1 3 3.1 CNCC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL81485 199151 0 5HT7R 5-HT7 receptor Human 7.7 pIC50 = 7.7 Binding
Binding affinity for human cloned 5-hydroxytryptamine 7 receptorBinding affinity for human cloned 5-hydroxytryptamine 7 receptor
ChEMBL 280 2 1 3 3.1 CNCC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
73351903 89025 0 5HT7R 5-HT7 receptor Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]LSD from human 5HT7 receptorDisplacement of [3H]LSD from human 5HT7 receptor
ChEMBL 360 3 2 4 3.1 Cc1[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376484 89025 0 5HT7R 5-HT7 receptor Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]LSD from human 5HT7 receptorDisplacement of [3H]LSD from human 5HT7 receptor
ChEMBL 360 3 2 4 3.1 Cc1[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
127029652 137536 0 5HT7R 5-HT7 receptor Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay
ChEMBL 516 8 2 5 3.4 CC1(c2ccc(F)cc2)NC(=O)N(CC(O)CN2CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O 10.1016/j.ejmech.2016.02.024
CHEMBL3771222 137536 0 5HT7R 5-HT7 receptor Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay
ChEMBL 516 8 2 5 3.4 CC1(c2ccc(F)cc2)NC(=O)N(CC(O)CN2CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O 10.1016/j.ejmech.2016.02.024
145947937 166888 0 5HT7R 5-HT7 receptor Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assayAntagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assay
ChEMBL 398 9 0 5 3.8 COc1ccccc1N1CCN(CCOCCOc2c(C)cc(C)cc2C)CC1 10.1016/j.bmcl.2018.04.059
CHEMBL4207653 166888 0 5HT7R 5-HT7 receptor Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assayAntagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assay
ChEMBL 398 9 0 5 3.8 COc1ccccc1N1CCN(CCOCCOc2c(C)cc(C)cc2C)CC1 10.1016/j.bmcl.2018.04.059
CHEMBL4302655 166888 0 5HT7R 5-HT7 receptor Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assayAntagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assay
ChEMBL 398 9 0 5 3.8 COc1ccccc1N1CCN(CCOCCOc2c(C)cc(C)cc2C)CC1 10.1016/j.bmcl.2018.04.059
46232819 194738 0 5HT7R 5-HT7 receptor Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 493 10 0 5 4.5 COc1ccccc1N1CCN(CCCN(CC2CC2)S(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmc.2009.12.067
CHEMBL603272 194738 0 5HT7R 5-HT7 receptor Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 493 10 0 5 4.5 COc1ccccc1N1CCN(CCCN(CC2CC2)S(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmc.2009.12.067
44452166 95125 0 5HT7R 5-HT7 receptor Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 543 10 1 7 4.1 CCOc1ccccc1N1CCN(CCCC(=O)NCc2nc3cc(F)ccc3c(=O)n2-c2ccccc2)CC1 10.1016/j.bmc.2007.11.049
CHEMBL258785 95125 0 5HT7R 5-HT7 receptor Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 543 10 1 7 4.1 CCOc1ccccc1N1CCN(CCCC(=O)NCc2nc3cc(F)ccc3c(=O)n2-c2ccccc2)CC1 10.1016/j.bmc.2007.11.049
44452166 95125 0 5HT7R 5-HT7 receptor Human 7.7 pIC50 = 7.7 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 543 10 1 7 4.1 CCOc1ccccc1N1CCN(CCCC(=O)NCc2nc3cc(F)ccc3c(=O)n2-c2ccccc2)CC1 10.1016/j.ejmech.2008.09.050
CHEMBL258785 95125 0 5HT7R 5-HT7 receptor Human 7.7 pIC50 = 7.7 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 543 10 1 7 4.1 CCOc1ccccc1N1CCN(CCCC(=O)NCc2nc3cc(F)ccc3c(=O)n2-c2ccccc2)CC1 10.1016/j.ejmech.2008.09.050
44452005 95259 0 5HT7R 5-HT7 receptor Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 559 10 1 8 3.8 COc1ccc(-n2c(CNC(=O)CCCN3CCN(c4ccccc4OC)CC3)nc3ccc(F)cc3c2=O)cc1 10.1016/j.bmc.2007.11.049
CHEMBL259407 95259 0 5HT7R 5-HT7 receptor Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 559 10 1 8 3.8 COc1ccc(-n2c(CNC(=O)CCCN3CCN(c4ccccc4OC)CC3)nc3ccc(F)cc3c2=O)cc1 10.1016/j.bmc.2007.11.049
44451954 159550 0 5HT7R 5-HT7 receptor Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 533 8 1 6 4.4 O=C(CCCN1CCN(c2cccc(Cl)c2)CC1)NCc1nc2cc(F)ccc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
CHEMBL411105 159550 0 5HT7R 5-HT7 receptor Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 533 8 1 6 4.4 O=C(CCCN1CCN(c2cccc(Cl)c2)CC1)NCc1nc2cc(F)ccc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
44452005 95259 0 5HT7R 5-HT7 receptor Human 6.7 pIC50 = 6.7 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 559 10 1 8 3.8 COc1ccc(-n2c(CNC(=O)CCCN3CCN(c4ccccc4OC)CC3)nc3ccc(F)cc3c2=O)cc1 10.1016/j.ejmech.2008.09.050
CHEMBL259407 95259 0 5HT7R 5-HT7 receptor Human 6.7 pIC50 = 6.7 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 559 10 1 8 3.8 COc1ccc(-n2c(CNC(=O)CCCN3CCN(c4ccccc4OC)CC3)nc3ccc(F)cc3c2=O)cc1 10.1016/j.ejmech.2008.09.050
44451954 159550 0 5HT7R 5-HT7 receptor Human 6.7 pIC50 = 6.7 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 533 8 1 6 4.4 O=C(CCCN1CCN(c2cccc(Cl)c2)CC1)NCc1nc2cc(F)ccc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
CHEMBL411105 159550 0 5HT7R 5-HT7 receptor Human 6.7 pIC50 = 6.7 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 533 8 1 6 4.4 O=C(CCCN1CCN(c2cccc(Cl)c2)CC1)NCc1nc2cc(F)ccc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
46232559 194678 0 5HT7R 5-HT7 receptor Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 505 9 0 4 5.6 O=S(=O)(c1cccc2ccccc12)N(CCCN1CCN(c2ccccc2)CC1)CC1CCCCC1 10.1016/j.bmc.2009.12.067
CHEMBL602882 194678 0 5HT7R 5-HT7 receptor Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 505 9 0 4 5.6 O=S(=O)(c1cccc2ccccc12)N(CCCN1CCN(c2ccccc2)CC1)CC1CCCCC1 10.1016/j.bmc.2009.12.067
134141985 146375 0 5HT7R 5-HT7 receptor Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay
ChEMBL 432 6 0 6 4.4 COc1ccccc1-c1cc(CN2CCN(c3ccccc3OC)CC2)cc2c1OCO2 10.1016/j.ejmech.2016.07.029
CHEMBL3927929 146375 0 5HT7R 5-HT7 receptor Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay
ChEMBL 432 6 0 6 4.4 COc1ccccc1-c1cc(CN2CCN(c3ccccc3OC)CC2)cc2c1OCO2 10.1016/j.ejmech.2016.07.029
44452196 95343 0 5HT7R 5-HT7 receptor Human 6.7 pIC50 = 6.7 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 509 8 1 6 4.2 Cc1ccc(N2CCN(CCCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)cc1C 10.1016/j.ejmech.2008.09.050
CHEMBL259827 95343 0 5HT7R 5-HT7 receptor Human 6.7 pIC50 = 6.7 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 509 8 1 6 4.2 Cc1ccc(N2CCN(CCCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)cc1C 10.1016/j.ejmech.2008.09.050
44451953 95592 0 5HT7R 5-HT7 receptor Human 6.7 pIC50 = 6.7 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 527 8 1 6 4.4 Cc1ccc(C)c(N2CCN(CCCC(=O)NCc3nc4ccc(F)cc4c(=O)n3-c3ccccc3)CC2)c1 10.1016/j.ejmech.2008.09.050
CHEMBL261149 95592 0 5HT7R 5-HT7 receptor Human 6.7 pIC50 = 6.7 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 527 8 1 6 4.4 Cc1ccc(C)c(N2CCN(CCCC(=O)NCc3nc4ccc(F)cc4c(=O)n3-c3ccccc3)CC2)c1 10.1016/j.ejmech.2008.09.050
44452080 154968 0 5HT7R 5-HT7 receptor Human 6.7 pIC50 = 6.7 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 533 8 1 6 4.4 O=C(CCCN1CCN(c2ccccc2Cl)CC1)NCc1nc2ccc(F)cc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
CHEMBL405892 154968 0 5HT7R 5-HT7 receptor Human 6.7 pIC50 = 6.7 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 533 8 1 6 4.4 O=C(CCCN1CCN(c2ccccc2Cl)CC1)NCc1nc2ccc(F)cc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
134141985 146375 0 5HT7R 5-HT7 receptor Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay
ChEMBL 432 6 0 6 4.4 COc1ccccc1-c1cc(CN2CCN(c3ccccc3OC)CC2)cc2c1OCO2 10.1016/j.ejmech.2016.07.029
CHEMBL3927929 146375 0 5HT7R 5-HT7 receptor Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay
ChEMBL 432 6 0 6 4.4 COc1ccccc1-c1cc(CN2CCN(c3ccccc3OC)CC2)cc2c1OCO2 10.1016/j.ejmech.2016.07.029
44452144 95613 0 5HT7R 5-HT7 receptor Human 5.7 pIC50 = 5.7 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 511 9 1 7 3.6 COc1ccc(N2CCN(CCCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)cc1 10.1016/j.ejmech.2008.09.050
CHEMBL261232 95613 0 5HT7R 5-HT7 receptor Human 5.7 pIC50 = 5.7 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 511 9 1 7 3.6 COc1ccc(N2CCN(CCCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)cc1 10.1016/j.ejmech.2008.09.050
44348383 15944 0 5HT7R 5-HT7 receptor Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human 5HT7 receptor expressed in HEK293 assessed as inhibition of 5HT-induced cAMP accumulationAntagonist activity at human 5HT7 receptor expressed in HEK293 assessed as inhibition of 5HT-induced cAMP accumulation
ChEMBL 205 3 1 2 2.7 CSc1ccc2c(c1)C(CCN)=CC2 10.1016/j.ejmech.2012.11.042
CHEMBL122536 15944 0 5HT7R 5-HT7 receptor Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human 5HT7 receptor expressed in HEK293 assessed as inhibition of 5HT-induced cAMP accumulationAntagonist activity at human 5HT7 receptor expressed in HEK293 assessed as inhibition of 5HT-induced cAMP accumulation
ChEMBL 205 3 1 2 2.7 CSc1ccc2c(c1)C(CCN)=CC2 10.1016/j.ejmech.2012.11.042
5 134 60 5HT7R 5-HT7 receptor Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/np0205102
5202 134 60 5HT7R 5-HT7 receptor Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/np0205102
CHEMBL39 134 60 5HT7R 5-HT7 receptor Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/np0205102
