Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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 Assay
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 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
CHEMBL5093342 218054 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL None None None CCCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5095971 218054 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL None None None CCCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
11329254 85250 None 0 Guinea pig Functional pEC50 = 5 5.0 - 1
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 85250 None 0 Guinea pig Functional pEC50 = 5 5.0 - 1
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
CHEMBL5093342 218054 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL None None None CCCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5095971 218054 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL None None None CCCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
5 139 None 45 Human Functional pEC50 = 7.0 7.0 -9 26
Agonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assayAgonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.1c00110
5202 139 None 45 Human Functional pEC50 = 7.0 7.0 -9 26
Agonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assayAgonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.1c00110
CHEMBL39 139 None 45 Human Functional pEC50 = 7.0 7.0 -9 26
Agonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assayAgonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.1c00110
DB08839 139 None 45 Human Functional pEC50 = 7.0 7.0 -9 26
Agonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assayAgonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.1c00110
134138168 147779 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 275 4 0 2 4.1 COc1ccccc1-c1cc(CN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
CHEMBL3931889 147779 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 275 4 0 2 4.1 COc1ccccc1-c1cc(CN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
5 139 None 45 Human Functional pEC50 = 7.0 7.0 -9 26
Agonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assayAgonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.1c00110
5202 139 None 45 Human Functional pEC50 = 7.0 7.0 -9 26
Agonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assayAgonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.1c00110
CHEMBL39 139 None 45 Human Functional pEC50 = 7.0 7.0 -9 26
Agonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assayAgonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.1c00110
DB08839 139 None 45 Human Functional pEC50 = 7.0 7.0 -9 26
Agonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assayAgonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.1c00110
135367816 164930 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 164930 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 164930 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 164930 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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
134138168 147779 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 275 4 0 2 4.1 COc1ccccc1-c1cc(CN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
CHEMBL3931889 147779 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 275 4 0 2 4.1 COc1ccccc1-c1cc(CN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
23643870 92917 None 0 Guinea pig Functional pEC50 = 5.9 5.9 - 1
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 92917 None 0 Guinea pig Functional pEC50 = 5.9 5.9 - 1
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
CHEMBL5081379 217234 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL None None None CCCNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5081379 217234 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL None None None CCCNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
135367820 164916 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 164916 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 164916 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 164916 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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
CHEMBL5094493 217989 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL None None None CCCN(CCC)CCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5094493 217989 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL None None None CCCN(CCC)CCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
92042876 151425 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assayAgonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assay
ChEMBL 261 4 1 2 3.7 CNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL3961059 151425 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assayAgonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assay
ChEMBL 261 4 1 2 3.7 CNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
5 139 None 45 Human Functional pEC50 = 7.8 7.8 -9 26
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 139 None 45 Human Functional pEC50 = 7.8 7.8 -9 26
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 139 None 45 Human Functional pEC50 = 7.8 7.8 -9 26
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 139 None 45 Human Functional pEC50 = 7.8 7.8 -9 26
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
92042876 151425 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assayAgonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assay
ChEMBL 261 4 1 2 3.7 CNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL3961059 151425 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assayAgonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assay
ChEMBL 261 4 1 2 3.7 CNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
3108374 92011 None 17 Human Functional pEC50 = 6.8 6.8 -1 5
Inverse agonist activity at 5-HT7 (unknown origin)Inverse agonist activity at 5-HT7 (unknown origin)
ChEMBL 295 2 0 3 3.5 COc1cc2c3c(c1OC)-c1ccccc1CC3N(C)CC2 10.1016/j.ejmech.2023.115414
CHEMBL2414990 92011 None 17 Human Functional pEC50 = 6.8 6.8 -1 5
Inverse agonist activity at 5-HT7 (unknown origin)Inverse agonist activity at 5-HT7 (unknown origin)
ChEMBL 295 2 0 3 3.5 COc1cc2c3c(c1OC)-c1ccccc1CC3N(C)CC2 10.1016/j.ejmech.2023.115414
67268994 164063 None 2 Human Functional pEC50 = 6.8 6.8 - 1
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 164063 None 2 Human Functional pEC50 = 6.8 6.8 - 1
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 164063 None 2 Human Functional pEC50 = 6.8 6.8 - 1
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 164063 None 2 Human Functional pEC50 = 6.8 6.8 - 1
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 164291 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 164291 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 164291 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 164291 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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
5 139 None 45 Human Functional pEC50 = 7.8 7.8 -9 26
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 139 None 45 Human Functional pEC50 = 7.8 7.8 -9 26
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 139 None 45 Human Functional pEC50 = 7.8 7.8 -9 26
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 139 None 45 Human Functional pEC50 = 7.8 7.8 -9 26
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 84702 None 0 Guinea pig Functional pEC50 = 4.8 4.8 - 1
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 84702 None 0 Guinea pig Functional pEC50 = 4.8 4.8 - 1
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 2350 None 5 Guinea pig Functional pEC50 = 5.8 5.8 - 1
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 2350 None 5 Guinea pig Functional pEC50 = 5.8 5.8 - 1
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 2350 None 5 Guinea pig Functional pEC50 = 5.8 5.8 - 1
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
CHEMBL5094234 218063 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL None None None CCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5096019 218063 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL None None None CCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5094234 218063 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL None None None CCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5096019 218063 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL None None None CCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
11785183 84747 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 84747 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 164164 None 6 Human Functional pEC50 = 6.7 6.7 - 1
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 164164 None 6 Human Functional pEC50 = 6.7 6.7 - 1
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
CHEMBL5084249 217394 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL None None None CCN(CC)CCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
124247485 164164 None 6 Human Functional pEC50 = 6.7 6.7 - 1
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 164164 None 6 Human Functional pEC50 = 6.7 6.7 - 1
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
CHEMBL5084249 217394 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL None None None CCN(CC)CCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
24825775 1523 None 16 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assayAgonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assay
ChEMBL 257 4 0 3 2.8 CN(CCc1cccc(c1)c1c(C)nn(c1C)C)C 10.1021/acs.jmedchem.1c00110
3929 1523 None 16 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assayAgonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assay
ChEMBL 257 4 0 3 2.8 CN(CCc1cccc(c1)c1c(C)nn(c1C)C)C 10.1021/acs.jmedchem.1c00110
CHEMBL4205349 1523 None 16 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assayAgonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assay
ChEMBL 257 4 0 3 2.8 CN(CCc1cccc(c1)c1c(C)nn(c1C)C)C 10.1021/acs.jmedchem.1c00110
24825775 1523 None 16 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assayAgonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assay
ChEMBL 257 4 0 3 2.8 CN(CCc1cccc(c1)c1c(C)nn(c1C)C)C 10.1021/acs.jmedchem.1c00110
3929 1523 None 16 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assayAgonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assay
ChEMBL 257 4 0 3 2.8 CN(CCc1cccc(c1)c1c(C)nn(c1C)C)C 10.1021/acs.jmedchem.1c00110
CHEMBL4205349 1523 None 16 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assayAgonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assay
ChEMBL 257 4 0 3 2.8 CN(CCc1cccc(c1)c1c(C)nn(c1C)C)C 10.1021/acs.jmedchem.1c00110
102364516 113607 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 113607 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 143402 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 143402 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 2353 None 4 Human Functional pEC50 = 5.6 5.6 -10 4
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 2353 None 4 Human Functional pEC50 = 5.6 5.6 -10 4
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 2353 None 4 Human Functional pEC50 = 5.6 5.6 -10 4
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
5 139 None 45 Human Functional pEC50 = 8.4 8.4 -9 26
Agonist activity at human 5-HT7A receptor expressed in HEK cell membranes incubated for 20 mins by cAMP functional assayAgonist activity at human 5-HT7A receptor expressed in HEK cell membranes incubated for 20 mins by cAMP functional assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2021.113243
5202 139 None 45 Human Functional pEC50 = 8.4 8.4 -9 26
Agonist activity at human 5-HT7A receptor expressed in HEK cell membranes incubated for 20 mins by cAMP functional assayAgonist activity at human 5-HT7A receptor expressed in HEK cell membranes incubated for 20 mins by cAMP functional assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2021.113243
CHEMBL39 139 None 45 Human Functional pEC50 = 8.4 8.4 -9 26
Agonist activity at human 5-HT7A receptor expressed in HEK cell membranes incubated for 20 mins by cAMP functional assayAgonist activity at human 5-HT7A receptor expressed in HEK cell membranes incubated for 20 mins by cAMP functional assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2021.113243
DB08839 139 None 45 Human Functional pEC50 = 8.4 8.4 -9 26
Agonist activity at human 5-HT7A receptor expressed in HEK cell membranes incubated for 20 mins by cAMP functional assayAgonist activity at human 5-HT7A receptor expressed in HEK cell membranes incubated for 20 mins by cAMP functional assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2021.113243
25107520 187699 None 0 Guinea pig Functional pEC50 = 6.5 6.5 - 1
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 187699 None 0 Guinea pig Functional pEC50 = 6.5 6.5 - 1
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 170916 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 170916 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 149263 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 149263 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 149263 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 149263 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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
5 139 None 45 Human Functional pEC50 = 8.4 8.4 -9 26
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.1c00110
5202 139 None 45 Human Functional pEC50 = 8.4 8.4 -9 26
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.1c00110
CHEMBL39 139 None 45 Human Functional pEC50 = 8.4 8.4 -9 26
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.1c00110
DB08839 139 None 45 Human Functional pEC50 = 8.4 8.4 -9 26
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.1c00110
135367857 164699 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 164699 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 164699 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 164699 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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
92042876 151425 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 261 4 1 2 3.7 CNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL3961059 151425 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 261 4 1 2 3.7 CNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
92042876 151425 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 261 4 1 2 3.7 CNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL3961059 151425 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 261 4 1 2 3.7 CNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
5 139 None 45 Human Functional pEC50 = 7.3 7.3 -9 26
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 139 None 45 Human Functional pEC50 = 7.3 7.3 -9 26
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 139 None 45 Human Functional pEC50 = 7.3 7.3 -9 26
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 139 None 45 Human Functional pEC50 = 7.3 7.3 -9 26
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
134138168 147779 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assayAgonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assay
ChEMBL 275 4 0 2 4.1 COc1ccccc1-c1cc(CN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
CHEMBL3931889 147779 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assayAgonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assay
ChEMBL 275 4 0 2 4.1 COc1ccccc1-c1cc(CN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
5 139 None 45 Human Functional pEC50 = 7.3 7.3 -9 26
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 139 None 45 Human Functional pEC50 = 7.3 7.3 -9 26
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 139 None 45 Human Functional pEC50 = 7.3 7.3 -9 26
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 139 None 45 Human Functional pEC50 = 7.3 7.3 -9 26
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
134138168 147779 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assayAgonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assay
ChEMBL 275 4 0 2 4.1 COc1ccccc1-c1cc(CN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
CHEMBL3931889 147779 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assayAgonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assay
ChEMBL 275 4 0 2 4.1 COc1ccccc1-c1cc(CN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
25107648 187329 None 0 Guinea pig Functional pEC50 = 6.3 6.3 - 1
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 187329 None 0 Guinea pig Functional pEC50 = 6.3 6.3 - 1
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 134 None 25 Human Functional pEC50 = 8.3 8.3 -204 8
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
4 134 None 25 Human Functional pEC50 = 8.3 8.3 -204 8
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 134 None 25 Human Functional pEC50 = 8.3 8.3 -204 8
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
5 139 None 45 Human Functional pEC50 = 8.2 8.2 -9 26
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 139 None 45 Human Functional pEC50 = 8.2 8.2 -9 26
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 139 None 45 Human Functional pEC50 = 8.2 8.2 -9 26
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 139 None 45 Human Functional pEC50 = 8.2 8.2 -9 26
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
5 139 None 45 Human Functional pEC50 = 8.2 8.2 -9 26
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 139 None 45 Human Functional pEC50 = 8.2 8.2 -9 26
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 139 None 45 Human Functional pEC50 = 8.2 8.2 -9 26
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 139 None 45 Human Functional pEC50 = 8.2 8.2 -9 26
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 151425 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 151425 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 151425 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 151425 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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
CHEMBL5074190 216802 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assayAgonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assay
ChEMBL None None None COc1ccccc1-c1cc(CCN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
CHEMBL5074190 216802 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assayAgonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assay
ChEMBL None None None COc1ccccc1-c1cc(CCN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
CHEMBL5083607 217362 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL None None None COc1ccccc1-c1cc(C2CCN(C)C2)ccc1Cl 10.1021/acs.jmedchem.1c00110
135453290 133675 None 29 Human Functional pEC50 = 5.3 5.3 -2818 7
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 133675 None 29 Human Functional pEC50 = 5.3 5.3 -2818 7
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
CHEMBL5083607 217362 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL None None None COc1ccccc1-c1cc(C2CCN(C)C2)ccc1Cl 10.1021/acs.jmedchem.1c00110
118709756 113611 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 113611 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 2351 None 38 Guinea pig Functional pEC50 = 6.2 6.2 - 1
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 2351 None 38 Guinea pig Functional pEC50 = 6.2 6.2 - 1
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 2351 None 38 Guinea pig Functional pEC50 = 6.2 6.2 - 1
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 134 None 25 Human Functional pEC50 = 6.2 6.2 -204 8
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
4 134 None 25 Human Functional pEC50 = 6.2 6.2 -204 8
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 134 None 25 Human Functional pEC50 = 6.2 6.2 -204 8
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 134 None 25 Guinea pig Functional pEC50 = 6.2 6.2 -2238 8
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
4 134 None 25 Guinea pig Functional pEC50 = 6.2 6.2 -2238 8
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 134 None 25 Guinea pig Functional pEC50 = 6.2 6.2 -2238 8
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 134 None 25 Guinea pig Functional pEC50 = 6.2 6.2 -2238 8
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
4 134 None 25 Guinea pig Functional pEC50 = 6.2 6.2 -2238 8
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 134 None 25 Guinea pig Functional pEC50 = 6.2 6.2 -2238 8
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 85156 None 0 Human Functional pEC50 = 5.2 5.2 - 1
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 85156 None 0 Human Functional pEC50 = 5.2 5.2 - 1
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
CHEMBL5083607 217362 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assayAgonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assay
ChEMBL None None None COc1ccccc1-c1cc(C2CCN(C)C2)ccc1Cl 10.1021/acs.jmedchem.1c00110
CHEMBL5083607 217362 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assayAgonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assay
ChEMBL None None None COc1ccccc1-c1cc(C2CCN(C)C2)ccc1Cl 10.1021/acs.jmedchem.1c00110
5 139 None 45 Human Functional pEC50 = 8.2 8.2 -9 26
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 139 None 45 Human Functional pEC50 = 8.2 8.2 -9 26
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 139 None 45 Human Functional pEC50 = 8.2 8.2 -9 26
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 139 None 45 Human Functional pEC50 = 8.2 8.2 -9 26
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
5 139 None 45 Human Functional pEC50 = 7.2 7.2 -9 26
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 139 None 45 Human Functional pEC50 = 7.2 7.2 -9 26
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 139 None 45 Human Functional pEC50 = 7.2 7.2 -9 26
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 139 None 45 Human Functional pEC50 = 7.2 7.2 -9 26
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
CHEMBL5091373 218057 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assayAgonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assay
ChEMBL None None None CNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5095981 218057 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assayAgonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assay
ChEMBL None None None CNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5091373 218057 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assayAgonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assay
ChEMBL None None None CNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5095981 218057 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assayAgonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assay
ChEMBL None None None CNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5091373 218057 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL None None None CNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5095981 218057 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL None None None CNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5091373 218057 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL None None None CNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5095981 218057 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL None None None CNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5077293 216979 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assayAgonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assay
ChEMBL None None None COc1ccccc1-c1cc(C2CCNC2)ccc1Cl 10.1021/acs.jmedchem.1c00110
CHEMBL5077293 216979 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assayAgonist activity at 5-HT7R (unknown origin) transfected in HEK293 cells expressing tTA-dependent luciferase reporter and beta arrestin 2-TEV fusion gene assessed as beta arrestin recruitment incubated for 22 hrs by Tango assay
ChEMBL None None None COc1ccccc1-c1cc(C2CCNC2)ccc1Cl 10.1021/acs.jmedchem.1c00110
CHEMBL5074880 216827 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL None None None CCNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5074880 216827 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL None None None CCNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
11431530 84659 None 0 Guinea pig Functional pEC50 = 5.1 5.1 - 1
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 84659 None 0 Guinea pig Functional pEC50 = 5.1 5.1 - 1
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
24825775 1523 None 16 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 257 4 0 3 2.8 CN(CCc1cccc(c1)c1c(C)nn(c1C)C)C 10.1021/acs.jmedchem.1c00110
3929 1523 None 16 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 257 4 0 3 2.8 CN(CCc1cccc(c1)c1c(C)nn(c1C)C)C 10.1021/acs.jmedchem.1c00110
CHEMBL4205349 1523 None 16 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 257 4 0 3 2.8 CN(CCc1cccc(c1)c1c(C)nn(c1C)C)C 10.1021/acs.jmedchem.1c00110
24825775 1523 None 16 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 257 4 0 3 2.8 CN(CCc1cccc(c1)c1c(C)nn(c1C)C)C 10.1021/acs.jmedchem.1c00110
3929 1523 None 16 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 257 4 0 3 2.8 CN(CCc1cccc(c1)c1c(C)nn(c1C)C)C 10.1021/acs.jmedchem.1c00110
CHEMBL4205349 1523 None 16 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 257 4 0 3 2.8 CN(CCc1cccc(c1)c1c(C)nn(c1C)C)C 10.1021/acs.jmedchem.1c00110
CHEMBL5074190 216802 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL None None None COc1ccccc1-c1cc(CCN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
CHEMBL5074190 216802 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL None None None COc1ccccc1-c1cc(CCN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
5 139 None 45 Human Functional pEC50 = 8.0 8.0 -9 26
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.1c00110
5202 139 None 45 Human Functional pEC50 = 8.0 8.0 -9 26
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.1c00110
CHEMBL39 139 None 45 Human Functional pEC50 = 8.0 8.0 -9 26
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.1c00110
DB08839 139 None 45 Human Functional pEC50 = 8.0 8.0 -9 26
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.1c00110
23643663 92897 None 0 Guinea pig Functional pEC50 = 6.1 6.1 - 1
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 92897 None 0 Guinea pig Functional pEC50 = 6.1 6.1 - 1
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
CHEMBL5077293 216979 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL None None None COc1ccccc1-c1cc(C2CCNC2)ccc1Cl 10.1021/acs.jmedchem.1c00110
CHEMBL5077293 216979 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysisAgonist activity at human 5-HT7R transfected in HEK293 cells assessed as Gs-mediated cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL None None None COc1ccccc1-c1cc(C2CCNC2)ccc1Cl 10.1021/acs.jmedchem.1c00110
3233 3512 None 28 Human Functional pIC50 = 9.3 9.3 8511 2
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.1c01093
3247 3512 None 28 Human Functional pIC50 = 9.3 9.3 8511 2
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.1c01093
6604889 3512 None 28 Human Functional pIC50 = 9.3 9.3 8511 2
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.1c01093
CHEMBL282199 3512 None 28 Human Functional pIC50 = 9.3 9.3 8511 2
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.1c01093
DB13988 3512 None 28 Human Functional pIC50 = 9.3 9.3 8511 2
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.1c01093
4106 2502 None 21 Human Functional pIC50 = 9.1 9.1 -7 7
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 2502 None 21 Human Functional pIC50 = 9.1 9.1 -7 7
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 2502 None 21 Human Functional pIC50 = 9.1 9.1 -7 7
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 2502 None 21 Human Functional pIC50 = 9.1 9.1 -7 7
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 3512 None 28 Human Functional pIC50 = 9.1 9.1 8511 2
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 3512 None 28 Human Functional pIC50 = 9.1 9.1 8511 2
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 3512 None 28 Human Functional pIC50 = 9.1 9.1 8511 2
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 3512 None 28 Human Functional pIC50 = 9.1 9.1 8511 2
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 3512 None 28 Human Functional pIC50 = 9.1 9.1 8511 2
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 3512 None 28 Human Functional pIC50 = 9.0 9.0 8511 2
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 3512 None 28 Human Functional pIC50 = 9.0 9.0 8511 2
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 3512 None 28 Human Functional pIC50 = 9.0 9.0 8511 2
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 3512 None 28 Human Functional pIC50 = 9.0 9.0 8511 2
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 3512 None 28 Human Functional pIC50 = 9.0 9.0 8511 2
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 3512 None 28 Human Functional pIC50 = 9.0 9.0 8511 2
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.1c01093
3247 3512 None 28 Human Functional pIC50 = 9.0 9.0 8511 2
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.1c01093
6604889 3512 None 28 Human Functional pIC50 = 9.0 9.0 8511 2
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.1c01093
CHEMBL282199 3512 None 28 Human Functional pIC50 = 9.0 9.0 8511 2
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.1c01093
DB13988 3512 None 28 Human Functional pIC50 = 9.0 9.0 8511 2
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.1c01093
3233 3512 None 28 Human Functional pIC50 = 9.0 9.0 8511 2
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 3512 None 28 Human Functional pIC50 = 9.0 9.0 8511 2
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 3512 None 28 Human Functional pIC50 = 9.0 9.0 8511 2
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 3512 None 28 Human Functional pIC50 = 9.0 9.0 8511 2
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 3512 None 28 Human Functional pIC50 = 9.0 9.0 8511 2
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 2502 None 21 Human Functional pIC50 = 8.8 8.8 -7 7
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 2502 None 21 Human Functional pIC50 = 8.8 8.8 -7 7
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 2502 None 21 Human Functional pIC50 = 8.8 8.8 -7 7
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 2502 None 21 Human Functional pIC50 = 8.8 8.8 -7 7
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
164609529 184570 None 0 Human Functional pIC50 = 7 7.0 -36 2
Antagonist activity at human 5-HT7A receptor expressed in HEK cell membranes assessed as reduction in serotonin-induced cAMP accumulation incubated for 20 mins by cAMP functional assayAntagonist activity at human 5-HT7A receptor expressed in HEK cell membranes assessed as reduction in serotonin-induced cAMP accumulation incubated for 20 mins by cAMP functional assay
ChEMBL 383 5 0 4 4.1 CC1(CCCN2CCN(c3ccccn3)CC2)Cc2cc(Cl)ccc2C1=O 10.1016/j.ejmech.2021.113243
CHEMBL4846823 184570 None 0 Human Functional pIC50 = 7 7.0 -36 2
Antagonist activity at human 5-HT7A receptor expressed in HEK cell membranes assessed as reduction in serotonin-induced cAMP accumulation incubated for 20 mins by cAMP functional assayAntagonist activity at human 5-HT7A receptor expressed in HEK cell membranes assessed as reduction in serotonin-induced cAMP accumulation incubated for 20 mins by cAMP functional assay
ChEMBL 383 5 0 4 4.1 CC1(CCCN2CCN(c3ccccn3)CC2)Cc2cc(Cl)ccc2C1=O 10.1016/j.ejmech.2021.113243
11391654 180631 None 0 Human Functional pIC50 = 7 7.0 - 1
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 180631 None 0 Human Functional pIC50 = 7 7.0 - 1
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
127028798 138271 None 0 Human Functional pIC50 = 6 6.0 - 1
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 138271 None 0 Human Functional pIC50 = 6 6.0 - 1
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
142601335 186527 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 256 2 2 3 2.2 Cc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4876193 186527 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 256 2 2 3 2.2 Cc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
145946966 167697 None 0 Human Functional pIC50 = 6.0 6.0 -144 3
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 167697 None 0 Human Functional pIC50 = 6.0 6.0 -144 3
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 167697 None 0 Human Functional pIC50 = 6.0 6.0 -144 3
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
142601335 186527 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 256 2 2 3 2.2 Cc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4876193 186527 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 256 2 2 3 2.2 Cc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
4106 2502 None 21 Human Functional pIC50 = 8.0 8.0 -7 7
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 2502 None 21 Human Functional pIC50 = 8.0 8.0 -7 7
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 2502 None 21 Human Functional pIC50 = 8.0 8.0 -7 7
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 2502 None 21 Human Functional pIC50 = 8.0 8.0 -7 7
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
117209912 185443 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 262 2 2 3 2.1 Clc1ccccc1-c1n[nH]cc1N1CCNCC1 10.1021/acs.jmedchem.1c01093
CHEMBL4859827 185443 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 262 2 2 3 2.1 Clc1ccccc1-c1n[nH]cc1N1CCNCC1 10.1021/acs.jmedchem.1c01093
117209912 185443 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 262 2 2 3 2.1 Clc1ccccc1-c1n[nH]cc1N1CCNCC1 10.1021/acs.jmedchem.1c01093
CHEMBL4859827 185443 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 262 2 2 3 2.1 Clc1ccccc1-c1n[nH]cc1N1CCNCC1 10.1021/acs.jmedchem.1c01093
135339817 181590 None 0 Human Functional pIC50 = 7.9 7.9 -1 5
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 181590 None 0 Human Functional pIC50 = 7.9 7.9 -1 5
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 2493 None 10 Human Functional pIC50 = 6.9 6.9 -97 3
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 2493 None 10 Human Functional pIC50 = 6.9 6.9 -97 3
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 2493 None 10 Human Functional pIC50 = 6.9 6.9 -97 3
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
156013673 177366 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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
CHEMBL4636148 177366 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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
127028797 138420 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 138420 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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
11536844 115186 None 0 Human Functional pIC50 = 7.8 7.8 2 2
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 115186 None 0 Human Functional pIC50 = 7.8 7.8 2 2
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
213046 2385 None 44 Human Functional pIC50 = 7.8 7.8 1 17
Antagonist activity at human 5-HT7A receptor expressed in HEK cell membranes assessed as reduction in serotonin-induced cAMP accumulation incubated for 20 mins by cAMP functional assayAntagonist activity at human 5-HT7A receptor expressed in HEK cell membranes assessed as reduction in serotonin-induced cAMP accumulation incubated for 20 mins by cAMP functional assay
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1016/j.ejmech.2021.113243
213046.0 2385 None 44 Human Functional pIC50 = 7.8 7.8 1 17
Antagonist activity at human 5-HT7A receptor expressed in HEK cell membranes assessed as reduction in serotonin-induced cAMP accumulation incubated for 20 mins by cAMP functional assayAntagonist activity at human 5-HT7A receptor expressed in HEK cell membranes assessed as reduction in serotonin-induced cAMP accumulation incubated for 20 mins by cAMP functional assay
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1016/j.ejmech.2021.113243
4168 2385 None 44 Human Functional pIC50 = 7.8 7.8 1 17
Antagonist activity at human 5-HT7A receptor expressed in HEK cell membranes assessed as reduction in serotonin-induced cAMP accumulation incubated for 20 mins by cAMP functional assayAntagonist activity at human 5-HT7A receptor expressed in HEK cell membranes assessed as reduction in serotonin-induced cAMP accumulation incubated for 20 mins by cAMP functional assay
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1016/j.ejmech.2021.113243
7461 2385 None 44 Human Functional pIC50 = 7.8 7.8 1 17
Antagonist activity at human 5-HT7A receptor expressed in HEK cell membranes assessed as reduction in serotonin-induced cAMP accumulation incubated for 20 mins by cAMP functional assayAntagonist activity at human 5-HT7A receptor expressed in HEK cell membranes assessed as reduction in serotonin-induced cAMP accumulation incubated for 20 mins by cAMP functional assay
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1016/j.ejmech.2021.113243
CHEMBL1237021 2385 None 44 Human Functional pIC50 = 7.8 7.8 1 17
Antagonist activity at human 5-HT7A receptor expressed in HEK cell membranes assessed as reduction in serotonin-induced cAMP accumulation incubated for 20 mins by cAMP functional assayAntagonist activity at human 5-HT7A receptor expressed in HEK cell membranes assessed as reduction in serotonin-induced cAMP accumulation incubated for 20 mins by cAMP functional assay
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1016/j.ejmech.2021.113243
DB08815 2385 None 44 Human Functional pIC50 = 7.8 7.8 1 17
Antagonist activity at human 5-HT7A receptor expressed in HEK cell membranes assessed as reduction in serotonin-induced cAMP accumulation incubated for 20 mins by cAMP functional assayAntagonist activity at human 5-HT7A receptor expressed in HEK cell membranes assessed as reduction in serotonin-induced cAMP accumulation incubated for 20 mins by cAMP functional assay
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1016/j.ejmech.2021.113243
142601318 185651 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 272 3 2 4 1.9 COc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4863036 185651 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 272 3 2 4 1.9 COc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
142601318 185651 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 272 3 2 4 1.9 COc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4863036 185651 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 272 3 2 4 1.9 COc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
11500509 120645 None 0 Human Functional pIC50 = 7.8 7.8 3 2
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 120645 None 0 Human Functional pIC50 = 7.8 7.8 3 2
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 120645 None 0 Human Functional pIC50 = 7.8 7.8 3 2
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
117209962 184975 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 242 2 2 3 1.8 Cc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4852622 184975 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 242 2 2 3 1.8 Cc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
117209962 184975 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 242 2 2 3 1.8 Cc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4852622 184975 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 242 2 2 3 1.8 Cc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
142601343 185709 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 256 2 2 3 2.2 Cc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4863868 185709 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 256 2 2 3 2.2 Cc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
142601343 185709 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 256 2 2 3 2.2 Cc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4863868 185709 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 256 2 2 3 2.2 Cc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
127029652 138415 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 138415 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 167825 None 0 Human Functional pIC50 = 5.7 5.7 -32 4
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 167825 None 0 Human Functional pIC50 = 5.7 5.7 -32 4
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 167825 None 0 Human Functional pIC50 = 5.7 5.7 -32 4
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
134141985 147264 None 0 Human Functional pIC50 = 4.7 4.7 - 1
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 147264 None 0 Human Functional pIC50 = 4.7 4.7 - 1
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
134141985 147264 None 0 Human Functional pIC50 = 4.7 4.7 - 1
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 147264 None 0 Human Functional pIC50 = 4.7 4.7 - 1
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
44348383 16310 None 0 Human Functional pIC50 = 8.7 8.7 - 1
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 16310 None 0 Human Functional pIC50 = 8.7 8.7 - 1
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
4106 2502 None 21 Human Functional pIC50 = 7.7 7.7 -7 7
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 2502 None 21 Human Functional pIC50 = 7.7 7.7 -7 7
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 2502 None 21 Human Functional pIC50 = 7.7 7.7 -7 7
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 2502 None 21 Human Functional pIC50 = 7.7 7.7 -7 7
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
102364516 113607 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 113607 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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
134157289 154170 None 0 Human Functional pIC50 = 4.6 4.6 - 1
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 154170 None 0 Human Functional pIC50 = 4.6 4.6 - 1
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
118709756 113611 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 113611 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 154170 None 0 Human Functional pIC50 = 4.6 4.6 - 1
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 154170 None 0 Human Functional pIC50 = 4.6 4.6 - 1
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
117209857 185244 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 246 2 2 3 1.6 Fc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4856702 185244 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 246 2 2 3 1.6 Fc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
142601328 185109 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 276 2 2 3 2.5 Clc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4854605 185109 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 276 2 2 3 2.5 Clc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
145946714 167657 None 0 Human Functional pIC50 = 5.6 5.6 -30 4
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 167657 None 0 Human Functional pIC50 = 5.6 5.6 -30 4
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 167657 None 0 Human Functional pIC50 = 5.6 5.6 -30 4
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
142601328 185109 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 276 2 2 3 2.5 Clc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4854605 185109 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 276 2 2 3 2.5 Clc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
117209857 185244 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 246 2 2 3 1.6 Fc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4856702 185244 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 246 2 2 3 1.6 Fc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
127029650 138353 None 0 Human Functional pIC50 = 4.6 4.6 - 1
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 138353 None 0 Human Functional pIC50 = 4.6 4.6 - 1
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
142601333 185869 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 260 2 2 3 2.0 Fc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4866412 185869 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 260 2 2 3 2.0 Fc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
142601328 185109 None 0 Human Functional pIC50 = 4.6 4.6 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in beta-arrestin recruitment incubated for 22 hrs by bright-Glo reagent based Tango assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in beta-arrestin recruitment incubated for 22 hrs by bright-Glo reagent based Tango assay
ChEMBL 276 2 2 3 2.5 Clc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4854605 185109 None 0 Human Functional pIC50 = 4.6 4.6 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in beta-arrestin recruitment incubated for 22 hrs by bright-Glo reagent based Tango assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in beta-arrestin recruitment incubated for 22 hrs by bright-Glo reagent based Tango assay
ChEMBL 276 2 2 3 2.5 Clc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
135367820 164916 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 164916 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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
142601333 185869 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 260 2 2 3 2.0 Fc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4866412 185869 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 260 2 2 3 2.0 Fc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
142601328 185109 None 0 Human Functional pIC50 = 4.6 4.6 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in beta-arrestin recruitment incubated for 22 hrs by bright-Glo reagent based Tango assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in beta-arrestin recruitment incubated for 22 hrs by bright-Glo reagent based Tango assay
ChEMBL 276 2 2 3 2.5 Clc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4854605 185109 None 0 Human Functional pIC50 = 4.6 4.6 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in beta-arrestin recruitment incubated for 22 hrs by bright-Glo reagent based Tango assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in beta-arrestin recruitment incubated for 22 hrs by bright-Glo reagent based Tango assay
ChEMBL 276 2 2 3 2.5 Clc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
135367820 164916 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 164916 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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
135367405 164291 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 164291 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 164291 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 164291 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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
156010865 177236 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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
CHEMBL4633786 177236 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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
71574210 86317 None 0 Human Functional pIC50 = 5.6 5.6 2 2
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 86317 None 0 Human Functional pIC50 = 5.6 5.6 2 2
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
206 2493 None 10 Human Functional pIC50 = 6.5 6.5 -97 3
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 2493 None 10 Human Functional pIC50 = 6.5 6.5 -97 3
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 2493 None 10 Human Functional pIC50 = 6.5 6.5 -97 3
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
3233 3512 None 28 Human Functional pIC50 = 8.4 8.4 8511 2
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 3512 None 28 Human Functional pIC50 = 8.4 8.4 8511 2
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 3512 None 28 Human Functional pIC50 = 8.4 8.4 8511 2
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 3512 None 28 Human Functional pIC50 = 8.4 8.4 8511 2
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 3512 None 28 Human Functional pIC50 = 8.4 8.4 8511 2
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 3512 None 28 Human Functional pIC50 = 8.4 8.4 8511 2
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 3512 None 28 Human Functional pIC50 = 8.4 8.4 8511 2
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 3512 None 28 Human Functional pIC50 = 8.4 8.4 8511 2
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 3512 None 28 Human Functional pIC50 = 8.4 8.4 8511 2
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 3512 None 28 Human Functional pIC50 = 8.4 8.4 8511 2
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
2470 3653 None 40 Human Functional pIC50 = 6.5 6.5 -5128 23
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 3653 None 40 Human Functional pIC50 = 6.5 6.5 -5128 23
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 3653 None 40 Human Functional pIC50 = 6.5 6.5 -5128 23
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 3653 None 40 Human Functional pIC50 = 6.5 6.5 -5128 23
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 3653 None 40 Human Functional pIC50 = 6.5 6.5 -5128 23
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
127028473 138360 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 138360 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 112689 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 112689 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 112689 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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
71574302 86298 None 0 Human Functional pIC50 = 5.4 5.4 -4 2
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 86298 None 0 Human Functional pIC50 = 5.4 5.4 -4 2
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
142601323 185947 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 272 3 2 4 1.9 COc1ccccc1-c1n[nH]cc1N1CCCNCC1 10.1021/acs.jmedchem.1c01093
CHEMBL4867560 185947 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 272 3 2 4 1.9 COc1ccccc1-c1n[nH]cc1N1CCCNCC1 10.1021/acs.jmedchem.1c01093
135367816 164930 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 164930 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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
117209971 186591 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 258 3 2 4 1.5 COc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4877051 186591 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 258 3 2 4 1.5 COc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
135367816 164930 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 164930 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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
142601323 185947 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 272 3 2 4 1.9 COc1ccccc1-c1n[nH]cc1N1CCCNCC1 10.1021/acs.jmedchem.1c01093
CHEMBL4867560 185947 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 272 3 2 4 1.9 COc1ccccc1-c1n[nH]cc1N1CCCNCC1 10.1021/acs.jmedchem.1c01093
117209971 186591 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 258 3 2 4 1.5 COc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4877051 186591 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 258 3 2 4 1.5 COc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
117209918 186516 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 258 3 2 4 1.5 COc1ccccc1-c1n[nH]cc1N1CCNCC1 10.1021/acs.jmedchem.1c01093
CHEMBL4876036 186516 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 258 3 2 4 1.5 COc1ccccc1-c1n[nH]cc1N1CCNCC1 10.1021/acs.jmedchem.1c01093
117209918 186516 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 258 3 2 4 1.5 COc1ccccc1-c1n[nH]cc1N1CCNCC1 10.1021/acs.jmedchem.1c01093
CHEMBL4876036 186516 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 258 3 2 4 1.5 COc1ccccc1-c1n[nH]cc1N1CCNCC1 10.1021/acs.jmedchem.1c01093
11536843 115187 None 0 Human Functional pIC50 = 7.4 7.4 1 2
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 115187 None 0 Human Functional pIC50 = 7.4 7.4 1 2
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
22001618 81844 None 10 Human Functional pIC50 = 6.4 6.4 - 1
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 81844 None 10 Human Functional pIC50 = 6.4 6.4 - 1
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
59511191 185629 None 1 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 228 2 2 3 1.5 c1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4862745 185629 None 1 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 228 2 2 3 1.5 c1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
59511191 185629 None 1 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 228 2 2 3 1.5 c1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4862745 185629 None 1 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 228 2 2 3 1.5 c1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
2737389 187692 None 22 Human Functional pIC50 = 6.3 6.3 - 1
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 238 2 1 2 2.8 c1ccc(-c2ccccc2N2CCNCC2)cc1 10.1021/jm3003679
CHEMBL494675 187692 None 22 Human Functional pIC50 = 6.3 6.3 - 1
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 238 2 1 2 2.8 c1ccc(-c2ccccc2N2CCNCC2)cc1 10.1021/jm3003679
90656694 111058 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human 5-HT7 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulationAntagonist activity at human 5-HT7 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation
ChEMBL 339 7 1 4 3.4 CN(CCCCN1CCN(c2ccccc2)CC1)c1cccc(O)c1 10.1016/j.ejmech.2014.04.034
CHEMBL3262428 111058 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human 5-HT7 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulationAntagonist activity at human 5-HT7 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation
ChEMBL 339 7 1 4 3.4 CN(CCCCN1CCN(c2ccccc2)CC1)c1cccc(O)c1 10.1016/j.ejmech.2014.04.034
117209911 186435 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 246 2 2 3 1.6 Fc1ccccc1-c1n[nH]cc1N1CCNCC1 10.1021/acs.jmedchem.1c01093
CHEMBL4874854 186435 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 246 2 2 3 1.6 Fc1ccccc1-c1n[nH]cc1N1CCNCC1 10.1021/acs.jmedchem.1c01093
117209911 186435 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 246 2 2 3 1.6 Fc1ccccc1-c1n[nH]cc1N1CCNCC1 10.1021/acs.jmedchem.1c01093
CHEMBL4874854 186435 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 246 2 2 3 1.6 Fc1ccccc1-c1n[nH]cc1N1CCNCC1 10.1021/acs.jmedchem.1c01093
134154531 152817 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 418 7 0 5 4.7 COc1ccccc1-c1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OC 10.1016/j.ejmech.2016.07.029
CHEMBL3973160 152817 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 418 7 0 5 4.7 COc1ccccc1-c1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OC 10.1016/j.ejmech.2016.07.029
71574306 86300 None 0 Human Functional pIC50 = 5.3 5.3 2 2
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)c1cc2ccccc2cn1 10.1016/j.ejmech.2012.11.042
CHEMBL2312639 86300 None 0 Human Functional pIC50 = 5.3 5.3 2 2
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)c1cc2ccccc2cn1 10.1016/j.ejmech.2012.11.042
134154531 152817 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 418 7 0 5 4.7 COc1ccccc1-c1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OC 10.1016/j.ejmech.2016.07.029
CHEMBL3973160 152817 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 418 7 0 5 4.7 COc1ccccc1-c1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OC 10.1016/j.ejmech.2016.07.029
145947560 167809 None 0 Human Functional pIC50 = 5.2 5.2 -19 4
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 344 6 0 3 4.2 Cc1cc(OCCCN2CCN(c3ccccc3)CC2)ccc1Cl 10.1016/j.bmcl.2018.04.059
CHEMBL4212812 167809 None 0 Human Functional pIC50 = 5.2 5.2 -19 4
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 344 6 0 3 4.2 Cc1cc(OCCCN2CCN(c3ccccc3)CC2)ccc1Cl 10.1016/j.bmcl.2018.04.059
CHEMBL4302457 167809 None 0 Human Functional pIC50 = 5.2 5.2 -19 4
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 344 6 0 3 4.2 Cc1cc(OCCCN2CCN(c3ccccc3)CC2)ccc1Cl 10.1016/j.bmcl.2018.04.059
11694810 120603 None 0 Human Functional pIC50 = 7.2 7.2 -1 2
Inhibition of human 5-HT7 receptor expressed in CHO cells assessed as cAMP production by EIA systemInhibition of human 5-HT7 receptor expressed in CHO cells assessed as cAMP production by EIA system
ChEMBL 281 1 3 2 1.3 CC1(O)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.05.027
CHEMBL3310123 120603 None 0 Human Functional pIC50 = 7.2 7.2 -1 2
Inhibition of human 5-HT7 receptor expressed in CHO cells assessed as cAMP production by EIA systemInhibition of human 5-HT7 receptor expressed in CHO cells assessed as cAMP production by EIA system
ChEMBL 281 1 3 2 1.3 CC1(O)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.05.027
CHEMBL3545474 120603 None 0 Human Functional pIC50 = 7.2 7.2 -1 2
Inhibition of human 5-HT7 receptor expressed in CHO cells assessed as cAMP production by EIA systemInhibition of human 5-HT7 receptor expressed in CHO cells assessed as cAMP production by EIA system
ChEMBL 281 1 3 2 1.3 CC1(O)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.05.027
127028153 138250 None 0 Human Functional pIC50 = 5.2 5.2 - 1
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 COc1cccc(N2CCN(CC(O)CN3C(=O)NC(C)(c4ccc(F)cc4)C3=O)CC2)c1 10.1016/j.ejmech.2016.02.024
CHEMBL3769441 138250 None 0 Human Functional pIC50 = 5.2 5.2 - 1
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 COc1cccc(N2CCN(CC(O)CN3C(=O)NC(C)(c4ccc(F)cc4)C3=O)CC2)c1 10.1016/j.ejmech.2016.02.024
142601325 185975 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 242 2 2 3 1.9 c1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4868035 185975 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 242 2 2 3 1.9 c1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
142601325 185975 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 242 2 2 3 1.9 c1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4868035 185975 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 242 2 2 3 1.9 c1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
117209964 186240 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 246 2 2 3 1.6 Fc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4871980 186240 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 246 2 2 3 1.6 Fc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
134137104 142779 None 0 Human Functional pIC50 = 5.2 5.2 - 1
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 402 6 0 4 5.0 COc1ccccc1-c1cc(CN2CCN(c3ccccc3OC)CC2)ccc1C 10.1016/j.ejmech.2016.07.029
CHEMBL3892079 142779 None 0 Human Functional pIC50 = 5.2 5.2 - 1
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 402 6 0 4 5.0 COc1ccccc1-c1cc(CN2CCN(c3ccccc3OC)CC2)ccc1C 10.1016/j.ejmech.2016.07.029
134137104 142779 None 0 Human Functional pIC50 = 5.2 5.2 - 1
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 402 6 0 4 5.0 COc1ccccc1-c1cc(CN2CCN(c3ccccc3OC)CC2)ccc1C 10.1016/j.ejmech.2016.07.029
CHEMBL3892079 142779 None 0 Human Functional pIC50 = 5.2 5.2 - 1
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 402 6 0 4 5.0 COc1ccccc1-c1cc(CN2CCN(c3ccccc3OC)CC2)ccc1C 10.1016/j.ejmech.2016.07.029
117209964 186240 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 246 2 2 3 1.6 Fc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4871980 186240 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 246 2 2 3 1.6 Fc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
155510732 169623 None 0 Human Functional pIC50 = 6.2 6.2 1 2
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 430 6 1 1 6.9 Fc1ccc(C2CCN(CCCc3c[nH]c4ccc(F)cc34)CC2)c(-c2ccccc2)c1 10.1016/j.bmcl.2019.126703
CHEMBL4434876 169623 None 0 Human Functional pIC50 = 6.2 6.2 1 2
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 430 6 1 1 6.9 Fc1ccc(C2CCN(CCCc3c[nH]c4ccc(F)cc34)CC2)c(-c2ccccc2)c1 10.1016/j.bmcl.2019.126703
142601329 186623 None 6 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 276 2 2 3 2.5 Clc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4877603 186623 None 6 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 276 2 2 3 2.5 Clc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
142601329 186623 None 6 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 276 2 2 3 2.5 Clc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4877603 186623 None 6 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 276 2 2 3 2.5 Clc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
124247485 164164 None 6 Human Functional pIC50 = 5.2 5.2 - 1
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 231 1 2 2 1.9 Fc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4209274 164164 None 6 Human Functional pIC50 = 5.2 5.2 - 1
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 231 1 2 2 1.9 Fc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
124247485 164164 None 6 Human Functional pIC50 = 5.2 5.2 - 1
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 231 1 2 2 1.9 Fc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4209274 164164 None 6 Human Functional pIC50 = 5.2 5.2 - 1
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 231 1 2 2 1.9 Fc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
142601337 186076 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 260 2 2 3 2.0 Fc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4869695 186076 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 260 2 2 3 2.0 Fc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
142601337 186076 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 260 2 2 3 2.0 Fc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4869695 186076 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 260 2 2 3 2.0 Fc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
142601335 186527 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in beta-arrestin recruitment incubated for 22 hrs by bright-Glo reagent based Tango assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in beta-arrestin recruitment incubated for 22 hrs by bright-Glo reagent based Tango assay
ChEMBL 256 2 2 3 2.2 Cc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4876193 186527 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in beta-arrestin recruitment incubated for 22 hrs by bright-Glo reagent based Tango assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in beta-arrestin recruitment incubated for 22 hrs by bright-Glo reagent based Tango assay
ChEMBL 256 2 2 3 2.2 Cc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
142601335 186527 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in beta-arrestin recruitment incubated for 22 hrs by bright-Glo reagent based Tango assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in beta-arrestin recruitment incubated for 22 hrs by bright-Glo reagent based Tango assay
ChEMBL 256 2 2 3 2.2 Cc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4876193 186527 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in beta-arrestin recruitment incubated for 22 hrs by bright-Glo reagent based Tango assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in beta-arrestin recruitment incubated for 22 hrs by bright-Glo reagent based Tango assay
ChEMBL 256 2 2 3 2.2 Cc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
67268994 164063 None 2 Human Functional pIC50 = 5.1 5.1 - 1
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 247 1 2 2 2.4 Clc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4207884 164063 None 2 Human Functional pIC50 = 5.1 5.1 - 1
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 247 1 2 2 2.4 Clc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
67268994 164063 None 2 Human Functional pIC50 = 5.1 5.1 - 1
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 247 1 2 2 2.4 Clc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4207884 164063 None 2 Human Functional pIC50 = 5.1 5.1 - 1
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 247 1 2 2 2.4 Clc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
71574212 86318 None 0 Human Functional pIC50 = 5.1 5.1 -4 2
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)c1cnc2ccccc2c1 10.1016/j.ejmech.2012.11.042
CHEMBL2312935 86318 None 0 Human Functional pIC50 = 5.1 5.1 -4 2
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)c1cnc2ccccc2c1 10.1016/j.ejmech.2012.11.042
127028472 138258 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 470 8 2 6 2.2 CCOc1ccccc1N1CCN(CC(O)CN2C(=O)NC(C)(c3ccc(F)cc3)C2=O)CC1 10.1016/j.ejmech.2016.02.024
CHEMBL3769534 138258 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 470 8 2 6 2.2 CCOc1ccccc1N1CCN(CC(O)CN2C(=O)NC(C)(c3ccc(F)cc3)C2=O)CC1 10.1016/j.ejmech.2016.02.024
71574204 86301 None 0 Human Functional pIC50 = 6.1 6.1 18 2
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)c1cncc2ccccc12 10.1016/j.ejmech.2012.11.042
CHEMBL2312640 86301 None 0 Human Functional pIC50 = 6.1 6.1 18 2
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)c1cncc2ccccc12 10.1016/j.ejmech.2012.11.042
135367857 164699 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 228 1 1 3 2.3 Cc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4215875 164699 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 228 1 1 3 2.3 Cc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
135367857 164699 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 228 1 1 3 2.3 Cc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4215875 164699 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 228 1 1 3 2.3 Cc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
117209864 186140 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 258 3 2 4 1.5 COc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4870675 186140 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 258 3 2 4 1.5 COc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
117209864 186140 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 258 3 2 4 1.5 COc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4870675 186140 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 258 3 2 4 1.5 COc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
117209965 185353 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 262 2 2 3 2.1 Clc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4858338 185353 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 262 2 2 3 2.1 Clc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
142601341 185478 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 272 3 2 4 1.9 COc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4860503 185478 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 272 3 2 4 1.9 COc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
117209965 185353 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 262 2 2 3 2.1 Clc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4858338 185353 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 262 2 2 3 2.1 Clc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
142601341 185478 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 272 3 2 4 1.9 COc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4860503 185478 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 272 3 2 4 1.9 COc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
117209858 184660 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 262 2 2 3 2.1 Clc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4848305 184660 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 262 2 2 3 2.1 Clc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
117209858 184660 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 262 2 2 3 2.1 Clc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4848305 184660 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysisAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis
ChEMBL 262 2 2 3 2.1 Clc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
3233 3512 None 28 Guinea pig Functional pKd = 8.0 8.0 - 2
Antagonist activity at 5HT7 receptor assessed as inhibition of 4-(2-Diphenyl)-N-(4-pyridinylmethyl)-1-piperazinehexanamide mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAntagonist activity at 5HT7 receptor assessed as inhibition of 4-(2-Diphenyl)-N-(4-pyridinylmethyl)-1-piperazinehexanamide mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm800615e
3247 3512 None 28 Guinea pig Functional pKd = 8.0 8.0 - 2
Antagonist activity at 5HT7 receptor assessed as inhibition of 4-(2-Diphenyl)-N-(4-pyridinylmethyl)-1-piperazinehexanamide mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAntagonist activity at 5HT7 receptor assessed as inhibition of 4-(2-Diphenyl)-N-(4-pyridinylmethyl)-1-piperazinehexanamide mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm800615e
6604889 3512 None 28 Guinea pig Functional pKd = 8.0 8.0 - 2
Antagonist activity at 5HT7 receptor assessed as inhibition of 4-(2-Diphenyl)-N-(4-pyridinylmethyl)-1-piperazinehexanamide mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAntagonist activity at 5HT7 receptor assessed as inhibition of 4-(2-Diphenyl)-N-(4-pyridinylmethyl)-1-piperazinehexanamide mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm800615e
CHEMBL282199 3512 None 28 Guinea pig Functional pKd = 8.0 8.0 - 2
Antagonist activity at 5HT7 receptor assessed as inhibition of 4-(2-Diphenyl)-N-(4-pyridinylmethyl)-1-piperazinehexanamide mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAntagonist activity at 5HT7 receptor assessed as inhibition of 4-(2-Diphenyl)-N-(4-pyridinylmethyl)-1-piperazinehexanamide mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm800615e
DB13988 3512 None 28 Guinea pig Functional pKd = 8.0 8.0 - 2
Antagonist activity at 5HT7 receptor assessed as inhibition of 4-(2-Diphenyl)-N-(4-pyridinylmethyl)-1-piperazinehexanamide mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAntagonist activity at 5HT7 receptor assessed as inhibition of 4-(2-Diphenyl)-N-(4-pyridinylmethyl)-1-piperazinehexanamide mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm800615e
3233 3512 None 28 Guinea pig Functional pKd = 7.9 7.9 - 2
Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 4-(2-dimethylaminophenyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazine hexanamide mediated relaxation of substance P-induced contractionAntagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 4-(2-dimethylaminophenyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazine hexanamide mediated relaxation of substance P-induced contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm070487n
3247 3512 None 28 Guinea pig Functional pKd = 7.9 7.9 - 2
Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 4-(2-dimethylaminophenyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazine hexanamide mediated relaxation of substance P-induced contractionAntagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 4-(2-dimethylaminophenyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazine hexanamide mediated relaxation of substance P-induced contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm070487n
6604889 3512 None 28 Guinea pig Functional pKd = 7.9 7.9 - 2
Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 4-(2-dimethylaminophenyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazine hexanamide mediated relaxation of substance P-induced contractionAntagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 4-(2-dimethylaminophenyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazine hexanamide mediated relaxation of substance P-induced contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm070487n
CHEMBL282199 3512 None 28 Guinea pig Functional pKd = 7.9 7.9 - 2
Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 4-(2-dimethylaminophenyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazine hexanamide mediated relaxation of substance P-induced contractionAntagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 4-(2-dimethylaminophenyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazine hexanamide mediated relaxation of substance P-induced contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm070487n
DB13988 3512 None 28 Guinea pig Functional pKd = 7.9 7.9 - 2
Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 4-(2-dimethylaminophenyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazine hexanamide mediated relaxation of substance P-induced contractionAntagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 4-(2-dimethylaminophenyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazine hexanamide mediated relaxation of substance P-induced contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm070487n
3233 3512 None 28 Guinea pig Functional pKd = 7.8 7.8 - 2
Antagonist activity at 5HT7 receptor assessed as inhibition of 6-(4-Biphenyl-2-yl-piperazin-1-yl)-hexanoic acid (1,2,3,4-tetrahydro-naphthalen-1-yl)-amide mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAntagonist activity at 5HT7 receptor assessed as inhibition of 6-(4-Biphenyl-2-yl-piperazin-1-yl)-hexanoic acid (1,2,3,4-tetrahydro-naphthalen-1-yl)-amide mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm800615e
3247 3512 None 28 Guinea pig Functional pKd = 7.8 7.8 - 2
Antagonist activity at 5HT7 receptor assessed as inhibition of 6-(4-Biphenyl-2-yl-piperazin-1-yl)-hexanoic acid (1,2,3,4-tetrahydro-naphthalen-1-yl)-amide mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAntagonist activity at 5HT7 receptor assessed as inhibition of 6-(4-Biphenyl-2-yl-piperazin-1-yl)-hexanoic acid (1,2,3,4-tetrahydro-naphthalen-1-yl)-amide mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm800615e
6604889 3512 None 28 Guinea pig Functional pKd = 7.8 7.8 - 2
Antagonist activity at 5HT7 receptor assessed as inhibition of 6-(4-Biphenyl-2-yl-piperazin-1-yl)-hexanoic acid (1,2,3,4-tetrahydro-naphthalen-1-yl)-amide mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAntagonist activity at 5HT7 receptor assessed as inhibition of 6-(4-Biphenyl-2-yl-piperazin-1-yl)-hexanoic acid (1,2,3,4-tetrahydro-naphthalen-1-yl)-amide mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm800615e
CHEMBL282199 3512 None 28 Guinea pig Functional pKd = 7.8 7.8 - 2
Antagonist activity at 5HT7 receptor assessed as inhibition of 6-(4-Biphenyl-2-yl-piperazin-1-yl)-hexanoic acid (1,2,3,4-tetrahydro-naphthalen-1-yl)-amide mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAntagonist activity at 5HT7 receptor assessed as inhibition of 6-(4-Biphenyl-2-yl-piperazin-1-yl)-hexanoic acid (1,2,3,4-tetrahydro-naphthalen-1-yl)-amide mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm800615e
DB13988 3512 None 28 Guinea pig Functional pKd = 7.8 7.8 - 2
Antagonist activity at 5HT7 receptor assessed as inhibition of 6-(4-Biphenyl-2-yl-piperazin-1-yl)-hexanoic acid (1,2,3,4-tetrahydro-naphthalen-1-yl)-amide mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAntagonist activity at 5HT7 receptor assessed as inhibition of 6-(4-Biphenyl-2-yl-piperazin-1-yl)-hexanoic acid (1,2,3,4-tetrahydro-naphthalen-1-yl)-amide mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm800615e
3233 3512 None 28 Guinea pig Functional pKd = 7.8 7.8 - 2
Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 4-(2-diphenyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazine hexanamide mediated relaxation of substance P-induced contractionAntagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 4-(2-diphenyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazine hexanamide mediated relaxation of substance P-induced contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm070487n
3247 3512 None 28 Guinea pig Functional pKd = 7.8 7.8 - 2
Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 4-(2-diphenyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazine hexanamide mediated relaxation of substance P-induced contractionAntagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 4-(2-diphenyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazine hexanamide mediated relaxation of substance P-induced contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm070487n
6604889 3512 None 28 Guinea pig Functional pKd = 7.8 7.8 - 2
Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 4-(2-diphenyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazine hexanamide mediated relaxation of substance P-induced contractionAntagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 4-(2-diphenyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazine hexanamide mediated relaxation of substance P-induced contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm070487n
CHEMBL282199 3512 None 28 Guinea pig Functional pKd = 7.8 7.8 - 2
Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 4-(2-diphenyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazine hexanamide mediated relaxation of substance P-induced contractionAntagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 4-(2-diphenyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazine hexanamide mediated relaxation of substance P-induced contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm070487n
DB13988 3512 None 28 Guinea pig Functional pKd = 7.8 7.8 - 2
Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 4-(2-diphenyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazine hexanamide mediated relaxation of substance P-induced contractionAntagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 4-(2-diphenyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazine hexanamide mediated relaxation of substance P-induced contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm070487n
3233 3512 None 28 Guinea pig Functional pKd = 7.8 7.8 - 2
Antagonist activity at 5HT7 receptor assessed as inhibition of 2-[6-[4-(2-Diphenyl)-1-piperazinyl]-1-oxohexyl]-1,2,3,4-tetrahydroisoquinoline mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAntagonist activity at 5HT7 receptor assessed as inhibition of 2-[6-[4-(2-Diphenyl)-1-piperazinyl]-1-oxohexyl]-1,2,3,4-tetrahydroisoquinoline mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm800615e
3247 3512 None 28 Guinea pig Functional pKd = 7.8 7.8 - 2
Antagonist activity at 5HT7 receptor assessed as inhibition of 2-[6-[4-(2-Diphenyl)-1-piperazinyl]-1-oxohexyl]-1,2,3,4-tetrahydroisoquinoline mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAntagonist activity at 5HT7 receptor assessed as inhibition of 2-[6-[4-(2-Diphenyl)-1-piperazinyl]-1-oxohexyl]-1,2,3,4-tetrahydroisoquinoline mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm800615e
6604889 3512 None 28 Guinea pig Functional pKd = 7.8 7.8 - 2
Antagonist activity at 5HT7 receptor assessed as inhibition of 2-[6-[4-(2-Diphenyl)-1-piperazinyl]-1-oxohexyl]-1,2,3,4-tetrahydroisoquinoline mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAntagonist activity at 5HT7 receptor assessed as inhibition of 2-[6-[4-(2-Diphenyl)-1-piperazinyl]-1-oxohexyl]-1,2,3,4-tetrahydroisoquinoline mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm800615e
CHEMBL282199 3512 None 28 Guinea pig Functional pKd = 7.8 7.8 - 2
Antagonist activity at 5HT7 receptor assessed as inhibition of 2-[6-[4-(2-Diphenyl)-1-piperazinyl]-1-oxohexyl]-1,2,3,4-tetrahydroisoquinoline mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAntagonist activity at 5HT7 receptor assessed as inhibition of 2-[6-[4-(2-Diphenyl)-1-piperazinyl]-1-oxohexyl]-1,2,3,4-tetrahydroisoquinoline mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm800615e
DB13988 3512 None 28 Guinea pig Functional pKd = 7.8 7.8 - 2
Antagonist activity at 5HT7 receptor assessed as inhibition of 2-[6-[4-(2-Diphenyl)-1-piperazinyl]-1-oxohexyl]-1,2,3,4-tetrahydroisoquinoline mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAntagonist activity at 5HT7 receptor assessed as inhibition of 2-[6-[4-(2-Diphenyl)-1-piperazinyl]-1-oxohexyl]-1,2,3,4-tetrahydroisoquinoline mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm800615e
24768520 93060 None 0 Guinea pig Functional pKd = 7.7 7.7 - 0
Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on substance P-induced contractionAntagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on substance P-induced contraction
ChEMBL 434 9 2 4 4.6 CNc1ccccc1N1CCN(CCCCCC(=O)NC2CCCc3ccccc32)CC1 10.1021/jm070487n
CHEMBL244161 93060 None 0 Guinea pig Functional pKd = 7.7 7.7 - 0
Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on substance P-induced contractionAntagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on substance P-induced contraction
ChEMBL 434 9 2 4 4.6 CNc1ccccc1N1CCN(CCCCCC(=O)NC2CCCc3ccccc32)CC1 10.1021/jm070487n
3233 3512 None 28 Guinea pig Functional pKd = 7.7 7.7 - 2
Antagonist activity at 5HT7 receptor assessed as inhibition of N-(4-Cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamide mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAntagonist activity at 5HT7 receptor assessed as inhibition of N-(4-Cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamide mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm800615e
3247 3512 None 28 Guinea pig Functional pKd = 7.7 7.7 - 2
Antagonist activity at 5HT7 receptor assessed as inhibition of N-(4-Cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamide mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAntagonist activity at 5HT7 receptor assessed as inhibition of N-(4-Cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamide mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm800615e
6604889 3512 None 28 Guinea pig Functional pKd = 7.7 7.7 - 2
Antagonist activity at 5HT7 receptor assessed as inhibition of N-(4-Cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamide mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAntagonist activity at 5HT7 receptor assessed as inhibition of N-(4-Cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamide mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm800615e
CHEMBL282199 3512 None 28 Guinea pig Functional pKd = 7.7 7.7 - 2
Antagonist activity at 5HT7 receptor assessed as inhibition of N-(4-Cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamide mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAntagonist activity at 5HT7 receptor assessed as inhibition of N-(4-Cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamide mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm800615e
DB13988 3512 None 28 Guinea pig Functional pKd = 7.7 7.7 - 2
Antagonist activity at 5HT7 receptor assessed as inhibition of N-(4-Cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamide mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAntagonist activity at 5HT7 receptor assessed as inhibition of N-(4-Cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamide mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm800615e
3233 3512 None 28 Guinea pig Functional pKd = 8.4 8.4 - 2
Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 6-(4-(2-chlorophenyl)piperazine-1-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)hexanamide mediated relaxation of substance P-induced contractionAntagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 6-(4-(2-chlorophenyl)piperazine-1-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)hexanamide mediated relaxation of substance P-induced contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm070487n
3247 3512 None 28 Guinea pig Functional pKd = 8.4 8.4 - 2
Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 6-(4-(2-chlorophenyl)piperazine-1-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)hexanamide mediated relaxation of substance P-induced contractionAntagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 6-(4-(2-chlorophenyl)piperazine-1-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)hexanamide mediated relaxation of substance P-induced contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm070487n
6604889 3512 None 28 Guinea pig Functional pKd = 8.4 8.4 - 2
Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 6-(4-(2-chlorophenyl)piperazine-1-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)hexanamide mediated relaxation of substance P-induced contractionAntagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 6-(4-(2-chlorophenyl)piperazine-1-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)hexanamide mediated relaxation of substance P-induced contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm070487n
CHEMBL282199 3512 None 28 Guinea pig Functional pKd = 8.4 8.4 - 2
Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 6-(4-(2-chlorophenyl)piperazine-1-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)hexanamide mediated relaxation of substance P-induced contractionAntagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 6-(4-(2-chlorophenyl)piperazine-1-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)hexanamide mediated relaxation of substance P-induced contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm070487n
DB13988 3512 None 28 Guinea pig Functional pKd = 8.4 8.4 - 2
Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 6-(4-(2-chlorophenyl)piperazine-1-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)hexanamide mediated relaxation of substance P-induced contractionAntagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 6-(4-(2-chlorophenyl)piperazine-1-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)hexanamide mediated relaxation of substance P-induced contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm070487n
3233 3512 None 28 Guinea pig Functional pKd = 7.5 7.5 - 2
Antagonist activity at 5HT7 receptor assessed as inhibition of 5-carboxamidotryptamine mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAntagonist activity at 5HT7 receptor assessed as inhibition of 5-carboxamidotryptamine mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm800615e
3247 3512 None 28 Guinea pig Functional pKd = 7.5 7.5 - 2
Antagonist activity at 5HT7 receptor assessed as inhibition of 5-carboxamidotryptamine mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAntagonist activity at 5HT7 receptor assessed as inhibition of 5-carboxamidotryptamine mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm800615e
6604889 3512 None 28 Guinea pig Functional pKd = 7.5 7.5 - 2
Antagonist activity at 5HT7 receptor assessed as inhibition of 5-carboxamidotryptamine mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAntagonist activity at 5HT7 receptor assessed as inhibition of 5-carboxamidotryptamine mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm800615e
CHEMBL282199 3512 None 28 Guinea pig Functional pKd = 7.5 7.5 - 2
Antagonist activity at 5HT7 receptor assessed as inhibition of 5-carboxamidotryptamine mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAntagonist activity at 5HT7 receptor assessed as inhibition of 5-carboxamidotryptamine mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm800615e
DB13988 3512 None 28 Guinea pig Functional pKd = 7.5 7.5 - 2
Antagonist activity at 5HT7 receptor assessed as inhibition of 5-carboxamidotryptamine mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAntagonist activity at 5HT7 receptor assessed as inhibition of 5-carboxamidotryptamine mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm800615e
3233 3512 None 28 Guinea pig Functional pKd = 7.5 7.5 - 2
Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 3-(2-aminoethyl)-1H-indole-5-carboxamide mediated relaxation of substance P-induced contractionAntagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 3-(2-aminoethyl)-1H-indole-5-carboxamide mediated relaxation of substance P-induced contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm070487n
3247 3512 None 28 Guinea pig Functional pKd = 7.5 7.5 - 2
Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 3-(2-aminoethyl)-1H-indole-5-carboxamide mediated relaxation of substance P-induced contractionAntagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 3-(2-aminoethyl)-1H-indole-5-carboxamide mediated relaxation of substance P-induced contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm070487n
6604889 3512 None 28 Guinea pig Functional pKd = 7.5 7.5 - 2
Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 3-(2-aminoethyl)-1H-indole-5-carboxamide mediated relaxation of substance P-induced contractionAntagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 3-(2-aminoethyl)-1H-indole-5-carboxamide mediated relaxation of substance P-induced contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm070487n
CHEMBL282199 3512 None 28 Guinea pig Functional pKd = 7.5 7.5 - 2
Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 3-(2-aminoethyl)-1H-indole-5-carboxamide mediated relaxation of substance P-induced contractionAntagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 3-(2-aminoethyl)-1H-indole-5-carboxamide mediated relaxation of substance P-induced contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm070487n
DB13988 3512 None 28 Guinea pig Functional pKd = 7.5 7.5 - 2
Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 3-(2-aminoethyl)-1H-indole-5-carboxamide mediated relaxation of substance P-induced contractionAntagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 3-(2-aminoethyl)-1H-indole-5-carboxamide mediated relaxation of substance P-induced contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm070487n
3233 3512 None 28 Guinea pig Functional pKd = 8.2 8.2 - 2
Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 6-(4-(2-nitrophenyl)piperazin-1-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)hexanamide mediated relaxation of substance P-induced contractionAntagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 6-(4-(2-nitrophenyl)piperazin-1-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)hexanamide mediated relaxation of substance P-induced contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm070487n
3247 3512 None 28 Guinea pig Functional pKd = 8.2 8.2 - 2
Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 6-(4-(2-nitrophenyl)piperazin-1-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)hexanamide mediated relaxation of substance P-induced contractionAntagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 6-(4-(2-nitrophenyl)piperazin-1-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)hexanamide mediated relaxation of substance P-induced contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm070487n
6604889 3512 None 28 Guinea pig Functional pKd = 8.2 8.2 - 2
Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 6-(4-(2-nitrophenyl)piperazin-1-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)hexanamide mediated relaxation of substance P-induced contractionAntagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 6-(4-(2-nitrophenyl)piperazin-1-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)hexanamide mediated relaxation of substance P-induced contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm070487n
CHEMBL282199 3512 None 28 Guinea pig Functional pKd = 8.2 8.2 - 2
Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 6-(4-(2-nitrophenyl)piperazin-1-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)hexanamide mediated relaxation of substance P-induced contractionAntagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 6-(4-(2-nitrophenyl)piperazin-1-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)hexanamide mediated relaxation of substance P-induced contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm070487n
DB13988 3512 None 28 Guinea pig Functional pKd = 8.2 8.2 - 2
Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 6-(4-(2-nitrophenyl)piperazin-1-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)hexanamide mediated relaxation of substance P-induced contractionAntagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 6-(4-(2-nitrophenyl)piperazin-1-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)hexanamide mediated relaxation of substance P-induced contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm070487n
3233 3512 None 28 Guinea pig Functional pKd = 8.1 8.1 - 2
Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 6-(4-phenylpiperazin-1-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)hexanamide mediated relaxation of substance P-induced contractionAntagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 6-(4-phenylpiperazin-1-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)hexanamide mediated relaxation of substance P-induced contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm070487n
3247 3512 None 28 Guinea pig Functional pKd = 8.1 8.1 - 2
Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 6-(4-phenylpiperazin-1-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)hexanamide mediated relaxation of substance P-induced contractionAntagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 6-(4-phenylpiperazin-1-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)hexanamide mediated relaxation of substance P-induced contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm070487n
6604889 3512 None 28 Guinea pig Functional pKd = 8.1 8.1 - 2
Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 6-(4-phenylpiperazin-1-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)hexanamide mediated relaxation of substance P-induced contractionAntagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 6-(4-phenylpiperazin-1-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)hexanamide mediated relaxation of substance P-induced contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm070487n
CHEMBL282199 3512 None 28 Guinea pig Functional pKd = 8.1 8.1 - 2
Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 6-(4-phenylpiperazin-1-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)hexanamide mediated relaxation of substance P-induced contractionAntagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 6-(4-phenylpiperazin-1-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)hexanamide mediated relaxation of substance P-induced contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm070487n
DB13988 3512 None 28 Guinea pig Functional pKd = 8.1 8.1 - 2
Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 6-(4-phenylpiperazin-1-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)hexanamide mediated relaxation of substance P-induced contractionAntagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 6-(4-phenylpiperazin-1-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)hexanamide mediated relaxation of substance P-induced contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm070487n
3233 3512 None 28 Guinea pig Functional pKd = 8.1 8.1 - 2
Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 4-[2-(1-methylethyl)phenyl]-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazine hexanamide mediated relaxation of substance P-induced contractionAntagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 4-[2-(1-methylethyl)phenyl]-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazine hexanamide mediated relaxation of substance P-induced contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm070487n
3247 3512 None 28 Guinea pig Functional pKd = 8.1 8.1 - 2
Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 4-[2-(1-methylethyl)phenyl]-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazine hexanamide mediated relaxation of substance P-induced contractionAntagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 4-[2-(1-methylethyl)phenyl]-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazine hexanamide mediated relaxation of substance P-induced contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm070487n
6604889 3512 None 28 Guinea pig Functional pKd = 8.1 8.1 - 2
Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 4-[2-(1-methylethyl)phenyl]-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazine hexanamide mediated relaxation of substance P-induced contractionAntagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 4-[2-(1-methylethyl)phenyl]-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazine hexanamide mediated relaxation of substance P-induced contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm070487n
CHEMBL282199 3512 None 28 Guinea pig Functional pKd = 8.1 8.1 - 2
Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 4-[2-(1-methylethyl)phenyl]-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazine hexanamide mediated relaxation of substance P-induced contractionAntagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 4-[2-(1-methylethyl)phenyl]-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazine hexanamide mediated relaxation of substance P-induced contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm070487n
DB13988 3512 None 28 Guinea pig Functional pKd = 8.1 8.1 - 2
Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 4-[2-(1-methylethyl)phenyl]-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazine hexanamide mediated relaxation of substance P-induced contractionAntagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 4-[2-(1-methylethyl)phenyl]-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazine hexanamide mediated relaxation of substance P-induced contraction
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm070487n
118731356 118256 None 0 Human Functional pKi = 7.7 7.7 - 0
Agonist activity at human 5HT7 receptor expressed in HEK293 cells assessed as cAMP concentration at 10'-6 M by adenylate cyclase activity based HTRF assay relative to controlAgonist activity at human 5HT7 receptor expressed in HEK293 cells assessed as cAMP concentration at 10'-6 M by adenylate cyclase activity based HTRF assay relative to control
ChEMBL 502 8 0 4 4.6 O=C([C@@H]1CCCN1C(=O)CCCCN1CCN(c2ccccc2-c2ccccc2)CC1)N1CCCCC1 10.1016/j.ejmech.2014.12.041
CHEMBL3409039 118256 None 0 Human Functional pKi = 7.7 7.7 - 0
Agonist activity at human 5HT7 receptor expressed in HEK293 cells assessed as cAMP concentration at 10'-6 M by adenylate cyclase activity based HTRF assay relative to controlAgonist activity at human 5HT7 receptor expressed in HEK293 cells assessed as cAMP concentration at 10'-6 M by adenylate cyclase activity based HTRF assay relative to control
ChEMBL 502 8 0 4 4.6 O=C([C@@H]1CCCN1C(=O)CCCCN1CCN(c2ccccc2-c2ccccc2)CC1)N1CCCCC1 10.1016/j.ejmech.2014.12.041
4806 4008 None 55 Human Functional pKi = 6.4 6.4 - 3
Antagonist activity at human 5HT7 receptor expressed in HEK-CNG cells assessed as effect on cAMP production by fluorescence based assayAntagonist activity at human 5HT7 receptor expressed in HEK-CNG cells assessed as effect on cAMP production by fluorescence based assay
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
71768094 4008 None 55 Human Functional pKi = 6.4 6.4 - 3
Antagonist activity at human 5HT7 receptor expressed in HEK-CNG cells assessed as effect on cAMP production by fluorescence based assayAntagonist activity at human 5HT7 receptor expressed in HEK-CNG cells assessed as effect on cAMP production by fluorescence based assay
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
71768094.0 4008 None 55 Human Functional pKi = 6.4 6.4 - 3
Antagonist activity at human 5HT7 receptor expressed in HEK-CNG cells assessed as effect on cAMP production by fluorescence based assayAntagonist activity at human 5HT7 receptor expressed in HEK-CNG cells assessed as effect on cAMP production by fluorescence based assay
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
7351 4008 None 55 Human Functional pKi = 6.4 6.4 - 3
Antagonist activity at human 5HT7 receptor expressed in HEK-CNG cells assessed as effect on cAMP production by fluorescence based assayAntagonist activity at human 5HT7 receptor expressed in HEK-CNG cells assessed as effect on cAMP production by fluorescence based assay
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
9966051 4008 None 55 Human Functional pKi = 6.4 6.4 - 3
Antagonist activity at human 5HT7 receptor expressed in HEK-CNG cells assessed as effect on cAMP production by fluorescence based assayAntagonist activity at human 5HT7 receptor expressed in HEK-CNG cells assessed as effect on cAMP production by fluorescence based assay
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
9966051.0 4008 None 55 Human Functional pKi = 6.4 6.4 - 3
Antagonist activity at human 5HT7 receptor expressed in HEK-CNG cells assessed as effect on cAMP production by fluorescence based assayAntagonist activity at human 5HT7 receptor expressed in HEK-CNG cells assessed as effect on cAMP production by fluorescence based assay
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
CHEMBL2104993 4008 None 55 Human Functional pKi = 6.4 6.4 - 3
Antagonist activity at human 5HT7 receptor expressed in HEK-CNG cells assessed as effect on cAMP production by fluorescence based assayAntagonist activity at human 5HT7 receptor expressed in HEK-CNG cells assessed as effect on cAMP production by fluorescence based assay
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
DB09068 4008 None 55 Human Functional pKi = 6.4 6.4 - 3
Antagonist activity at human 5HT7 receptor expressed in HEK-CNG cells assessed as effect on cAMP production by fluorescence based assayAntagonist activity at human 5HT7 receptor expressed in HEK-CNG cells assessed as effect on cAMP production by fluorescence based assay
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
118731351 118252 None 0 Human Functional pKi = 8.2 8.2 - 0
Agonist activity at human 5HT7 receptor expressed in HEK293 cells assessed as cAMP concentration at 10'-6 M by adenylate cyclase activity based HTRF assay relative to controlAgonist activity at human 5HT7 receptor expressed in HEK293 cells assessed as cAMP concentration at 10'-6 M by adenylate cyclase activity based HTRF assay relative to control
ChEMBL 496 8 1 4 4.1 NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCCCN1CCN(c2ccccc2-c2ccccc2)CC1 10.1016/j.ejmech.2014.12.041
CHEMBL3409035 118252 None 0 Human Functional pKi = 8.2 8.2 - 0
Agonist activity at human 5HT7 receptor expressed in HEK293 cells assessed as cAMP concentration at 10'-6 M by adenylate cyclase activity based HTRF assay relative to controlAgonist activity at human 5HT7 receptor expressed in HEK293 cells assessed as cAMP concentration at 10'-6 M by adenylate cyclase activity based HTRF assay relative to control
ChEMBL 496 8 1 4 4.1 NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCCCN1CCN(c2ccccc2-c2ccccc2)CC1 10.1016/j.ejmech.2014.12.041
118731356 118256 None 0 Human Functional pKi = 7.0 7.0 - 0
Antagonist activity at human 5HT7 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP concentration at 10'-6 M by adenylate cyclase activity based HTRF assay relative to controlAntagonist activity at human 5HT7 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP concentration at 10'-6 M by adenylate cyclase activity based HTRF assay relative to control
ChEMBL 502 8 0 4 4.6 O=C([C@@H]1CCCN1C(=O)CCCCN1CCN(c2ccccc2-c2ccccc2)CC1)N1CCCCC1 10.1016/j.ejmech.2014.12.041
CHEMBL3409039 118256 None 0 Human Functional pKi = 7.0 7.0 - 0
Antagonist activity at human 5HT7 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP concentration at 10'-6 M by adenylate cyclase activity based HTRF assay relative to controlAntagonist activity at human 5HT7 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP concentration at 10'-6 M by adenylate cyclase activity based HTRF assay relative to control
ChEMBL 502 8 0 4 4.6 O=C([C@@H]1CCCN1C(=O)CCCCN1CCN(c2ccccc2-c2ccccc2)CC1)N1CCCCC1 10.1016/j.ejmech.2014.12.041
118731351 118252 None 0 Human Functional pKi = 7.0 7.0 - 0
Antagonist activity at human 5HT7 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP concentration at 10'-6 M by adenylate cyclase activity based HTRF assay relative to controlAntagonist activity at human 5HT7 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP concentration at 10'-6 M by adenylate cyclase activity based HTRF assay relative to control
ChEMBL 496 8 1 4 4.1 NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCCCN1CCN(c2ccccc2-c2ccccc2)CC1 10.1016/j.ejmech.2014.12.041
CHEMBL3409035 118252 None 0 Human Functional pKi = 7.0 7.0 - 0
Antagonist activity at human 5HT7 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP concentration at 10'-6 M by adenylate cyclase activity based HTRF assay relative to controlAntagonist activity at human 5HT7 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP concentration at 10'-6 M by adenylate cyclase activity based HTRF assay relative to control
ChEMBL 496 8 1 4 4.1 NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCCCN1CCN(c2ccccc2-c2ccccc2)CC1 10.1016/j.ejmech.2014.12.041
240 944 None 25 Human Functional pEC50 = 8.2 8.2 -1 22
NoneNone
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
2769 944 None 25 Human Functional pEC50 = 8.2 8.2 -1 22
NoneNone
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
44279790 944 None 25 Human Functional pEC50 = 8.2 8.2 -1 22
NoneNone
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
660 944 None 25 Human Functional pEC50 = 8.2 8.2 -1 22
NoneNone
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL1729 944 None 25 Human Functional pEC50 = 8.2 8.2 -1 22
NoneNone
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL560739 944 None 25 Human Functional pEC50 = 8.2 8.2 -1 22
NoneNone
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
DB00604 944 None 25 Human Functional pEC50 = 8.2 8.2 -1 22
NoneNone
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
4223 3992 None 57 Rat Functional pIC50 = 8.3 8.3 -562 17
Inhibition of rat hydroxytryptamine 7 receptorInhibition of rat hydroxytryptamine 7 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
6918314 3992 None 57 Rat Functional pIC50 = 8.3 8.3 -562 17
Inhibition of rat hydroxytryptamine 7 receptorInhibition of rat hydroxytryptamine 7 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
6918314.0 3992 None 57 Rat Functional pIC50 = 8.3 8.3 -562 17
Inhibition of rat hydroxytryptamine 7 receptorInhibition of rat hydroxytryptamine 7 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
7427 3992 None 57 Rat Functional pIC50 = 8.3 8.3 -562 17
Inhibition of rat hydroxytryptamine 7 receptorInhibition of rat hydroxytryptamine 7 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
CHEMBL439849 3992 None 57 Rat Functional pIC50 = 8.3 8.3 -562 17
Inhibition of rat hydroxytryptamine 7 receptorInhibition of rat hydroxytryptamine 7 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
DB06684 3992 None 57 Rat Functional pIC50 = 8.3 8.3 -562 17
Inhibition of rat hydroxytryptamine 7 receptorInhibition of rat hydroxytryptamine 7 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None


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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
Sel. page Common
name		 GPCRdb
ID		 Reference
ligand		 Vendors

 Species

 Assay
Type		 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
135398737 958 None 57 Human Binding pAC50 = 7.0 7.0 -13 91
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
135398737.0 958 None 57 Human Binding pAC50 = 7.0 7.0 -13 91
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
38 958 None 57 Human Binding pAC50 = 7.0 7.0 -13 91
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
722 958 None 57 Human Binding pAC50 = 7.0 7.0 -13 91
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL42 958 None 57 Human Binding pAC50 = 7.0 7.0 -13 91
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
DB00363 958 None 57 Human Binding pAC50 = 7.0 7.0 -13 91
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
3158 56283 None 21 Human Binding pAC50 = 5.8 5.8 - 20
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
3158.0 56283 None 21 Human Binding pAC50 = 5.8 5.8 - 20
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1628227 56283 None 21 Human Binding pAC50 = 5.8 5.8 - 20
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
DB01142 56283 None 21 Human Binding pAC50 = 5.8 5.8 - 20
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
2585 803 None 59 Human Binding pAC50 = 5.8 5.8 - 22
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
2585.0 803 None 59 Human Binding pAC50 = 5.8 5.8 - 22
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
522 803 None 59 Human Binding pAC50 = 5.8 5.8 - 22
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
551 803 None 59 Human Binding pAC50 = 5.8 5.8 - 22
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
CHEMBL723 803 None 59 Human Binding pAC50 = 5.8 5.8 - 22
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
DB01136 803 None 59 Human Binding pAC50 = 5.8 5.8 - 22
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
2247 505 None 55 Human Binding pAC50 = 5.8 5.8 - 41
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
249 505 None 55 Human Binding pAC50 = 5.8 5.8 - 41
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
2603 505 None 55 Human Binding pAC50 = 5.8 5.8 - 41
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
CHEMBL296419 505 None 55 Human Binding pAC50 = 5.8 5.8 - 41
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
DB00637 505 None 55 Human Binding pAC50 = 5.8 5.8 - 41
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
2284 3182 None 26 Human Binding pAC50 = 5.7 5.7 - 28
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
4926 3182 None 26 Human Binding pAC50 = 5.7 5.7 - 28
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
7281 3182 None 26 Human Binding pAC50 = 5.7 5.7 - 28
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL564 3182 None 26 Human Binding pAC50 = 5.7 5.7 - 28
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00420 3182 None 26 Human Binding pAC50 = 5.7 5.7 - 28
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
2337 3256 None 51 Human Binding pAC50 = 5.7 5.7 -28 62
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
50 3256 None 51 Human Binding pAC50 = 5.7 5.7 -28 62
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
5002 3256 None 51 Human Binding pAC50 = 5.7 5.7 -28 62
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
5002.0 3256 None 51 Human Binding pAC50 = 5.7 5.7 -28 62
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL716 3256 None 51 Human Binding pAC50 = 5.7 5.7 -28 62
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
DB01224 3256 None 51 Human Binding pAC50 = 5.7 5.7 -28 62
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
1890 2759 None 31 Human Binding pAC50 = 6.6 6.6 -8 26
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
4449 2759 None 31 Human Binding pAC50 = 6.6 6.6 -8 26
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
7247 2759 None 31 Human Binding pAC50 = 6.6 6.6 -8 26
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
CHEMBL623 2759 None 31 Human Binding pAC50 = 6.6 6.6 -8 26
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
DB01149 2759 None 31 Human Binding pAC50 = 6.6 6.6 -8 26
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
212 3806 None 35 Human Binding pAC50 = 6.6 6.6 -7 25
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
2639 3806 None 35 Human Binding pAC50 = 6.6 6.6 -7 25
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
941651 3806 None 35 Human Binding pAC50 = 6.6 6.6 -7 25
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
941651.0 3806 None 35 Human Binding pAC50 = 6.6 6.6 -7 25
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
CHEMBL1201 3806 None 35 Human Binding pAC50 = 6.6 6.6 -7 25
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
DB01623 3806 None 35 Human Binding pAC50 = 6.6 6.6 -7 25
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
2389 3331 None 72 Human Binding pAC50 = 7.5 7.5 -7 67
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
5073 3331 None 72 Human Binding pAC50 = 7.5 7.5 -7 67
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
5073.0 3331 None 72 Human Binding pAC50 = 7.5 7.5 -7 67
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
96 3331 None 72 Human Binding pAC50 = 7.5 7.5 -7 67
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
CHEMBL85 3331 None 72 Human Binding pAC50 = 7.5 7.5 -7 67
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
DB00734 3331 None 72 Human Binding pAC50 = 7.5 7.5 -7 67
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
135 2532 None 33 Human Binding pAC50 = 6.4 6.4 -83 57
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
1796 2532 None 33 Human Binding pAC50 = 6.4 6.4 -83 57
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
4184 2532 None 33 Human Binding pAC50 = 6.4 6.4 -83 57
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
4184.0 2532 None 33 Human Binding pAC50 = 6.4 6.4 -83 57
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
CHEMBL6437 2532 None 33 Human Binding pAC50 = 6.4 6.4 -83 57
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
DB06148 2532 None 33 Human Binding pAC50 = 6.4 6.4 -83 57
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
2543 3707 None 46 Human Binding pAC50 = 5.3 5.3 -93 31
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1038/s41467-023-40064-9
5358 3707 None 46 Human Binding pAC50 = 5.3 5.3 -93 31
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1038/s41467-023-40064-9
5358.0 3707 None 46 Human Binding pAC50 = 5.3 5.3 -93 31
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1038/s41467-023-40064-9
54 3707 None 46 Human Binding pAC50 = 5.3 5.3 -93 31
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1038/s41467-023-40064-9
CHEMBL128 3707 None 46 Human Binding pAC50 = 5.3 5.3 -93 31
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1038/s41467-023-40064-9
DB00669 3707 None 46 Human Binding pAC50 = 5.3 5.3 -93 31
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1038/s41467-023-40064-9
191 403 None 60 Human Binding pAC50 = 6.2 6.2 -41 28
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
201 403 None 60 Human Binding pAC50 = 6.2 6.2 -41 28
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
2170 403 None 60 Human Binding pAC50 = 6.2 6.2 -41 28
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
2170.0 403 None 60 Human Binding pAC50 = 6.2 6.2 -41 28
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
CHEMBL1113 403 None 60 Human Binding pAC50 = 6.2 6.2 -41 28
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
DB00543 403 None 60 Human Binding pAC50 = 6.2 6.2 -41 28
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
135398745 2914 None 65 Human Binding pAC50 = 6.2 6.2 -95 65
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
135398745.0 2914 None 65 Human Binding pAC50 = 6.2 6.2 -95 65
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
47 2914 None 65 Human Binding pAC50 = 6.2 6.2 -95 65
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
CHEMBL715 2914 None 65 Human Binding pAC50 = 6.2 6.2 -95 65
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
DB00334 2914 None 65 Human Binding pAC50 = 6.2 6.2 -95 65
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
1400 1957 None 46 Human Binding pAC50 = 5.2 5.2 - 3
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
3658 1957 None 46 Human Binding pAC50 = 5.2 5.2 - 3
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
3658.0 1957 None 46 Human Binding pAC50 = 5.2 5.2 - 3
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
7199 1957 None 46 Human Binding pAC50 = 5.2 5.2 - 3
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
91513 1957 None 46 Human Binding pAC50 = 5.2 5.2 - 3
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL896 1957 None 46 Human Binding pAC50 = 5.2 5.2 - 3
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
DB00557 1957 None 46 Human Binding pAC50 = 5.2 5.2 - 3
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
2726 919 None 48 Human Binding pAC50 = 6.1 6.1 -13 72
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2726.0 919 None 48 Human Binding pAC50 = 6.1 6.1 -13 72
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
621 919 None 48 Human Binding pAC50 = 6.1 6.1 -13 72
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
83 919 None 48 Human Binding pAC50 = 6.1 6.1 -13 72
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL71 919 None 48 Human Binding pAC50 = 6.1 6.1 -13 72
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB00477 919 None 48 Human Binding pAC50 = 6.1 6.1 -13 72
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
1613 2348 None 42 Human Binding pAC50 = 6.1 6.1 -19 44
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
205 2348 None 42 Human Binding pAC50 = 6.1 6.1 -19 44
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
3964 2348 None 42 Human Binding pAC50 = 6.1 6.1 -19 44
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
3964.0 2348 None 42 Human Binding pAC50 = 6.1 6.1 -19 44
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
CHEMBL831 2348 None 42 Human Binding pAC50 = 6.1 6.1 -19 44
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
DB00408 2348 None 42 Human Binding pAC50 = 6.1 6.1 -19 44
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
135409453 3773 None 26 Human Binding pAC50 = 6.1 6.1 - 19
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
226 3773 None 26 Human Binding pAC50 = 6.1 6.1 - 19
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
CHEMBL76370 3773 None 26 Human Binding pAC50 = 6.1 6.1 - 19
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
1353 1911 None 63 Human Binding pAC50 = 5.1 5.1 -263 85
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3559 1911 None 63 Human Binding pAC50 = 5.1 5.1 -263 85
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3559.0 1911 None 63 Human Binding pAC50 = 5.1 5.1 -263 85
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
86 1911 None 63 Human Binding pAC50 = 5.1 5.1 -263 85
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
CHEMBL54 1911 None 63 Human Binding pAC50 = 5.1 5.1 -263 85
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
DB00502 1911 None 63 Human Binding pAC50 = 5.1 5.1 -263 85
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
392622 56328 None 57 Human Binding pAC50 = 5.1 5.1 - 4
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 720 17 4 9 5.9 CC(C)c1nc(CN(C)C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C[C@H](O)[C@H](Cc2ccccc2)NC(=O)OCc2cncs2)C(C)C)cs1 10.1038/s41467-023-40064-9
CHEMBL163 56328 None 57 Human Binding pAC50 = 5.1 5.1 - 4
Binding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR7 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 720 17 4 9 5.9 CC(C)c1nc(CN(C)C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C[C@H](O)[C@H](Cc2ccccc2)NC(=O)OCc2cncs2)C(C)C)cs1 10.1038/s41467-023-40064-9
4106 2502 None 21 Human Binding pEC50 = 9.2 9.2 -4 33
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 2502 None 21 Human Binding pEC50 = 9.2 9.2 -4 33
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 2502 None 21 Human Binding pEC50 = 9.2 9.2 -4 33
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 2502 None 21 Human Binding pEC50 = 9.2 9.2 -4 33
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
5 139 None 45 Human Binding pEC50 = 8.3 8.3 -3 54
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 139 None 45 Human Binding pEC50 = 8.3 8.3 -3 54
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 139 None 45 Human Binding pEC50 = 8.3 8.3 -3 54
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 139 None 45 Human Binding pEC50 = 8.3 8.3 -3 54
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
5 139 None 45 Human Binding pEC50 = 8.2 8.2 -3 54
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 139 None 45 Human Binding pEC50 = 8.2 8.2 -3 54
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 139 None 45 Human Binding pEC50 = 8.2 8.2 -3 54
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 139 None 45 Human Binding pEC50 = 8.2 8.2 -3 54
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
5 139 None 45 Human Binding pIC50 = 9.6 9.6 -3 54
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 139 None 45 Human Binding pIC50 = 9.6 9.6 -3 54
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 139 None 45 Human Binding pIC50 = 9.6 9.6 -3 54
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 139 None 45 Human Binding pIC50 = 9.6 9.6 -3 54
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
5 139 None 45 Human Binding pIC50 = 9.6 9.6 -3 54
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 139 None 45 Human Binding pIC50 = 9.6 9.6 -3 54
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 139 None 45 Human Binding pIC50 = 9.6 9.6 -3 54
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 139 None 45 Human Binding pIC50 = 9.6 9.6 -3 54
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
5 139 None 45 Human Binding pIC50 = 9.5 9.5 -3 54
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 139 None 45 Human Binding pIC50 = 9.5 9.5 -3 54
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 139 None 45 Human Binding pIC50 = 9.5 9.5 -3 54
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 139 None 45 Human Binding pIC50 = 9.5 9.5 -3 54
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
72548703 161661 None 0 Human Binding pIC50 = 9.4 9.4 - 0
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
CHEMBL4128926 161661 None 0 Human Binding pIC50 = 9.4 9.4 - 0
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
5 139 None 45 Human Binding pIC50 = 9.3 9.3 -3 54
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 139 None 45 Human Binding pIC50 = 9.3 9.3 -3 54
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 139 None 45 Human Binding pIC50 = 9.3 9.3 -3 54
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 139 None 45 Human Binding pIC50 = 9.3 9.3 -3 54
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
5 139 None 45 Human Binding pIC50 = 9.3 9.3 -3 54
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 139 None 45 Human Binding pIC50 = 9.3 9.3 -3 54
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 139 None 45 Human Binding pIC50 = 9.3 9.3 -3 54
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 139 None 45 Human Binding pIC50 = 9.3 9.3 -3 54
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
5 139 None 45 Human Binding pIC50 = 9.2 9.2 -3 54
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 139 None 45 Human Binding pIC50 = 9.2 9.2 -3 54
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 139 None 45 Human Binding pIC50 = 9.2 9.2 -3 54
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 139 None 45 Human Binding pIC50 = 9.2 9.2 -3 54
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
5 139 None 45 Human Binding pIC50 = 8.8 8.8 -3 54
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 139 None 45 Human Binding pIC50 = 8.8 8.8 -3 54
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 139 None 45 Human Binding pIC50 = 8.8 8.8 -3 54
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 139 None 45 Human Binding pIC50 = 8.8 8.8 -3 54
Inhibition of human 5HT7 receptorInhibition of human 5HT7 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm701575k
11430418 18793 None 9 Human Binding pIC50 = 6 6.0 - 1
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 18793 None 9 Human Binding pIC50 = 6 6.0 - 1
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 160897 None 0 Human Binding pIC50 = 6 6.0 - 0
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 160897 None 0 Human Binding pIC50 = 6 6.0 - 0
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 160897 None 0 Human Binding pIC50 = 6 6.0 - 0
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 160897 None 0 Human Binding pIC50 = 6 6.0 - 0
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 102558 None 0 Human Binding pIC50 = 6 6.0 - 0
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 102558 None 0 Human Binding pIC50 = 6 6.0 - 0
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 102558 None 0 Human Binding pIC50 = 6 6.0 - 0
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 15671 None 0 Human Binding pIC50 = 6 6.0 - 0
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 15671 None 0 Human Binding pIC50 = 6 6.0 - 0
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
44576978 187378 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 187378 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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
72197485 102544 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 102544 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 102544 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 187804 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 187804 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 96132 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 96132 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 96199 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 96199 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 96288 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 96288 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 161331 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 161331 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 66516 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 66516 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 66516 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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
24882509 96292 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 96292 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 96132 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 96132 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 96199 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 96199 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 203379 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 203379 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 96288 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 96288 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 161331 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 161331 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 2532 None 33 Human Binding pIC50 = 6.9 6.9 -83 57
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 2532 None 33 Human Binding pIC50 = 6.9 6.9 -83 57
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 2532 None 33 Human Binding pIC50 = 6.9 6.9 -83 57
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
4184.0 2532 None 33 Human Binding pIC50 = 6.9 6.9 -83 57
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 2532 None 33 Human Binding pIC50 = 6.9 6.9 -83 57
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 2532 None 33 Human Binding pIC50 = 6.9 6.9 -83 57
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 203438 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 203438 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 10510 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 10510 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 96080 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 96080 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 96294 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 96294 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 175815 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 175815 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 96292 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 96292 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 187865 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 187865 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 203518 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 203518 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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
141 1427 None 18 Human Binding pIC50 = 6.9 6.9 1 28
Displacement of [3H] LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cells incubated for 120 mins by spectrophotometric analysisDisplacement of [3H] LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cells incubated for 120 mins by spectrophotometric analysis
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.3c00143
6089 1427 None 18 Human Binding pIC50 = 6.9 6.9 1 28
Displacement of [3H] LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cells incubated for 120 mins by spectrophotometric analysisDisplacement of [3H] LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cells incubated for 120 mins by spectrophotometric analysis
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.3c00143
CHEMBL12420 1427 None 18 Human Binding pIC50 = 6.9 6.9 1 28
Displacement of [3H] LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cells incubated for 120 mins by spectrophotometric analysisDisplacement of [3H] LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cells incubated for 120 mins by spectrophotometric analysis
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.3c00143
DB01488 1427 None 18 Human Binding pIC50 = 6.9 6.9 1 28
Displacement of [3H] LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cells incubated for 120 mins by spectrophotometric analysisDisplacement of [3H] LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cells incubated for 120 mins by spectrophotometric analysis
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.3c00143
44451927 96080 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 96080 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 96294 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 96294 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 203312 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 203312 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 201322 None 0 Human Binding pIC50 = 5.9 5.9 - 1
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 201322 None 0 Human Binding pIC50 = 5.9 5.9 - 1
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 203173 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 203173 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 187798 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 187798 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 203408 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 203408 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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
44452278 96133 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 96133 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 96295 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 96295 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 96133 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 96133 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 96295 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 96295 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 95816 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 95816 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 95816 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 95816 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 199281 None 0 Human Binding pIC50 = 5.9 5.9 - 1
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 199281 None 0 Human Binding pIC50 = 5.9 5.9 - 1
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
44452223 96044 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 96044 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 187641 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 187641 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 96044 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 96044 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 56679 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 56679 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 80192 None 12 Human Binding pIC50 = 6.8 6.8 - 0
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 80192 None 12 Human Binding pIC50 = 6.8 6.8 - 0
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 10058 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 10058 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 111079 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 111079 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 203382 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 203382 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 160028 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 160028 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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
44452276 160028 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 160028 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 1553 None 11 Human Binding pIC50 = 5.8 5.8 -13 7
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 1553 None 11 Human Binding pIC50 = 5.8 5.8 -13 7
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 1553 None 11 Human Binding pIC50 = 5.8 5.8 -13 7
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 203476 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 203476 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 203348 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 203348 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 102549 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 102549 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 102549 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 15609 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 15609 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 96240 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 96240 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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
44452115 96431 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 96431 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 156112 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 156112 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 96431 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 96431 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 156112 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 156112 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 96240 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 96240 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 203417 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 203417 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 176212 None 0 Human Binding pIC50 = 6.8 6.8 -3 2
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 176212 None 0 Human Binding pIC50 = 6.8 6.8 -3 2
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 176212 None 0 Human Binding pIC50 = 6.8 6.8 -3 2
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 176212 None 0 Human Binding pIC50 = 6.8 6.8 -3 2
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 202477 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 202477 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 203269 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 203269 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 208051 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 208051 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 89729 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 89729 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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
46232819 203611 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 203611 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 95862 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 95862 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 95862 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 95862 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 95998 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 95998 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 160469 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 160469 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 95998 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 95998 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 160469 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 160469 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 203551 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 203551 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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
44452196 96082 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 96082 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 96332 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 96332 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 155867 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 155867 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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
44452144 96353 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 96353 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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
5 139 None 45 Human Binding pIC50 = 8.6 8.6 -3 54
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 139 None 45 Human Binding pIC50 = 8.6 8.6 -3 54
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 139 None 45 Human Binding pIC50 = 8.6 8.6 -3 54
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 139 None 45 Human Binding pIC50 = 8.6 8.6 -3 54
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 3512 None 28 Human Binding pIC50 = 8.6 8.6 2 17
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 3512 None 28 Human Binding pIC50 = 8.6 8.6 2 17
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 3512 None 28 Human Binding pIC50 = 8.6 8.6 2 17
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 3512 None 28 Human Binding pIC50 = 8.6 8.6 2 17
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 3512 None 28 Human Binding pIC50 = 8.6 8.6 2 17
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 3512 None 28 Human Binding pIC50 = 8.6 8.6 2 17
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 3512 None 28 Human Binding pIC50 = 8.6 8.6 2 17
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 3512 None 28 Human Binding pIC50 = 8.6 8.6 2 17
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 3512 None 28 Human Binding pIC50 = 8.6 8.6 2 17
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 3512 None 28 Human Binding pIC50 = 8.6 8.6 2 17
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 188160 None 0 Human Binding pIC50 = 7.7 7.7 -4 6
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 188160 None 0 Human Binding pIC50 = 7.7 7.7 -4 6
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 167085 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 167085 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 96082 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 96082 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 96332 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 96332 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 155867 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 155867 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 96353 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 96353 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 56686 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 56686 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 9830 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 9830 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 15602 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 15602 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 15699 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 15699 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 96289 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 96289 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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
44452170 167085 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 167085 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 96289 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 96289 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 11032 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 11032 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 171749 None 0 Human Binding pIC50 = 6.7 6.7 -1 2
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 171749 None 0 Human Binding pIC50 = 6.7 6.7 -1 2
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 171749 None 0 Human Binding pIC50 = 6.7 6.7 -1 2
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 171749 None 0 Human Binding pIC50 = 6.7 6.7 -1 2
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 96116 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 96116 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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
44451929 96116 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 96116 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 187477 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 187477 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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
46232729 203913 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 203913 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 96263 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 96263 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 96263 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 96263 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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
44452302 96324 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 96324 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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
46232689 203416 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 203416 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 96324 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 96324 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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
44451957 158588 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 158588 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 158588 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 158588 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 154695 None 0 Human Binding pIC50 = 4.6 4.6 - 0
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 154695 None 0 Human Binding pIC50 = 4.6 4.6 - 0
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
44452143 96352 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 96352 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 96352 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 96352 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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
44451952 160467 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 160467 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 160467 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 160467 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 157593 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 157593 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 157593 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 157593 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 96250 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 96250 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 158229 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 158229 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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
46866711 15677 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 15677 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 192830 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 192830 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 96250 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 96250 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 158229 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 158229 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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
4106 2502 None 21 Human Binding pIC50 = 8.5 8.5 -4 33
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 2502 None 21 Human Binding pIC50 = 8.5 8.5 -4 33
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 2502 None 21 Human Binding pIC50 = 8.5 8.5 -4 33
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 2502 None 21 Human Binding pIC50 = 8.5 8.5 -4 33
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
4223 3992 None 57 Rat Binding pIC50 = 5.5 5.5 - 17
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 3992 None 57 Rat Binding pIC50 = 5.5 5.5 - 17
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
6918314.0 3992 None 57 Rat Binding pIC50 = 5.5 5.5 - 17
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 3992 None 57 Rat Binding pIC50 = 5.5 5.5 - 17
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 3992 None 57 Rat Binding pIC50 = 5.5 5.5 - 17
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 3992 None 57 Rat Binding pIC50 = 5.5 5.5 - 17
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 1552 None 18 Human Binding pIC50 = 5.5 5.5 - 0
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 1552 None 18 Human Binding pIC50 = 5.5 5.5 - 0
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 1552 None 18 Human Binding pIC50 = 5.5 5.5 - 0
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 15599 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 15599 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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
73347306 89728 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 89728 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 203314 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 203314 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 203653 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 203653 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 187640 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 187640 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 7452 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 7452 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 203349 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 203349 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 187539 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 187539 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 203309 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 203309 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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
44452357 95959 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 95959 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 96406 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 96406 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 203554 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 203554 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 95959 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 95959 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 96406 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 96406 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 203576 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 203576 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 95817 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 95817 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 166464 None 0 Human Binding pIC50 = 7.4 7.4 2 3
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 166464 None 0 Human Binding pIC50 = 7.4 7.4 2 3
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 95817 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 95817 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 89736 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 89736 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 187866 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 187866 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 187903 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 187903 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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
42635028 193324 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 193324 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 15698 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 15698 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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
44452329 158830 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 158830 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 158830 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 158830 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 7454 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 7454 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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
46232654 203477 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 203477 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 96126 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 96126 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 96229 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 96229 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 95999 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 95999 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 96126 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 96126 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 96229 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 96229 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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
44452171 168800 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 168800 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 203418 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 203418 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 10053 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 10053 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 15697 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 15697 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 96134 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 96134 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 158642 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 158642 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 168800 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 168800 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 96134 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 96134 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 158642 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 158642 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 203474 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 203474 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 7436 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 7436 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 96002 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 96002 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 96002 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 96002 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 96405 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 96405 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 187542 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 187542 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 95906 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 95906 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 96405 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 96405 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 187668 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 187668 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 184014 None 30 Human Binding pIC50 = 4.3 4.3 - 0
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 184014 None 30 Human Binding pIC50 = 4.3 4.3 - 0
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 4076 None 15 Human Binding pIC50 = 5.3 5.3 - 1
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 4076 None 15 Human Binding pIC50 = 5.3 5.3 - 1
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 4076 None 15 Human Binding pIC50 = 5.3 5.3 - 1
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 95906 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 95906 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 95951 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 95951 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 89727 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 89727 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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
44452007 95951 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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-c2ccc(OC)cc2)CC1 10.1016/j.bmc.2007.11.049
CHEMBL259199 95951 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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-c2ccc(OC)cc2)CC1 10.1016/j.bmc.2007.11.049
46232858 203239 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 4.6 O=S(=O)(c1ccc2ccccc2c1)N(CCCN1CCN(c2ccc(F)cc2)CC1)CC1CC1 10.1016/j.bmc.2009.12.067
CHEMBL600606 203239 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 4.6 O=S(=O)(c1ccc2ccccc2c1)N(CCCN1CCN(c2ccc(F)cc2)CC1)CC1CC1 10.1016/j.bmc.2009.12.067
45278883 7651 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibition of 5HT7 receptorInhibition of 5HT7 receptor
ChEMBL 553 8 1 5 5.8 Cc1c(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(-c2ccccc2)n1N1CCCCC1 10.1016/j.bmcl.2010.01.093
CHEMBL1088313 7651 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibition of 5HT7 receptorInhibition of 5HT7 receptor
ChEMBL 553 8 1 5 5.8 Cc1c(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(-c2ccccc2)n1N1CCCCC1 10.1016/j.bmcl.2010.01.093
72197668 102550 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 360 5 2 5 3.5 COc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
CHEMBL2393246 102550 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 360 5 2 5 3.5 COc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
CHEMBL3040325 102550 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 360 5 2 5 3.5 COc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
44451959 96333 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 513 7 1 6 4.0 Cc1cccc(C)c1N1CCN(CCC(=O)NCc2nc3ccccc3c(=O)n2-c2ccc(F)cc2)CC1 10.1016/j.bmc.2007.11.049
CHEMBL261151 96333 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 513 7 1 6 4.0 Cc1cccc(C)c1N1CCN(CCC(=O)NCc2nc3ccccc3c(=O)n2-c2ccc(F)cc2)CC1 10.1016/j.bmc.2007.11.049
44451984 96417 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 513 7 1 6 4.0 Cc1ccc(N2CCN(CCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccc(F)cc3)CC2)c(C)c1 10.1016/j.bmc.2007.11.049
CHEMBL261653 96417 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 513 7 1 6 4.0 Cc1ccc(N2CCN(CCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccc(F)cc3)CC2)c(C)c1 10.1016/j.bmc.2007.11.049
46232623 203195 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 535 10 0 5 5.6 COc1ccccc1N1CCN(CCCN(CC2CCCCC2)S(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmc.2009.12.067
CHEMBL600210 203195 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 535 10 0 5 5.6 COc1ccccc1N1CCN(CCCN(CC2CCCCC2)S(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmc.2009.12.067
46232770 203298 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 458 10 0 6 3.2 O=[N+]([O-])c1ccc(S(=O)(=O)N(CCCN2CCN(c3ccccc3)CC2)CC2CC2)cc1 10.1016/j.bmc.2009.12.067
CHEMBL601037 203298 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 458 10 0 6 3.2 O=[N+]([O-])c1ccc(S(=O)(=O)N(CCCN2CCN(c3ccccc3)CC2)CC2CC2)cc1 10.1016/j.bmc.2009.12.067
44451959 96333 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 513 7 1 6 4.0 Cc1cccc(C)c1N1CCN(CCC(=O)NCc2nc3ccccc3c(=O)n2-c2ccc(F)cc2)CC1 10.1016/j.ejmech.2008.09.050
CHEMBL261151 96333 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 513 7 1 6 4.0 Cc1cccc(C)c1N1CCN(CCC(=O)NCc2nc3ccccc3c(=O)n2-c2ccc(F)cc2)CC1 10.1016/j.ejmech.2008.09.050
44451984 96417 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 513 7 1 6 4.0 Cc1ccc(N2CCN(CCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccc(F)cc3)CC2)c(C)c1 10.1016/j.ejmech.2008.09.050
CHEMBL261653 96417 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 513 7 1 6 4.0 Cc1ccc(N2CCN(CCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccc(F)cc3)CC2)c(C)c1 10.1016/j.ejmech.2008.09.050
44451986 159458 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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(c2ccccc2Cl)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
CHEMBL410042 159458 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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(c2ccccc2Cl)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
44451986 159458 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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(c2ccccc2Cl)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
CHEMBL410042 159458 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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(c2ccccc2Cl)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
10407367 199249 None 0 Human Binding pIC50 = 6.3 6.3 - 1
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 379 5 0 5 3.6 CN(C)CCn1cc(S(=O)(=O)c2cccc3ccccc23)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565552 199249 None 0 Human Binding pIC50 = 6.3 6.3 - 1
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 379 5 0 5 3.6 CN(C)CCn1cc(S(=O)(=O)c2cccc3ccccc23)c2cccnc21 10.1016/j.bmc.2009.05.055
44452008 95999 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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)NCc1nc2cc(F)ccc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
CHEMBL259408 95999 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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)NCc1nc2cc(F)ccc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
45278886 7652 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibition of 5HT7 receptorInhibition of 5HT7 receptor
ChEMBL 564 8 1 4 6.8 Cc1c(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(-c2ccccc2)n1-c1ccc(F)cc1 10.1016/j.bmcl.2010.01.093
CHEMBL1088314 7652 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibition of 5HT7 receptorInhibition of 5HT7 receptor
ChEMBL 564 8 1 4 6.8 Cc1c(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(-c2ccccc2)n1-c1ccc(F)cc1 10.1016/j.bmcl.2010.01.093
46233014 203475 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 441 7 1 4 3.9 CC(CCN1CCN(c2ccc(F)cc2)CC1)NS(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmc.2009.12.067
CHEMBL602279 203475 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 441 7 1 4 3.9 CC(CCN1CCN(c2ccc(F)cc2)CC1)NS(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmc.2009.12.067
42389457 187839 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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(c2ccc(F)cc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmc.2008.04.023
CHEMBL495445 187839 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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(c2ccc(F)cc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmc.2008.04.023
44452193 96123 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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-c2cccc(OC)c2)CC1 10.1016/j.ejmech.2008.09.050
CHEMBL260022 96123 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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-c2cccc(OC)c2)CC1 10.1016/j.ejmech.2008.09.050
44451982 96378 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 527 8 1 6 4.4 Cc1cccc(N2CCN(CCCC(=O)NCc3nc4ccc(F)cc4c(=O)n3-c3ccccc3)CC2)c1C 10.1016/j.ejmech.2008.09.050
CHEMBL261434 96378 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 527 8 1 6 4.4 Cc1cccc(N2CCN(CCCC(=O)NCc3nc4ccc(F)cc4c(=O)n3-c3ccccc3)CC2)c1C 10.1016/j.ejmech.2008.09.050
16 2253 None 10 Rat Binding pIC50 = 6.3 6.3 - 1
Compound was tested for the displacement of [3H]5-HT binding to cloned rat 5-hydroxytryptamine 7 receptor stably expressed in CHO cellsCompound was tested for the displacement of [3H]5-HT binding to cloned rat 5-hydroxytryptamine 7 receptor stably expressed in CHO cells
ChEMBL 462 9 3 6 3.6 OC[C@@H](c1ccc(cc1)F)NC1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10.1021/jm9910021
9847194 2253 None 10 Rat Binding pIC50 = 6.3 6.3 - 1
Compound was tested for the displacement of [3H]5-HT binding to cloned rat 5-hydroxytryptamine 7 receptor stably expressed in CHO cellsCompound was tested for the displacement of [3H]5-HT binding to cloned rat 5-hydroxytryptamine 7 receptor stably expressed in CHO cells
ChEMBL 462 9 3 6 3.6 OC[C@@H](c1ccc(cc1)F)NC1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10.1021/jm9910021
CHEMBL313714 2253 None 10 Rat Binding pIC50 = 6.3 6.3 - 1
Compound was tested for the displacement of [3H]5-HT binding to cloned rat 5-hydroxytryptamine 7 receptor stably expressed in CHO cellsCompound was tested for the displacement of [3H]5-HT binding to cloned rat 5-hydroxytryptamine 7 receptor stably expressed in CHO cells
ChEMBL 462 9 3 6 3.6 OC[C@@H](c1ccc(cc1)F)NC1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10.1021/jm9910021
44452193 96123 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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-c2cccc(OC)c2)CC1 10.1016/j.bmc.2007.11.049
CHEMBL260022 96123 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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-c2cccc(OC)c2)CC1 10.1016/j.bmc.2007.11.049
44451982 96378 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 527 8 1 6 4.4 Cc1cccc(N2CCN(CCCC(=O)NCc3nc4ccc(F)cc4c(=O)n3-c3ccccc3)CC2)c1C 10.1016/j.bmc.2007.11.049
CHEMBL261434 96378 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 527 8 1 6 4.4 Cc1cccc(N2CCN(CCCC(=O)NCc3nc4ccc(F)cc4c(=O)n3-c3ccccc3)CC2)c1C 10.1016/j.bmc.2007.11.049
46700867 176094 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [3H]LSD from human 5-HT7 receptor expressed in CHO-K1 cell membranes after 60 minsDisplacement of [3H]LSD from human 5-HT7 receptor expressed in CHO-K1 cell membranes after 60 mins
ChEMBL 377 14 1 4 5.0 CCCCCCCCCCNC(=O)/C=C/c1cc(OC)c(OC)c(OC)c1 10.1016/j.ejmech.2019.04.009
CHEMBL4588956 176094 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [3H]LSD from human 5-HT7 receptor expressed in CHO-K1 cell membranes after 60 minsDisplacement of [3H]LSD from human 5-HT7 receptor expressed in CHO-K1 cell membranes after 60 mins
ChEMBL 377 14 1 4 5.0 CCCCCCCCCCNC(=O)/C=C/c1cc(OC)c(OC)c(OC)c1 10.1016/j.ejmech.2019.04.009
42635205 187901 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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(c2ccc(C(F)(F)F)cc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmc.2008.04.023
CHEMBL495884 187901 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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(c2ccc(C(F)(F)F)cc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmc.2008.04.023
46232588 203414 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 485 10 0 5 4.5 COc1ccc(S(=O)(=O)N(CCCN2CCN(c3ccccc3)CC2)CC2CCCCC2)cc1 10.1016/j.bmc.2009.12.067
CHEMBL601872 203414 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 485 10 0 5 4.5 COc1ccc(S(=O)(=O)N(CCCN2CCN(c3ccccc3)CC2)CC2CCCCC2)cc1 10.1016/j.bmc.2009.12.067
42635389 187475 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 433 9 1 6 2.6 COc1ccc(S(=O)(=O)NC(C)CCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2008.04.023
CHEMBL493402 187475 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 433 9 1 6 2.6 COc1ccc(S(=O)(=O)NC(C)CCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2008.04.023
44452275 96290 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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)NCc3nc4cc(F)ccc4c(=O)n3-c3ccccc3)CC2)cc1C 10.1016/j.bmc.2007.11.049
CHEMBL260903 96290 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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)NCc3nc4cc(F)ccc4c(=O)n3-c3ccccc3)CC2)cc1C 10.1016/j.bmc.2007.11.049
44452298 96365 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 541 9 1 7 3.9 CC(=O)c1ccc(N2CCN(CCCC(=O)NCc3nc4ccc(F)cc4c(=O)n3-c3ccccc3)CC2)cc1 10.1016/j.bmc.2007.11.049
CHEMBL261337 96365 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 541 9 1 7 3.9 CC(=O)c1ccc(N2CCN(CCCC(=O)NCc3nc4ccc(F)cc4c(=O)n3-c3ccccc3)CC2)cc1 10.1016/j.bmc.2007.11.049
44452275 96290 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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)NCc3nc4cc(F)ccc4c(=O)n3-c3ccccc3)CC2)cc1C 10.1016/j.ejmech.2008.09.050
CHEMBL260903 96290 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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)NCc3nc4cc(F)ccc4c(=O)n3-c3ccccc3)CC2)cc1C 10.1016/j.ejmech.2008.09.050
44452298 96365 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 541 9 1 7 3.9 CC(=O)c1ccc(N2CCN(CCCC(=O)NCc3nc4ccc(F)cc4c(=O)n3-c3ccccc3)CC2)cc1 10.1016/j.ejmech.2008.09.050
CHEMBL261337 96365 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 541 9 1 7 3.9 CC(=O)c1ccc(N2CCN(CCCC(=O)NCc3nc4ccc(F)cc4c(=O)n3-c3ccccc3)CC2)cc1 10.1016/j.ejmech.2008.09.050
46232861 203550 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 532 9 0 5 4.9 O=S(=O)(c1cccc2cccnc12)N(CCCN1CCN(c2cccc(C(F)(F)F)c2)CC1)CC1CC1 10.1016/j.bmc.2009.12.067
CHEMBL602878 203550 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 532 9 0 5 4.9 O=S(=O)(c1cccc2cccnc12)N(CCCN1CCN(c2cccc(C(F)(F)F)c2)CC1)CC1CC1 10.1016/j.bmc.2009.12.067
54577891 66596 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Inhibition of 5HT7 receptor by competition binding assayInhibition of 5HT7 receptor by competition binding assay
ChEMBL 471 6 1 5 4.3 Cc1nc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)c(C)n1-c1ccccc1 10.1021/jm200682b
CHEMBL1852516 66596 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Inhibition of 5HT7 receptor by competition binding assayInhibition of 5HT7 receptor by competition binding assay
ChEMBL 471 6 1 5 4.3 Cc1nc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)c(C)n1-c1ccccc1 10.1021/jm200682b
CHEMBL3216758 66596 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Inhibition of 5HT7 receptor by competition binding assayInhibition of 5HT7 receptor by competition binding assay
ChEMBL 471 6 1 5 4.3 Cc1nc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)c(C)n1-c1ccccc1 10.1021/jm200682b
44451979 96377 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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)c(C)c1 10.1016/j.ejmech.2008.09.050
CHEMBL261433 96377 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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)c(C)c1 10.1016/j.ejmech.2008.09.050
72198754 90914 None 0 Human Binding pIC50 = 7.2 7.2 - 1
Inhibition of human 5-HT7 receptorInhibition of human 5-HT7 receptor
ChEMBL 443 8 0 4 4.8 COc1ccccc1N1CCN(CCCCCN2Cc3ccc4ccccc4c3C2=O)CC1 10.1016/j.ejmech.2013.01.044
CHEMBL2392349 90914 None 0 Human Binding pIC50 = 7.2 7.2 - 1
Inhibition of human 5-HT7 receptorInhibition of human 5-HT7 receptor
ChEMBL 443 8 0 4 4.8 COc1ccccc1N1CCN(CCCCCN2Cc3ccc4ccccc4c3C2=O)CC1 10.1016/j.ejmech.2013.01.044
53320010 56680 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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(c2cccc3c2C(=O)CCN3S(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2010.12.007
CHEMBL1642117 56680 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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(c2cccc3c2C(=O)CCN3S(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2010.12.007
44451979 96377 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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)c(C)c1 10.1016/j.bmc.2007.11.049
CHEMBL261433 96377 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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)c(C)c1 10.1016/j.bmc.2007.11.049
185617 186660 None 53 Human Binding pIC50 = 4.2 4.2 - 0
Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells
ChEMBL 462 4 7 11 -0.2 O=C(O)[C@H]1O[C@@H](Oc2cc3oc(-c4ccc(O)cc4)cc(=O)c3c(O)c2O)[C@H](O)[C@@H](O)[C@@H]1O 10.1021/np0205102
CHEMBL487805 186660 None 53 Human Binding pIC50 = 4.2 4.2 - 0
Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells
ChEMBL 462 4 7 11 -0.2 O=C(O)[C@H]1O[C@@H](Oc2cc3oc(-c4ccc(O)cc4)cc(=O)c3c(O)c2O)[C@H](O)[C@@H](O)[C@@H]1O 10.1021/np0205102
44452279 161382 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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)c(C)c1 10.1016/j.ejmech.2008.09.050
CHEMBL412153 161382 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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)c(C)c1 10.1016/j.ejmech.2008.09.050
44452279 161382 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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)c(C)c1 10.1016/j.bmc.2007.11.049
CHEMBL412153 161382 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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)c(C)c1 10.1016/j.bmc.2007.11.049
44452331 96160 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 481 8 1 6 3.6 O=C(CCCN1CCN(c2ccccc2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
CHEMBL260249 96160 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 481 8 1 6 3.6 O=C(CCCN1CCN(c2ccccc2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
44452331 96160 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 481 8 1 6 3.6 O=C(CCCN1CCN(c2ccccc2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
CHEMBL260249 96160 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 481 8 1 6 3.6 O=C(CCCN1CCN(c2ccccc2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
46232976 203575 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 423 7 1 4 3.7 CC(CCN1CCN(c2ccccc2)CC1)NS(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmc.2009.12.067
CHEMBL603092 203575 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 423 7 1 4 3.7 CC(CCN1CCN(c2ccccc2)CC1)NS(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmc.2009.12.067
10949380 164118 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of human 5-hydroxytryptamine 7 receptorInhibition of human 5-hydroxytryptamine 7 receptor
ChEMBL 399 3 1 6 4.3 Cc1ccc2nc(O)n(C3CCN(Cc4cc5c(cc4Cl)OCO5)CC3)c2c1 10.1021/jm010878g
CHEMBL420863 164118 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of human 5-hydroxytryptamine 7 receptorInhibition of human 5-hydroxytryptamine 7 receptor
ChEMBL 399 3 1 6 4.3 Cc1ccc2nc(O)n(C3CCN(Cc4cc5c(cc4Cl)OCO5)CC3)c2c1 10.1021/jm010878g
46232620 203293 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 553 10 0 5 5.5 COc1ccc(S(=O)(=O)N(CCCN2CCN(c3cccc(C(F)(F)F)c3)CC2)CC2CCCCC2)cc1 10.1016/j.bmc.2009.12.067
CHEMBL601022 203293 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 553 10 0 5 5.5 COc1ccc(S(=O)(=O)N(CCCN2CCN(c3cccc(C(F)(F)F)c3)CC2)CC2CCCCC2)cc1 10.1016/j.bmc.2009.12.067
44452010 96043 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 485 7 1 6 3.4 O=C(CCN1CCN(c2ccccc2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccc(F)cc1 10.1016/j.bmc.2007.11.049
CHEMBL259619 96043 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 485 7 1 6 3.4 O=C(CCN1CCN(c2ccccc2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccc(F)cc1 10.1016/j.bmc.2007.11.049
44452141 96305 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 541 9 1 7 3.9 CC(=O)c1ccc(N2CCN(CCCC(=O)NCc3nc4cc(F)ccc4c(=O)n3-c3ccccc3)CC2)cc1 10.1016/j.bmc.2007.11.049
CHEMBL261018 96305 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 541 9 1 7 3.9 CC(=O)c1ccc(N2CCN(CCCC(=O)NCc3nc4cc(F)ccc4c(=O)n3-c3ccccc3)CC2)cc1 10.1016/j.bmc.2007.11.049
44452010 96043 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 485 7 1 6 3.4 O=C(CCN1CCN(c2ccccc2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccc(F)cc1 10.1016/j.ejmech.2008.09.050
CHEMBL259619 96043 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 485 7 1 6 3.4 O=C(CCN1CCN(c2ccccc2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccc(F)cc1 10.1016/j.ejmech.2008.09.050
44452141 96305 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 541 9 1 7 3.9 CC(=O)c1ccc(N2CCN(CCCC(=O)NCc3nc4cc(F)ccc4c(=O)n3-c3ccccc3)CC2)cc1 10.1016/j.ejmech.2008.09.050
CHEMBL261018 96305 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 541 9 1 7 3.9 CC(=O)c1ccc(N2CCN(CCCC(=O)NCc3nc4cc(F)ccc4c(=O)n3-c3ccccc3)CC2)cc1 10.1016/j.ejmech.2008.09.050
42389129 193220 None 1 Human Binding pIC50 = 6.2 6.2 - 0
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 409 7 1 4 3.3 O=S(=O)(NCCCN1CCN(c2ccccc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmc.2008.04.023
CHEMBL522694 193220 None 1 Human Binding pIC50 = 6.2 6.2 - 0
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 409 7 1 4 3.3 O=S(=O)(NCCCN1CCN(c2ccccc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmc.2008.04.023
73356443 89735 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]LSD from human 5HT7 receptorDisplacement of [3H]LSD from human 5HT7 receptor
ChEMBL 294 2 2 2 4.6 Cc1[nH]c2ccc(-c3ccsc3)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376490 89735 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]LSD from human 5HT7 receptorDisplacement of [3H]LSD from human 5HT7 receptor
ChEMBL 294 2 2 2 4.6 Cc1[nH]c2ccc(-c3ccsc3)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
44452221 96001 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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)c(C)c1 10.1016/j.bmc.2007.11.049
CHEMBL259414 96001 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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)c(C)c1 10.1016/j.bmc.2007.11.049
44452221 96001 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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)c(C)c1 10.1016/j.ejmech.2008.09.050
CHEMBL259414 96001 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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)c(C)c1 10.1016/j.ejmech.2008.09.050
44452199 96124 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 497 8 1 7 3.2 COc1ccc(N2CCN(CCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)cc1 10.1016/j.ejmech.2008.09.050
CHEMBL260023 96124 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 497 8 1 7 3.2 COc1ccc(N2CCN(CCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)cc1 10.1016/j.ejmech.2008.09.050
44452199 96124 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 497 8 1 7 3.2 COc1ccc(N2CCN(CCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)cc1 10.1016/j.bmc.2007.11.049
CHEMBL260023 96124 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 497 8 1 7 3.2 COc1ccc(N2CCN(CCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)cc1 10.1016/j.bmc.2007.11.049
11071079 110656 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibition of human 5-hydroxytryptamine 7 receptorInhibition of human 5-hydroxytryptamine 7 receptor
ChEMBL 496 9 0 3 6.0 O=C(OCCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
CHEMBL325516 110656 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibition of human 5-hydroxytryptamine 7 receptorInhibition of human 5-hydroxytryptamine 7 receptor
ChEMBL 496 9 0 3 6.0 O=C(OCCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
44452332 96161 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 481 7 1 6 3.5 Cc1ccc(N2CCN(CCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)cc1 10.1016/j.ejmech.2008.09.050
CHEMBL260250 96161 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 481 7 1 6 3.5 Cc1ccc(N2CCN(CCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)cc1 10.1016/j.ejmech.2008.09.050
44452362 96562 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 530 8 1 8 3.3 O=C(CCN1CCN(c2ccc([N+](=O)[O-])cc2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccc(F)cc1 10.1016/j.ejmech.2008.09.050
CHEMBL262589 96562 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 530 8 1 8 3.3 O=C(CCN1CCN(c2ccc([N+](=O)[O-])cc2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccc(F)cc1 10.1016/j.ejmech.2008.09.050
44452324 96291 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 567 8 1 6 4.8 O=C(CCCN1CCN(c2cccc(C(F)(F)F)c2)CC1)NCc1nc2ccc(F)cc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
CHEMBL260906 96291 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 567 8 1 6 4.8 O=C(CCCN1CCN(c2cccc(C(F)(F)F)c2)CC1)NCc1nc2ccc(F)cc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
44452332 96161 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 481 7 1 6 3.5 Cc1ccc(N2CCN(CCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)cc1 10.1016/j.bmc.2007.11.049
CHEMBL260250 96161 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 481 7 1 6 3.5 Cc1ccc(N2CCN(CCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)cc1 10.1016/j.bmc.2007.11.049
44452362 96562 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 530 8 1 8 3.3 O=C(CCN1CCN(c2ccc([N+](=O)[O-])cc2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccc(F)cc1 10.1016/j.bmc.2007.11.049
CHEMBL262589 96562 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 530 8 1 8 3.3 O=C(CCN1CCN(c2ccc([N+](=O)[O-])cc2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccc(F)cc1 10.1016/j.bmc.2007.11.049
44452324 96291 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 567 8 1 6 4.8 O=C(CCCN1CCN(c2cccc(C(F)(F)F)c2)CC1)NCc1nc2ccc(F)cc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
CHEMBL260906 96291 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 567 8 1 6 4.8 O=C(CCCN1CCN(c2cccc(C(F)(F)F)c2)CC1)NCc1nc2ccc(F)cc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
44452327 96325 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 527 8 1 6 4.4 Cc1cccc(N2CCN(CCCC(=O)NCc3nc4cc(F)ccc4c(=O)n3-c3ccccc3)CC2)c1C 10.1016/j.ejmech.2008.09.050
CHEMBL261102 96325 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 527 8 1 6 4.4 Cc1cccc(N2CCN(CCCC(=O)NCc3nc4cc(F)ccc4c(=O)n3-c3ccccc3)CC2)c1C 10.1016/j.ejmech.2008.09.050
46232859 203240 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 464 9 0 5 3.8 O=S(=O)(c1cccc2cccnc12)N(CCCN1CCN(c2ccccc2)CC1)CC1CC1 10.1016/j.bmc.2009.12.067
CHEMBL600607 203240 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 464 9 0 5 3.8 O=S(=O)(c1cccc2cccnc12)N(CCCN1CCN(c2ccccc2)CC1)CC1CC1 10.1016/j.bmc.2009.12.067
44452327 96325 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 527 8 1 6 4.4 Cc1cccc(N2CCN(CCCC(=O)NCc3nc4cc(F)ccc4c(=O)n3-c3ccccc3)CC2)c1C 10.1016/j.bmc.2007.11.049
CHEMBL261102 96325 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 527 8 1 6 4.4 Cc1cccc(N2CCN(CCCC(=O)NCc3nc4cc(F)ccc4c(=O)n3-c3ccccc3)CC2)c1C 10.1016/j.bmc.2007.11.049
10937901 9912 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibition of human 5-hydroxytryptamine 7 receptorInhibition of human 5-hydroxytryptamine 7 receptor
ChEMBL 385 3 1 6 4.0 Oc1nc2ccccc2n1C1CCN(Cc2cc3c(cc2Cl)OCO3)CC1 10.1021/jm010878g
CHEMBL114379 9912 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibition of human 5-hydroxytryptamine 7 receptorInhibition of human 5-hydroxytryptamine 7 receptor
ChEMBL 385 3 1 6 4.0 Oc1nc2ccccc2n1C1CCN(Cc2cc3c(cc2Cl)OCO3)CC1 10.1021/jm010878g
44452040 96296 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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)NCc1nc2cc(F)ccc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
CHEMBL260971 96296 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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)NCc1nc2cc(F)ccc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
44452041 96340 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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)NCc1nc2cc(F)ccc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
CHEMBL261187 96340 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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)NCc1nc2cc(F)ccc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
44452040 96296 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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)NCc1nc2cc(F)ccc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
CHEMBL260971 96296 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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)NCc1nc2cc(F)ccc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
44452041 96340 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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)NCc1nc2cc(F)ccc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
CHEMBL261187 96340 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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)NCc1nc2cc(F)ccc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
44452243 158640 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 559 10 1 8 3.8 COc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccc(F)cc3c(=O)n2-c2ccccc2OC)CC1 10.1016/j.bmc.2007.11.049
CHEMBL409156 158640 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 559 10 1 8 3.8 COc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccc(F)cc3c(=O)n2-c2ccccc2OC)CC1 10.1016/j.bmc.2007.11.049
44452243 158640 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 559 10 1 8 3.8 COc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccc(F)cc3c(=O)n2-c2ccccc2OC)CC1 10.1016/j.ejmech.2008.09.050
CHEMBL409156 158640 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 559 10 1 8 3.8 COc1ccccc1N1CCN(CCCC(=O)NCc2nc3ccc(F)cc3c(=O)n2-c2ccccc2OC)CC1 10.1016/j.ejmech.2008.09.050
44452224 96045 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 497 8 1 7 3.2 COc1ccccc1N1CCN(CCC(=O)NCc2nc3ccccc3c(=O)n2-c2ccccc2)CC1 10.1016/j.ejmech.2008.09.050
CHEMBL259626 96045 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 497 8 1 7 3.2 COc1ccccc1N1CCN(CCC(=O)NCc2nc3ccccc3c(=O)n2-c2ccccc2)CC1 10.1016/j.ejmech.2008.09.050
44452224 96045 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 497 8 1 7 3.2 COc1ccccc1N1CCN(CCC(=O)NCc2nc3ccccc3c(=O)n2-c2ccccc2)CC1 10.1016/j.bmc.2007.11.049
CHEMBL259626 96045 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 497 8 1 7 3.2 COc1ccccc1N1CCN(CCC(=O)NCc2nc3ccccc3c(=O)n2-c2ccccc2)CC1 10.1016/j.bmc.2007.11.049
44452246 96239 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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)NCc2nc3cc(F)ccc3c(=O)n2-c2ccccc2)CC1 10.1016/j.ejmech.2008.09.050
CHEMBL260705 96239 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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)NCc2nc3cc(F)ccc3c(=O)n2-c2ccccc2)CC1 10.1016/j.ejmech.2008.09.050
44342270 9932 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibition of human 5-hydroxytryptamine 7 receptorInhibition of human 5-hydroxytryptamine 7 receptor
ChEMBL 355 3 1 4 4.5 Cc1ccc(CN2CCC(n3c(O)nc4ccccc43)CC2)c(Cl)c1 10.1021/jm010878g
CHEMBL114484 9932 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibition of human 5-hydroxytryptamine 7 receptorInhibition of human 5-hydroxytryptamine 7 receptor
ChEMBL 355 3 1 4 4.5 Cc1ccc(CN2CCC(n3c(O)nc4ccccc43)CC2)c(Cl)c1 10.1021/jm010878g
44452246 96239 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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)NCc2nc3cc(F)ccc3c(=O)n2-c2ccccc2)CC1 10.1016/j.bmc.2007.11.049
CHEMBL260705 96239 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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)NCc2nc3cc(F)ccc3c(=O)n2-c2ccccc2)CC1 10.1016/j.bmc.2007.11.049
46232587 204041 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 500 10 0 6 4.4 O=[N+]([O-])c1ccc(S(=O)(=O)N(CCCN2CCN(c3ccccc3)CC2)CC2CCCCC2)cc1 10.1016/j.bmc.2009.12.067
CHEMBL605582 204041 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 500 10 0 6 4.4 O=[N+]([O-])c1ccc(S(=O)(=O)N(CCCN2CCN(c3ccccc3)CC2)CC2CCCCC2)cc1 10.1016/j.bmc.2009.12.067
46232652 203447 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 573 9 0 4 6.6 O=S(=O)(c1ccc2ccccc2c1)N(CCCN1CCN(c2cccc(C(F)(F)F)c2)CC1)CC1CCCCC1 10.1016/j.bmc.2009.12.067
CHEMBL602087 203447 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 573 9 0 4 6.6 O=S(=O)(c1ccc2ccccc2c1)N(CCCN1CCN(c2cccc(C(F)(F)F)c2)CC1)CC1CCCCC1 10.1016/j.bmc.2009.12.067
42635027 187503 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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(c3cccc(C(F)(F)F)c3)CC2)cc1 10.1016/j.bmc.2008.04.023
CHEMBL493625 187503 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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(c3cccc(C(F)(F)F)c3)CC2)cc1 10.1016/j.bmc.2008.04.023
44452042 160258 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 509 8 1 7 3.4 CC(=O)c1ccc(N2CCN(CCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)cc1 10.1016/j.ejmech.2008.09.050
CHEMBL410922 160258 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 509 8 1 7 3.4 CC(=O)c1ccc(N2CCN(CCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)cc1 10.1016/j.ejmech.2008.09.050
141 1427 None 18 Human Binding pIC50 = 7.1 7.1 1 28
Displacement of [3H] LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cells incubated for 120 mins by spectrophotometric analysisDisplacement of [3H] LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cells incubated for 120 mins by spectrophotometric analysis
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.3c00143
6089 1427 None 18 Human Binding pIC50 = 7.1 7.1 1 28
Displacement of [3H] LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cells incubated for 120 mins by spectrophotometric analysisDisplacement of [3H] LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cells incubated for 120 mins by spectrophotometric analysis
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.3c00143
CHEMBL12420 1427 None 18 Human Binding pIC50 = 7.1 7.1 1 28
Displacement of [3H] LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cells incubated for 120 mins by spectrophotometric analysisDisplacement of [3H] LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cells incubated for 120 mins by spectrophotometric analysis
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.3c00143
DB01488 1427 None 18 Human Binding pIC50 = 7.1 7.1 1 28
Displacement of [3H] LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cells incubated for 120 mins by spectrophotometric analysisDisplacement of [3H] LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cells incubated for 120 mins by spectrophotometric analysis
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.3c00143
44452167 95903 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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-c2cccc(OC)c2)CC1 10.1016/j.ejmech.2008.09.050
CHEMBL258995 95903 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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-c2cccc(OC)c2)CC1 10.1016/j.ejmech.2008.09.050
44452042 160258 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 509 8 1 7 3.4 CC(=O)c1ccc(N2CCN(CCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)cc1 10.1016/j.bmc.2007.11.049
CHEMBL410922 160258 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 509 8 1 7 3.4 CC(=O)c1ccc(N2CCN(CCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)cc1 10.1016/j.bmc.2007.11.049
44452167 95903 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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-c2cccc(OC)c2)CC1 10.1016/j.bmc.2007.11.049
CHEMBL258995 95903 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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-c2cccc(OC)c2)CC1 10.1016/j.bmc.2007.11.049
44452142 96306 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 567 8 1 6 4.8 O=C(CCCN1CCN(c2cccc(C(F)(F)F)c2)CC1)NCc1nc2cc(F)ccc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
CHEMBL261019 96306 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 567 8 1 6 4.8 O=C(CCCN1CCN(c2cccc(C(F)(F)F)c2)CC1)NCc1nc2cc(F)ccc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
44452142 96306 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 567 8 1 6 4.8 O=C(CCCN1CCN(c2cccc(C(F)(F)F)c2)CC1)NCc1nc2cc(F)ccc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
CHEMBL261019 96306 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 567 8 1 6 4.8 O=C(CCCN1CCN(c2cccc(C(F)(F)F)c2)CC1)NCc1nc2cc(F)ccc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
44452359 159460 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 529 9 1 7 3.8 COc1cccc(N2CCN(CCCC(=O)NCc3nc4ccc(F)cc4c(=O)n3-c3ccccc3)CC2)c1 10.1016/j.bmc.2007.11.049
CHEMBL410043 159460 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 529 9 1 7 3.8 COc1cccc(N2CCN(CCCC(=O)NCc3nc4ccc(F)cc4c(=O)n3-c3ccccc3)CC2)c1 10.1016/j.bmc.2007.11.049
44452359 159460 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 529 9 1 7 3.8 COc1cccc(N2CCN(CCCC(=O)NCc3nc4ccc(F)cc4c(=O)n3-c3ccccc3)CC2)c1 10.1016/j.ejmech.2008.09.050
CHEMBL410043 159460 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 529 9 1 7 3.8 COc1cccc(N2CCN(CCCC(=O)NCc3nc4ccc(F)cc4c(=O)n3-c3ccccc3)CC2)c1 10.1016/j.ejmech.2008.09.050
44452082 159494 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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)NCc1nc2cc(F)ccc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
CHEMBL410075 159494 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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)NCc1nc2cc(F)ccc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
46232817 203412 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 461 10 0 5 3.4 COc1ccc(S(=O)(=O)N(CCCN2CCN(c3ccc(F)cc3)CC2)CC2CC2)cc1 10.1016/j.bmc.2009.12.067
CHEMBL601859 203412 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 461 10 0 5 3.4 COc1ccc(S(=O)(=O)N(CCCN2CCN(c3ccc(F)cc3)CC2)CC2CC2)cc1 10.1016/j.bmc.2009.12.067
44452082 159494 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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)NCc1nc2cc(F)ccc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
CHEMBL410075 159494 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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)NCc1nc2cc(F)ccc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
42389303 187540 None 0 Human Binding pIC50 = 5.0 5.0 - 0
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(N2CCN(CCCNS(=O)(=O)c3ccc(OC)cc3)CC2)cc1 10.1016/j.bmc.2008.04.023
CHEMBL493811 187540 None 0 Human Binding pIC50 = 5.0 5.0 - 0
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(N2CCN(CCCNS(=O)(=O)c3ccc(OC)cc3)CC2)cc1 10.1016/j.bmc.2008.04.023
44452301 96323 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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)NCc3nc4cc(F)ccc4c(=O)n3-c3ccccc3)CC2)c(C)c1 10.1016/j.ejmech.2008.09.050
CHEMBL261099 96323 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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)NCc3nc4cc(F)ccc4c(=O)n3-c3ccccc3)CC2)c(C)c1 10.1016/j.ejmech.2008.09.050
44451985 96418 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 467 7 1 6 3.2 O=C(CCN1CCN(c2ccccc2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
CHEMBL261654 96418 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 467 7 1 6 3.2 O=C(CCN1CCN(c2ccccc2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.ejmech.2008.09.050
44452301 96323 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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)NCc3nc4cc(F)ccc4c(=O)n3-c3ccccc3)CC2)c(C)c1 10.1016/j.bmc.2007.11.049
CHEMBL261099 96323 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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)NCc3nc4cc(F)ccc4c(=O)n3-c3ccccc3)CC2)c(C)c1 10.1016/j.bmc.2007.11.049
44451985 96418 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 467 7 1 6 3.2 O=C(CCN1CCN(c2ccccc2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
CHEMBL261654 96418 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 467 7 1 6 3.2 O=C(CCN1CCN(c2ccccc2)CC1)NCc1nc2ccccc2c(=O)n1-c1ccccc1 10.1016/j.bmc.2007.11.049
14748689 187379 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 373 8 1 4 2.2 O=S(=O)(NCCCN1CCN(Cc2ccccc2)CC1)c1ccccc1 10.1016/j.bmc.2008.04.023
CHEMBL492794 187379 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 373 8 1 4 2.2 O=S(=O)(NCCCN1CCN(Cc2ccccc2)CC1)c1ccccc1 10.1016/j.bmc.2008.04.023
44452305 96362 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 495 7 1 6 3.8 Cc1cccc(N2CCN(CCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)c1C 10.1016/j.bmc.2007.11.049
CHEMBL261291 96362 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 495 7 1 6 3.8 Cc1cccc(N2CCN(CCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)c1C 10.1016/j.bmc.2007.11.049
44452305 96362 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 495 7 1 6 3.8 Cc1cccc(N2CCN(CCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)c1C 10.1016/j.ejmech.2008.09.050
CHEMBL261291 96362 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 495 7 1 6 3.8 Cc1cccc(N2CCN(CCC(=O)NCc3nc4ccccc4c(=O)n3-c3ccccc3)CC2)c1C 10.1016/j.ejmech.2008.09.050
44452078 95892 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 541 10 1 8 3.6 COc1ccc(-n2c(CNC(=O)CCCN3CCN(c4ccccc4OC)CC3)nc3ccccc3c2=O)cc1 10.1016/j.bmc.2007.11.049
CHEMBL258956 95892 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 541 10 1 8 3.6 COc1ccc(-n2c(CNC(=O)CCCN3CCN(c4ccccc4OC)CC3)nc3ccccc3c2=O)cc1 10.1016/j.bmc.2007.11.049
44452078 95892 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 541 10 1 8 3.6 COc1ccc(-n2c(CNC(=O)CCCN3CCN(c4ccccc4OC)CC3)nc3ccccc3c2=O)cc1 10.1016/j.ejmech.2008.09.050
CHEMBL258956 95892 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 541 10 1 8 3.6 COc1ccc(-n2c(CNC(=O)CCCN3CCN(c4ccccc4OC)CC3)nc3ccccc3c2=O)cc1 10.1016/j.ejmech.2008.09.050
44452195 157159 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 541 10 1 8 3.6 COc1cccc(-n2c(CNC(=O)CCCN3CCN(c4ccccc4OC)CC3)nc3ccccc3c2=O)c1 10.1016/j.ejmech.2008.09.050
CHEMBL407411 157159 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Inhibition of 5HT7 receptor by radioligand binding assayInhibition of 5HT7 receptor by radioligand binding assay
ChEMBL 541 10 1 8 3.6 COc1cccc(-n2c(CNC(=O)CCCN3CCN(c4ccccc4OC)CC3)nc3ccccc3c2=O)c1 10.1016/j.ejmech.2008.09.050
44452195 157159 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 541 10 1 8 3.6 COc1cccc(-n2c(CNC(=O)CCCN3CCN(c4ccccc4OC)CC3)nc3ccccc3c2=O)c1 10.1016/j.bmc.2007.11.049
CHEMBL407411 157159 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]LSD from human recombinant 5HT7 receptorDisplacement of [3H]LSD from human recombinant 5HT7 receptor
ChEMBL 541 10 1 8 3.6 COc1cccc(-n2c(CNC(=O)CCCN3CCN(c4ccccc4OC)CC3)nc3ccccc3c2=O)c1 10.1016/j.bmc.2007.11.049
46232621 204069 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 503 10 0 5 4.6 COc1ccc(S(=O)(=O)N(CCCN2CCN(c3ccc(F)cc3)CC2)CC2CCCCC2)cc1 10.1016/j.bmc.2009.12.067
CHEMBL605787 204069 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 503 10 0 5 4.6 COc1ccc(S(=O)(=O)N(CCCN2CCN(c3ccc(F)cc3)CC2)CC2CCCCC2)cc1 10.1016/j.bmc.2009.12.067
3066250 70310 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Inhibitory activity against 5-hydroxytryptamine 7 receptor in humanInhibitory activity against 5-hydroxytryptamine 7 receptor in human
ChEMBL 242 2 2 2 2.9 COc1ccc2[nH]c(C)c(C3=CCNCC3)c2c1 10.1016/j.bmcl.2005.06.067
CHEMBL194305 70310 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Inhibitory activity against 5-hydroxytryptamine 7 receptor in humanInhibitory activity against 5-hydroxytryptamine 7 receptor in human
ChEMBL 242 2 2 2 2.9 COc1ccc2[nH]c(C)c(C3=CCNCC3)c2c1 10.1016/j.bmcl.2005.06.067
11005810 10469 None 0 Human Binding pIC50 = 6 6.0 - 0
Inhibition of human 5-hydroxytryptamine 7 receptorInhibition of human 5-hydroxytryptamine 7 receptor
ChEMBL 517 10 1 4 6.2 N#Cc1ccc(CCOC(=O)NC2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
CHEMBL116463 10469 None 0 Human Binding pIC50 = 6 6.0 - 0
Inhibition of human 5-hydroxytryptamine 7 receptorInhibition of human 5-hydroxytryptamine 7 receptor
ChEMBL 517 10 1 4 6.2 N#Cc1ccc(CCOC(=O)NC2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
71061887 93171 None 0 Human Binding pKd = 8.9 8.9 66 2
Displacement of [3H]5-CT from human 5HT7 receptor transfected in HEK293 cells after 60 mins by Scatchard plot analysisDisplacement of [3H]5-CT from human 5HT7 receptor transfected in HEK293 cells after 60 mins by Scatchard plot analysis
ChEMBL 472 11 1 5 4.8 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)NCc3ccncc3)CC2)cc1 10.1016/j.bmc.2014.01.016
CHEMBL2442996 93171 None 0 Human Binding pKd = 8.9 8.9 66 2
Displacement of [3H]5-CT from human 5HT7 receptor transfected in HEK293 cells after 60 mins by Scatchard plot analysisDisplacement of [3H]5-CT from human 5HT7 receptor transfected in HEK293 cells after 60 mins by Scatchard plot analysis
ChEMBL 472 11 1 5 4.8 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)NCc3ccncc3)CC2)cc1 10.1016/j.bmc.2014.01.016
11785183 84747 None 0 Human Binding pKd = 7.8 7.8 -1 4
Activity at SB-269970 desensitized 5HT7 receptor assessed as reduction of substance P-induced contraction of Dunkin-Hartley guinea pig ileumActivity at SB-269970 desensitized 5HT7 receptor assessed as reduction 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 84747 None 0 Human Binding pKd = 7.8 7.8 -1 4
Activity at SB-269970 desensitized 5HT7 receptor assessed as reduction of substance P-induced contraction of Dunkin-Hartley guinea pig ileumActivity at SB-269970 desensitized 5HT7 receptor assessed as reduction 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
11224758 2353 None 4 Human Binding pKd = 7.7 7.7 -4 6
Activity at SB-269970 desensitized 5HT7 receptor assessed as reduction of substance P-induced contraction of Dunkin-Hartley guinea pig ileumActivity at SB-269970 desensitized 5HT7 receptor assessed as reduction 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 2353 None 4 Human Binding pKd = 7.7 7.7 -4 6
Activity at SB-269970 desensitized 5HT7 receptor assessed as reduction of substance P-induced contraction of Dunkin-Hartley guinea pig ileumActivity at SB-269970 desensitized 5HT7 receptor assessed as reduction 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 2353 None 4 Human Binding pKd = 7.7 7.7 -4 6
Activity at SB-269970 desensitized 5HT7 receptor assessed as reduction of substance P-induced contraction of Dunkin-Hartley guinea pig ileumActivity at SB-269970 desensitized 5HT7 receptor assessed as reduction 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
11282296 143402 None 0 Human Binding pKd = 7.6 7.6 -6 4
Activity at SB-269970 desensitized 5HT7 receptor assessed as reduction of substance P-induced contraction of Dunkin-Hartley guinea pig ileumActivity at SB-269970 desensitized 5HT7 receptor assessed as reduction 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 143402 None 0 Human Binding pKd = 7.6 7.6 -6 4
Activity at SB-269970 desensitized 5HT7 receptor assessed as reduction of substance P-induced contraction of Dunkin-Hartley guinea pig ileumActivity at SB-269970 desensitized 5HT7 receptor assessed as reduction 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
5 139 None 45 Human Binding pKd = 8.4 8.4 -3 54
Displacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2014.08.023
5202 139 None 45 Human Binding pKd = 8.4 8.4 -3 54
Displacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2014.08.023
CHEMBL39 139 None 45 Human Binding pKd = 8.4 8.4 -3 54
Displacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2014.08.023
DB08839 139 None 45 Human Binding pKd = 8.4 8.4 -3 54
Displacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2014.08.023
1809 134 None 25 Human Binding pKd = 7.5 7.5 -7 37
Activity at SB-269970 desensitized 5HT7 receptor assessed as reduction of substance P-induced contraction of Dunkin-Hartley guinea pig ileumActivity at SB-269970 desensitized 5HT7 receptor assessed as reduction 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
4 134 None 25 Human Binding pKd = 7.5 7.5 -7 37
Activity at SB-269970 desensitized 5HT7 receptor assessed as reduction of substance P-induced contraction of Dunkin-Hartley guinea pig ileumActivity at SB-269970 desensitized 5HT7 receptor assessed as reduction 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 134 None 25 Human Binding pKd = 7.5 7.5 -7 37
Activity at SB-269970 desensitized 5HT7 receptor assessed as reduction of substance P-induced contraction of Dunkin-Hartley guinea pig ileumActivity at SB-269970 desensitized 5HT7 receptor assessed as reduction 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
11191128 85244 None 0 Human Binding pKd = 7.2 7.2 -5 4
Activity at SB-269970 desensitized 5HT7 receptor assessed as reduction of substance P-induced contraction of Dunkin-Hartley guinea pig ileumActivity at SB-269970 desensitized 5HT7 receptor assessed as reduction of substance P-induced contraction of Dunkin-Hartley guinea pig ileum
ChEMBL 421 8 2 4 4.3 O=C(CCCCCN1CCN(c2ccccc2O)CC1)NC1CCCc2ccccc21 10.1021/jm049702f
CHEMBL225512 85244 None 0 Human Binding pKd = 7.2 7.2 -5 4
Activity at SB-269970 desensitized 5HT7 receptor assessed as reduction of substance P-induced contraction of Dunkin-Hartley guinea pig ileumActivity at SB-269970 desensitized 5HT7 receptor assessed as reduction of substance P-induced contraction of Dunkin-Hartley guinea pig ileum
ChEMBL 421 8 2 4 4.3 O=C(CCCCCN1CCN(c2ccccc2O)CC1)NC1CCCc2ccccc21 10.1021/jm049702f
11432177 85156 None 0 Human Binding pKd = 8.0 8.0 -1 4
Activity at SB-269970 desensitized 5HT7 receptor assessed as reduction of substance P-induced contraction of Dunkin-Hartley guinea pig ileumActivity at SB-269970 desensitized 5HT7 receptor assessed as reduction 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 85156 None 0 Human Binding pKd = 8.0 8.0 -1 4
Activity at SB-269970 desensitized 5HT7 receptor assessed as reduction of substance P-induced contraction of Dunkin-Hartley guinea pig ileumActivity at SB-269970 desensitized 5HT7 receptor assessed as reduction 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
3233 3512 None 28 Human Binding pKd = 8.0 8.0 2 17
Binding affinity to 5HT7 receptorBinding affinity to 5HT7 receptor
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2011.05.010
3247 3512 None 28 Human Binding pKd = 8.0 8.0 2 17
Binding affinity to 5HT7 receptorBinding affinity to 5HT7 receptor
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2011.05.010
6604889 3512 None 28 Human Binding pKd = 8.0 8.0 2 17
Binding affinity to 5HT7 receptorBinding affinity to 5HT7 receptor
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2011.05.010
CHEMBL282199 3512 None 28 Human Binding pKd = 8.0 8.0 2 17
Binding affinity to 5HT7 receptorBinding affinity to 5HT7 receptor
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2011.05.010
DB13988 3512 None 28 Human Binding pKd = 8.0 8.0 2 17
Binding affinity to 5HT7 receptorBinding affinity to 5HT7 receptor
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2011.05.010
1809 134 None 25 Rat Binding pKi = 10.5 10.5 -2 37
Binding affinity against Rat 5-hydroxytryptamine 7 receptor using [3H]5-HTBinding affinity against Rat 5-hydroxytryptamine 7 receptor using [3H]5-HT
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm9911433
4 134 None 25 Rat Binding pKi = 10.5 10.5 -2 37
Binding affinity against Rat 5-hydroxytryptamine 7 receptor using [3H]5-HTBinding affinity against Rat 5-hydroxytryptamine 7 receptor using [3H]5-HT
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm9911433
CHEMBL18840 134 None 25 Rat Binding pKi = 10.5 10.5 -2 37
Binding affinity against Rat 5-hydroxytryptamine 7 receptor using [3H]5-HTBinding affinity against Rat 5-hydroxytryptamine 7 receptor using [3H]5-HT
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm9911433
56944082 112141 None 0 Human Binding pKi = 10 10.0 169 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 466 8 1 6 3.5 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1ccc(F)c(Cl)c1 10.1021/jm401895u
CHEMBL3289972 112141 None 0 Human Binding pKi = 10 10.0 169 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 466 8 1 6 3.5 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1ccc(F)c(Cl)c1 10.1021/jm401895u
5 139 None 45 Human Binding pKi = 10.0 10.0 -3 54
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 139 None 45 Human Binding pKi = 10.0 10.0 -3 54
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 139 None 45 Human Binding pKi = 10.0 10.0 -3 54
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 139 None 45 Human Binding pKi = 10.0 10.0 -3 54
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
1809 134 None 25 Rat Binding pKi = 9.9 9.9 -2 37
Binding affinity at rat 5-hydroxytryptamine 7 receptor.Binding affinity at rat 5-hydroxytryptamine 7 receptor.