DB08839 134 60 5HT7R 5-HT7 receptor Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/np0205102
3233 3296 35 5HT7R 5-HT7 receptor Human 8.6 pIC50 = 8.6 Binding
Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assayAntagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2019.07.046
3247 3296 35 5HT7R 5-HT7 receptor Human 8.6 pIC50 = 8.6 Binding
Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assayAntagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2019.07.046
6604889 3296 35 5HT7R 5-HT7 receptor Human 8.6 pIC50 = 8.6 Binding
Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assayAntagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2019.07.046
CHEMBL282199 3296 35 5HT7R 5-HT7 receptor Human 8.6 pIC50 = 8.6 Binding
Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assayAntagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2019.07.046
DB13988 3296 35 5HT7R 5-HT7 receptor Human 8.6 pIC50 = 8.6 Binding
Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assayAntagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2019.07.046
3233 3296 35 5HT7R 5-HT7 receptor Human 8.6 pIC50 = 8.6 Binding
Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assayAntagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2019.07.046
3247 3296 35 5HT7R 5-HT7 receptor Human 8.6 pIC50 = 8.6 Binding
Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assayAntagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2019.07.046
6604889 3296 35 5HT7R 5-HT7 receptor Human 8.6 pIC50 = 8.6 Binding
Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assayAntagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2019.07.046
CHEMBL282199 3296 35 5HT7R 5-HT7 receptor Human 8.6 pIC50 = 8.6 Binding
Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assayAntagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2019.07.046
DB13988 3296 35 5HT7R 5-HT7 receptor Human 8.6 pIC50 = 8.6 Binding
Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assayAntagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2019.07.046
42388639 185376 0 5HT7R 5-HT7 receptor Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membraneDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membrane
ChEMBL 439 8 1 5 3.3 COc1ccccc1N1CCN(CCCNS(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmc.2008.04.023
CHEMBL497749 185376 0 5HT7R 5-HT7 receptor Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membraneDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membrane
ChEMBL 439 8 1 5 3.3 COc1ccccc1N1CCN(CCCNS(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmc.2008.04.023
44452170 166163 0 5HT7R 5-HT7 receptor Human 7.7 pIC50 = 7.7 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 511 9 1 7 3.6 COc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccccc3c(=O)n2-c2ccccc2)CC1 10.1016/j.ejmech.2008.09.050
CHEMBL428781 166163 0 5HT7R 5-HT7 receptor Human 7.7 pIC50 = 7.7 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 511 9 1 7 3.6 COc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccccc3c(=O)n2-c2ccccc2)CC1 10.1016/j.ejmech.2008.09.050
44452196 95343 0 5HT7R 5-HT7 receptor Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 509 8 1 6 4.2 Cc1ccc(N2CCN(CCCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)cc1C 10.1016/j.bmc.2007.11.049
CHEMBL259827 95343 0 5HT7R 5-HT7 receptor Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 509 8 1 6 4.2 Cc1ccc(N2CCN(CCCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)cc1C 10.1016/j.bmc.2007.11.049
44451953 95592 0 5HT7R 5-HT7 receptor Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 527 8 1 6 4.4 Cc1ccc(C)c(N2CCN(CCCC(=O)NCc3nc4ccc(F)cc4c(=O)n3-c3ccccc3)CC2)c1 10.1016/j.bmc.2007.11.049
CHEMBL261149 95592 0 5HT7R 5-HT7 receptor Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 527 8 1 6 4.4 Cc1ccc(C)c(N2CCN(CCCC(=O)NCc3nc4ccc(F)cc4c(=O)n3-c3ccccc3)CC2)c1 10.1016/j.bmc.2007.11.049
44452080 154968 0 5HT7R 5-HT7 receptor Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 533 8 1 6 4.4 O=C(CCCN1CCN(c2ccccc2Cl)CC1)NCc1nc2ccc(F)cc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
CHEMBL405892 154968 0 5HT7R 5-HT7 receptor Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 533 8 1 6 4.4 O=C(CCCN1CCN(c2ccccc2Cl)CC1)NCc1nc2ccc(F)cc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
44452144 95613 0 5HT7R 5-HT7 receptor Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 511 9 1 7 3.6 COc1ccc(N2CCN(CCCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)cc1 10.1016/j.bmc.2007.11.049
CHEMBL261232 95613 0 5HT7R 5-HT7 receptor Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 511 9 1 7 3.6 COc1ccc(N2CCN(CCCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)cc1 10.1016/j.bmc.2007.11.049
51003551 56156 0 5HT7R 5-HT7 receptor Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]LSD from human 5HT7 receptor expressed in cellsDisplacement of [3H]LSD from human 5HT7 receptor expressed in cells
ChEMBL 449 3 0 5 3.8 CC1CC(=O)c2c(N3CCN(C)CC3)cccc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
CHEMBL1642123 56156 0 5HT7R 5-HT7 receptor Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]LSD from human 5HT7 receptor expressed in cellsDisplacement of [3H]LSD from human 5HT7 receptor expressed in cells
ChEMBL 449 3 0 5 3.8 CC1CC(=O)c2c(N3CCN(C)CC3)cccc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
10907460 9555 0 5HT7R 5-HT7 receptor Human 5.7 pIC50 = 5.7 Binding
Inhibition of human 5-hydroxytryptamine 7 receptorInhibition of human 5-hydroxytryptamine 7 receptor
ChEMBL 521 11 1 3 5.8 CCOc1ccc(CCNC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
CHEMBL113956 9555 0 5HT7R 5-HT7 receptor Human 5.7 pIC50 = 5.7 Binding
Inhibition of human 5-hydroxytryptamine 7 receptorInhibition of human 5-hydroxytryptamine 7 receptor
ChEMBL 521 11 1 3 5.8 CCOc1ccc(CCNC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
49864292 15235 0 5HT7R 5-HT7 receptor Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]LSD from human 5HT7 expressed in CHOKI cellsDisplacement of [3H]LSD from human 5HT7 expressed in CHOKI cells
ChEMBL 471 6 0 4 5.0 CN1CCN(c2cccc(N(Cc3ccccc3)S(=O)(=O)c3ccc4ccccc4c3)c2)CC1 10.1016/j.bmcl.2010.06.150
CHEMBL1221452 15235 0 5HT7R 5-HT7 receptor Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]LSD from human 5HT7 expressed in CHOKI cellsDisplacement of [3H]LSD from human 5HT7 expressed in CHOKI cells
ChEMBL 471 6 0 4 5.0 CN1CCN(c2cccc(N(Cc3ccccc3)S(=O)(=O)c3ccc4ccccc4c3)c2)CC1 10.1016/j.bmcl.2010.06.150
49864724 15333 0 5HT7R 5-HT7 receptor Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]LSD from human 5HT7 expressed in CHOKI cellsDisplacement of [3H]LSD from human 5HT7 expressed in CHOKI cells
ChEMBL 409 5 0 4 3.8 CCN(c1cccc(N2CCN(C)CC2)c1)S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.150
CHEMBL1222364 15333 0 5HT7R 5-HT7 receptor Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]LSD from human 5HT7 expressed in CHOKI cellsDisplacement of [3H]LSD from human 5HT7 expressed in CHOKI cells
ChEMBL 409 5 0 4 3.8 CCN(c1cccc(N2CCN(C)CC2)c1)S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.150
44452274 95549 0 5HT7R 5-HT7 receptor Human 6.7 pIC50 = 6.7 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 541 10 1 8 3.6 COc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccccc3c(=O)n2-c2ccccc2OC)CC1 10.1016/j.ejmech.2008.09.050
CHEMBL260902 95549 0 5HT7R 5-HT7 receptor Human 6.7 pIC50 = 6.7 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 541 10 1 8 3.6 COc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccccc3c(=O)n2-c2ccccc2OC)CC1 10.1016/j.ejmech.2008.09.050
4106 2350 9 5HT7R 5-HT7 receptor Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2016.02.024
5358812 2350 9 5HT7R 5-HT7 receptor Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2016.02.024
89 2350 9 5HT7R 5-HT7 receptor Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2016.02.024
CHEMBL93240 2350 9 5HT7R 5-HT7 receptor Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2016.02.024
44452170 166163 0 5HT7R 5-HT7 receptor Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 511 9 1 7 3.6 COc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccccc3c(=O)n2-c2ccccc2)CC1 10.1016/j.bmc.2007.11.049
CHEMBL428781 166163 0 5HT7R 5-HT7 receptor Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 511 9 1 7 3.6 COc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccccc3c(=O)n2-c2ccccc2)CC1 10.1016/j.bmc.2007.11.049
44452274 95549 0 5HT7R 5-HT7 receptor Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 541 10 1 8 3.6 COc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccccc3c(=O)n2-c2ccccc2OC)CC1 10.1016/j.bmc.2007.11.049
CHEMBL260902 95549 0 5HT7R 5-HT7 receptor Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 541 10 1 8 3.6 COc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccccc3c(=O)n2-c2ccccc2OC)CC1 10.1016/j.bmc.2007.11.049
11730467 10745 0 5HT7R 5-HT7 receptor Human 5.7 pIC50 = 5.7 Binding
Inhibition of human 5-hydroxytryptamine 7 receptorInhibition of human 5-hydroxytryptamine 7 receptor
ChEMBL 476 10 0 2 6.0 O=C(CCCc1ccccc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