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm030826m
4 134 None 25 Rat Binding pKi = 9.9 9.9 -2 37
Binding affinity at rat 5-hydroxytryptamine 7 receptor.Binding affinity at rat 5-hydroxytryptamine 7 receptor.
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm030826m
CHEMBL18840 134 None 25 Rat Binding pKi = 9.9 9.9 -2 37
Binding affinity at rat 5-hydroxytryptamine 7 receptor.Binding affinity at rat 5-hydroxytryptamine 7 receptor.
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm030826m
5 139 None 45 Human Binding pKi = 9.9 9.9 -3 54
Displacement of [3H]LSD from human 5HT7 receptorDisplacement of [3H]LSD from human 5HT7 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm2006782
5202 139 None 45 Human Binding pKi = 9.9 9.9 -3 54
Displacement of [3H]LSD from human 5HT7 receptorDisplacement of [3H]LSD from human 5HT7 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm2006782
CHEMBL39 139 None 45 Human Binding pKi = 9.9 9.9 -3 54
Displacement of [3H]LSD from human 5HT7 receptorDisplacement of [3H]LSD from human 5HT7 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm2006782
DB08839 139 None 45 Human Binding pKi = 9.9 9.9 -3 54
Displacement of [3H]LSD from human 5HT7 receptorDisplacement of [3H]LSD from human 5HT7 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm2006782
23643664 2350 None 5 Rat Binding pKi = 9.9 9.9 -1 5
Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells
ChEMBL 481 9 1 3 6.2 O=C(NC1CCCc2c1cccc2)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1021/jm070487n
8434 2350 None 5 Rat Binding pKi = 9.9 9.9 -1 5
Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells
ChEMBL 481 9 1 3 6.2 O=C(NC1CCCc2c1cccc2)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1021/jm070487n
CHEMBL243954 2350 None 5 Rat Binding pKi = 9.9 9.9 -1 5
Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells
ChEMBL 481 9 1 3 6.2 O=C(NC1CCCc2c1cccc2)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1021/jm070487n
42631003 202074 None 10 Human Binding pKi = 9.8 9.8 2 8
Binding affinity to 5-HT7 receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT7 receptor (unknown origin) assessed as inhibition constant
ChEMBL 304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1016/j.ejmech.2022.114464
CHEMBL592752 202074 None 10 Human Binding pKi = 9.8 9.8 2 8
Binding affinity to 5-HT7 receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT7 receptor (unknown origin) assessed as inhibition constant
ChEMBL 304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1016/j.ejmech.2022.114464
42631003 202074 None 10 Human Binding pKi = 9.8 9.8 2 8
Displacement of [3H]lysergic acid from 5-HT7 receptor (unknown origin)Displacement of [3H]lysergic acid from 5-HT7 receptor (unknown origin)
ChEMBL 304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1021/acs.jmedchem.7b01898
CHEMBL592752 202074 None 10 Human Binding pKi = 9.8 9.8 2 8
Displacement of [3H]lysergic acid from 5-HT7 receptor (unknown origin)Displacement of [3H]lysergic acid from 5-HT7 receptor (unknown origin)
ChEMBL 304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1021/acs.jmedchem.7b01898
168271260 190625 None 0 Human Binding pKi = 9.8 9.8 - 1
Binding affinity to human recombinant 5-HT7 receptor expressed in CHO cells assessed as inhibition constantBinding affinity to human recombinant 5-HT7 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 432 7 0 5 3.0 O=S(=O)(c1ccccc1F)N1CCC[C@@H]1CCCN1CCN(c2ccccn2)CC1 10.1021/acs.jmedchem.2c00633
CHEMBL5179460 190625 None 0 Human Binding pKi = 9.8 9.8 - 1
Binding affinity to human recombinant 5-HT7 receptor expressed in CHO cells assessed as inhibition constantBinding affinity to human recombinant 5-HT7 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 432 7 0 5 3.0 O=S(=O)(c1ccccc1F)N1CCC[C@@H]1CCCN1CCN(c2ccccn2)CC1 10.1021/acs.jmedchem.2c00633
5 139 None 45 Human Binding pKi = 9.8 9.8 -3 54
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 139 None 45 Human Binding pKi = 9.8 9.8 -3 54
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 139 None 45 Human Binding pKi = 9.8 9.8 -3 54
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 139 None 45 Human Binding pKi = 9.8 9.8 -3 54
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
10450593 124332 None 0 Human Binding pKi = 9.7 9.7 75 3
Displacement of [3H]5CT from 5HT7 receptorDisplacement of [3H]5CT from 5HT7 receptor
ChEMBL 351 8 2 4 4.9 C[C@H](Nc1ccnc(NCCOc2ccc(F)cc2)c1)c1ccccc1 10.1016/j.bmcl.2010.03.012
CHEMBL363452 124332 None 0 Human Binding pKi = 9.7 9.7 75 3
Displacement of [3H]5CT from 5HT7 receptorDisplacement of [3H]5CT from 5HT7 receptor
ChEMBL 351 8 2 4 4.9 C[C@H](Nc1ccnc(NCCOc2ccc(F)cc2)c1)c1ccccc1 10.1016/j.bmcl.2010.03.012
10450593 124332 None 0 Human Binding pKi = 9.7 9.7 75 3
Binding affinity against 5-Hydroxy tryptamine 7 receptorBinding affinity against 5-Hydroxy tryptamine 7 receptor
ChEMBL 351 8 2 4 4.9 C[C@H](Nc1ccnc(NCCOc2ccc(F)cc2)c1)c1ccccc1 10.1016/j.bmcl.2004.06.007
CHEMBL363452 124332 None 0 Human Binding pKi = 9.7 9.7 75 3
Binding affinity against 5-Hydroxy tryptamine 7 receptorBinding affinity against 5-Hydroxy tryptamine 7 receptor
ChEMBL 351 8 2 4 4.9 C[C@H](Nc1ccnc(NCCOc2ccc(F)cc2)c1)c1ccccc1 10.1016/j.bmcl.2004.06.007
66801551 112186 None 0 Human Binding pKi = 9.7 9.7 3 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 519 8 1 6 5.6 Cc1c(S(=O)(=O)NCCCCN2CCC(c3noc4cc(F)ccc34)CC2)sc2ccc(F)cc12 10.1021/jm401895u
CHEMBL3290016 112186 None 0 Human Binding pKi = 9.7 9.7 3 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 519 8 1 6 5.6 Cc1c(S(=O)(=O)NCCCCN2CCC(c3noc4cc(F)ccc34)CC2)sc2ccc(F)cc12 10.1021/jm401895u
46224879 204004 None 3 Human Binding pKi = 9.7 9.7 1 7
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 302 2 0 2 4.6 Cc1ccc2c(c1)c1c(n2/C=C\c2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL605405 204004 None 3 Human Binding pKi = 9.7 9.7 1 7
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 302 2 0 2 4.6 Cc1ccc2c(c1)c1c(n2/C=C\c2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
168287666 191769 None 0 Human Binding pKi = 9.7 9.7 - 1
Binding affinity to human recombinant 5-HT7 receptor expressed in CHO cells assessed as inhibition constantBinding affinity to human recombinant 5-HT7 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 465 7 0 4 4.2 O=S(=O)(c1ccccc1F)N1CCC[C@@H]1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00633
CHEMBL5196234 191769 None 0 Human Binding pKi = 9.7 9.7 - 1
Binding affinity to human recombinant 5-HT7 receptor expressed in CHO cells assessed as inhibition constantBinding affinity to human recombinant 5-HT7 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 465 7 0 4 4.2 O=S(=O)(c1ccccc1F)N1CCC[C@@H]1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00633
11224758 2353 None 4 Human Binding pKi = 9.7 9.7 -4 6
Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-countingDisplacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-counting
ChEMBL 451 9 1 4 5.3 CSc1ccccc1N1CCN(CC1)CCCCCC(=O)NC1CCCc2c1cccc2 10.1016/j.ejmech.2014.03.005
8435 2353 None 4 Human Binding pKi = 9.7 9.7 -4 6
Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-countingDisplacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-counting
ChEMBL 451 9 1 4 5.3 CSc1ccccc1N1CCN(CC1)CCCCCC(=O)NC1CCCc2c1cccc2 10.1016/j.ejmech.2014.03.005
CHEMBL225284 2353 None 4 Human Binding pKi = 9.7 9.7 -4 6
Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-countingDisplacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-counting
ChEMBL 451 9 1 4 5.3 CSc1ccccc1N1CCN(CC1)CCCCCC(=O)NC1CCCc2c1cccc2 10.1016/j.ejmech.2014.03.005
11224758 2353 None 4 Human Binding pKi = 9.7 9.7 -4 6
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells after 1 hr
ChEMBL 451 9 1 4 5.3 CSc1ccccc1N1CCN(CC1)CCCCCC(=O)NC1CCCc2c1cccc2 10.1016/j.ejmech.2014.12.041
8435 2353 None 4 Human Binding pKi = 9.7 9.7 -4 6
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells after 1 hr
ChEMBL 451 9 1 4 5.3 CSc1ccccc1N1CCN(CC1)CCCCCC(=O)NC1CCCc2c1cccc2 10.1016/j.ejmech.2014.12.041
CHEMBL225284 2353 None 4 Human Binding pKi = 9.7 9.7 -4 6
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells after 1 hr
ChEMBL 451 9 1 4 5.3 CSc1ccccc1N1CCN(CC1)CCCCCC(=O)NC1CCCc2c1cccc2 10.1016/j.ejmech.2014.12.041
11224758 2353 None 4 Human Binding pKi = 9.7 9.7 -4 6
Displacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry
ChEMBL 451 9 1 4 5.3 CSc1ccccc1N1CCN(CC1)CCCCCC(=O)NC1CCCc2c1cccc2 10.1016/j.ejmech.2014.08.023
8435 2353 None 4 Human Binding pKi = 9.7 9.7 -4 6
Displacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry
ChEMBL 451 9 1 4 5.3 CSc1ccccc1N1CCN(CC1)CCCCCC(=O)NC1CCCc2c1cccc2 10.1016/j.ejmech.2014.08.023
CHEMBL225284 2353 None 4 Human Binding pKi = 9.7 9.7 -4 6
Displacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry
ChEMBL 451 9 1 4 5.3 CSc1ccccc1N1CCN(CC1)CCCCCC(=O)NC1CCCc2c1cccc2 10.1016/j.ejmech.2014.08.023
11224758 2353 None 4 Rat Binding pKi = 9.7 9.7 4 6
Displacement of [3H]LSD from rat cloned 5-Hydroxytryptamine receptor 7 after 60 minsDisplacement of [3H]LSD from rat cloned 5-Hydroxytryptamine receptor 7 after 60 mins
ChEMBL 451 9 1 4 5.3 CSc1ccccc1N1CCN(CC1)CCCCCC(=O)NC1CCCc2c1cccc2 10.1021/acs.jmedchem.5b00982
8435 2353 None 4 Rat Binding pKi = 9.7 9.7 4 6
Displacement of [3H]LSD from rat cloned 5-Hydroxytryptamine receptor 7 after 60 minsDisplacement of [3H]LSD from rat cloned 5-Hydroxytryptamine receptor 7 after 60 mins
ChEMBL 451 9 1 4 5.3 CSc1ccccc1N1CCN(CC1)CCCCCC(=O)NC1CCCc2c1cccc2 10.1021/acs.jmedchem.5b00982
CHEMBL225284 2353 None 4 Rat Binding pKi = 9.7 9.7 4 6
Displacement of [3H]LSD from rat cloned 5-Hydroxytryptamine receptor 7 after 60 minsDisplacement of [3H]LSD from rat cloned 5-Hydroxytryptamine receptor 7 after 60 mins
ChEMBL 451 9 1 4 5.3 CSc1ccccc1N1CCN(CC1)CCCCCC(=O)NC1CCCc2c1cccc2 10.1021/acs.jmedchem.5b00982
11224758 2353 None 4 Rat Binding pKi = 9.7 9.7 4 6
Displacement of [3H]LSD from rat recombinant 5-HT7 receptor expressed in HEK293 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]LSD from rat recombinant 5-HT7 receptor expressed in HEK293 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 451 9 1 4 5.3 CSc1ccccc1N1CCN(CC1)CCCCCC(=O)NC1CCCc2c1cccc2 10.1021/acs.jmedchem.7b01898
8435 2353 None 4 Rat Binding pKi = 9.7 9.7 4 6
Displacement of [3H]LSD from rat recombinant 5-HT7 receptor expressed in HEK293 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]LSD from rat recombinant 5-HT7 receptor expressed in HEK293 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 451 9 1 4 5.3 CSc1ccccc1N1CCN(CC1)CCCCCC(=O)NC1CCCc2c1cccc2 10.1021/acs.jmedchem.7b01898
CHEMBL225284 2353 None 4 Rat Binding pKi = 9.7 9.7 4 6
Displacement of [3H]LSD from rat recombinant 5-HT7 receptor expressed in HEK293 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]LSD from rat recombinant 5-HT7 receptor expressed in HEK293 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 451 9 1 4 5.3 CSc1ccccc1N1CCN(CC1)CCCCCC(=O)NC1CCCc2c1cccc2 10.1021/acs.jmedchem.7b01898
11224758 2353 None 4 Rat Binding pKi = 9.7 9.7 4 6
Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells
ChEMBL 451 9 1 4 5.3 CSc1ccccc1N1CCN(CC1)CCCCCC(=O)NC1CCCc2c1cccc2 10.1021/jm049702f
8435 2353 None 4 Rat Binding pKi = 9.7 9.7 4 6
Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells
ChEMBL 451 9 1 4 5.3 CSc1ccccc1N1CCN(CC1)CCCCCC(=O)NC1CCCc2c1cccc2 10.1021/jm049702f
CHEMBL225284 2353 None 4 Rat Binding pKi = 9.7 9.7 4 6
Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells
ChEMBL 451 9 1 4 5.3 CSc1ccccc1N1CCN(CC1)CCCCCC(=O)NC1CCCc2c1cccc2 10.1021/jm049702f
5 139 None 45 Human Binding pKi = 9.7 9.7 -3 54
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 139 None 45 Human Binding pKi = 9.7 9.7 -3 54
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 139 None 45 Human Binding pKi = 9.7 9.7 -3 54
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 139 None 45 Human Binding pKi = 9.7 9.7 -3 54
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
10402615 204974 None 0 Rat Binding pKi = 9.6 9.6 20 3
Binding affinity at rat 5-hydroxytryptamine 7 receptor.Binding affinity at rat 5-hydroxytryptamine 7 receptor.
ChEMBL 301 2 0 1 4.9 CN(C)[C@H]1CCc2c(cccc2-c2cccc3ccccc23)C1 10.1021/jm030826m
CHEMBL611472 204974 None 0 Rat Binding pKi = 9.6 9.6 20 3
Binding affinity at rat 5-hydroxytryptamine 7 receptor.Binding affinity at rat 5-hydroxytryptamine 7 receptor.
ChEMBL 301 2 0 1 4.9 CN(C)[C@H]1CCc2c(cccc2-c2cccc3ccccc23)C1 10.1021/jm030826m
42631003 202074 None 10 Human Binding pKi = 9.6 9.6 2 8
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 304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL592752 202074 None 10 Human Binding pKi = 9.6 9.6 2 8
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 304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
145989143 167282 None 0 Human Binding pKi = 9.6 9.6 2 2
Displacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cell membranes after 120 mins by TopCount scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cell membranes after 120 mins by TopCount scintillation counting method
ChEMBL 399 5 1 2 5.3 Fc1ccc2[nH]cc(CCN3CCN(c4ccccc4-c4ccccc4)CC3)c2c1 10.1016/j.ejmech.2017.12.063
CHEMBL4291322 167282 None 0 Human Binding pKi = 9.6 9.6 2 2
Displacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cell membranes after 120 mins by TopCount scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cell membranes after 120 mins by TopCount scintillation counting method
ChEMBL 399 5 1 2 5.3 Fc1ccc2[nH]cc(CCN3CCN(c4ccccc4-c4ccccc4)CC3)c2c1 10.1016/j.ejmech.2017.12.063
44393091 65378 None 0 Human Binding pKi = 9.5 9.5 - 1
Binding affinity against 5-Hydroxy tryptamine 7 receptorBinding affinity against 5-Hydroxy tryptamine 7 receptor
ChEMBL 317 7 2 3 4.9 C[C@H](Nc1ccnc(NCCc2ccccc2)c1)c1ccccc1 10.1016/j.bmcl.2004.06.007
CHEMBL182923 65378 None 0 Human Binding pKi = 9.5 9.5 - 1
Binding affinity against 5-Hydroxy tryptamine 7 receptorBinding affinity against 5-Hydroxy tryptamine 7 receptor
ChEMBL 317 7 2 3 4.9 C[C@H](Nc1ccnc(NCCc2ccccc2)c1)c1ccccc1 10.1016/j.bmcl.2004.06.007
44393169 65617 None 0 Human Binding pKi = 9.5 9.5 - 1
Binding affinity against 5-Hydroxy tryptamine 7 receptorBinding affinity against 5-Hydroxy tryptamine 7 receptor
ChEMBL 352 8 2 5 4.3 C[C@H](Nc1ccnc(NCCOc2ccc(F)cc2)n1)c1ccccc1 10.1016/j.bmcl.2004.06.007
CHEMBL183277 65617 None 0 Human Binding pKi = 9.5 9.5 - 1
Binding affinity against 5-Hydroxy tryptamine 7 receptorBinding affinity against 5-Hydroxy tryptamine 7 receptor
ChEMBL 352 8 2 5 4.3 C[C@H](Nc1ccnc(NCCOc2ccc(F)cc2)n1)c1ccccc1 10.1016/j.bmcl.2004.06.007
71454999 81453 None 0 Human Binding pKi = 9.5 9.5 169 4
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr
ChEMBL 420 8 1 4 3.8 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2012.07.043
CHEMBL2159465 81453 None 0 Human Binding pKi = 9.5 9.5 169 4
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr
ChEMBL 420 8 1 4 3.8 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2012.07.043
1809 134 None 25 Human Binding pKi = 9.5 9.5 -7 37
Displacement of [3H]-5-CT from human cloned 5HT7 receptorDisplacement of [3H]-5-CT from human cloned 5HT7 receptor
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm3003679
4 134 None 25 Human Binding pKi = 9.5 9.5 -7 37
Displacement of [3H]-5-CT from human cloned 5HT7 receptorDisplacement of [3H]-5-CT from human cloned 5HT7 receptor
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm3003679
CHEMBL18840 134 None 25 Human Binding pKi = 9.5 9.5 -7 37
Displacement of [3H]-5-CT from human cloned 5HT7 receptorDisplacement of [3H]-5-CT from human cloned 5HT7 receptor
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm3003679
46233450 202699 None 0 Human Binding pKi = 9.5 9.5 - 1
Displacement of [3H]5CT from human cloned 5HT7B receptor expressed in HEK293 cellsDisplacement of [3H]5CT from human cloned 5HT7B receptor expressed in HEK293 cells
ChEMBL 357 6 0 1 6.5 CCCN(CCC)[C@H]1CCc2c(cccc2-c2cccc3ccccc23)C1 10.1016/j.bmc.2010.01.035
CHEMBL596959 202699 None 0 Human Binding pKi = 9.5 9.5 - 1
Displacement of [3H]5CT from human cloned 5HT7B receptor expressed in HEK293 cellsDisplacement of [3H]5CT from human cloned 5HT7B receptor expressed in HEK293 cells
ChEMBL 357 6 0 1 6.5 CCCN(CCC)[C@H]1CCc2c(cccc2-c2cccc3ccccc23)C1 10.1016/j.bmc.2010.01.035
10413595 161935 None 0 Human Binding pKi = 9.5 9.5 -1 11
Compound was evaluated for binding affinity against human cloned 5-hydroxytryptamine 7 receptor in HEK 293 cells using [3H]5-CT as the radioligand (n=3)Compound was evaluated for binding affinity against human cloned 5-hydroxytryptamine 7 receptor in HEK 293 cells using [3H]5-CT as the radioligand (n=3)
ChEMBL 499 4 1 5 2.5 COc1ccc(S(=O)(=O)N2CCc3ccc(I)cc32)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL414628 161935 None 0 Human Binding pKi = 9.5 9.5 -1 11
Compound was evaluated for binding affinity against human cloned 5-hydroxytryptamine 7 receptor in HEK 293 cells using [3H]5-CT as the radioligand (n=3)Compound was evaluated for binding affinity against human cloned 5-hydroxytryptamine 7 receptor in HEK 293 cells using [3H]5-CT as the radioligand (n=3)
ChEMBL 499 4 1 5 2.5 COc1ccc(S(=O)(=O)N2CCc3ccc(I)cc32)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
168283786 190979 None 0 Human Binding pKi = 9.5 9.5 - 1
Binding affinity to human recombinant 5-HT7 receptor expressed in CHO cells assessed as inhibition constantBinding affinity to human recombinant 5-HT7 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 465 7 0 4 4.2 O=S(=O)(c1ccc(F)cc1)N1CCC[C@@H]1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00633
CHEMBL5184712 190979 None 0 Human Binding pKi = 9.5 9.5 - 1
Binding affinity to human recombinant 5-HT7 receptor expressed in CHO cells assessed as inhibition constantBinding affinity to human recombinant 5-HT7 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 465 7 0 4 4.2 O=S(=O)(c1ccc(F)cc1)N1CCC[C@@H]1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00633
3233 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by liquid scintillation countingDisplacement of [3H]-LSD from 5HT7 receptor (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by liquid scintillation counting
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.1c01093
3247 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by liquid scintillation countingDisplacement of [3H]-LSD from 5HT7 receptor (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by liquid scintillation counting
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.1c01093
6604889 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by liquid scintillation countingDisplacement of [3H]-LSD from 5HT7 receptor (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by liquid scintillation counting
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.1c01093
CHEMBL282199 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by liquid scintillation countingDisplacement of [3H]-LSD from 5HT7 receptor (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by liquid scintillation counting
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.1c01093
DB13988 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by liquid scintillation countingDisplacement of [3H]-LSD from 5HT7 receptor (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by liquid scintillation counting
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.1c01093
3233 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting methodDisplacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting method
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2016.01.043
3247 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting methodDisplacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting method
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2016.01.043
6604889 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting methodDisplacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting method
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2016.01.043
CHEMBL282199 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting methodDisplacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting method
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2016.01.043
DB13988 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting methodDisplacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting method
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2016.01.043
3233 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]LSD from human 5-HT7 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT7 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.8b00642
3247 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]LSD from human 5-HT7 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT7 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.8b00642
6604889 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]LSD from human 5-HT7 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT7 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.8b00642
CHEMBL282199 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]LSD from human 5-HT7 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT7 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.8b00642
DB13988 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]LSD from human 5-HT7 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT7 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.8b00642
3233 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by liquid scintillation countingDisplacement of [3H]-LSD from 5HT7 receptor (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by liquid scintillation counting
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.1c01093
3247 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by liquid scintillation countingDisplacement of [3H]-LSD from 5HT7 receptor (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by liquid scintillation counting
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.1c01093
6604889 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by liquid scintillation countingDisplacement of [3H]-LSD from 5HT7 receptor (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by liquid scintillation counting
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.1c01093
CHEMBL282199 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by liquid scintillation countingDisplacement of [3H]-LSD from 5HT7 receptor (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by liquid scintillation counting
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.1c01093
DB13988 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by liquid scintillation countingDisplacement of [3H]-LSD from 5HT7 receptor (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by liquid scintillation counting
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.1c01093
3233 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]D-lysergic acid diethylamide from 5HT7R (unknown origin) expressed in HEK293 cell membranes incubated for 1.5 hrs in absence of light by liquid scintillation countingDisplacement of [3H]D-lysergic acid diethylamide from 5HT7R (unknown origin) expressed in HEK293 cell membranes incubated for 1.5 hrs in absence of light by liquid scintillation counting
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 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]D-lysergic acid diethylamide from 5HT7R (unknown origin) expressed in HEK293 cell membranes incubated for 1.5 hrs in absence of light by liquid scintillation countingDisplacement of [3H]D-lysergic acid diethylamide from 5HT7R (unknown origin) expressed in HEK293 cell membranes incubated for 1.5 hrs in absence of light by liquid scintillation counting
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 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]D-lysergic acid diethylamide from 5HT7R (unknown origin) expressed in HEK293 cell membranes incubated for 1.5 hrs in absence of light by liquid scintillation countingDisplacement of [3H]D-lysergic acid diethylamide from 5HT7R (unknown origin) expressed in HEK293 cell membranes incubated for 1.5 hrs in absence of light by liquid scintillation counting
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 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]D-lysergic acid diethylamide from 5HT7R (unknown origin) expressed in HEK293 cell membranes incubated for 1.5 hrs in absence of light by liquid scintillation countingDisplacement of [3H]D-lysergic acid diethylamide from 5HT7R (unknown origin) expressed in HEK293 cell membranes incubated for 1.5 hrs in absence of light by liquid scintillation counting
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 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]D-lysergic acid diethylamide from 5HT7R (unknown origin) expressed in HEK293 cell membranes incubated for 1.5 hrs in absence of light by liquid scintillation countingDisplacement of [3H]D-lysergic acid diethylamide from 5HT7R (unknown origin) expressed in HEK293 cell membranes incubated for 1.5 hrs in absence of light by liquid scintillation counting
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 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting methodDisplacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting method
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2016.01.043
3247 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting methodDisplacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting method
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2016.01.043
6604889 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting methodDisplacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting method
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2016.01.043
CHEMBL282199 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting methodDisplacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting method
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2016.01.043
DB13988 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting methodDisplacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting method
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2016.01.043
3233 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]LSD from 5-HT7R (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting methodDisplacement of [3H]LSD from 5-HT7R (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting method
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2014.07.026
3247 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]LSD from 5-HT7R (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting methodDisplacement of [3H]LSD from 5-HT7R (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting method
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2014.07.026
6604889 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]LSD from 5-HT7R (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting methodDisplacement of [3H]LSD from 5-HT7R (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting method
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2014.07.026
CHEMBL282199 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]LSD from 5-HT7R (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting methodDisplacement of [3H]LSD from 5-HT7R (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting method
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2014.07.026
DB13988 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]LSD from 5-HT7R (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting methodDisplacement of [3H]LSD from 5-HT7R (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting method
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2014.07.026
3233 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]LSD from human 5-HT7 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT7 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.8b00642
3247 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]LSD from human 5-HT7 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT7 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.8b00642
6604889 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]LSD from human 5-HT7 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT7 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.8b00642
CHEMBL282199 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]LSD from human 5-HT7 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT7 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.8b00642
DB13988 3512 None 28 Human Binding pKi = 9.5 9.5 2 17
Displacement of [3H]LSD from human 5-HT7 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT7 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.8b00642
1809 134 None 25 Human Binding pKi = 9.5 9.5 -7 37
Displacement of [3H]-5-CT from human 5-HT7R expressed in human HEK293 cells assessed as inhibitory constant incubated for 60 mins by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT7R expressed in human HEK293 cells assessed as inhibitory constant incubated for 60 mins by radioligand binding assay
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1016/j.ejmech.2020.112395
4 134 None 25 Human Binding pKi = 9.5 9.5 -7 37
Displacement of [3H]-5-CT from human 5-HT7R expressed in human HEK293 cells assessed as inhibitory constant incubated for 60 mins by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT7R expressed in human HEK293 cells assessed as inhibitory constant incubated for 60 mins by radioligand binding assay
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1016/j.ejmech.2020.112395
CHEMBL18840 134 None 25 Human Binding pKi = 9.5 9.5 -7 37
Displacement of [3H]-5-CT from human 5-HT7R expressed in human HEK293 cells assessed as inhibitory constant incubated for 60 mins by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT7R expressed in human HEK293 cells assessed as inhibitory constant incubated for 60 mins by radioligand binding assay
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1016/j.ejmech.2020.112395
11524413 96428 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometryDisplacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometry
ChEMBL 411 7 1 3 4.9 CCC1(CCCCN2CCN(c3ccc(Cl)cc3)CC2)C(=O)Nc2ccccc21 10.1021/jm200547z
CHEMBL261719 96428 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometryDisplacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometry
ChEMBL 411 7 1 3 4.9 CCC1(CCCCN2CCN(c3ccc(Cl)cc3)CC2)C(=O)Nc2ccccc21 10.1021/jm200547z
11589069 96300 None 0 Human Binding pKi = 9.4 9.4 10 8
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 383 6 1 3 4.4 O=C1Nc2ccccc2C1CCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm070279v
CHEMBL260994 96300 None 0 Human Binding pKi = 9.4 9.4 10 8
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 383 6 1 3 4.4 O=C1Nc2ccccc2C1CCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm070279v
11524413 96428 None 0 Human Binding pKi = 9.4 9.4 - 1
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 411 7 1 3 4.9 CCC1(CCCCN2CCN(c3ccc(Cl)cc3)CC2)C(=O)Nc2ccccc21 10.1021/jm070279v
CHEMBL261719 96428 None 0 Human Binding pKi = 9.4 9.4 - 1
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 411 7 1 3 4.9 CCC1(CCCCN2CCN(c3ccc(Cl)cc3)CC2)C(=O)Nc2ccccc21 10.1021/jm070279v
11524413 96428 None 0 Human Binding pKi = 9.4 9.4 - 1
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 411 7 1 3 4.9 CCC1(CCCCN2CCN(c3ccc(Cl)cc3)CC2)C(=O)Nc2ccccc21 10.1021/jm070279v
CHEMBL261719 96428 None 0 Human Binding pKi = 9.4 9.4 - 1
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 411 7 1 3 4.9 CCC1(CCCCN2CCN(c3ccc(Cl)cc3)CC2)C(=O)Nc2ccccc21 10.1021/jm070279v
44126269 203941 None 4 Human Binding pKi = 9.4 9.4 2 6
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 318 3 0 2 4.5 Cc1ccc(CCn2c3c(c4cc(C)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
CHEMBL605081 203941 None 4 Human Binding pKi = 9.4 9.4 2 6
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 318 3 0 2 4.5 Cc1ccc(CCn2c3c(c4cc(C)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
1809 134 None 25 Human Binding pKi = 9.4 9.4 -7 37
Binding affinity against 5-hydroxytryptamine 7 human receptorsBinding affinity against 5-hydroxytryptamine 7 human receptors
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm0341204
4 134 None 25 Human Binding pKi = 9.4 9.4 -7 37
Binding affinity against 5-hydroxytryptamine 7 human receptorsBinding affinity against 5-hydroxytryptamine 7 human receptors
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm0341204
CHEMBL18840 134 None 25 Human Binding pKi = 9.4 9.4 -7 37
Binding affinity against 5-hydroxytryptamine 7 human receptorsBinding affinity against 5-hydroxytryptamine 7 human receptors
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm0341204
44393073 64484 None 0 Human Binding pKi = 9.4 9.4 - 1
Binding affinity against 5-Hydroxy tryptamine 7 receptorBinding affinity against 5-Hydroxy tryptamine 7 receptor
ChEMBL 333 8 2 4 4.7 C[C@H](Nc1ccnc(NCCOc2ccccc2)c1)c1ccccc1 10.1016/j.bmcl.2004.06.007
CHEMBL181356 64484 None 0 Human Binding pKi = 9.4 9.4 - 1
Binding affinity against 5-Hydroxy tryptamine 7 receptorBinding affinity against 5-Hydroxy tryptamine 7 receptor
ChEMBL 333 8 2 4 4.7 C[C@H](Nc1ccnc(NCCOc2ccccc2)c1)c1ccccc1 10.1016/j.bmcl.2004.06.007
44393092 64601 None 0 Human Binding pKi = 9.4 9.4 - 1
Binding affinity against 5-Hydroxy tryptamine 7 receptorBinding affinity against 5-Hydroxy tryptamine 7 receptor
ChEMBL 335 7 2 3 5.0 C[C@H](Nc1ccnc(NCCc2ccc(F)cc2)c1)c1ccccc1 10.1016/j.bmcl.2004.06.007
CHEMBL181605 64601 None 0 Human Binding pKi = 9.4 9.4 - 1
Binding affinity against 5-Hydroxy tryptamine 7 receptorBinding affinity against 5-Hydroxy tryptamine 7 receptor
ChEMBL 335 7 2 3 5.0 C[C@H](Nc1ccnc(NCCc2ccc(F)cc2)c1)c1ccccc1 10.1016/j.bmcl.2004.06.007
44393193 65662 None 0 Human Binding pKi = 9.4 9.4 32 2
Binding affinity against 5-Hydroxy tryptamine 7 receptorBinding affinity against 5-Hydroxy tryptamine 7 receptor
ChEMBL 351 8 2 4 4.9 C[C@H](Nc1cc(NCCOc2ccc(F)cc2)ccn1)c1ccccc1 10.1016/j.bmcl.2004.06.007
CHEMBL183423 65662 None 0 Human Binding pKi = 9.4 9.4 32 2
Binding affinity against 5-Hydroxy tryptamine 7 receptorBinding affinity against 5-Hydroxy tryptamine 7 receptor
ChEMBL 351 8 2 4 4.9 C[C@H](Nc1cc(NCCOc2ccc(F)cc2)ccn1)c1ccccc1 10.1016/j.bmcl.2004.06.007
44393192 66274 None 0 Human Binding pKi = 9.4 9.4 - 1
Binding affinity against 5-Hydroxy tryptamine 7 receptorBinding affinity against 5-Hydroxy tryptamine 7 receptor
ChEMBL 333 8 2 4 4.7 C[C@H](Nc1cc(NCCOc2ccccc2)ccn1)c1ccccc1 10.1016/j.bmcl.2004.06.007
CHEMBL184607 66274 None 0 Human Binding pKi = 9.4 9.4 - 1
Binding affinity against 5-Hydroxy tryptamine 7 receptorBinding affinity against 5-Hydroxy tryptamine 7 receptor
ChEMBL 333 8 2 4 4.7 C[C@H](Nc1cc(NCCOc2ccccc2)ccn1)c1ccccc1 10.1016/j.bmcl.2004.06.007
2389 3331 None 72 Human Binding pKi = 9.4 9.4 -7 67
Displacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2018.01.002
5073 3331 None 72 Human Binding pKi = 9.4 9.4 -7 67
Displacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2018.01.002
5073.0 3331 None 72 Human Binding pKi = 9.4 9.4 -7 67
Displacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2018.01.002
96 3331 None 72 Human Binding pKi = 9.4 9.4 -7 67
Displacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2018.01.002
CHEMBL85 3331 None 72 Human Binding pKi = 9.4 9.4 -7 67
Displacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2018.01.002
DB00734 3331 None 72 Human Binding pKi = 9.4 9.4 -7 67
Displacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2018.01.002
145985050 165785 None 0 Human Binding pKi = 9.4 9.4 -3 5
Displacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 508 6 0 6 4.9 O=S(=O)(c1cncc2ccccc12)N1CCC[C@H]1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4245263 165785 None 0 Human Binding pKi = 9.4 9.4 -3 5
Displacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 508 6 0 6 4.9 O=S(=O)(c1cncc2ccccc12)N1CCC[C@H]1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1016/j.ejmech.2018.01.002
1809 134 None 25 Human Binding pKi = 9.4 9.4 -7 37
Displacement of [3H]-5-CT from human recombinant 5-HT7 receptor expressed in CHO-K1 cells after 120 minsDisplacement of [3H]-5-CT from human recombinant 5-HT7 receptor expressed in CHO-K1 cells after 120 mins
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1016/j.ejmech.2013.09.018
4 134 None 25 Human Binding pKi = 9.4 9.4 -7 37
Displacement of [3H]-5-CT from human recombinant 5-HT7 receptor expressed in CHO-K1 cells after 120 minsDisplacement of [3H]-5-CT from human recombinant 5-HT7 receptor expressed in CHO-K1 cells after 120 mins
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1016/j.ejmech.2013.09.018
CHEMBL18840 134 None 25 Human Binding pKi = 9.4 9.4 -7 37
Displacement of [3H]-5-CT from human recombinant 5-HT7 receptor expressed in CHO-K1 cells after 120 minsDisplacement of [3H]-5-CT from human recombinant 5-HT7 receptor expressed in CHO-K1 cells after 120 mins
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1016/j.ejmech.2013.09.018
24854273 158464 None 0 Human Binding pKi = 9.4 9.4 112 2
Displacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometryDisplacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometry
ChEMBL 411 7 1 3 4.9 CCC1(CCCCN2CCN(c3cccc(Cl)c3)CC2)C(=O)Nc2ccccc21 10.1021/jm200547z
CHEMBL408976 158464 None 0 Human Binding pKi = 9.4 9.4 112 2
Displacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometryDisplacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometry
ChEMBL 411 7 1 3 4.9 CCC1(CCCCN2CCN(c3cccc(Cl)c3)CC2)C(=O)Nc2ccccc21 10.1021/jm200547z
56944763 112174 None 0 Human Binding pKi = 9.4 9.4 4 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 453 6 1 5 4.3 O=S(=O)(NCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
CHEMBL3290004 112174 None 0 Human Binding pKi = 9.4 9.4 4 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 453 6 1 5 4.3 O=S(=O)(NCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
44266163 97108 None 1 Human Binding pKi = 9.4 9.4 4 2
Binding affinity at human cloned 5-hydroxytryptamine 7 receptor.Binding affinity at human cloned 5-hydroxytryptamine 7 receptor.
ChEMBL 387 4 1 2 4.4 O=C1c2ccccc2CCCN1CCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(03)00077-5
CHEMBL267062 97108 None 1 Human Binding pKi = 9.4 9.4 4 2
Binding affinity at human cloned 5-hydroxytryptamine 7 receptor.Binding affinity at human cloned 5-hydroxytryptamine 7 receptor.
ChEMBL 387 4 1 2 4.4 O=C1c2ccccc2CCCN1CCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(03)00077-5
24854273 158464 None 0 Human Binding pKi = 9.4 9.4 112 2
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 411 7 1 3 4.9 CCC1(CCCCN2CCN(c3cccc(Cl)c3)CC2)C(=O)Nc2ccccc21 10.1021/jm070279v
CHEMBL408976 158464 None 0 Human Binding pKi = 9.4 9.4 112 2
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 411 7 1 3 4.9 CCC1(CCCCN2CCN(c3cccc(Cl)c3)CC2)C(=O)Nc2ccccc21 10.1021/jm070279v
24854187 96280 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometryDisplacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometry
ChEMBL 395 7 1 3 4.4 CCC1(CCCCN2CCN(c3ccc(F)cc3)CC2)C(=O)Nc2ccccc21 10.1021/jm200547z
CHEMBL260872 96280 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometryDisplacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometry
ChEMBL 395 7 1 3 4.4 CCC1(CCCCN2CCN(c3ccc(F)cc3)CC2)C(=O)Nc2ccccc21 10.1021/jm200547z
24854187 96280 None 0 Human Binding pKi = 9.4 9.4 - 1
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 395 7 1 3 4.4 CCC1(CCCCN2CCN(c3ccc(F)cc3)CC2)C(=O)Nc2ccccc21 10.1021/jm070279v
CHEMBL260872 96280 None 0 Human Binding pKi = 9.4 9.4 - 1
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 395 7 1 3 4.4 CCC1(CCCCN2CCN(c3ccc(F)cc3)CC2)C(=O)Nc2ccccc21 10.1021/jm070279v
132578545 154648 None 0 Human Binding pKi = 9.3 9.3 33 9
Displacement of [3H]-LSD from human 5-HT7 receptor by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT7 receptor by liquid scintillation counting method
ChEMBL 325 3 0 2 4.1 O=C1c2ccc(Cl)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
CHEMBL3898250 154648 None 0 Human Binding pKi = 9.3 9.3 33 9
Displacement of [3H]-LSD from human 5-HT7 receptor by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT7 receptor by liquid scintillation counting method
ChEMBL 325 3 0 2 4.1 O=C1c2ccc(Cl)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
CHEMBL3991133 154648 None 0 Human Binding pKi = 9.3 9.3 33 9
Displacement of [3H]-LSD from human 5-HT7 receptor by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT7 receptor by liquid scintillation counting method
ChEMBL 325 3 0 2 4.1 O=C1c2ccc(Cl)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
25192947 164761 None 0 Human Binding pKi = 9.3 9.3 - 1
Antagonist activity at 5-HT7 receptor (unknown origin)Antagonist activity at 5-HT7 receptor (unknown origin)
ChEMBL 273 4 1 4 2.5 Cc1nn(C)c(C)c1-c1ccc(O)c(CCN(C)C)c1 10.1016/j.ejmech.2019.111705
CHEMBL4216782 164761 None 0 Human Binding pKi = 9.3 9.3 - 1
Antagonist activity at 5-HT7 receptor (unknown origin)Antagonist activity at 5-HT7 receptor (unknown origin)
ChEMBL 273 4 1 4 2.5 Cc1nn(C)c(C)c1-c1ccc(O)c(CCN(C)C)c1 10.1016/j.ejmech.2019.111705
25192947 164761 None 0 Human Binding pKi = 9.3 9.3 - 1
Binding affinity to 5-HT7 receptor (unknown origin)Binding affinity to 5-HT7 receptor (unknown origin)
ChEMBL 273 4 1 4 2.5 Cc1nn(C)c(C)c1-c1ccc(O)c(CCN(C)C)c1 10.1021/acs.jmedchem.7b01898
CHEMBL4216782 164761 None 0 Human Binding pKi = 9.3 9.3 - 1
Binding affinity to 5-HT7 receptor (unknown origin)Binding affinity to 5-HT7 receptor (unknown origin)
ChEMBL 273 4 1 4 2.5 Cc1nn(C)c(C)c1-c1ccc(O)c(CCN(C)C)c1 10.1021/acs.jmedchem.7b01898
1809 134 None 25 Human Binding pKi = 9.3 9.3 -7 37
Binding affinity to human recombinant 5-hydroxytryptamine 7 receptor in mammalian cells using [3H]5-CT as radioligandBinding affinity to human recombinant 5-hydroxytryptamine 7 receptor in mammalian cells using [3H]5-CT as radioligand
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm0104264
4 134 None 25 Human Binding pKi = 9.3 9.3 -7 37
Binding affinity to human recombinant 5-hydroxytryptamine 7 receptor in mammalian cells using [3H]5-CT as radioligandBinding affinity to human recombinant 5-hydroxytryptamine 7 receptor in mammalian cells using [3H]5-CT as radioligand
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm0104264
CHEMBL18840 134 None 25 Human Binding pKi = 9.3 9.3 -7 37
Binding affinity to human recombinant 5-hydroxytryptamine 7 receptor in mammalian cells using [3H]5-CT as radioligandBinding affinity to human recombinant 5-hydroxytryptamine 7 receptor in mammalian cells using [3H]5-CT as radioligand
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm0104264
11653869 96346 None 0 Human Binding pKi = 9.3 9.3 134 2
Displacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometryDisplacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometry
ChEMBL 383 6 1 3 4.4 O=C1Nc2ccccc2C1CCCCN1CCN(c2cccc(Cl)c2)CC1 10.1021/jm200547z
CHEMBL261209 96346 None 0 Human Binding pKi = 9.3 9.3 134 2
Displacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometryDisplacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometry
ChEMBL 383 6 1 3 4.4 O=C1Nc2ccccc2C1CCCCN1CCN(c2cccc(Cl)c2)CC1 10.1021/jm200547z
11653869 96346 None 0 Human Binding pKi = 9.3 9.3 134 2
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 383 6 1 3 4.4 O=C1Nc2ccccc2C1CCCCN1CCN(c2cccc(Cl)c2)CC1 10.1021/jm070279v
CHEMBL261209 96346 None 0 Human Binding pKi = 9.3 9.3 134 2
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 383 6 1 3 4.4 O=C1Nc2ccccc2C1CCCCN1CCN(c2cccc(Cl)c2)CC1 10.1021/jm070279v
16362 3125 None 49 Rat Binding pKi = 9.3 9.3 -5 29
Binding affinity towards rat 5-hydroxytryptamine 7 receptorBinding affinity towards rat 5-hydroxytryptamine 7 receptor
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1021/jm030030n
16362.0 3125 None 49 Rat Binding pKi = 9.3 9.3 -5 29
Binding affinity towards rat 5-hydroxytryptamine 7 receptorBinding affinity towards rat 5-hydroxytryptamine 7 receptor
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1021/jm030030n
2172 3125 None 49 Rat Binding pKi = 9.3 9.3 -5 29
Binding affinity towards rat 5-hydroxytryptamine 7 receptorBinding affinity towards rat 5-hydroxytryptamine 7 receptor
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1021/jm030030n
90 3125 None 49 Rat Binding pKi = 9.3 9.3 -5 29
Binding affinity towards rat 5-hydroxytryptamine 7 receptorBinding affinity towards rat 5-hydroxytryptamine 7 receptor
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1021/jm030030n
CHEMBL1423 3125 None 49 Rat Binding pKi = 9.3 9.3 -5 29
Binding affinity towards rat 5-hydroxytryptamine 7 receptorBinding affinity towards rat 5-hydroxytryptamine 7 receptor
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1021/jm030030n
DB01100 3125 None 49 Rat Binding pKi = 9.3 9.3 -5 29
Binding affinity towards rat 5-hydroxytryptamine 7 receptorBinding affinity towards rat 5-hydroxytryptamine 7 receptor
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1021/jm030030n
213046 2385 None 44 Human Binding pKi = 9.3 9.3 2 8
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1016/j.ejmech.2019.111736
213046.0 2385 None 44 Human Binding pKi = 9.3 9.3 2 8
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1016/j.ejmech.2019.111736
4168 2385 None 44 Human Binding pKi = 9.3 9.3 2 8
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1016/j.ejmech.2019.111736
7461 2385 None 44 Human Binding pKi = 9.3 9.3 2 8
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1016/j.ejmech.2019.111736
CHEMBL1237021 2385 None 44 Human Binding pKi = 9.3 9.3 2 8
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1016/j.ejmech.2019.111736
DB08815 2385 None 44 Human Binding pKi = 9.3 9.3 2 8
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1016/j.ejmech.2019.111736
213046 2385 None 44 Human Binding pKi = 9.3 9.3 2 8
Displacement of [3H]-5-CT from human recombinant 5HT7b receptor measured after 2 hrsDisplacement of [3H]-5-CT from human recombinant 5HT7b receptor measured after 2 hrs
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1016/j.bmc.2020.115459
213046.0 2385 None 44 Human Binding pKi = 9.3 9.3 2 8
Displacement of [3H]-5-CT from human recombinant 5HT7b receptor measured after 2 hrsDisplacement of [3H]-5-CT from human recombinant 5HT7b receptor measured after 2 hrs
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1016/j.bmc.2020.115459
4168 2385 None 44 Human Binding pKi = 9.3 9.3 2 8
Displacement of [3H]-5-CT from human recombinant 5HT7b receptor measured after 2 hrsDisplacement of [3H]-5-CT from human recombinant 5HT7b receptor measured after 2 hrs
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1016/j.bmc.2020.115459
7461 2385 None 44 Human Binding pKi = 9.3 9.3 2 8
Displacement of [3H]-5-CT from human recombinant 5HT7b receptor measured after 2 hrsDisplacement of [3H]-5-CT from human recombinant 5HT7b receptor measured after 2 hrs
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1016/j.bmc.2020.115459
CHEMBL1237021 2385 None 44 Human Binding pKi = 9.3 9.3 2 8
Displacement of [3H]-5-CT from human recombinant 5HT7b receptor measured after 2 hrsDisplacement of [3H]-5-CT from human recombinant 5HT7b receptor measured after 2 hrs
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1016/j.bmc.2020.115459
DB08815 2385 None 44 Human Binding pKi = 9.3 9.3 2 8
Displacement of [3H]-5-CT from human recombinant 5HT7b receptor measured after 2 hrsDisplacement of [3H]-5-CT from human recombinant 5HT7b receptor measured after 2 hrs
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1016/j.bmc.2020.115459
132578545 154648 None 0 Human Binding pKi = 9.3 9.3 33 9
Displacement of [3H]-LSD from human 5-HT7 receptor by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT7 receptor by liquid scintillation counting method
ChEMBL 325 3 0 2 4.1 O=C1c2ccc(Cl)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
CHEMBL3898250 154648 None 0 Human Binding pKi = 9.3 9.3 33 9
Displacement of [3H]-LSD from human 5-HT7 receptor by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT7 receptor by liquid scintillation counting method
ChEMBL 325 3 0 2 4.1 O=C1c2ccc(Cl)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
CHEMBL3991133 154648 None 0 Human Binding pKi = 9.3 9.3 33 9
Displacement of [3H]-LSD from human 5-HT7 receptor by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT7 receptor by liquid scintillation counting method
ChEMBL 325 3 0 2 4.1 O=C1c2ccc(Cl)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
66801167 112172 None 0 Human Binding pKi = 9.3 9.3 3 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 467 7 1 5 4.7 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cccc2ccccc12 10.1021/jm401895u
CHEMBL3290002 112172 None 0 Human Binding pKi = 9.3 9.3 3 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 467 7 1 5 4.7 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cccc2ccccc12 10.1021/jm401895u
1809 134 None 25 Rat Binding pKi = 9.3 9.3 -2 37
Displacement of [3H]LSD from rat cloned 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from rat cloned 5HT7 receptor expressed in HEK293 cells
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm800615e
4 134 None 25 Rat Binding pKi = 9.3 9.3 -2 37
Displacement of [3H]LSD from rat cloned 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from rat cloned 5HT7 receptor expressed in HEK293 cells
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm800615e
CHEMBL18840 134 None 25 Rat Binding pKi = 9.3 9.3 -2 37
Displacement of [3H]LSD from rat cloned 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from rat cloned 5HT7 receptor expressed in HEK293 cells
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm800615e
1809 134 None 25 Rat Binding pKi = 9.3 9.3 -2 37
Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm070487n
4 134 None 25 Rat Binding pKi = 9.3 9.3 -2 37
Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm070487n
CHEMBL18840 134 None 25 Rat Binding pKi = 9.3 9.3 -2 37
Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm070487n
44340836 161828 None 0 Human Binding pKi = 9.3 9.3 60 2
Binding affinity for human cloned 5-hydroxytryptamine 7 receptor in HEK 293 using [3H]5-CT as a radioligandBinding affinity for human cloned 5-hydroxytryptamine 7 receptor in HEK 293 using [3H]5-CT as a radioligand
ChEMBL 471 7 1 4 4.4 O=S(=O)(c1ccc2cc[nH]c2c1)N1CCC[C@@H]1CCN1CCC(Oc2ccc(F)cc2)CC1 10.1016/s0960-894x(02)00690-x
CHEMBL413707 161828 None 0 Human Binding pKi = 9.3 9.3 60 2
Binding affinity for human cloned 5-hydroxytryptamine 7 receptor in HEK 293 using [3H]5-CT as a radioligandBinding affinity for human cloned 5-hydroxytryptamine 7 receptor in HEK 293 using [3H]5-CT as a radioligand
ChEMBL 471 7 1 4 4.4 O=S(=O)(c1ccc2cc[nH]c2c1)N1CCC[C@@H]1CCN1CCC(Oc2ccc(F)cc2)CC1 10.1016/s0960-894x(02)00690-x
1809 134 None 25 Rat Binding pKi = 9.3 9.3 -2 37
Binding affinity to the rat 5-hydroxytryptamine 7 receptorBinding affinity to the rat 5-hydroxytryptamine 7 receptor
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm020994z
4 134 None 25 Rat Binding pKi = 9.3 9.3 -2 37
Binding affinity to the rat 5-hydroxytryptamine 7 receptorBinding affinity to the rat 5-hydroxytryptamine 7 receptor
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm020994z
CHEMBL18840 134 None 25 Rat Binding pKi = 9.3 9.3 -2 37
Binding affinity to the rat 5-hydroxytryptamine 7 receptorBinding affinity to the rat 5-hydroxytryptamine 7 receptor
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm020994z
1809 134 None 25 Rat Binding pKi = 9.3 9.3 -2 37
Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1016/j.bmc.2007.05.010
1809 134 None 25 Rat Binding pKi = 9.3 9.3 -2 37
Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm049702f
4 134 None 25 Rat Binding pKi = 9.3 9.3 -2 37
Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1016/j.bmc.2007.05.010
4 134 None 25 Rat Binding pKi = 9.3 9.3 -2 37
Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm049702f
CHEMBL18840 134 None 25 Rat Binding pKi = 9.3 9.3 -2 37
Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1016/j.bmc.2007.05.010
CHEMBL18840 134 None 25 Rat Binding pKi = 9.3 9.3 -2 37
Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm049702f
4106 2502 None 21 Human Binding pKi = 9.3 9.3 -4 33
Displacement of [3H]-LSD from recombinant human 5HT7 receptor expressed in CHOK1 cell membranes measured after 120 mins by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT7 receptor expressed in CHOK1 cell membranes measured after 120 mins by microbeta counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2020.112149
5358812 2502 None 21 Human Binding pKi = 9.3 9.3 -4 33
Displacement of [3H]-LSD from recombinant human 5HT7 receptor expressed in CHOK1 cell membranes measured after 120 mins by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT7 receptor expressed in CHOK1 cell membranes measured after 120 mins by microbeta counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2020.112149
89 2502 None 21 Human Binding pKi = 9.3 9.3 -4 33
Displacement of [3H]-LSD from recombinant human 5HT7 receptor expressed in CHOK1 cell membranes measured after 120 mins by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT7 receptor expressed in CHOK1 cell membranes measured after 120 mins by microbeta counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2020.112149
CHEMBL93240 2502 None 21 Human Binding pKi = 9.3 9.3 -4 33
Displacement of [3H]-LSD from recombinant human 5HT7 receptor expressed in CHOK1 cell membranes measured after 120 mins by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT7 receptor expressed in CHOK1 cell membranes measured after 120 mins by microbeta counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2020.112149
145983405 166533 None 0 Human Binding pKi = 9.3 9.3 32 2
Displacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cell membranes after 120 mins by TopCount scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cell membranes after 120 mins by TopCount scintillation counting method
ChEMBL 449 6 1 2 6.0 Fc1cccc(-c2c(F)cccc2N2CCN(CCCc3c[nH]c4ccc(F)cc34)CC2)c1 10.1016/j.ejmech.2017.12.063
CHEMBL4277476 166533 None 0 Human Binding pKi = 9.3 9.3 32 2
Displacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cell membranes after 120 mins by TopCount scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cell membranes after 120 mins by TopCount scintillation counting method
ChEMBL 449 6 1 2 6.0 Fc1cccc(-c2c(F)cccc2N2CCN(CCCc3c[nH]c4ccc(F)cc34)CC2)c1 10.1016/j.ejmech.2017.12.063
44266221 210825 None 0 Human Binding pKi = 9.3 9.3 12 2
Binding affinity at human cloned 5-hydroxytryptamine 7 receptor.Binding affinity at human cloned 5-hydroxytryptamine 7 receptor.
ChEMBL 405 4 0 3 4.5 O=C1c2ccccc2CCCN1CCN1CCC(n2ccc3cc(F)ccc32)CC1 10.1016/s0960-894x(03)00077-5
CHEMBL9951 210825 None 0 Human Binding pKi = 9.3 9.3 12 2
Binding affinity at human cloned 5-hydroxytryptamine 7 receptor.Binding affinity at human cloned 5-hydroxytryptamine 7 receptor.
ChEMBL 405 4 0 3 4.5 O=C1c2ccccc2CCCN1CCN1CCC(n2ccc3cc(F)ccc32)CC1 10.1016/s0960-894x(03)00077-5
4106 2502 None 21 Human Binding pKi = 9.3 9.3 -4 33
Displacement of [3H]-LSD from human 5-HT7 receptor transfected in CHO-K1 cells measured after 120 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT7 receptor transfected in CHO-K1 cells measured after 120 mins by scintillation counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/acs.jmedchem.1c00497
5358812 2502 None 21 Human Binding pKi = 9.3 9.3 -4 33
Displacement of [3H]-LSD from human 5-HT7 receptor transfected in CHO-K1 cells measured after 120 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT7 receptor transfected in CHO-K1 cells measured after 120 mins by scintillation counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/acs.jmedchem.1c00497
89 2502 None 21 Human Binding pKi = 9.3 9.3 -4 33
Displacement of [3H]-LSD from human 5-HT7 receptor transfected in CHO-K1 cells measured after 120 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT7 receptor transfected in CHO-K1 cells measured after 120 mins by scintillation counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/acs.jmedchem.1c00497
CHEMBL93240 2502 None 21 Human Binding pKi = 9.3 9.3 -4 33
Displacement of [3H]-LSD from human 5-HT7 receptor transfected in CHO-K1 cells measured after 120 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT7 receptor transfected in CHO-K1 cells measured after 120 mins by scintillation counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/acs.jmedchem.1c00497
25107716 2351 None 38 Rat Binding pKi = 9.2 9.2 3 7
Binding affinity to rat 5HT7 receptorBinding affinity to rat 5HT7 receptor
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1016/j.bmc.2014.01.016
8436 2351 None 38 Rat Binding pKi = 9.2 9.2 3 7
Binding affinity to rat 5HT7 receptorBinding affinity to rat 5HT7 receptor
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1016/j.bmc.2014.01.016
CHEMBL522691 2351 None 38 Rat Binding pKi = 9.2 9.2 3 7
Binding affinity to rat 5HT7 receptorBinding affinity to rat 5HT7 receptor
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1016/j.bmc.2014.01.016
25107716 2351 None 38 Rat Binding pKi = 9.2 9.2 3 7
Binding affinity to rat cloned 5HT7 receptorBinding affinity to rat cloned 5HT7 receptor
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1021/jm3003679
8436 2351 None 38 Rat Binding pKi = 9.2 9.2 3 7
Binding affinity to rat cloned 5HT7 receptorBinding affinity to rat cloned 5HT7 receptor
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1021/jm3003679
CHEMBL522691 2351 None 38 Rat Binding pKi = 9.2 9.2 3 7
Binding affinity to rat cloned 5HT7 receptorBinding affinity to rat cloned 5HT7 receptor
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1021/jm3003679
25107716 2351 None 38 Human Binding pKi = 9.2 9.2 -3 7
Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-countingDisplacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-counting
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1016/j.ejmech.2014.03.005
8436 2351 None 38 Human Binding pKi = 9.2 9.2 -3 7
Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-countingDisplacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-counting
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1016/j.ejmech.2014.03.005
CHEMBL522691 2351 None 38 Human Binding pKi = 9.2 9.2 -3 7
Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-countingDisplacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-counting
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1016/j.ejmech.2014.03.005
25107716 2351 None 38 Human Binding pKi = 9.2 9.2 -3 7
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1016/j.ejmech.2012.07.043
8436 2351 None 38 Human Binding pKi = 9.2 9.2 -3 7
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1016/j.ejmech.2012.07.043
CHEMBL522691 2351 None 38 Human Binding pKi = 9.2 9.2 -3 7
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1016/j.ejmech.2012.07.043
25107716 2351 None 38 Rat Binding pKi = 9.2 9.2 3 7
Displacement of [3H]LSD from rat cloned 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from rat cloned 5HT7 receptor expressed in HEK293 cells
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1021/jm800615e
8436 2351 None 38 Rat Binding pKi = 9.2 9.2 3 7
Displacement of [3H]LSD from rat cloned 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from rat cloned 5HT7 receptor expressed in HEK293 cells
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1021/jm800615e
CHEMBL522691 2351 None 38 Rat Binding pKi = 9.2 9.2 3 7
Displacement of [3H]LSD from rat cloned 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from rat cloned 5HT7 receptor expressed in HEK293 cells
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1021/jm800615e
23642275 482 None 26 Human Binding pKi = 9.2 9.2 3 8
Antagonist activity at 5-HT7 receptor (unknown origin)Antagonist activity at 5-HT7 receptor (unknown origin)
ChEMBL 283 2 0 3 3.1 CN([C@H]1CCc2c(C1)cccc2c1c(C)nn(c1C)C)C 10.1016/j.ejmech.2019.111705
8433 482 None 26 Human Binding pKi = 9.2 9.2 3 8
Antagonist activity at 5-HT7 receptor (unknown origin)Antagonist activity at 5-HT7 receptor (unknown origin)
ChEMBL 283 2 0 3 3.1 CN([C@H]1CCc2c(C1)cccc2c1c(C)nn(c1C)C)C 10.1016/j.ejmech.2019.111705
CHEMBL2164327 482 None 26 Human Binding pKi = 9.2 9.2 3 8
Antagonist activity at 5-HT7 receptor (unknown origin)Antagonist activity at 5-HT7 receptor (unknown origin)
ChEMBL 283 2 0 3 3.1 CN([C@H]1CCc2c(C1)cccc2c1c(C)nn(c1C)C)C 10.1016/j.ejmech.2019.111705
9881600 55213 None 7 Human Binding pKi = 9.2 9.2 8 5
Antagonist activity at 5-HT7 receptor (unknown origin)Antagonist activity at 5-HT7 receptor (unknown origin)
ChEMBL 258 5 0 3 3.4 CN(C)CCSc1cccc(-c2ccccc2)n1 10.1016/j.ejmech.2019.111705
CHEMBL161765 55213 None 7 Human Binding pKi = 9.2 9.2 8 5
Antagonist activity at 5-HT7 receptor (unknown origin)Antagonist activity at 5-HT7 receptor (unknown origin)
ChEMBL 258 5 0 3 3.4 CN(C)CCSc1cccc(-c2ccccc2)n1 10.1016/j.ejmech.2019.111705
44393180 66686 None 0 Human Binding pKi = 9.2 9.2 - 1
Binding affinity against 5-Hydroxy tryptamine 7 receptorBinding affinity against 5-Hydroxy tryptamine 7 receptor
ChEMBL 318 7 2 4 4.3 C[C@H](Nc1ccnc(NCCc2ccccc2)n1)c1ccccc1 10.1016/j.bmcl.2004.06.007
CHEMBL185384 66686 None 0 Human Binding pKi = 9.2 9.2 - 1
Binding affinity against 5-Hydroxy tryptamine 7 receptorBinding affinity against 5-Hydroxy tryptamine 7 receptor
ChEMBL 318 7 2 4 4.3 C[C@H](Nc1ccnc(NCCc2ccccc2)n1)c1ccccc1 10.1016/j.bmcl.2004.06.007
23642275 482 None 26 Human Binding pKi = 9.2 9.2 3 8
Binding affinity to 5-HT7 receptor (unknown origin)Binding affinity to 5-HT7 receptor (unknown origin)
ChEMBL 283 2 0 3 3.1 CN([C@H]1CCc2c(C1)cccc2c1c(C)nn(c1C)C)C 10.1021/acs.jmedchem.7b01898
8433 482 None 26 Human Binding pKi = 9.2 9.2 3 8
Binding affinity to 5-HT7 receptor (unknown origin)Binding affinity to 5-HT7 receptor (unknown origin)
ChEMBL 283 2 0 3 3.1 CN([C@H]1CCc2c(C1)cccc2c1c(C)nn(c1C)C)C 10.1021/acs.jmedchem.7b01898
CHEMBL2164327 482 None 26 Human Binding pKi = 9.2 9.2 3 8
Binding affinity to 5-HT7 receptor (unknown origin)Binding affinity to 5-HT7 receptor (unknown origin)
ChEMBL 283 2 0 3 3.1 CN([C@H]1CCc2c(C1)cccc2c1c(C)nn(c1C)C)C 10.1021/acs.jmedchem.7b01898
9881600 55213 None 7 Human Binding pKi = 9.2 9.2 8 5
Binding affinity to 5HT7 receptor (unknown origin) assessed as inhibitory constantBinding affinity to 5HT7 receptor (unknown origin) assessed as inhibitory constant
ChEMBL 258 5 0 3 3.4 CN(C)CCSc1cccc(-c2ccccc2)n1 10.1016/j.ejmech.2019.111690
CHEMBL161765 55213 None 7 Human Binding pKi = 9.2 9.2 8 5
Binding affinity to 5HT7 receptor (unknown origin) assessed as inhibitory constantBinding affinity to 5HT7 receptor (unknown origin) assessed as inhibitory constant
ChEMBL 258 5 0 3 3.4 CN(C)CCSc1cccc(-c2ccccc2)n1 10.1016/j.ejmech.2019.111690
23642275 482 None 26 Human Binding pKi = 9.2 9.2 3 8
Binding affinity to human 5HT7 receptor expressed in HEK-293F cellsBinding affinity to human 5HT7 receptor expressed in HEK-293F cells
ChEMBL 283 2 0 3 3.1 CN([C@H]1CCc2c(C1)cccc2c1c(C)nn(c1C)C)C 10.1016/j.bmc.2013.02.038
8433 482 None 26 Human Binding pKi = 9.2 9.2 3 8
Binding affinity to human 5HT7 receptor expressed in HEK-293F cellsBinding affinity to human 5HT7 receptor expressed in HEK-293F cells
ChEMBL 283 2 0 3 3.1 CN([C@H]1CCc2c(C1)cccc2c1c(C)nn(c1C)C)C 10.1016/j.bmc.2013.02.038
CHEMBL2164327 482 None 26 Human Binding pKi = 9.2 9.2 3 8
Binding affinity to human 5HT7 receptor expressed in HEK-293F cellsBinding affinity to human 5HT7 receptor expressed in HEK-293F cells
ChEMBL 283 2 0 3 3.1 CN([C@H]1CCc2c(C1)cccc2c1c(C)nn(c1C)C)C 10.1016/j.bmc.2013.02.038
9881600 55213 None 7 Human Binding pKi = 9.2 9.2 8 5
Binding affinity towards human 5-hydroxytryptamine 7 receptor by the displacement of [3H]-5-HT radioligand from the cloned receptor expressed in CHO cellsBinding affinity towards human 5-hydroxytryptamine 7 receptor by the displacement of [3H]-5-HT radioligand from the cloned receptor expressed in CHO cells
ChEMBL 258 5 0 3 3.4 CN(C)CCSc1cccc(-c2ccccc2)n1 10.1016/j.bmcl.2003.11.050
CHEMBL161765 55213 None 7 Human Binding pKi = 9.2 9.2 8 5
Binding affinity towards human 5-hydroxytryptamine 7 receptor by the displacement of [3H]-5-HT radioligand from the cloned receptor expressed in CHO cellsBinding affinity towards human 5-hydroxytryptamine 7 receptor by the displacement of [3H]-5-HT radioligand from the cloned receptor expressed in CHO cells
ChEMBL 258 5 0 3 3.4 CN(C)CCSc1cccc(-c2ccccc2)n1 10.1016/j.bmcl.2003.11.050
66803474 156407 None 0 Human Binding pKi = 9.2 9.2 3 4
Displacement of [3H]-LSD from human 5-HT7 receptor expressed in CHO-K1 cell membranes after 120 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT7 receptor expressed in CHO-K1 cell membranes after 120 mins by scintillation counting
ChEMBL 429 6 2 3 4.2 Cc1cccc(S(=O)(=O)NCCN2CC=C(c3c[nH]c4ccc(Cl)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4065568 156407 None 0 Human Binding pKi = 9.2 9.2 3 4
Displacement of [3H]-LSD from human 5-HT7 receptor expressed in CHO-K1 cell membranes after 120 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT7 receptor expressed in CHO-K1 cell membranes after 120 mins by scintillation counting
ChEMBL 429 6 2 3 4.2 Cc1cccc(S(=O)(=O)NCCN2CC=C(c3c[nH]c4ccc(Cl)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
11681111 120648 None 0 Human Binding pKi = 9.2 9.2 7 2
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cells
ChEMBL 309 3 2 2 2.4 CCC1(OC)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
CHEMBL3343666 120648 None 0 Human Binding pKi = 9.2 9.2 7 2
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cells
ChEMBL 309 3 2 2 2.4 CCC1(OC)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
CHEMBL3545815 120648 None 0 Human Binding pKi = 9.2 9.2 7 2
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cells
ChEMBL 309 3 2 2 2.4 CCC1(OC)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
4431 2729 None 18 Human Binding pKi = 9.2 9.2 -20 12
Displacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry
ChEMBL 393 7 0 5 2.9 COc1ccccc1N1CCN(CC1)CCCCN1C(=O)c2c(C1=O)cccc2 10.1016/j.ejmech.2014.08.023
73 2729 None 18 Human Binding pKi = 9.2 9.2 -20 12
Displacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry
ChEMBL 393 7 0 5 2.9 COc1ccccc1N1CCN(CC1)CCCCN1C(=O)c2c(C1=O)cccc2 10.1016/j.ejmech.2014.08.023
CHEMBL8618 2729 None 18 Human Binding pKi = 9.2 9.2 -20 12
Displacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry
ChEMBL 393 7 0 5 2.9 COc1ccccc1N1CCN(CC1)CCCCN1C(=O)c2c(C1=O)cccc2 10.1016/j.ejmech.2014.08.023
9881600 55213 None 7 Human Binding pKi = 9.2 9.2 8 5
Displacement of [3H]5CT from 5HT7B receptorDisplacement of [3H]5CT from 5HT7B receptor
ChEMBL 258 5 0 3 3.4 CN(C)CCSc1cccc(-c2ccccc2)n1 10.1016/j.bmc.2010.01.035
CHEMBL161765 55213 None 7 Human Binding pKi = 9.2 9.2 8 5
Displacement of [3H]5CT from 5HT7B receptorDisplacement of [3H]5CT from 5HT7B receptor
ChEMBL 258 5 0 3 3.4 CN(C)CCSc1cccc(-c2ccccc2)n1 10.1016/j.bmc.2010.01.035
24854371 95928 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometryDisplacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometry
ChEMBL 445 7 1 3 5.6 CCC1(CCCCN2CCN(c3ccc(Cl)c(Cl)c3)CC2)C(=O)Nc2ccccc21 10.1021/jm200547z
CHEMBL259087 95928 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometryDisplacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometry
ChEMBL 445 7 1 3 5.6 CCC1(CCCCN2CCN(c3ccc(Cl)c(Cl)c3)CC2)C(=O)Nc2ccccc21 10.1021/jm200547z
23642275 482 None 26 Human Binding pKi = 9.2 9.2 3 8
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 283 2 0 3 3.1 CN([C@H]1CCc2c(C1)cccc2c1c(C)nn(c1C)C)C 10.1039/C8MD00313K
8433 482 None 26 Human Binding pKi = 9.2 9.2 3 8
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 283 2 0 3 3.1 CN([C@H]1CCc2c(C1)cccc2c1c(C)nn(c1C)C)C 10.1039/C8MD00313K
CHEMBL2164327 482 None 26 Human Binding pKi = 9.2 9.2 3 8
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 283 2 0 3 3.1 CN([C@H]1CCc2c(C1)cccc2c1c(C)nn(c1C)C)C 10.1039/C8MD00313K
56933434 112160 None 0 Human Binding pKi = 9.2 9.2 6 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 431 7 1 5 3.8 Cc1cccc(S(=O)(=O)NCCCN2CCC(c3noc4cc(F)ccc34)CC2)c1 10.1021/jm401895u
CHEMBL3289991 112160 None 0 Human Binding pKi = 9.2 9.2 6 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 431 7 1 5 3.8 Cc1cccc(S(=O)(=O)NCCCN2CCC(c3noc4cc(F)ccc34)CC2)c1 10.1021/jm401895u
25107716 2351 None 38 Human Binding pKi = 9.2 9.2 -3 7
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysis
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1039/C8MD00313K
8436 2351 None 38 Human Binding pKi = 9.2 9.2 -3 7
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysis
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1039/C8MD00313K
CHEMBL522691 2351 None 38 Human Binding pKi = 9.2 9.2 -3 7
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysis
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1039/C8MD00313K
24853955 156284 None 0 Human Binding pKi = 9.2 9.2 - 1
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 429 7 1 3 5.1 CCC1(CCCCN2CCN(c3ccc(F)c(Cl)c3)CC2)C(=O)Nc2ccccc21 10.1021/jm070279v
CHEMBL406414 156284 None 0 Human Binding pKi = 9.2 9.2 - 1
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 429 7 1 3 5.1 CCC1(CCCCN2CCN(c3ccc(F)c(Cl)c3)CC2)C(=O)Nc2ccccc21 10.1021/jm070279v
5 139 None 45 Rat Binding pKi = 9.2 9.2 -5 54
Binding affinity at rat 5-hydroxytryptamine 7 receptor.Binding affinity at rat 5-hydroxytryptamine 7 receptor.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030826m
5202 139 None 45 Rat Binding pKi = 9.2 9.2 -5 54
Binding affinity at rat 5-hydroxytryptamine 7 receptor.Binding affinity at rat 5-hydroxytryptamine 7 receptor.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030826m
CHEMBL39 139 None 45 Rat Binding pKi = 9.2 9.2 -5 54
Binding affinity at rat 5-hydroxytryptamine 7 receptor.Binding affinity at rat 5-hydroxytryptamine 7 receptor.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030826m
DB08839 139 None 45 Rat Binding pKi = 9.2 9.2 -5 54
Binding affinity at rat 5-hydroxytryptamine 7 receptor.Binding affinity at rat 5-hydroxytryptamine 7 receptor.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030826m
44437334 150586 None 0 Rat Binding pKi = 9.2 9.2 - 1
Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells at 10 uMDisplacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells at 10 uM
ChEMBL 694 18 0 9 5.9 COc1ccccc1N1CCN(CCc2cccc(OCCOCCOc3cccc(CCN4CCN(c5ccccc5OC)CC4)c3)c2)CC1 10.1016/j.bmc.2007.05.010
CHEMBL395444 150586 None 0 Rat Binding pKi = 9.2 9.2 - 1
Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells at 10 uMDisplacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells at 10 uM
ChEMBL 694 18 0 9 5.9 COc1ccccc1N1CCN(CCc2cccc(OCCOCCOc3cccc(CCN4CCN(c5ccccc5OC)CC4)c3)c2)CC1 10.1016/j.bmc.2007.05.010
24854371 95928 None 0 Human Binding pKi = 9.2 9.2 - 1
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 445 7 1 3 5.6 CCC1(CCCCN2CCN(c3ccc(Cl)c(Cl)c3)CC2)C(=O)Nc2ccccc21 10.1021/jm070279v
CHEMBL259087 95928 None 0 Human Binding pKi = 9.2 9.2 - 1
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 445 7 1 3 5.6 CCC1(CCCCN2CCN(c3ccc(Cl)c(Cl)c3)CC2)C(=O)Nc2ccccc21 10.1021/jm070279v
24854037 95927 None 0 Human Binding pKi = 9.2 9.2 - 1
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 425 7 1 3 5.2 CCC1(CCCCN2CCN(c3ccc(C)c(Cl)c3)CC2)C(=O)Nc2ccccc21 10.1021/jm070279v
CHEMBL259086 95927 None 0 Human Binding pKi = 9.2 9.2 - 1
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 425 7 1 3 5.2 CCC1(CCCCN2CCN(c3ccc(C)c(Cl)c3)CC2)C(=O)Nc2ccccc21 10.1021/jm070279v
24854041 96032 None 0 Human Binding pKi = 9.2 9.2 - 1
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 429 7 1 3 5.1 CCC1(CCCCN2CCN(c3cccc(Cl)c3)CC2)C(=O)Nc2cc(F)ccc21 10.1021/jm070279v
CHEMBL259549 96032 None 0 Human Binding pKi = 9.2 9.2 - 1
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 429 7 1 3 5.1 CCC1(CCCCN2CCN(c3cccc(Cl)c3)CC2)C(=O)Nc2cc(F)ccc21 10.1021/jm070279v
9934709 167927 None 0 Human Binding pKi = 9.2 9.2 1 2
Binding affinity for human cloned 5-hydroxytryptamine 7 receptor in HEK 293 using [3H]5-CT as a radioligandBinding affinity for human cloned 5-hydroxytryptamine 7 receptor in HEK 293 using [3H]5-CT as a radioligand
ChEMBL 476 6 2 3 5.1 O=S(=O)(c1ccc2cc[nH]c2c1)N1CCC[C@@H]1CCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(02)00690-x
CHEMBL430706 167927 None 0 Human Binding pKi = 9.2 9.2 1 2
Binding affinity for human cloned 5-hydroxytryptamine 7 receptor in HEK 293 using [3H]5-CT as a radioligandBinding affinity for human cloned 5-hydroxytryptamine 7 receptor in HEK 293 using [3H]5-CT as a radioligand
ChEMBL 476 6 2 3 5.1 O=S(=O)(c1ccc2cc[nH]c2c1)N1CCC[C@@H]1CCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(02)00690-x
9934709 167927 None 0 Human Binding pKi = 9.2 9.2 1 2
Displacement of [3H]5CT from 5HT7 receptorDisplacement of [3H]5CT from 5HT7 receptor
ChEMBL 476 6 2 3 5.1 O=S(=O)(c1ccc2cc[nH]c2c1)N1CCC[C@@H]1CCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2010.03.012
CHEMBL430706 167927 None 0 Human Binding pKi = 9.2 9.2 1 2
Displacement of [3H]5CT from 5HT7 receptorDisplacement of [3H]5CT from 5HT7 receptor
ChEMBL 476 6 2 3 5.1 O=S(=O)(c1ccc2cc[nH]c2c1)N1CCC[C@@H]1CCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2010.03.012
102364516 113607 None 0 Human Binding pKi = 9.2 9.2 - 1
Antagonist activity at 5-HT7 receptor (unknown origin)Antagonist activity at 5-HT7 receptor (unknown origin)
ChEMBL 346 6 0 2 4.0 O=C1Cc2ccccc2N1CC/C=C/CCN1CCc2ccccc2C1 10.1016/j.ejmech.2019.111705
CHEMBL3321794 113607 None 0 Human Binding pKi = 9.2 9.2 - 1
Antagonist activity at 5-HT7 receptor (unknown origin)Antagonist activity at 5-HT7 receptor (unknown origin)
ChEMBL 346 6 0 2 4.0 O=C1Cc2ccccc2N1CC/C=C/CCN1CCc2ccccc2C1 10.1016/j.ejmech.2019.111705
10015688 51689 None 0 Human Binding pKi = 9.2 9.2 12 4
Binding affinity towards human 5-hydroxytryptamine 7 receptor by the displacement of [3H]-5-HT radioligand from the cloned receptor expressed in CHO cellsBinding affinity towards human 5-hydroxytryptamine 7 receptor by the displacement of [3H]-5-HT radioligand from the cloned receptor expressed in CHO cells
ChEMBL 264 5 0 3 3.8 CN(C)CCSc1cccc(C2CCCCC2)n1 10.1016/j.bmcl.2003.11.050
CHEMBL158402 51689 None 0 Human Binding pKi = 9.2 9.2 12 4
Binding affinity towards human 5-hydroxytryptamine 7 receptor by the displacement of [3H]-5-HT radioligand from the cloned receptor expressed in CHO cellsBinding affinity towards human 5-hydroxytryptamine 7 receptor by the displacement of [3H]-5-HT radioligand from the cloned receptor expressed in CHO cells
ChEMBL 264 5 0 3 3.8 CN(C)CCSc1cccc(C2CCCCC2)n1 10.1016/j.bmcl.2003.11.050
10015688 51689 None 0 Human Binding pKi = 9.2 9.2 12 4
Displacement of [3H]5CT from human cloned 5HT7B receptor expressed in HEK293 cellsDisplacement of [3H]5CT from human cloned 5HT7B receptor expressed in HEK293 cells
ChEMBL 264 5 0 3 3.8 CN(C)CCSc1cccc(C2CCCCC2)n1 10.1016/j.bmc.2010.01.035
CHEMBL158402 51689 None 0 Human Binding pKi = 9.2 9.2 12 4
Displacement of [3H]5CT from human cloned 5HT7B receptor expressed in HEK293 cellsDisplacement of [3H]5CT from human cloned 5HT7B receptor expressed in HEK293 cells
ChEMBL 264 5 0 3 3.8 CN(C)CCSc1cccc(C2CCCCC2)n1 10.1016/j.bmc.2010.01.035
102364516 113607 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [3H]LSD from human 5-HT7 expressed in HEK-293 cells after 120 mins by scintillation spectrometryDisplacement of [3H]LSD from human 5-HT7 expressed in HEK-293 cells after 120 mins by scintillation spectrometry
ChEMBL 346 6 0 2 4.0 O=C1Cc2ccccc2N1CC/C=C/CCN1CCc2ccccc2C1 10.1021/jm500880c
CHEMBL3321794 113607 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [3H]LSD from human 5-HT7 expressed in HEK-293 cells after 120 mins by scintillation spectrometryDisplacement of [3H]LSD from human 5-HT7 expressed in HEK-293 cells after 120 mins by scintillation spectrometry
ChEMBL 346 6 0 2 4.0 O=C1Cc2ccccc2N1CC/C=C/CCN1CCc2ccccc2C1 10.1021/jm500880c
66801263 112139 None 0 Human Binding pKi = 9.2 9.2 14 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 482 8 1 6 4.0 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm401895u
CHEMBL3289970 112139 None 0 Human Binding pKi = 9.2 9.2 14 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 482 8 1 6 4.0 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm401895u
66801210 112187 None 0 Human Binding pKi = 9.2 9.2 1 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 535 8 1 6 6.1 Cc1c(S(=O)(=O)NCCCCN2CCC(c3noc4cc(F)ccc34)CC2)sc2ccc(Cl)cc12 10.1021/jm401895u
CHEMBL3290017 112187 None 0 Human Binding pKi = 9.2 9.2 1 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 535 8 1 6 6.1 Cc1c(S(=O)(=O)NCCCCN2CCC(c3noc4cc(F)ccc34)CC2)sc2ccc(Cl)cc12 10.1021/jm401895u
44340854 10061 None 0 Human Binding pKi = 9.2 9.2 61 2
Binding affinity for human cloned 5-hydroxytryptamine 7 receptor in HEK 293 using [3H]5-CT as a radioligandBinding affinity for human cloned 5-hydroxytryptamine 7 receptor in HEK 293 using [3H]5-CT as a radioligand
ChEMBL 493 6 2 6 4.1 O=S(=O)(c1ccc2cc[nH]c2c1)N1CCC[C@@H]1CCN1CCC(n2c(O)nc3ccccc32)CC1 10.1016/s0960-894x(02)00690-x
CHEMBL115262 10061 None 0 Human Binding pKi = 9.2 9.2 61 2
Binding affinity for human cloned 5-hydroxytryptamine 7 receptor in HEK 293 using [3H]5-CT as a radioligandBinding affinity for human cloned 5-hydroxytryptamine 7 receptor in HEK 293 using [3H]5-CT as a radioligand
ChEMBL 493 6 2 6 4.1 O=S(=O)(c1ccc2cc[nH]c2c1)N1CCC[C@@H]1CCN1CCC(n2c(O)nc3ccccc32)CC1 10.1016/s0960-894x(02)00690-x
3233 3512 None 28 Human Binding pKi = 9.2 9.2 2 17
Displacement of [3H]-5-HT from human 5-HT7 receptor expressed in CHOK1 cell membranes after 30 mins by liquid scintillation spectrometryDisplacement of [3H]-5-HT from human 5-HT7 receptor expressed in CHOK1 cell membranes after 30 mins by liquid scintillation spectrometry
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmcl.2016.06.080
3247 3512 None 28 Human Binding pKi = 9.2 9.2 2 17
Displacement of [3H]-5-HT from human 5-HT7 receptor expressed in CHOK1 cell membranes after 30 mins by liquid scintillation spectrometryDisplacement of [3H]-5-HT from human 5-HT7 receptor expressed in CHOK1 cell membranes after 30 mins by liquid scintillation spectrometry
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmcl.2016.06.080
6604889 3512 None 28 Human Binding pKi = 9.2 9.2 2 17
Displacement of [3H]-5-HT from human 5-HT7 receptor expressed in CHOK1 cell membranes after 30 mins by liquid scintillation spectrometryDisplacement of [3H]-5-HT from human 5-HT7 receptor expressed in CHOK1 cell membranes after 30 mins by liquid scintillation spectrometry
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmcl.2016.06.080
CHEMBL282199 3512 None 28 Human Binding pKi = 9.2 9.2 2 17
Displacement of [3H]-5-HT from human 5-HT7 receptor expressed in CHOK1 cell membranes after 30 mins by liquid scintillation spectrometryDisplacement of [3H]-5-HT from human 5-HT7 receptor expressed in CHOK1 cell membranes after 30 mins by liquid scintillation spectrometry
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmcl.2016.06.080
DB13988 3512 None 28 Human Binding pKi = 9.2 9.2 2 17
Displacement of [3H]-5-HT from human 5-HT7 receptor expressed in CHOK1 cell membranes after 30 mins by liquid scintillation spectrometryDisplacement of [3H]-5-HT from human 5-HT7 receptor expressed in CHOK1 cell membranes after 30 mins by liquid scintillation spectrometry
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmcl.2016.06.080
3233 3512 None 28 Human Binding pKi = 9.2 9.2 2 17
Displacement of [3H]-5-HT from recombinant human 5-HT7A receptor expressed in CHOK1 cell membranes after 40 mins by liquid scintillation counting methodDisplacement of [3H]-5-HT from recombinant human 5-HT7A receptor expressed in CHOK1 cell membranes after 40 mins by liquid scintillation counting method
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2016.12.039
3247 3512 None 28 Human Binding pKi = 9.2 9.2 2 17
Displacement of [3H]-5-HT from recombinant human 5-HT7A receptor expressed in CHOK1 cell membranes after 40 mins by liquid scintillation counting methodDisplacement of [3H]-5-HT from recombinant human 5-HT7A receptor expressed in CHOK1 cell membranes after 40 mins by liquid scintillation counting method
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2016.12.039
6604889 3512 None 28 Human Binding pKi = 9.2 9.2 2 17
Displacement of [3H]-5-HT from recombinant human 5-HT7A receptor expressed in CHOK1 cell membranes after 40 mins by liquid scintillation counting methodDisplacement of [3H]-5-HT from recombinant human 5-HT7A receptor expressed in CHOK1 cell membranes after 40 mins by liquid scintillation counting method
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2016.12.039
CHEMBL282199 3512 None 28 Human Binding pKi = 9.2 9.2 2 17
Displacement of [3H]-5-HT from recombinant human 5-HT7A receptor expressed in CHOK1 cell membranes after 40 mins by liquid scintillation counting methodDisplacement of [3H]-5-HT from recombinant human 5-HT7A receptor expressed in CHOK1 cell membranes after 40 mins by liquid scintillation counting method
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2016.12.039
DB13988 3512 None 28 Human Binding pKi = 9.2 9.2 2 17
Displacement of [3H]-5-HT from recombinant human 5-HT7A receptor expressed in CHOK1 cell membranes after 40 mins by liquid scintillation counting methodDisplacement of [3H]-5-HT from recombinant human 5-HT7A receptor expressed in CHOK1 cell membranes after 40 mins by liquid scintillation counting method
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2016.12.039
3233 3512 None 28 Human Binding pKi = 9.2 9.2 2 17
Displacement of [3H]-8-OH-DPAT from human 5-HT7 receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-8-OH-DPAT from human 5-HT7 receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysis
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmcl.2015.02.042
3247 3512 None 28 Human Binding pKi = 9.2 9.2 2 17
Displacement of [3H]-8-OH-DPAT from human 5-HT7 receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-8-OH-DPAT from human 5-HT7 receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysis
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmcl.2015.02.042
6604889 3512 None 28 Human Binding pKi = 9.2 9.2 2 17
Displacement of [3H]-8-OH-DPAT from human 5-HT7 receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-8-OH-DPAT from human 5-HT7 receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysis
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmcl.2015.02.042
CHEMBL282199 3512 None 28 Human Binding pKi = 9.2 9.2 2 17
Displacement of [3H]-8-OH-DPAT from human 5-HT7 receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-8-OH-DPAT from human 5-HT7 receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysis
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmcl.2015.02.042
DB13988 3512 None 28 Human Binding pKi = 9.2 9.2 2 17
Displacement of [3H]-8-OH-DPAT from human 5-HT7 receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-8-OH-DPAT from human 5-HT7 receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysis
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmcl.2015.02.042
168297777 193013 None 0 Rat Binding pKi = 9.1 9.1 - 1
Binding affinity to rat brain 5-HT7 receptor assessed as inhibition constant incubated for 60 minsBinding affinity to rat brain 5-HT7 receptor assessed as inhibition constant incubated for 60 mins
ChEMBL 398 8 0 4 3.3 CC1CCN(CC[C@H]2CCCN2S(=O)(=O)c2cccc(OCCF)c2)CC1 10.1021/acs.jmedchem.2c00633
CHEMBL5184185 193013 None 0 Rat Binding pKi = 9.1 9.1 - 1
Binding affinity to rat brain 5-HT7 receptor assessed as inhibition constant incubated for 60 minsBinding affinity to rat brain 5-HT7 receptor assessed as inhibition constant incubated for 60 mins
ChEMBL 398 8 0 4 3.3 CC1CCN(CC[C@H]2CCCN2S(=O)(=O)c2cccc(OCCF)c2)CC1 10.1021/acs.jmedchem.2c00633
CHEMBL5222088 193013 None 0 Rat Binding pKi = 9.1 9.1 - 1
Binding affinity to rat brain 5-HT7 receptor assessed as inhibition constant incubated for 60 minsBinding affinity to rat brain 5-HT7 receptor assessed as inhibition constant incubated for 60 mins
ChEMBL 398 8 0 4 3.3 CC1CCN(CC[C@H]2CCCN2S(=O)(=O)c2cccc(OCCF)c2)CC1 10.1021/acs.jmedchem.2c00633
145974165 164683 None 0 Human Binding pKi = 9.1 9.1 8 2
Displacement of [3H]-LSD from recombinant human 5-HT7 receptor expressed in CHO cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5-HT7 receptor expressed in CHO cell membranes measured after 60 mins by scintillation counting method
ChEMBL 410 5 0 2 6.0 Clc1ccc(CCN2CCN(c3ccccc3-c3ccccc3)CC2)cc1Cl 10.1016/j.bmcl.2017.11.007
CHEMBL4215605 164683 None 0 Human Binding pKi = 9.1 9.1 8 2
Displacement of [3H]-LSD from recombinant human 5-HT7 receptor expressed in CHO cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5-HT7 receptor expressed in CHO cell membranes measured after 60 mins by scintillation counting method
ChEMBL 410 5 0 2 6.0 Clc1ccc(CCN2CCN(c3ccccc3-c3ccccc3)CC2)cc1Cl 10.1016/j.bmcl.2017.11.007
118717217 120640 None 0 Human Binding pKi = 9.1 9.1 2 2
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cells
ChEMBL 325 4 2 3 1.6 COCC1(OC)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
CHEMBL3343667 120640 None 0 Human Binding pKi = 9.1 9.1 2 2
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cells
ChEMBL 325 4 2 3 1.6 COCC1(OC)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
CHEMBL3545762 120640 None 0 Human Binding pKi = 9.1 9.1 2 2
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cells
ChEMBL 325 4 2 3 1.6 COCC1(OC)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
24829343 159113 None 0 Human Binding pKi = 9.1 9.1 24 9
Antagonist activity at 5-HT7 receptor (unknown origin)Antagonist activity at 5-HT7 receptor (unknown origin)
ChEMBL 429 7 1 3 5.1 CCC1(CCCCN2CCN(c3ccc(Cl)cc3)CC2)C(=O)Nc2cc(F)ccc21 10.1016/j.ejmech.2019.111705
CHEMBL409662 159113 None 0 Human Binding pKi = 9.1 9.1 24 9
Antagonist activity at 5-HT7 receptor (unknown origin)Antagonist activity at 5-HT7 receptor (unknown origin)
ChEMBL 429 7 1 3 5.1 CCC1(CCCCN2CCN(c3ccc(Cl)cc3)CC2)C(=O)Nc2cc(F)ccc21 10.1016/j.ejmech.2019.111705
24829343 159113 None 0 Human Binding pKi = 9.1 9.1 24 9
Displacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometryDisplacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometry
ChEMBL 429 7 1 3 5.1 CCC1(CCCCN2CCN(c3ccc(Cl)cc3)CC2)C(=O)Nc2cc(F)ccc21 10.1021/jm200547z
CHEMBL409662 159113 None 0 Human Binding pKi = 9.1 9.1 24 9
Displacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometryDisplacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometry
ChEMBL 429 7 1 3 5.1 CCC1(CCCCN2CCN(c3ccc(Cl)cc3)CC2)C(=O)Nc2cc(F)ccc21 10.1021/jm200547z
24829343 159113 None 0 Human Binding pKi = 9.1 9.1 24 9
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 429 7 1 3 5.1 CCC1(CCCCN2CCN(c3ccc(Cl)cc3)CC2)C(=O)Nc2cc(F)ccc21 10.1021/jm070279v
CHEMBL409662 159113 None 0 Human Binding pKi = 9.1 9.1 24 9
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 429 7 1 3 5.1 CCC1(CCCCN2CCN(c3ccc(Cl)cc3)CC2)C(=O)Nc2cc(F)ccc21 10.1021/jm070279v
145991084 166966 None 0 Human Binding pKi = 9.1 9.1 7 2
Displacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cell membranes after 120 mins by TopCount scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cell membranes after 120 mins by TopCount scintillation counting method
ChEMBL 417 5 1 2 5.5 Fc1cccc(-c2ccccc2N2CCN(CCc3c[nH]c4ccc(F)cc34)CC2)c1 10.1016/j.ejmech.2017.12.063
CHEMBL4285796 166966 None 0 Human Binding pKi = 9.1 9.1 7 2
Displacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cell membranes after 120 mins by TopCount scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cell membranes after 120 mins by TopCount scintillation counting method
ChEMBL 417 5 1 2 5.5 Fc1cccc(-c2ccccc2N2CCN(CCc3c[nH]c4ccc(F)cc34)CC2)c1 10.1016/j.ejmech.2017.12.063
44340835 10411 None 0 Human Binding pKi = 9.1 9.1 117 2
Binding affinity for human cloned 5-hydroxytryptamine 7 receptor in HEK 293 using [3H]5-CT as a radioligandBinding affinity for human cloned 5-hydroxytryptamine 7 receptor in HEK 293 using [3H]5-CT as a radioligand
ChEMBL 499 7 1 4 5.0 O=C(c1ccc(Cl)cc1)C1CCN(CC[C@H]2CCCN2S(=O)(=O)c2ccc3cc[nH]c3c2)CC1 10.1016/s0960-894x(02)00690-x
CHEMBL116292 10411 None 0 Human Binding pKi = 9.1 9.1 117 2
Binding affinity for human cloned 5-hydroxytryptamine 7 receptor in HEK 293 using [3H]5-CT as a radioligandBinding affinity for human cloned 5-hydroxytryptamine 7 receptor in HEK 293 using [3H]5-CT as a radioligand
ChEMBL 499 7 1 4 5.0 O=C(c1ccc(Cl)cc1)C1CCN(CC[C@H]2CCCN2S(=O)(=O)c2ccc3cc[nH]c3c2)CC1 10.1016/s0960-894x(02)00690-x
155568606 176212 None 0 Human Binding pKi = 9.1 9.1 -3 2
Displacement of [3H]-LSD from human recombinant 5-HT7 receptor expressed in CHO cells incubated for 60 mins by microbeta2 scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT7 receptor expressed in CHO cells incubated for 60 mins by microbeta2 scintillation counter
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 176212 None 0 Human Binding pKi = 9.1 9.1 -3 2
Displacement of [3H]-LSD from human recombinant 5-HT7 receptor expressed in CHO cells incubated for 60 mins by microbeta2 scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT7 receptor expressed in CHO cells incubated for 60 mins by microbeta2 scintillation counter
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
5 139 None 45 Human Binding pKi = 9.1 9.1 -3 54
Displacement of [3H]LSD from human 5-HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human 5-HT7 receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2014.12.045
5202 139 None 45 Human Binding pKi = 9.1 9.1 -3 54
Displacement of [3H]LSD from human 5-HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human 5-HT7 receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2014.12.045
CHEMBL39 139 None 45 Human Binding pKi = 9.1 9.1 -3 54
Displacement of [3H]LSD from human 5-HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human 5-HT7 receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2014.12.045
DB08839 139 None 45 Human Binding pKi = 9.1 9.1 -3 54
Displacement of [3H]LSD from human 5-HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human 5-HT7 receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2014.12.045
5 139 None 45 Human Binding pKi = 9.1 9.1 -3 54
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 10.1021/jm401895u
5202 139 None 45 Human Binding pKi = 9.1 9.1 -3 54
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 10.1021/jm401895u
CHEMBL39 139 None 45 Human Binding pKi = 9.1 9.1 -3 54
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 10.1021/jm401895u
DB08839 139 None 45 Human Binding pKi = 9.1 9.1 -3 54
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 10.1021/jm401895u
66801158 112147 None 0 Human Binding pKi = 9.1 9.1 -1 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 464 8 1 6 3.9 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
CHEMBL3289978 112147 None 0 Human Binding pKi = 9.1 9.1 -1 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 464 8 1 6 3.9 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
56944665 112173 None 0 Human Binding pKi = 9.1 9.1 -1 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 481 8 1 5 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cccc2ccccc12 10.1021/jm401895u
CHEMBL3290003 112173 None 0 Human Binding pKi = 9.1 9.1 -1 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 481 8 1 5 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cccc2ccccc12 10.1021/jm401895u
56944668 112175 None 0 Human Binding pKi = 9.1 9.1 1 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 467 7 1 5 4.7 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
CHEMBL3290005 112175 None 0 Human Binding pKi = 9.1 9.1 1 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 467 7 1 5 4.7 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
25107518 187390 None 0 Rat Binding pKi = 9.1 9.1 20 4
Displacement of [3H]LSD from rat cloned 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from rat cloned 5HT7 receptor expressed in HEK293 cells
ChEMBL 441 10 1 3 5.4 O=C(CCCCCN1CCN(c2ccccc2-c2ccccc2)CC1)NCc1ccccc1 10.1021/jm800615e
CHEMBL492871 187390 None 0 Rat Binding pKi = 9.1 9.1 20 4
Displacement of [3H]LSD from rat cloned 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from rat cloned 5HT7 receptor expressed in HEK293 cells
ChEMBL 441 10 1 3 5.4 O=C(CCCCCN1CCN(c2ccccc2-c2ccccc2)CC1)NCc1ccccc1 10.1021/jm800615e
9971032 204662 None 0 Rat Binding pKi = 9.1 9.1 - 1
Binding affinity at rat 5-hydroxytryptamine 7 receptor.Binding affinity at rat 5-hydroxytryptamine 7 receptor.
ChEMBL 282 2 1 1 4.0 Cc1[nH]c(C)c(-c2cccc3c2CC[C@H](N(C)C)C3)c1C 10.1021/jm030826m
CHEMBL609675 204662 None 0 Rat Binding pKi = 9.1 9.1 - 1
Binding affinity at rat 5-hydroxytryptamine 7 receptor.Binding affinity at rat 5-hydroxytryptamine 7 receptor.
ChEMBL 282 2 1 1 4.0 Cc1[nH]c(C)c(-c2cccc3c2CC[C@H](N(C)C)C3)c1C 10.1021/jm030826m
44340850 9904 None 0 Human Binding pKi = 9.1 9.1 22 2
Binding affinity for human cloned 5-hydroxytryptamine 7 receptor in HEK 293 using [3H]5-CT as a radioligandBinding affinity for human cloned 5-hydroxytryptamine 7 receptor in HEK 293 using [3H]5-CT as a radioligand
ChEMBL 483 7 1 4 4.4 O=C(c1ccc(F)cc1)C1CCN(CC[C@H]2CCCN2S(=O)(=O)c2ccc3cc[nH]c3c2)CC1 10.1016/s0960-894x(02)00690-x
CHEMBL114345 9904 None 0 Human Binding pKi = 9.1 9.1 22 2
Binding affinity for human cloned 5-hydroxytryptamine 7 receptor in HEK 293 using [3H]5-CT as a radioligandBinding affinity for human cloned 5-hydroxytryptamine 7 receptor in HEK 293 using [3H]5-CT as a radioligand
ChEMBL 483 7 1 4 4.4 O=C(c1ccc(F)cc1)C1CCN(CC[C@H]2CCCN2S(=O)(=O)c2ccc3cc[nH]c3c2)CC1 10.1016/s0960-894x(02)00690-x
155516399 170174 None 0 Human Binding pKi = 9.1 9.1 47 2
Displacement of [3H]-5-HT from human 5HT7 receptor expressed in CHO-K1 cells incubated for 40 mins in presence of serotonin by liquid scintillation counterDisplacement of [3H]-5-HT from human 5HT7 receptor expressed in CHO-K1 cells incubated for 40 mins in presence of serotonin by liquid scintillation counter
ChEMBL 368 6 1 5 3.1 O=c1[nH]c(CCCCN2CCN(c3ccccc3)CC2)nc2ccsc12 10.1016/j.ejmech.2019.111690
CHEMBL4443201 170174 None 0 Human Binding pKi = 9.1 9.1 47 2
Displacement of [3H]-5-HT from human 5HT7 receptor expressed in CHO-K1 cells incubated for 40 mins in presence of serotonin by liquid scintillation counterDisplacement of [3H]-5-HT from human 5HT7 receptor expressed in CHO-K1 cells incubated for 40 mins in presence of serotonin by liquid scintillation counter
ChEMBL 368 6 1 5 3.1 O=c1[nH]c(CCCCN2CCN(c3ccccc3)CC2)nc2ccsc12 10.1016/j.ejmech.2019.111690
10069973 52415 None 0 Rat Binding pKi = 9.1 9.1 4 5
Binding affinity to the rat 5-hydroxytryptamine 7 receptorBinding affinity to the rat 5-hydroxytryptamine 7 receptor
ChEMBL 407 9 0 6 4.4 COc1ccccc1C(=O)CCCCCN1CCN(c2noc3ccccc23)CC1 10.1021/jm020994z
CHEMBL159022 52415 None 0 Rat Binding pKi = 9.1 9.1 4 5
Binding affinity to the rat 5-hydroxytryptamine 7 receptorBinding affinity to the rat 5-hydroxytryptamine 7 receptor
ChEMBL 407 9 0 6 4.4 COc1ccccc1C(=O)CCCCCN1CCN(c2noc3ccccc23)CC1 10.1021/jm020994z
155552188 174168 None 0 Human Binding pKi = 9.1 9.1 7 2
Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHO cell membranes incubated for 120 mins by scintillation counting methodDisplacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHO cell membranes incubated for 120 mins by scintillation counting method
ChEMBL 421 6 2 3 4.6 Fc1ccc(N2CCN(CCCc3c[nH]c4ccc(F)cc34)CC2)c(-c2cn[nH]c2)c1 10.1016/j.bmcl.2019.126703
CHEMBL4544153 174168 None 0 Human Binding pKi = 9.1 9.1 7 2
Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHO cell membranes incubated for 120 mins by scintillation counting methodDisplacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHO cell membranes incubated for 120 mins by scintillation counting method
ChEMBL 421 6 2 3 4.6 Fc1ccc(N2CCN(CCCc3c[nH]c4ccc(F)cc34)CC2)c(-c2cn[nH]c2)c1 10.1016/j.bmcl.2019.126703
1809 134 None 25 Human Binding pKi = 9.1 9.1 -7 37
Displacement of [3H]5-HT from human 5-hydroxytryptamine 7 receptorDisplacement of [3H]5-HT from human 5-hydroxytryptamine 7 receptor
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm030030n
4 134 None 25 Human Binding pKi = 9.1 9.1 -7 37
Displacement of [3H]5-HT from human 5-hydroxytryptamine 7 receptorDisplacement of [3H]5-HT from human 5-hydroxytryptamine 7 receptor
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm030030n
CHEMBL18840 134 None 25 Human Binding pKi = 9.1 9.1 -7 37
Displacement of [3H]5-HT from human 5-hydroxytryptamine 7 receptorDisplacement of [3H]5-HT from human 5-hydroxytryptamine 7 receptor
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm030030n
4106 2502 None 21 Human Binding pKi = 9.1 9.1 -4 33
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm401895u
5358812 2502 None 21 Human Binding pKi = 9.1 9.1 -4 33
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm401895u
89 2502 None 21 Human Binding pKi = 9.1 9.1 -4 33
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm401895u
CHEMBL93240 2502 None 21 Human Binding pKi = 9.1 9.1 -4 33
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm401895u
66801234 112164 None 0 Human Binding pKi = 9.1 9.1 1 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 469 7 1 5 4.3 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc(F)c(Cl)c1 10.1021/jm401895u
CHEMBL3289995 112164 None 0 Human Binding pKi = 9.1 9.1 1 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 469 7 1 5 4.3 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc(F)c(Cl)c1 10.1021/jm401895u
66801271 112168 None 0 Human Binding pKi = 9.1 9.1 5 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 423 7 1 6 3.6 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cccs1 10.1021/jm401895u
CHEMBL3289999 112168 None 0 Human Binding pKi = 9.1 9.1 5 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 423 7 1 6 3.6 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cccs1 10.1021/jm401895u
66801139 112179 None 0 Human Binding pKi = 9.1 9.1 1 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 473 7 1 6 4.7 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1csc2ccccc12 10.1021/jm401895u
CHEMBL3290009 112179 None 0 Human Binding pKi = 9.1 9.1 1 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 473 7 1 6 4.7 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1csc2ccccc12 10.1021/jm401895u
23643870 92917 None 0 Rat Binding pKi = 9.1 9.1 35 3
Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells
ChEMBL 448 9 1 4 4.6 CN(C)c1ccccc1N1CCN(CCCCCC(=O)NC2CCCc3ccccc32)CC1 10.1021/jm070487n
CHEMBL243955 92917 None 0 Rat Binding pKi = 9.1 9.1 35 3
Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells
ChEMBL 448 9 1 4 4.6 CN(C)c1ccccc1N1CCN(CCCCCC(=O)NC2CCCc3ccccc32)CC1 10.1021/jm070487n
44437328 91016 None 0 Rat Binding pKi = 9.1 9.1 - 1
Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells at 10 uMDisplacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells at 10 uM
ChEMBL 678 17 0 8 6.7 COc1ccccc1N1CCN(CCc2cccc(OCCCCOc3cccc(CCN4CCN(c5ccccc5OC)CC4)c3)c2)CC1 10.1016/j.bmc.2007.05.010
CHEMBL239656 91016 None 0 Rat Binding pKi = 9.1 9.1 - 1
Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells at 10 uMDisplacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells at 10 uM
ChEMBL 678 17 0 8 6.7 COc1ccccc1N1CCN(CCc2cccc(OCCCCOc3cccc(CCN4CCN(c5ccccc5OC)CC4)c3)c2)CC1 10.1016/j.bmc.2007.05.010
1809 134 None 25 Human Binding pKi = 9.0 9.0 -7 37
Binding affinity to 5-HT7 receptor (unknown origin)Binding affinity to 5-HT7 receptor (unknown origin)
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/acs.jmedchem.7b01898
4 134 None 25 Human Binding pKi = 9.0 9.0 -7 37
Binding affinity to 5-HT7 receptor (unknown origin)Binding affinity to 5-HT7 receptor (unknown origin)
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/acs.jmedchem.7b01898
CHEMBL18840 134 None 25 Human Binding pKi = 9.0 9.0 -7 37
Binding affinity to 5-HT7 receptor (unknown origin)Binding affinity to 5-HT7 receptor (unknown origin)
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/acs.jmedchem.7b01898
107 141 None 65 Rat Binding pKi = 9.0 9.0 -1 30
Binding affinity at rat 5-hydroxytryptamine 7 receptor.Binding affinity at rat 5-hydroxytryptamine 7 receptor.
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1021/jm030826m
1833 141 None 65 Rat Binding pKi = 9.0 9.0 -1 30
Binding affinity at rat 5-hydroxytryptamine 7 receptor.Binding affinity at rat 5-hydroxytryptamine 7 receptor.
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1021/jm030826m
CHEMBL8165 141 None 65 Rat Binding pKi = 9.0 9.0 -1 30
Binding affinity at rat 5-hydroxytryptamine 7 receptor.Binding affinity at rat 5-hydroxytryptamine 7 receptor.
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1021/jm030826m
25107520 187699 None 0 Rat Binding pKi = 9.0 9.0 70 3
Displacement of [3H]LSD from rat cloned 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from rat cloned 5HT7 receptor expressed in HEK293 cells
ChEMBL 442 10 1 4 4.7 O=C(CCCCCN1CCN(c2ccccc2-c2ccccc2)CC1)NCc1ccncc1 10.1021/jm800615e
CHEMBL494709 187699 None 0 Rat Binding pKi = 9.0 9.0 70 3
Displacement of [3H]LSD from rat cloned 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from rat cloned 5HT7 receptor expressed in HEK293 cells
ChEMBL 442 10 1 4 4.7 O=C(CCCCCN1CCN(c2ccccc2-c2ccccc2)CC1)NCc1ccncc1 10.1021/jm800615e
141745651 175450 None 0 Human Binding pKi = 9 9.0 1 2
Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHO cell membranes incubated for 120 mins by scintillation counting methodDisplacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHO cell membranes incubated for 120 mins by scintillation counting method
ChEMBL 380 4 1 4 4.3 Fc1ccc2[nH]cc(CCN3CCN(c4nsc5ccccc45)CC3)c2c1 10.1016/j.bmcl.2019.126703
CHEMBL4574299 175450 None 0 Human Binding pKi = 9 9.0 1 2
Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHO cell membranes incubated for 120 mins by scintillation counting methodDisplacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHO cell membranes incubated for 120 mins by scintillation counting method
ChEMBL 380 4 1 4 4.3 Fc1ccc2[nH]cc(CCN3CCN(c4nsc5ccccc45)CC3)c2c1 10.1016/j.bmcl.2019.126703
118713589 114438 None 0 Human Binding pKi = 9 9.0 10 2
Displacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry
ChEMBL 381 6 0 5 4.0 Cc1ccccc1N1CCN(CCCCn2c(=O)sc3ccccc32)CC1 10.1016/j.ejmech.2014.08.023
CHEMBL3331258 114438 None 0 Human Binding pKi = 9 9.0 10 2
Displacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry
ChEMBL 381 6 0 5 4.0 Cc1ccccc1N1CCN(CCCCn2c(=O)sc3ccccc32)CC1 10.1016/j.ejmech.2014.08.023
44393134 64870 None 0 Human Binding pKi = 9 9.0 39 2
Binding affinity against 5-Hydroxy tryptamine 7 receptorBinding affinity against 5-Hydroxy tryptamine 7 receptor
ChEMBL 352 8 2 5 4.3 CC(Nc1nccc(NCCOc2ccc(F)cc2)n1)c1ccccc1 10.1016/j.bmcl.2004.06.007
CHEMBL182071 64870 None 0 Human Binding pKi = 9 9.0 39 2
Binding affinity against 5-Hydroxy tryptamine 7 receptorBinding affinity against 5-Hydroxy tryptamine 7 receptor
ChEMBL 352 8 2 5 4.3 CC(Nc1nccc(NCCOc2ccc(F)cc2)n1)c1ccccc1 10.1016/j.bmcl.2004.06.007
4184551 192770 None 5 Human Binding pKi = 9 9.0 - 1
Binding affinity to 5-HT7R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT7R (unknown origin) assessed as inhibition constant
ChEMBL 352 5 1 4 2.7 CC1CCN(CCC2CCCN2S(=O)(=O)c2cccc(O)c2)CC1 10.1016/j.bmcl.2021.128275
CHEMBL5218527 192770 None 5 Human Binding pKi = 9 9.0 - 1
Binding affinity to 5-HT7R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT7R (unknown origin) assessed as inhibition constant
ChEMBL 352 5 1 4 2.7 CC1CCN(CCC2CCCN2S(=O)(=O)c2cccc(O)c2)CC1 10.1016/j.bmcl.2021.128275
3233 3512 None 28 Human Binding pKi = 9 9.0 2 17
Binding affinity to 5HT7 receptorBinding affinity to 5HT7 receptor
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmcl.2010.11.078
3247 3512 None 28 Human Binding pKi = 9 9.0 2 17
Binding affinity to 5HT7 receptorBinding affinity to 5HT7 receptor
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmcl.2010.11.078
6604889 3512 None 28 Human Binding pKi = 9 9.0 2 17
Binding affinity to 5HT7 receptorBinding affinity to 5HT7 receptor
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmcl.2010.11.078
CHEMBL282199 3512 None 28 Human Binding pKi = 9 9.0 2 17
Binding affinity to 5HT7 receptorBinding affinity to 5HT7 receptor
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmcl.2010.11.078
DB13988 3512 None 28 Human Binding pKi = 9 9.0 2 17
Binding affinity to 5HT7 receptorBinding affinity to 5HT7 receptor
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmcl.2010.11.078
7059581 167141 None 1 Rat Binding pKi = 9 9.0 -1 2
Binding affinity towards 5-hydroxytryptamine 7 receptorBinding affinity towards 5-hydroxytryptamine 7 receptor
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)[C@@H](N1CCN(C)CC1)Cc1ccccc1S2 10.1016/s0960-894x(00)00166-9
CHEMBL428892 167141 None 1 Rat Binding pKi = 9 9.0 -1 2
Binding affinity towards 5-hydroxytryptamine 7 receptorBinding affinity towards 5-hydroxytryptamine 7 receptor
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)[C@@H](N1CCN(C)CC1)Cc1ccccc1S2 10.1016/s0960-894x(00)00166-9
3233 3512 None 28 Human Binding pKi = 9 9.0 2 17
Binding affinity towards human 5-hydroxytryptamine 7 receptor on HEK293 cells using radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine 7 receptor on HEK293 cells using radioligand [3H]LSD
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/s0960-894x(02)00438-9
3247 3512 None 28 Human Binding pKi = 9 9.0 2 17
Binding affinity towards human 5-hydroxytryptamine 7 receptor on HEK293 cells using radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine 7 receptor on HEK293 cells using radioligand [3H]LSD
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/s0960-894x(02)00438-9
6604889 3512 None 28 Human Binding pKi = 9 9.0 2 17
Binding affinity towards human 5-hydroxytryptamine 7 receptor on HEK293 cells using radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine 7 receptor on HEK293 cells using radioligand [3H]LSD
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/s0960-894x(02)00438-9
CHEMBL282199 3512 None 28 Human Binding pKi = 9 9.0 2 17
Binding affinity towards human 5-hydroxytryptamine 7 receptor on HEK293 cells using radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine 7 receptor on HEK293 cells using radioligand [3H]LSD
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/s0960-894x(02)00438-9
DB13988 3512 None 28 Human Binding pKi = 9 9.0 2 17
Binding affinity towards human 5-hydroxytryptamine 7 receptor on HEK293 cells using radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine 7 receptor on HEK293 cells using radioligand [3H]LSD
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/s0960-894x(02)00438-9
11725453 99134 None 0 Human Binding pKi = 9 9.0 1 6
Binding affinity towards human 5-hydroxytryptamine 7 receptor on HEK293 cells using radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine 7 receptor on HEK293 cells using radioligand [3H]LSD
ChEMBL 350 1 0 2 5.3 Cc1cccc(C#N)c1-c1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1016/s0960-894x(02)00438-9
CHEMBL28056 99134 None 0 Human Binding pKi = 9 9.0 1 6
Binding affinity towards human 5-hydroxytryptamine 7 receptor on HEK293 cells using radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine 7 receptor on HEK293 cells using radioligand [3H]LSD
ChEMBL 350 1 0 2 5.3 Cc1cccc(C#N)c1-c1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1016/s0960-894x(02)00438-9
3233 3512 None 28 Rat Binding pKi = 9 9.0 -2 17
Binding affinity towards rat 5-HT7 receptor expressed in HEK cellsBinding affinity towards rat 5-HT7 receptor expressed in HEK cells
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm049743b
3247 3512 None 28 Rat Binding pKi = 9 9.0 -2 17
Binding affinity towards rat 5-HT7 receptor expressed in HEK cellsBinding affinity towards rat 5-HT7 receptor expressed in HEK cells
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm049743b
6604889 3512 None 28 Rat Binding pKi = 9 9.0 -2 17
Binding affinity towards rat 5-HT7 receptor expressed in HEK cellsBinding affinity towards rat 5-HT7 receptor expressed in HEK cells
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm049743b
CHEMBL282199 3512 None 28 Rat Binding pKi = 9 9.0 -2 17
Binding affinity towards rat 5-HT7 receptor expressed in HEK cellsBinding affinity towards rat 5-HT7 receptor expressed in HEK cells
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm049743b
DB13988 3512 None 28 Rat Binding pKi = 9 9.0 -2 17
Binding affinity towards rat 5-HT7 receptor expressed in HEK cellsBinding affinity towards rat 5-HT7 receptor expressed in HEK cells
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm049743b
7059581 167141 None 1 Rat Binding pKi = 9 9.0 -1 2
Binding affinity towards rat 5-HT7 receptor expressed in HEK cellsBinding affinity towards rat 5-HT7 receptor expressed in HEK cells
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)[C@@H](N1CCN(C)CC1)Cc1ccccc1S2 10.1021/jm049743b
CHEMBL428892 167141 None 1 Rat Binding pKi = 9 9.0 -1 2
Binding affinity towards rat 5-HT7 receptor expressed in HEK cellsBinding affinity towards rat 5-HT7 receptor expressed in HEK cells
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)[C@@H](N1CCN(C)CC1)Cc1ccccc1S2 10.1021/jm049743b
127025243 137830 None 0 Human Binding pKi = 9 9.0 60 5
Displacement of [3H]-5-CT from human 5-HT7B receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5-HT7B receptor expressed in HEK293 cells after 1 hr
ChEMBL 446 8 1 4 4.3 CC(C)c1cccc(OCCN2C3CCC2CC(NS(=O)(=O)c2ccc(F)cc2)C3)c1 10.1016/j.ejmech.2015.11.040
CHEMBL3759205 137830 None 0 Human Binding pKi = 9 9.0 60 5
Displacement of [3H]-5-CT from human 5-HT7B receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5-HT7B receptor expressed in HEK293 cells after 1 hr
ChEMBL 446 8 1 4 4.3 CC(C)c1cccc(OCCN2C3CCC2CC(NS(=O)(=O)c2ccc(F)cc2)C3)c1 10.1016/j.ejmech.2015.11.040
145985692 165539 None 0 Human Binding pKi = 9 9.0 -3 5
Displacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 0 7 4.2 O=S(=O)(c1cccc2cnccc12)N1CCC[C@@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4239091 165539 None 0 Human Binding pKi = 9 9.0 -3 5
Displacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 0 7 4.2 O=S(=O)(c1cccc2cnccc12)N1CCC[C@@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
118626161 165694 None 0 Human Binding pKi = 9 9.0 -1 5
Displacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 0 7 4.2 O=S(=O)(c1cccc2ncccc12)N1CCC[C@@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4242858 165694 None 0 Human Binding pKi = 9 9.0 -1 5
Displacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 0 7 4.2 O=S(=O)(c1cccc2ncccc12)N1CCC[C@@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
118626129 165737 None 0 Human Binding pKi = 9 9.0 3 5
Displacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 506 6 0 6 4.8 O=S(=O)(c1cccc2ncccc12)N1CCC[C@@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4243848 165737 None 0 Human Binding pKi = 9 9.0 3 5
Displacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 506 6 0 6 4.8 O=S(=O)(c1cccc2ncccc12)N1CCC[C@@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
156021386 178195 None 0 Human Binding pKi = 9 9.0 7 2
Displacement of [3H]-5-carboxamidotryptamine from human 5-HT7A receptor expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting methodDisplacement of [3H]-5-carboxamidotryptamine from human 5-HT7A receptor expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting method
ChEMBL 285 2 0 1 4.4 CN(C)[C@H]1CCc2c(cccc2-c2ccccc2Cl)C1 10.1016/j.bmc.2019.115262
CHEMBL4647808 178195 None 0 Human Binding pKi = 9 9.0 7 2
Displacement of [3H]-5-carboxamidotryptamine from human 5-HT7A receptor expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting methodDisplacement of [3H]-5-carboxamidotryptamine from human 5-HT7A receptor expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting method
ChEMBL 285 2 0 1 4.4 CN(C)[C@H]1CCc2c(cccc2-c2ccccc2Cl)C1 10.1016/j.bmc.2019.115262
4106 2502 None 21 Human Binding pKi = 9 9.0 -4 33
Displacement of [3H]-LSD from human 5-HT7 receptor expressed in CHO-K1 cell membranes after 120 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT7 receptor expressed in CHO-K1 cell membranes after 120 mins by scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/acs.jmedchem.7b00839
5358812 2502 None 21 Human Binding pKi = 9 9.0 -4 33
Displacement of [3H]-LSD from human 5-HT7 receptor expressed in CHO-K1 cell membranes after 120 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT7 receptor expressed in CHO-K1 cell membranes after 120 mins by scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/acs.jmedchem.7b00839
89 2502 None 21 Human Binding pKi = 9 9.0 -4 33
Displacement of [3H]-LSD from human 5-HT7 receptor expressed in CHO-K1 cell membranes after 120 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT7 receptor expressed in CHO-K1 cell membranes after 120 mins by scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/acs.jmedchem.7b00839
CHEMBL93240 2502 None 21 Human Binding pKi = 9 9.0 -4 33
Displacement of [3H]-LSD from human 5-HT7 receptor expressed in CHO-K1 cell membranes after 120 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT7 receptor expressed in CHO-K1 cell membranes after 120 mins by scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/acs.jmedchem.7b00839
66803595 159822 None 0 Human Binding pKi = 9 9.0 1 4
Displacement of [3H]-LSD from human 5-HT7 receptor expressed in CHO-K1 cell membranes after 120 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT7 receptor expressed in CHO-K1 cell membranes after 120 mins by scintillation counting
ChEMBL 431 6 3 4 3.6 O=S(=O)(NCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(O)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4104622 159822 None 0 Human Binding pKi = 9 9.0 1 4
Displacement of [3H]-LSD from human 5-HT7 receptor expressed in CHO-K1 cell membranes after 120 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT7 receptor expressed in CHO-K1 cell membranes after 120 mins by scintillation counting
ChEMBL 431 6 3 4 3.6 O=S(=O)(NCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(O)c1 10.1021/acs.jmedchem.7b00839
155531753 171749 None 0 Human Binding pKi = 9 9.0 -1 2
Displacement of [3H]-LSD from human recombinant 5-HT7 receptor expressed in CHO cells incubated for 60 mins by microbeta2 scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT7 receptor expressed in CHO cells incubated for 60 mins by microbeta2 scintillation counter
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 171749 None 0 Human Binding pKi = 9 9.0 -1 2
Displacement of [3H]-LSD from human recombinant 5-HT7 receptor expressed in CHO cells incubated for 60 mins by microbeta2 scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT7 receptor expressed in CHO cells incubated for 60 mins by microbeta2 scintillation counter
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
19605739 170115 None 10 Human Binding pKi = 9 9.0 - 1
Displacement of [3H]5-HT from recombinant human 5-HT7 receptor expressed in African green monkey COS7 cellsDisplacement of [3H]5-HT from recombinant human 5-HT7 receptor expressed in African green monkey COS7 cells
ChEMBL 204 3 3 2 1.4 NCCc1c[nH]c2ccc(C(=O)O)cc12 10.1016/j.ejmech.2019.111705
CHEMBL4442472 170115 None 10 Human Binding pKi = 9 9.0 - 1
Displacement of [3H]5-HT from recombinant human 5-HT7 receptor expressed in African green monkey COS7 cellsDisplacement of [3H]5-HT from recombinant human 5-HT7 receptor expressed in African green monkey COS7 cells
ChEMBL 204 3 3 2 1.4 NCCc1c[nH]c2ccc(C(=O)O)cc12 10.1016/j.ejmech.2019.111705
2389 3331 None 72 Human Binding pKi = 9 9.0 -7 67
Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm070516u
5073 3331 None 72 Human Binding pKi = 9 9.0 -7 67
Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm070516u
5073.0 3331 None 72 Human Binding pKi = 9 9.0 -7 67
Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm070516u
96 3331 None 72 Human Binding pKi = 9 9.0 -7 67
Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm070516u
CHEMBL85 3331 None 72 Human Binding pKi = 9 9.0 -7 67
Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm070516u
DB00734 3331 None 72 Human Binding pKi = 9 9.0 -7 67
Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm070516u
16006607 95725 None 2 Human Binding pKi = 9 9.0 10 5
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in HEK293-EBNA cells
ChEMBL 219 2 2 4 2.1 CC(C)Oc1cccc2c1N=C(N)NC2C 10.1016/j.bmcl.2007.10.080
CHEMBL258075 95725 None 2 Human Binding pKi = 9 9.0 10 5
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in HEK293-EBNA cells
ChEMBL 219 2 2 4 2.1 CC(C)Oc1cccc2c1N=C(N)NC2C 10.1016/j.bmcl.2007.10.080
7059581 167141 None 1 Human Binding pKi = 9 9.0 1 2
Non-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptorNon-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptor
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)[C@@H](N1CCN(C)CC1)Cc1ccccc1S2 10.1021/jm030841r
CHEMBL428892 167141 None 1 Human Binding pKi = 9 9.0 1 2
Non-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptorNon-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptor
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)[C@@H](N1CCN(C)CC1)Cc1ccccc1S2 10.1021/jm030841r
11661471 159622 None 0 Human Binding pKi = 9.0 9.0 - 1
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 408 7 1 2 5.9 CCC1(CCCCN2CC=C(c3ccc(Cl)cc3)CC2)C(=O)Nc2ccccc21 10.1021/jm070279v
CHEMBL410226 159622 None 0 Human Binding pKi = 9.0 9.0 - 1
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 408 7 1 2 5.9 CCC1(CCCCN2CC=C(c3ccc(Cl)cc3)CC2)C(=O)Nc2ccccc21 10.1021/jm070279v
10346043 47134 None 0 Human Binding pKi = 9.0 9.0 -1 3
Compound was evaluated for binding affinity against human cloned 5-hydroxytryptamine 7 receptor in HEK 293 cells using [3H]5-CT as the radioligand(n=6)Compound was evaluated for binding affinity against human cloned 5-hydroxytryptamine 7 receptor in HEK 293 cells using [3H]5-CT as the radioligand(n=6)
ChEMBL 503 5 2 5 3.4 COc1ccc(S(=O)(=O)Nc2cc(Br)ccc2Br)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL154274 47134 None 0 Human Binding pKi = 9.0 9.0 -1 3
Compound was evaluated for binding affinity against human cloned 5-hydroxytryptamine 7 receptor in HEK 293 cells using [3H]5-CT as the radioligand(n=6)Compound was evaluated for binding affinity against human cloned 5-hydroxytryptamine 7 receptor in HEK 293 cells using [3H]5-CT as the radioligand(n=6)
ChEMBL 503 5 2 5 3.4 COc1ccc(S(=O)(=O)Nc2cc(Br)ccc2Br)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
10379532 99329 None 0 Human Binding pKi = 9.0 9.0 1 6
Displacement of [3H]5CT from 5HT7 receptorDisplacement of [3H]5CT from 5HT7 receptor
ChEMBL 291 1 0 2 3.7 CO[C@@]1(C)c2cccc3c2-c2c1ccc1c2[C@@H](C3)N(C)CC1 10.1016/j.bmcl.2010.03.012
CHEMBL281923 99329 None 0 Human Binding pKi = 9.0 9.0 1 6
Displacement of [3H]5CT from 5HT7 receptorDisplacement of [3H]5CT from 5HT7 receptor
ChEMBL 291 1 0 2 3.7 CO[C@@]1(C)c2cccc3c2-c2c1ccc1c2[C@@H](C3)N(C)CC1 10.1016/j.bmcl.2010.03.012
10062885 99330 None 0 Human Binding pKi = 9.0 9.0 1 6
Binding affinity at 5HT7 receptorBinding affinity at 5HT7 receptor
ChEMBL 291 1 0 2 3.7 CO[C@]1(C)c2cccc3c2-c2c1ccc1c2[C@@H](C3)N(C)CC1 10.1021/jm060959i
CHEMBL281924 99330 None 0 Human Binding pKi = 9.0 9.0 1 6
Binding affinity at 5HT7 receptorBinding affinity at 5HT7 receptor
ChEMBL 291 1 0 2 3.7 CO[C@]1(C)c2cccc3c2-c2c1ccc1c2[C@@H](C3)N(C)CC1 10.1021/jm060959i
78108787 192076 None 0 Human Binding pKi = 9.0 9.0 - 1
Binding affinity to human recombinant 5-HT7 receptor assessed as inhibition constantBinding affinity to human recombinant 5-HT7 receptor assessed as inhibition constant
ChEMBL 363 6 1 3 4.0 Cc1ccc(N2CCN(CCCCC3C(=O)Nc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00633
CHEMBL5201016 192076 None 0 Human Binding pKi = 9.0 9.0 - 1
Binding affinity to human recombinant 5-HT7 receptor assessed as inhibition constantBinding affinity to human recombinant 5-HT7 receptor assessed as inhibition constant
ChEMBL 363 6 1 3 4.0 Cc1ccc(N2CCN(CCCCC3C(=O)Nc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00633
10379532 99329 None 0 Human Binding pKi = 9.0 9.0 1 6
Binding affinity towards human 5-hydroxytryptamine 7 receptorBinding affinity towards human 5-hydroxytryptamine 7 receptor
ChEMBL 291 1 0 2 3.7 CO[C@@]1(C)c2cccc3c2-c2c1ccc1c2[C@@H](C3)N(C)CC1 10.1021/jm030030n
CHEMBL281923 99329 None 0 Human Binding pKi = 9.0 9.0 1 6
Binding affinity towards human 5-hydroxytryptamine 7 receptorBinding affinity towards human 5-hydroxytryptamine 7 receptor
ChEMBL 291 1 0 2 3.7 CO[C@@]1(C)c2cccc3c2-c2c1ccc1c2[C@@H](C3)N(C)CC1 10.1021/jm030030n
10062885 99330 None 0 Human Binding pKi = 9.0 9.0 1 6
Binding affinity towards human 5-hydroxytryptamine 7 receptorBinding affinity towards human 5-hydroxytryptamine 7 receptor
ChEMBL 291 1 0 2 3.7 CO[C@]1(C)c2cccc3c2-c2c1ccc1c2[C@@H](C3)N(C)CC1 10.1021/jm030030n
CHEMBL281924 99330 None 0 Human Binding pKi = 9.0 9.0 1 6
Binding affinity towards human 5-hydroxytryptamine 7 receptorBinding affinity towards human 5-hydroxytryptamine 7 receptor
ChEMBL 291 1 0 2 3.7 CO[C@]1(C)c2cccc3c2-c2c1ccc1c2[C@@H](C3)N(C)CC1 10.1021/jm030030n
10062885 99330 None 0 Human Binding pKi = 9.0 9.0 1 6
Displacement of [3H]-LSD from human 5-HT7 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT7 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 291 1 0 2 3.7 CO[C@]1(C)c2cccc3c2-c2c1ccc1c2[C@@H](C3)N(C)CC1 10.1016/j.bmc.2020.115578
CHEMBL281924 99330 None 0 Human Binding pKi = 9.0 9.0 1 6
Displacement of [3H]-LSD from human 5-HT7 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT7 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 291 1 0 2 3.7 CO[C@]1(C)c2cccc3c2-c2c1ccc1c2[C@@H](C3)N(C)CC1 10.1016/j.bmc.2020.115578
10379532 99329 None 0 Rat Binding pKi = 9.0 9.0 -1 6
Displacement of [3H]5-HT from over-expressed rat 5-hydroxytryptamine 7 receptorDisplacement of [3H]5-HT from over-expressed rat 5-hydroxytryptamine 7 receptor
ChEMBL 291 1 0 2 3.7 CO[C@@]1(C)c2cccc3c2-c2c1ccc1c2[C@@H](C3)N(C)CC1 10.1021/jm9911433
CHEMBL281923 99329 None 0 Rat Binding pKi = 9.0 9.0 -1 6
Displacement of [3H]5-HT from over-expressed rat 5-hydroxytryptamine 7 receptorDisplacement of [3H]5-HT from over-expressed rat 5-hydroxytryptamine 7 receptor
ChEMBL 291 1 0 2 3.7 CO[C@@]1(C)c2cccc3c2-c2c1ccc1c2[C@@H](C3)N(C)CC1 10.1021/jm9911433
10062885 99330 None 0 Rat Binding pKi = 9.0 9.0 -1 6
Displacement of [3H]5-HT from over-expressed rat 5-hydroxytryptamine 7 receptorDisplacement of [3H]5-HT from over-expressed rat 5-hydroxytryptamine 7 receptor
ChEMBL 291 1 0 2 3.7 CO[C@]1(C)c2cccc3c2-c2c1ccc1c2[C@@H](C3)N(C)CC1 10.1021/jm9911433
CHEMBL281924 99330 None 0 Rat Binding pKi = 9.0 9.0 -1 6
Displacement of [3H]5-HT from over-expressed rat 5-hydroxytryptamine 7 receptorDisplacement of [3H]5-HT from over-expressed rat 5-hydroxytryptamine 7 receptor
ChEMBL 291 1 0 2 3.7 CO[C@]1(C)c2cccc3c2-c2c1ccc1c2[C@@H](C3)N(C)CC1 10.1021/jm9911433
24854044 97352 None 0 Human Binding pKi = 9.0 9.0 - 1
Displacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometryDisplacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometry
ChEMBL 445 7 1 3 5.6 CCC1(CCCCN2CCN(c3ccc(Cl)cc3)CC2)C(=O)Nc2ccc(Cl)cc21 10.1021/jm200547z
CHEMBL269083 97352 None 0 Human Binding pKi = 9.0 9.0 - 1
Displacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometryDisplacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometry
ChEMBL 445 7 1 3 5.6 CCC1(CCCCN2CCN(c3ccc(Cl)cc3)CC2)C(=O)Nc2ccc(Cl)cc21 10.1021/jm200547z
56944664 112136 None 0 Human Binding pKi = 9.0 9.0 23 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 428 8 1 6 3.0 Cc1cccc(S(=O)(=O)NCCCCN2CCN(c3noc4ccccc34)CC2)c1 10.1021/jm401895u
CHEMBL3289968 112136 None 0 Human Binding pKi = 9.0 9.0 23 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 428 8 1 6 3.0 Cc1cccc(S(=O)(=O)NCCCCN2CCN(c3noc4ccccc34)CC2)c1 10.1021/jm401895u
56944764 112159 None 0 Human Binding pKi = 9.0 9.0 3 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 417 6 1 5 3.4 Cc1cccc(S(=O)(=O)NCCN2CCC(c3noc4cc(F)ccc34)CC2)c1 10.1021/jm401895u
CHEMBL3289990 112159 None 0 Human Binding pKi = 9.0 9.0 3 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 417 6 1 5 3.4 Cc1cccc(S(=O)(=O)NCCN2CCC(c3noc4cc(F)ccc34)CC2)c1 10.1021/jm401895u
23643663 92897 None 0 Rat Binding pKi = 9.0 9.0 13 3
Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells
ChEMBL 447 9 1 3 5.7 CC(C)c1ccccc1N1CCN(CCCCCC(=O)NC2CCCc3ccccc32)CC1 10.1021/jm070487n
CHEMBL243744 92897 None 0 Rat Binding pKi = 9.0 9.0 13 3
Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells
ChEMBL 447 9 1 3 5.7 CC(C)c1ccccc1N1CCN(CCCCCC(=O)NC2CCCc3ccccc32)CC1 10.1021/jm070487n
145981875 166616 None 0 Human Binding pKi = 9.0 9.0 7 2
Displacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cell membranes after 120 mins by TopCount scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cell membranes after 120 mins by TopCount scintillation counting method
ChEMBL 431 6 1 2 5.9 Fc1cccc(-c2ccccc2N2CCN(CCCc3c[nH]c4ccc(F)cc34)CC2)c1 10.1016/j.ejmech.2017.12.063
CHEMBL4278933 166616 None 0 Human Binding pKi = 9.0 9.0 7 2
Displacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cell membranes after 120 mins by TopCount scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cell membranes after 120 mins by TopCount scintillation counting method
ChEMBL 431 6 1 2 5.9 Fc1cccc(-c2ccccc2N2CCN(CCCc3c[nH]c4ccc(F)cc34)CC2)c1 10.1016/j.ejmech.2017.12.063
145992877 166992 None 0 Human Binding pKi = 9.0 9.0 11 2
Displacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cell membranes after 120 mins by TopCount scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cell membranes after 120 mins by TopCount scintillation counting method
ChEMBL 413 6 1 2 5.7 Fc1ccc2[nH]cc(CCCN3CCN(c4ccccc4-c4ccccc4)CC3)c2c1 10.1016/j.ejmech.2017.12.063
CHEMBL4286174 166992 None 0 Human Binding pKi = 9.0 9.0 11 2
Displacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cell membranes after 120 mins by TopCount scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cell membranes after 120 mins by TopCount scintillation counting method
ChEMBL 413 6 1 2 5.7 Fc1ccc2[nH]cc(CCCN3CCN(c4ccccc4-c4ccccc4)CC3)c2c1 10.1016/j.ejmech.2017.12.063
3044582 192522 None 1 Human Binding pKi = 9.0 9.0 - 1
Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in CHO-K1 cells membrane by scintillation counter analysisDisplacement of [3H]-5-CT from human 5-HT7 receptor expressed in CHO-K1 cells membrane by scintillation counter analysis
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)CC(N1CCN(C)CC1)c1ccccc1S2 10.1016/j.ejmech.2022.114218
CHEMBL5208064 192522 None 1 Human Binding pKi = 9.0 9.0 - 1
Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in CHO-K1 cells membrane by scintillation counter analysisDisplacement of [3H]-5-CT from human 5-HT7 receptor expressed in CHO-K1 cells membrane by scintillation counter analysis
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)CC(N1CCN(C)CC1)c1ccccc1S2 10.1016/j.ejmech.2022.114218
1809 134 None 25 Human Binding pKi = 8.9 8.9 -7 37
PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.6019/CHEMBL5442175
4 134 None 25 Human Binding pKi = 8.9 8.9 -7 37
PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.6019/CHEMBL5442175
CHEMBL18840 134 None 25 Human Binding pKi = 8.9 8.9 -7 37
PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.6019/CHEMBL5442175
11524003 159621 None 0 Human Binding pKi = 8.9 8.9 - 1
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 392 7 1 2 5.4 CCC1(CCCCN2CC=C(c3ccc(F)cc3)CC2)C(=O)Nc2ccccc21 10.1021/jm070279v
CHEMBL410225 159621 None 0 Human Binding pKi = 8.9 8.9 - 1
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 392 7 1 2 5.4 CCC1(CCCCN2CC=C(c3ccc(F)cc3)CC2)C(=O)Nc2ccccc21 10.1021/jm070279v
3233 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Binding affinity to human cloned 5HT7 receptor expressed in HEK293 cellsBinding affinity to human cloned 5HT7 receptor expressed in HEK293 cells
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmcl.2009.06.038
3247 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Binding affinity to human cloned 5HT7 receptor expressed in HEK293 cellsBinding affinity to human cloned 5HT7 receptor expressed in HEK293 cells
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmcl.2009.06.038
6604889 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Binding affinity to human cloned 5HT7 receptor expressed in HEK293 cellsBinding affinity to human cloned 5HT7 receptor expressed in HEK293 cells
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmcl.2009.06.038
CHEMBL282199 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Binding affinity to human cloned 5HT7 receptor expressed in HEK293 cellsBinding affinity to human cloned 5HT7 receptor expressed in HEK293 cells