CHEMBL117537 10745 0 5HT7R 5-HT7 receptor Human 5.7 pIC50 = 5.7 Binding
Inhibition of human 5-hydroxytryptamine 7 receptorInhibition of human 5-hydroxytryptamine 7 receptor
ChEMBL 476 10 0 2 6.0 O=C(CCCc1ccccc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
155531753 170807 0 5HT7R 5-HT7 receptor Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assayAntagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assay
ChEMBL 548 11 1 7 4.5 COc1ccc(/C=C2\NC(=O)N(CCCCN3CCN(c4ccccc4OC)CC3)C2=O)cc1OC1CCCC1 10.1016/j.bmc.2019.07.046
CHEMBL4465959 170807 0 5HT7R 5-HT7 receptor Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assayAntagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assay
ChEMBL 548 11 1 7 4.5 COc1ccc(/C=C2\NC(=O)N(CCCCN3CCN(c4ccccc4OC)CC3)C2=O)cc1OC1CCCC1 10.1016/j.bmc.2019.07.046
155531753 170807 0 5HT7R 5-HT7 receptor Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assayAntagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assay
ChEMBL 548 11 1 7 4.5 COc1ccc(/C=C2\NC(=O)N(CCCCN3CCN(c4ccccc4OC)CC3)C2=O)cc1OC1CCCC1 10.1016/j.bmc.2019.07.046
CHEMBL4465959 170807 0 5HT7R 5-HT7 receptor Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assayAntagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assay
ChEMBL 548 11 1 7 4.5 COc1ccc(/C=C2\NC(=O)N(CCCCN3CCN(c4ccccc4OC)CC3)C2=O)cc1OC1CCCC1 10.1016/j.bmc.2019.07.046
44451929 95377 0 5HT7R 5-HT7 receptor Human 5.7 pIC50 = 5.7 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 533 8 1 6 4.4 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)NCc1nc2cc(F)ccc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
CHEMBL260003 95377 0 5HT7R 5-HT7 receptor Human 5.7 pIC50 = 5.7 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 533 8 1 6 4.4 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)NCc1nc2cc(F)ccc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
102364516 112804 0 5HT7R 5-HT7 receptor Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human 5-HT7 expressed in HEK-293 cells assessed as inhibition in serotonin-induced increase in cAMP level after 45 mins by HTRF assayAntagonist activity at human 5-HT7 expressed in HEK-293 cells assessed as inhibition in serotonin-induced increase in cAMP level after 45 mins by HTRF assay
ChEMBL 346 6 0 2 4.0 O=C1Cc2ccccc2N1CC/C=C/CCN1CCc2ccccc2C1 10.1021/jm500880c
CHEMBL3321794 112804 0 5HT7R 5-HT7 receptor Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human 5-HT7 expressed in HEK-293 cells assessed as inhibition in serotonin-induced increase in cAMP level after 45 mins by HTRF assayAntagonist activity at human 5-HT7 expressed in HEK-293 cells assessed as inhibition in serotonin-induced increase in cAMP level after 45 mins by HTRF assay
ChEMBL 346 6 0 2 4.0 O=C1Cc2ccccc2N1CC/C=C/CCN1CCc2ccccc2C1 10.1021/jm500880c
44451929 95377 0 5HT7R 5-HT7 receptor Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 533 8 1 6 4.4 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)NCc1nc2cc(F)ccc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
CHEMBL260003 95377 0 5HT7R 5-HT7 receptor Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 533 8 1 6 4.4 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)NCc1nc2cc(F)ccc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
42635570 184694 0 5HT7R 5-HT7 receptor Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membraneDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membrane
ChEMBL 439 8 1 5 3.3 COc1cccc(N2CCN(CCCNS(=O)(=O)c3ccc4ccccc4c3)CC2)c1 10.1016/j.bmc.2008.04.023
CHEMBL493416 184694 0 5HT7R 5-HT7 receptor Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membraneDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membrane
ChEMBL 439 8 1 5 3.3 COc1cccc(N2CCN(CCCNS(=O)(=O)c3ccc4ccccc4c3)CC2)c1 10.1016/j.bmc.2008.04.023
134157289 153279 0 5HT7R 5-HT7 receptor Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay
ChEMBL 422 6 0 4 5.3 COc1ccccc1-c1cc(CN2CCN(c3ccccc3OC)CC2)ccc1Cl 10.1016/j.ejmech.2016.07.029
CHEMBL3984812 153279 0 5HT7R 5-HT7 receptor Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay
ChEMBL 422 6 0 4 5.3 COc1ccccc1-c1cc(CN2CCN(c3ccccc3OC)CC2)ccc1Cl 10.1016/j.ejmech.2016.07.029
46232729 195040 0 5HT7R 5-HT7 receptor Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 574 9 0 5 6.3 O=S(=O)(c1cccc2cccnc12)N(CCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1)CC1CCCCC1 10.1016/j.bmc.2009.12.067
CHEMBL604952 195040 0 5HT7R 5-HT7 receptor Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 574 9 0 5 6.3 O=S(=O)(c1cccc2cccnc12)N(CCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1)CC1CCCCC1 10.1016/j.bmc.2009.12.067
44452139 95523 0 5HT7R 5-HT7 receptor Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 559 10 1 8 3.8 COc1cccc(-n2c(CNC(=O)CCCN3CCN(c4ccccc4OC)CC3)nc3ccc(F)cc3c2=O)c1 10.1016/j.bmc.2007.11.049
CHEMBL260804 95523 0 5HT7R 5-HT7 receptor Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 559 10 1 8 3.8 COc1cccc(-n2c(CNC(=O)CCCN3CCN(c4ccccc4OC)CC3)nc3ccc(F)cc3c2=O)c1 10.1016/j.bmc.2007.11.049
44452139 95523 0 5HT7R 5-HT7 receptor Human 6.6 pIC50 = 6.6 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 559 10 1 8 3.8 COc1cccc(-n2c(CNC(=O)CCCN3CCN(c4ccccc4OC)CC3)nc3ccc(F)cc3c2=O)c1 10.1016/j.ejmech.2008.09.050
CHEMBL260804 95523 0 5HT7R 5-HT7 receptor Human 6.6 pIC50 = 6.6 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 559 10 1 8 3.8 COc1cccc(-n2c(CNC(=O)CCCN3CCN(c4ccccc4OC)CC3)nc3ccc(F)cc3c2=O)c1 10.1016/j.ejmech.2008.09.050
118709756 112808 0 5HT7R 5-HT7 receptor Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human 5-HT7 expressed in HEK-293 cells assessed as inhibition in serotonin-induced increase in cAMP level after 45 mins by HTRF assayAntagonist activity at human 5-HT7 expressed in HEK-293 cells assessed as inhibition in serotonin-induced increase in cAMP level after 45 mins by HTRF assay
ChEMBL 352 6 0 2 4.4 O=C1Cc2ccccc2N1CC/C=C/CCN1CC[C@H]2CCCC[C@@H]2C1 10.1021/jm500880c
CHEMBL3321798 112808 0 5HT7R 5-HT7 receptor Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human 5-HT7 expressed in HEK-293 cells assessed as inhibition in serotonin-induced increase in cAMP level after 45 mins by HTRF assayAntagonist activity at human 5-HT7 expressed in HEK-293 cells assessed as inhibition in serotonin-induced increase in cAMP level after 45 mins by HTRF assay
ChEMBL 352 6 0 2 4.4 O=C1Cc2ccccc2N1CC/C=C/CCN1CC[C@H]2CCCC[C@@H]2C1 10.1021/jm500880c
134157289 153279 0 5HT7R 5-HT7 receptor Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay
ChEMBL 422 6 0 4 5.3 COc1ccccc1-c1cc(CN2CCN(c3ccccc3OC)CC2)ccc1Cl 10.1016/j.ejmech.2016.07.029
CHEMBL3984812 153279 0 5HT7R 5-HT7 receptor Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay
ChEMBL 422 6 0 4 5.3 COc1ccccc1-c1cc(CN2CCN(c3ccccc3OC)CC2)ccc1Cl 10.1016/j.ejmech.2016.07.029
145946714 166723 0 5HT7R 5-HT7 receptor Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assayAntagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assay
ChEMBL 398 9 0 5 3.8 COc1ccccc1N1CCN(CCOCCOc2cc(C)cc(C)c2C)CC1 10.1016/j.bmcl.2018.04.059
CHEMBL4213352 166723 0 5HT7R 5-HT7 receptor Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assayAntagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assay
ChEMBL 398 9 0 5 3.8 COc1ccccc1N1CCN(CCOCCOc2cc(C)cc(C)c2C)CC1 10.1016/j.bmcl.2018.04.059
CHEMBL4300399 166723 0 5HT7R 5-HT7 receptor Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assayAntagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assay
ChEMBL 398 9 0 5 3.8 COc1ccccc1N1CCN(CCOCCOc2cc(C)cc(C)c2C)CC1 10.1016/j.bmcl.2018.04.059
44452302 95584 0 5HT7R 5-HT7 receptor Human 5.6 pIC50 = 5.6 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 499 8 1 6 3.7 O=C(CCCN1CCN(c2ccc(F)cc2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
CHEMBL261100 95584 0 5HT7R 5-HT7 receptor Human 5.6 pIC50 = 5.6 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 499 8 1 6 3.7 O=C(CCCN1CCN(c2ccc(F)cc2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
127029650 137474 0 5HT7R 5-HT7 receptor Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay
ChEMBL 494 6 2 5 3.1 CC1(c2ccc(F)cc2)NC(=O)N(CC(O)CN2CCN(c3ccc(Cl)c(Cl)c3)CC2)C1=O 10.1016/j.ejmech.2016.02.024
CHEMBL3770581 137474 0 5HT7R 5-HT7 receptor Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay
ChEMBL 494 6 2 5 3.1 CC1(c2ccc(F)cc2)NC(=O)N(CC(O)CN2CCN(c3ccc(Cl)c(Cl)c3)CC2)C1=O 10.1016/j.ejmech.2016.02.024
46232689 194543 0 5HT7R 5-HT7 receptor Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 536 10 0 6 5.0 COc1ccccc1N1CCN(CCCN(CC2CCCCC2)S(=O)(=O)c2cccc3cccnc23)CC1 10.1016/j.bmc.2009.12.067
CHEMBL601885 194543 0 5HT7R 5-HT7 receptor Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 536 10 0 6 5.0 COc1ccccc1N1CCN(CCCN(CC2CCCCC2)S(=O)(=O)c2cccc3cccnc23)CC1 10.1016/j.bmc.2009.12.067
44452302 95584 0 5HT7R 5-HT7 receptor Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 499 8 1 6 3.7 O=C(CCCN1CCN(c2ccc(F)cc2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
CHEMBL261100 95584 0 5HT7R 5-HT7 receptor Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 499 8 1 6 3.7 O=C(CCCN1CCN(c2ccc(F)cc2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
135367820 163997 0 5HT7R 5-HT7 receptor Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay
ChEMBL 232 1 1 3 2.2 Fc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4218672 163997 0 5HT7R 5-HT7 receptor Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay
ChEMBL 232 1 1 3 2.2 Fc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
135367820 163997 0 5HT7R 5-HT7 receptor Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay
ChEMBL 232 1 1 3 2.2 Fc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4218672 163997 0 5HT7R 5-HT7 receptor Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay
ChEMBL 232 1 1 3 2.2 Fc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
44451957 157673 0 5HT7R 5-HT7 receptor Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 515 8 1 7 3.4 COc1ccc(N2CCN(CCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccc(F)cc3)CC2)cc1 10.1016/j.bmc.2007.11.049
CHEMBL409107 157673 0 5HT7R 5-HT7 receptor Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 515 8 1 7 3.4 COc1ccc(N2CCN(CCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccc(F)cc3)CC2)cc1 10.1016/j.bmc.2007.11.049
44451957 157673 0 5HT7R 5-HT7 receptor Human 5.6 pIC50 = 5.6 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 515 8 1 7 3.4 COc1ccc(N2CCN(CCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccc(F)cc3)CC2)cc1 10.1016/j.ejmech.2008.09.050
CHEMBL409107 157673 0 5HT7R 5-HT7 receptor Human 5.6 pIC50 = 5.6 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 515 8 1 7 3.4 COc1ccc(N2CCN(CCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccc(F)cc3)CC2)cc1 10.1016/j.ejmech.2008.09.050
11304851 153800 0 5HT7R 5-HT7 receptor Human 4.6 pIC50 = 4.6 Binding
Inhibition of 5HT7 receptorInhibition of 5HT7 receptor
ChEMBL 426 4 3 8 3.7 O=[N+]([O-])c1cc(O)c2c(c1)S(=O)(=O)N=C(Nc1ccccc1Oc1ccccc1)N2 10.1016/j.bmcl.2007.05.011
CHEMBL399203 153800 0 5HT7R 5-HT7 receptor Human 4.6 pIC50 = 4.6 Binding
Inhibition of 5HT7 receptorInhibition of 5HT7 receptor
ChEMBL 426 4 3 8 3.7 O=[N+]([O-])c1cc(O)c2c(c1)S(=O)(=O)N=C(Nc1ccccc1Oc1ccccc1)N2 10.1016/j.bmcl.2007.05.011
135367405 163372 0 5HT7R 5-HT7 receptor Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay
ChEMBL 227 1 2 2 2.1 Cc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4210782 163372 0 5HT7R 5-HT7 receptor Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay
ChEMBL 227 1 2 2 2.1 Cc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
135367405 163372 0 5HT7R 5-HT7 receptor Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay
ChEMBL 227 1 2 2 2.1 Cc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4210782 163372 0 5HT7R 5-HT7 receptor Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay
ChEMBL 227 1 2 2 2.1 Cc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
44452143 95612 0 5HT7R 5-HT7 receptor Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 525 10 1 7 4.0 CCOc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccccc3c(=O)n2-c2ccccc2)CC1 10.1016/j.bmc.2007.11.049
CHEMBL261231 95612 0 5HT7R 5-HT7 receptor Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 525 10 1 7 4.0 CCOc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccccc3c(=O)n2-c2ccccc2)CC1 10.1016/j.bmc.2007.11.049
44452143 95612 0 5HT7R 5-HT7 receptor Human 7.6 pIC50 = 7.6 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 525 10 1 7 4.0 CCOc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccccc3c(=O)n2-c2ccccc2)CC1 10.1016/j.ejmech.2008.09.050
CHEMBL261231 95612 0 5HT7R 5-HT7 receptor Human 7.6 pIC50 = 7.6 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 525 10 1 7 4.0 CCOc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccccc3c(=O)n2-c2ccccc2)CC1 10.1016/j.ejmech.2008.09.050
CHEMBL4633786 176280 0 5HT7R 5-HT7 receptor Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell preincubated for 30 mins followed by incubation with agonist for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysisAntagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell preincubated for 30 mins followed by incubation with agonist for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysis
ChEMBL 307 0 1 4 3.6 CN1CCc2cccc3c2C1Cc1cc2sc(N)nc2cc1-3 10.1016/j.bmc.2020.115578
44451952 159548 0 5HT7R 5-HT7 receptor Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 527 8 1 6 4.4 Cc1ccc(N2CCN(CCCC(=O)NCc3nc4ccc(F)cc4c(=O)n3-c3ccccc3)CC2)cc1C 10.1016/j.bmc.2007.11.049
CHEMBL411104 159548 0 5HT7R 5-HT7 receptor Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 527 8 1 6 4.4 Cc1ccc(N2CCN(CCCC(=O)NCc3nc4ccc(F)cc4c(=O)n3-c3ccccc3)CC2)cc1C 10.1016/j.bmc.2007.11.049
44451952 159548 0 5HT7R 5-HT7 receptor Human 6.6 pIC50 = 6.6 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 527 8 1 6 4.4 Cc1ccc(N2CCN(CCCC(=O)NCc3nc4ccc(F)cc4c(=O)n3-c3ccccc3)CC2)cc1C 10.1016/j.ejmech.2008.09.050
CHEMBL411104 159548 0 5HT7R 5-HT7 receptor Human 6.6 pIC50 = 6.6 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 527 8 1 6 4.4 Cc1ccc(N2CCN(CCCC(=O)NCc3nc4ccc(F)cc4c(=O)n3-c3ccccc3)CC2)cc1C 10.1016/j.ejmech.2008.09.050
44452006 156684 0 5HT7R 5-HT7 receptor Human 6.6 pIC50 = 6.6 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 567 8 1 6 5.1 O=C(CCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1)NCc1nc2ccc(F)cc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
CHEMBL407966 156684 0 5HT7R 5-HT7 receptor Human 6.6 pIC50 = 6.6 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 567 8 1 6 5.1 O=C(CCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1)NCc1nc2ccc(F)cc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
44452006 156684 0 5HT7R 5-HT7 receptor Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 567 8 1 6 5.1 O=C(CCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1)NCc1nc2ccc(F)cc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
CHEMBL407966 156684 0 5HT7R 5-HT7 receptor Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 567 8 1 6 5.1 O=C(CCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1)NCc1nc2ccc(F)cc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
44452037 95510 0 5HT7R 5-HT7 receptor Human 7.5 pIC50 = 7.5 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 555 11 1 8 4.0 CCOc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccccc3c(=O)n2-c2ccc(OC)cc2)CC1 10.1016/j.ejmech.2008.09.050
CHEMBL260756 95510 0 5HT7R 5-HT7 receptor Human 7.5 pIC50 = 7.5 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 555 11 1 8 4.0 CCOc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccccc3c(=O)n2-c2ccc(OC)cc2)CC1 10.1016/j.ejmech.2008.09.050
44452273 157315 0 5HT7R 5-HT7 receptor Human 7.5 pIC50 = 7.5 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 555 11 1 8 4.0 CCOc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccccc3c(=O)n2-c2ccccc2OC)CC1 10.1016/j.ejmech.2008.09.050
CHEMBL408717 157315 0 5HT7R 5-HT7 receptor Human 7.5 pIC50 = 7.5 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 555 11 1 8 4.0 CCOc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccccc3c(=O)n2-c2ccccc2OC)CC1 10.1016/j.ejmech.2008.09.050
71574210 85616 0 5HT7R 5-HT7 receptor Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human 5HT7 receptor expressed in HEK293 assessed as inhibition of 5HT-induced cAMP accumulationAntagonist activity at human 5HT7 receptor expressed in HEK293 assessed as inhibition of 5HT-induced cAMP accumulation
ChEMBL 478 7 1 5 4.0 O=S(=O)(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2cccnc2c1 10.1016/j.ejmech.2012.11.042
CHEMBL2312934 85616 0 5HT7R 5-HT7 receptor Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human 5HT7 receptor expressed in HEK293 assessed as inhibition of 5HT-induced cAMP accumulationAntagonist activity at human 5HT7 receptor expressed in HEK293 assessed as inhibition of 5HT-induced cAMP accumulation
ChEMBL 478 7 1 5 4.0 O=S(=O)(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2cccnc2c1 10.1016/j.ejmech.2012.11.042
46866711 15311 0 5HT7R 5-HT7 receptor Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]LSD from human 5HT7 expressed in CHOKI cellsDisplacement of [3H]LSD from human 5HT7 expressed in CHOKI cells
ChEMBL 423 5 0 4 4.2 CC(C)N(c1cccc(N2CCN(C)CC2)c1)S(=O)(=O)c1cccc2ccccc12 10.1016/j.bmcl.2010.06.150
CHEMBL1222234 15311 0 5HT7R 5-HT7 receptor Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]LSD from human 5HT7 expressed in CHOKI cellsDisplacement of [3H]LSD from human 5HT7 expressed in CHOKI cells
ChEMBL 423 5 0 4 4.2 CC(C)N(c1cccc(N2CCN(C)CC2)c1)S(=O)(=O)c1cccc2ccccc12 10.1016/j.bmcl.2010.06.150
42388975 187671 0 5HT7R 5-HT7 receptor Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membraneDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membrane
ChEMBL 407 8 1 5 2.3 COc1ccc(S(=O)(=O)NCCCN2CCN(c3ccccc3F)CC2)cc1 10.1016/j.bmc.2008.04.023
CHEMBL522006 187671 0 5HT7R 5-HT7 receptor Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membraneDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membrane
ChEMBL 407 8 1 5 2.3 COc1ccc(S(=O)(=O)NCCCN2CCN(c3ccccc3F)CC2)cc1 10.1016/j.bmc.2008.04.023