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmcl.2009.06.038
DB13988 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Binding affinity to human cloned 5HT7 receptor expressed in HEK293 cellsBinding affinity to human cloned 5HT7 receptor expressed in HEK293 cells
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmcl.2009.06.038
3233 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2011.09.044
3247 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2011.09.044
6604889 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2011.09.044
CHEMBL282199 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2011.09.044
DB13988 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2011.09.044
3233 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2012.07.043
3247 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2012.07.043
6604889 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2012.07.043
CHEMBL282199 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2012.07.043
DB13988 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2012.07.043
118717211 120642 None 0 Human Binding pKi = 8.9 8.9 33 2
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cells
ChEMBL 295 2 3 2 1.7 CCC1(O)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
CHEMBL3343663 120642 None 0 Human Binding pKi = 8.9 8.9 33 2
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cells
ChEMBL 295 2 3 2 1.7 CCC1(O)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
CHEMBL3545801 120642 None 0 Human Binding pKi = 8.9 8.9 33 2
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cells
ChEMBL 295 2 3 2 1.7 CCC1(O)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
11524003 159621 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometryDisplacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometry
ChEMBL 392 7 1 2 5.4 CCC1(CCCCN2CC=C(c3ccc(F)cc3)CC2)C(=O)Nc2ccccc21 10.1021/jm200547z
CHEMBL410225 159621 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometryDisplacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometry
ChEMBL 392 7 1 2 5.4 CCC1(CCCCN2CC=C(c3ccc(F)cc3)CC2)C(=O)Nc2ccccc21 10.1021/jm200547z
66801346 112162 None 0 Human Binding pKi = 8.9 8.9 1 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 485 7 1 5 4.8 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm401895u
CHEMBL3289993 112162 None 0 Human Binding pKi = 8.9 8.9 1 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 485 7 1 5 4.8 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm401895u
24854181 96485 None 0 Human Binding pKi = 8.9 8.9 - 1
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 425 8 1 3 5.3 CCC1(CCCCCN2CCN(c3ccc(Cl)cc3)CC2)C(=O)Nc2ccccc21 10.1021/jm070279v
CHEMBL262068 96485 None 0 Human Binding pKi = 8.9 8.9 - 1
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 425 8 1 3 5.3 CCC1(CCCCCN2CCN(c3ccc(Cl)cc3)CC2)C(=O)Nc2ccccc21 10.1021/jm070279v
3233 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Antagonist activity at 5-HT7 receptor (unknown origin)Antagonist activity at 5-HT7 receptor (unknown origin)
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2019.111705
3247 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Antagonist activity at 5-HT7 receptor (unknown origin)Antagonist activity at 5-HT7 receptor (unknown origin)
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2019.111705
6604889 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Antagonist activity at 5-HT7 receptor (unknown origin)Antagonist activity at 5-HT7 receptor (unknown origin)
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2019.111705
CHEMBL282199 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Antagonist activity at 5-HT7 receptor (unknown origin)Antagonist activity at 5-HT7 receptor (unknown origin)
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2019.111705
DB13988 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Antagonist activity at 5-HT7 receptor (unknown origin)Antagonist activity at 5-HT7 receptor (unknown origin)
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2019.111705
3233 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Binding affinity for human cloned 5-hydroxytryptamine 7 receptor in HEK 293 using [3H]5-CT as a radioligandBinding affinity for human cloned 5-hydroxytryptamine 7 receptor in HEK 293 using [3H]5-CT as a radioligand
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/s0960-894x(02)00690-x
3247 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Binding affinity for human cloned 5-hydroxytryptamine 7 receptor in HEK 293 using [3H]5-CT as a radioligandBinding affinity for human cloned 5-hydroxytryptamine 7 receptor in HEK 293 using [3H]5-CT as a radioligand
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/s0960-894x(02)00690-x
6604889 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Binding affinity for human cloned 5-hydroxytryptamine 7 receptor in HEK 293 using [3H]5-CT as a radioligandBinding affinity for human cloned 5-hydroxytryptamine 7 receptor in HEK 293 using [3H]5-CT as a radioligand
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/s0960-894x(02)00690-x
CHEMBL282199 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Binding affinity for human cloned 5-hydroxytryptamine 7 receptor in HEK 293 using [3H]5-CT as a radioligandBinding affinity for human cloned 5-hydroxytryptamine 7 receptor in HEK 293 using [3H]5-CT as a radioligand
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/s0960-894x(02)00690-x
DB13988 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Binding affinity for human cloned 5-hydroxytryptamine 7 receptor in HEK 293 using [3H]5-CT as a radioligandBinding affinity for human cloned 5-hydroxytryptamine 7 receptor in HEK 293 using [3H]5-CT as a radioligand
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/s0960-894x(02)00690-x
3233 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Binding affinity towards 5-hydroxytryptamine 7 receptor (a) (human cloned receptor) in HEK 293 cells using [3H]5-CT as radioligand.Binding affinity towards 5-hydroxytryptamine 7 receptor (a) (human cloned receptor) in HEK 293 cells using [3H]5-CT as radioligand.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
3247 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Binding affinity towards 5-hydroxytryptamine 7 receptor (a) (human cloned receptor) in HEK 293 cells using [3H]5-CT as radioligand.Binding affinity towards 5-hydroxytryptamine 7 receptor (a) (human cloned receptor) in HEK 293 cells using [3H]5-CT as radioligand.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
6604889 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Binding affinity towards 5-hydroxytryptamine 7 receptor (a) (human cloned receptor) in HEK 293 cells using [3H]5-CT as radioligand.Binding affinity towards 5-hydroxytryptamine 7 receptor (a) (human cloned receptor) in HEK 293 cells using [3H]5-CT as radioligand.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
CHEMBL282199 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Binding affinity towards 5-hydroxytryptamine 7 receptor (a) (human cloned receptor) in HEK 293 cells using [3H]5-CT as radioligand.Binding affinity towards 5-hydroxytryptamine 7 receptor (a) (human cloned receptor) in HEK 293 cells using [3H]5-CT as radioligand.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
DB13988 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Binding affinity towards 5-hydroxytryptamine 7 receptor (a) (human cloned receptor) in HEK 293 cells using [3H]5-CT as radioligand.Binding affinity towards 5-hydroxytryptamine 7 receptor (a) (human cloned receptor) in HEK 293 cells using [3H]5-CT as radioligand.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
3233 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Binding affinity towards cloned human 5-hydroxytryptamine 7 receptor was determined in HEK293 cells using [3H]5-CT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 7 receptor was determined in HEK293 cells using [3H]5-CT as radioligand
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm030841r
3247 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Binding affinity towards cloned human 5-hydroxytryptamine 7 receptor was determined in HEK293 cells using [3H]5-CT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 7 receptor was determined in HEK293 cells using [3H]5-CT as radioligand
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm030841r
6604889 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Binding affinity towards cloned human 5-hydroxytryptamine 7 receptor was determined in HEK293 cells using [3H]5-CT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 7 receptor was determined in HEK293 cells using [3H]5-CT as radioligand
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm030841r
CHEMBL282199 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Binding affinity towards cloned human 5-hydroxytryptamine 7 receptor was determined in HEK293 cells using [3H]5-CT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 7 receptor was determined in HEK293 cells using [3H]5-CT as radioligand
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm030841r
DB13988 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Binding affinity towards cloned human 5-hydroxytryptamine 7 receptor was determined in HEK293 cells using [3H]5-CT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 7 receptor was determined in HEK293 cells using [3H]5-CT as radioligand
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm030841r
3233 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Displacement of [3H]-5-CT from human 5-HT7a receptor expressed in HEK293 cellsDisplacement of [3H]-5-CT from human 5-HT7a receptor expressed in HEK293 cells
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2016.09.019
3247 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Displacement of [3H]-5-CT from human 5-HT7a receptor expressed in HEK293 cellsDisplacement of [3H]-5-CT from human 5-HT7a receptor expressed in HEK293 cells
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2016.09.019
6604889 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Displacement of [3H]-5-CT from human 5-HT7a receptor expressed in HEK293 cellsDisplacement of [3H]-5-CT from human 5-HT7a receptor expressed in HEK293 cells
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2016.09.019
CHEMBL282199 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Displacement of [3H]-5-CT from human 5-HT7a receptor expressed in HEK293 cellsDisplacement of [3H]-5-CT from human 5-HT7a receptor expressed in HEK293 cells
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2016.09.019
DB13988 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Displacement of [3H]-5-CT from human 5-HT7a receptor expressed in HEK293 cellsDisplacement of [3H]-5-CT from human 5-HT7a receptor expressed in HEK293 cells
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2016.09.019
3233 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Binding affinity to 5HT7 receptor (unknown origin)Binding affinity to 5HT7 receptor (unknown origin)
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2013.02.038
3247 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Binding affinity to 5HT7 receptor (unknown origin)Binding affinity to 5HT7 receptor (unknown origin)
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2013.02.038
6604889 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Binding affinity to 5HT7 receptor (unknown origin)Binding affinity to 5HT7 receptor (unknown origin)
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2013.02.038
CHEMBL282199 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Binding affinity to 5HT7 receptor (unknown origin)Binding affinity to 5HT7 receptor (unknown origin)
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2013.02.038
DB13988 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Binding affinity to 5HT7 receptor (unknown origin)Binding affinity to 5HT7 receptor (unknown origin)
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2013.02.038
3233 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Binding affinity to human 5-HT7 receptor by radioligand binding assayBinding affinity to human 5-HT7 receptor by radioligand binding assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.7b01898
3247 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Binding affinity to human 5-HT7 receptor by radioligand binding assayBinding affinity to human 5-HT7 receptor by radioligand binding assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.7b01898
6604889 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Binding affinity to human 5-HT7 receptor by radioligand binding assayBinding affinity to human 5-HT7 receptor by radioligand binding assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.7b01898
CHEMBL282199 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Binding affinity to human 5-HT7 receptor by radioligand binding assayBinding affinity to human 5-HT7 receptor by radioligand binding assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.7b01898
DB13988 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Binding affinity to human 5-HT7 receptor by radioligand binding assayBinding affinity to human 5-HT7 receptor by radioligand binding assay
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.7b01898
3233 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Displacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2014.08.023
3247 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Displacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2014.08.023
6604889 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Displacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2014.08.023
CHEMBL282199 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Displacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2014.08.023
DB13988 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Displacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2014.08.023
3233 3512 None 28 Rat Binding pKi = 8.9 8.9 -2 17
Displacement of [3H]5-HT from rat 5-hydroxytryptamine 7 receptor expressed in CHO cellsDisplacement of [3H]5-HT from rat 5-hydroxytryptamine 7 receptor expressed in CHO cells
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm0108505
3247 3512 None 28 Rat Binding pKi = 8.9 8.9 -2 17
Displacement of [3H]5-HT from rat 5-hydroxytryptamine 7 receptor expressed in CHO cellsDisplacement of [3H]5-HT from rat 5-hydroxytryptamine 7 receptor expressed in CHO cells
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm0108505
6604889 3512 None 28 Rat Binding pKi = 8.9 8.9 -2 17
Displacement of [3H]5-HT from rat 5-hydroxytryptamine 7 receptor expressed in CHO cellsDisplacement of [3H]5-HT from rat 5-hydroxytryptamine 7 receptor expressed in CHO cells
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm0108505
CHEMBL282199 3512 None 28 Rat Binding pKi = 8.9 8.9 -2 17
Displacement of [3H]5-HT from rat 5-hydroxytryptamine 7 receptor expressed in CHO cellsDisplacement of [3H]5-HT from rat 5-hydroxytryptamine 7 receptor expressed in CHO cells
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm0108505
DB13988 3512 None 28 Rat Binding pKi = 8.9 8.9 -2 17
Displacement of [3H]5-HT from rat 5-hydroxytryptamine 7 receptor expressed in CHO cellsDisplacement of [3H]5-HT from rat 5-hydroxytryptamine 7 receptor expressed in CHO cells
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm0108505
24825775 1523 None 16 Human Binding pKi = 8.9 8.9 346 2
Displacement of [3H] D-lysergic acid diethylamide from 5-HT7R (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by microbeta scintillation counter analysisDisplacement of [3H] D-lysergic acid diethylamide from 5-HT7R (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by microbeta scintillation counter analysis
ChEMBL 257 4 0 3 2.8 CN(CCc1cccc(c1)c1c(C)nn(c1C)C)C 10.1021/acs.jmedchem.1c00110
3929 1523 None 16 Human Binding pKi = 8.9 8.9 346 2
Displacement of [3H] D-lysergic acid diethylamide from 5-HT7R (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by microbeta scintillation counter analysisDisplacement of [3H] D-lysergic acid diethylamide from 5-HT7R (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by microbeta scintillation counter analysis
ChEMBL 257 4 0 3 2.8 CN(CCc1cccc(c1)c1c(C)nn(c1C)C)C 10.1021/acs.jmedchem.1c00110
CHEMBL4205349 1523 None 16 Human Binding pKi = 8.9 8.9 346 2
Displacement of [3H] D-lysergic acid diethylamide from 5-HT7R (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by microbeta scintillation counter analysisDisplacement of [3H] D-lysergic acid diethylamide from 5-HT7R (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by microbeta scintillation counter analysis
ChEMBL 257 4 0 3 2.8 CN(CCc1cccc(c1)c1c(C)nn(c1C)C)C 10.1021/acs.jmedchem.1c00110
3233 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Binding affinity towards human 5-hydroxytryptamine 7 receptorBinding affinity towards human 5-hydroxytryptamine 7 receptor
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm030030n
3247 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Binding affinity towards human 5-hydroxytryptamine 7 receptorBinding affinity towards human 5-hydroxytryptamine 7 receptor
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm030030n
6604889 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Binding affinity towards human 5-hydroxytryptamine 7 receptorBinding affinity towards human 5-hydroxytryptamine 7 receptor
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm030030n
CHEMBL282199 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Binding affinity towards human 5-hydroxytryptamine 7 receptorBinding affinity towards human 5-hydroxytryptamine 7 receptor
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm030030n
DB13988 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Binding affinity towards human 5-hydroxytryptamine 7 receptorBinding affinity towards human 5-hydroxytryptamine 7 receptor
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm030030n
15803947 52370 None 1 Human Binding pKi = 8.9 8.9 13 4
Binding affinity towards human 5-hydroxytryptamine 7 receptor by the displacement of [3H]-5-HT radioligand from the cloned receptor expressed in CHO cellsBinding affinity towards human 5-hydroxytryptamine 7 receptor by the displacement of [3H]-5-HT radioligand from the cloned receptor expressed in CHO cells
ChEMBL 161 3 0 2 2.1 CN(C)CCSC(C)(C)C 10.1016/j.bmcl.2003.11.050
CHEMBL158973 52370 None 1 Human Binding pKi = 8.9 8.9 13 4
Binding affinity towards human 5-hydroxytryptamine 7 receptor by the displacement of [3H]-5-HT radioligand from the cloned receptor expressed in CHO cellsBinding affinity towards human 5-hydroxytryptamine 7 receptor by the displacement of [3H]-5-HT radioligand from the cloned receptor expressed in CHO cells
ChEMBL 161 3 0 2 2.1 CN(C)CCSC(C)(C)C 10.1016/j.bmcl.2003.11.050
24825775 1523 None 16 Human Binding pKi = 8.9 8.9 346 2
Displacement of [3H] D-lysergic acid diethylamide from 5-HT7R (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by microbeta scintillation counter analysisDisplacement of [3H] D-lysergic acid diethylamide from 5-HT7R (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by microbeta scintillation counter analysis
ChEMBL 257 4 0 3 2.8 CN(CCc1cccc(c1)c1c(C)nn(c1C)C)C 10.1021/acs.jmedchem.1c00110
3929 1523 None 16 Human Binding pKi = 8.9 8.9 346 2
Displacement of [3H] D-lysergic acid diethylamide from 5-HT7R (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by microbeta scintillation counter analysisDisplacement of [3H] D-lysergic acid diethylamide from 5-HT7R (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by microbeta scintillation counter analysis
ChEMBL 257 4 0 3 2.8 CN(CCc1cccc(c1)c1c(C)nn(c1C)C)C 10.1021/acs.jmedchem.1c00110
CHEMBL4205349 1523 None 16 Human Binding pKi = 8.9 8.9 346 2
Displacement of [3H] D-lysergic acid diethylamide from 5-HT7R (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by microbeta scintillation counter analysisDisplacement of [3H] D-lysergic acid diethylamide from 5-HT7R (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by microbeta scintillation counter analysis
ChEMBL 257 4 0 3 2.8 CN(CCc1cccc(c1)c1c(C)nn(c1C)C)C 10.1021/acs.jmedchem.1c00110
3233 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Displacement of [3H]-5-CT from human 5-HT7a receptor expressed in HEK293 cellsDisplacement of [3H]-5-CT from human 5-HT7a receptor expressed in HEK293 cells
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2016.09.019
3247 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Displacement of [3H]-5-CT from human 5-HT7a receptor expressed in HEK293 cellsDisplacement of [3H]-5-CT from human 5-HT7a receptor expressed in HEK293 cells
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2016.09.019
6604889 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Displacement of [3H]-5-CT from human 5-HT7a receptor expressed in HEK293 cellsDisplacement of [3H]-5-CT from human 5-HT7a receptor expressed in HEK293 cells
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2016.09.019
CHEMBL282199 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Displacement of [3H]-5-CT from human 5-HT7a receptor expressed in HEK293 cellsDisplacement of [3H]-5-CT from human 5-HT7a receptor expressed in HEK293 cells
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2016.09.019
DB13988 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
Displacement of [3H]-5-CT from human 5-HT7a receptor expressed in HEK293 cellsDisplacement of [3H]-5-CT from human 5-HT7a receptor expressed in HEK293 cells
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.bmc.2016.09.019
118717223 120646 None 0 Human Binding pKi = 8.9 8.9 7 2
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cells
ChEMBL 321 1 2 2 2.2 NC(N)=NC(=O)c1ccc2c(c1)C1(CCOCC1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
CHEMBL3343671 120646 None 0 Human Binding pKi = 8.9 8.9 7 2
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cells
ChEMBL 321 1 2 2 2.2 NC(N)=NC(=O)c1ccc2c(c1)C1(CCOCC1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
CHEMBL3545813 120646 None 0 Human Binding pKi = 8.9 8.9 7 2
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cells
ChEMBL 321 1 2 2 2.2 NC(N)=NC(=O)c1ccc2c(c1)C1(CCOCC1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
56944859 112171 None 0 Human Binding pKi = 8.9 8.9 -1 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 453 6 1 5 4.3 O=S(=O)(NCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cccc2ccccc12 10.1021/jm401895u
CHEMBL3290001 112171 None 0 Human Binding pKi = 8.9 8.9 -1 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 453 6 1 5 4.3 O=S(=O)(NCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cccc2ccccc12 10.1021/jm401895u
56944384 112184 None 0 Human Binding pKi = 8.9 8.9 -1 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 521 8 1 6 5.8 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccc(Cl)cc2s1 10.1021/jm401895u
CHEMBL3290014 112184 None 0 Human Binding pKi = 8.9 8.9 -1 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 521 8 1 6 5.8 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccc(Cl)cc2s1 10.1021/jm401895u
66801565 112190 None 0 Human Binding pKi = 8.9 8.9 7 3
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 474 7 1 7 4.1 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cccc2scnc12 10.1021/jm401895u
CHEMBL3290020 112190 None 0 Human Binding pKi = 8.9 8.9 7 3
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 474 7 1 7 4.1 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cccc2scnc12 10.1021/jm401895u
3233 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.6019/CHEMBL5442175
3247 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.6019/CHEMBL5442175
6604889 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.6019/CHEMBL5442175
CHEMBL282199 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.6019/CHEMBL5442175
DB13988 3512 None 28 Human Binding pKi = 8.9 8.9 2 17
PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.6019/CHEMBL5442175
2389 3331 None 72 Rat Binding pKi = 8.9 8.9 -7 67
Binding affinity towards rat 5-hydroxytryptamine 7 receptorBinding affinity towards rat 5-hydroxytryptamine 7 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm030030n
5073 3331 None 72 Rat Binding pKi = 8.9 8.9 -7 67
Binding affinity towards rat 5-hydroxytryptamine 7 receptorBinding affinity towards rat 5-hydroxytryptamine 7 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm030030n
5073.0 3331 None 72 Rat Binding pKi = 8.9 8.9 -7 67
Binding affinity towards rat 5-hydroxytryptamine 7 receptorBinding affinity towards rat 5-hydroxytryptamine 7 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm030030n
96 3331 None 72 Rat Binding pKi = 8.9 8.9 -7 67
Binding affinity towards rat 5-hydroxytryptamine 7 receptorBinding affinity towards rat 5-hydroxytryptamine 7 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm030030n
CHEMBL85 3331 None 72 Rat Binding pKi = 8.9 8.9 -7 67
Binding affinity towards rat 5-hydroxytryptamine 7 receptorBinding affinity towards rat 5-hydroxytryptamine 7 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm030030n
DB00734 3331 None 72 Rat Binding pKi = 8.9 8.9 -7 67
Binding affinity towards rat 5-hydroxytryptamine 7 receptorBinding affinity towards rat 5-hydroxytryptamine 7 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm030030n
60196080 81838 None 1 Human Binding pKi = 8.9 8.9 12 2
Displacement of [3H]-5-CT from human cloned 5HT7 receptorDisplacement of [3H]-5-CT from human cloned 5HT7 receptor
ChEMBL 252 2 1 2 3.1 Cc1ccccc1-c1cccc(N2CCNCC2)c1 10.1021/jm3003679
CHEMBL2164330 81838 None 1 Human Binding pKi = 8.9 8.9 12 2
Displacement of [3H]-5-CT from human cloned 5HT7 receptorDisplacement of [3H]-5-CT from human cloned 5HT7 receptor
ChEMBL 252 2 1 2 3.1 Cc1ccccc1-c1cccc(N2CCNCC2)c1 10.1021/jm3003679
2737389 187692 None 22 Human Binding pKi = 8.9 8.9 53 5
Displacement of [3H]-5-CT from human cloned 5HT7 receptorDisplacement of [3H]-5-CT from human cloned 5HT7 receptor
ChEMBL 238 2 1 2 2.8 c1ccc(-c2ccccc2N2CCNCC2)cc1 10.1021/jm3003679
CHEMBL494675 187692 None 22 Human Binding pKi = 8.9 8.9 53 5
Displacement of [3H]-5-CT from human cloned 5HT7 receptorDisplacement of [3H]-5-CT from human cloned 5HT7 receptor
ChEMBL 238 2 1 2 2.8 c1ccc(-c2ccccc2N2CCNCC2)cc1 10.1021/jm3003679
11637931 120647 None 0 Human Binding pKi = 8.9 8.9 2 2
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cells
ChEMBL 295 2 2 2 2.0 COC1(C)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
CHEMBL3343665 120647 None 0 Human Binding pKi = 8.9 8.9 2 2
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cells
ChEMBL 295 2 2 2 2.0 COC1(C)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
CHEMBL3545814 120647 None 0 Human Binding pKi = 8.9 8.9 2 2
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cells
ChEMBL 295 2 2 2 2.0 COC1(C)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
5 139 None 45 Human Binding pKi = 8.9 8.9 -3 54
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in HEK293 cells after 30 mins by microbeta counting analysisDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in HEK293 cells after 30 mins by microbeta counting analysis
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2014.04.034
5202 139 None 45 Human Binding pKi = 8.9 8.9 -3 54
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in HEK293 cells after 30 mins by microbeta counting analysisDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in HEK293 cells after 30 mins by microbeta counting analysis
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2014.04.034
CHEMBL39 139 None 45 Human Binding pKi = 8.9 8.9 -3 54
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in HEK293 cells after 30 mins by microbeta counting analysisDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in HEK293 cells after 30 mins by microbeta counting analysis
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2014.04.034
DB08839 139 None 45 Human Binding pKi = 8.9 8.9 -3 54
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in HEK293 cells after 30 mins by microbeta counting analysisDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in HEK293 cells after 30 mins by microbeta counting analysis
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2014.04.034
56944666 112176 None 0 Human Binding pKi = 8.9 8.9 -1 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 481 8 1 5 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
CHEMBL3290006 112176 None 0 Human Binding pKi = 8.9 8.9 -1 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 481 8 1 5 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
2737389 187692 None 22 Human Binding pKi = 8.9 8.9 53 5
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysis
ChEMBL 238 2 1 2 2.8 c1ccc(-c2ccccc2N2CCNCC2)cc1 10.1039/C8MD00313K
CHEMBL494675 187692 None 22 Human Binding pKi = 8.9 8.9 53 5
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysis
ChEMBL 238 2 1 2 2.8 c1ccc(-c2ccccc2N2CCNCC2)cc1 10.1039/C8MD00313K
162643494 181755 None 0 Human Binding pKi = 8.8 8.8 3 4
Displacement of [3H]-LSD from recombinant human 5HT7 receptor expressed in CHOK1 cell membranes measured after 120 mins by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT7 receptor expressed in CHOK1 cell membranes measured after 120 mins by microbeta counting method
ChEMBL 437 7 1 5 3.6 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1ccc(F)c(Cl)c1 10.1016/j.ejmech.2020.112149
CHEMBL4775997 181755 None 0 Human Binding pKi = 8.8 8.8 3 4
Displacement of [3H]-LSD from recombinant human 5HT7 receptor expressed in CHOK1 cell membranes measured after 120 mins by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT7 receptor expressed in CHOK1 cell membranes measured after 120 mins by microbeta counting method
ChEMBL 437 7 1 5 3.6 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1ccc(F)c(Cl)c1 10.1016/j.ejmech.2020.112149
24854111 95812 None 0 Human Binding pKi = 8.8 8.8 - 1
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 425 8 1 3 5.3 CCC1(CCCCCN2CCN(c3cccc(Cl)c3)CC2)C(=O)Nc2ccccc21 10.1021/jm070279v
CHEMBL258496 95812 None 0 Human Binding pKi = 8.8 8.8 - 1
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 425 8 1 3 5.3 CCC1(CCCCCN2CCN(c3cccc(Cl)c3)CC2)C(=O)Nc2ccccc21 10.1021/jm070279v
66801229 112120 None 0 Human Binding pKi = 8.8 8.8 -1 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 452 6 1 6 3.6 O=S(=O)(NCCN1CCN(c2nsc3ccccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
CHEMBL3289952 112120 None 0 Human Binding pKi = 8.8 8.8 -1 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 452 6 1 6 3.6 O=S(=O)(NCCN1CCN(c2nsc3ccccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
66800939 112121 None 0 Human Binding pKi = 8.8 8.8 1 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 466 7 1 6 3.9 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
CHEMBL3289953 112121 None 0 Human Binding pKi = 8.8 8.8 1 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 466 7 1 6 3.9 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
56944667 112161 None 0 Human Binding pKi = 8.8 8.8 1 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 445 8 1 5 4.2 Cc1cccc(S(=O)(=O)NCCCCN2CCC(c3noc4cc(F)ccc34)CC2)c1 10.1021/jm401895u
CHEMBL3289992 112161 None 0 Human Binding pKi = 8.8 8.8 1 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 445 8 1 5 4.2 Cc1cccc(S(=O)(=O)NCCCCN2CCC(c3noc4cc(F)ccc34)CC2)c1 10.1021/jm401895u
24854183 95955 None 0 Human Binding pKi = 8.8 8.8 - 1
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 413 7 1 3 4.6 CCC1(CCCCN2CCN(c3ccc(F)cc3)CC2)C(=O)Nc2ccc(F)cc21 10.1021/jm070279v
CHEMBL259216 95955 None 0 Human Binding pKi = 8.8 8.8 - 1
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 413 7 1 3 4.6 CCC1(CCCCN2CCN(c3ccc(F)cc3)CC2)C(=O)Nc2ccc(F)cc21 10.1021/jm070279v
CHEMBL5094234 218063 None 0 Human Binding pKi = 8.8 8.8 2 8
Displacement of [3H] D-lysergic acid diethylamide from 5-HT7R (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by microbeta scintillation counter analysisDisplacement of [3H] D-lysergic acid diethylamide from 5-HT7R (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by microbeta scintillation counter analysis
ChEMBL None None None CCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5096019 218063 None 0 Human Binding pKi = 8.8 8.8 2 8
Displacement of [3H] D-lysergic acid diethylamide from 5-HT7R (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by microbeta scintillation counter analysisDisplacement of [3H] D-lysergic acid diethylamide from 5-HT7R (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by microbeta scintillation counter analysis
ChEMBL None None None CCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
134155116 151057 None 0 Human Binding pKi = 8.8 8.8 12 7
Displacement of [3H]-LSD from human 5-HT7 receptor by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT7 receptor by liquid scintillation counting method
ChEMBL 309 3 0 2 3.6 O=C1c2ccc(F)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
CHEMBL3958215 151057 None 0 Human Binding pKi = 8.8 8.8 12 7
Displacement of [3H]-LSD from human 5-HT7 receptor by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT7 receptor by liquid scintillation counting method
ChEMBL 309 3 0 2 3.6 O=C1c2ccc(F)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
CHEMBL5091373 218057 None 0 Human Binding pKi = 8.8 8.8 1 9
Displacement of [3H] D-lysergic acid diethylamide from 5-HT7R (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by microbeta scintillation counter analysisDisplacement of [3H] D-lysergic acid diethylamide from 5-HT7R (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by microbeta scintillation counter analysis
ChEMBL None None None CNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5095981 218057 None 0 Human Binding pKi = 8.8 8.8 1 9
Displacement of [3H] D-lysergic acid diethylamide from 5-HT7R (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by microbeta scintillation counter analysisDisplacement of [3H] D-lysergic acid diethylamide from 5-HT7R (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by microbeta scintillation counter analysis
ChEMBL None None None CNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
134155116 151057 None 0 Human Binding pKi = 8.8 8.8 12 7
Displacement of [3H]-LSD from human 5-HT7 receptor by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT7 receptor by liquid scintillation counting method
ChEMBL 309 3 0 2 3.6 O=C1c2ccc(F)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
CHEMBL3958215 151057 None 0 Human Binding pKi = 8.8 8.8 12 7
Displacement of [3H]-LSD from human 5-HT7 receptor by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT7 receptor by liquid scintillation counting method
ChEMBL 309 3 0 2 3.6 O=C1c2ccc(F)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
132525570 163740 None 0 Human Binding pKi = 8.8 8.8 6 5
Displacement of [3H]5-CT from human 5-HT7b receptor expressed in HEK293 cell membranesDisplacement of [3H]5-CT from human 5-HT7b receptor expressed in HEK293 cell membranes
ChEMBL 300 5 0 5 2.8 CCCCc1cc(-c2ccoc2)nc(N2CCN(C)CC2)n1 10.1021/acs.jmedchem.7b01898
CHEMBL4204059 163740 None 0 Human Binding pKi = 8.8 8.8 6 5
Displacement of [3H]5-CT from human 5-HT7b receptor expressed in HEK293 cell membranesDisplacement of [3H]5-CT from human 5-HT7b receptor expressed in HEK293 cell membranes
ChEMBL 300 5 0 5 2.8 CCCCc1cc(-c2ccoc2)nc(N2CCN(C)CC2)n1 10.1021/acs.jmedchem.7b01898
56944565 112112 None 0 Human Binding pKi = 8.8 8.8 -3 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 444 8 1 6 3.5 Cc1cccc(S(=O)(=O)NCCCCN2CCN(c3nsc4ccccc34)CC2)c1 10.1021/jm401895u
CHEMBL3289944 112112 None 0 Human Binding pKi = 8.8 8.8 -3 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 444 8 1 6 3.5 Cc1cccc(S(=O)(=O)NCCCCN2CCN(c3nsc4ccccc34)CC2)c1 10.1021/jm401895u
56944383 112182 None 0 Human Binding pKi = 8.8 8.8 -3 12
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 487 8 1 6 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
CHEMBL3290012 112182 None 0 Human Binding pKi = 8.8 8.8 -3 12
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 487 8 1 6 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
44437330 152278 None 0 Rat Binding pKi = 8.8 8.8 - 1
Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells at 10 uMDisplacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells at 10 uM
ChEMBL 706 19 0 8 7.5 COc1ccccc1N1CCN(CCc2cccc(OCCCCCCOc3cccc(CCN4CCN(c5ccccc5OC)CC4)c3)c2)CC1 10.1016/j.bmc.2007.05.010
CHEMBL396844 152278 None 0 Rat Binding pKi = 8.8 8.8 - 1
Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells at 10 uMDisplacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells at 10 uM
ChEMBL 706 19 0 8 7.5 COc1ccccc1N1CCN(CCc2cccc(OCCCCCCOc3cccc(CCN4CCN(c5ccccc5OC)CC4)c3)c2)CC1 10.1016/j.bmc.2007.05.010
44266268 210256 None 0 Human Binding pKi = 8.8 8.8 10 2
Binding affinity at human cloned 5-hydroxytryptamine 7 receptor.Binding affinity at human cloned 5-hydroxytryptamine 7 receptor.
ChEMBL 394 5 0 3 3.8 O=C(c1ccc(F)cc1)C1CCN(CCN2CCCc3ccccc3C2=O)CC1 10.1016/s0960-894x(03)00077-5
CHEMBL9616 210256 None 0 Human Binding pKi = 8.8 8.8 10 2
Binding affinity at human cloned 5-hydroxytryptamine 7 receptor.Binding affinity at human cloned 5-hydroxytryptamine 7 receptor.
ChEMBL 394 5 0 3 3.8 O=C(c1ccc(F)cc1)C1CCN(CCN2CCCc3ccccc3C2=O)CC1 10.1016/s0960-894x(03)00077-5
162652285 180381 None 0 Human Binding pKi = 8.8 8.8 2 4
Displacement of [3H]-LSD from recombinant human 5HT7 receptor expressed in CHOK1 cell membranes measured after 120 mins by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT7 receptor expressed in CHOK1 cell membranes measured after 120 mins by microbeta counting method
ChEMBL 399 7 1 5 3.1 Cc1cccc(S(=O)(=O)N[C@@H]2CCN(CCCc3noc4ccccc34)C2)c1 10.1016/j.ejmech.2020.112149
CHEMBL4750664 180381 None 0 Human Binding pKi = 8.8 8.8 2 4
Displacement of [3H]-LSD from recombinant human 5HT7 receptor expressed in CHOK1 cell membranes measured after 120 mins by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT7 receptor expressed in CHOK1 cell membranes measured after 120 mins by microbeta counting method
ChEMBL 399 7 1 5 3.1 Cc1cccc(S(=O)(=O)N[C@@H]2CCN(CCCc3noc4ccccc34)C2)c1 10.1016/j.ejmech.2020.112149
162654074 180685 None 0 Human Binding pKi = 8.8 8.8 -3 4
Displacement of [3H]-LSD from recombinant human 5HT7 receptor expressed in CHOK1 cell membranes measured after 120 mins by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT7 receptor expressed in CHOK1 cell membranes measured after 120 mins by microbeta counting method
ChEMBL 435 7 1 5 4.0 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1cccc2ccccc12 10.1016/j.ejmech.2020.112149
CHEMBL4754138 180685 None 0 Human Binding pKi = 8.8 8.8 -3 4
Displacement of [3H]-LSD from recombinant human 5HT7 receptor expressed in CHOK1 cell membranes measured after 120 mins by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT7 receptor expressed in CHOK1 cell membranes measured after 120 mins by microbeta counting method
ChEMBL 435 7 1 5 4.0 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1cccc2ccccc12 10.1016/j.ejmech.2020.112149
11500509 120645 None 0 Human Binding pKi = 8.8 8.8 3 3
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cells
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 120645 None 0 Human Binding pKi = 8.8 8.8 3 3
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cells
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 120645 None 0 Human Binding pKi = 8.8 8.8 3 3
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cells
ChEMBL 307 1 2 2 2.1 NC(N)=NC(=O)c1ccc2c(c1)C1(CCCO1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
66801107 112109 None 0 Human Binding pKi = 8.8 8.8 -1 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 430 7 1 6 3.1 Cc1cccc(S(=O)(=O)NCCCN2CCN(c3nsc4ccccc34)CC2)c1 10.1021/jm401895u
CHEMBL3289709 112109 None 0 Human Binding pKi = 8.8 8.8 -1 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 430 7 1 6 3.1 Cc1cccc(S(=O)(=O)NCCCN2CCN(c3nsc4ccccc34)CC2)c1 10.1021/jm401895u
4106 2502 None 21 Human Binding pKi = 8.8 8.8 -4 33
Displacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2018.04.059
5358812 2502 None 21 Human Binding pKi = 8.8 8.8 -4 33
Displacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2018.04.059
89 2502 None 21 Human Binding pKi = 8.8 8.8 -4 33
Displacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2018.04.059
CHEMBL93240 2502 None 21 Human Binding pKi = 8.8 8.8 -4 33
Displacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2018.04.059
4106 2502 None 21 Human Binding pKi = 8.8 8.8 -4 33
Displacement of [3H]SB269970 from human 5-HT7 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysisDisplacement of [3H]SB269970 from human 5-HT7 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysis
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmc.2023.117256
5358812 2502 None 21 Human Binding pKi = 8.8 8.8 -4 33
Displacement of [3H]SB269970 from human 5-HT7 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysisDisplacement of [3H]SB269970 from human 5-HT7 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysis
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmc.2023.117256
89 2502 None 21 Human Binding pKi = 8.8 8.8 -4 33
Displacement of [3H]SB269970 from human 5-HT7 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysisDisplacement of [3H]SB269970 from human 5-HT7 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysis
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmc.2023.117256
CHEMBL93240 2502 None 21 Human Binding pKi = 8.8 8.8 -4 33
Displacement of [3H]SB269970 from human 5-HT7 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysisDisplacement of [3H]SB269970 from human 5-HT7 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysis
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmc.2023.117256
118713592 114442 None 0 Human Binding pKi = 8.8 8.8 3 2
Displacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry
ChEMBL 401 6 0 5 4.3 O=c1sc2ccccc2n1CCCCN1CCN(c2cccc(Cl)c2)CC1 10.1016/j.ejmech.2014.08.023
CHEMBL3331261 114442 None 0 Human Binding pKi = 8.8 8.8 3 2
Displacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry
ChEMBL 401 6 0 5 4.3 O=c1sc2ccccc2n1CCCCN1CCN(c2cccc(Cl)c2)CC1 10.1016/j.ejmech.2014.08.023
11187960 66251 None 0 Rat Binding pKi = 8.8 8.8 6 2
Inhibition of [3H]-5-HT binding to rat 5-hydroxytryptamine 7 receptorInhibition of [3H]-5-HT binding to rat 5-hydroxytryptamine 7 receptor
ChEMBL 337 7 0 2 5.3 CCCN(CCC)[C@H]1CCc2c(cccc2-c2ccccc2OC)C1 10.1021/jm0498102
CHEMBL184535 66251 None 0 Rat Binding pKi = 8.8 8.8 6 2
Inhibition of [3H]-5-HT binding to rat 5-hydroxytryptamine 7 receptorInhibition of [3H]-5-HT binding to rat 5-hydroxytryptamine 7 receptor
ChEMBL 337 7 0 2 5.3 CCCN(CCC)[C@H]1CCc2c(cccc2-c2ccccc2OC)C1 10.1021/jm0498102
44437329 151689 None 0 Rat Binding pKi = 8.8 8.8 -8 2
Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells at 10 uMDisplacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells at 10 uM
ChEMBL 692 18 0 8 7.1 COc1ccccc1N1CCN(CCc2cccc(OCCCCCOc3cccc(CCN4CCN(c5ccccc5OC)CC4)c3)c2)CC1 10.1016/j.bmc.2007.05.010
CHEMBL396349 151689 None 0 Rat Binding pKi = 8.8 8.8 -8 2
Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells at 10 uMDisplacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells at 10 uM
ChEMBL 692 18 0 8 7.1 COc1ccccc1N1CCN(CCc2cccc(OCCCCCOc3cccc(CCN4CCN(c5ccccc5OC)CC4)c3)c2)CC1 10.1016/j.bmc.2007.05.010
1809 134 None 25 Rat Binding pKi = 8.7 8.7 -2 37
Displacement of [3H]-5-CT from 5-HT7 receptor in Sprague-Dawley rat hypothalamus after 120 minsDisplacement of [3H]-5-CT from 5-HT7 receptor in Sprague-Dawley rat hypothalamus after 120 mins
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm400766k
4 134 None 25 Rat Binding pKi = 8.7 8.7 -2 37
Displacement of [3H]-5-CT from 5-HT7 receptor in Sprague-Dawley rat hypothalamus after 120 minsDisplacement of [3H]-5-CT from 5-HT7 receptor in Sprague-Dawley rat hypothalamus after 120 mins
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm400766k
CHEMBL18840 134 None 25 Rat Binding pKi = 8.7 8.7 -2 37
Displacement of [3H]-5-CT from 5-HT7 receptor in Sprague-Dawley rat hypothalamus after 120 minsDisplacement of [3H]-5-CT from 5-HT7 receptor in Sprague-Dawley rat hypothalamus after 120 mins
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm400766k
118717220 120644 None 0 Human Binding pKi = 8.7 8.7 -1 2
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cells
ChEMBL 305 1 2 1 2.9 NC(N)=NC(=O)c1ccc2c(c1)C1(CCCC1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
CHEMBL3343669 120644 None 0 Human Binding pKi = 8.7 8.7 -1 2
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cells
ChEMBL 305 1 2 1 2.9 NC(N)=NC(=O)c1ccc2c(c1)C1(CCCC1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
CHEMBL3545811 120644 None 0 Human Binding pKi = 8.7 8.7 -1 2
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cells
ChEMBL 305 1 2 1 2.9 NC(N)=NC(=O)c1ccc2c(c1)C1(CCCC1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
56944564 112122 None 0 Human Binding pKi = 8.7 8.7 -2 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 480 8 1 6 4.3 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
CHEMBL3289954 112122 None 0 Human Binding pKi = 8.7 8.7 -2 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 480 8 1 6 4.3 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
24854185 157800 None 0 Human Binding pKi = 8.7 8.7 - 1
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 439 8 1 3 5.6 CC(C)CC1(CCCCN2CCN(c3cccc(Cl)c3)CC2)C(=O)Nc2ccccc21 10.1021/jm070279v
CHEMBL408191 157800 None 0 Human Binding pKi = 8.7 8.7 - 1
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 439 8 1 3 5.6 CC(C)CC1(CCCCN2CCN(c3cccc(Cl)c3)CC2)C(=O)Nc2ccccc21 10.1021/jm070279v
44340834 110281 None 0 Human Binding pKi = 8.7 8.7 169 2
Binding affinity for human cloned 5-hydroxytryptamine 7 receptor in HEK 293 using [3H]5-CT as a radioligandBinding affinity for human cloned 5-hydroxytryptamine 7 receptor in HEK 293 using [3H]5-CT as a radioligand
ChEMBL 494 6 1 6 4.0 O=c1oc2ccccc2n1C1CCN(CC[C@H]2CCCN2S(=O)(=O)c2ccc3cc[nH]c3c2)CC1 10.1016/s0960-894x(02)00690-x
CHEMBL323778 110281 None 0 Human Binding pKi = 8.7 8.7 169 2
Binding affinity for human cloned 5-hydroxytryptamine 7 receptor in HEK 293 using [3H]5-CT as a radioligandBinding affinity for human cloned 5-hydroxytryptamine 7 receptor in HEK 293 using [3H]5-CT as a radioligand
ChEMBL 494 6 1 6 4.0 O=c1oc2ccccc2n1C1CCN(CC[C@H]2CCCN2S(=O)(=O)c2ccc3cc[nH]c3c2)CC1 10.1016/s0960-894x(02)00690-x
155567938 176138 None 0 Human Binding pKi = 8.7 8.7 20 2
Displacement of [3H]-5-HT from human 5HT7 receptor expressed in CHO-K1 cells incubated for 40 mins in presence of serotonin by liquid scintillation counterDisplacement of [3H]-5-HT from human 5HT7 receptor expressed in CHO-K1 cells incubated for 40 mins in presence of serotonin by liquid scintillation counter
ChEMBL 386 8 2 5 2.8 NC(=O)c1sccc1NC(=O)CCCCN1CCN(c2ccccc2)CC1 10.1016/j.ejmech.2019.111690
CHEMBL4590226 176138 None 0 Human Binding pKi = 8.7 8.7 20 2
Displacement of [3H]-5-HT from human 5HT7 receptor expressed in CHO-K1 cells incubated for 40 mins in presence of serotonin by liquid scintillation counterDisplacement of [3H]-5-HT from human 5HT7 receptor expressed in CHO-K1 cells incubated for 40 mins in presence of serotonin by liquid scintillation counter
ChEMBL 386 8 2 5 2.8 NC(=O)c1sccc1NC(=O)CCCCN1CCN(c2ccccc2)CC1 10.1016/j.ejmech.2019.111690
10834268 166922 None 0 Human Binding pKi = 8.7 8.7 - 1
Binding affinity to human recombinant 5-hydroxytryptamine 7 receptor in mammalian cells using [3H]5-CT as radioligandBinding affinity to human recombinant 5-hydroxytryptamine 7 receptor in mammalian cells using [3H]5-CT as radioligand
ChEMBL 390 6 1 4 3.6 O=C1Nc2cccc3c2C1(CCCCN1CCN(c2ccccn2)CC1)CCC3 10.1021/jm0104264
CHEMBL428494 166922 None 0 Human Binding pKi = 8.7 8.7 - 1
Binding affinity to human recombinant 5-hydroxytryptamine 7 receptor in mammalian cells using [3H]5-CT as radioligandBinding affinity to human recombinant 5-hydroxytryptamine 7 receptor in mammalian cells using [3H]5-CT as radioligand
ChEMBL 390 6 1 4 3.6 O=C1Nc2cccc3c2C1(CCCCN1CCN(c2ccccn2)CC1)CCC3 10.1021/jm0104264
10834268 166922 None 0 Human Binding pKi = 8.7 8.7 - 1
Compound was evaluated for its ability to displace [3H]5-CT binding from cloned human 5-hydroxytryptamine 7 receptor expressed in COS-7 cells.Compound was evaluated for its ability to displace [3H]5-CT binding from cloned human 5-hydroxytryptamine 7 receptor expressed in COS-7 cells.
ChEMBL 390 6 1 4 3.6 O=C1Nc2cccc3c2C1(CCCCN1CCN(c2ccccn2)CC1)CCC3 10.1021/jm980519u
CHEMBL428494 166922 None 0 Human Binding pKi = 8.7 8.7 - 1
Compound was evaluated for its ability to displace [3H]5-CT binding from cloned human 5-hydroxytryptamine 7 receptor expressed in COS-7 cells.Compound was evaluated for its ability to displace [3H]5-CT binding from cloned human 5-hydroxytryptamine 7 receptor expressed in COS-7 cells.
ChEMBL 390 6 1 4 3.6 O=C1Nc2cccc3c2C1(CCCCN1CCN(c2ccccn2)CC1)CCC3 10.1021/jm980519u
168288462 191814 None 0 Human Binding pKi = 8.7 8.7 2 2
Binding affinity to human recombinant 5-HT7 receptor expressed in CHO cells assessed as inhibition constantBinding affinity to human recombinant 5-HT7 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 461 8 0 5 3.6 COc1ccccc1N1CCN(CCC[C@H]2CCCN2S(=O)(=O)c2ccccc2F)CC1 10.1021/acs.jmedchem.2c00633
CHEMBL5196950 191814 None 0 Human Binding pKi = 8.7 8.7 2 2
Binding affinity to human recombinant 5-HT7 receptor expressed in CHO cells assessed as inhibition constantBinding affinity to human recombinant 5-HT7 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 461 8 0 5 3.6 COc1ccccc1N1CCN(CCC[C@H]2CCCN2S(=O)(=O)c2ccccc2F)CC1 10.1021/acs.jmedchem.2c00633
60195993 81842 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [3H]-5-CT from human cloned 5HT7 receptorDisplacement of [3H]-5-CT from human cloned 5HT7 receptor
ChEMBL 266 2 1 2 3.4 Cc1ccc(-c2ccccc2N2CCNCC2)cc1C 10.1021/jm3003679
CHEMBL2164334 81842 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [3H]-5-CT from human cloned 5HT7 receptorDisplacement of [3H]-5-CT from human cloned 5HT7 receptor
ChEMBL 266 2 1 2 3.4 Cc1ccc(-c2ccccc2N2CCNCC2)cc1C 10.1021/jm3003679
3233 3512 None 28 Human Binding pKi = 8.7 8.7 2 17
Displacement of [3H]-5-HT from human 5HT7 receptor expressed in CHO-K1 cells incubated for 40 mins in presence of serotonin by liquid scintillation counterDisplacement of [3H]-5-HT from human 5HT7 receptor expressed in CHO-K1 cells incubated for 40 mins in presence of serotonin by liquid scintillation counter
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2019.111690
3247 3512 None 28 Human Binding pKi = 8.7 8.7 2 17
Displacement of [3H]-5-HT from human 5HT7 receptor expressed in CHO-K1 cells incubated for 40 mins in presence of serotonin by liquid scintillation counterDisplacement of [3H]-5-HT from human 5HT7 receptor expressed in CHO-K1 cells incubated for 40 mins in presence of serotonin by liquid scintillation counter
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2019.111690
6604889 3512 None 28 Human Binding pKi = 8.7 8.7 2 17
Displacement of [3H]-5-HT from human 5HT7 receptor expressed in CHO-K1 cells incubated for 40 mins in presence of serotonin by liquid scintillation counterDisplacement of [3H]-5-HT from human 5HT7 receptor expressed in CHO-K1 cells incubated for 40 mins in presence of serotonin by liquid scintillation counter
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2019.111690
CHEMBL282199 3512 None 28 Human Binding pKi = 8.7 8.7 2 17
Displacement of [3H]-5-HT from human 5HT7 receptor expressed in CHO-K1 cells incubated for 40 mins in presence of serotonin by liquid scintillation counterDisplacement of [3H]-5-HT from human 5HT7 receptor expressed in CHO-K1 cells incubated for 40 mins in presence of serotonin by liquid scintillation counter
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2019.111690
DB13988 3512 None 28 Human Binding pKi = 8.7 8.7 2 17
Displacement of [3H]-5-HT from human 5HT7 receptor expressed in CHO-K1 cells incubated for 40 mins in presence of serotonin by liquid scintillation counterDisplacement of [3H]-5-HT from human 5HT7 receptor expressed in CHO-K1 cells incubated for 40 mins in presence of serotonin by liquid scintillation counter
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1016/j.ejmech.2019.111690
56944383 112182 None 0 Human Binding pKi = 8.7 8.7 -3 12
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 487 8 1 6 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
CHEMBL3290012 112182 None 0 Human Binding pKi = 8.7 8.7 -3 12
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 487 8 1 6 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
24854105 158025 None 0 Human Binding pKi = 8.7 8.7 - 1
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 401 6 1 3 4.5 O=C1Nc2ccc(F)cc2C1CCCCN1CCN(c2cccc(Cl)c2)CC1 10.1021/jm070279v
CHEMBL408450 158025 None 0 Human Binding pKi = 8.7 8.7 - 1
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 401 6 1 3 4.5 O=C1Nc2ccc(F)cc2C1CCCCN1CCN(c2cccc(Cl)c2)CC1 10.1021/jm070279v
155542678 173265 None 0 Human Binding pKi = 8.7 8.7 281 2
Antagonist activity at 5-HT7 receptor (unknown origin)Antagonist activity at 5-HT7 receptor (unknown origin)
ChEMBL 487 7 1 4 4.9 O=S(=O)(c1ccc2cc[nH]c2c1)N1CCC[C@H]1CCN1CCC(Oc2ccc(Cl)cc2)CC1 10.1016/j.ejmech.2019.111705
CHEMBL4521657 173265 None 0 Human Binding pKi = 8.7 8.7 281 2
Antagonist activity at 5-HT7 receptor (unknown origin)Antagonist activity at 5-HT7 receptor (unknown origin)
ChEMBL 487 7 1 4 4.9 O=S(=O)(c1ccc2cc[nH]c2c1)N1CCC[C@H]1CCN1CCC(Oc2ccc(Cl)cc2)CC1 10.1016/j.ejmech.2019.111705
10028436 3532 None 9 Rat Binding pKi = 8.7 8.7 1 12
Binding affinity for rat serotonin 5-HT7 receptor expressed in Sf9 cells using [3H]5-HT radioligandBinding affinity for rat serotonin 5-HT7 receptor expressed in Sf9 cells using [3H]5-HT radioligand
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/j.bmcl.2004.11.013
3237 3532 None 9 Rat Binding pKi = 8.7 8.7 1 12
Binding affinity for rat serotonin 5-HT7 receptor expressed in Sf9 cells using [3H]5-HT radioligandBinding affinity for rat serotonin 5-HT7 receptor expressed in Sf9 cells using [3H]5-HT radioligand
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/j.bmcl.2004.11.013
CHEMBL95104 3532 None 9 Rat Binding pKi = 8.7 8.7 1 12
Binding affinity for rat serotonin 5-HT7 receptor expressed in Sf9 cells using [3H]5-HT radioligandBinding affinity for rat serotonin 5-HT7 receptor expressed in Sf9 cells using [3H]5-HT radioligand
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/j.bmcl.2004.11.013
44396223 123877 None 0 Rat Binding pKi = 8.7 8.7 281 2
Inhibition of [3H]-5-HT binding to rat 5-hydroxytryptamine 7 receptorInhibition of [3H]-5-HT binding to rat 5-hydroxytryptamine 7 receptor
ChEMBL 486 7 0 4 5.0 O=S(=O)(c1ccc2c(c1)CC=C2)N1CCC[C@@H]1CCN1CCC(Oc2ccc(Cl)cc2)CC1 10.1021/jm0498102
CHEMBL362354 123877 None 0 Rat Binding pKi = 8.7 8.7 281 2
Inhibition of [3H]-5-HT binding to rat 5-hydroxytryptamine 7 receptorInhibition of [3H]-5-HT binding to rat 5-hydroxytryptamine 7 receptor
ChEMBL 486 7 0 4 5.0 O=S(=O)(c1ccc2c(c1)CC=C2)N1CCC[C@@H]1CCN1CCC(Oc2ccc(Cl)cc2)CC1 10.1021/jm0498102
10573876 10465 None 0 Human Binding pKi = 8.7 8.7 199 7
Binding affinity towards 5-hydroxytryptamine 7 receptor (a) (human cloned receptor) in HEK 293 cells using [3H]5-CT as radioligand.Binding affinity towards 5-hydroxytryptamine 7 receptor (a) (human cloned receptor) in HEK 293 cells using [3H]5-CT as radioligand.
ChEMBL 414 5 0 3 3.7 CC1CCN(CC[C@H]2CCCN2S(=O)(=O)c2cccc(Br)c2)CC1 10.1021/jm991151j
CHEMBL116448 10465 None 0 Human Binding pKi = 8.7 8.7 199 7
Binding affinity towards 5-hydroxytryptamine 7 receptor (a) (human cloned receptor) in HEK 293 cells using [3H]5-CT as radioligand.Binding affinity towards 5-hydroxytryptamine 7 receptor (a) (human cloned receptor) in HEK 293 cells using [3H]5-CT as radioligand.
ChEMBL 414 5 0 3 3.7 CC1CCN(CC[C@H]2CCCN2S(=O)(=O)c2cccc(Br)c2)CC1 10.1021/jm991151j
8431 1484 None 11 Human Binding pKi = 8.7 8.7 22 5
Binding affinity towards 5-hydroxytryptamine 7 receptor (human cloned receptor) in HEK 293 cells using [3H]5-CT as radioligand.Binding affinity towards 5-hydroxytryptamine 7 receptor (human cloned receptor) in HEK 293 cells using [3H]5-CT as radioligand.
ChEMBL 386 6 1 2 5.2 O=C1Nc2c3C1(CCCCN1CCC(=CC1)c1ccccc1)CCCc3ccc2 10.1021/jm991151j
9843179 1484 None 11 Human Binding pKi = 8.7 8.7 22 5
Binding affinity towards 5-hydroxytryptamine 7 receptor (human cloned receptor) in HEK 293 cells using [3H]5-CT as radioligand.Binding affinity towards 5-hydroxytryptamine 7 receptor (human cloned receptor) in HEK 293 cells using [3H]5-CT as radioligand.
ChEMBL 386 6 1 2 5.2 O=C1Nc2c3C1(CCCCN1CCC(=CC1)c1ccccc1)CCCc3ccc2 10.1021/jm991151j
CHEMBL69257 1484 None 11 Human Binding pKi = 8.7 8.7 22 5
Binding affinity towards 5-hydroxytryptamine 7 receptor (human cloned receptor) in HEK 293 cells using [3H]5-CT as radioligand.Binding affinity towards 5-hydroxytryptamine 7 receptor (human cloned receptor) in HEK 293 cells using [3H]5-CT as radioligand.
ChEMBL 386 6 1 2 5.2 O=C1Nc2c3C1(CCCCN1CCC(=CC1)c1ccccc1)CCCc3ccc2 10.1021/jm991151j
44368731 119755 None 0 Human Binding pKi = 8.7 8.7 - 1
Binding affinity towards cloned human 5-hydroxytryptamine 7 receptor was determined in HEK293 cells using [3H]5-CT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 7 receptor was determined in HEK293 cells using [3H]5-CT as radioligand
ChEMBL 414 5 0 3 3.7 CC1CCN(CC[C@@H]2CCCN2S(=O)(=O)c2cccc(Br)c2)CC1 10.1021/jm030841r
CHEMBL347286 119755 None 0 Human Binding pKi = 8.7 8.7 - 1
Binding affinity towards cloned human 5-hydroxytryptamine 7 receptor was determined in HEK293 cells using [3H]5-CT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 7 receptor was determined in HEK293 cells using [3H]5-CT as radioligand
ChEMBL 414 5 0 3 3.7 CC1CCN(CC[C@@H]2CCCN2S(=O)(=O)c2cccc(Br)c2)CC1 10.1021/jm030841r
11047374 18916 None 0 Human Binding pKi = 8.7 8.7 - 1
Binding affinity towards human recombinant 5-hydroxytryptamine 7 receptor using [3H]5-CT as radioligandBinding affinity towards human recombinant 5-hydroxytryptamine 7 receptor using [3H]5-CT as radioligand
ChEMBL 388 6 1 2 5.3 O=C1Nc2cccc3c2C1(CCCCN1CCC(c2ccccc2)CC1)CCC3 10.1016/s0960-894x(00)00166-9
CHEMBL12846 18916 None 0 Human Binding pKi = 8.7 8.7 - 1
Binding affinity towards human recombinant 5-hydroxytryptamine 7 receptor using [3H]5-CT as radioligandBinding affinity towards human recombinant 5-hydroxytryptamine 7 receptor using [3H]5-CT as radioligand
ChEMBL 388 6 1 2 5.3 O=C1Nc2cccc3c2C1(CCCCN1CCC(c2ccccc2)CC1)CCC3 10.1016/s0960-894x(00)00166-9
10834268 166922 None 0 Human Binding pKi = 8.7 8.7 - 1
Binding affinity towards human recombinant 5-hydroxytryptamine 7 receptor using [3H]5-CT as radioligandBinding affinity towards human recombinant 5-hydroxytryptamine 7 receptor using [3H]5-CT as radioligand
ChEMBL 390 6 1 4 3.6 O=C1Nc2cccc3c2C1(CCCCN1CCN(c2ccccn2)CC1)CCC3 10.1016/s0960-894x(00)00166-9
CHEMBL428494 166922 None 0 Human Binding pKi = 8.7 8.7 - 1
Binding affinity towards human recombinant 5-hydroxytryptamine 7 receptor using [3H]5-CT as radioligandBinding affinity towards human recombinant 5-hydroxytryptamine 7 receptor using [3H]5-CT as radioligand
ChEMBL 390 6 1 4 3.6 O=C1Nc2cccc3c2C1(CCCCN1CCN(c2ccccn2)CC1)CCC3 10.1016/s0960-894x(00)00166-9
8431 1484 None 11 Human Binding pKi = 8.7 8.7 22 5
Binding affinity towards human recombinant 5-hydroxytryptamine 7 receptor was determined using [3H]5-CT as radioligandBinding affinity towards human recombinant 5-hydroxytryptamine 7 receptor was determined using [3H]5-CT as radioligand
ChEMBL 386 6 1 2 5.2 O=C1Nc2c3C1(CCCCN1CCC(=CC1)c1ccccc1)CCCc3ccc2 10.1021/jm030841r
9843179 1484 None 11 Human Binding pKi = 8.7 8.7 22 5
Binding affinity towards human recombinant 5-hydroxytryptamine 7 receptor was determined using [3H]5-CT as radioligandBinding affinity towards human recombinant 5-hydroxytryptamine 7 receptor was determined using [3H]5-CT as radioligand
ChEMBL 386 6 1 2 5.2 O=C1Nc2c3C1(CCCCN1CCC(=CC1)c1ccccc1)CCCc3ccc2 10.1021/jm030841r
CHEMBL69257 1484 None 11 Human Binding pKi = 8.7 8.7 22 5
Binding affinity towards human recombinant 5-hydroxytryptamine 7 receptor was determined using [3H]5-CT as radioligandBinding affinity towards human recombinant 5-hydroxytryptamine 7 receptor was determined using [3H]5-CT as radioligand
ChEMBL 386 6 1 2 5.2 O=C1Nc2c3C1(CCCCN1CCC(=CC1)c1ccccc1)CCCc3ccc2 10.1021/jm030841r
10834268 166922 None 0 Human Binding pKi = 8.7 8.7 - 1
Binding affinity towards human recombinant 5-hydroxytryptamine 7 receptor was determined using [3H]5-CT as radioligandBinding affinity towards human recombinant 5-hydroxytryptamine 7 receptor was determined using [3H]5-CT as radioligand
ChEMBL 390 6 1 4 3.6 O=C1Nc2cccc3c2C1(CCCCN1CCN(c2ccccn2)CC1)CCC3 10.1021/jm030841r
CHEMBL428494 166922 None 0 Human Binding pKi = 8.7 8.7 - 1
Binding affinity towards human recombinant 5-hydroxytryptamine 7 receptor was determined using [3H]5-CT as radioligandBinding affinity towards human recombinant 5-hydroxytryptamine 7 receptor was determined using [3H]5-CT as radioligand
ChEMBL 390 6 1 4 3.6 O=C1Nc2cccc3c2C1(CCCCN1CCN(c2ccccn2)CC1)CCC3 10.1021/jm030841r
10433930 51104 None 0 Human Binding pKi = 8.7 8.7 -1 5
Compound was evaluated for binding affinity against human cloned 5-hydroxytryptamine 7 receptor in HEK 293 cells using [3H]5-CT as the radioligand (n=3)Compound was evaluated for binding affinity against human cloned 5-hydroxytryptamine 7 receptor in HEK 293 cells using [3H]5-CT as the radioligand (n=3)
ChEMBL 449 5 2 5 3.9 COc1ccc(S(=O)(=O)Nc2cc(Cl)cc(Cl)c2Cl)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL157910 51104 None 0 Human Binding pKi = 8.7 8.7 -1 5
Compound was evaluated for binding affinity against human cloned 5-hydroxytryptamine 7 receptor in HEK 293 cells using [3H]5-CT as the radioligand (n=3)Compound was evaluated for binding affinity against human cloned 5-hydroxytryptamine 7 receptor in HEK 293 cells using [3H]5-CT as the radioligand (n=3)
ChEMBL 449 5 2 5 3.9 COc1ccc(S(=O)(=O)Nc2cc(Cl)cc(Cl)c2Cl)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
10028436 3532 None 9 Human Binding pKi = 8.7 8.7 -1 12
Compound was tested for its binding affinity in 5-hydroxytryptamine 7 receptor (using human cloned receptors in HEK 293 and [3H]5-CT as a radioligand )Compound was tested for its binding affinity in 5-hydroxytryptamine 7 receptor (using human cloned receptors in HEK 293 and [3H]5-CT as a radioligand )
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/s0960-894x(02)00690-x
3237 3532 None 9 Human Binding pKi = 8.7 8.7 -1 12
Compound was tested for its binding affinity in 5-hydroxytryptamine 7 receptor (using human cloned receptors in HEK 293 and [3H]5-CT as a radioligand )Compound was tested for its binding affinity in 5-hydroxytryptamine 7 receptor (using human cloned receptors in HEK 293 and [3H]5-CT as a radioligand )
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/s0960-894x(02)00690-x
CHEMBL95104 3532 None 9 Human Binding pKi = 8.7 8.7 -1 12
Compound was tested for its binding affinity in 5-hydroxytryptamine 7 receptor (using human cloned receptors in HEK 293 and [3H]5-CT as a radioligand )Compound was tested for its binding affinity in 5-hydroxytryptamine 7 receptor (using human cloned receptors in HEK 293 and [3H]5-CT as a radioligand )
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/s0960-894x(02)00690-x
46203758 124615 None 0 Rat Binding pKi = 8 8.0 - 1
Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.
ChEMBL 339 5 1 4 3.6 COc1ccc(-c2ccccc2OC(F)(F)F)cc1OC1CNC1 nan
CHEMBL3640556 124615 None 0 Rat Binding pKi = 8 8.0 - 1
Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.
ChEMBL 339 5 1 4 3.6 COc1ccc(-c2ccccc2OC(F)(F)F)cc1OC1CNC1 nan
44393072 169379 None 0 Human Binding pKi = 8 8.0 - 1
Binding affinity against 5-Hydroxy tryptamine 7 receptorBinding affinity against 5-Hydroxy tryptamine 7 receptor
ChEMBL 353 8 2 6 3.7 C[C@H](Nc1nc(F)nc(NCCOc2ccccc2)n1)c1ccccc1 10.1016/j.bmcl.2004.06.008
CHEMBL441312 169379 None 0 Human Binding pKi = 8 8.0 - 1
Binding affinity against 5-Hydroxy tryptamine 7 receptorBinding affinity against 5-Hydroxy tryptamine 7 receptor
ChEMBL 353 8 2 6 3.7 C[C@H](Nc1nc(F)nc(NCCOc2ccccc2)n1)c1ccccc1 10.1016/j.bmcl.2004.06.008
2389 3331 None 72 Human Binding pKi = 8 8.0 -7 67
Binding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
5073 3331 None 72 Human Binding pKi = 8 8.0 -7 67
Binding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
5073.0 3331 None 72 Human Binding pKi = 8 8.0 -7 67
Binding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
96 3331 None 72 Human Binding pKi = 8 8.0 -7 67
Binding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
CHEMBL85 3331 None 72 Human Binding pKi = 8 8.0 -7 67
Binding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
DB00734 3331 None 72 Human Binding pKi = 8 8.0 -7 67
Binding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
10171 56 None 11 Rat Binding pKi = 8 8.0 -5 6
Binding affinity towards 5-hydroxytryptamine 7 receptorBinding affinity towards 5-hydroxytryptamine 7 receptor
ChEMBL 401 3 1 2 3.7 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)CC 10.1016/s0960-894x(00)00166-9
272 56 None 11 Rat Binding pKi = 8 8.0 -5 6
Binding affinity towards 5-hydroxytryptamine 7 receptorBinding affinity towards 5-hydroxytryptamine 7 receptor
ChEMBL 401 3 1 2 3.7 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)CC 10.1016/s0960-894x(00)00166-9
CHEMBL274384 56 None 11 Rat Binding pKi = 8 8.0 -5 6
Binding affinity towards 5-hydroxytryptamine 7 receptorBinding affinity towards 5-hydroxytryptamine 7 receptor
ChEMBL 401 3 1 2 3.7 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)CC 10.1016/s0960-894x(00)00166-9
10499156 114155 None 1 Human Binding pKi = 8 8.0 - 1
Binding affinity towards 5-hydroxytryptamine 7 receptor (a) (human cloned receptor) in HEK 293 cells using [3H]5-CT as radioligand.Binding affinity towards 5-hydroxytryptamine 7 receptor (a) (human cloned receptor) in HEK 293 cells using [3H]5-CT as radioligand.
ChEMBL 366 6 0 4 3.0 COc1cccc(S(=O)(=O)N2CCC[C@@H]2CCN2CCC(C)CC2)c1 10.1021/jm991151j
CHEMBL332701 114155 None 1 Human Binding pKi = 8 8.0 - 1
Binding affinity towards 5-hydroxytryptamine 7 receptor (a) (human cloned receptor) in HEK 293 cells using [3H]5-CT as radioligand.Binding affinity towards 5-hydroxytryptamine 7 receptor (a) (human cloned receptor) in HEK 293 cells using [3H]5-CT as radioligand.
ChEMBL 366 6 0 4 3.0 COc1cccc(S(=O)(=O)N2CCC[C@@H]2CCN2CCC(C)CC2)c1 10.1021/jm991151j
10249573 210052 None 0 Human Binding pKi = 8 8.0 1 11
Binding affinity towards 5-hydroxytryptamine 7 receptor (a) (human cloned receptor) in HEK 293 cells using [3H]5-CT as radioligand.Binding affinity towards 5-hydroxytryptamine 7 receptor (a) (human cloned receptor) in HEK 293 cells using [3H]5-CT as radioligand.
ChEMBL 386 5 0 3 4.1 CC1CCN(CC[C@H]2CCCN2S(=O)(=O)c2cccc3ccccc23)CC1 10.1021/jm991151j
CHEMBL94984 210052 None 0 Human Binding pKi = 8 8.0 1 11
Binding affinity towards 5-hydroxytryptamine 7 receptor (a) (human cloned receptor) in HEK 293 cells using [3H]5-CT as radioligand.Binding affinity towards 5-hydroxytryptamine 7 receptor (a) (human cloned receptor) in HEK 293 cells using [3H]5-CT as radioligand.
ChEMBL 386 5 0 3 4.1 CC1CCN(CC[C@H]2CCCN2S(=O)(=O)c2cccc3ccccc23)CC1 10.1021/jm991151j
44368705 45882 None 0 Human Binding pKi = 8 8.0 - 1
Binding affinity towards cloned human 5-hydroxytryptamine 7 receptor was determined in HEK293 cells using [3H]5-CT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 7 receptor was determined in HEK293 cells using [3H]5-CT as radioligand
ChEMBL 366 6 0 4 3.0 COc1cccc(S(=O)(=O)N2CCC[C@H]2CCN2CCC(C)CC2)c1 10.1021/jm030841r
CHEMBL153156 45882 None 0 Human Binding pKi = 8 8.0 - 1
Binding affinity towards cloned human 5-hydroxytryptamine 7 receptor was determined in HEK293 cells using [3H]5-CT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 7 receptor was determined in HEK293 cells using [3H]5-CT as radioligand
ChEMBL 366 6 0 4 3.0 COc1cccc(S(=O)(=O)N2CCC[C@H]2CCN2CCC(C)CC2)c1 10.1021/jm030841r
10596321 209923 None 0 Human Binding pKi = 8 8.0 - 1
Binding affinity towards cloned human 5-hydroxytryptamine 7 receptor was determined in HEK293 cells using [3H]5-CT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 7 receptor was determined in HEK293 cells using [3H]5-CT as radioligand
ChEMBL 386 5 0 3 4.1 CC1CCN(CC[C@@H]2CCCN2S(=O)(=O)c2cccc3ccccc23)CC1 10.1021/jm030841r
CHEMBL94261 209923 None 0 Human Binding pKi = 8 8.0 - 1
Binding affinity towards cloned human 5-hydroxytryptamine 7 receptor was determined in HEK293 cells using [3H]5-CT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 7 receptor was determined in HEK293 cells using [3H]5-CT as radioligand
ChEMBL 386 5 0 3 4.1 CC1CCN(CC[C@@H]2CCCN2S(=O)(=O)c2cccc3ccccc23)CC1 10.1021/jm030841r
44460708 208066 None 0 Human Binding pKi = 8 8.0 - 1
Binding affinity towards human 5-hydroxytryptamine 7 receptorBinding affinity towards human 5-hydroxytryptamine 7 receptor
ChEMBL 331 3 0 3 3.9 Clc1ccc2ccn(CCN3CCCN4CCCCC4C3)c2c1 10.1021/jm030030n
CHEMBL81607 208066 None 0 Human Binding pKi = 8 8.0 - 1
Binding affinity towards human 5-hydroxytryptamine 7 receptorBinding affinity towards human 5-hydroxytryptamine 7 receptor
ChEMBL 331 3 0 3 3.9 Clc1ccc2ccn(CCN3CCCN4CCCCC4C3)c2c1 10.1021/jm030030n
10249573 210052 None 0 Human Binding pKi = 8 8.0 1 11
Binding affinity towards human 5-hydroxytryptamine 7 receptorBinding affinity towards human 5-hydroxytryptamine 7 receptor
ChEMBL 386 5 0 3 4.1 CC1CCN(CC[C@H]2CCCN2S(=O)(=O)c2cccc3ccccc23)CC1 10.1021/jm030030n
CHEMBL94984 210052 None 0 Human Binding pKi = 8 8.0 1 11
Binding affinity towards human 5-hydroxytryptamine 7 receptorBinding affinity towards human 5-hydroxytryptamine 7 receptor
ChEMBL 386 5 0 3 4.1 CC1CCN(CC[C@H]2CCCN2S(=O)(=O)c2cccc3ccccc23)CC1 10.1021/jm030030n
44461065 208002 None 0 Human Binding pKi = 8 8.0 - 1
Binding affinity towards human 5-hydroxytryptamine 7 receptor on HEK293 cells using radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine 7 receptor on HEK293 cells using radioligand [3H]LSD
ChEMBL 389 4 0 3 4.4 Brc1ccc2ccn(CCN3CCCN(C4CCCC4)CC3)c2c1 10.1016/s0960-894x(02)00438-9
CHEMBL81022 208002 None 0 Human Binding pKi = 8 8.0 - 1
Binding affinity towards human 5-hydroxytryptamine 7 receptor on HEK293 cells using radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine 7 receptor on HEK293 cells using radioligand [3H]LSD
ChEMBL 389 4 0 3 4.4 Brc1ccc2ccn(CCN3CCCN(C4CCCC4)CC3)c2c1 10.1016/s0960-894x(02)00438-9
44460708 208066 None 0 Human Binding pKi = 8 8.0 - 1
Binding affinity towards human 5-hydroxytryptamine 7 receptor on HEK293 cells using radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine 7 receptor on HEK293 cells using radioligand [3H]LSD
ChEMBL 331 3 0 3 3.9 Clc1ccc2ccn(CCN3CCCN4CCCCC4C3)c2c1 10.1016/s0960-894x(02)00438-9
CHEMBL81607 208066 None 0 Human Binding pKi = 8 8.0 - 1
Binding affinity towards human 5-hydroxytryptamine 7 receptor on HEK293 cells using radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine 7 receptor on HEK293 cells using radioligand [3H]LSD
ChEMBL 331 3 0 3 3.9 Clc1ccc2ccn(CCN3CCCN4CCCCC4C3)c2c1 10.1016/s0960-894x(02)00438-9
10249573 210052 None 0 Rat Binding pKi = 8 8.0 -1 11
Binding affinity towards rat 5-HT7 receptor expressed in HEK cellsBinding affinity towards rat 5-HT7 receptor expressed in HEK cells
ChEMBL 386 5 0 3 4.1 CC1CCN(CC[C@H]2CCCN2S(=O)(=O)c2cccc3ccccc23)CC1 10.1021/jm049743b
CHEMBL94984 210052 None 0 Rat Binding pKi = 8 8.0 -1 11
Binding affinity towards rat 5-HT7 receptor expressed in HEK cellsBinding affinity towards rat 5-HT7 receptor expressed in HEK cells
ChEMBL 386 5 0 3 4.1 CC1CCN(CC[C@H]2CCCN2S(=O)(=O)c2cccc3ccccc23)CC1 10.1021/jm049743b
5 139 None 45 Rat Binding pKi = 8 8.0 -5 54
Binding affinity towards rat 5-hydroxytryptamine 7 receptorBinding affinity towards rat 5-hydroxytryptamine 7 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
5202 139 None 45 Rat Binding pKi = 8 8.0 -5 54
Binding affinity towards rat 5-hydroxytryptamine 7 receptorBinding affinity towards rat 5-hydroxytryptamine 7 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
CHEMBL39 139 None 45 Rat Binding pKi = 8 8.0 -5 54
Binding affinity towards rat 5-hydroxytryptamine 7 receptorBinding affinity towards rat 5-hydroxytryptamine 7 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
DB08839 139 None 45 Rat Binding pKi = 8 8.0 -5 54
Binding affinity towards rat 5-hydroxytryptamine 7 receptorBinding affinity towards rat 5-hydroxytryptamine 7 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
9894665 103868 None 1 Human Binding pKi = 8 8.0 -30 8
Binding affinity towards recombinant human 5-hydroxytryptamine 7 receptor was determined using [3H]LSD as radioligandBinding affinity towards recombinant human 5-hydroxytryptamine 7 receptor was determined using [3H]LSD as radioligand
ChEMBL 585 10 2 8 3.3 CC(C)Oc1ccccc1N1CCN(C[C@@H](O)CNC(=O)c2ccc3c(c2)C(=O)N(c2ccc(N(C)C)cc2)C3=O)CC1 10.1021/jm9905918
CHEMBL309106 103868 None 1 Human Binding pKi = 8 8.0 -30 8
Binding affinity towards recombinant human 5-hydroxytryptamine 7 receptor was determined using [3H]LSD as radioligandBinding affinity towards recombinant human 5-hydroxytryptamine 7 receptor was determined using [3H]LSD as radioligand
ChEMBL 585 10 2 8 3.3 CC(C)Oc1ccccc1N1CCN(C[C@@H](O)CNC(=O)c2ccc3c(c2)C(=O)N(c2ccc(N(C)C)cc2)C3=O)CC1 10.1021/jm9905918
46203758 124615 None 0 Rat Binding pKi = 8 8.0 - 1
Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.
ChEMBL 339 5 1 4 3.6 COc1ccc(-c2ccccc2OC(F)(F)F)cc1OC1CNC1 nan
CHEMBL3640556 124615 None 0 Rat Binding pKi = 8 8.0 - 1
Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.