44452037 95510 0 5HT7R 5-HT7 receptor Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 555 11 1 8 4.0 CCOc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccccc3c(=O)n2-c2ccc(OC)cc2)CC1 10.1016/j.bmc.2007.11.049
CHEMBL260756 95510 0 5HT7R 5-HT7 receptor Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 555 11 1 8 4.0 CCOc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccccc3c(=O)n2-c2ccc(OC)cc2)CC1 10.1016/j.bmc.2007.11.049
44452273 157315 0 5HT7R 5-HT7 receptor Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 555 11 1 8 4.0 CCOc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccccc3c(=O)n2-c2ccccc2OC)CC1 10.1016/j.bmc.2007.11.049
CHEMBL408717 157315 0 5HT7R 5-HT7 receptor Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 555 11 1 8 4.0 CCOc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccccc3c(=O)n2-c2ccccc2OC)CC1 10.1016/j.bmc.2007.11.049
206 2342 7 5HT7R 5-HT7 receptor Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human 5-HT7 expressed in HEK-293 cells assessed as inhibition in serotonin-induced increase in cAMP level after 45 mins by HTRF assayAntagonist activity at human 5-HT7 expressed in HEK-293 cells assessed as inhibition in serotonin-induced increase in cAMP level after 45 mins by HTRF assay
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1021/jm500880c
68848 2342 7 5HT7R 5-HT7 receptor Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human 5-HT7 expressed in HEK-293 cells assessed as inhibition in serotonin-induced increase in cAMP level after 45 mins by HTRF assayAntagonist activity at human 5-HT7 expressed in HEK-293 cells assessed as inhibition in serotonin-induced increase in cAMP level after 45 mins by HTRF assay
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1021/jm500880c
CHEMBL12314 2342 7 5HT7R 5-HT7 receptor Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human 5-HT7 expressed in HEK-293 cells assessed as inhibition in serotonin-induced increase in cAMP level after 45 mins by HTRF assayAntagonist activity at human 5-HT7 expressed in HEK-293 cells assessed as inhibition in serotonin-induced increase in cAMP level after 45 mins by HTRF assay
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1021/jm500880c
4106 2350 9 5HT7R 5-HT7 receptor Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmc.2007.11.049
5358812 2350 9 5HT7R 5-HT7 receptor Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmc.2007.11.049
89 2350 9 5HT7R 5-HT7 receptor Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmc.2007.11.049
CHEMBL93240 2350 9 5HT7R 5-HT7 receptor Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmc.2007.11.049
3233 3296 35 5HT7R 5-HT7 receptor Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2016.07.029
3247 3296 35 5HT7R 5-HT7 receptor Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2016.07.029
6604889 3296 35 5HT7R 5-HT7 receptor Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2016.07.029
CHEMBL282199 3296 35 5HT7R 5-HT7 receptor Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2016.07.029
DB13988 3296 35 5HT7R 5-HT7 receptor Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2016.07.029
3233 3296 35 5HT7R 5-HT7 receptor Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2016.07.029
3247 3296 35 5HT7R 5-HT7 receptor Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2016.07.029
6604889 3296 35 5HT7R 5-HT7 receptor Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2016.07.029
CHEMBL282199 3296 35 5HT7R 5-HT7 receptor Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2016.07.029
DB13988 3296 35 5HT7R 5-HT7 receptor Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2016.07.029
4223 3745 82 5HT7R 5-HT7 receptor Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat hydroxytryptamine 7 receptorInhibition of rat hydroxytryptamine 7 receptor
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/jm040793q
6918314 3745 82 5HT7R 5-HT7 receptor Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat hydroxytryptamine 7 receptorInhibition of rat hydroxytryptamine 7 receptor
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/jm040793q
7427 3745 82 5HT7R 5-HT7 receptor Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat hydroxytryptamine 7 receptorInhibition of rat hydroxytryptamine 7 receptor
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/jm040793q
CHEMBL439849 3745 82 5HT7R 5-HT7 receptor Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat hydroxytryptamine 7 receptorInhibition of rat hydroxytryptamine 7 receptor
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/jm040793q
DB06684 3745 82 5HT7R 5-HT7 receptor Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat hydroxytryptamine 7 receptorInhibition of rat hydroxytryptamine 7 receptor
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/jm040793q
10131112 1449 16 5HT7R 5-HT7 receptor Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against 5-hydroxytryptamine 7 receptor in humanInhibitory activity against 5-hydroxytryptamine 7 receptor in human
ChEMBL 246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C 10.1016/j.bmcl.2005.06.067
8428 1449 16 5HT7R 5-HT7 receptor Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against 5-hydroxytryptamine 7 receptor in humanInhibitory activity against 5-hydroxytryptamine 7 receptor in human
ChEMBL 246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C 10.1016/j.bmcl.2005.06.067
CHEMBL364005 1449 16 5HT7R 5-HT7 receptor Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against 5-hydroxytryptamine 7 receptor in humanInhibitory activity against 5-hydroxytryptamine 7 receptor in human
ChEMBL 246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C 10.1016/j.bmcl.2005.06.067
49864289 15232 0 5HT7R 5-HT7 receptor Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]LSD from human 5HT7 expressed in CHOKI cellsDisplacement of [3H]LSD from human 5HT7 expressed in CHOKI cells
ChEMBL 435 6 0 4 4.2 CN1CCN(c2cccc(N(CC3CC3)S(=O)(=O)c3ccc4ccccc4c3)c2)CC1 10.1016/j.bmcl.2010.06.150
CHEMBL1221449 15232 0 5HT7R 5-HT7 receptor Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]LSD from human 5HT7 expressed in CHOKI cellsDisplacement of [3H]LSD from human 5HT7 expressed in CHOKI cells
ChEMBL 435 6 0 4 4.2 CN1CCN(c2cccc(N(CC3CC3)S(=O)(=O)c3ccc4ccccc4c3)c2)CC1 10.1016/j.bmcl.2010.06.150
2470 3432 34 5HT7R 5-HT7 receptor Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell preincubated for 30 mins followed by incubation with agonist for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysisAntagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell preincubated for 30 mins followed by incubation with agonist for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysis
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmc.2020.115578
3300 3432 34 5HT7R 5-HT7 receptor Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell preincubated for 30 mins followed by incubation with agonist for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysisAntagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell preincubated for 30 mins followed by incubation with agonist for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysis
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmc.2020.115578
5265 3432 34 5HT7R 5-HT7 receptor Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell preincubated for 30 mins followed by incubation with agonist for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysisAntagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell preincubated for 30 mins followed by incubation with agonist for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysis
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmc.2020.115578
99 3432 34 5HT7R 5-HT7 receptor Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell preincubated for 30 mins followed by incubation with agonist for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysisAntagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell preincubated for 30 mins followed by incubation with agonist for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysis
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmc.2020.115578
CHEMBL267930 3432 34 5HT7R 5-HT7 receptor Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell preincubated for 30 mins followed by incubation with agonist for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysisAntagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell preincubated for 30 mins followed by incubation with agonist for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysis
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmc.2020.115578
73347306 89024 0 5HT7R 5-HT7 receptor Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]LSD from human 5HT7 receptorDisplacement of [3H]LSD from human 5HT7 receptor
ChEMBL 230 1 2 1 3.0 Cc1[nH]c2ccc(F)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376483 89024 0 5HT7R 5-HT7 receptor Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]LSD from human 5HT7 receptorDisplacement of [3H]LSD from human 5HT7 receptor
ChEMBL 230 1 2 1 3.0 Cc1[nH]c2ccc(F)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
46232772 194442 0 5HT7R 5-HT7 receptor Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 473 11 0 6 3.3 COc1ccc(S(=O)(=O)N(CCCN2CCN(c3ccccc3OC)CC2)CC2CC2)cc1 10.1016/j.bmc.2009.12.067
CHEMBL601250 194442 0 5HT7R 5-HT7 receptor Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 473 11 0 6 3.3 COc1ccc(S(=O)(=O)N(CCCN2CCN(c3ccccc3OC)CC2)CC2CC2)cc1 10.1016/j.bmc.2009.12.067
46232977 194780 0 5HT7R 5-HT7 receptor Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 453 8 1 5 3.7 COc1ccccc1N1CCN(CCC(C)NS(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmc.2009.12.067
CHEMBL603499 194780 0 5HT7R 5-HT7 receptor Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 453 8 1 5 3.7 COc1ccccc1N1CCN(CCC(C)NS(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmc.2009.12.067
42389293 184857 0 5HT7R 5-HT7 receptor Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membraneDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membrane
ChEMBL 439 8 1 5 3.3 COc1ccc(N2CCN(CCCNS(=O)(=O)c3ccc4ccccc4c3)CC2)cc1 10.1016/j.bmc.2008.04.023
CHEMBL494427 184857 0 5HT7R 5-HT7 receptor Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membraneDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membrane
ChEMBL 439 8 1 5 3.3 COc1ccc(N2CCN(CCCNS(=O)(=O)c3ccc4ccccc4c3)CC2)cc1 10.1016/j.bmc.2008.04.023
45278805 7188 0 5HT7R 5-HT7 receptor Human 6.5 pIC50 = 6.5 Binding
Inhibition of 5HT7 receptorInhibition of 5HT7 receptor
ChEMBL 484 7 1 4 5.2 Cc1c(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(-c2ccccc2)n1C 10.1016/j.bmcl.2010.01.093
CHEMBL1086754 7188 0 5HT7R 5-HT7 receptor Human 6.5 pIC50 = 6.5 Binding
Inhibition of 5HT7 receptorInhibition of 5HT7 receptor
ChEMBL 484 7 1 4 5.2 Cc1c(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(-c2ccccc2)n1C 10.1016/j.bmcl.2010.01.093
46232731 194477 0 5HT7R 5-HT7 receptor Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 481 9 0 4 4.3 O=S(=O)(c1ccc(C(F)(F)F)cc1)N(CCCN1CCN(c2ccccc2)CC1)CC1CC1 10.1016/j.bmc.2009.12.067
CHEMBL601458 194477 0 5HT7R 5-HT7 receptor Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 481 9 0 4 4.3 O=S(=O)(c1ccc(C(F)(F)F)cc1)N(CCCN1CCN(c2ccccc2)CC1)CC1CC1 10.1016/j.bmc.2009.12.067
42635029 184756 0 5HT7R 5-HT7 receptor Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membraneDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membrane
ChEMBL 419 9 1 6 2.2 COc1ccc(S(=O)(=O)NCCCN2CCN(c3cccc(OC)c3)CC2)cc1 10.1016/j.bmc.2008.04.023
CHEMBL493810 184756 0 5HT7R 5-HT7 receptor Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membraneDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membrane
ChEMBL 419 9 1 6 2.2 COc1ccc(S(=O)(=O)NCCCN2CCN(c3cccc(OC)c3)CC2)cc1 10.1016/j.bmc.2008.04.023
46232820 194437 0 5HT7R 5-HT7 receptor Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 531 9 0 4 5.5 O=S(=O)(c1ccc2ccccc2c1)N(CCCN1CCN(c2cccc(C(F)(F)F)c2)CC1)CC1CC1 10.1016/j.bmc.2009.12.067
CHEMBL601220 194437 0 5HT7R 5-HT7 receptor Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 531 9 0 4 5.5 O=S(=O)(c1ccc2ccccc2c1)N(CCCN1CCN(c2cccc(C(F)(F)F)c2)CC1)CC1CC1 10.1016/j.bmc.2009.12.067
127028473 137481 0 5HT7R 5-HT7 receptor Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay
ChEMBL 451 6 2 6 1.6 CC1(c2ccc(F)cc2)NC(=O)N(CC(O)CN2CCN(c3ccccc3C#N)CC2)C1=O 10.1016/j.ejmech.2016.02.024
CHEMBL3770639 137481 0 5HT7R 5-HT7 receptor Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay
ChEMBL 451 6 2 6 1.6 CC1(c2ccc(F)cc2)NC(=O)N(CC(O)CN2CCN(c3ccccc3C#N)CC2)C1=O 10.1016/j.ejmech.2016.02.024
86288948 111890 0 5HT7R 5-HT7 receptor Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay
ChEMBL 456 7 2 6 1.8 COc1ccccc1N1CCN(CC(O)CN2C(=O)NC(C)(c3ccc(F)cc3)C2=O)CC1 10.1016/j.ejmech.2016.02.024
CHEMBL3233679 111890 0 5HT7R 5-HT7 receptor Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay
ChEMBL 456 7 2 6 1.8 COc1ccccc1N1CCN(CC(O)CN2C(=O)NC(C)(c3ccc(F)cc3)C2=O)CC1 10.1016/j.ejmech.2016.02.024
CHEMBL3302600 111890 0 5HT7R 5-HT7 receptor Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay
ChEMBL 456 7 2 6 1.8 COc1ccccc1N1CCN(CC(O)CN2C(=O)NC(C)(c3ccc(F)cc3)C2=O)CC1 10.1016/j.ejmech.2016.02.024
44452357 95220 0 5HT7R 5-HT7 receptor Human 6.5 pIC50 = 6.5 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 529 9 1 7 3.8 COc1ccc(N2CCN(CCCC(=O)NCc3nc4ccc(F)cc4c(=O)n3-c3ccccc3)CC2)cc1 10.1016/j.ejmech.2008.09.050
CHEMBL259236 95220 0 5HT7R 5-HT7 receptor Human 6.5 pIC50 = 6.5 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 529 9 1 7 3.8 COc1ccc(N2CCN(CCCC(=O)NCc3nc4ccc(F)cc4c(=O)n3-c3ccccc3)CC2)cc1 10.1016/j.ejmech.2008.09.050
44452118 95666 0 5HT7R 5-HT7 receptor Human 6.5 pIC50 = 6.5 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 549 8 1 6 4.6 O=C(CCCN1CCN(c2cccc(C(F)(F)F)c2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
CHEMBL261573 95666 0 5HT7R 5-HT7 receptor Human 6.5 pIC50 = 6.5 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 549 8 1 6 4.6 O=C(CCCN1CCN(c2cccc(C(F)(F)F)c2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
46232975 194681 0 5HT7R 5-HT7 receptor Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 482 9 0 5 4.0 O=S(=O)(c1cccc2cccnc12)N(CCCN1CCN(c2ccc(F)cc2)CC1)CC1CC1 10.1016/j.bmc.2009.12.067
CHEMBL602889 194681 0 5HT7R 5-HT7 receptor Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 482 9 0 5 4.0 O=S(=O)(c1cccc2cccnc12)N(CCCN1CCN(c2ccc(F)cc2)CC1)CC1CC1 10.1016/j.bmc.2009.12.067
44452357 95220 0 5HT7R 5-HT7 receptor Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 529 9 1 7 3.8 COc1ccc(N2CCN(CCCC(=O)NCc3nc4ccc(F)cc4c(=O)n3-c3ccccc3)CC2)cc1 10.1016/j.bmc.2007.11.049
CHEMBL259236 95220 0 5HT7R 5-HT7 receptor Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 529 9 1 7 3.8 COc1ccc(N2CCN(CCCC(=O)NCc3nc4ccc(F)cc4c(=O)n3-c3ccccc3)CC2)cc1 10.1016/j.bmc.2007.11.049
44452118 95666 0 5HT7R 5-HT7 receptor Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 549 8 1 6 4.6 O=C(CCCN1CCN(c2cccc(C(F)(F)F)c2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
CHEMBL261573 95666 0 5HT7R 5-HT7 receptor Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 549 8 1 6 4.6 O=C(CCCN1CCN(c2cccc(C(F)(F)F)c2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
46232978 194703 0 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 491 7 1 4 4.7 CC(CCN1CCN(c2cccc(C(F)(F)F)c2)CC1)NS(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmc.2009.12.067
CHEMBL603093 194703 0 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 491 7 1 4 4.7 CC(CCN1CCN(c2cccc(C(F)(F)F)c2)CC1)NS(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmc.2009.12.067
44451931 95080 0 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 501 7 1 6 3.9 O=C(CCN1CCN(c2ccc(Cl)cc2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
CHEMBL258525 95080 0 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 501 7 1 6 3.9 O=C(CCN1CCN(c2ccc(Cl)cc2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
11166042 165543 0 5HT7R 5-HT7 receptor Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membraneDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membrane
ChEMBL 419 9 1 6 2.2 COc1ccc(S(=O)(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2008.04.023
CHEMBL427518 165543 0 5HT7R 5-HT7 receptor Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membraneDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membrane
ChEMBL 419 9 1 6 2.2 COc1ccc(S(=O)(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2008.04.023
44451931 95080 0 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 501 7 1 6 3.9 O=C(CCN1CCN(c2ccc(Cl)cc2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
CHEMBL258525 95080 0 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 501 7 1 6 3.9 O=C(CCN1CCN(c2ccc(Cl)cc2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
73351905 89032 0 5HT7R 5-HT7 receptor Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]LSD from human 5HT7 receptorDisplacement of [3H]LSD from human 5HT7 receptor
ChEMBL 288 2 2 1 4.5 Cc1[nH]c2ccc(-c3ccccc3)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376491 89032 0 5HT7R 5-HT7 receptor Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]LSD from human 5HT7 receptorDisplacement of [3H]LSD from human 5HT7 receptor
ChEMBL 288 2 2 1 4.5 Cc1[nH]c2ccc(-c3ccccc3)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
42635571 185082 0 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membraneDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membrane
ChEMBL 421 8 1 5 2.7 COc1ccc(S(=O)(=O)NC(C)CCN2CCN(c3ccc(F)cc3)CC2)cc1 10.1016/j.bmc.2008.04.023
CHEMBL495685 185082 0 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membraneDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membrane
ChEMBL 421 8 1 5 2.7 COc1ccc(S(=O)(=O)NC(C)CCN2CCN(c3ccc(F)cc3)CC2)cc1 10.1016/j.bmc.2008.04.023
42635572 185119 0 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membraneDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membrane
ChEMBL 403 8 1 5 2.6 COc1ccc(S(=O)(=O)NC(C)CCN2CCN(c3ccccc3)CC2)cc1 10.1016/j.bmc.2008.04.023