ChEMBL 339 5 1 4 3.6 COc1ccc(-c2ccccc2OC(F)(F)F)cc1OC1CNC1 nan
CHEMBL5074880 216827 None 0 Human Binding pKi = 8 8.0 1 9
Displacement of [3H] D-lysergic acid diethylamide from 5-HT7R (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by microbeta scintillation counter analysisDisplacement of [3H] D-lysergic acid diethylamide from 5-HT7R (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by microbeta scintillation counter analysis
ChEMBL None None None CCNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
127028472 138258 None 0 Human Binding pKi = 8 8.0 9 3
Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cellsDisplacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells
ChEMBL 470 8 2 6 2.2 CCOc1ccccc1N1CCN(CC(O)CN2C(=O)NC(C)(c3ccc(F)cc3)C2=O)CC1 10.1016/j.ejmech.2016.02.024
CHEMBL3769534 138258 None 0 Human Binding pKi = 8 8.0 9 3
Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cellsDisplacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells
ChEMBL 470 8 2 6 2.2 CCOc1ccccc1N1CCN(CC(O)CN2C(=O)NC(C)(c3ccc(F)cc3)C2=O)CC1 10.1016/j.ejmech.2016.02.024
127038281 137174 None 0 Human Binding pKi = 8 8.0 1 4
Displacement of [3H]-5-CT from human 5-HT7B receptor expressed in HEK293 cells incubated for 1 hrDisplacement of [3H]-5-CT from human 5-HT7B receptor expressed in HEK293 cells incubated for 1 hr
ChEMBL 494 10 0 6 4.0 Cn1cc(S(=O)(=O)N(CC2CC2)C2CCN(CCOc3ccccc3-c3ccccc3)CC2)cn1 10.1016/j.bmc.2015.11.041
CHEMBL3747240 137174 None 0 Human Binding pKi = 8 8.0 1 4
Displacement of [3H]-5-CT from human 5-HT7B receptor expressed in HEK293 cells incubated for 1 hrDisplacement of [3H]-5-CT from human 5-HT7B receptor expressed in HEK293 cells incubated for 1 hr
ChEMBL 494 10 0 6 4.0 Cn1cc(S(=O)(=O)N(CC2CC2)C2CCN(CCOc3ccccc3-c3ccccc3)CC2)cn1 10.1016/j.bmc.2015.11.041
127041259 137185 None 0 Human Binding pKi = 8 8.0 4 4
Displacement of [3H]-5-CT from human 5-HT7B receptor expressed in HEK293 cells incubated for 1 hrDisplacement of [3H]-5-CT from human 5-HT7B receptor expressed in HEK293 cells incubated for 1 hr
ChEMBL 420 8 0 6 2.7 CC(C)c1ccccc1OCCN1CCC(N(C)S(=O)(=O)c2cnn(C)c2)CC1 10.1016/j.bmc.2015.11.041
CHEMBL3747459 137185 None 0 Human Binding pKi = 8 8.0 4 4
Displacement of [3H]-5-CT from human 5-HT7B receptor expressed in HEK293 cells incubated for 1 hrDisplacement of [3H]-5-CT from human 5-HT7B receptor expressed in HEK293 cells incubated for 1 hr
ChEMBL 420 8 0 6 2.7 CC(C)c1ccccc1OCCN1CCC(N(C)S(=O)(=O)c2cnn(C)c2)CC1 10.1016/j.bmc.2015.11.041
145985505 165720 None 0 Human Binding pKi = 8 8.0 -3 5
Displacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 491 6 0 7 3.7 O=S(=O)(c1cccc2cnccc12)N1CCC[C@H]1CCN1CCN(c2noc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4243579 165720 None 0 Human Binding pKi = 8 8.0 -3 5
Displacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 491 6 0 7 3.7 O=S(=O)(c1cccc2cnccc12)N1CCC[C@H]1CCN1CCN(c2noc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
134145903 148966 None 0 Human Binding pKi = 8 8.0 5 4
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 455 10 1 3 5.9 C[C@H](NC(=O)CCCCCN1CCN(c2ccccc2-c2ccccc2)CC1)c1ccccc1 10.1016/j.ejmech.2016.05.005
CHEMBL3941529 148966 None 0 Human Binding pKi = 8 8.0 5 4
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 455 10 1 3 5.9 C[C@H](NC(=O)CCCCCN1CCN(c2ccccc2-c2ccccc2)CC1)c1ccccc1 10.1016/j.ejmech.2016.05.005
71456781 81459 None 0 Human Binding pKi = 8 8.0 1 4
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr
ChEMBL 428 8 1 5 3.8 O=S(=O)(NC1CCN(CCOc2ccccc2-c2ccccc2)C1)c1cccs1 10.1016/j.ejmech.2012.07.043
CHEMBL2159471 81459 None 0 Human Binding pKi = 8 8.0 1 4
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr
ChEMBL 428 8 1 5 3.8 O=S(=O)(NC1CCN(CCOc2ccccc2-c2ccccc2)C1)c1cccs1 10.1016/j.ejmech.2012.07.043
71458651 81465 None 0 Human Binding pKi = 8 8.0 1 4
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr
ChEMBL 439 8 1 5 3.8 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2cccc3cccnc23)C1 10.1016/j.ejmech.2012.07.043
CHEMBL2159477 81465 None 0 Human Binding pKi = 8 8.0 1 4
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr
ChEMBL 439 8 1 5 3.8 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2cccc3cccnc23)C1 10.1016/j.ejmech.2012.07.043
71456784 81480 None 0 Human Binding pKi = 8 8.0 1 4
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr
ChEMBL 440 8 1 4 3.9 O=S(=O)(N[C@H]1CCN(CCOc2ccccc2-c2ccccc2)C1)c1ccc(F)cc1 10.1016/j.ejmech.2012.07.043
CHEMBL2159492 81480 None 0 Human Binding pKi = 8 8.0 1 4
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr
ChEMBL 440 8 1 4 3.9 O=S(=O)(N[C@H]1CCN(CCOc2ccccc2-c2ccccc2)C1)c1ccc(F)cc1 10.1016/j.ejmech.2012.07.043
242 470 None 70 Human Binding pKi = 8 8.0 -15 51
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells measured after 1 hr by Microbeta plate reader methodDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells measured after 1 hr by Microbeta plate reader method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2022.114193
34 470 None 70 Human Binding pKi = 8 8.0 -15 51
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells measured after 1 hr by Microbeta plate reader methodDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells measured after 1 hr by Microbeta plate reader method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2022.114193
60795 470 None 70 Human Binding pKi = 8 8.0 -15 51
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells measured after 1 hr by Microbeta plate reader methodDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells measured after 1 hr by Microbeta plate reader method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2022.114193
60795.0 470 None 70 Human Binding pKi = 8 8.0 -15 51
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells measured after 1 hr by Microbeta plate reader methodDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells measured after 1 hr by Microbeta plate reader method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2022.114193
CHEMBL1112 470 None 70 Human Binding pKi = 8 8.0 -15 51
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells measured after 1 hr by Microbeta plate reader methodDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells measured after 1 hr by Microbeta plate reader method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2022.114193
DB01238 470 None 70 Human Binding pKi = 8 8.0 -15 51
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells measured after 1 hr by Microbeta plate reader methodDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells measured after 1 hr by Microbeta plate reader method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2022.114193
118731352 118253 None 0 Human Binding pKi = 8 8.0 2 2
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells after 1 hr
ChEMBL 510 9 1 4 4.5 NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCCCCN1CCN(c2ccccc2-c2ccccc2)CC1 10.1016/j.ejmech.2014.12.041
CHEMBL3409036 118253 None 0 Human Binding pKi = 8 8.0 2 2
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells after 1 hr
ChEMBL 510 9 1 4 4.5 NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCCCCN1CCN(c2ccccc2-c2ccccc2)CC1 10.1016/j.ejmech.2014.12.041
118731362 118262 None 0 Human Binding pKi = 8 8.0 4 2
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells after 1 hr
ChEMBL 564 8 0 4 5.6 O=C([C@@H]1Cc2ccccc2CN1C(=O)CCCCN1CCN(c2ccccc2-c2ccccc2)CC1)N1CCCCC1 10.1016/j.ejmech.2014.12.041
CHEMBL3409045 118262 None 0 Human Binding pKi = 8 8.0 4 2
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells after 1 hr
ChEMBL 564 8 0 4 5.6 O=C([C@@H]1Cc2ccccc2CN1C(=O)CCCCN1CCN(c2ccccc2-c2ccccc2)CC1)N1CCCCC1 10.1016/j.ejmech.2014.12.041
145947590 167805 None 0 Human Binding pKi = 8 8.0 8 3
Displacement of [3H]-5-CT from human 5HT7BR expressed in HEK293 cell membranes after 1 hr by Microbeta scintillation counting methodDisplacement of [3H]-5-CT from human 5HT7BR expressed in HEK293 cell membranes after 1 hr by Microbeta scintillation counting method
ChEMBL 516 7 2 6 2.4 COc1ccccc1N1CCN(CC(O)CN2C(=O)NC(C)(c3ccc(Br)cc3)C2=O)CC1 10.1016/j.ejmech.2018.01.093
CHEMBL4170657 167805 None 0 Human Binding pKi = 8 8.0 8 3
Displacement of [3H]-5-CT from human 5HT7BR expressed in HEK293 cell membranes after 1 hr by Microbeta scintillation counting methodDisplacement of [3H]-5-CT from human 5HT7BR expressed in HEK293 cell membranes after 1 hr by Microbeta scintillation counting method
ChEMBL 516 7 2 6 2.4 COc1ccccc1N1CCN(CC(O)CN2C(=O)NC(C)(c3ccc(Br)cc3)C2=O)CC1 10.1016/j.ejmech.2018.01.093
CHEMBL4302436 167805 None 0 Human Binding pKi = 8 8.0 8 3
Displacement of [3H]-5-CT from human 5HT7BR expressed in HEK293 cell membranes after 1 hr by Microbeta scintillation counting methodDisplacement of [3H]-5-CT from human 5HT7BR expressed in HEK293 cell membranes after 1 hr by Microbeta scintillation counting method
ChEMBL 516 7 2 6 2.4 COc1ccccc1N1CCN(CC(O)CN2C(=O)NC(C)(c3ccc(Br)cc3)C2=O)CC1 10.1016/j.ejmech.2018.01.093
145947976 167816 None 0 Human Binding pKi = 8 8.0 41 3
Displacement of [3H]-5-CT from human 5HT7BR expressed in HEK293 cell membranes after 1 hr by Microbeta scintillation counting methodDisplacement of [3H]-5-CT from human 5HT7BR expressed in HEK293 cell membranes after 1 hr by Microbeta scintillation counting method
ChEMBL 438 7 2 6 1.6 COc1ccccc1N1CCN(CC(O)CN2C(=O)NC(C)(c3ccccc3)C2=O)CC1 10.1016/j.ejmech.2018.01.093
CHEMBL4168743 167816 None 0 Human Binding pKi = 8 8.0 41 3
Displacement of [3H]-5-CT from human 5HT7BR expressed in HEK293 cell membranes after 1 hr by Microbeta scintillation counting methodDisplacement of [3H]-5-CT from human 5HT7BR expressed in HEK293 cell membranes after 1 hr by Microbeta scintillation counting method
ChEMBL 438 7 2 6 1.6 COc1ccccc1N1CCN(CC(O)CN2C(=O)NC(C)(c3ccccc3)C2=O)CC1 10.1016/j.ejmech.2018.01.093
CHEMBL4302539 167816 None 0 Human Binding pKi = 8 8.0 41 3
Displacement of [3H]-5-CT from human 5HT7BR expressed in HEK293 cell membranes after 1 hr by Microbeta scintillation counting methodDisplacement of [3H]-5-CT from human 5HT7BR expressed in HEK293 cell membranes after 1 hr by Microbeta scintillation counting method
ChEMBL 438 7 2 6 1.6 COc1ccccc1N1CCN(CC(O)CN2C(=O)NC(C)(c3ccccc3)C2=O)CC1 10.1016/j.ejmech.2018.01.093
56944952 157459 None 0 Human Binding pKi = 8 8.0 -2 4
Displacement of [3H]-LSD from human 5-HT7 receptor expressed in CHO-K1 cell membranes after 120 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT7 receptor expressed in CHO-K1 cell membranes after 120 mins by scintillation counting
ChEMBL 447 7 2 3 4.4 O=S(=O)(NCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc(F)cc1 10.1021/acs.jmedchem.7b00839
CHEMBL4077937 157459 None 0 Human Binding pKi = 8 8.0 -2 4
Displacement of [3H]-LSD from human 5-HT7 receptor expressed in CHO-K1 cell membranes after 120 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT7 receptor expressed in CHO-K1 cell membranes after 120 mins by scintillation counting
ChEMBL 447 7 2 3 4.4 O=S(=O)(NCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc(F)cc1 10.1021/acs.jmedchem.7b00839
24854103 96208 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometryDisplacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometry
ChEMBL 463 7 1 3 5.7 CCC1(CCCCN2CCN(c3ccc(Cl)cc3)CC2)C(=O)Nc2cc(F)c(Cl)cc21 10.1021/jm200547z
CHEMBL260551 96208 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometryDisplacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometry
ChEMBL 463 7 1 3 5.7 CCC1(CCCCN2CCN(c3ccc(Cl)cc3)CC2)C(=O)Nc2cc(F)c(Cl)cc21 10.1021/jm200547z
127052458 140827 None 0 Human Binding pKi = 8 8.0 3 7
Displacement of [3H]LSD from human 5-HT7 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT7 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 5 1 3 3.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(O)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818056 140827 None 0 Human Binding pKi = 8 8.0 3 7
Displacement of [3H]LSD from human 5-HT7 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT7 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 5 1 3 3.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(O)cc1 10.1016/j.bmc.2016.05.053
90644074 112135 None 0 Human Binding pKi = 8 8.0 151 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 414 7 1 6 2.6 Cc1cccc(S(=O)(=O)NCCCN2CCN(c3noc4ccccc34)CC2)c1 10.1021/jm401895u
CHEMBL3289967 112135 None 0 Human Binding pKi = 8 8.0 151 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 414 7 1 6 2.6 Cc1cccc(S(=O)(=O)NCCCN2CCN(c3noc4ccccc34)CC2)c1 10.1021/jm401895u
56943695 112185 None 0 Human Binding pKi = 8 8.0 -4 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 505 7 1 6 5.2 Cc1c(S(=O)(=O)NCCCN2CCC(c3noc4cc(F)ccc34)CC2)sc2ccc(F)cc12 10.1021/jm401895u
CHEMBL3290015 112185 None 0 Human Binding pKi = 8 8.0 -4 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 505 7 1 6 5.2 Cc1c(S(=O)(=O)NCCCN2CCC(c3noc4cc(F)ccc34)CC2)sc2ccc(F)cc12 10.1021/jm401895u
10171 56 None 11 Human Binding pKi = 8 8.0 -11 6
Non-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptorNon-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptor
ChEMBL 401 3 1 2 3.7 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)CC 10.1021/jm030841r
272 56 None 11 Human Binding pKi = 8 8.0 -11 6
Non-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptorNon-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptor
ChEMBL 401 3 1 2 3.7 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)CC 10.1021/jm030841r
CHEMBL274384 56 None 11 Human Binding pKi = 8 8.0 -11 6
Non-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptorNon-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptor
ChEMBL 401 3 1 2 3.7 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)CC 10.1021/jm030841r
90656682 111041 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in HEK293 cells after 30 mins by microbeta counting analysisDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in HEK293 cells after 30 mins by microbeta counting analysis
ChEMBL 311 6 2 4 3.0 Oc1cccc(NCCCN2CCN(c3ccccc3)CC2)c1 10.1016/j.ejmech.2014.04.034
CHEMBL3262411 111041 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in HEK293 cells after 30 mins by microbeta counting analysisDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in HEK293 cells after 30 mins by microbeta counting analysis
ChEMBL 311 6 2 4 3.0 Oc1cccc(NCCCN2CCN(c3ccccc3)CC2)c1 10.1016/j.ejmech.2014.04.034
11525867 96279 None 0 Human Binding pKi = 8.0 8.0 - 1
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 479 7 1 3 6.2 CCC1(CCCCN2CCN(c3ccc(Cl)cc3)CC2)C(=O)Nc2c(Cl)cc(Cl)cc21 10.1021/jm070279v
CHEMBL260870 96279 None 0 Human Binding pKi = 8.0 8.0 - 1
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 479 7 1 3 6.2 CCC1(CCCCN2CCN(c3ccc(Cl)cc3)CC2)C(=O)Nc2c(Cl)cc(Cl)cc21 10.1021/jm070279v
44266289 98216 None 0 Human Binding pKi = 8.0 8.0 - 1
Binding affinity at human cloned 5-hydroxytryptamine 7 receptor.Binding affinity at human cloned 5-hydroxytryptamine 7 receptor.
ChEMBL 404 4 1 5 3.5 O=C1c2ccccc2CCCN1CCN1CCC(n2c(O)nc3ccccc32)CC1 10.1016/s0960-894x(03)00077-5
CHEMBL273872 98216 None 0 Human Binding pKi = 8.0 8.0 - 1
Binding affinity at human cloned 5-hydroxytryptamine 7 receptor.Binding affinity at human cloned 5-hydroxytryptamine 7 receptor.
ChEMBL 404 4 1 5 3.5 O=C1c2ccccc2CCCN1CCN1CCC(n2c(O)nc3ccccc32)CC1 10.1016/s0960-894x(03)00077-5
127052458 140827 None 0 Human Binding pKi = 8.0 8.0 3 7
Displacement of [3H]LSD from human 5-HT7 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT7 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 5 1 3 3.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(O)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818056 140827 None 0 Human Binding pKi = 8.0 8.0 3 7
Displacement of [3H]LSD from human 5-HT7 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT7 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 5 1 3 3.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(O)cc1 10.1016/j.bmc.2016.05.053
242 470 None 70 Human Binding pKi = 8.0 8.0 -15 51
Displacement of [3H]-LSD from human 5-HT7 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT7 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2021.113243
34 470 None 70 Human Binding pKi = 8.0 8.0 -15 51
Displacement of [3H]-LSD from human 5-HT7 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT7 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2021.113243
60795 470 None 70 Human Binding pKi = 8.0 8.0 -15 51
Displacement of [3H]-LSD from human 5-HT7 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT7 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2021.113243
60795.0 470 None 70 Human Binding pKi = 8.0 8.0 -15 51
Displacement of [3H]-LSD from human 5-HT7 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT7 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2021.113243
CHEMBL1112 470 None 70 Human Binding pKi = 8.0 8.0 -15 51
Displacement of [3H]-LSD from human 5-HT7 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT7 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2021.113243
DB01238 470 None 70 Human Binding pKi = 8.0 8.0 -15 51
Displacement of [3H]-LSD from human 5-HT7 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT7 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2021.113243
242 470 None 70 Human Binding pKi = 8.0 8.0 -15 51
Displacement of [3H]-LSD from human 5HT7 receptor by liquid scintillation countingDisplacement of [3H]-LSD from human 5HT7 receptor by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2020.115943
34 470 None 70 Human Binding pKi = 8.0 8.0 -15 51
Displacement of [3H]-LSD from human 5HT7 receptor by liquid scintillation countingDisplacement of [3H]-LSD from human 5HT7 receptor by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2020.115943
60795 470 None 70 Human Binding pKi = 8.0 8.0 -15 51
Displacement of [3H]-LSD from human 5HT7 receptor by liquid scintillation countingDisplacement of [3H]-LSD from human 5HT7 receptor by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2020.115943
60795.0 470 None 70 Human Binding pKi = 8.0 8.0 -15 51
Displacement of [3H]-LSD from human 5HT7 receptor by liquid scintillation countingDisplacement of [3H]-LSD from human 5HT7 receptor by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2020.115943
CHEMBL1112 470 None 70 Human Binding pKi = 8.0 8.0 -15 51
Displacement of [3H]-LSD from human 5HT7 receptor by liquid scintillation countingDisplacement of [3H]-LSD from human 5HT7 receptor by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2020.115943
DB01238 470 None 70 Human Binding pKi = 8.0 8.0 -15 51
Displacement of [3H]-LSD from human 5HT7 receptor by liquid scintillation countingDisplacement of [3H]-LSD from human 5HT7 receptor by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2020.115943
242 470 None 70 Human Binding pKi = 8.0 8.0 -15 51
Displacement of [3H]LSD from human 5-HT7 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT7 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2016.05.053
34 470 None 70 Human Binding pKi = 8.0 8.0 -15 51
Displacement of [3H]LSD from human 5-HT7 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT7 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2016.05.053
60795 470 None 70 Human Binding pKi = 8.0 8.0 -15 51
Displacement of [3H]LSD from human 5-HT7 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT7 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2016.05.053
60795.0 470 None 70 Human Binding pKi = 8.0 8.0 -15 51
Displacement of [3H]LSD from human 5-HT7 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT7 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2016.05.053
CHEMBL1112 470 None 70 Human Binding pKi = 8.0 8.0 -15 51
Displacement of [3H]LSD from human 5-HT7 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT7 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2016.05.053
DB01238 470 None 70 Human Binding pKi = 8.0 8.0 -15 51
Displacement of [3H]LSD from human 5-HT7 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT7 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2016.05.053
10714877 114436 None 1 Human Binding pKi = 8.0 8.0 1 2
Displacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry
ChEMBL 381 7 0 6 3.2 COc1ccccc1N1CCN(CCCCn2c(=O)oc3ccccc32)CC1 10.1016/j.ejmech.2014.08.023
CHEMBL3331256 114436 None 1 Human Binding pKi = 8.0 8.0 1 2
Displacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry
ChEMBL 381 7 0 6 3.2 COc1ccccc1N1CCN(CCCCn2c(=O)oc3ccccc32)CC1 10.1016/j.ejmech.2014.08.023
11825614 102665 None 0 Human Binding pKi = 8.0 8.0 - 1
Binding affinity to human recombinant 5-hydroxytryptamine 7 receptor in mammalian cells using [3H]5-CT as radioligandBinding affinity to human recombinant 5-hydroxytryptamine 7 receptor in mammalian cells using [3H]5-CT as radioligand
ChEMBL 403 6 1 3 4.5 Cc1ccccc1N1CCN(CCCCC23CCCc4cccc(c42)NC3=O)CC1 10.1021/jm0104264
CHEMBL304167 102665 None 0 Human Binding pKi = 8.0 8.0 - 1
Binding affinity to human recombinant 5-hydroxytryptamine 7 receptor in mammalian cells using [3H]5-CT as radioligandBinding affinity to human recombinant 5-hydroxytryptamine 7 receptor in mammalian cells using [3H]5-CT as radioligand
ChEMBL 403 6 1 3 4.5 Cc1ccccc1N1CCN(CCCCC23CCCc4cccc(c42)NC3=O)CC1 10.1021/jm0104264
46204726 124634 None 0 Rat Binding pKi = 8.0 8.0 - 1
Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.
ChEMBL 327 3 1 2 4.4 FC(F)(F)c1ccccc1-c1ccc(Cl)c(OC2CNC2)c1 nan
CHEMBL3640574 124634 None 0 Rat Binding pKi = 8.0 8.0 - 1
Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.
ChEMBL 327 3 1 2 4.4 FC(F)(F)c1ccccc1-c1ccc(Cl)c(OC2CNC2)c1 nan
46204726 124634 None 0 Rat Binding pKi = 8.0 8.0 - 1
Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.
ChEMBL 327 3 1 2 4.4 FC(F)(F)c1ccccc1-c1ccc(Cl)c(OC2CNC2)c1 nan
CHEMBL3640574 124634 None 0 Rat Binding pKi = 8.0 8.0 - 1
Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.
ChEMBL 327 3 1 2 4.4 FC(F)(F)c1ccccc1-c1ccc(Cl)c(OC2CNC2)c1 nan
134155476 151314 None 0 Human Binding pKi = 8.0 8.0 7 4
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 455 10 1 3 5.9 C[C@@H](NC(=O)CCCCCN1CCN(c2ccccc2-c2ccccc2)CC1)c1ccccc1 10.1016/j.ejmech.2016.05.005
CHEMBL3960056 151314 None 0 Human Binding pKi = 8.0 8.0 7 4
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 455 10 1 3 5.9 C[C@@H](NC(=O)CCCCCN1CCN(c2ccccc2-c2ccccc2)CC1)c1ccccc1 10.1016/j.ejmech.2016.05.005
2726 919 None 48 Human Binding pKi = 8.0 8.0 -13 72
Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHOK1 cellsDisplacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHOK1 cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmc.2013.02.038
2726.0 919 None 48 Human Binding pKi = 8.0 8.0 -13 72
Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHOK1 cellsDisplacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHOK1 cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmc.2013.02.038
621 919 None 48 Human Binding pKi = 8.0 8.0 -13 72
Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHOK1 cellsDisplacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHOK1 cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmc.2013.02.038
83 919 None 48 Human Binding pKi = 8.0 8.0 -13 72
Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHOK1 cellsDisplacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHOK1 cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmc.2013.02.038
CHEMBL71 919 None 48 Human Binding pKi = 8.0 8.0 -13 72
Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHOK1 cellsDisplacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHOK1 cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmc.2013.02.038
DB00477 919 None 48 Human Binding pKi = 8.0 8.0 -13 72
Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHOK1 cellsDisplacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHOK1 cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmc.2013.02.038
76336186 106458 None 0 Human Binding pKi = 8.0 8.0 -1 2
Displacement of [3H]-5-CT from cloned human 5HT7B receptor expressed in HEK293 cells after 1 hr by scintillation countingDisplacement of [3H]-5-CT from cloned human 5HT7B receptor expressed in HEK293 cells after 1 hr by scintillation counting
ChEMBL 397 5 0 4 5.0 COc1ccccc1N1CCN(Cc2cn(-c3ccccc3)c3ccccc23)CC1 10.1016/j.ejmech.2014.01.055
CHEMBL3121435 106458 None 0 Human Binding pKi = 8.0 8.0 -1 2
Displacement of [3H]-5-CT from cloned human 5HT7B receptor expressed in HEK293 cells after 1 hr by scintillation countingDisplacement of [3H]-5-CT from cloned human 5HT7B receptor expressed in HEK293 cells after 1 hr by scintillation counting
ChEMBL 397 5 0 4 5.0 COc1ccccc1N1CCN(Cc2cn(-c3ccccc3)c3ccccc23)CC1 10.1016/j.ejmech.2014.01.055
CHEMBL3139448 106458 None 0 Human Binding pKi = 8.0 8.0 -1 2
Displacement of [3H]-5-CT from cloned human 5HT7B receptor expressed in HEK293 cells after 1 hr by scintillation countingDisplacement of [3H]-5-CT from cloned human 5HT7B receptor expressed in HEK293 cells after 1 hr by scintillation counting
ChEMBL 397 5 0 4 5.0 COc1ccccc1N1CCN(Cc2cn(-c3ccccc3)c3ccccc23)CC1 10.1016/j.ejmech.2014.01.055
11667458 66020 None 0 Human Binding pKi = 8.0 8.0 5 2
Displacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometryDisplacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometry
ChEMBL 350 6 1 4 3.1 O=C1Nc2ccccc2C1CCCCN1CCN(c2ccccn2)CC1 10.1021/jm200547z
CHEMBL1836788 66020 None 0 Human Binding pKi = 8.0 8.0 5 2
Displacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometryDisplacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometry
ChEMBL 350 6 1 4 3.1 O=C1Nc2ccccc2C1CCCCN1CCN(c2ccccn2)CC1 10.1021/jm200547z
11407754 98234 None 0 Rat Binding pKi = 7 7.0 - 1
Binding affinity against 5-hydroxytryptamine 7 receptor using [3H]-5-CT in rat hypothalamus membranesBinding affinity against 5-hydroxytryptamine 7 receptor using [3H]-5-CT in rat hypothalamus membranes
ChEMBL 429 8 0 4 4.8 COc1ccccc1N1CCN(CCCCCN2C(=O)c3cccc4cccc2c34)CC1 10.1016/s0960-894x(00)00166-9
CHEMBL273982 98234 None 0 Rat Binding pKi = 7 7.0 - 1
Binding affinity against 5-hydroxytryptamine 7 receptor using [3H]-5-CT in rat hypothalamus membranesBinding affinity against 5-hydroxytryptamine 7 receptor using [3H]-5-CT in rat hypothalamus membranes
ChEMBL 429 8 0 4 4.8 COc1ccccc1N1CCN(CCCCCN2C(=O)c3cccc4cccc2c34)CC1 10.1016/s0960-894x(00)00166-9
49850870 56405 None 0 Human Binding pKi = 7 7.0 -794 9
Binding affinity to human recombinant 5-HT7 receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT7 receptor by radioligand displacement assay
ChEMBL 424 6 1 5 3.3 Cc1ccc2c(N3CCN(CCc4cccc(NS(C)(=O)=O)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1631535 56405 None 0 Human Binding pKi = 7 7.0 -794 9
Binding affinity to human recombinant 5-HT7 receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT7 receptor by radioligand displacement assay
ChEMBL 424 6 1 5 3.3 Cc1ccc2c(N3CCN(CCc4cccc(NS(C)(=O)=O)c4)CC3)cccc2n1 10.1021/jm100714c
242 470 None 70 Human Binding pKi = 7 7.0 -15 51
Binding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
34 470 None 70 Human Binding pKi = 7 7.0 -15 51
Binding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
60795 470 None 70 Human Binding pKi = 7 7.0 -15 51
Binding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
60795.0 470 None 70 Human Binding pKi = 7 7.0 -15 51
Binding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
CHEMBL1112 470 None 70 Human Binding pKi = 7 7.0 -15 51
Binding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
DB01238 470 None 70 Human Binding pKi = 7 7.0 -15 51
Binding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
135398737 958 None 57 Human Binding pKi = 7 7.0 -13 91
Binding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
135398737.0 958 None 57 Human Binding pKi = 7 7.0 -13 91
Binding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
38 958 None 57 Human Binding pKi = 7 7.0 -13 91
Binding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
722 958 None 57 Human Binding pKi = 7 7.0 -13 91
Binding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
CHEMBL42 958 None 57 Human Binding pKi = 7 7.0 -13 91
Binding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
DB00363 958 None 57 Human Binding pKi = 7 7.0 -13 91
Binding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
11407754 98234 None 0 Rat Binding pKi = 7 7.0 - 1
Binding affinity towards 5-hydroxytryptamine receptor 7 on rat hypothalamus membranes using [3H]5-CT as radioligand.Binding affinity towards 5-hydroxytryptamine receptor 7 on rat hypothalamus membranes using [3H]5-CT as radioligand.
ChEMBL 429 8 0 4 4.8 COc1ccccc1N1CCN(CCCCCN2C(=O)c3cccc4cccc2c34)CC1 10.1021/jm030841r
CHEMBL273982 98234 None 0 Rat Binding pKi = 7 7.0 - 1
Binding affinity towards 5-hydroxytryptamine receptor 7 on rat hypothalamus membranes using [3H]5-CT as radioligand.Binding affinity towards 5-hydroxytryptamine receptor 7 on rat hypothalamus membranes using [3H]5-CT as radioligand.
ChEMBL 429 8 0 4 4.8 COc1ccccc1N1CCN(CCCCCN2C(=O)c3cccc4cccc2c34)CC1 10.1021/jm030841r
44374234 55571 None 0 Human Binding pKi = 7 7.0 12 2
Binding affinity towards human 5-hydroxytryptamine 7 receptor by the displacement of [3H]-5-HT radioligand from the cloned receptor expressed in CHO cellsBinding affinity towards human 5-hydroxytryptamine 7 receptor by the displacement of [3H]-5-HT radioligand from the cloned receptor expressed in CHO cells
ChEMBL 258 5 0 3 3.4 CN(C)CCSc1ccnc(-c2ccccc2)c1 10.1016/j.bmcl.2003.11.050
CHEMBL162071 55571 None 0 Human Binding pKi = 7 7.0 12 2
Binding affinity towards human 5-hydroxytryptamine 7 receptor by the displacement of [3H]-5-HT radioligand from the cloned receptor expressed in CHO cellsBinding affinity towards human 5-hydroxytryptamine 7 receptor by the displacement of [3H]-5-HT radioligand from the cloned receptor expressed in CHO cells
ChEMBL 258 5 0 3 3.4 CN(C)CCSc1ccnc(-c2ccccc2)c1 10.1016/j.bmcl.2003.11.050
10737314 97324 None 0 Human Binding pKi = 7 7.0 - 1
Binding affinity towards human recombinant 5-hydroxytryptamine 7 receptor using [3H]5-CT as radioligandBinding affinity towards human recombinant 5-hydroxytryptamine 7 receptor using [3H]5-CT as radioligand
ChEMBL 361 4 1 3 3.4 O=C1Nc2cccc3c2C1(CCN1CCN(c2ccccc2)CC1)CCC3 10.1016/s0960-894x(00)00166-9
CHEMBL268921 97324 None 0 Human Binding pKi = 7 7.0 - 1
Binding affinity towards human recombinant 5-hydroxytryptamine 7 receptor using [3H]5-CT as radioligandBinding affinity towards human recombinant 5-hydroxytryptamine 7 receptor using [3H]5-CT as radioligand
ChEMBL 361 4 1 3 3.4 O=C1Nc2cccc3c2C1(CCN1CCN(c2ccccc2)CC1)CCC3 10.1016/s0960-894x(00)00166-9
10737314 97324 None 0 Human Binding pKi = 7 7.0 - 1
Binding affinity towards human recombinant 5-hydroxytryptamine 7 receptor was determined using [3H]5-CT as radioligandBinding affinity towards human recombinant 5-hydroxytryptamine 7 receptor was determined using [3H]5-CT as radioligand
ChEMBL 361 4 1 3 3.4 O=C1Nc2cccc3c2C1(CCN1CCN(c2ccccc2)CC1)CCC3 10.1021/jm030841r
CHEMBL268921 97324 None 0 Human Binding pKi = 7 7.0 - 1
Binding affinity towards human recombinant 5-hydroxytryptamine 7 receptor was determined using [3H]5-CT as radioligandBinding affinity towards human recombinant 5-hydroxytryptamine 7 receptor was determined using [3H]5-CT as radioligand
ChEMBL 361 4 1 3 3.4 O=C1Nc2cccc3c2C1(CCN1CCN(c2ccccc2)CC1)CCC3 10.1021/jm030841r
11166042 166464 None 0 Rat Binding pKi = 7 7.0 -2 3
Binding affinity towards rat 5-HT7 receptor expressed in HEK cellsBinding affinity towards rat 5-HT7 receptor expressed in HEK cells
ChEMBL 419 9 1 6 2.2 COc1ccc(S(=O)(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1021/jm049743b
CHEMBL427518 166464 None 0 Rat Binding pKi = 7 7.0 -2 3
Binding affinity towards rat 5-HT7 receptor expressed in HEK cellsBinding affinity towards rat 5-HT7 receptor expressed in HEK cells
ChEMBL 419 9 1 6 2.2 COc1ccc(S(=O)(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1021/jm049743b
135 2532 None 33 Rat Binding pKi = 7 7.0 -50 57
Binding affinity towards rat 5-hydroxytryptamine 7 receptorBinding affinity towards rat 5-hydroxytryptamine 7 receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm030030n
1796 2532 None 33 Rat Binding pKi = 7 7.0 -50 57
Binding affinity towards rat 5-hydroxytryptamine 7 receptorBinding affinity towards rat 5-hydroxytryptamine 7 receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm030030n
4184 2532 None 33 Rat Binding pKi = 7 7.0 -50 57
Binding affinity towards rat 5-hydroxytryptamine 7 receptorBinding affinity towards rat 5-hydroxytryptamine 7 receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm030030n
4184.0 2532 None 33 Rat Binding pKi = 7 7.0 -50 57
Binding affinity towards rat 5-hydroxytryptamine 7 receptorBinding affinity towards rat 5-hydroxytryptamine 7 receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm030030n
CHEMBL6437 2532 None 33 Rat Binding pKi = 7 7.0 -50 57
Binding affinity towards rat 5-hydroxytryptamine 7 receptorBinding affinity towards rat 5-hydroxytryptamine 7 receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm030030n
DB06148 2532 None 33 Rat Binding pKi = 7 7.0 -50 57
Binding affinity towards rat 5-hydroxytryptamine 7 receptorBinding affinity towards rat 5-hydroxytryptamine 7 receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm030030n
CHEMBL5071978 216760 None 0 Human Binding pKi = 7 7.0 -1 6
Displacement of [3H] D-lysergic acid diethylamide from 5-HT7R (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by microbeta scintillation counter analysisDisplacement of [3H] D-lysergic acid diethylamide from 5-HT7R (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by microbeta scintillation counter analysis
ChEMBL None None None CCN(CC)Cc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
127041874 137134 None 0 Human Binding pKi = 7 7.0 -2 4
Displacement of [3H]-5-CT from human 5-HT7B receptor expressed in HEK293 cells incubated for 1 hrDisplacement of [3H]-5-CT from human 5-HT7B receptor expressed in HEK293 cells incubated for 1 hr
ChEMBL 450 8 0 4 4.5 CN(C1CCN(CCOc2ccccc2-c2ccccc2)CC1)S(=O)(=O)c1ccccc1 10.1016/j.bmc.2015.11.041
CHEMBL3746713 137134 None 0 Human Binding pKi = 7 7.0 -2 4
Displacement of [3H]-5-CT from human 5-HT7B receptor expressed in HEK293 cells incubated for 1 hrDisplacement of [3H]-5-CT from human 5-HT7B receptor expressed in HEK293 cells incubated for 1 hr
ChEMBL 450 8 0 4 4.5 CN(C1CCN(CCOc2ccccc2-c2ccccc2)CC1)S(=O)(=O)c1ccccc1 10.1016/j.bmc.2015.11.041
145975905 163923 None 0 Human Binding pKi = 7 7.0 5 4
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 376 4 1 4 2.4 O=C1Nc2ccccc2C12CCN(CCN1CCN(c3ccccc3)CC1)C2 10.1016/j.bmcl.2018.06.019
CHEMBL4206366 163923 None 0 Human Binding pKi = 7 7.0 5 4
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 376 4 1 4 2.4 O=C1Nc2ccccc2C12CCN(CCN1CCN(c3ccccc3)CC1)C2 10.1016/j.bmcl.2018.06.019
11414582 181444 None 0 Rat Binding pKi = 7 7.0 -16 4
Displacement of [3H]-CT from rat 5-HT7 receptor expressed in HEK293 cells by competitive radioligand binding assayDisplacement of [3H]-CT from rat 5-HT7 receptor expressed in HEK293 cells by competitive radioligand binding assay
ChEMBL 271 2 1 3 2.7 Fc1ccc(-c2c3c(nn2C2CC2)CCNCC3)cc1 10.1016/j.bmcl.2020.127669
CHEMBL4762886 181444 None 0 Rat Binding pKi = 7 7.0 -16 4
Displacement of [3H]-CT from rat 5-HT7 receptor expressed in HEK293 cells by competitive radioligand binding assayDisplacement of [3H]-CT from rat 5-HT7 receptor expressed in HEK293 cells by competitive radioligand binding assay
ChEMBL 271 2 1 3 2.7 Fc1ccc(-c2c3c(nn2C2CC2)CCNCC3)cc1 10.1016/j.bmcl.2020.127669
2470 3653 None 40 Human Binding pKi = 7 7.0 -1258 59
Displacement of [3H]5-HT from recombinant human 5-HT7 receptor expressed in African green monkey COS7 cellsDisplacement of [3H]5-HT from recombinant human 5-HT7 receptor expressed in African green monkey COS7 cells
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.ejmech.2019.111705
3300 3653 None 40 Human Binding pKi = 7 7.0 -1258 59
Displacement of [3H]5-HT from recombinant human 5-HT7 receptor expressed in African green monkey COS7 cellsDisplacement of [3H]5-HT from recombinant human 5-HT7 receptor expressed in African green monkey COS7 cells
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.ejmech.2019.111705
5265 3653 None 40 Human Binding pKi = 7 7.0 -1258 59
Displacement of [3H]5-HT from recombinant human 5-HT7 receptor expressed in African green monkey COS7 cellsDisplacement of [3H]5-HT from recombinant human 5-HT7 receptor expressed in African green monkey COS7 cells
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.ejmech.2019.111705
99 3653 None 40 Human Binding pKi = 7 7.0 -1258 59
Displacement of [3H]5-HT from recombinant human 5-HT7 receptor expressed in African green monkey COS7 cellsDisplacement of [3H]5-HT from recombinant human 5-HT7 receptor expressed in African green monkey COS7 cells
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.ejmech.2019.111705
CHEMBL267930 3653 None 40 Human Binding pKi = 7 7.0 -1258 59
Displacement of [3H]5-HT from recombinant human 5-HT7 receptor expressed in African green monkey COS7 cellsDisplacement of [3H]5-HT from recombinant human 5-HT7 receptor expressed in African green monkey COS7 cells
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.ejmech.2019.111705
44439409 91250 None 0 Human Binding pKi = 7 7.0 15 3
Displacement of [3H]5CT from 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]5CT from 5HT7 receptor expressed in HEK293 cells
ChEMBL 322 5 0 3 4.0 CC(=O)OC1CCc2ccc(/N=C/N(C)Cc3ccccc3)cc21 10.1016/j.bmcl.2007.01.093
CHEMBL240025 91250 None 0 Human Binding pKi = 7 7.0 15 3
Displacement of [3H]5CT from 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]5CT from 5HT7 receptor expressed in HEK293 cells
ChEMBL 322 5 0 3 4.0 CC(=O)OC1CCc2ccc(/N=C/N(C)Cc3ccccc3)cc21 10.1016/j.bmcl.2007.01.093
44439404 91819 None 0 Human Binding pKi = 7 7.0 15 3
Displacement of [3H]5CT from 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]5CT from 5HT7 receptor expressed in HEK293 cells
ChEMBL 334 3 0 3 4.0 CC(=O)OC1CCc2ccc(/N=C/N3CCc4ccccc4C3)cc21 10.1016/j.bmcl.2007.01.093
CHEMBL241103 91819 None 0 Human Binding pKi = 7 7.0 15 3
Displacement of [3H]5CT from 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]5CT from 5HT7 receptor expressed in HEK293 cells
ChEMBL 334 3 0 3 4.0 CC(=O)OC1CCc2ccc(/N=C/N3CCc4ccccc4C3)cc21 10.1016/j.bmcl.2007.01.093
21509921 104514 None 0 Human Binding pKi = 7 7.0 -9 24
Displacement of [3H]LSD from 5-HT7 receptor (unknown origin)Displacement of [3H]LSD from 5-HT7 receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104091 104514 None 0 Human Binding pKi = 7 7.0 -9 24
Displacement of [3H]LSD from 5-HT7 receptor (unknown origin)Displacement of [3H]LSD from 5-HT7 receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
11808247 18082 None 0 Human Binding pKi = 7 7.0 -1 9
Displacement of [3H]LSD from human 5-HT7 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT7 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL126667 18082 None 0 Human Binding pKi = 7 7.0 -1 9
Displacement of [3H]LSD from human 5-HT7 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT7 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819366 18082 None 0 Human Binding pKi = 7 7.0 -1 9
Displacement of [3H]LSD from human 5-HT7 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT7 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
9888211 21423 None 17 Human Binding pKi = 7 7.0 -125 10
Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells
ChEMBL 417 6 1 3 4.5 O=C1c2ccccc2C(=O)N1CCCCN1CC=C(c2c[nH]c3ccc(F)cc23)CC1 10.1021/jm070516u
CHEMBL131495 21423 None 17 Human Binding pKi = 7 7.0 -125 10
Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells
ChEMBL 417 6 1 3 4.5 O=C1c2ccccc2C(=O)N1CCCCN1CC=C(c2c[nH]c3ccc(F)cc23)CC1 10.1021/jm070516u
10317515 99813 None 1 Rat Binding pKi = 7 7.0 -19 3
Binding affinity towards 5-HT 7 receptor in rat hypothalamus membranes using [3H]5-CT as radioligandBinding affinity towards 5-HT 7 receptor in rat hypothalamus membranes using [3H]5-CT as radioligand
ChEMBL 378 3 0 4 1.8 O=C1C2CCCN2C(=O)CN1CN1CCN(c2cccc3ccccc23)CC1 10.1016/s0960-894x(03)00160-4
CHEMBL285066 99813 None 1 Rat Binding pKi = 7 7.0 -19 3
Binding affinity towards 5-HT 7 receptor in rat hypothalamus membranes using [3H]5-CT as radioligandBinding affinity towards 5-HT 7 receptor in rat hypothalamus membranes using [3H]5-CT as radioligand
ChEMBL 378 3 0 4 1.8 O=C1C2CCCN2C(=O)CN1CN1CCN(c2cccc3ccccc23)CC1 10.1016/s0960-894x(03)00160-4
46204086 124622 None 0 Rat Binding pKi = 6 6.0 - 1
Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.
ChEMBL 269 4 1 3 3.0 COc1ccc(-c2cccc(C)c2)cc1OC1CNC1 nan
CHEMBL3640562 124622 None 0 Rat Binding pKi = 6 6.0 - 1
Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.
ChEMBL 269 4 1 3 3.0 COc1ccc(-c2cccc(C)c2)cc1OC1CNC1 nan
11327643 119646 None 0 Human Binding pKi = 6 6.0 1 2
Binding affinity to 5HT7 (unknown origin)Binding affinity to 5HT7 (unknown origin)
ChEMBL 421 6 0 4 4.0 O=S1(=O)c2cccc3cccc(c23)N1CCCCN1CCN(c2ccccc2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL346191 119646 None 0 Human Binding pKi = 6 6.0 1 2
Binding affinity to 5HT7 (unknown origin)Binding affinity to 5HT7 (unknown origin)
ChEMBL 421 6 0 4 4.0 O=S1(=O)c2cccc3cccc(c23)N1CCCCN1CCN(c2ccccc2)CC1 10.1016/j.bmc.2019.06.028
240 944 None 25 Human Binding pKi = 6 6.0 -199 25
Binding affinity to human serotonin 5-HT7 receptorBinding affinity to human serotonin 5-HT7 receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
2769 944 None 25 Human Binding pKi = 6 6.0 -199 25
Binding affinity to human serotonin 5-HT7 receptorBinding affinity to human serotonin 5-HT7 receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
44279790 944 None 25 Human Binding pKi = 6 6.0 -199 25
Binding affinity to human serotonin 5-HT7 receptorBinding affinity to human serotonin 5-HT7 receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
660 944 None 25 Human Binding pKi = 6 6.0 -199 25
Binding affinity to human serotonin 5-HT7 receptorBinding affinity to human serotonin 5-HT7 receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
CHEMBL1729 944 None 25 Human Binding pKi = 6 6.0 -199 25
Binding affinity to human serotonin 5-HT7 receptorBinding affinity to human serotonin 5-HT7 receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
CHEMBL560739 944 None 25 Human Binding pKi = 6 6.0 -199 25
Binding affinity to human serotonin 5-HT7 receptorBinding affinity to human serotonin 5-HT7 receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
DB00604 944 None 25 Human Binding pKi = 6 6.0 -199 25
Binding affinity to human serotonin 5-HT7 receptorBinding affinity to human serotonin 5-HT7 receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
135398745 2914 None 65 Human Binding pKi = 6 6.0 -95 65
Binding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
135398745.0 2914 None 65 Human Binding pKi = 6 6.0 -95 65
Binding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
47 2914 None 65 Human Binding pKi = 6 6.0 -95 65
Binding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
CHEMBL715 2914 None 65 Human Binding pKi = 6 6.0 -95 65
Binding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
DB00334 2914 None 65 Human Binding pKi = 6 6.0 -95 65
Binding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
2337 3256 None 51 Human Binding pKi = 6 6.0 -28 62
Binding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
50 3256 None 51 Human Binding pKi = 6 6.0 -28 62
Binding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
5002 3256 None 51 Human Binding pKi = 6 6.0 -28 62
Binding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
5002.0 3256 None 51 Human Binding pKi = 6 6.0 -28 62
Binding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
CHEMBL716 3256 None 51 Human Binding pKi = 6 6.0 -28 62
Binding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
DB01224 3256 None 51 Human Binding pKi = 6 6.0 -28 62
Binding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
11327643 119646 None 0 Rat Binding pKi = 6 6.0 -1 2
Binding affinity towards 5-hydroxytryptamine receptor 7 on rat hypothalamus membranes using [3H]5-CT as radioligand.Binding affinity towards 5-hydroxytryptamine receptor 7 on rat hypothalamus membranes using [3H]5-CT as radioligand.
ChEMBL 421 6 0 4 4.0 O=S1(=O)c2cccc3cccc(c23)N1CCCCN1CCN(c2ccccc2)CC1 10.1021/jm030841r
CHEMBL346191 119646 None 0 Rat Binding pKi = 6 6.0 -1 2
Binding affinity towards 5-hydroxytryptamine receptor 7 on rat hypothalamus membranes using [3H]5-CT as radioligand.Binding affinity towards 5-hydroxytryptamine receptor 7 on rat hypothalamus membranes using [3H]5-CT as radioligand.
ChEMBL 421 6 0 4 4.0 O=S1(=O)c2cccc3cccc(c23)N1CCCCN1CCN(c2ccccc2)CC1 10.1021/jm030841r
9827938 11775 None 0 Human Binding pKi = 6 6.0 -39 12
Binding affinity towards human 5-hydroxytryptamine receptor 7 expressed in HEK 293 cells using the radioligand [3H]5-CTBinding affinity towards human 5-hydroxytryptamine receptor 7 expressed in HEK 293 cells using the radioligand [3H]5-CT
ChEMBL 517 13 1 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL1181680 11775 None 0 Human Binding pKi = 6 6.0 -39 12
Binding affinity towards human 5-hydroxytryptamine receptor 7 expressed in HEK 293 cells using the radioligand [3H]5-CTBinding affinity towards human 5-hydroxytryptamine receptor 7 expressed in HEK 293 cells using the radioligand [3H]5-CT
ChEMBL 517 13 1 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL188486 11775 None 0 Human Binding pKi = 6 6.0 -39 12
Binding affinity towards human 5-hydroxytryptamine receptor 7 expressed in HEK 293 cells using the radioligand [3H]5-CTBinding affinity towards human 5-hydroxytryptamine receptor 7 expressed in HEK 293 cells using the radioligand [3H]5-CT
ChEMBL 517 13 1 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
46204086 124622 None 0 Rat Binding pKi = 6 6.0 - 1
Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.
ChEMBL 269 4 1 3 3.0 COc1ccc(-c2cccc(C)c2)cc1OC1CNC1 nan
CHEMBL3640562 124622 None 0 Rat Binding pKi = 6 6.0 - 1
Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.
ChEMBL 269 4 1 3 3.0 COc1ccc(-c2cccc(C)c2)cc1OC1CNC1 nan
10125797 161905 None 6 Human Binding pKi = 6 6.0 -407 4
Displacement of [3H]-5-carboxamidotryptamine from human 5-HT7A receptor expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting methodDisplacement of [3H]-5-carboxamidotryptamine from human 5-HT7A receptor expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting method
ChEMBL 247 5 1 2 3.4 CCCN(CCC)[C@H]1CCc2cccc(O)c2C1 10.1016/j.bmc.2019.115262
CHEMBL41436 161905 None 6 Human Binding pKi = 6 6.0 -407 4
Displacement of [3H]-5-carboxamidotryptamine from human 5-HT7A receptor expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting methodDisplacement of [3H]-5-carboxamidotryptamine from human 5-HT7A receptor expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting method
ChEMBL 247 5 1 2 3.4 CCCN(CCC)[C@H]1CCc2cccc(O)c2C1 10.1016/j.bmc.2019.115262
CHEMBL541621 161905 None 6 Human Binding pKi = 6 6.0 -407 4
Displacement of [3H]-5-carboxamidotryptamine from human 5-HT7A receptor expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting methodDisplacement of [3H]-5-carboxamidotryptamine from human 5-HT7A receptor expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting method
ChEMBL 247 5 1 2 3.4 CCCN(CCC)[C@H]1CCc2cccc(O)c2C1 10.1016/j.bmc.2019.115262
153287574 175351 None 0 Human Binding pKi = 6 6.0 -13 10
Displacement of [3H]-LSD from human recombinant 5-HT7 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT7 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 266 2 1 2 4.0 CC[C@H]1c2ccccc2N(c2ccccc2)C[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
CHEMBL4572167 175351 None 0 Human Binding pKi = 6 6.0 -13 10
Displacement of [3H]-LSD from human recombinant 5-HT7 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT7 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 266 2 1 2 4.0 CC[C@H]1c2ccccc2N(c2ccccc2)C[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
146709966 175883 None 0 Human Binding pKi = 6 6.0 -338 3
Displacement of [3H]-LSD from human recombinant 5-HT7 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT7 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 241 1 1 2 3.4 CC[C@H]1c2ccc3ccccc3c2OC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
CHEMBL4583909 175883 None 0 Human Binding pKi = 6 6.0 -338 3
Displacement of [3H]-LSD from human recombinant 5-HT7 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT7 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 241 1 1 2 3.4 CC[C@H]1c2ccc3ccccc3c2OC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
153287539 176178 None 0 Human Binding pKi = 6 6.0 -3 2
Displacement of [3H]-LSD from human recombinant 5-HT7 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT7 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 265 1 1 2 3.6 C[C@@]12COc3ccc(-c4ccccc4)cc3[C@@H]1CCN2 10.1021/acsmedchemlett.9b00225
CHEMBL4591008 176178 None 0 Human Binding pKi = 6 6.0 -3 2
Displacement of [3H]-LSD from human recombinant 5-HT7 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT7 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 265 1 1 2 3.6 C[C@@]12COc3ccc(-c4ccccc4)cc3[C@@H]1CCN2 10.1021/acsmedchemlett.9b00225
2543 3707 None 46 Human Binding pKi = 6 6.0 -93 31
Displacement of [3H]5-HT from recombinant human 5-HT7 receptor expressed in African green monkey COS7 cellsDisplacement of [3H]5-HT from recombinant human 5-HT7 receptor expressed in African green monkey COS7 cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/j.ejmech.2019.111705
5358 3707 None 46 Human Binding pKi = 6 6.0 -93 31
Displacement of [3H]5-HT from recombinant human 5-HT7 receptor expressed in African green monkey COS7 cellsDisplacement of [3H]5-HT from recombinant human 5-HT7 receptor expressed in African green monkey COS7 cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/j.ejmech.2019.111705
5358.0 3707 None 46 Human Binding pKi = 6 6.0 -93 31
Displacement of [3H]5-HT from recombinant human 5-HT7 receptor expressed in African green monkey COS7 cellsDisplacement of [3H]5-HT from recombinant human 5-HT7 receptor expressed in African green monkey COS7 cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/j.ejmech.2019.111705
54 3707 None 46 Human Binding pKi = 6 6.0 -93 31
Displacement of [3H]5-HT from recombinant human 5-HT7 receptor expressed in African green monkey COS7 cellsDisplacement of [3H]5-HT from recombinant human 5-HT7 receptor expressed in African green monkey COS7 cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/j.ejmech.2019.111705
CHEMBL128 3707 None 46 Human Binding pKi = 6 6.0 -93 31
Displacement of [3H]5-HT from recombinant human 5-HT7 receptor expressed in African green monkey COS7 cellsDisplacement of [3H]5-HT from recombinant human 5-HT7 receptor expressed in African green monkey COS7 cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/j.ejmech.2019.111705
DB00669 3707 None 46 Human Binding pKi = 6 6.0 -93 31
Displacement of [3H]5-HT from recombinant human 5-HT7 receptor expressed in African green monkey COS7 cellsDisplacement of [3H]5-HT from recombinant human 5-HT7 receptor expressed in African green monkey COS7 cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/j.ejmech.2019.111705
44439403 91818 None 0 Human Binding pKi = 6 6.0 -5 3
Displacement of [3H]5CT from 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]5CT from 5HT7 receptor expressed in HEK293 cells
ChEMBL 394 5 0 5 4.0 COc1cc2c(cc1OC)CN(/C=N/c1ccc3c(c1)C(OC(C)=O)CC3)CC2 10.1016/j.bmcl.2007.01.093
CHEMBL241102 91818 None 0 Human Binding pKi = 6 6.0 -5 3
Displacement of [3H]5CT from 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]5CT from 5HT7 receptor expressed in HEK293 cells
ChEMBL 394 5 0 5 4.0 COc1cc2c(cc1OC)CN(/C=N/c1ccc3c(c1)C(OC(C)=O)CC3)CC2 10.1016/j.bmcl.2007.01.093
76524414 140956 None 0 Human Binding pKi = 6 6.0 -77 8
Displacement of [3H]LSD from human recombinant 5HT7 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human recombinant 5HT7 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 426 6 1 4 5.8 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCCc1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL3819434 140956 None 0 Human Binding pKi = 6 6.0 -77 8
Displacement of [3H]LSD from human recombinant 5HT7 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human recombinant 5HT7 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 426 6 1 4 5.8 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCCc1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL3819713 140956 None 0 Human Binding pKi = 6 6.0 -77 8
Displacement of [3H]LSD from human recombinant 5HT7 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human recombinant 5HT7 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 426 6 1 4 5.8 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCCc1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
9913554 101046 None 0 Human Binding pKi = 6 6.0 -1258 14
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 7 receptor in HEK293 cells, using [3H]5-CT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 7 receptor in HEK293 cells, using [3H]5-CT as radioligand
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@H]2C1 10.1016/s0960-894x(02)00172-5
CHEMBL29433 101046 None 0 Human Binding pKi = 6 6.0 -1258 14
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 7 receptor in HEK293 cells, using [3H]5-CT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 7 receptor in HEK293 cells, using [3H]5-CT as radioligand
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@H]2C1 10.1016/s0960-894x(02)00172-5
46204732 124638 None 0 Rat Binding pKi = 5 5.0 - 1
Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.
ChEMBL 250 3 1 3 2.6 N#Cc1ccc(-c2ccccc2)cc1OC1CNC1 nan
CHEMBL3640578 124638 None 0 Rat Binding pKi = 5 5.0 - 1
Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.
ChEMBL 250 3 1 3 2.6 N#Cc1ccc(-c2ccccc2)cc1OC1CNC1 nan
46204734 124641 None 0 Rat Binding pKi = 5 5.0 - 1
Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.
ChEMBL 264 3 1 3 2.9 Cc1cc(C#N)c(OC2CNC2)cc1-c1ccccc1 nan
CHEMBL3640580 124641 None 0 Rat Binding pKi = 5 5.0 - 1
Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.
ChEMBL 264 3 1 3 2.9 Cc1cc(C#N)c(OC2CNC2)cc1-c1ccccc1 nan
46205044 124646 None 0 Rat Binding pKi = 5 5.0 - 1
Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.
ChEMBL 297 5 1 3 3.8 Cc1ccccc1-c1ccc(OC(C)C)c(OC2CNC2)c1 nan
CHEMBL3640585 124646 None 0 Rat Binding pKi = 5 5.0 - 1
Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.
ChEMBL 297 5 1 3 3.8 Cc1ccccc1-c1ccc(OC(C)C)c(OC2CNC2)c1 nan
10668422 98218 None 0 Human Binding pKi = 5 5.0 - 1
Binding affinity towards cloned human 5-hydroxytryptamine 7 receptor in HEK 293 cellsBinding affinity towards cloned human 5-hydroxytryptamine 7 receptor in HEK 293 cells
ChEMBL 395 6 1 3 4.3 O=C1Nc2cccc3c2C1(CCCCN1CCN(C2CCCCC2)CC1)CCC3 10.1016/s0960-894x(00)00166-9
CHEMBL273890 98218 None 0 Human Binding pKi = 5 5.0 - 1
Binding affinity towards cloned human 5-hydroxytryptamine 7 receptor in HEK 293 cellsBinding affinity towards cloned human 5-hydroxytryptamine 7 receptor in HEK 293 cells
ChEMBL 395 6 1 3 4.3 O=C1Nc2cccc3c2C1(CCCCN1CCN(C2CCCCC2)CC1)CCC3 10.1016/s0960-894x(00)00166-9
10643153 98576 None 0 Human Binding pKi = 5 5.0 - 1
Binding affinity towards cloned human 5-hydroxytryptamine 7 receptor in HEK 293 cellsBinding affinity towards cloned human 5-hydroxytryptamine 7 receptor in HEK 293 cells
ChEMBL 374 6 0 3 4.0 C[C@H]1CCCN(CC[C@H](C)N(C)S(=O)(=O)c2cccc3ccccc23)C1 10.1016/s0960-894x(00)00166-9
CHEMBL276255 98576 None 0 Human Binding pKi = 5 5.0 - 1
Binding affinity towards cloned human 5-hydroxytryptamine 7 receptor in HEK 293 cellsBinding affinity towards cloned human 5-hydroxytryptamine 7 receptor in HEK 293 cells
ChEMBL 374 6 0 3 4.0 C[C@H]1CCCN(CC[C@H](C)N(C)S(=O)(=O)c2cccc3ccccc23)C1 10.1016/s0960-894x(00)00166-9
46204732 124638 None 0 Rat Binding pKi = 5 5.0 - 1
Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.
ChEMBL 250 3 1 3 2.6 N#Cc1ccc(-c2ccccc2)cc1OC1CNC1 nan
CHEMBL3640578 124638 None 0 Rat Binding pKi = 5 5.0 - 1
Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.
ChEMBL 250 3 1 3 2.6 N#Cc1ccc(-c2ccccc2)cc1OC1CNC1 nan
46204734 124641 None 0 Rat Binding pKi = 5 5.0 - 1
Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.
ChEMBL 264 3 1 3 2.9 Cc1cc(C#N)c(OC2CNC2)cc1-c1ccccc1 nan
CHEMBL3640580 124641 None 0 Rat Binding pKi = 5 5.0 - 1
Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.
ChEMBL 264 3 1 3 2.9 Cc1cc(C#N)c(OC2CNC2)cc1-c1ccccc1 nan
46205044 124646 None 0 Rat Binding pKi = 5 5.0 - 1
Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.
ChEMBL 297 5 1 3 3.8 Cc1ccccc1-c1ccc(OC(C)C)c(OC2CNC2)c1 nan
CHEMBL3640585 124646 None 0 Rat Binding pKi = 5 5.0 - 1
Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.
ChEMBL 297 5 1 3 3.8 Cc1ccccc1-c1ccc(OC(C)C)c(OC2CNC2)c1 nan
13149 2545 None 18 Human Binding pKi = 5 5.0 -165 17
Displacement of [3H]5-CT from human recombinant 5-HT7A receptor expressed in HEK cells by radioligand completion assayDisplacement of [3H]5-CT from human recombinant 5-HT7A receptor expressed in HEK cells by radioligand completion assay
ChEMBL 398 5 1 5 3.8 CC[C@@H]1CN2CCC3=C([C@@H]2C[C@@H]1/C(=C\OC)/C(=O)OC)NC4=C3C(=CC=C4)OC 10.1021/acs.jmedchem.1c00726
3034396 2545 None 18 Human Binding pKi = 5 5.0 -165 17
Displacement of [3H]5-CT from human recombinant 5-HT7A receptor expressed in HEK cells by radioligand completion assayDisplacement of [3H]5-CT from human recombinant 5-HT7A receptor expressed in HEK cells by radioligand completion assay
ChEMBL 398 5 1 5 3.8 CC[C@@H]1CN2CCC3=C([C@@H]2C[C@@H]1/C(=C\OC)/C(=O)OC)NC4=C3C(=CC=C4)OC 10.1021/acs.jmedchem.1c00726
CHEMBL299031 2545 None 18 Human Binding pKi = 5 5.0 -165 17
Displacement of [3H]5-CT from human recombinant 5-HT7A receptor expressed in HEK cells by radioligand completion assayDisplacement of [3H]5-CT from human recombinant 5-HT7A receptor expressed in HEK cells by radioligand completion assay
ChEMBL 398 5 1 5 3.8 CC[C@@H]1CN2CCC3=C([C@@H]2C[C@@H]1/C(=C\OC)/C(=O)OC)NC4=C3C(=CC=C4)OC 10.1021/acs.jmedchem.1c00726
11462900 57026 None 0 Rat Binding pKi = 5 5.0 - 1
Displacement of [3H]5-CT from rat recombinant 5HT7 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]5-CT from rat recombinant 5HT7 receptor expressed in HEK293 cells after 60 mins
ChEMBL 372 4 1 3 4.7 FC(F)(F)Oc1ccc(-c2cn(Cc3ccccc3)c3c2CNCC3)cc1 10.1016/j.bmcl.2010.11.078
CHEMBL1644270 57026 None 0 Rat Binding pKi = 5 5.0 - 1
Displacement of [3H]5-CT from rat recombinant 5HT7 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]5-CT from rat recombinant 5HT7 receptor expressed in HEK293 cells after 60 mins
ChEMBL 372 4 1 3 4.7 FC(F)(F)Oc1ccc(-c2cn(Cc3ccccc3)c3c2CNCC3)cc1 10.1016/j.bmcl.2010.11.078
53316608 57032 None 0 Rat Binding pKi = 5 5.0 - 1
Displacement of [3H]5-CT from rat recombinant 5HT7 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]5-CT from rat recombinant 5HT7 receptor expressed in HEK293 cells after 60 mins
ChEMBL 344 3 1 2 5.1 CC(C)(C)c1ccc(-c2cn(Cc3ccccc3)c3c2CNCC3)cc1 10.1016/j.bmcl.2010.11.078
CHEMBL1644276 57032 None 0 Rat Binding pKi = 5 5.0 - 1
Displacement of [3H]5-CT from rat recombinant 5HT7 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]5-CT from rat recombinant 5HT7 receptor expressed in HEK293 cells after 60 mins
ChEMBL 344 3 1 2 5.1 CC(C)(C)c1ccc(-c2cn(Cc3ccccc3)c3c2CNCC3)cc1 10.1016/j.bmcl.2010.11.078
53316609 57033 None 0 Rat Binding pKi = 5 5.0 - 1
Displacement of [3H]5-CT from rat recombinant 5HT7 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]5-CT from rat recombinant 5HT7 receptor expressed in HEK293 cells after 60 mins
ChEMBL 322 3 1 2 4.5 Clc1cccc(-c2cn(Cc3ccccc3)c3c2CNCC3)c1 10.1016/j.bmcl.2010.11.078
CHEMBL1644277 57033 None 0 Rat Binding pKi = 5 5.0 - 1
Displacement of [3H]5-CT from rat recombinant 5HT7 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]5-CT from rat recombinant 5HT7 receptor expressed in HEK293 cells after 60 mins
ChEMBL 322 3 1 2 4.5 Clc1cccc(-c2cn(Cc3ccccc3)c3c2CNCC3)c1 10.1016/j.bmcl.2010.11.078
11449570 57037 None 0 Rat Binding pKi = 5 5.0 - 1
Displacement of [3H]5-CT from rat recombinant 5HT7 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]5-CT from rat recombinant 5HT7 receptor expressed in HEK293 cells after 60 mins
ChEMBL 304 3 2 3 3.6 Oc1ccc(-c2cn(Cc3ccccc3)c3c2CNCC3)cc1 10.1016/j.bmcl.2010.11.078
CHEMBL1644281 57037 None 0 Rat Binding pKi = 5 5.0 - 1
Displacement of [3H]5-CT from rat recombinant 5HT7 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]5-CT from rat recombinant 5HT7 receptor expressed in HEK293 cells after 60 mins
ChEMBL 304 3 2 3 3.6 Oc1ccc(-c2cn(Cc3ccccc3)c3c2CNCC3)cc1 10.1016/j.bmcl.2010.11.078
25229646 63565 None 25 Human Binding pKi = 5 5.0 - 1
GPCRScan assay: inhibition of 5-HT7AGPCRScan assay: inhibition of 5-HT7A
ChEMBL 388 4 1 6 2.5 N#CC1(c2ccccn2)CCN(Cc2cc(C(=O)O)c(=O)n3ccccc23)CC1 10.6019/CHEMBL4507295
CHEMBL1800285 63565 None 25 Human Binding pKi = 5 5.0 - 1
GPCRScan assay: inhibition of 5-HT7AGPCRScan assay: inhibition of 5-HT7A
ChEMBL 388 4 1 6 2.5 N#CC1(c2ccccn2)CCN(Cc2cc(C(=O)O)c(=O)n3ccccc23)CC1 10.6019/CHEMBL4507295
CHEMBL4584981 216496 None 0 Human Binding pKi = 5 5.0 - 1
GPCRScan assay: inhibition of 5-HT7AGPCRScan assay: inhibition of 5-HT7A
ChEMBL None None None CO[C@@H](C)c1c(Nc2ccc([C@@H](N(C)C(=O)C3CCS(=O)(=O)CC3)C(F)(F)F)cc2)cnc2cc(Cl)nn12 10.6019/CHEMBL4507320
3251 4072 None 43 Human Binding pKi = 5 5.0 -33113 12
Inhibition of 5HT7 receptorInhibition of 5HT7 receptor
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm1009956
5684 4072 None 43 Human Binding pKi = 5 5.0 -33113 12
Inhibition of 5HT7 receptorInhibition of 5HT7 receptor
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm1009956
80 4072 None 43 Human Binding pKi = 5 5.0 -33113 12
Inhibition of 5HT7 receptorInhibition of 5HT7 receptor
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm1009956
CHEMBL31354 4072 None 43 Human Binding pKi = 5 5.0 -33113 12
Inhibition of 5HT7 receptorInhibition of 5HT7 receptor
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm1009956
44368373 119622 None 0 Human Binding pKi = 4 4.0 - 1
Binding affinity towards cloned human 5-hydroxytryptamine 7 receptor was determined in HEK293 cells using [3H]5-CT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 7 receptor was determined in HEK293 cells using [3H]5-CT as radioligand
ChEMBL 373 6 0 3 4.8 CC([C@@H](C)CCN1CCC[C@H](C)C1)S(=O)(=O)c1cccc2ccccc12 10.1021/jm030841r
CHEMBL345971 119622 None 0 Human Binding pKi = 4 4.0 - 1
Binding affinity towards cloned human 5-hydroxytryptamine 7 receptor was determined in HEK293 cells using [3H]5-CT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 7 receptor was determined in HEK293 cells using [3H]5-CT as radioligand
ChEMBL 373 6 0 3 4.8 CC([C@@H](C)CCN1CCC[C@H](C)C1)S(=O)(=O)c1cccc2ccccc12 10.1021/jm030841r
10668422 98218 None 0 Human Binding pKi = 4 4.0 - 1
Binding affinity towards human recombinant 5-hydroxytryptamine 7 receptor was determined using [3H]5-CT as radioligandBinding affinity towards human recombinant 5-hydroxytryptamine 7 receptor was determined using [3H]5-CT as radioligand
ChEMBL 395 6 1 3 4.3 O=C1Nc2cccc3c2C1(CCCCN1CCN(C2CCCCC2)CC1)CCC3 10.1021/jm030841r
CHEMBL273890 98218 None 0 Human Binding pKi = 4 4.0 - 1
Binding affinity towards human recombinant 5-hydroxytryptamine 7 receptor was determined using [3H]5-CT as radioligandBinding affinity towards human recombinant 5-hydroxytryptamine 7 receptor was determined using [3H]5-CT as radioligand
ChEMBL 395 6 1 3 4.3 O=C1Nc2cccc3c2C1(CCCCN1CCN(C2CCCCC2)CC1)CCC3 10.1021/jm030841r
171355796 194280 None 0 Human Binding pKi = 6 6.0 -1 3
Displacement of [3H]SB269970 from human 5-HT7 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysisDisplacement of [3H]SB269970 from human 5-HT7 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysis
ChEMBL 422 7 0 5 3.5 O=C1CC2Cc3ccsc3C2=NN1CCCCN1CCN(Cc2ccccc2)CC1 10.1016/j.bmc.2023.117256
CHEMBL5282788 194280 None 0 Human Binding pKi = 6 6.0 -1 3
Displacement of [3H]SB269970 from human 5-HT7 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysisDisplacement of [3H]SB269970 from human 5-HT7 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysis
ChEMBL 422 7 0 5 3.5 O=C1CC2Cc3ccsc3C2=NN1CCCCN1CCN(Cc2ccccc2)CC1 10.1016/j.bmc.2023.117256
76524414 140956 None 0 Human Binding pKi = 6 6.0 -77 8
Displacement of [3H]LSD from human recombinant 5HT7 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human recombinant 5HT7 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 426 6 1 4 5.8 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCCc1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL3819434 140956 None 0 Human Binding pKi = 6 6.0 -77 8
Displacement of [3H]LSD from human recombinant 5HT7 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human recombinant 5HT7 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 426 6 1 4 5.8 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCCc1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL3819713 140956 None 0 Human Binding pKi = 6 6.0 -77 8
Displacement of [3H]LSD from human recombinant 5HT7 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human recombinant 5HT7 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 426 6 1 4 5.8 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCCc1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
118724647 120670 None 0 Human Binding pKi = 6 6.0 -5 4
Displacement of [3H]]-5-CT from human cloned 5-HT7R expressed in HEK293 cellsDisplacement of [3H]]-5-CT from human cloned 5-HT7R expressed in HEK293 cells
ChEMBL 381 6 0 7 1.7 Cn1c(=O)c2c(ncn2CCCCCN2CCc3ccccc3C2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3361004 120670 None 0 Human Binding pKi = 6 6.0 -5 4
Displacement of [3H]]-5-CT from human cloned 5-HT7R expressed in HEK293 cellsDisplacement of [3H]]-5-CT from human cloned 5-HT7R expressed in HEK293 cells
ChEMBL 381 6 0 7 1.7 Cn1c(=O)c2c(ncn2CCCCCN2CCc3ccccc3C2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3546104 120670 None 0 Human Binding pKi = 6 6.0 -5 4
Displacement of [3H]]-5-CT from human cloned 5-HT7R expressed in HEK293 cellsDisplacement of [3H]]-5-CT from human cloned 5-HT7R expressed in HEK293 cells
ChEMBL 381 6 0 7 1.7 Cn1c(=O)c2c(ncn2CCCCCN2CCc3ccccc3C2)n(C)c1=O 10.1016/j.bmc.2014.11.008
11603887 102645 None 0 Rat Binding pKi = 7 7.0 -3 2
Displacement of [3H]-5-CT from 5-HT7 receptor in Sprague-Dawley rat hypothalamus after 120 minsDisplacement of [3H]-5-CT from 5-HT7 receptor in Sprague-Dawley rat hypothalamus after 120 mins
ChEMBL 407 10 1 4 3.5 O=C1C2CCCN2C(=O)N1CCCCNCCOc1ccccc1-c1ccccc1 10.1021/jm400766k
CHEMBL2431046 102645 None 0 Rat Binding pKi = 7 7.0 -3 2
Displacement of [3H]-5-CT from 5-HT7 receptor in Sprague-Dawley rat hypothalamus after 120 minsDisplacement of [3H]-5-CT from 5-HT7 receptor in Sprague-Dawley rat hypothalamus after 120 mins
ChEMBL 407 10 1 4 3.5 O=C1C2CCCN2C(=O)N1CCCCNCCOc1ccccc1-c1ccccc1 10.1021/jm400766k
CHEMBL3040877 102645 None 0 Rat Binding pKi = 7 7.0 -3 2
Displacement of [3H]-5-CT from 5-HT7 receptor in Sprague-Dawley rat hypothalamus after 120 minsDisplacement of [3H]-5-CT from 5-HT7 receptor in Sprague-Dawley rat hypothalamus after 120 mins
ChEMBL 407 10 1 4 3.5 O=C1C2CCCN2C(=O)N1CCCCNCCOc1ccccc1-c1ccccc1 10.1021/jm400766k
90654670 110147 None 0 Human Binding pKi = 7 7.0 1 2
Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-countingDisplacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-counting
ChEMBL 427 9 1 6 2.4 NC(=O)[C@@H]1CCCN1C(=O)CCCCCCN1CCN(c2noc3ccccc23)CC1 10.1016/j.ejmech.2014.03.005
CHEMBL3235742 110147 None 0 Human Binding pKi = 7 7.0 1 2
Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-countingDisplacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-counting
ChEMBL 427 9 1 6 2.4 NC(=O)[C@@H]1CCCN1C(=O)CCCCCCN1CCN(c2noc3ccccc23)CC1 10.1016/j.ejmech.2014.03.005
136180321 117779 None 0 Human Binding pKi = 7 7.0 1 2
Displacement of [3H]-8-OH-DPAT from human 5-HT7 receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-8-OH-DPAT from human 5-HT7 receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysis
ChEMBL 410 7 1 4 4.1 O=c1[nH]c(CCCCCN2CCN(c3ccc(Cl)cc3)CC2)nc2ccccc12 10.1016/j.bmcl.2015.02.042
CHEMBL3401483 117779 None 0 Human Binding pKi = 7 7.0 1 2
Displacement of [3H]-8-OH-DPAT from human 5-HT7 receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-8-OH-DPAT from human 5-HT7 receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysis
ChEMBL 410 7 1 4 4.1 O=c1[nH]c(CCCCCN2CCN(c3ccc(Cl)cc3)CC2)nc2ccccc12 10.1016/j.bmcl.2015.02.042
11291892 133582 None 3 Rat Binding pKi = 7 7.0 -24 3
In vitro inhibition of [3H]5-CT binding to 5-hydroxytryptamine 7 receptor in rat hypothalamus membranesIn vitro inhibition of [3H]5-CT binding to 5-hydroxytryptamine 7 receptor in rat hypothalamus membranes
ChEMBL 378 3 0 4 1.8 O=C1[C@@H]2CCCN2C(=O)CN1CN1CCN(c2cccc3ccccc23)CC1 10.1021/jm048999e
CHEMBL370758 133582 None 3 Rat Binding pKi = 7 7.0 -24 3
In vitro inhibition of [3H]5-CT binding to 5-hydroxytryptamine 7 receptor in rat hypothalamus membranesIn vitro inhibition of [3H]5-CT binding to 5-hydroxytryptamine 7 receptor in rat hypothalamus membranes
ChEMBL 378 3 0 4 1.8 O=C1[C@@H]2CCCN2C(=O)CN1CN1CCN(c2cccc3ccccc23)CC1 10.1021/jm048999e
10994400 207579 None 0 Human Binding pKi = 7 7.0 -109 4
Tested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 7 receptor incubated with 1 nM [3H]LSDTested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 7 receptor incubated with 1 nM [3H]LSD
ChEMBL 439 5 1 2 4.4 OC(c1ccc(F)cc1)C1CCN(CCc2ccccc2I)CC1 10.1021/jm0200411
CHEMBL77855 207579 None 0 Human Binding pKi = 7 7.0 -109 4
Tested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 7 receptor incubated with 1 nM [3H]LSDTested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 7 receptor incubated with 1 nM [3H]LSD
ChEMBL 439 5 1 2 4.4 OC(c1ccc(F)cc1)C1CCN(CCc2ccccc2I)CC1 10.1021/jm0200411
2880253 162802 None 6 Human Binding pKi = 5 5.0 -1 3
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 351 7 1 2 5.4 CCC1(C)CC(CCNCc2ccccc2)(c2ccc(C)cc2)CCO1 10.1016/j.ejmech.2018.04.010
CHEMBL4170813 162802 None 6 Human Binding pKi = 5 5.0 -1 3
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 351 7 1 2 5.4 CCC1(C)CC(CCNCc2ccccc2)(c2ccc(C)cc2)CCO1 10.1016/j.ejmech.2018.04.010
71457409 82994 None 0 Human Binding pKi = 6.0 6.0 -3981 5
Binding affinity to human 5HT7 by Cerep protocol based assayBinding affinity to human 5HT7 by Cerep protocol based assay
ChEMBL 461 5 0 4 4.9 CCCN1CCC(COc2nc3c(I)cccc3c3ncccc23)CC1 10.1021/jm300943r
CHEMBL2181168 82994 None 0 Human Binding pKi = 6.0 6.0 -3981 5
Binding affinity to human 5HT7 by Cerep protocol based assayBinding affinity to human 5HT7 by Cerep protocol based assay
ChEMBL 461 5 0 4 4.9 CCCN1CCC(COc2nc3c(I)cccc3c3ncccc23)CC1 10.1021/jm300943r
134147951 149892 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]D-lysergic acid diethylamide from 5HT7R (unknown origin) expressed in HEK293 cell membranes incubated for 1.5 hrs in absence of light by liquid scintillation countingDisplacement of [3H]D-lysergic acid diethylamide from 5HT7R (unknown origin) expressed in HEK293 cell membranes incubated for 1.5 hrs in absence of light by liquid scintillation counting
ChEMBL 271 5 0 3 3.4 COc1ccccc1-c1cc(CN(C)C)ccc1OC 10.1016/j.ejmech.2016.07.029
CHEMBL3948597 149892 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]D-lysergic acid diethylamide from 5HT7R (unknown origin) expressed in HEK293 cell membranes incubated for 1.5 hrs in absence of light by liquid scintillation countingDisplacement of [3H]D-lysergic acid diethylamide from 5HT7R (unknown origin) expressed in HEK293 cell membranes incubated for 1.5 hrs in absence of light by liquid scintillation counting
ChEMBL 271 5 0 3 3.4 COc1ccccc1-c1cc(CN(C)C)ccc1OC 10.1016/j.ejmech.2016.07.029
10737314 97324 None 0 Human Binding pKi = 7.0 7.0 - 1
Compound was evaluated for its ability to displace [3H]5-CT binding from cloned human 5-hydroxytryptamine 7 receptor expressed in COS-7 cells.Compound was evaluated for its ability to displace [3H]5-CT binding from cloned human 5-hydroxytryptamine 7 receptor expressed in COS-7 cells.