CHEMBL495890 185119 0 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membraneDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membrane
ChEMBL 403 8 1 5 2.6 COc1ccc(S(=O)(=O)NC(C)CCN2CCN(c3ccccc3)CC2)cc1 10.1016/j.bmc.2008.04.023
71574302 85597 0 5HT7R 5-HT7 receptor Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human 5HT7 receptor expressed in HEK293 assessed as inhibition of 5HT-induced cAMP accumulationAntagonist activity at human 5HT7 receptor expressed in HEK293 assessed as inhibition of 5HT-induced cAMP accumulation
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2cccnc2c1 10.1016/j.ejmech.2012.11.042
CHEMBL2312637 85597 0 5HT7R 5-HT7 receptor Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human 5HT7 receptor expressed in HEK293 assessed as inhibition of 5HT-induced cAMP accumulationAntagonist activity at human 5HT7 receptor expressed in HEK293 assessed as inhibition of 5HT-induced cAMP accumulation
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2cccnc2c1 10.1016/j.ejmech.2012.11.042
42635028 187880 0 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membraneDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membrane
ChEMBL 457 8 1 5 3.2 COc1ccc(S(=O)(=O)NCCCN2CCN(c3ccc(C(F)(F)F)cc3)CC2)cc1 10.1016/j.bmc.2008.04.023
CHEMBL523519 187880 0 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membraneDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membrane
ChEMBL 457 8 1 5 3.2 COc1ccc(S(=O)(=O)NCCCN2CCN(c3ccc(C(F)(F)F)cc3)CC2)cc1 10.1016/j.bmc.2008.04.023
49864723 15332 0 5HT7R 5-HT7 receptor Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]LSD from human 5HT7 expressed in CHOKI cellsDisplacement of [3H]LSD from human 5HT7 expressed in CHOKI cells
ChEMBL 423 6 0 4 4.2 CCCN(c1cccc(N2CCN(C)CC2)c1)S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.150
CHEMBL1222363 15332 0 5HT7R 5-HT7 receptor Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]LSD from human 5HT7 expressed in CHOKI cellsDisplacement of [3H]LSD from human 5HT7 expressed in CHOKI cells
ChEMBL 423 6 0 4 4.2 CCCN(c1cccc(N2CCN(C)CC2)c1)S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.150
135367816 164011 0 5HT7R 5-HT7 receptor Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay
ChEMBL 248 1 1 3 2.7 Clc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4218801 164011 0 5HT7R 5-HT7 receptor Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay
ChEMBL 248 1 1 3 2.7 Clc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
135367816 164011 0 5HT7R 5-HT7 receptor Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay
ChEMBL 248 1 1 3 2.7 Clc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4218801 164011 0 5HT7R 5-HT7 receptor Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay
ChEMBL 248 1 1 3 2.7 Clc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
44452329 157914 0 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 499 8 1 6 3.7 O=C(CCCN1CCN(c2ccccc2F)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
CHEMBL409358 157914 0 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 499 8 1 6 3.7 O=C(CCCN1CCN(c2ccccc2F)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
44452329 157914 0 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 499 8 1 6 3.7 O=C(CCCN1CCN(c2ccccc2F)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
CHEMBL409358 157914 0 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 499 8 1 6 3.7 O=C(CCCN1CCN(c2ccccc2F)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
45278882 7190 0 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Binding
Inhibition of 5HT7 receptorInhibition of 5HT7 receptor
ChEMBL 512 9 1 4 6.1 CCCn1c(-c2ccccc2)cc(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1C 10.1016/j.bmcl.2010.01.093
CHEMBL1086756 7190 0 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Binding
Inhibition of 5HT7 receptorInhibition of 5HT7 receptor
ChEMBL 512 9 1 4 6.1 CCCn1c(-c2ccccc2)cc(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1C 10.1016/j.bmcl.2010.01.093
11536843 114382 0 5HT7R 5-HT7 receptor Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human 5-HT7 receptor expressed in CHO cells assessed as cAMP production by EIA systemAntagonist activity at human 5-HT7 receptor expressed in CHO cells assessed as cAMP production by EIA system
ChEMBL 307 1 2 2 2.1 NC(N)=NC(=O)c1ccc2c(c1)[C@@]1(CCCO1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
CHEMBL3343673 114382 0 5HT7R 5-HT7 receptor Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human 5-HT7 receptor expressed in CHO cells assessed as cAMP production by EIA systemAntagonist activity at human 5-HT7 receptor expressed in CHO cells assessed as cAMP production by EIA system
ChEMBL 307 1 2 2 2.1 NC(N)=NC(=O)c1ccc2c(c1)[C@@]1(CCCO1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
46232654 194604 0 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 506 9 0 5 5.0 O=S(=O)(c1cccc2cccnc12)N(CCCN1CCN(c2ccccc2)CC1)CC1CCCCC1 10.1016/j.bmc.2009.12.067
CHEMBL602285 194604 0 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 506 9 0 5 5.0 O=S(=O)(c1cccc2cccnc12)N(CCCN1CCN(c2ccccc2)CC1)CC1CCCCC1 10.1016/j.bmc.2009.12.067
44452197 95387 0 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 509 8 1 6 4.2 Cc1ccc(C)c(N2CCN(CCCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)c1 10.1016/j.ejmech.2008.09.050
CHEMBL260029 95387 0 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 509 8 1 6 4.2 Cc1ccc(C)c(N2CCN(CCCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)c1 10.1016/j.ejmech.2008.09.050
44452081 95489 0 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 517 8 1 6 3.9 O=C(CCCN1CCN(c2ccc(F)cc2)CC1)NCc1nc2ccc(F)cc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
CHEMBL260648 95489 0 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 517 8 1 6 3.9 O=C(CCCN1CCN(c2ccc(F)cc2)CC1)NCc1nc2ccc(F)cc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
44452008 95260 0 5HT7R 5-HT7 receptor Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 533 8 1 6 4.4 O=C(CCCN1CCN(c2ccccc2Cl)CC1)NCc1nc2cc(F)ccc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
CHEMBL259408 95260 0 5HT7R 5-HT7 receptor Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 533 8 1 6 4.4 O=C(CCCN1CCN(c2ccccc2Cl)CC1)NCc1nc2cc(F)ccc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
44452197 95387 0 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 509 8 1 6 4.2 Cc1ccc(C)c(N2CCN(CCCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)c1 10.1016/j.bmc.2007.11.049
CHEMBL260029 95387 0 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 509 8 1 6 4.2 Cc1ccc(C)c(N2CCN(CCCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)c1 10.1016/j.bmc.2007.11.049
44452081 95489 0 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 517 8 1 6 3.9 O=C(CCCN1CCN(c2ccc(F)cc2)CC1)NCc1nc2ccc(F)cc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
CHEMBL260648 95489 0 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 517 8 1 6 3.9 O=C(CCCN1CCN(c2ccc(F)cc2)CC1)NCc1nc2ccc(F)cc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
22001618 81165 4 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human 5HT7A receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation by ELISAAntagonist activity at human 5HT7A receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation by ELISA
ChEMBL 268 3 1 3 2.8 COc1ccc(-c2ccccc2N2CCNCC2)cc1 10.1021/jm3003679
CHEMBL2164336 81165 4 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human 5HT7A receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation by ELISAAntagonist activity at human 5HT7A receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation by ELISA
ChEMBL 268 3 1 3 2.8 COc1ccc(-c2ccccc2N2CCNCC2)cc1 10.1021/jm3003679
44452171 167859 0 5HT7R 5-HT7 receptor Human 7.4 pIC50 = 7.4 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 511 9 1 7 3.6 CCOc1ccccc1N1CCN(CCC(=O)NCc2nc3ccccc3c(=O)n2-c2ccccc2)CC1 10.1016/j.ejmech.2008.09.050
CHEMBL436700 167859 0 5HT7R 5-HT7 receptor Human 7.4 pIC50 = 7.4 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 511 9 1 7 3.6 CCOc1ccccc1N1CCN(CCC(=O)NCc2nc3ccccc3c(=O)n2-c2ccccc2)CC1 10.1016/j.ejmech.2008.09.050
46232691 194545 0 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 524 9 0 5 5.2 O=S(=O)(c1cccc2cccnc12)N(CCCN1CCN(c2ccc(F)cc2)CC1)CC1CCCCC1 10.1016/j.bmc.2009.12.067
CHEMBL601887 194545 0 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 524 9 0 5 5.2 O=S(=O)(c1cccc2cccnc12)N(CCCN1CCN(c2ccc(F)cc2)CC1)CC1CCCCC1 10.1016/j.bmc.2009.12.067
11761059 9776 0 5HT7R 5-HT7 receptor Human 5.4 pIC50 = 5.4 Binding
Inhibition of human 5-hydroxytryptamine 7 receptorInhibition of human 5-hydroxytryptamine 7 receptor
ChEMBL 394 4 1 8 3.1 O=[N+]([O-])c1cc2c(cc1CN1CC=C(n3c(O)nc4ccccc43)CC1)OCO2 10.1021/jm010878g
CHEMBL115229 9776 0 5HT7R 5-HT7 receptor Human 5.4 pIC50 = 5.4 Binding
Inhibition of human 5-hydroxytryptamine 7 receptorInhibition of human 5-hydroxytryptamine 7 receptor
ChEMBL 394 4 1 8 3.1 O=[N+]([O-])c1cc2c(cc1CN1CC=C(n3c(O)nc4ccccc43)CC1)OCO2 10.1021/jm010878g
49864722 15331 0 5HT7R 5-HT7 receptor Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]LSD from human 5HT7 expressed in CHOKI cellsDisplacement of [3H]LSD from human 5HT7 expressed in CHOKI cells
ChEMBL 395 4 0 4 3.4 CN1CCN(c2cccc(N(C)S(=O)(=O)c3ccc4ccccc4c3)c2)CC1 10.1016/j.bmcl.2010.06.150
CHEMBL1222362 15331 0 5HT7R 5-HT7 receptor Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]LSD from human 5HT7 expressed in CHOKI cellsDisplacement of [3H]LSD from human 5HT7 expressed in CHOKI cells
ChEMBL 395 4 0 4 3.4 CN1CCN(c2cccc(N(C)S(=O)(=O)c3ccc4ccccc4c3)c2)CC1 10.1016/j.bmcl.2010.06.150
44452328 95395 0 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 567 8 1 6 5.1 O=C(CCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1)NCc1nc2cc(F)ccc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
CHEMBL260076 95395 0 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 567 8 1 6 5.1 O=C(CCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1)NCc1nc2cc(F)ccc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
44452249 157727 0 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 515 8 1 6 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
CHEMBL409157 157727 0 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 515 8 1 6 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
44452171 167859 0 5HT7R 5-HT7 receptor Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 511 9 1 7 3.6 CCOc1ccccc1N1CCN(CCC(=O)NCc2nc3ccccc3c(=O)n2-c2ccccc2)CC1 10.1016/j.bmc.2007.11.049
CHEMBL436700 167859 0 5HT7R 5-HT7 receptor Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 511 9 1 7 3.6 CCOc1ccccc1N1CCN(CCC(=O)NCc2nc3ccccc3c(=O)n2-c2ccccc2)CC1 10.1016/j.bmc.2007.11.049
44452328 95395 0 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 567 8 1 6 5.1 O=C(CCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1)NCc1nc2cc(F)ccc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
CHEMBL260076 95395 0 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 567 8 1 6 5.1 O=C(CCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1)NCc1nc2cc(F)ccc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
44452249 157727 0 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 515 8 1 6 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
CHEMBL409157 157727 0 5HT7R 5-HT7 receptor Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 515 8 1 6 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
46232560 194601 0 5HT7R 5-HT7 receptor Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 523 9 0 4 5.5 O=S(=O)(c1ccc(C(F)(F)F)cc1)N(CCCN1CCN(c2ccccc2)CC1)CC1CCCCC1 10.1016/j.bmc.2009.12.067
CHEMBL602274 194601 0 5HT7R 5-HT7 receptor Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells
ChEMBL 523 9 0 4 5.5 O=S(=O)(c1ccc(C(F)(F)F)cc1)N(CCCN1CCN(c2ccccc2)CC1)CC1CCCCC1 10.1016/j.bmc.2009.12.067
45109862 7172 0 5HT7R 5-HT7 receptor Human 6.3 pIC50 = 6.3 Binding
Inhibition of 5HT7 receptorInhibition of 5HT7 receptor
ChEMBL 470 7 2 3 5.2 Cc1[nH]c(-c2ccccc2)cc1C(=O)NCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2010.01.093
CHEMBL1086626 7172 0 5HT7R 5-HT7 receptor Human 6.3 pIC50 = 6.3 Binding
Inhibition of 5HT7 receptorInhibition of 5HT7 receptor
ChEMBL 470 7 2 3 5.2 Cc1[nH]c(-c2ccccc2)cc1C(=O)NCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2010.01.093
44452222 95263 0 5HT7R 5-HT7 receptor Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 509 8 1 6 4.2 Cc1cccc(N2CCN(CCCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)c1C 10.1016/j.bmc.2007.11.049
CHEMBL259415 95263 0 5HT7R 5-HT7 receptor Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 509 8 1 6 4.2 Cc1cccc(N2CCN(CCCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)c1C 10.1016/j.bmc.2007.11.049
44452222 95263 0 5HT7R 5-HT7 receptor Human 6.3 pIC50 = 6.3 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 509 8 1 6 4.2 Cc1cccc(N2CCN(CCCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)c1C 10.1016/j.ejmech.2008.09.050
CHEMBL259415 95263 0 5HT7R 5-HT7 receptor Human 6.3 pIC50 = 6.3 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 509 8 1 6 4.2 Cc1cccc(N2CCN(CCCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)c1C 10.1016/j.ejmech.2008.09.050
44452117 95665 0 5HT7R 5-HT7 receptor Human 6.3 pIC50 = 6.3 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 499 8 1 6 3.7 O=C(CCCN1CCN(c2ccccc2)CC1)NCc1nc2ccc(F)cc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
CHEMBL261572 95665 0 5HT7R 5-HT7 receptor Human 6.3 pIC50 = 6.3 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 499 8 1 6 3.7 O=C(CCCN1CCN(c2ccccc2)CC1)NCc1nc2ccc(F)cc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
42389467 184759 0 5HT7R 5-HT7 receptor Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membraneDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membrane
ChEMBL 407 8 1 5 2.3 COc1ccc(S(=O)(=O)NCCCN2CCN(c3ccc(F)cc3)CC2)cc1 10.1016/j.bmc.2008.04.023
CHEMBL493816 184759 0 5HT7R 5-HT7 receptor Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membraneDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membrane
ChEMBL 407 8 1 5 2.3 COc1ccc(S(=O)(=O)NCCCN2CCN(c3ccc(F)cc3)CC2)cc1 10.1016/j.bmc.2008.04.023
44452217 95169 0 5HT7R 5-HT7 receptor Human 7.3 pIC50 = 7.3 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 573 11 1 8 4.2 CCOc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccc(F)cc3c(=O)n2-c2ccccc2OC)CC1 10.1016/j.ejmech.2008.09.050
CHEMBL259001 95169 0 5HT7R 5-HT7 receptor Human 7.3 pIC50 = 7.3 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 573 11 1 8 4.2 CCOc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccc(F)cc3c(=O)n2-c2ccccc2OC)CC1 10.1016/j.ejmech.2008.09.050
44452117 95665 0 5HT7R 5-HT7 receptor Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 499 8 1 6 3.7 O=C(CCCN1CCN(c2ccccc2)CC1)NCc1nc2ccc(F)cc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
CHEMBL261572 95665 0 5HT7R 5-HT7 receptor Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 499 8 1 6 3.7 O=C(CCCN1CCN(c2ccccc2)CC1)NCc1nc2ccc(F)cc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
36418162 184885 0 5HT7R 5-HT7 receptor Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membraneDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membrane
ChEMBL 423 8 1 4 3.3 O=S(=O)(NCCCN1CCN(Cc2ccccc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmc.2008.04.023
CHEMBL494573 184885 0 5HT7R 5-HT7 receptor Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membraneDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membrane
ChEMBL 423 8 1 4 3.3 O=S(=O)(NCCCN1CCN(Cc2ccccc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmc.2008.04.023
637308 183031 24 5HT7R 5-HT7 receptor Human 4.3 pIC50 = 4.3 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 314 6 2 5 2.9 COc1cc(/C=C/C(=O)OCCc2ccc(O)cc2)ccc1O 10.1021/np050301s
CHEMBL481245 183031 24 5HT7R 5-HT7 receptor Human 4.3 pIC50 = 4.3 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 314 6 2 5 2.9 COc1cc(/C=C/C(=O)OCCc2ccc(O)cc2)ccc1O 10.1021/np050301s
10337743 3827 10 5HT7R 5-HT7 receptor Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]LSD from human cloned 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human cloned 5HT7 receptor expressed in CHO cells
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmc.2009.05.055
8429 3827 10 5HT7R 5-HT7 receptor Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]LSD from human cloned 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human cloned 5HT7 receptor expressed in CHO cells
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmc.2009.05.055
CHEMBL571858 3827 10 5HT7R 5-HT7 receptor Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]LSD from human cloned 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human cloned 5HT7 receptor expressed in CHO cells
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmc.2009.05.055
44452217 95169 0 5HT7R 5-HT7 receptor Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 573 11 1 8 4.2 CCOc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccc(F)cc3c(=O)n2-c2ccccc2OC)CC1 10.1016/j.bmc.2007.11.049
CHEMBL259001 95169 0 5HT7R 5-HT7 receptor Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 573 11 1 8 4.2 CCOc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccc(F)cc3c(=O)n2-c2ccccc2OC)CC1 10.1016/j.bmc.2007.11.049
44452007 95214 0 5HT7R 5-HT7 receptor Human 7.3 pIC50 = 7.3 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 573 11 1 8 4.2 CCOc1ccccc1N1CCN(CCCC(=O)NCc2nc3cc(F)ccc3c(=O)n2-c2ccc(OC)cc2)CC1 10.1016/j.ejmech.2008.09.050
CHEMBL259199 95214 0 5HT7R 5-HT7 receptor Human 7.3 pIC50 = 7.3 Binding
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 573 11 1 8 4.2 CCOc1ccccc1N1CCN(CCCC(=O)NCc2nc3cc(F)ccc3c(=O)n2-c2ccc(OC)cc2)CC1 10.1016/j.ejmech.2008.09.050
73354882 89023 1 5HT7R 5-HT7 receptor Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]LSD from human 5HT7 receptorDisplacement of [3H]LSD from human 5HT7 receptor
ChEMBL 290 1 2 1 3.6 Cc1[nH]c2ccc(Br)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376482 89023 1 5HT7R 5-HT7 receptor Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]LSD from human 5HT7 receptorDisplacement of [3H]LSD from human 5HT7 receptor
ChEMBL 290 1 2 1