ChEMBL 361 4 1 3 3.4 O=C1Nc2cccc3c2C1(CCN1CCN(c2ccccc2)CC1)CCC3 10.1021/jm980519u
CHEMBL268921 97324 None 0 Human Binding pKi = 7.0 7.0 - 1
Compound was evaluated for its ability to displace [3H]5-CT binding from cloned human 5-hydroxytryptamine 7 receptor expressed in COS-7 cells.Compound was evaluated for its ability to displace [3H]5-CT binding from cloned human 5-hydroxytryptamine 7 receptor expressed in COS-7 cells.
ChEMBL 361 4 1 3 3.4 O=C1Nc2cccc3c2C1(CCN1CCN(c2ccccc2)CC1)CCC3 10.1021/jm980519u
CHEMBL5076882 216954 None 0 Human Binding pKi = 7.0 7.0 -26 4
Displacement of [3H]-LSD from human 5-HT7 receptor transfected in CHO-K1 cells measured after 120 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT7 receptor transfected in CHO-K1 cells measured after 120 mins by scintillation counting method
ChEMBL None None None C[C@H]1C[C@H](NS(=O)(=O)c2cccc(Cl)c2)CN1CCCc1noc2cc(F)ccc12 10.1021/acs.jmedchem.1c00497
CHEMBL5083505 217355 None 0 Human Binding pKi = 7.0 7.0 -2 4
Displacement of [3H]-LSD from human 5-HT7 receptor transfected in CHO-K1 cells measured after 120 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT7 receptor transfected in CHO-K1 cells measured after 120 mins by scintillation counting method
ChEMBL None None None O=S(=O)(CC1CCN(CCCc2noc3cc(F)ccc23)C1)c1cccc(F)c1 10.1021/acs.jmedchem.1c00497
1534 103095 None 23 Human Binding pKi = 7.0 7.0 1 12
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
9287 103095 None 23 Human Binding pKi = 7.0 7.0 1 12
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
CHEMBL30713 103095 None 23 Human Binding pKi = 7.0 7.0 1 12
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
10314060 168703 None 0 Human Binding pKi = 7.0 7.0 -72 7
In vitro binding affinity to human 5-hydroxytryptamine 7 receptorIn vitro binding affinity to human 5-hydroxytryptamine 7 receptor
ChEMBL 322 4 1 4 2.9 COc1ccccc1N1CCN(Cc2c[nH]c3ncccc23)CC1 10.1016/s0960-894x(01)00241-4
CHEMBL435949 168703 None 0 Human Binding pKi = 7.0 7.0 -72 7
In vitro binding affinity to human 5-hydroxytryptamine 7 receptorIn vitro binding affinity to human 5-hydroxytryptamine 7 receptor
ChEMBL 322 4 1 4 2.9 COc1ccccc1N1CCN(Cc2c[nH]c3ncccc23)CC1 10.1016/s0960-894x(01)00241-4
122442272 138435 None 0 Human Binding pKi = 6.0 6.0 -40 15
Binding affinity to human 5HT7 receptor by radioligand binding assayBinding affinity to human 5HT7 receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769968 138435 None 0 Human Binding pKi = 6.0 6.0 -40 15
Binding affinity to human 5HT7 receptor by radioligand binding assayBinding affinity to human 5HT7 receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771384 138435 None 0 Human Binding pKi = 6.0 6.0 -40 15
Binding affinity to human 5HT7 receptor by radioligand binding assayBinding affinity to human 5HT7 receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
18137015 164435 None 0 Human Binding pKi = 6.0 6.0 1 2
Displacement of [3H]-5-CT from human serotonin 5-HT7B receptor expressed in HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-5-CT from human serotonin 5-HT7B receptor expressed in HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 394 7 1 4 3.2 O=S(=O)(NC1CCN(CCOc2ccccc2Cl)CC1)c1ccccc1 10.1021/acs.jmedchem.8b00828
CHEMBL4212558 164435 None 0 Human Binding pKi = 6.0 6.0 1 2
Displacement of [3H]-5-CT from human serotonin 5-HT7B receptor expressed in HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-5-CT from human serotonin 5-HT7B receptor expressed in HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 394 7 1 4 3.2 O=S(=O)(NC1CCN(CCOc2ccccc2Cl)CC1)c1ccccc1 10.1021/acs.jmedchem.8b00828
23369457 189624 None 0 Human Binding pKi = 6.0 6.0 -2 2
Inhibition of human 5HT7 receptor expressed in HEK293 cells by competitive binding assayInhibition of human 5HT7 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 322 4 1 4 2.2 O=c1[nH]c2ccccc2n1CCN1CCN(c2ccccc2)CC1 10.1016/j.bmcl.2009.02.008
CHEMBL514058 189624 None 0 Human Binding pKi = 6.0 6.0 -2 2
Inhibition of human 5HT7 receptor expressed in HEK293 cells by competitive binding assayInhibition of human 5HT7 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 322 4 1 4 2.2 O=c1[nH]c2ccccc2n1CCN1CCN(c2ccccc2)CC1 10.1016/j.bmcl.2009.02.008
10754042 99854 None 0 Rat Binding pKi = 7.0 7.0 2 4
Displacement of [3H]5-HT from over-expressed rat 5-hydroxytryptamine 7 receptorDisplacement of [3H]5-HT from over-expressed rat 5-hydroxytryptamine 7 receptor
ChEMBL 263 0 1 2 2.8 CN1CCc2ccc3c4c2[C@H]1Cc1cccc(c1-4)[C@@H]3O 10.1021/jm9911433
CHEMBL285352 99854 None 0 Rat Binding pKi = 7.0 7.0 2 4
Displacement of [3H]5-HT from over-expressed rat 5-hydroxytryptamine 7 receptorDisplacement of [3H]5-HT from over-expressed rat 5-hydroxytryptamine 7 receptor
ChEMBL 263 0 1 2 2.8 CN1CCc2ccc3c4c2[C@H]1Cc1cccc(c1-4)[C@@H]3O 10.1021/jm9911433
1534 103095 None 23 Human Binding pKi = 7.0 7.0 1 12
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
9287 103095 None 23 Human Binding pKi = 7.0 7.0 1 12
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
CHEMBL30713 103095 None 23 Human Binding pKi = 7.0 7.0 1 12
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
134135372 144485 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]D-lysergic acid diethylamide from 5HT7R (unknown origin) expressed in HEK293 cell membranes incubated for 1.5 hrs in absence of light by liquid scintillation countingDisplacement of [3H]D-lysergic acid diethylamide from 5HT7R (unknown origin) expressed in HEK293 cell membranes incubated for 1.5 hrs in absence of light by liquid scintillation counting
ChEMBL 295 4 0 2 4.6 COc1ccccc1-c1cccc(CN2CCC(C)CC2)c1 10.1016/j.ejmech.2016.07.029
CHEMBL3906019 144485 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]D-lysergic acid diethylamide from 5HT7R (unknown origin) expressed in HEK293 cell membranes incubated for 1.5 hrs in absence of light by liquid scintillation countingDisplacement of [3H]D-lysergic acid diethylamide from 5HT7R (unknown origin) expressed in HEK293 cell membranes incubated for 1.5 hrs in absence of light by liquid scintillation counting
ChEMBL 295 4 0 2 4.6 COc1ccccc1-c1cccc(CN2CCC(C)CC2)c1 10.1016/j.ejmech.2016.07.029
168291659 192147 None 0 Human Binding pKi = 6.0 6.0 -14 5
Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 356 8 3 8 1.4 Nc1nc(N)nc(NCCCCCN2CCN(c3ccccc3)CC2)n1 10.1016/j.ejmech.2021.113931
CHEMBL5202120 192147 None 0 Human Binding pKi = 6.0 6.0 -14 5
Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 356 8 3 8 1.4 Nc1nc(N)nc(NCCCCCN2CCN(c3ccccc3)CC2)n1 10.1016/j.ejmech.2021.113931
135414318 210244 None 0 Rat Binding pKi = 7.0 7.0 - 1
Binding affinity towards rat 5-hydroxytryptamine 7 receptorBinding affinity towards rat 5-hydroxytryptamine 7 receptor
ChEMBL 298 0 1 5 3.1 CN1CCN(C2=Nc3ccccc3Nc3sccc32)CC1 10.1021/jm030030n
CHEMBL96055 210244 None 0 Rat Binding pKi = 7.0 7.0 - 1
Binding affinity towards rat 5-hydroxytryptamine 7 receptorBinding affinity towards rat 5-hydroxytryptamine 7 receptor
ChEMBL 298 0 1 5 3.1 CN1CCN(C2=Nc3ccccc3Nc3sccc32)CC1 10.1021/jm030030n
145978146 164011 None 0 Human Binding pKi = 7.0 7.0 4 2
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr by microbeta counting analysisDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr by microbeta counting analysis
ChEMBL 450 9 2 5 3.1 CC(C)c1ccccc1OCC(O)CN1CCC(NS(=O)(=O)c2ccc(F)cc2)CC1 10.1016/j.bmc.2017.03.057
CHEMBL4207310 164011 None 0 Human Binding pKi = 7.0 7.0 4 2
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr by microbeta counting analysisDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr by microbeta counting analysis
ChEMBL 450 9 2 5 3.1 CC(C)c1ccccc1OCC(O)CN1CCC(NS(=O)(=O)c2ccc(F)cc2)CC1 10.1016/j.bmc.2017.03.057
156013326 177599 None 0 Human Binding pKi = 7.0 7.0 1 3
Displacement of [3H]-LSD from human 5-HT7A receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT7A receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 350 4 1 4 3.8 COc1cc2c3c(c1OCC1CC1)-c1cc(N)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
CHEMBL4639400 177599 None 0 Human Binding pKi = 7.0 7.0 1 3
Displacement of [3H]-LSD from human 5-HT7A receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT7A receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 350 4 1 4 3.8 COc1cc2c3c(c1OCC1CC1)-c1cc(N)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
124247485 164164 None 6 Human Binding pKi = 7.0 7.0 -1 8
Displacement of [3H]LSD from human 5-HT7 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT7 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 231 1 2 2 1.9 Fc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4209274 164164 None 6 Human Binding pKi = 7.0 7.0 -1 8
Displacement of [3H]LSD from human 5-HT7 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT7 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 231 1 2 2 1.9 Fc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
124247485 164164 None 6 Human Binding pKi = 7.0 7.0 -1 8
Displacement of [3H]LSD from human 5-HT7 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT7 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 231 1 2 2 1.9 Fc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4209274 164164 None 6 Human Binding pKi = 7.0 7.0 -1 8
Displacement of [3H]LSD from human 5-HT7 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT7 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 231 1 2 2 1.9 Fc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
2950739 163058 None 6 Human Binding pKi = 5.0 5.0 -4 3
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 351 9 1 4 4.6 COc1ccc(CNCCC(c2ccco2)c2ccccc2OC)cc1 10.1016/j.ejmech.2018.04.010
CHEMBL4174845 163058 None 6 Human Binding pKi = 5.0 5.0 -4 3
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 351 9 1 4 4.6 COc1ccc(CNCCC(c2ccco2)c2ccccc2OC)cc1 10.1016/j.ejmech.2018.04.010
57403525 70178 None 0 Human Binding pKi = 6.0 6.0 -691 10
Displacement of [3H]LSD from human 5-HT7 receptor by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT7 receptor by liquid scintillation counting
ChEMBL 361 6 1 2 4.8 OC1(c2ccc(Cl)cc2)CCN(CCCCc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
CHEMBL1940402 70178 None 0 Human Binding pKi = 6.0 6.0 -691 10
Displacement of [3H]LSD from human 5-HT7 receptor by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT7 receptor by liquid scintillation counting
ChEMBL 361 6 1 2 4.8 OC1(c2ccc(Cl)cc2)CCN(CCCCc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
21533446 70179 None 0 Human Binding pKi = 6.0 6.0 -281 10
Displacement of [3H]LSD from human 5-HT7 receptor by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT7 receptor by liquid scintillation counting
ChEMBL 379 6 1 3 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
CHEMBL1940403 70179 None 0 Human Binding pKi = 6.0 6.0 -281 10
Displacement of [3H]LSD from human 5-HT7 receptor by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT7 receptor by liquid scintillation counting
ChEMBL 379 6 1 3 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
122483264 138179 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting methodDisplacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting method
ChEMBL 334 6 0 3 5.1 O=C(CCCCCN1CCCC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
CHEMBL3763534 138179 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting methodDisplacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting method
ChEMBL 334 6 0 3 5.1 O=C(CCCCCN1CCCC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
CHEMBL3765840 138179 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting methodDisplacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting method
ChEMBL 334 6 0 3 5.1 O=C(CCCCCN1CCCC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
71726944 102459 None 0 Human Binding pKi = 5.0 5.0 1 3
Displacement of [3H]5-CT from human 5HT7b receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]5-CT from human 5HT7b receptor expressed in HEK293 cells after 1 hr
ChEMBL 342 2 0 4 3.3 CN1CCN(Cc2cccc3c(=O)c4ccc(Cl)cc4oc23)CC1 10.1016/j.bmcl.2013.05.062
CHEMBL3039669 102459 None 0 Human Binding pKi = 5.0 5.0 1 3
Displacement of [3H]5-CT from human 5HT7b receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]5-CT from human 5HT7b receptor expressed in HEK293 cells after 1 hr
ChEMBL 342 2 0 4 3.3 CN1CCN(Cc2cccc3c(=O)c4ccc(Cl)cc4oc23)CC1 10.1016/j.bmcl.2013.05.062
CHEMBL3215698 102459 None 0 Human Binding pKi = 5.0 5.0 1 3
Displacement of [3H]5-CT from human 5HT7b receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]5-CT from human 5HT7b receptor expressed in HEK293 cells after 1 hr
ChEMBL 342 2 0 4 3.3 CN1CCN(Cc2cccc3c(=O)c4ccc(Cl)cc4oc23)CC1 10.1016/j.bmcl.2013.05.062
44388796 128127 None 0 Rat Binding pKi = 7.0 7.0 - 1
Binding affinity against rat 5-HT7R expressed in HEK293 cellsBinding affinity against rat 5-HT7R expressed in HEK293 cells
ChEMBL 415 5 0 4 4.8 COc1ccccc1N1CCN(Cc2ccn(-c3ccccc3C(F)(F)F)c2)CC1 10.1016/j.bmcl.2005.05.059
CHEMBL366516 128127 None 0 Rat Binding pKi = 7.0 7.0 - 1
Binding affinity against rat 5-HT7R expressed in HEK293 cellsBinding affinity against rat 5-HT7R expressed in HEK293 cells
ChEMBL 415 5 0 4 4.8 COc1ccccc1N1CCN(Cc2ccn(-c3ccccc3C(F)(F)F)c2)CC1 10.1016/j.bmcl.2005.05.059
11131952 49368 None 0 Rat Binding pKi = 7.0 7.0 -1 2
Binding affinity to the rat 5-hydroxytryptamine 7 receptorBinding affinity to the rat 5-hydroxytryptamine 7 receptor
ChEMBL 353 8 1 5 3.4 O=C(CCCCCN1CCN(c2ccccn2)CC1)c1ccccc1O 10.1021/jm020994z
CHEMBL156385 49368 None 0 Rat Binding pKi = 7.0 7.0 -1 2
Binding affinity to the rat 5-hydroxytryptamine 7 receptorBinding affinity to the rat 5-hydroxytryptamine 7 receptor
ChEMBL 353 8 1 5 3.4 O=C(CCCCCN1CCN(c2ccccn2)CC1)c1ccccc1O 10.1021/jm020994z
156016142 177853 None 0 Human Binding pKi = 7.0 7.0 -5 5
Displacement of [3H]-5-CT from human 5HT7b receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-5-CT from human 5HT7b receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 506 8 0 6 5.3 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmc.2020.115459
CHEMBL4642594 177853 None 0 Human Binding pKi = 7.0 7.0 -5 5
Displacement of [3H]-5-CT from human 5HT7b receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-5-CT from human 5HT7b receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 506 8 0 6 5.3 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmc.2020.115459
155554326 175052 None 0 Human Binding pKi = 7.0 7.0 -13 5
Displacement of [3H]-5CT from human 5-HT7R expressed in human HEK293 cellsDisplacement of [3H]-5CT from human 5-HT7R expressed in human HEK293 cells
ChEMBL 457 9 0 6 3.2 COc1ccccc1N1CCN(CCCCCCN2C(=O)c3ccccc3S2(=O)=O)CC1 10.1016/j.bmcl.2021.128028
CHEMBL4565558 175052 None 0 Human Binding pKi = 7.0 7.0 -13 5
Displacement of [3H]-5CT from human 5-HT7R expressed in human HEK293 cellsDisplacement of [3H]-5CT from human 5-HT7R expressed in human HEK293 cells
ChEMBL 457 9 0 6 3.2 COc1ccccc1N1CCN(CCCCCCN2C(=O)c3ccccc3S2(=O)=O)CC1 10.1016/j.bmcl.2021.128028
10638372 174490 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHOK1 cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHOK1 cells
ChEMBL 306 4 0 2 3.0 O=C1Cc2ccccc2N1CCCN1CCc2ccccc2C1 10.1021/jm8014553
CHEMBL455210 174490 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHOK1 cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHOK1 cells
ChEMBL 306 4 0 2 3.0 O=C1Cc2ccccc2N1CCCN1CCc2ccccc2C1 10.1021/jm8014553
145946265 167612 None 0 Human Binding pKi = 6.0 6.0 -1 5
Displacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 396 10 0 4 3.9 Cc1cc(C)c(OCCOCCN2CCN(CCc3ccccc3)CC2)c(C)c1 10.1016/j.bmcl.2018.04.059
CHEMBL4203310 167612 None 0 Human Binding pKi = 6.0 6.0 -1 5
Displacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 396 10 0 4 3.9 Cc1cc(C)c(OCCOCCN2CCN(CCc3ccccc3)CC2)c(C)c1 10.1016/j.bmcl.2018.04.059
CHEMBL4299892 167612 None 0 Human Binding pKi = 6.0 6.0 -1 5
Displacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 396 10 0 4 3.9 Cc1cc(C)c(OCCOCCN2CCN(CCc3ccccc3)CC2)c(C)c1 10.1016/j.bmcl.2018.04.059
122483264 138179 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting methodDisplacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting method
ChEMBL 334 6 0 3 5.1 O=C(CCCCCN1CCCC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
CHEMBL3763534 138179 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting methodDisplacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting method
ChEMBL 334 6 0 3 5.1 O=C(CCCCCN1CCCC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
CHEMBL3765840 138179 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting methodDisplacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting method
ChEMBL 334 6 0 3 5.1 O=C(CCCCCN1CCCC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
155536533 172289 None 0 Human Binding pKi = 7.0 7.0 -2 2
Displacement of [3H]-5-HT from human 5HT7 receptor expressed in CHO-K1 cells incubated for 40 mins in presence of serotonin by liquid scintillation counterDisplacement of [3H]-5-HT from human 5HT7 receptor expressed in CHO-K1 cells incubated for 40 mins in presence of serotonin by liquid scintillation counter
ChEMBL 444 7 1 5 4.8 O=c1[nH]c(CCCCN2CCN(c3ccccc3)CC2)nc2cc(-c3ccccc3)sc12 10.1016/j.ejmech.2019.111690
CHEMBL4473636 172289 None 0 Human Binding pKi = 7.0 7.0 -2 2
Displacement of [3H]-5-HT from human 5HT7 receptor expressed in CHO-K1 cells incubated for 40 mins in presence of serotonin by liquid scintillation counterDisplacement of [3H]-5-HT from human 5HT7 receptor expressed in CHO-K1 cells incubated for 40 mins in presence of serotonin by liquid scintillation counter
ChEMBL 444 7 1 5 4.8 O=c1[nH]c(CCCCN2CCN(c3ccccc3)CC2)nc2cc(-c3ccccc3)sc12 10.1016/j.ejmech.2019.111690
155547693 173675 None 0 Human Binding pKi = 5.0 5.0 -51 5
Displacement of [3H]-5-CT from human 5-HT7R expressed in human HEK293 cells assessed as inhibitory constant incubated for 1 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT7R expressed in human HEK293 cells assessed as inhibitory constant incubated for 1 hr by radioligand binding assay
ChEMBL 314 4 1 7 1.1 Cc1cccc(OCc2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2019.06.022
CHEMBL4532712 173675 None 0 Human Binding pKi = 5.0 5.0 -51 5
Displacement of [3H]-5-CT from human 5-HT7R expressed in human HEK293 cells assessed as inhibitory constant incubated for 1 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT7R expressed in human HEK293 cells assessed as inhibitory constant incubated for 1 hr by radioligand binding assay
ChEMBL 314 4 1 7 1.1 Cc1cccc(OCc2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2019.06.022
164937988 195320 None 4 Human Binding pKi = 7.0 7.0 -23 21
Binding affinity to 5-HT7 (unknown origin) assessed as inhibition constantBinding affinity to 5-HT7 (unknown origin) assessed as inhibition constant
ChEMBL 338 5 0 5 3.4 c1ccc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1021/acs.jmedchem.3c00734
CHEMBL5400876 195320 None 4 Human Binding pKi = 7.0 7.0 -23 21
Binding affinity to 5-HT7 (unknown origin) assessed as inhibition constantBinding affinity to 5-HT7 (unknown origin) assessed as inhibition constant
ChEMBL 338 5 0 5 3.4 c1ccc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1021/acs.jmedchem.3c00734
90654683 110160 None 0 Human Binding pKi = 7.0 7.0 6 2
Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-countingDisplacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-counting
ChEMBL 452 8 1 4 2.9 NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCCCCN1CCN(c2ccc(F)cc2)CC1 10.1016/j.ejmech.2014.03.005
CHEMBL3235755 110160 None 0 Human Binding pKi = 7.0 7.0 6 2
Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-countingDisplacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-counting
ChEMBL 452 8 1 4 2.9 NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCCCCN1CCN(c2ccc(F)cc2)CC1 10.1016/j.ejmech.2014.03.005
44437860 91270 None 0 Human Binding pKi = 7.0 7.0 -48 3
Displacement of [3H]5-CT from human 5HT7 expressed in HEK293 cellsDisplacement of [3H]5-CT from human 5HT7 expressed in HEK293 cells
ChEMBL 411 6 0 4 3.2 CC1C(=O)N(CCCCN2CCN(c3cccc(C(F)(F)F)c3)CC2)C(=O)C1C 10.1016/j.bmc.2007.07.029
CHEMBL240110 91270 None 0 Human Binding pKi = 7.0 7.0 -48 3
Displacement of [3H]5-CT from human 5HT7 expressed in HEK293 cellsDisplacement of [3H]5-CT from human 5HT7 expressed in HEK293 cells
ChEMBL 411 6 0 4 3.2 CC1C(=O)N(CCCCN2CCN(c3cccc(C(F)(F)F)c3)CC2)C(=O)C1C 10.1016/j.bmc.2007.07.029
53325849 57025 None 0 Rat Binding pKi = 7.0 7.0 - 1
Displacement of [3H]5-CT from rat recombinant 5HT7 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]5-CT from rat recombinant 5HT7 receptor expressed in HEK293 cells after 60 mins
ChEMBL 322 3 1 2 4.5 Clc1ccc(-c2cn(Cc3ccccc3)c3c2CNCC3)cc1 10.1016/j.bmcl.2010.11.078
CHEMBL1644269 57025 None 0 Rat Binding pKi = 7.0 7.0 - 1
Displacement of [3H]5-CT from rat recombinant 5HT7 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]5-CT from rat recombinant 5HT7 receptor expressed in HEK293 cells after 60 mins
ChEMBL 322 3 1 2 4.5 Clc1ccc(-c2cn(Cc3ccccc3)c3c2CNCC3)cc1 10.1016/j.bmcl.2010.11.078
54758201 66014 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometryDisplacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometry
ChEMBL 451 6 1 3 5.7 O=C1Nc2c(Cl)cc(Cl)cc2C1CCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm200547z
CHEMBL1836782 66014 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometryDisplacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometry
ChEMBL 451 6 1 3 5.7 O=C1Nc2c(Cl)cc(Cl)cc2C1CCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm200547z
60165413 75386 None 0 Human Binding pKi = 7.0 7.0 -31 7
Displacement of [3H]LSD from human 5HT7 receptor by liquid scintillation countingDisplacement of [3H]LSD from human 5HT7 receptor by liquid scintillation counting
ChEMBL 378 7 0 4 5.5 O=C(CCCCN1CCC(c2ccccc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL2037531 75386 None 0 Human Binding pKi = 7.0 7.0 -31 7
Displacement of [3H]LSD from human 5HT7 receptor by liquid scintillation countingDisplacement of [3H]LSD from human 5HT7 receptor by liquid scintillation counting
ChEMBL 378 7 0 4 5.5 O=C(CCCCN1CCC(c2ccccc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
168288780 191557 None 0 Human Binding pKi = 6.0 6.0 -63 5
Displacement of [3H]-5-CT from human full length 5HT7BR expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-5-CT from human full length 5HT7BR expressed in HEK293 cells by radioligand binding assay
ChEMBL 447 8 0 6 3.9 O=c1n(CCCCCCN2CCN(c3cccc(C(F)(F)F)c3)CC2)nc2ccccn12 10.1016/j.ejmech.2022.114319
CHEMBL5193103 191557 None 0 Human Binding pKi = 6.0 6.0 -63 5
Displacement of [3H]-5-CT from human full length 5HT7BR expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-5-CT from human full length 5HT7BR expressed in HEK293 cells by radioligand binding assay
ChEMBL 447 8 0 6 3.9 O=c1n(CCCCCCN2CCN(c3cccc(C(F)(F)F)c3)CC2)nc2ccccn12 10.1016/j.ejmech.2022.114319
122483226 138193 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting methodDisplacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting method
ChEMBL 377 5 0 4 3.8 CC(=O)N1CCN(CCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
CHEMBL3763504 138193 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting methodDisplacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting method
ChEMBL 377 5 0 4 3.8 CC(=O)N1CCN(CCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
CHEMBL3765871 138193 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting methodDisplacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting method
ChEMBL 377 5 0 4 3.8 CC(=O)N1CCN(CCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
122483226 138193 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting methodDisplacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting method
ChEMBL 377 5 0 4 3.8 CC(=O)N1CCN(CCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
CHEMBL3763504 138193 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting methodDisplacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting method
ChEMBL 377 5 0 4 3.8 CC(=O)N1CCN(CCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
CHEMBL3765871 138193 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting methodDisplacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting method
ChEMBL 377 5 0 4 3.8 CC(=O)N1CCN(CCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
90654703 110145 None 0 Human Binding pKi = 7.0 7.0 26 2
Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-countingDisplacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-counting
ChEMBL 399 7 1 6 1.6 NC(=O)[C@@H]1CCCN1C(=O)CCCCN1CCN(c2noc3ccccc23)CC1 10.1016/j.ejmech.2014.03.005
CHEMBL3235740 110145 None 0 Human Binding pKi = 7.0 7.0 26 2
Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-countingDisplacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-counting
ChEMBL 399 7 1 6 1.6 NC(=O)[C@@H]1CCCN1C(=O)CCCCN1CCN(c2noc3ccccc23)CC1 10.1016/j.ejmech.2014.03.005
134147935 149777 None 0 Human Binding pKi = 7.0 7.0 18 4
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 487 10 1 6 3.6 N#Cc1ccc(CNC(=O)CCOCCN2CCN(c3cccnc3-c3ccc(F)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3947670 149777 None 0 Human Binding pKi = 7.0 7.0 18 4
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 487 10 1 6 3.6 N#Cc1ccc(CNC(=O)CCOCCN2CCN(c3cccnc3-c3ccc(F)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
154956306 179770 None 0 Rat Binding pKi = 7.0 7.0 -12 6
Displacement of [3H]5-CT from rat cerebral cortex 5HT7 receptor measured after 30 mins by liquid scintillation counting methodDisplacement of [3H]5-CT from rat cerebral cortex 5HT7 receptor measured after 30 mins by liquid scintillation counting method
ChEMBL 435 6 0 6 4.5 Cn1ccc2ccc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc2c1=O 10.1016/j.ejmech.2020.112709
CHEMBL4743324 179770 None 0 Rat Binding pKi = 7.0 7.0 -12 6
Displacement of [3H]5-CT from rat cerebral cortex 5HT7 receptor measured after 30 mins by liquid scintillation counting methodDisplacement of [3H]5-CT from rat cerebral cortex 5HT7 receptor measured after 30 mins by liquid scintillation counting method
ChEMBL 435 6 0 6 4.5 Cn1ccc2ccc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc2c1=O 10.1016/j.ejmech.2020.112709
90656690 111048 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in HEK293 cells after 30 mins by microbeta counting analysisDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in HEK293 cells after 30 mins by microbeta counting analysis
ChEMBL 325 7 2 4 2.8 OCc1cccc(NCCCN2CCN(c3ccccc3)CC2)c1 10.1016/j.ejmech.2014.04.034
CHEMBL3262418 111048 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in HEK293 cells after 30 mins by microbeta counting analysisDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in HEK293 cells after 30 mins by microbeta counting analysis
ChEMBL 325 7 2 4 2.8 OCc1cccc(NCCCN2CCN(c3ccccc3)CC2)c1 10.1016/j.ejmech.2014.04.034
118728522 117781 None 0 Human Binding pKi = 6.0 6.0 -3 2
Displacement of [3H]-8-OH-DPAT from human 5-HT7 receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-8-OH-DPAT from human 5-HT7 receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysis
ChEMBL 390 8 0 5 3.4 O=c1c2ccccc2ncn1CCCCCN1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2015.02.042
CHEMBL3401485 117781 None 0 Human Binding pKi = 6.0 6.0 -3 2
Displacement of [3H]-8-OH-DPAT from human 5-HT7 receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-8-OH-DPAT from human 5-HT7 receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysis
ChEMBL 390 8 0 5 3.4 O=c1c2ccccc2ncn1CCCCCN1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2015.02.042
164616670 184719 None 0 Human Binding pKi = 5.0 5.0 -53 3
Displacement of [3H]-5-CT from human 5-HT7R expressed in human HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-5-CT from human 5-HT7R expressed in human HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 424 7 1 7 3.8 CCCCC(Oc1cc(Cl)cc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4849077 184719 None 0 Human Binding pKi = 5.0 5.0 -53 3
Displacement of [3H]-5-CT from human 5-HT7R expressed in human HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-5-CT from human 5-HT7R expressed in human HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 424 7 1 7 3.8 CCCCC(Oc1cc(Cl)cc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
11726532 97079 None 0 Rat Binding pKi = 7.0 7.0 -141 4
Binding affinity to the rat 5-hydroxytryptamine 7 receptorBinding affinity to the rat 5-hydroxytryptamine 7 receptor
ChEMBL 368 8 0 5 3.5 COc1cccc(C(=O)CCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm020994z
CHEMBL26677 97079 None 0 Rat Binding pKi = 7.0 7.0 -141 4
Binding affinity to the rat 5-hydroxytryptamine 7 receptorBinding affinity to the rat 5-hydroxytryptamine 7 receptor
ChEMBL 368 8 0 5 3.5 COc1cccc(C(=O)CCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm020994z
44460669 208061 None 0 Human Binding pKi = 7.0 7.0 - 1
Binding affinity towards human 5-hydroxytryptamine 7 receptor on HEK293 cells using radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine 7 receptor on HEK293 cells using radioligand [3H]LSD
ChEMBL 283 4 0 3 2.9 C=Cc1ccc2ccn(CCN3CCCN(C)CC3)c2c1 10.1016/s0960-894x(02)00438-9
CHEMBL81576 208061 None 0 Human Binding pKi = 7.0 7.0 - 1
Binding affinity towards human 5-hydroxytryptamine 7 receptor on HEK293 cells using radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine 7 receptor on HEK293 cells using radioligand [3H]LSD
ChEMBL 283 4 0 3 2.9 C=Cc1ccc2ccn(CCN3CCCN(C)CC3)c2c1 10.1016/s0960-894x(02)00438-9
44460724 208078 None 0 Human Binding pKi = 7.0 7.0 - 1
Binding affinity towards human 5-hydroxytryptamine 7 receptor on HEK293 cells using radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine 7 receptor on HEK293 cells using radioligand [3H]LSD
ChEMBL 339 4 0 4 4.0 CN1CCCN(CCn2ccc3ccc(-c4ccsc4)cc32)CC1 10.1016/s0960-894x(02)00438-9
CHEMBL81684 208078 None 0 Human Binding pKi = 7.0 7.0 - 1
Binding affinity towards human 5-hydroxytryptamine 7 receptor on HEK293 cells using radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine 7 receptor on HEK293 cells using radioligand [3H]LSD
ChEMBL 339 4 0 4 4.0 CN1CCCN(CCn2ccc3ccc(-c4ccsc4)cc32)CC1 10.1016/s0960-894x(02)00438-9
168289915 191663 None 0 Human Binding pKi = 7.0 7.0 -2 5
Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 553 11 4 8 4.9 Nc1nc(NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)nc(NCCc2c[nH]c3ccccc23)n1 10.1016/j.ejmech.2021.113931
CHEMBL5194614 191663 None 0 Human Binding pKi = 7.0 7.0 -2 5
Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 553 11 4 8 4.9 Nc1nc(NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)nc(NCCc2c[nH]c3ccccc23)n1 10.1016/j.ejmech.2021.113931
60195992 81841 None 1 Human Binding pKi = 7.0 7.0 -1 2
Displacement of [3H]-5-CT from human cloned 5HT7 receptorDisplacement of [3H]-5-CT from human cloned 5HT7 receptor
ChEMBL 256 2 1 2 2.9 Fc1ccc(-c2cccc(N3CCNCC3)c2)cc1 10.1021/jm3003679
CHEMBL2164333 81841 None 1 Human Binding pKi = 7.0 7.0 -1 2
Displacement of [3H]-5-CT from human cloned 5HT7 receptorDisplacement of [3H]-5-CT from human cloned 5HT7 receptor
ChEMBL 256 2 1 2 2.9 Fc1ccc(-c2cccc(N3CCNCC3)c2)cc1 10.1021/jm3003679
10938620 206524 None 0 Human Binding pKi = 7.0 7.0 - 1
Binding affinity to human recombinant 5-hydroxytryptamine 7 receptor in mammalian cells using [3H]5-CT as radioligandBinding affinity to human recombinant 5-hydroxytryptamine 7 receptor in mammalian cells using [3H]5-CT as radioligand
ChEMBL 416 7 1 3 5.2 COc1ccc2c3c1CCCC3(CCCCN1CC=C(c3ccccc3)CC1)C(=O)N2 10.1021/jm0104264
CHEMBL70048 206524 None 0 Human Binding pKi = 7.0 7.0 - 1
Binding affinity to human recombinant 5-hydroxytryptamine 7 receptor in mammalian cells using [3H]5-CT as radioligandBinding affinity to human recombinant 5-hydroxytryptamine 7 receptor in mammalian cells using [3H]5-CT as radioligand
ChEMBL 416 7 1 3 5.2 COc1ccc2c3c1CCCC3(CCCCN1CC=C(c3ccccc3)CC1)C(=O)N2 10.1021/jm0104264
155538236 172474 None 0 Human Binding pKi = 6.0 6.0 -40 5
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 496 7 1 5 5.2 O=c1c(-c2ccccc2)c2n(c(=O)n1CCCCN1CCCC(c3c[nH]c4ccccc34)C1)CCCC2 10.1016/j.ejmech.2019.07.027
CHEMBL4476164 172474 None 0 Human Binding pKi = 6.0 6.0 -40 5
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 496 7 1 5 5.2 O=c1c(-c2ccccc2)c2n(c(=O)n1CCCCN1CCCC(c3c[nH]c4ccccc34)C1)CCCC2 10.1016/j.ejmech.2019.07.027
155515920 176789 None 0 Human Binding pKi = 6.0 6.0 -109 4
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 432 4 2 6 4.3 COc1ccc2c(c1)c(-c1[nH]c(N)nc1C)cn2S(=O)(=O)c1cccc2ccccc12 10.1016/j.ejmech.2019.06.001
CHEMBL4442332 176789 None 0 Human Binding pKi = 6.0 6.0 -109 4
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 432 4 2 6 4.3 COc1ccc2c(c1)c(-c1[nH]c(N)nc1C)cn2S(=O)(=O)c1cccc2ccccc12 10.1016/j.ejmech.2019.06.001
CHEMBL4598348 176789 None 0 Human Binding pKi = 6.0 6.0 -109 4
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 432 4 2 6 4.3 COc1ccc2c(c1)c(-c1[nH]c(N)nc1C)cn2S(=O)(=O)c1cccc2ccccc12 10.1016/j.ejmech.2019.06.001
28 3496 None 35 Human Binding pKi = 6.0 6.0 -2137 17
PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.6019/CHEMBL5442175
3292447 3496 None 35 Human Binding pKi = 6.0 6.0 -2137 17
PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.6019/CHEMBL5442175
CHEMBL20963 3496 None 35 Human Binding pKi = 6.0 6.0 -2137 17
PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.6019/CHEMBL5442175
46203754 124612 None 0 Rat Binding pKi = 8.0 8.0 - 1
Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.
ChEMBL 283 4 1 3 3.3 COc1ccc(-c2cccc(C)c2C)cc1OC1CNC1 nan
CHEMBL3640553 124612 None 0 Rat Binding pKi = 8.0 8.0 - 1
Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.
ChEMBL 283 4 1 3 3.3 COc1ccc(-c2cccc(C)c2C)cc1OC1CNC1 nan
10024070 67210 None 0 Rat Binding pKi = 8.0 8.0 - 1
Binding affinity towards rat 5-HT7 receptor expressed in HEK cellsBinding affinity towards rat 5-HT7 receptor expressed in HEK cells
ChEMBL 402 8 0 4 3.5 CCN(CCCN1CCc2cc(OC)ccc2C1)S(=O)(=O)c1ccc(C)cc1 10.1021/jm049743b
CHEMBL187764 67210 None 0 Rat Binding pKi = 8.0 8.0 - 1
Binding affinity towards rat 5-HT7 receptor expressed in HEK cellsBinding affinity towards rat 5-HT7 receptor expressed in HEK cells
ChEMBL 402 8 0 4 3.5 CCN(CCCN1CCc2cc(OC)ccc2C1)S(=O)(=O)c1ccc(C)cc1 10.1021/jm049743b
46203754 124612 None 0 Rat Binding pKi = 8.0 8.0 - 1
Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.
ChEMBL 283 4 1 3 3.3 COc1ccc(-c2cccc(C)c2C)cc1OC1CNC1 nan
CHEMBL3640553 124612 None 0 Rat Binding pKi = 8.0 8.0 - 1
Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.
ChEMBL 283 4 1 3 3.3 COc1ccc(-c2cccc(C)c2C)cc1OC1CNC1 nan
71458652 81466 None 0 Human Binding pKi = 8.0 8.0 -1 4
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr
ChEMBL 410 8 1 5 3.0 CSc1ccccc1OCCN1CCC(NS(=O)(=O)c2ccc(F)cc2)C1 10.1016/j.ejmech.2012.07.043
CHEMBL2159478 81466 None 0 Human Binding pKi = 8.0 8.0 -1 4
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr
ChEMBL 410 8 1 5 3.0 CSc1ccccc1OCCN1CCC(NS(=O)(=O)c2ccc(F)cc2)C1 10.1016/j.ejmech.2012.07.043
118731353 118176 None 0 Human Binding pKi = 8.0 8.0 5 2
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells after 1 hr
ChEMBL 524 10 1 4 4.9 NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCCCCCN1CCN(c2ccccc2-c2ccccc2)CC1 10.1016/j.ejmech.2014.12.041
CHEMBL3407516 118176 None 0 Human Binding pKi = 8.0 8.0 5 2
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells after 1 hr
ChEMBL 524 10 1 4 4.9 NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCCCCCN1CCN(c2ccccc2-c2ccccc2)CC1 10.1016/j.ejmech.2014.12.041
145980458 166813 None 0 Human Binding pKi = 8.0 8.0 1 3
Displacement of [3H]-5-carboxamidotryptamine from human 5-HT7B receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-5-carboxamidotryptamine from human 5-HT7B receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 476 6 2 5 2.9 CC1(c2ccc(F)cc2)NC(=O)N(CC(O)CN2CCN(c3cccc4ccccc34)CC2)C1=O 10.1039/C8MD00168E
CHEMBL4282860 166813 None 0 Human Binding pKi = 8.0 8.0 1 3
Displacement of [3H]-5-carboxamidotryptamine from human 5-HT7B receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-5-carboxamidotryptamine from human 5-HT7B receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 476 6 2 5 2.9 CC1(c2ccc(F)cc2)NC(=O)N(CC(O)CN2CCN(c3cccc4ccccc34)CC2)C1=O 10.1039/C8MD00168E
155526720 171313 None 0 Human Binding pKi = 8.0 8.0 3 2
Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHO cell membranes incubated for 120 mins by scintillation counting methodDisplacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHO cell membranes incubated for 120 mins by scintillation counting method
ChEMBL 437 6 1 3 5.9 Fc1ccc(N2CCN(CCCc3c[nH]c4ccc(F)cc34)CC2)c(-c2cccs2)c1 10.1016/j.bmcl.2019.126703
CHEMBL4459410 171313 None 0 Human Binding pKi = 8.0 8.0 3 2
Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHO cell membranes incubated for 120 mins by scintillation counting methodDisplacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHO cell membranes incubated for 120 mins by scintillation counting method
ChEMBL 437 6 1 3 5.9 Fc1ccc(N2CCN(CCCc3c[nH]c4ccc(F)cc34)CC2)c(-c2cccs2)c1 10.1016/j.bmcl.2019.126703
155552707 174152 None 0 Human Binding pKi = 8.0 8.0 1 2
Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHO cell membranes incubated for 120 mins by scintillation counting methodDisplacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHO cell membranes incubated for 120 mins by scintillation counting method
ChEMBL 421 6 1 3 5.5 Fc1ccc(N2CCN(CCCc3c[nH]c4ccc(F)cc34)CC2)c(-c2ccoc2)c1 10.1016/j.bmcl.2019.126703
CHEMBL4543789 174152 None 0 Human Binding pKi = 8.0 8.0 1 2
Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHO cell membranes incubated for 120 mins by scintillation counting methodDisplacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHO cell membranes incubated for 120 mins by scintillation counting method
ChEMBL 421 6 1 3 5.5 Fc1ccc(N2CCN(CCCc3c[nH]c4ccc(F)cc34)CC2)c(-c2ccoc2)c1 10.1016/j.bmcl.2019.126703
2726 919 None 48 Human Binding pKi = 8.0 8.0 -13 72
Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHOK1 cellsDisplacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHOK1 cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmc.2013.02.038
2726.0 919 None 48 Human Binding pKi = 8.0 8.0 -13 72
Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHOK1 cellsDisplacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHOK1 cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmc.2013.02.038
621 919 None 48 Human Binding pKi = 8.0 8.0 -13 72
Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHOK1 cellsDisplacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHOK1 cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmc.2013.02.038
83 919 None 48 Human Binding pKi = 8.0 8.0 -13 72
Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHOK1 cellsDisplacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHOK1 cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmc.2013.02.038
CHEMBL71 919 None 48 Human Binding pKi = 8.0 8.0 -13 72
Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHOK1 cellsDisplacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHOK1 cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmc.2013.02.038
DB00477 919 None 48 Human Binding pKi = 8.0 8.0 -13 72
Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHOK1 cellsDisplacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHOK1 cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmc.2013.02.038
54758204 66016 None 0 Human Binding pKi = 8.0 8.0 6 2
Displacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometryDisplacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometry
ChEMBL 395 7 1 3 4.4 CCC1(CCCCN2CCN(c3cccc(F)c3)CC2)C(=O)Nc2ccccc21 10.1021/jm200547z
CHEMBL1836784 66016 None 0 Human Binding pKi = 8.0 8.0 6 2
Displacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometryDisplacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometry
ChEMBL 395 7 1 3 4.4 CCC1(CCCCN2CCN(c3cccc(F)c3)CC2)C(=O)Nc2ccccc21 10.1021/jm200547z
11393666 193095 None 0 Human Binding pKi = 8.0 8.0 -28 19
Displacement of [3H]LSD from recombinant human 5-HT7 receptor measured after 120 mins by scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5-HT7 receptor measured after 120 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
CHEMBL5201983 193095 None 0 Human Binding pKi = 8.0 8.0 -28 19
Displacement of [3H]LSD from recombinant human 5-HT7 receptor measured after 120 mins by scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5-HT7 receptor measured after 120 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
CHEMBL5222597 193095 None 0 Human Binding pKi = 8.0 8.0 -28 19
Displacement of [3H]LSD from recombinant human 5-HT7 receptor measured after 120 mins by scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5-HT7 receptor measured after 120 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
42618267 182929 None 0 Human Binding pKi = 8.0 8.0 6 2
Inhibition of human 5HT7 receptor expressed in HEK293 cells by competitive binding assayInhibition of human 5HT7 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 398 7 1 4 4.0 O=c1[nH]c2ccccc2n1CCCCCN1CCN(c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2009.02.008
CHEMBL479105 182929 None 0 Human Binding pKi = 8.0 8.0 6 2
Inhibition of human 5HT7 receptor expressed in HEK293 cells by competitive binding assayInhibition of human 5HT7 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 398 7 1 4 4.0 O=c1[nH]c2ccccc2n1CCCCCN1CCN(c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2009.02.008
11683077 66023 None 0 Human Binding pKi = 8.0 8.0 1 2
Displacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometryDisplacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometry
ChEMBL 414 6 1 2 5.7 O=C1Nc2ccccc2C1CCCCN1CC=C(c2cccc(C(F)(F)F)c2)CC1 10.1021/jm200547z
CHEMBL1836791 66023 None 0 Human Binding pKi = 8.0 8.0 1 2
Displacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometryDisplacement of [3H]CT from human 5-HT7 receptor expressed in CHO cells by scintillation spectrometry
ChEMBL 414 6 1 2 5.7 O=C1Nc2ccccc2C1CCCCN1CC=C(c2cccc(C(F)(F)F)c2)CC1 10.1021/jm200547z
71061887 93171 None 0 Human Binding pKi = 8.0 8.0 66 2
Displacement of [3H]5-CT from human 5HT7 receptor transfected in HEK293 cells after 60 minsDisplacement of [3H]5-CT from human 5HT7 receptor transfected in HEK293 cells after 60 mins
ChEMBL 472 11 1 5 4.8 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)NCc3ccncc3)CC2)cc1 10.1016/j.bmc.2014.01.016
CHEMBL2442996 93171 None 0 Human Binding pKi = 8.0 8.0 66 2
Displacement of [3H]5-CT from human 5HT7 receptor transfected in HEK293 cells after 60 minsDisplacement of [3H]5-CT from human 5HT7 receptor transfected in HEK293 cells after 60 mins
ChEMBL 472 11 1 5 4.8 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)NCc3ccncc3)CC2)cc1 10.1016/j.bmc.2014.01.016
71061887 93171 None 0 Human Binding pKi = 8.0 8.0 66 2
Displacement of [3H]5-CT from human 5HT7A receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]5-CT from human 5HT7A receptor expressed in HEK293 cells after 60 mins
ChEMBL 472 11 1 5 4.8 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)NCc3ccncc3)CC2)cc1 10.1016/j.bmcl.2013.09.025
CHEMBL2442996 93171 None 0 Human Binding pKi = 8.0 8.0 66 2
Displacement of [3H]5-CT from human 5HT7A receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]5-CT from human 5HT7A receptor expressed in HEK293 cells after 60 mins
ChEMBL 472 11 1 5 4.8 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)NCc3ccncc3)CC2)cc1 10.1016/j.bmcl.2013.09.025
44266284 97397 None 0 Human Binding pKi = 8.0 8.0 - 1
Binding affinity at human cloned 5-hydroxytryptamine 7 receptor.Binding affinity at human cloned 5-hydroxytryptamine 7 receptor.
ChEMBL 377 5 0 3 5.1 Cc1ccccc1OC1CCN(CCC2CCCc3ccccc3C2=O)CC1 10.1016/s0960-894x(03)00077-5
CHEMBL269400 97397 None 0 Human Binding pKi = 8.0 8.0 - 1
Binding affinity at human cloned 5-hydroxytryptamine 7 receptor.Binding affinity at human cloned 5-hydroxytryptamine 7 receptor.
ChEMBL 377 5 0 3 5.1 Cc1ccccc1OC1CCN(CCC2CCCc3ccccc3C2=O)CC1 10.1016/s0960-894x(03)00077-5
22273749 210646 None 0 Human Binding pKi = 8.0 8.0 - 1
Binding affinity at human cloned 5-hydroxytryptamine 7 receptor.Binding affinity at human cloned 5-hydroxytryptamine 7 receptor.
ChEMBL 363 4 0 3 4.7 COc1ccccc1C1CCN(CC2CCc3ccccc3C(=O)C2)CC1 10.1016/s0960-894x(03)00077-5
CHEMBL9840 210646 None 0 Human Binding pKi = 8.0 8.0 - 1
Binding affinity at human cloned 5-hydroxytryptamine 7 receptor.Binding affinity at human cloned 5-hydroxytryptamine 7 receptor.
ChEMBL 363 4 0 3 4.7 COc1ccccc1C1CCN(CC2CCc3ccccc3C(=O)C2)CC1 10.1016/s0960-894x(03)00077-5
135398737 958 None 57 Human Binding pKi = 7.9 7.9 -13 91
Displacement of [3H]-LSD from human 5-HT7A receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT7A receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2020.115578
135398737.0 958 None 57 Human Binding pKi = 7.9 7.9 -13 91
Displacement of [3H]-LSD from human 5-HT7A receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT7A receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2020.115578
38 958 None 57 Human Binding pKi = 7.9 7.9 -13 91
Displacement of [3H]-LSD from human 5-HT7A receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT7A receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2020.115578
722 958 None 57 Human Binding pKi = 7.9 7.9 -13 91
Displacement of [3H]-LSD from human 5-HT7A receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT7A receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2020.115578
CHEMBL42 958 None 57 Human Binding pKi = 7.9 7.9 -13 91
Displacement of [3H]-LSD from human 5-HT7A receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT7A receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2020.115578
DB00363 958 None 57 Human Binding pKi = 7.9 7.9 -13 91
Displacement of [3H]-LSD from human 5-HT7A receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT7A receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2020.115578
11191128 85244 None 0 Rat Binding pKi = 7.9 7.9 2 4
Displacement of [3H]LSD from rat cloned 5-Hydroxytryptamine receptor 7 after 60 minsDisplacement of [3H]LSD from rat cloned 5-Hydroxytryptamine receptor 7 after 60 mins
ChEMBL 421 8 2 4 4.3 O=C(CCCCCN1CCN(c2ccccc2O)CC1)NC1CCCc2ccccc21 10.1021/acs.jmedchem.5b00982
CHEMBL225512 85244 None 0 Rat Binding pKi = 7.9 7.9 2 4
Displacement of [3H]LSD from rat cloned 5-Hydroxytryptamine receptor 7 after 60 minsDisplacement of [3H]LSD from rat cloned 5-Hydroxytryptamine receptor 7 after 60 mins
ChEMBL 421 8 2 4 4.3 O=C(CCCCCN1CCN(c2ccccc2O)CC1)NC1CCCc2ccccc21 10.1021/acs.jmedchem.5b00982
11191128 85244 None 0 Rat Binding pKi = 7.9 7.9 2 4
Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells
ChEMBL 421 8 2 4 4.3 O=C(CCCCCN1CCN(c2ccccc2O)CC1)NC1CCCc2ccccc21 10.1021/jm049702f
CHEMBL225512 85244 None 0 Rat Binding pKi = 7.9 7.9 2 4
Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells
ChEMBL 421 8 2 4 4.3 O=C(CCCCCN1CCN(c2ccccc2O)CC1)NC1CCCc2ccccc21 10.1021/jm049702f
134137732 147857 None 0 Human Binding pKi = 7.9 7.9 11 4
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 485 11 1 4 5.9 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)N[C@H](C)c3ccccc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3932551 147857 None 0 Human Binding pKi = 7.9 7.9 11 4
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 485 11 1 4 5.9 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)N[C@H](C)c3ccccc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
179 400 None 72 Human Binding pKi = 7.9 7.9 -9 50
Displacement of [3H]LSD from 5-HT7R (unknown origin) assessed as inhibition constant by competition binding assayDisplacement of [3H]LSD from 5-HT7R (unknown origin) assessed as inhibition constant by competition binding assay
ChEMBL 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC 10.1016/j.bmcl.2021.128275
2159 400 None 72 Human Binding pKi = 7.9 7.9 -9 50
Displacement of [3H]LSD from 5-HT7R (unknown origin) assessed as inhibition constant by competition binding assayDisplacement of [3H]LSD from 5-HT7R (unknown origin) assessed as inhibition constant by competition binding assay
ChEMBL 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC 10.1016/j.bmcl.2021.128275
2159.0 400 None 72 Human Binding pKi = 7.9 7.9 -9 50
Displacement of [3H]LSD from 5-HT7R (unknown origin) assessed as inhibition constant by competition binding assayDisplacement of [3H]LSD from 5-HT7R (unknown origin) assessed as inhibition constant by competition binding assay
ChEMBL 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC 10.1016/j.bmcl.2021.128275
963 400 None 72 Human Binding pKi = 7.9 7.9 -9 50
Displacement of [3H]LSD from 5-HT7R (unknown origin) assessed as inhibition constant by competition binding assayDisplacement of [3H]LSD from 5-HT7R (unknown origin) assessed as inhibition constant by competition binding assay
ChEMBL 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC 10.1016/j.bmcl.2021.128275
CHEMBL243712 400 None 72 Human Binding pKi = 7.9 7.9 -9 50
Displacement of [3H]LSD from 5-HT7R (unknown origin) assessed as inhibition constant by competition binding assayDisplacement of [3H]LSD from 5-HT7R (unknown origin) assessed as inhibition constant by competition binding assay
ChEMBL 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC 10.1016/j.bmcl.2021.128275
DB06288 400 None 72 Human Binding pKi = 7.9 7.9 -9 50
Displacement of [3H]LSD from 5-HT7R (unknown origin) assessed as inhibition constant by competition binding assayDisplacement of [3H]LSD from 5-HT7R (unknown origin) assessed as inhibition constant by competition binding assay
ChEMBL 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC 10.1016/j.bmcl.2021.128275
90656711 111031 None 0 Human Binding pKi = 7.9 7.9 - 1
Binding affinity to human recombinant 5-HT7 receptor expressed in CHO cells after 30 mins by radioligand displacement assayBinding affinity to human recombinant 5-HT7 receptor expressed in CHO cells after 30 mins by radioligand displacement assay
ChEMBL 371 4 2 3 4.4 Oc1ccc2[nH]cc(CCN3CCN(c4cccc5ccccc45)CC3)c2c1 10.1016/j.ejmech.2014.04.034
CHEMBL3262393 111031 None 0 Human Binding pKi = 7.9 7.9 - 1
Binding affinity to human recombinant 5-HT7 receptor expressed in CHO cells after 30 mins by radioligand displacement assayBinding affinity to human recombinant 5-HT7 receptor expressed in CHO cells after 30 mins by radioligand displacement assay
ChEMBL 371 4 2 3 4.4 Oc1ccc2[nH]cc(CCN3CCN(c4cccc5ccccc45)CC3)c2c1 10.1016/j.ejmech.2014.04.034
90656711 111031 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in HEK293 cells after 30 mins by microbeta counting analysisDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in HEK293 cells after 30 mins by microbeta counting analysis
ChEMBL 371 4 2 3 4.4 Oc1ccc2[nH]cc(CCN3CCN(c4cccc5ccccc45)CC3)c2c1 10.1016/j.ejmech.2014.04.034
CHEMBL3262393 111031 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in HEK293 cells after 30 mins by microbeta counting analysisDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in HEK293 cells after 30 mins by microbeta counting analysis
ChEMBL 371 4 2 3 4.4 Oc1ccc2[nH]cc(CCN3CCN(c4cccc5ccccc45)CC3)c2c1 10.1016/j.ejmech.2014.04.034
118713683 114452 None 0 Human Binding pKi = 7.9 7.9 -9 2
Displacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry
ChEMBL 409 9 0 6 4.0 COc1ccccc1N1CCN(CCCCCCn2c(=O)oc3ccccc32)CC1 10.1016/j.ejmech.2014.08.023
CHEMBL3331386 114452 None 0 Human Binding pKi = 7.9 7.9 -9 2
Displacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry
ChEMBL 409 9 0 6 4.0 COc1ccccc1N1CCN(CCCCCCn2c(=O)oc3ccccc32)CC1 10.1016/j.ejmech.2014.08.023
44266245 167313 None 0 Human Binding pKi = 7.9 7.9 6 2
Binding affinity at human cloned 5-hydroxytryptamine 7 receptor.Binding affinity at human cloned 5-hydroxytryptamine 7 receptor.
ChEMBL 398 5 0 3 4.3 O=C1c2ccccc2CCCN1CCN1CCC(Oc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(03)00077-5
CHEMBL429202 167313 None 0 Human Binding pKi = 7.9 7.9 6 2
Binding affinity at human cloned 5-hydroxytryptamine 7 receptor.Binding affinity at human cloned 5-hydroxytryptamine 7 receptor.
ChEMBL 398 5 0 3 4.3 O=C1c2ccccc2CCCN1CCN1CCC(Oc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(03)00077-5
136180320 117778 None 0 Human Binding pKi = 7.9 7.9 -1 2
Displacement of [3H]-8-OH-DPAT from human 5-HT7 receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-8-OH-DPAT from human 5-HT7 receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysis
ChEMBL 410 7 1 4 4.1 O=c1[nH]c(CCCCCN2CCN(c3cccc(Cl)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2015.02.042
CHEMBL3401482 117778 None 0 Human Binding pKi = 7.9 7.9 -1 2
Displacement of [3H]-8-OH-DPAT from human 5-HT7 receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-8-OH-DPAT from human 5-HT7 receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysis
ChEMBL 410 7 1 4 4.1 O=c1[nH]c(CCCCCN2CCN(c3cccc(Cl)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2015.02.042
164622487 186228 None 0 Human Binding pKi = 7.9 7.9 -1 5
Displacement of [3H]-LSD from human 5-HT7 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT7 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 339 4 0 4 2.8 O=C1c2ccc(F)cc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL4871850 186228 None 0 Human Binding pKi = 7.9 7.9 -1 5
Displacement of [3H]-LSD from human 5-HT7 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT7 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 339 4 0 4 2.8 O=C1c2ccc(F)cc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
2470 3653 None 40 Human Binding pKi = 7.0 7.0 -1258 59
Binding affinity towards human 5-hydroxytryptamine 7 receptorBinding affinity towards human 5-hydroxytryptamine 7 receptor
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
3300 3653 None 40 Human Binding pKi = 7.0 7.0 -1258 59
Binding affinity towards human 5-hydroxytryptamine 7 receptorBinding affinity towards human 5-hydroxytryptamine 7 receptor
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
5265 3653 None 40 Human Binding pKi = 7.0 7.0 -1258 59
Binding affinity towards human 5-hydroxytryptamine 7 receptorBinding affinity towards human 5-hydroxytryptamine 7 receptor
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
99 3653 None 40 Human Binding pKi = 7.0 7.0 -1258 59
Binding affinity towards human 5-hydroxytryptamine 7 receptorBinding affinity towards human 5-hydroxytryptamine 7 receptor
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
CHEMBL267930 3653 None 40 Human Binding pKi = 7.0 7.0 -1258 59
Binding affinity towards human 5-hydroxytryptamine 7 receptorBinding affinity towards human 5-hydroxytryptamine 7 receptor
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
CHEMBL5071978 216760 None 0 Human Binding pKi = 7.0 7.0 -1 6
Displacement of [3H] D-lysergic acid diethylamide from 5-HT7R (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by microbeta scintillation counter analysisDisplacement of [3H] D-lysergic acid diethylamide from 5-HT7R (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by microbeta scintillation counter analysis
ChEMBL None None None CCN(CC)Cc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
145976686 164017 None 0 Human Binding pKi = 7.0 7.0 24 2
Displacement of [3H]-5-CT from human serotonin 5-HT7B receptor expressed in HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-5-CT from human serotonin 5-HT7B receptor expressed in HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 564 7 1 4 3.9 O=S(=O)(NC1CCN(CCOc2cccc(Br)c2I)CC1)c1ccccc1 10.1021/acs.jmedchem.8b00828
CHEMBL4207365 164017 None 0 Human Binding pKi = 7.0 7.0 24 2
Displacement of [3H]-5-CT from human serotonin 5-HT7B receptor expressed in HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-5-CT from human serotonin 5-HT7B receptor expressed in HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 564 7 1 4 3.9 O=S(=O)(NC1CCN(CCOc2cccc(Br)c2I)CC1)c1ccccc1 10.1021/acs.jmedchem.8b00828
56944861 157166 None 0 Human Binding pKi = 7.0 7.0 -42 4
Displacement of [3H]-LSD from human 5-HT7 receptor expressed in CHO-K1 cell membranes after 120 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT7 receptor expressed in CHO-K1 cell membranes after 120 mins by scintillation counting
ChEMBL 493 8 2 3 5.8 O=S(=O)(NCCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc2ccccc2c1 10.1021/acs.jmedchem.7b00839
CHEMBL4074195 157166 None 0 Human Binding pKi = 7.0 7.0 -42 4
Displacement of [3H]-LSD from human 5-HT7 receptor expressed in CHO-K1 cell membranes after 120 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT7 receptor expressed in CHO-K1 cell membranes after 120 mins by scintillation counting
ChEMBL 493 8 2 3 5.8 O=S(=O)(NCCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc2ccccc2c1 10.1021/acs.jmedchem.7b00839
2470 3653 None 40 Human Binding pKi = 7.0 7.0 -1258 59
Displacement of [3H]5-HT from human 5-hydroxytryptamine 7 receptorDisplacement of [3H]5-HT from human 5-hydroxytryptamine 7 receptor
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
3300 3653 None 40 Human Binding pKi = 7.0 7.0 -1258 59
Displacement of [3H]5-HT from human 5-hydroxytryptamine 7 receptorDisplacement of [3H]5-HT from human 5-hydroxytryptamine 7 receptor
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
5265 3653 None 40 Human Binding pKi = 7.0 7.0 -1258 59
Displacement of [3H]5-HT from human 5-hydroxytryptamine 7 receptorDisplacement of [3H]5-HT from human 5-hydroxytryptamine 7 receptor
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
99 3653 None 40 Human Binding pKi = 7.0 7.0 -1258 59
Displacement of [3H]5-HT from human 5-hydroxytryptamine 7 receptorDisplacement of [3H]5-HT from human 5-hydroxytryptamine 7 receptor
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
CHEMBL267930 3653 None 40 Human Binding pKi = 7.0 7.0 -1258 59
Displacement of [3H]5-HT from human 5-hydroxytryptamine 7 receptorDisplacement of [3H]5-HT from human 5-hydroxytryptamine 7 receptor
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
2470 3653 None 40 Human Binding pKi = 7.0 7.0 -1258 59
Displacement of [3H]5-HT from human 5HT7 receptor expressed in African green monkey COS7 cell membrane incubated for 30 minsDisplacement of [3H]5-HT from human 5HT7 receptor expressed in African green monkey COS7 cell membrane incubated for 30 mins
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmc.2016.06.011
3300 3653 None 40 Human Binding pKi = 7.0 7.0 -1258 59
Displacement of [3H]5-HT from human 5HT7 receptor expressed in African green monkey COS7 cell membrane incubated for 30 minsDisplacement of [3H]5-HT from human 5HT7 receptor expressed in African green monkey COS7 cell membrane incubated for 30 mins
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmc.2016.06.011
5265 3653 None 40 Human Binding pKi = 7.0 7.0 -1258 59
Displacement of [3H]5-HT from human 5HT7 receptor expressed in African green monkey COS7 cell membrane incubated for 30 minsDisplacement of [3H]5-HT from human 5HT7 receptor expressed in African green monkey COS7 cell membrane incubated for 30 mins
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmc.2016.06.011
99 3653 None 40 Human Binding pKi = 7.0 7.0 -1258 59
Displacement of [3H]5-HT from human 5HT7 receptor expressed in African green monkey COS7 cell membrane incubated for 30 minsDisplacement of [3H]5-HT from human 5HT7 receptor expressed in African green monkey COS7 cell membrane incubated for 30 mins
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmc.2016.06.011
CHEMBL267930 3653 None 40 Human Binding pKi = 7.0 7.0 -1258 59
Displacement of [3H]5-HT from human 5HT7 receptor expressed in African green monkey COS7 cell membrane incubated for 30 minsDisplacement of [3H]5-HT from human 5HT7 receptor expressed in African green monkey COS7 cell membrane incubated for 30 mins
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmc.2016.06.011
11207101 75971 None 0 Rat Binding pKi = 6.0 6.0 - 1
Binding affinity towards rat 5-HT7 receptor expressed in HEK cellsBinding affinity towards rat 5-HT7 receptor expressed in HEK cells
ChEMBL 236 4 0 4 1.5 COc1ccc2c(c1)N(CCN(C)C)CCO2 10.1021/jm049743b
CHEMBL2051975 75971 None 0 Rat Binding pKi = 6.0 6.0 - 1
Binding affinity towards rat 5-HT7 receptor expressed in HEK cellsBinding affinity towards rat 5-HT7 receptor expressed in HEK cells
ChEMBL 236 4 0 4 1.5 COc1ccc2c(c1)N(CCN(C)C)CCO2 10.1021/jm049743b
9818448 127547 None 2 Rat Binding pKi = 6.0 6.0 -17 3
Binding affinity towards rat 5-HT7 receptor expressed in HEK cellsBinding affinity towards rat 5-HT7 receptor expressed in HEK cells
ChEMBL 318 4 1 2 4.5 COc1ccc2[nH]cc(C3=CCN(Cc4ccccc4)CC3)c2c1 10.1021/jm049743b
CHEMBL366081 127547 None 2 Rat Binding pKi = 6.0 6.0 -17 3
Binding affinity towards rat 5-HT7 receptor expressed in HEK cellsBinding affinity towards rat 5-HT7 receptor expressed in HEK cells
ChEMBL 318 4 1 2 4.5 COc1ccc2[nH]cc(C3=CCN(Cc4ccccc4)CC3)c2c1 10.1021/jm049743b
1353 1911 None 63 Human Binding pKi = 6.0 6.0 -263 85
Displacement of [3H]-5-carboxyamidotryptamine from human 5HT7 receptor by liquid scintillation counting methodDisplacement of [3H]-5-carboxyamidotryptamine from human 5HT7 receptor by liquid scintillation counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2016.06.011
3559 1911 None 63 Human Binding pKi = 6.0 6.0 -263 85
Displacement of [3H]-5-carboxyamidotryptamine from human 5HT7 receptor by liquid scintillation counting methodDisplacement of [3H]-5-carboxyamidotryptamine from human 5HT7 receptor by liquid scintillation counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2016.06.011
3559.0 1911 None 63 Human Binding pKi = 6.0 6.0 -263 85
Displacement of [3H]-5-carboxyamidotryptamine from human 5HT7 receptor by liquid scintillation counting methodDisplacement of [3H]-5-carboxyamidotryptamine from human 5HT7 receptor by liquid scintillation counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2016.06.011
86 1911 None 63 Human Binding pKi = 6.0 6.0 -263 85
Displacement of [3H]-5-carboxyamidotryptamine from human 5HT7 receptor by liquid scintillation counting methodDisplacement of [3H]-5-carboxyamidotryptamine from human 5HT7 receptor by liquid scintillation counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2016.06.011
CHEMBL54 1911 None 63 Human Binding pKi = 6.0 6.0 -263 85
Displacement of [3H]-5-carboxyamidotryptamine from human 5HT7 receptor by liquid scintillation counting methodDisplacement of [3H]-5-carboxyamidotryptamine from human 5HT7 receptor by liquid scintillation counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2016.06.011
DB00502 1911 None 63 Human Binding pKi = 6.0 6.0 -263 85
Displacement of [3H]-5-carboxyamidotryptamine from human 5HT7 receptor by liquid scintillation counting methodDisplacement of [3H]-5-carboxyamidotryptamine from human 5HT7 receptor by liquid scintillation counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2016.06.011
198914 146791 None 6 Human Binding pKi = 6.0 6.0 79 2
Displacement of [3H]5CT from 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]5CT from 5HT7 receptor expressed in HEK293 cells
ChEMBL 264 1 3 2 3.1 Oc1cccc(C2NCCc3c2[nH]c2ccccc32)c1 10.1016/j.bmcl.2007.01.093
CHEMBL392401 146791 None 6 Human Binding pKi = 6.0 6.0 79 2
Displacement of [3H]5CT from 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]5CT from 5HT7 receptor expressed in HEK293 cells
ChEMBL 264 1 3 2 3.1 Oc1cccc(C2NCCc3c2[nH]c2ccccc32)c1 10.1016/j.bmcl.2007.01.093
5048 3133 None 50 Human Binding pKi = 6.0 6.0 -537 10
PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.6019/CHEMBL5442175
8924 3133 None 50 Human Binding pKi = 6.0 6.0 -537 10
PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.6019/CHEMBL5442175
9948102 3133 None 50 Human Binding pKi = 6.0 6.0 -537 10
PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.6019/CHEMBL5442175
9948102.0 3133 None 50 Human Binding pKi = 6.0 6.0 -537 10
PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.6019/CHEMBL5442175
CHEMBL462605 3133 None 50 Human Binding pKi = 6.0 6.0 -537 10
PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.6019/CHEMBL5442175
DB11642 3133 None 50 Human Binding pKi = 6.0 6.0 -537 10
PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.6019/CHEMBL5442175
71460455 81397 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr
ChEMBL 430 9 1 4 4.6 CCOc1ccccc1C(=O)NC1CCN(CCOc2cccc(-c3ccccc3)c2)C1 10.1016/j.ejmech.2012.07.043
CHEMBL2159314 81397 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr
ChEMBL 430 9 1 4 4.6 CCOc1ccccc1C(=O)NC1CCN(CCOc2cccc(-c3ccccc3)c2)C1 10.1016/j.ejmech.2012.07.043
71462156 81402 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr
ChEMBL 445 6 1 4 5.1 O=C(NC1CCN(CCSc2cccc(Cl)c2Cl)C1)c1ccc2ccccc2n1 10.1016/j.ejmech.2012.07.043
CHEMBL2159319 81402 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr
ChEMBL 445 6 1 4 5.1 O=C(NC1CCN(CCSc2cccc(Cl)c2Cl)C1)c1ccc2ccccc2n1 10.1016/j.ejmech.2012.07.043
2435 722 None 63 Human Binding pKi = 6.0 6.0 -186 13
PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.6019/CHEMBL5442175
2435.0 722 None 63 Human Binding pKi = 6.0 6.0 -186 13
PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.6019/CHEMBL5442175
395 722 None 63 Human Binding pKi = 6.0 6.0 -186 13
PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.6019/CHEMBL5442175
520 722 None 63 Human Binding pKi = 6.0 6.0 -186 13
PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.6019/CHEMBL5442175
5386 722 None 63 Human Binding pKi = 6.0 6.0 -186 13
PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.6019/CHEMBL5442175
CHEMBL844 722 None 63 Human Binding pKi = 6.0 6.0 -186 13
PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.6019/CHEMBL5442175
DB00484 722 None 63 Human Binding pKi = 6.0 6.0 -186 13
PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.6019/CHEMBL5442175
90654673 110150 None 0 Human Binding pKi = 7.0 7.0 -54 2
Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-countingDisplacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-counting
ChEMBL 494 10 1 5 3.9 CSc1ccccc1N1CCN(CCCCCCC(=O)N2Cc3ccccc3C[C@H]2C(N)=O)CC1 10.1016/j.ejmech.2014.03.005
CHEMBL3235745 110150 None 0 Human Binding pKi = 7.0 7.0 -54 2
Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-countingDisplacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-counting
ChEMBL 494 10 1 5 3.9 CSc1ccccc1N1CCN(CCCCCCC(=O)N2Cc3ccccc3C[C@H]2C(N)=O)CC1 10.1016/j.ejmech.2014.03.005
11154555 800 None 50 Human Binding pKi = 7.0 7.0 -138 24
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2019.111736
11154555.0 800 None 50 Human Binding pKi = 7.0 7.0 -138 24
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2019.111736
5037 800 None 50 Human Binding pKi = 7.0 7.0 -138 24
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2019.111736
7671 800 None 50 Human Binding pKi = 7.0 7.0 -138 24
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2019.111736
CHEMBL2028019 800 None 50 Human Binding pKi = 7.0 7.0 -138 24
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2019.111736
CHEMBL3085826 800 None 50 Human Binding pKi = 7.0 7.0 -138 24
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2019.111736
DB06016 800 None 50 Human Binding pKi = 7.0 7.0 -138 24
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2019.111736
118736376 119012 None 0 Human Binding pKi = 7.0 7.0 -5 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHOK1 cells incubated for 60 mins by microbeta plate reader based methodDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHOK1 cells incubated for 60 mins by microbeta plate reader based method
ChEMBL 531 7 0 9 3.3 Cc1cn2c3c(=O)n(C)c(=O)n(C)c3nc2n1CCCCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1016/j.ejmech.2015.04.046
CHEMBL3423340 119012 None 0 Human Binding pKi = 7.0 7.0 -5 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHOK1 cells incubated for 60 mins by microbeta plate reader based methodDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHOK1 cells incubated for 60 mins by microbeta plate reader based method
ChEMBL 531 7 0 9 3.3 Cc1cn2c3c(=O)n(C)c(=O)n(C)c3nc2n1CCCCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1016/j.ejmech.2015.04.046
127052487 140887 None 0 Human Binding pKi = 7.0 7.0 -6 6
Displacement of [3H]LSD from human recombinant 5HT7 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human recombinant 5HT7 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 422 6 2 3 5.1 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2016.06.011
CHEMBL3818805 140887 None 0 Human Binding pKi = 7.0 7.0 -6 6
Displacement of [3H]LSD from human recombinant 5HT7 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human recombinant 5HT7 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 422 6 2 3 5.1 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2016.06.011
90656681 111043 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in HEK293 cells after 30 mins by microbeta counting analysisDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in HEK293 cells after 30 mins by microbeta counting analysis
ChEMBL 327 6 0 3 3.5 CN(CCCN1CCN(c2ccccc2)CC1)c1cccc(F)c1 10.1016/j.ejmech.2014.04.034
CHEMBL3262413 111043 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in HEK293 cells after 30 mins by microbeta counting analysisDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in HEK293 cells after 30 mins by microbeta counting analysis
ChEMBL 327 6 0 3 3.5 CN(CCCN1CCN(c2ccccc2)CC1)c1cccc(F)c1 10.1016/j.ejmech.2014.04.034
2146 3100 None 45 Human Binding pKi = 6.0 6.0 -14 11
PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.6019/CHEMBL5442175
485 3100 None 45 Human Binding pKi = 6.0 6.0 -14 11
PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.6019/CHEMBL5442175
6041 3100 None 45 Human Binding pKi = 6.0 6.0 -14 11
PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.6019/CHEMBL5442175
6041.0 3100 None 45 Human Binding pKi = 6.0 6.0 -14 11
PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.6019/CHEMBL5442175
CHEMBL1215 3100 None 45 Human Binding pKi = 6.0 6.0 -14 11
PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.6019/CHEMBL5442175
DB00388 3100 None 45 Human Binding pKi = 6.0 6.0 -14 11
PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.6019/CHEMBL5442175
155561995 175826 None 0 Human Binding pKi = 6.0 6.0 -36 5
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 532 7 1 5 5.4 O=c1c(-c2ccc(F)cc2)c2n(c(=O)n1CCCCN1CCCC(c3c[nH]c4ccc(F)cc34)C1)CCCC2 10.1016/j.ejmech.2019.07.027
CHEMBL4582567 175826 None 0 Human Binding pKi = 6.0 6.0 -36 5
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 532 7 1 5 5.4 O=c1c(-c2ccc(F)cc2)c2n(c(=O)n1CCCCN1CCCC(c3c[nH]c4ccc(F)cc34)C1)CCCC2 10.1016/j.ejmech.2019.07.027
155522218 170740 None 0 Human Binding pKi = 6.0 6.0 -51 5
Displacement of [3H]-5-CT from recombinant human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysisDisplacement of [3H]-5-CT from recombinant human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis
ChEMBL 492 7 1 5 5.3 O=c1c(-c2ccccc2)c2ccccn2c(=O)n1CCCCN1CCCC(c2c[nH]c3ccccc23)C1 10.1016/j.ejmech.2019.01.031
CHEMBL4451231 170740 None 0 Human Binding pKi = 6.0 6.0 -51 5
Displacement of [3H]-5-CT from recombinant human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysisDisplacement of [3H]-5-CT from recombinant human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis
ChEMBL 492 7 1 5 5.3 O=c1c(-c2ccccc2)c2ccccn2c(=O)n1CCCCN1CCCC(c2c[nH]c3ccccc23)C1 10.1016/j.ejmech.2019.01.031
145983018 165612 None 0 Human Binding pKi = 6.0 6.0 -125 5
Displacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 1 7 3.0 O=c1[nH]c2c(N3CCN(CC[C@@H]4CCCN4S(=O)(=O)c4cccc5ncccc45)CC3)cccc2o1 10.1016/j.ejmech.2018.01.002
CHEMBL4240910 165612 None 0 Human Binding pKi = 6.0 6.0 -125 5
Displacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 1 7 3.0 O=c1[nH]c2c(N3CCN(CC[C@@H]4CCCN4S(=O)(=O)c4cccc5ncccc45)CC3)cccc2o1 10.1016/j.ejmech.2018.01.002
46204083 124618 None 0 Rat Binding pKi = 7.0 7.0 - 1
Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.
ChEMBL 357 4 1 3 4.4 COc1ccc(-c2c(Cl)cccc2C(F)(F)F)cc1OC1CNC1 nan
CHEMBL3640559 124618 None 0 Rat Binding pKi = 7.0 7.0 - 1
Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.
ChEMBL 357 4 1 3 4.4 COc1ccc(-c2c(Cl)cccc2C(F)(F)F)cc1OC1CNC1 nan
46204083 124618 None 0 Rat Binding pKi = 7.0 7.0 - 1
Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.
ChEMBL 357 4 1 3 4.4 COc1ccc(-c2c(Cl)cccc2C(F)(F)F)cc1OC1CNC1 nan
CHEMBL3640559 124618 None 0 Rat Binding pKi = 7.0 7.0 - 1
Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.
ChEMBL 357 4 1 3 4.4 COc1ccc(-c2c(Cl)cccc2C(F)(F)F)cc1OC1CNC1 nan
118724648 116529 None 0 Human Binding pKi = 7.0 7.0 -5 3
Displacement of [3H]]-5-CT from human cloned 5-HT7R expressed in HEK293 cellsDisplacement of [3H]]-5-CT from human cloned 5-HT7R expressed in HEK293 cells
ChEMBL 515 7 0 10 1.5 Cn1c(=O)c2c(nc(N3CCOCC3)n2CCCCN2CCN(c3cccc(Cl)c3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3361005 116529 None 0 Human Binding pKi = 7.0 7.0 -5 3
Displacement of [3H]]-5-CT from human cloned 5-HT7R expressed in HEK293 cellsDisplacement of [3H]]-5-CT from human cloned 5-HT7R expressed in HEK293 cells
ChEMBL 515 7 0 10 1.5 Cn1c(=O)c2c(nc(N3CCOCC3)n2CCCCN2CCN(c3cccc(Cl)c3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
127052487 140887 None 0 Human Binding pKi = 7.0 7.0 -6 6
Displacement of [3H]LSD from human recombinant 5HT7 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human recombinant 5HT7 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 422 6 2 3 5.1 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2016.06.011
CHEMBL3818805 140887 None 0 Human Binding pKi = 7.0 7.0 -6 6
Displacement of [3H]LSD from human recombinant 5HT7 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human recombinant 5HT7 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 422 6 2 3 5.1 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2016.06.011
49756 206770 None 10 Rat Binding pKi = 6.0 6.0 -14 8
Binding affinity at rat 5-hydroxytryptamine 7 receptor.Binding affinity at rat 5-hydroxytryptamine 7 receptor.
ChEMBL 232 4 1 2 2.6 COc1ccc2[nH]c(C)c(CCN(C)C)c2c1 10.1021/jm030826m
CHEMBL7143 206770 None 10 Rat Binding pKi = 6.0 6.0 -14 8
Binding affinity at rat 5-hydroxytryptamine 7 receptor.Binding affinity at rat 5-hydroxytryptamine 7 receptor.
ChEMBL 232 4 1 2 2.6 COc1ccc2[nH]c(C)c(CCN(C)C)c2c1 10.1021/jm030826m
1353 1911 None 63 Human Binding pKi = 6.0 6.0 -263 85
Displacement of [3H]-5-carboxyamidotryptamine from human 5HT7 receptor by liquid scintillation counting methodDisplacement of [3H]-5-carboxyamidotryptamine from human 5HT7 receptor by liquid scintillation counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2016.06.011
3559 1911 None 63 Human Binding pKi = 6.0 6.0 -263 85
Displacement of [3H]-5-carboxyamidotryptamine from human 5HT7 receptor by liquid scintillation counting methodDisplacement of [3H]-5-carboxyamidotryptamine from human 5HT7 receptor by liquid scintillation counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2016.06.011
3559.0 1911 None 63 Human Binding pKi = 6.0 6.0 -263 85
Displacement of [3H]-5-carboxyamidotryptamine from human 5HT7 receptor by liquid scintillation counting methodDisplacement of [3H]-5-carboxyamidotryptamine from human 5HT7 receptor by liquid scintillation counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2016.06.011
86 1911 None 63 Human Binding pKi = 6.0 6.0 -263 85
Displacement of [3H]-5-carboxyamidotryptamine from human 5HT7 receptor by liquid scintillation counting methodDisplacement of [3H]-5-carboxyamidotryptamine from human 5HT7 receptor by liquid scintillation counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2016.06.011
CHEMBL54 1911 None 63 Human Binding pKi = 6.0 6.0 -263 85
Displacement of [3H]-5-carboxyamidotryptamine from human 5HT7 receptor by liquid scintillation counting methodDisplacement of [3H]-5-carboxyamidotryptamine from human 5HT7 receptor by liquid scintillation counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2016.06.011
DB00502 1911 None 63 Human Binding pKi = 6.0 6.0 -263 85
Displacement of [3H]-5-carboxyamidotryptamine from human 5HT7 receptor by liquid scintillation counting methodDisplacement of [3H]-5-carboxyamidotryptamine from human 5HT7 receptor by liquid scintillation counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2016.06.011
134154108 152709 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]D-lysergic acid diethylamide from 5HT7R (unknown origin) expressed in HEK293 cell membranes incubated for 1.5 hrs in absence of light by liquid scintillation countingDisplacement of [3H]D-lysergic acid diethylamide from 5HT7R (unknown origin) expressed in HEK293 cell membranes incubated for 1.5 hrs in absence of light by liquid scintillation counting
ChEMBL 309 4 0 2 4.9 COc1ccccc1-c1cc(CN2CCC(C)CC2)ccc1C 10.1016/j.ejmech.2016.07.029
CHEMBL3972166 152709 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]D-lysergic acid diethylamide from 5HT7R (unknown origin) expressed in HEK293 cell membranes incubated for 1.5 hrs in absence of light by liquid scintillation countingDisplacement of [3H]D-lysergic acid diethylamide from 5HT7R (unknown origin) expressed in HEK293 cell membranes incubated for 1.5 hrs in absence of light by liquid scintillation counting
ChEMBL 309 4 0 2 4.9 COc1ccccc1-c1cc(CN2CCC(C)CC2)ccc1C 10.1016/j.ejmech.2016.07.029
90654701 110143 None 0 Human Binding pKi = 7.0 7.0 -1 2
Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-countingDisplacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-counting
ChEMBL 426 7 1 4 2.8 NC(=O)[C@@H]1CCCN1C(=O)CCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.ejmech.2014.03.005
CHEMBL3235738 110143 None 0 Human Binding pKi = 7.0 7.0 -1 2
Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-countingDisplacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-counting
ChEMBL 426 7 1 4 2.8 NC(=O)[C@@H]1CCCN1C(=O)CCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.ejmech.2014.03.005
57398619 71590 None 0 Human Binding pKi = 7.0 7.0 7 3
Displacement of [3H]5-CT form human cloned 5HT7 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]5-CT form human cloned 5HT7 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 444 7 1 5 3.4 O=S(=O)(NCCCN1CCN(c2ccc(Cl)cc2)CC1)c1cncc2ccccc12 10.1016/j.bmc.2011.12.039
CHEMBL1949962 71590 None 0 Human Binding pKi = 7.0 7.0 7 3
Displacement of [3H]5-CT form human cloned 5HT7 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]5-CT form human cloned 5HT7 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 444 7 1 5 3.4 O=S(=O)(NCCCN1CCN(c2ccc(Cl)cc2)CC1)c1cncc2ccccc12 10.1016/j.bmc.2011.12.039
CHEMBL1963099 71590 None 0 Human Binding pKi = 7.0 7.0 7 3
Displacement of [3H]5-CT form human cloned 5HT7 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]5-CT form human cloned 5HT7 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 444 7 1 5 3.4 O=S(=O)(NCCCN1CCN(c2ccc(Cl)cc2)CC1)c1cncc2ccccc12 10.1016/j.bmc.2011.12.039
136180318 117776 None 0 Human Binding pKi = 6.0 6.0 -14 2
Displacement of [3H]-8-OH-DPAT from human 5-HT7 receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-8-OH-DPAT from human 5-HT7 receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysis
ChEMBL 396 6 1 4 3.7 O=c1[nH]c(CCCCN2CCN(c3ccc(Cl)cc3)CC2)nc2ccccc12 10.1016/j.bmcl.2015.02.042
CHEMBL3401480 117776 None 0 Human Binding pKi = 6.0 6.0 -14 2
Displacement of [3H]-8-OH-DPAT from human 5-HT7 receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-8-OH-DPAT from human 5-HT7 receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysis
ChEMBL 396 6 1 4 3.7 O=c1[nH]c(CCCCN2CCN(c3ccc(Cl)cc3)CC2)nc2ccccc12 10.1016/j.bmcl.2015.02.042
46204089 124625 None 0 Rat Binding pKi = 6.9 6.9 - 1
Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.
ChEMBL 283 4 1 3 3.3 COc1ccc(-c2cc(C)ccc2C)cc1OC1CNC1 nan
CHEMBL3640565 124625 None 0 Rat Binding pKi = 6.9 6.9 - 1
Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.
ChEMBL 283 4 1 3 3.3 COc1ccc(-c2cc(C)ccc2C)cc1OC1CNC1 nan
46204089 124625 None 0 Rat Binding pKi = 6.9 6.9 - 1
Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.
ChEMBL 283 4 1 3 3.3 COc1ccc(-c2cc(C)ccc2C)cc1OC1CNC1 nan
CHEMBL3640565 124625 None 0 Rat Binding pKi = 6.9 6.9 - 1
Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.
ChEMBL 283 4 1 3 3.3 COc1ccc(-c2cc(C)ccc2C)cc1OC1CNC1 nan
44286416 141505 None 0 Human Binding pKi = 6.9 6.9 -11 5
Displacement of [3H]-5-CT from human 5HT7b receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-5-CT from human 5HT7b receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 448 8 0 6 4.3 O=C1c2ccccc2C(=O)N1CCCCCCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmc.2020.115459
CHEMBL38409 141505 None 0 Human Binding pKi = 6.9 6.9 -11 5
Displacement of [3H]-5-CT from human 5HT7b receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-5-CT from human 5HT7b receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 448 8 0 6 4.3 O=C1c2ccccc2C(=O)N1CCCCCCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmc.2020.115459
156014787 177650 None 0 Human Binding pKi = 6.9 6.9 3 4
Displacement of [3H]-LSD from human 5-HT7A receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT7A receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 428 6 1 5 3.6 COc1cc2c3c(c1OCC1CC1)-c1cc(NS(C)(=O)=O)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
CHEMBL4640281 177650 None 0 Human Binding pKi = 6.9 6.9 3 4
Displacement of [3H]-LSD from human 5-HT7A receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT7A receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 428 6 1 5 3.6 COc1cc2c3c(c1OCC1CC1)-c1cc(NS(C)(=O)=O)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
15443 117874 None 64 Human Binding pKi = 6.9 6.9 -17 9
Displacement of [3H]-LSD from human 5-HT7 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT7 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.ejmech.2021.113243
CHEMBL340211 117874 None 64 Human Binding pKi = 6.9 6.9 -17 9
Displacement of [3H]-LSD from human 5-HT7 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT7 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.ejmech.2021.113243
15443 117874 None 64 Human Binding pKi = 6.9 6.9 -17 9
Displacement of [3H]-LSD from human 5HT7 receptor by liquid scintillation countingDisplacement of [3H]-LSD from human 5HT7 receptor by liquid scintillation counting
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL340211 117874 None 64 Human Binding pKi = 6.9 6.9 -17 9
Displacement of [3H]-LSD from human 5HT7 receptor by liquid scintillation countingDisplacement of [3H]-LSD from human 5HT7 receptor by liquid scintillation counting
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
162673483 183878 None 0 Human Binding pKi = 5.9 5.9 -2 2
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 396 8 2 5 2.3 COc1ccccc1N1CCN(CCCC(=O)Nc2ccccc2C(N)=O)CC1 10.1016/j.ejmech.2020.112437
CHEMBL4796251 183878 None 0 Human Binding pKi = 5.9 5.9 -2 2
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 396 8 2 5 2.3 COc1ccccc1N1CCN(CCCC(=O)Nc2ccccc2C(N)=O)CC1 10.1016/j.ejmech.2020.112437
CHEMBL4803945 183878 None 0 Human Binding pKi = 5.9 5.9 -2 2
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 396 8 2 5 2.3 COc1ccccc1N1CCN(CCCC(=O)Nc2ccccc2C(N)=O)CC1 10.1016/j.ejmech.2020.112437
71458622 81389 None 0 Human Binding pKi = 5.9 5.9 - 1
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr
ChEMBL 376 7 1 5 3.7 CSc1ccccc1OCCN1CCC(NC(=O)c2cccs2)CC1 10.1016/j.ejmech.2012.07.043
CHEMBL2159306 81389 None 0 Human Binding pKi = 5.9 5.9 - 1
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr
ChEMBL 376 7 1 5 3.7 CSc1ccccc1OCCN1CCC(NC(=O)c2cccs2)CC1 10.1016/j.ejmech.2012.07.043
71727068 91301 None 0 Human Binding pKi = 5.9 5.9 -2 4
Displacement of [3H]5-CT from human 5HT7b receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]5-CT from human 5HT7b receptor expressed in HEK293 cells after 1 hr
ChEMBL 430 5 0 6 4.3 COc1ccc2c(=O)c3cc(CN4CCN(c5ccccc5OC)CC4)ccc3oc2c1 10.1016/j.bmcl.2013.05.062
CHEMBL2401934 91301 None 0 Human Binding pKi = 5.9 5.9 -2 4
Displacement of [3H]5-CT from human 5HT7b receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]5-CT from human 5HT7b receptor expressed in HEK293 cells after 1 hr
ChEMBL 430 5 0 6 4.3 COc1ccc2c(=O)c3cc(CN4CCN(c5ccccc5OC)CC4)ccc3oc2c1 10.1016/j.bmcl.2013.05.062
CHEMBL2401938 91301 None 0 Human Binding pKi = 5.9 5.9 -2 4
Displacement of [3H]5-CT from human 5HT7b receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]5-CT from human 5HT7b receptor expressed in HEK293 cells after 1 hr
ChEMBL 430 5 0 6 4.3 COc1ccc2c(=O)c3cc(CN4CCN(c5ccccc5OC)CC4)ccc3oc2c1 10.1016/j.bmcl.2013.05.062
155510928 176574 None 0 Human Binding pKi = 5.9 5.9 -575 4
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 368 4 2 6 2.9 COc1ccc2c(c1)c(-c1cnc(N)[nH]1)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
CHEMBL4435010 176574 None 0 Human Binding pKi = 5.9 5.9 -575 4
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 368 4 2 6 2.9 COc1ccc2c(c1)c(-c1cnc(N)[nH]1)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
CHEMBL4596543 176574 None 0 Human Binding pKi = 5.9 5.9 -575 4
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 368 4 2 6 2.9 COc1ccc2c(c1)c(-c1cnc(N)[nH]1)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
13069623 120673 None 0 Human Binding pKi = 5.9 5.9 -50 4
Displacement of [3H]]-5-CT from human cloned 5-HT7R expressed in HEK293 cellsDisplacement of [3H]]-5-CT from human cloned 5-HT7R expressed in HEK293 cells
ChEMBL 396 6 0 8 1.0 Cn1c(=O)c2c(ncn2CCCCN2CCN(c3ccccc3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3360994 120673 None 0 Human Binding pKi = 5.9 5.9 -50 4
Displacement of [3H]]-5-CT from human cloned 5-HT7R expressed in HEK293 cellsDisplacement of [3H]]-5-CT from human cloned 5-HT7R expressed in HEK293 cells
ChEMBL 396 6 0 8 1.0 Cn1c(=O)c2c(ncn2CCCCN2CCN(c3ccccc3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3546108 120673 None 0 Human Binding pKi = 5.9 5.9 -50 4
Displacement of [3H]]-5-CT from human cloned 5-HT7R expressed in HEK293 cellsDisplacement of [3H]]-5-CT from human cloned 5-HT7R expressed in HEK293 cells
ChEMBL 396 6 0 8 1.0 Cn1c(=O)c2c(ncn2CCCCN2CCN(c3ccccc3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
44456400 12838 None 0 Human Binding pKi = 5.9 5.9 -4 10
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in HEK cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in HEK cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL1188501 12838 None 0 Human Binding pKi = 5.9 5.9 -4 10
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in HEK cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in HEK cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL2436555 12838 None 0 Human Binding pKi = 5.9 5.9 -4 10
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in HEK cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in HEK cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL536539 12838 None 0 Human Binding pKi = 5.9 5.9 -4 10
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in HEK cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in HEK cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
10317139 67097 None 0 Rat Binding pKi = 4.9 4.9 -758 2
In vitro ability to displace the radioligand [3H]5-CT from binding to rat 5-hydroxytryptamine 7 receptorIn vitro ability to displace the radioligand [3H]5-CT from binding to rat 5-hydroxytryptamine 7 receptor
ChEMBL 371 4 0 5 2.3 COc1ccccc1N1CCN([C@H]2CC[C@H](N3C(=O)CCC3=O)CC2)CC1 10.1016/j.bmcl.2004.09.029
CHEMBL187270 67097 None 0 Rat Binding pKi = 4.9 4.9 -758 2
In vitro ability to displace the radioligand [3H]5-CT from binding to rat 5-hydroxytryptamine 7 receptorIn vitro ability to displace the radioligand [3H]5-CT from binding to rat 5-hydroxytryptamine 7 receptor
ChEMBL 371 4 0 5 2.3 COc1ccccc1N1CCN([C@H]2CC[C@H](N3C(=O)CCC3=O)CC2)CC1 10.1016/j.bmcl.2004.09.029
145973438 164618 None 0 Human Binding pKi = 5.9 5.9 2 2
Displacement of [3H]-5-CT from human serotonin 5-HT7B receptor expressed in HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-5-CT from human serotonin 5-HT7B receptor expressed in HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 394 7 1 4 3.2 O=S(=O)(NC1CCN(CCOc2ccccc2)CC1)c1ccc(Cl)cc1 10.1021/acs.jmedchem.8b00828
CHEMBL4214853 164618 None 0 Human Binding pKi = 5.9 5.9 2 2
Displacement of [3H]-5-CT from human serotonin 5-HT7B receptor expressed in HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-5-CT from human serotonin 5-HT7B receptor expressed in HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 394 7 1 4 3.2 O=S(=O)(NC1CCN(CCOc2ccccc2)CC1)c1ccc(Cl)cc1 10.1021/acs.jmedchem.8b00828
145971588 164648 None 0 Human Binding pKi = 5.9 5.9 -1 2
Displacement of [3H]-5-CT from human serotonin 5-HT7B receptor expressed in HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-5-CT from human serotonin 5-HT7B receptor expressed in HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 438 7 1 4 3.3 O=S(=O)(NC1CCN(CCOc2ccccc2)CC1)c1cccc(Br)c1 10.1021/acs.jmedchem.8b00828
CHEMBL4215182 164648 None 0 Human Binding pKi = 5.9 5.9 -1 2
Displacement of [3H]-5-CT from human serotonin 5-HT7B receptor expressed in HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-5-CT from human serotonin 5-HT7B receptor expressed in HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 438 7 1 4 3.3 O=S(=O)(NC1CCN(CCOc2ccccc2)CC1)c1cccc(Br)c1 10.1021/acs.jmedchem.8b00828
155539483 172965 None 0 Human Binding pKi = 5.9 5.9 -162 5
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 504 7 2 3 5.4 O=C1CC(c2c[nH]c3ccc(F)cc23)C(=O)N1CCCCN1CCC(c2c[nH]c3ccc(F)cc23)CC1 10.1016/j.ejmech.2019.111736
CHEMBL4515160 172965 None 0 Human Binding pKi = 5.9 5.9 -162 5
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 504 7 2 3 5.4 O=C1CC(c2c[nH]c3ccc(F)cc23)C(=O)N1CCCCN1CCC(c2c[nH]c3ccc(F)cc23)CC1 10.1016/j.ejmech.2019.111736
44456400 12838 None 0 Human Binding pKi = 5.9 5.9 -4 10
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in HEK cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in HEK cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL1188501 12838 None 0 Human Binding pKi = 5.9 5.9 -4 10
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in HEK cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in HEK cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL2436555 12838 None 0 Human Binding pKi = 5.9 5.9 -4 10
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in HEK cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in HEK cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL536539 12838 None 0 Human Binding pKi = 5.9 5.9 -4 10
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in HEK cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in HEK cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
122181336 121944 None 0 Rat Binding pKi = 6.9 6.9 -8 3
Displacement of [3H]-5-CT from 5-HT7 receptor in rat hypothalamic membrane by liquid scintillation analysisDisplacement of [3H]-5-CT from 5-HT7 receptor in rat hypothalamic membrane by liquid scintillation analysis
ChEMBL 432 6 1 4 3.4 O=C1NC2(CCCc3ccccc32)C(=O)N1CCCCN1CCN(c2ccccc2)CC1 10.1016/j.bmc.2015.04.026
CHEMBL3590088 121944 None 0 Rat Binding pKi = 6.9 6.9 -8 3
Displacement of [3H]-5-CT from 5-HT7 receptor in rat hypothalamic membrane by liquid scintillation analysisDisplacement of [3H]-5-CT from 5-HT7 receptor in rat hypothalamic membrane by liquid scintillation analysis
ChEMBL 432 6 1 4 3.4 O=C1NC2(CCCc3ccccc32)C(=O)N1CCCCN1CCN(c2ccccc2)CC1 10.1016/j.bmc.2015.04.026
118731347 118248 None 0 Human Binding pKi = 6.9 6.9 -7 2
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells after 1 hr
ChEMBL 428 10 1 4 3.4 CC(C)c1ccccc1N1CCN(CCCCCCC(=O)N2CCC[C@H]2C(N)=O)CC1 10.1016/j.ejmech.2014.12.041
CHEMBL3409031 118248 None 0 Human Binding pKi = 6.9 6.9 -7 2
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells after 1 hr
ChEMBL 428 10 1 4 3.4 CC(C)c1ccccc1N1CCN(CCCCCCC(=O)N2CCC[C@H]2C(N)=O)CC1 10.1016/j.ejmech.2014.12.041
44455426 155239 None 0 Human Binding pKi = 6.9 6.9 -1 12
Inhibition of human cloned 5HT7 receptor by competitive binding experimentInhibition of human cloned 5HT7 receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL402143 155239 None 0 Human Binding pKi = 6.9 6.9 -1 12
Inhibition of human cloned 5HT7 receptor by competitive binding experimentInhibition of human cloned 5HT7 receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
72198191 89854 None 0 Human Binding pKi = 5.9 5.9 -144 4
Displacement of [3H]-5CT from human 5HT7 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5CT from human 5HT7 receptor expressed in HEK293 cells after 1 hr
ChEMBL 458 5 2 3 4.5 O=C1CC(c2c[nH]c3ccccc23)C(=O)N1CCN1CCC(c2c[nH]c3ccc(F)cc23)CC1 10.1016/j.ejmech.2013.02.033
CHEMBL2377445 89854 None 0 Human Binding pKi = 5.9 5.9 -144 4
Displacement of [3H]-5CT from human 5HT7 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5CT from human 5HT7 receptor expressed in HEK293 cells after 1 hr
ChEMBL 458 5 2 3 4.5 O=C1CC(c2c[nH]c3ccccc23)C(=O)N1CCN1CCC(c2c[nH]c3ccc(F)cc23)CC1 10.1016/j.ejmech.2013.02.033
46205373 124654 None 0 Rat Binding pKi = 6.9 6.9 - 1
Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.
ChEMBL 321 3 1 2 4.5 COc1ccc(-c2cccc(C(F)(F)F)c2)cc1C1CCNC1 nan
CHEMBL3640593 124654 None 0 Rat Binding pKi = 6.9 6.9 - 1
Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.Binding Assay: Receptor binding was performed using membrane fractions prepared from the HEK-293 cell line recombinantly expressing rat 5-HT7 receptors (NCBI accession NM022938). Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assays using 5-carboxamido[3H]tryptamine ([3H]5-CT) (Amersham Biosciences, cat. 90000403) detection. HitHunter cAMP assays are in-vitro based competitive immunoassays. The assay was performed on the HEK-293 cell line stably transfected with r5-HT7 receptor. Cells were pre-incubated with test compounds for 10 minutes.
ChEMBL 321 3 1 2 4.5 COc1ccc(-c2cccc(C(F)(F)F)c2)cc1C1CCNC1 nan
46205373 124654 None 0 Rat Binding pKi = 6.9 6.9 - 1
Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.
ChEMBL 321 3 1 2 4.5 COc1ccc(-c2cccc(C(F)(F)F)c2)cc1C1CCNC1 nan
CHEMBL3640593 124654 None 0 Rat Binding pKi = 6.9 6.9 - 1
Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.Biological Assay: Compound affinity for the rat 5-HT7 receptor subtype was evaluated by competitive radioligand binding assay using 5-carboxamido[H3]typtamine ([3H]5-CT)(Amersham Biosciences) detection.
ChEMBL 321 3 1 2 4.5 COc1ccc(-c2cccc(C(F)(F)F)c2)cc1C1CCNC1 nan
122181339 121947 None 0 Rat Binding pKi = 6.9 6.9 -22 3
Displacement of [3H]-5-CT from 5-HT7 receptor in rat hypothalamic membrane by liquid scintillation analysisDisplacement of [3H]-5-CT from 5-HT7 receptor in rat hypothalamic membrane by liquid scintillation analysis
ChEMBL 500 6 1 4 4.4 O=C1NC2(CCCc3ccccc32)C(=O)N1CCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2015.04.026
CHEMBL3590091 121947 None 0 Rat Binding pKi = 6.9 6.9 -22 3
Displacement of [3H]-5-CT from 5-HT7 receptor in rat hypothalamic membrane by liquid scintillation analysisDisplacement of [3H]-5-CT from 5-HT7 receptor in rat hypothalamic membrane by liquid scintillation analysis
ChEMBL 500 6 1 4 4.4 O=C1NC2(CCCc3ccccc32)C(=O)N1CCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2015.04.026
156013203 177587 None 0 Human Binding pKi = 6.9 6.9 -3 5
Displacement of [3H]-5-CT from human 5HT7b receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-5-CT from human 5HT7b receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 477 8 0 4 4.7 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmc.2020.115459
CHEMBL4639203 177587 None 0 Human Binding pKi = 6.9 6.9 -3 5
Displacement of [3H]-5-CT from human 5HT7b receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-5-CT from human 5HT7b receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 477 8 0 4 4.7 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmc.2020.115459
156021656 178292 None 0 Human Binding pKi = 6.9 6.9 -3 2
Displacement of [3H]-5-carboxamidotryptamine from human 5-HT7A receptor expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting methodDisplacement of [3H]-5-carboxamidotryptamine from human 5-HT7A receptor expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting method
ChEMBL 269 2 0 1 3.9 CN(C)C1CCc2c(cccc2-c2ccc(F)cc2)C1 10.1016/j.bmc.2019.115262
CHEMBL4649308 178292 None 0 Human Binding pKi = 6.9 6.9 -3 2
Displacement of [3H]-5-carboxamidotryptamine from human 5-HT7A receptor expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting methodDisplacement of [3H]-5-carboxamidotryptamine from human 5-HT7A receptor expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting method
ChEMBL 269 2 0 1 3.9 CN(C)C1CCc2c(cccc2-c2ccc(F)cc2)C1 10.1016/j.bmc.2019.115262
162647097 179825 None 0 Human Binding pKi = 6.9 6.9 -125 4
Displacement of [3H]-LSD from recombinant human 5HT7 receptor expressed in CHOK1 cell membranes measured after 120 mins by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT7 receptor expressed in CHOK1 cell membranes measured after 120 mins by microbeta counting method
ChEMBL 465 8 1 6 4.0 COc1ccc2cc(S(=O)(=O)N[C@@H]3CCN(CCCc4noc5ccccc45)C3)ccc2c1 10.1016/j.ejmech.2020.112149
CHEMBL4744007 179825 None 0 Human Binding pKi = 6.9 6.9 -125 4
Displacement of [3H]-LSD from recombinant human 5HT7 receptor expressed in CHOK1 cell membranes measured after 120 mins by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT7 receptor expressed in CHOK1 cell membranes measured after 120 mins by microbeta counting method
ChEMBL 465 8 1 6 4.0 COc1ccc2cc(S(=O)(=O)N[C@@H]3CCN(CCCc4noc5ccccc45)C3)ccc2c1 10.1016/j.ejmech.2020.112149
156020908 178136 None 0 Human Binding pKi = 6.9 6.9 -2 5
Displacement of [3H]-5-CT from human 5HT7b receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-5-CT from human 5HT7b receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 498 8 0 6 5.4 O=C1c2cccc3cccc(c23)C(=O)N1CCCCCCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmc.2020.115459
CHEMBL4646868 178136 None 0 Human Binding pKi = 6.9 6.9 -2 5
Displacement of [3H]-5-CT from human 5HT7b receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-5-CT from human 5HT7b receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 498 8 0 6 5.4 O=C1c2cccc3cccc(c23)C(=O)N1CCCCCCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmc.2020.115459
54758298 66029 None 0 Human Binding pKi = 6.9 6.9 -4 3
Displacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry
ChEMBL 401 6 1 3 4.5 O=C1Nc2cc(F)ccc2C1CCCCN1CCN(c2cccc(Cl)c2)CC1 10.1016/j.ejmech.2014.08.023
CHEMBL1836857 66029 None 0 Human Binding pKi = 6.9 6.9 -4 3
Displacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry
ChEMBL 401 6 1 3 4.5 O=C1Nc2cc(F)ccc2C1CCCCN1CCN(c2cccc(Cl)c2)CC1 10.1016/j.ejmech.2014.08.023
11207101 75971 None 0 Rat Binding pKi = 5.9 5.9 - 1
Binding affinity towards rat 5-HT7 receptor expressed in HEK cellsBinding affinity towards rat 5-HT7 receptor expressed in HEK cells
ChEMBL 236 4 0 4 1.5 COc1ccc2c(c1)N(CCN(C)C)CCO2 10.1021/jm049743b
CHEMBL2051975 75971 None 0 Rat Binding pKi = 5.9 5.9 - 1
Binding affinity towards rat 5-HT7 receptor expressed in HEK cellsBinding affinity towards rat 5-HT7 receptor expressed in HEK cells
ChEMBL 236 4 0 4 1.5 COc1ccc2c(c1)N(CCN(C)C)CCO2 10.1021/jm049743b
44263956 206906 None 0 Rat Binding pKi = 5.9 5.9 -2 2
Binding affinity towards rat 5-HT7 receptor expressed in HEK cellsBinding affinity towards rat 5-HT7 receptor expressed in HEK cells
ChEMBL 232 4 0 3 2.3 COc1ccc2c(c1)c(CCN(C)C)cn2C 10.1021/jm049743b
CHEMBL7220 206906 None 0 Rat Binding pKi = 5.9 5.9 -2 2
Binding affinity towards rat 5-HT7 receptor expressed in HEK cellsBinding affinity towards rat 5-HT7 receptor expressed in HEK cells
ChEMBL 232 4 0 3 2.3 COc1ccc2c(c1)c(CCN(C)C)cn2C 10.1021/jm049743b
90654700 110142 None 0 Human Binding pKi = 5.9 5.9 -2 2
Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-countingDisplacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-counting
ChEMBL 390 8 1 4 2.0 NC(=O)[C@@H]1CCCN1C(=O)CCCCCN1CCN(c2ccc(F)cc2)CC1 10.1016/j.ejmech.2014.03.005
CHEMBL3235737 110142 None 0 Human Binding pKi = 5.9 5.9 -2 2
Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-countingDisplacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-counting
ChEMBL 390 8 1 4 2.0 NC(=O)[C@@H]1CCCN1C(=O)CCCCCN1CCN(c2ccc(F)cc2)CC1 10.1016/j.ejmech.2014.03.005
71454899 81191 None 0 Human Binding pKi = 5.9 5.9 - 1
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr
ChEMBL 428 10 1 5 4.3 CCOc1ccccc1C(=O)NCC1CCN(CCOc2ccccc2SC)CC1 10.1016/j.ejmech.2012.07.043
CHEMBL2158026 81191 None 0 Human Binding pKi = 5.9 5.9 - 1
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr
ChEMBL 428 10 1 5 4.3 CCOc1ccccc1C(=O)NCC1CCN(CCOc2ccccc2SC)CC1 10.1016/j.ejmech.2012.07.043
155526651 171277 None 0 Human Binding pKi = 6.9 6.9 -5 5
Displacement of [3H]-5-CT from recombinant human 5HT7B receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-5-CT from recombinant human 5HT7B receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 464 8 0 4 5.7 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc3cccnc23)CC1 10.1016/j.bmcl.2019.06.029
CHEMBL4458938 171277 None 0 Human Binding pKi = 6.9 6.9 -5 5
Displacement of [3H]-5-CT from recombinant human 5HT7B receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-5-CT from recombinant human 5HT7B receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 464 8 0 4 5.7 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc3cccnc23)CC1 10.1016/j.bmcl.2019.06.029
155540823 172643 None 0 Human Binding pKi = 6.9 6.9 -7 2
Displacement of [3H]-5-HT from human 5-HT7 receptor expressed in CHOK1 cell membranes after 30 mins by liquid scintillation spectrometryDisplacement of [3H]-5-HT from human 5-HT7 receptor expressed in CHOK1 cell membranes after 30 mins by liquid scintillation spectrometry
ChEMBL 456 7 0 5 3.6 CCOc1ccccc1N1CCN(CCC(=O)N2CCN(c3cccc(Cl)c3)CC2)CC1 10.1016/j.bmcl.2016.06.080
CHEMBL4483779 172643 None 0 Human Binding pKi = 6.9 6.9 -7 2
Displacement of [3H]-5-HT from human 5-HT7 receptor expressed in CHOK1 cell membranes after 30 mins by liquid scintillation spectrometryDisplacement of [3H]-5-HT from human 5-HT7 receptor expressed in CHOK1 cell membranes after 30 mins by liquid scintillation spectrometry
ChEMBL 456 7 0 5 3.6 CCOc1ccccc1N1CCN(CCC(=O)N2CCN(c3cccc(Cl)c3)CC2)CC1 10.1016/j.bmcl.2016.06.080
2726 919 None 48 Human Binding pKi = 6.9 6.9 -13 72
Displacement of [3H]LSD from 5-HT7 receptor (unknown origin)Displacement of [3H]LSD from 5-HT7 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
2726.0 919 None 48 Human Binding pKi = 6.9 6.9 -13 72
Displacement of [3H]LSD from 5-HT7 receptor (unknown origin)Displacement of [3H]LSD from 5-HT7 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
621 919 None 48 Human Binding pKi = 6.9 6.9 -13 72
Displacement of [3H]LSD from 5-HT7 receptor (unknown origin)Displacement of [3H]LSD from 5-HT7 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
83 919 None 48 Human Binding pKi = 6.9 6.9 -13 72
Displacement of [3H]LSD from 5-HT7 receptor (unknown origin)Displacement of [3H]LSD from 5-HT7 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
CHEMBL71 919 None 48 Human Binding pKi = 6.9 6.9 -13 72
Displacement of [3H]LSD from 5-HT7 receptor (unknown origin)Displacement of [3H]LSD from 5-HT7 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
DB00477 919 None 48 Human Binding pKi = 6.9 6.9 -13 72
Displacement of [3H]LSD from 5-HT7 receptor (unknown origin)Displacement of [3H]LSD from 5-HT7 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
11409589 85164 None 0 Rat Binding pKi = 6.9 6.9 -1 2
Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells
ChEMBL 435 9 1 4 4.6 COc1cccc(N2CCN(CCCCCC(=O)NC3CCCc4ccccc43)CC2)c1 10.1021/jm049702f
CHEMBL224883 85164 None 0 Rat Binding pKi = 6.9 6.9 -1 2
Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells
ChEMBL 435 9 1 4 4.6 COc1cccc(N2CCN(CCCCCC(=O)NC3CCCc4ccccc43)CC2)c1 10.1021/jm049702f
127029649 138259 None 0 Human Binding pKi = 5.9 5.9 5 3
Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cellsDisplacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells
ChEMBL 462 6 2 5 2.1 CC1(c2ccc(F)cc2)NC(=O)N(CC(O)CN2CCN(c3ccc(F)cc3F)CC2)C1=O 10.1016/j.ejmech.2016.02.024
CHEMBL3769536 138259 None 0 Human Binding pKi = 5.9 5.9 5 3
Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cellsDisplacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells
ChEMBL 462 6 2 5 2.1 CC1(c2ccc(F)cc2)NC(=O)N(CC(O)CN2CCN(c3ccc(F)cc3F)CC2)C1=O 10.1016/j.ejmech.2016.02.024
126720403 162705 None 0 Human Binding pKi = 4.9 4.9 -933 5
Displacement of [3H]-5-CT from human 5HT7BR expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-5-CT from human 5HT7BR expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 353 4 1 5 3.2 CC(C)c1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(F)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4169236 162705 None 0 Human Binding pKi = 4.9 4.9 -933 5
Displacement of [3H]-5-CT from human 5HT7BR expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-5-CT from human 5HT7BR expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 353 4 1 5 3.2 CC(C)c1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(F)c1 10.1016/j.ejmech.2017.12.053
155542321 173228 None 0 Human Binding pKi = 4.9 4.9 -1096 5
Displacement of [3H]-5-CT from human 5-HT7R expressed in human HEK293 cells assessed as inhibitory constant incubated for 1 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT7R expressed in human HEK293 cells assessed as inhibitory constant incubated for 1 hr by radioligand binding assay
ChEMBL 356 5 1 7 2.2 Cc1ccc(C(C)C)c(OCc2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2019.06.022
CHEMBL4520796 173228 None 0 Human Binding pKi = 4.9 4.9 -1096 5
Displacement of [3H]-5-CT from human 5-HT7R expressed in human HEK293 cells assessed as inhibitory constant incubated for 1 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT7R expressed in human HEK293 cells assessed as inhibitory constant incubated for 1 hr by radioligand binding assay
ChEMBL 356 5 1 7 2.2 Cc1ccc(C(C)C)c(OCc2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2019.06.022
155542321 173228 None 0 Human Binding pKi = 4.9 4.9 -1096 5
Displacement of [3H]-5Carboxyamidotryptamine from human 5-HT7R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-5Carboxyamidotryptamine from human 5-HT7R expressed in HEK293 cells by radioligand binding assay
ChEMBL 356 5 1 7 2.2 Cc1ccc(C(C)C)c(OCc2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2022.114645
CHEMBL4520796 173228 None 0 Human Binding pKi = 4.9 4.9 -1096 5
Displacement of [3H]-5Carboxyamidotryptamine from human 5-HT7R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-5Carboxyamidotryptamine from human 5-HT7R expressed in HEK293 cells by radioligand binding assay
ChEMBL 356 5 1 7 2.2 Cc1ccc(C(C)C)c(OCc2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2022.114645
90654685 110162 None 0 Human Binding pKi = 5.9 5.9 -5 2
Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-countingDisplacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-counting
ChEMBL 522 5 1 4 4.4 NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)c1ccc(CN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.ejmech.2014.03.005
CHEMBL3235757 110162 None 0 Human Binding pKi = 5.9 5.9 -5 2
Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-countingDisplacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-counting
ChEMBL 522 5 1 4 4.4 NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)c1ccc(CN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.ejmech.2014.03.005
162670959 183860 None 0 Human Binding pKi = 5.9 5.9 -2 2
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 409 7 1 4 4.5 COc1ccccc1N1CCN(CCCC(=O)Nc2ccc(C(C)(C)C)cc2)CC1 10.1016/j.ejmech.2020.112437
CHEMBL4791316 183860 None 0 Human Binding pKi = 5.9 5.9 -2 2
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 409 7 1 4 4.5 COc1ccccc1N1CCN(CCCC(=O)Nc2ccc(C(C)(C)C)cc2)CC1 10.1016/j.ejmech.2020.112437
CHEMBL4803791 183860 None 0 Human Binding pKi = 5.9 5.9 -2 2
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 409 7 1 4 4.5 COc1ccccc1N1CCN(CCCC(=O)Nc2ccc(C(C)(C)C)cc2)CC1 10.1016/j.ejmech.2020.112437
90654694 110136 None 0 Human Binding pKi = 5.9 5.9 -27 2
Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-countingDisplacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-counting
ChEMBL 402 9 1 5 1.9 COc1ccccc1N1CCN(CCCCCC(=O)N2CCC[C@H]2C(N)=O)CC1 10.1016/j.ejmech.2014.03.005
CHEMBL3235731 110136 None 0 Human Binding pKi = 5.9 5.9 -27 2
Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-countingDisplacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-counting
ChEMBL 402 9 1 5 1.9 COc1ccccc1N1CCN(CCCCCC(=O)N2CCC[C@H]2C(N)=O)CC1 10.1016/j.ejmech.2014.03.005
10947658 28710 None 0 Human Binding pKi = 7.9 7.9 -10 16
Binding affinities against 5-hydroxytryptamine 7 receptorBinding affinities against 5-hydroxytryptamine 7 receptor
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
CHEMBL137781 28710 None 0 Human Binding pKi = 7.9 7.9 -10 16
Binding affinities against 5-hydroxytryptamine 7 receptorBinding affinities against 5-hydroxytryptamine 7 receptor
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
46214153 110758 None 0 Rat Binding pKi = 7.9 7.9 3 5
Binding affinity to rat 5HT7 receptorBinding affinity to rat 5HT7 receptor
ChEMBL 367 5 1 3 4.0 Clc1cccc(COc2ccc(Br)cc2OC2CNC2)c1 10.1021/ml500082j
CHEMBL3260334 110758 None 0 Rat Binding pKi = 7.9 7.9 3 5
Binding affinity to rat 5HT7 receptorBinding affinity to rat 5HT7 receptor
ChEMBL 367 5 1 3 4.0 Clc1cccc(COc2ccc(Br)cc2OC2CNC2)c1 10.1021/ml500082j
44374299 119601 None 0 Human Binding pKi = 7.9 7.9 17 3
Binding affinity towards human 5-hydroxytryptamine 7 receptor by the displacement of [3H]-5-HT radioligand from the cloned receptor expressed in CHO cellsBinding affinity towards human 5-hydroxytryptamine 7 receptor by the displacement of [3H]-5-HT radioligand from the cloned receptor expressed in CHO cells
ChEMBL 264 5 0 4 3.5 CN(C)CCSc1nc(-c2ccccc2)cs1 10.1016/j.bmcl.2003.11.050
CHEMBL345803 119601 None 0 Human Binding pKi = 7.9 7.9 17 3
Binding affinity towards human 5-hydroxytryptamine 7 receptor by the displacement of [3H]-5-HT radioligand from the cloned receptor expressed in CHO cellsBinding affinity towards human 5-hydroxytryptamine 7 receptor by the displacement of [3H]-5-HT radioligand from the cloned receptor expressed in CHO cells
ChEMBL 264 5 0 4 3.5 CN(C)CCSc1nc(-c2ccccc2)cs1 10.1016/j.bmcl.2003.11.050
11603514 71514 None 0 Rat Binding pKi = 7.9 7.9 1 4
Displacement of [3H]-5-CT from 5HT7 receptor in Sprague-Dawley albinus rat hyphalamic membranes after 120 minsDisplacement of [3H]-5-CT from 5HT7 receptor in Sprague-Dawley albinus rat hyphalamic membranes after 120 mins
ChEMBL 390 11 1 5 4.0 O=C1CSC(=O)N1CCCCCCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1926760 71514 None 0 Rat Binding pKi = 7.9 7.9 1 4
Displacement of [3H]-5-CT from 5HT7 receptor in Sprague-Dawley albinus rat hyphalamic membranes after 120 minsDisplacement of [3H]-5-CT from 5HT7 receptor in Sprague-Dawley albinus rat hyphalamic membranes after 120 mins
ChEMBL 390 11 1 5 4.0 O=C1CSC(=O)N1CCCCCCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1962492 71514 None 0 Rat Binding pKi = 7.9 7.9 1 4
Displacement of [3H]-5-CT from 5HT7 receptor in Sprague-Dawley albinus rat hyphalamic membranes after 120 minsDisplacement of [3H]-5-CT from 5HT7 receptor in Sprague-Dawley albinus rat hyphalamic membranes after 120 mins
ChEMBL 390 11 1 5 4.0 O=C1CSC(=O)N1CCCCCCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
127026450 137844 None 0 Human Binding pKi = 7.9 7.9 10 2
Displacement of [3H]-5-CT from human 5-HT7B receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5-HT7B receptor expressed in HEK293 cells after 1 hr
ChEMBL 480 8 1 4 4.8 O=S(=O)(NC1CC2CCC(C1)N2CCOc1cccc(-c2ccccc2)c1)c1cccc(F)c1 10.1016/j.ejmech.2015.11.040
CHEMBL3759281 137844 None 0 Human Binding pKi = 7.9 7.9 10 2
Displacement of [3H]-5-CT from human 5-HT7B receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5-HT7B receptor expressed in HEK293 cells after 1 hr
ChEMBL 480 8 1 4 4.8 O=S(=O)(NC1CC2CCC(C1)N2CCOc1cccc(-c2ccccc2)c1)c1cccc(F)c1 10.1016/j.ejmech.2015.11.040
145985233 165618 None 0 Human Binding pKi = 7.9 7.9 -7 5
Displacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 508 6 0 6 4.9 O=S(=O)(c1cccc2ncccc12)N1CCC[C@H]1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4241050 165618 None 0 Human Binding pKi = 7.9 7.9 -7 5
Displacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 508 6 0 6 4.9 O=S(=O)(c1cccc2ncccc12)N1CCC[C@H]1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1016/j.ejmech.2018.01.002
145984737 165674 None 0 Human Binding pKi = 7.9 7.9 -23 5
Displacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 0 7 4.2 O=S(=O)(c1cccc2cnccc12)N1CCC[C@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4242392 165674 None 0 Human Binding pKi = 7.9 7.9 -23 5
Displacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 0 7 4.2 O=S(=O)(c1cccc2cnccc12)N1CCC[C@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
145985527 165804 None 0 Human Binding pKi = 7.9 7.9 1 5
Displacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 520 6 1 4 5.7 O=S(=O)(c1cccc2ncccc12)N1CCC[C@@H]1CCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4245622 165804 None 0 Human Binding pKi = 7.9 7.9 1 5
Displacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 520 6 1 4 5.7 O=S(=O)(c1cccc2ncccc12)N1CCC[C@@H]1CCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1 10.1016/j.ejmech.2018.01.002
145985823 166019 None 0 Human Binding pKi = 7.9 7.9 -6 5
Displacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 508 6 0 6 4.9 O=S(=O)(c1cccc2ncccc12)N1CCC[C@@H]1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4250475 166019 None 0 Human Binding pKi = 7.9 7.9 -6 5
Displacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 508 6 0 6 4.9 O=S(=O)(c1cccc2ncccc12)N1CCC[C@@H]1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1016/j.ejmech.2018.01.002
134153716 152573 None 0 Human Binding pKi = 7.9 7.9 9 4
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 510 11 1 5 5.8 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)N[C@H](C)c3ccc(C#N)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3971125 152573 None 0 Human Binding pKi = 7.9 7.9 9 4
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 510 11 1 5 5.8 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)N[C@H](C)c3ccc(C#N)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
71453252 81392 None 0 Human Binding pKi = 7.9 7.9 15 2
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr
ChEMBL 476 8 1 5 4.9 O=S(=O)(NC1CCN(CCOc2ccccc2-c2ccccc2)CC1)c1ccc(Cl)s1 10.1016/j.ejmech.2012.07.043
CHEMBL2159309 81392 None 0 Human Binding pKi = 7.9 7.9 15 2
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr
ChEMBL 476 8 1 5 4.9 O=S(=O)(NC1CCN(CCOc2ccccc2-c2ccccc2)CC1)c1ccc(Cl)s1 10.1016/j.ejmech.2012.07.043
71453282 81479 None 0 Human Binding pKi = 7.9 7.9 -1 4
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr
ChEMBL 462 8 1 5 4.5 O=S(=O)(N[C@H]1CCN(CCOc2ccccc2-c2ccccc2)C1)c1ccc(Cl)s1 10.1016/j.ejmech.2012.07.043
CHEMBL2159491 81479 None 0 Human Binding pKi = 7.9 7.9 -1 4
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr
ChEMBL 462 8 1 5 4.5 O=S(=O)(N[C@H]1CCN(CCOc2ccccc2-c2ccccc2)C1)c1ccc(Cl)s1 10.1016/j.ejmech.2012.07.043
71574210 86317 None 0 Human Binding pKi = 7.9 7.9 1 5
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 after 1 hr
ChEMBL 478 7 1 5 4.0 O=S(=O)(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2cccnc2c1 10.1016/j.ejmech.2012.11.042
CHEMBL2312934 86317 None 0 Human Binding pKi = 7.9 7.9 1 5
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 after 1 hr
ChEMBL 478 7 1 5 4.0 O=S(=O)(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2cccnc2c1 10.1016/j.ejmech.2012.11.042
118731351 118252 None 0 Human Binding pKi = 7.9 7.9 3 4
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells after 1 hr
ChEMBL 496 8 1 4 4.1 NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCCCN1CCN(c2ccccc2-c2ccccc2)CC1 10.1016/j.ejmech.2014.12.041
CHEMBL3409035 118252 None 0 Human Binding pKi = 7.9 7.9 3 4
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells after 1 hr
ChEMBL 496 8 1 4 4.1 NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCCCN1CCN(c2ccccc2-c2ccccc2)CC1 10.1016/j.ejmech.2014.12.041
118731365 118265 None 0 Human Binding pKi = 7.9 7.9 3 2
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells after 1 hr
ChEMBL 592 10 0 4 6.4 O=C([C@@H]1Cc2ccccc2CN1C(=O)CCCCCCN1CCN(c2ccccc2-c2ccccc2)CC1)N1CCCCC1 10.1016/j.ejmech.2014.12.041
CHEMBL3409048 118265 None 0 Human Binding pKi = 7.9 7.9 3 2
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells after 1 hr
ChEMBL 592 10 0 4 6.4 O=C([C@@H]1Cc2ccccc2CN1C(=O)CCCCCCN1CCN(c2ccccc2-c2ccccc2)CC1)N1CCCCC1 10.1016/j.ejmech.2014.12.041
145947977 167817 None 0 Human Binding pKi = 7.9 7.9 48 3
Displacement of [3H]-5-CT from human 5HT7BR expressed in HEK293 cell membranes after 1 hr by Microbeta scintillation counting methodDisplacement of [3H]-5-CT from human 5HT7BR expressed in HEK293 cell membranes after 1 hr by Microbeta scintillation counting method
ChEMBL 433 6 2 6 1.5 CC1(c2ccccc2)NC(=O)N(CC(O)CN2CCN(c3ccccc3C#N)CC2)C1=O 10.1016/j.ejmech.2018.01.093
CHEMBL4162279 167817 None 0 Human Binding pKi = 7.9 7.9 48 3
Displacement of [3H]-5-CT from human 5HT7BR expressed in HEK293 cell membranes after 1 hr by Microbeta scintillation counting methodDisplacement of [3H]-5-CT from human 5HT7BR expressed in HEK293 cell membranes after 1 hr by Microbeta scintillation counting method
ChEMBL 433 6 2 6 1.5 CC1(c2ccccc2)NC(=O)N(CC(O)CN2CCN(c3ccccc3C#N)CC2)C1=O 10.1016/j.ejmech.2018.01.093
CHEMBL4302540 167817 None 0 Human Binding pKi = 7.9 7.9 48 3
Displacement of [3H]-5-CT from human 5HT7BR expressed in HEK293 cell membranes after 1 hr by Microbeta scintillation counting methodDisplacement of [3H]-5-CT from human 5HT7BR expressed in HEK293 cell membranes after 1 hr by Microbeta scintillation counting method
ChEMBL 433 6 2 6 1.5 CC1(c2ccccc2)NC(=O)N(CC(O)CN2CCN(c3ccccc3C#N)CC2)C1=O 10.1016/j.ejmech.2018.01.093
23642275 482 None 26 Human Binding pKi = 7.9 7.9 3 8
Displacement of [3H]-5-carboxamidotryptamine from human 5-HT7A receptor expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting methodDisplacement of [3H]-5-carboxamidotryptamine from human 5-HT7A receptor expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting method
ChEMBL 283 2 0 3 3.1 CN([C@H]1CCc2c(C1)cccc2c1c(C)nn(c1C)C)C 10.1016/j.bmc.2019.115262
8433 482 None 26 Human Binding pKi = 7.9 7.9 3 8
Displacement of [3H]-5-carboxamidotryptamine from human 5-HT7A receptor expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting methodDisplacement of [3H]-5-carboxamidotryptamine from human 5-HT7A receptor expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting method
ChEMBL 283 2 0 3 3.1 CN([C@H]1CCc2c(C1)cccc2c1c(C)nn(c1C)C)C 10.1016/j.bmc.2019.115262
CHEMBL2164327 482 None 26 Human Binding pKi = 7.9 7.9 3 8
Displacement of [3H]-5-carboxamidotryptamine from human 5-HT7A receptor expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting methodDisplacement of [3H]-5-carboxamidotryptamine from human 5-HT7A receptor expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting method
ChEMBL 283 2 0 3 3.1 CN([C@H]1CCc2c(C1)cccc2c1c(C)nn(c1C)C)C 10.1016/j.bmc.2019.115262
71453252 81392 None 0 Human Binding pKi = 7.9 7.9 15 2
Displacement of [3H]-5-carboxyamidotryptamine from human serotonin 5-HT7B receptor expressed in HEK293 cells after 1 hr by microplate reader based assayDisplacement of [3H]-5-carboxyamidotryptamine from human serotonin 5-HT7B receptor expressed in HEK293 cells after 1 hr by microplate reader based assay
ChEMBL 476 8 1 5 4.9 O=S(=O)(NC1CCN(CCOc2ccccc2-c2ccccc2)CC1)c1ccc(Cl)s1 10.1039/C5MD00166H
CHEMBL2159309 81392 None 0 Human Binding pKi = 7.9 7.9 15 2
Displacement of [3H]-5-carboxyamidotryptamine from human serotonin 5-HT7B receptor expressed in HEK293 cells after 1 hr by microplate reader based assayDisplacement of [3H]-5-carboxyamidotryptamine from human serotonin 5-HT7B receptor expressed in HEK293 cells after 1 hr by microplate reader based assay
ChEMBL 476 8 1 5 4.9 O=S(=O)(NC1CCN(CCOc2ccccc2-c2ccccc2)CC1)c1ccc(Cl)s1 10.1039/C5MD00166H
142601335 186527 None 0 Human Binding pKi = 7.9 7.9 44 7
Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by liquid scintillation countingDisplacement of [3H]-LSD from 5HT7 receptor (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by liquid scintillation counting
ChEMBL 256 2 2 3 2.2 Cc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4876193 186527 None 0 Human Binding pKi = 7.9 7.9 44 7
Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by liquid scintillation countingDisplacement of [3H]-LSD from 5HT7 receptor (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by liquid scintillation counting
ChEMBL 256 2 2 3 2.2 Cc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
66803497 158603 None 0 Human Binding pKi = 7.9 7.9 -2 4
Displacement of [3H]-LSD from human 5-HT7 receptor expressed in CHO-K1 cell membranes after 120 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT7 receptor expressed in CHO-K1 cell membranes after 120 mins by scintillation counting
ChEMBL 463 7 2 3 4.9 O=S(=O)(NCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(Cl)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4091193 158603 None 0 Human Binding pKi = 7.9 7.9 -2 4
Displacement of [3H]-LSD from human 5-HT7 receptor expressed in CHO-K1 cell membranes after 120 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT7 receptor expressed in CHO-K1 cell membranes after 120 mins by scintillation counting
ChEMBL 463 7 2 3 4.9 O=S(=O)(NCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(Cl)c1 10.1021/acs.jmedchem.7b00839
145964944 164176 None 0 Human Binding pKi = 7.9 7.9 -14 2
Displacement of [3H]-LSD from recombinant human 5-HT7 receptor expressed in CHO cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5-HT7 receptor expressed in CHO cell membranes measured after 60 mins by scintillation counting method
ChEMBL 391 4 0 4 5.0 Clc1ccc(CCN2CCN(c3nsc4ccccc34)CC2)cc1Cl 10.1016/j.bmcl.2017.11.007
CHEMBL4209430 164176 None 0 Human Binding pKi = 7.9 7.9 -14 2
Displacement of [3H]-LSD from recombinant human 5-HT7 receptor expressed in CHO cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5-HT7 receptor expressed in CHO cell membranes measured after 60 mins by scintillation counting method
ChEMBL 391 4 0 4 5.0 Clc1ccc(CCN2CCN(c3nsc4ccccc34)CC2)cc1Cl 10.1016/j.bmcl.2017.11.007
10862787 103092 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]5-CT from human 5HT7 receptor expressed in in COS7 cells incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]5-CT from human 5HT7 receptor expressed in in COS7 cells incubated for 30 mins by liquid scintillation counting method
ChEMBL 423 6 1 3 4.9 O=C1Nc2cccc3c2C1(CCCCN1CCN(c2ccccc2Cl)CC1)CCC3 10.1016/j.bmc.2019.06.028
CHEMBL307101 103092 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]5-CT from human 5HT7 receptor expressed in in COS7 cells incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]5-CT from human 5HT7 receptor expressed in in COS7 cells incubated for 30 mins by liquid scintillation counting method
ChEMBL 423 6 1 3 4.9 O=C1Nc2cccc3c2C1(CCCCN1CCN(c2ccccc2Cl)CC1)CCC3 10.1016/j.bmc.2019.06.028
90656696 111061 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in HEK293 cells after 30 mins by microbeta counting analysisDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in HEK293 cells after 30 mins by microbeta counting analysis
ChEMBL 367 9 1 4 4.2 CN(CCCCCCN1CCN(c2ccccc2)CC1)c1cccc(O)c1 10.1016/j.ejmech.2014.04.034
CHEMBL3262430 111061 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in HEK293 cells after 30 mins by microbeta counting analysisDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in HEK293 cells after 30 mins by microbeta counting analysis
ChEMBL 367 9 1 4 4.2 CN(CCCCCCN1CCN(c2ccccc2)CC1)c1cccc(O)c1 10.1016/j.ejmech.2014.04.034
44374299 119601 None 0 Human Binding pKi = 7.9 7.9 17 3
Displacement of [3H]5CT from human cloned 5HT7B receptor expressed in HEK293 cellsDisplacement of [3H]5CT from human cloned 5HT7B receptor expressed in HEK293 cells
ChEMBL 264 5 0 4 3.5 CN(C)CCSc1nc(-c2ccccc2)cs1 10.1016/j.bmc.2010.01.035
CHEMBL345803 119601 None 0 Human Binding pKi = 7.9 7.9 17 3
Displacement of [3H]5CT from human cloned 5HT7B receptor expressed in HEK293 cellsDisplacement of [3H]5CT from human cloned 5HT7B receptor expressed in HEK293 cells
ChEMBL 264 5 0 4 3.5 CN(C)CCSc1nc(-c2ccccc2)cs1 10.1016/j.bmc.2010.01.035
127051844 140934 None 0 Human Binding pKi = 7.9 7.9 1 9
Displacement of [3H]LSD from human 5-HT7 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT7 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 322 6 1 3 2.8 NC(=O)c1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819427 140934 None 0 Human Binding pKi = 7.9 7.9 1 9
Displacement of [3H]LSD from human 5-HT7 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT7 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 322 6 1 3 2.8 NC(=O)c1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
145988193 167175 None 0 Human Binding pKi = 7.9 7.9 5 2
Displacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cell membranes after 120 mins by TopCount scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cell membranes after 120 mins by TopCount scintillation counting method
ChEMBL 449 6 1 2 6.0 Fc1cccc(-c2cc(F)ccc2N2CCN(CCCc3c[nH]c4ccc(F)cc34)CC2)c1 10.1016/j.ejmech.2017.12.063
CHEMBL4289605 167175 None 0 Human Binding pKi = 7.9 7.9 5 2
Displacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cell membranes after 120 mins by TopCount scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cell membranes after 120 mins by TopCount scintillation counting method
ChEMBL 449 6 1 2 6.0 Fc1cccc(-c2cc(F)ccc2N2CCN(CCCc3c[nH]c4ccc(F)cc34)CC2)c1 10.1016/j.ejmech.2017.12.063
90656672 111055 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in HEK293 cells after 30 mins by microbeta counting analysisDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in HEK293 cells after 30 mins by microbeta counting analysis
ChEMBL 451 8 1 5 3.8 O=S(=O)(c1ccccc1)N(CCCN1CCN(c2ccccc2)CC1)c1cccc(O)c1 10.1016/j.ejmech.2014.04.034
CHEMBL3262425 111055 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in HEK293 cells after 30 mins by microbeta counting analysisDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in HEK293 cells after 30 mins by microbeta counting analysis
ChEMBL 451 8 1 5 3.8 O=S(=O)(c1ccccc1)N(CCCN1CCN(c2ccccc2)CC1)c1cccc(O)c1 10.1016/j.ejmech.2014.04.034
155565215 175714 None 0 Human Binding pKi = 7.9 7.9 10 2
Displacement of [3H]-5-HT from human 5HT7 receptor expressed in CHO-K1 cells incubated for 40 mins in presence of serotonin by liquid scintillation counterDisplacement of [3H]-5-HT from human 5HT7 receptor expressed in CHO-K1 cells incubated for 40 mins in presence of serotonin by liquid scintillation counter
ChEMBL 433 6 1 7 3.5 Nn1c(CCCCN2CCN(c3ccccc3)CC2)nc2c(sc3ccccc32)c1=O 10.1016/j.ejmech.2019.111690
CHEMBL4580230 175714 None 0 Human Binding pKi = 7.9 7.9 10 2
Displacement of [3H]-5-HT from human 5HT7 receptor expressed in CHO-K1 cells incubated for 40 mins in presence of serotonin by liquid scintillation counterDisplacement of [3H]-5-HT from human 5HT7 receptor expressed in CHO-K1 cells incubated for 40 mins in presence of serotonin by liquid scintillation counter
ChEMBL 433 6 1 7 3.5 Nn1c(CCCCN2CCN(c3ccccc3)CC2)nc2c(sc3ccccc32)c1=O 10.1016/j.ejmech.2019.111690
10862787 103092 None 0 Human Binding pKi = 7.9 7.9 - 1
Binding affinity to human recombinant 5-hydroxytryptamine 7 receptor in mammalian cells using [3H]5-CT as radioligandBinding affinity to human recombinant 5-hydroxytryptamine 7 receptor in mammalian cells using [3H]5-CT as radioligand
ChEMBL 423 6 1 3 4.9 O=C1Nc2cccc3c2C1(CCCCN1CCN(c2ccccc2Cl)CC1)CCC3 10.1021/jm0104264
CHEMBL307101 103092 None 0 Human Binding pKi = 7.9 7.9 - 1
Binding affinity to human recombinant 5-hydroxytryptamine 7 receptor in mammalian cells using [3H]5-CT as radioligandBinding affinity to human recombinant 5-hydroxytryptamine 7 receptor in mammalian cells using [3H]5-CT as radioligand
ChEMBL 423 6 1 3 4.9 O=C1Nc2cccc3c2C1(CCCCN1CCN(c2ccccc2Cl)CC1)CCC3 10.1021/jm0104264
11826723 206701 None 0 Human Binding pKi = 7.9 7.9 - 1
Binding affinity to human recombinant 5-hydroxytryptamine 7 receptor in mammalian cells using [3H]5-CT as radioligandBinding affinity to human recombinant 5-hydroxytryptamine 7 receptor in mammalian cells using [3H]5-CT as radioligand
ChEMBL 464 6 1 2 5.9 O=C1Nc2ccc(Br)c3c2C1(CCCCN1CC=C(c2ccccc2)CC1)CCC3 10.1021/jm0104264
CHEMBL71057 206701 None 0 Human Binding pKi = 7.9 7.9 - 1
Binding affinity to human recombinant 5-hydroxytryptamine 7 receptor in mammalian cells using [3H]5-CT as radioligandBinding affinity to human recombinant 5-hydroxytryptamine 7 receptor in mammalian cells using [3H]5-CT as radioligand
ChEMBL 464 6 1 2 5.9 O=C1Nc2ccc(Br)c3c2C1(CCCCN1CC=C(c2ccccc2)CC1)CCC3 10.1021/jm0104264
142601335 186527 None 0 Human Binding pKi = 7.9 7.9 44 7
Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by liquid scintillation countingDisplacement of [3H]-LSD from 5HT7 receptor (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by liquid scintillation counting
ChEMBL 256 2 2 3 2.2 Cc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4876193 186527 None 0 Human Binding pKi = 7.9 7.9 44 7
Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by liquid scintillation countingDisplacement of [3H]-LSD from 5HT7 receptor (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by liquid scintillation counting
ChEMBL 256 2 2 3 2.2 Cc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
127051844 140934 None 0 Human Binding pKi = 7.9 7.9 1 9
Displacement of [3H]LSD from human 5-HT7 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT7 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 322 6 1 3 2.8 NC(=O)c1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819427 140934 None 0 Human Binding pKi = 7.9 7.9 1 9
Displacement of [3H]LSD from human 5-HT7 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT7 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 322 6 1 3 2.8 NC(=O)c1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
72734860 104012 None 0 Human Binding pKi = 7.9 7.9 -6 5
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cells by liquid scintillation counting analysisDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cells by liquid scintillation counting analysis
ChEMBL 251 1 2 1 1.7 NC(N)=NC(=O)c1ccc2c(c1)Cc1ccccc1-2 10.1016/j.bmc.2013.10.010
CHEMBL3092753 104012 None 0 Human Binding pKi = 7.9 7.9 -6 5
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cells by liquid scintillation counting analysisDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cells by liquid scintillation counting analysis
ChEMBL 251 1 2 1 1.7 NC(N)=NC(=O)c1ccc2c(c1)Cc1ccccc1-2 10.1016/j.bmc.2013.10.010
44456395 95724 None 0 Human Binding pKi = 7.9 7.9 1 5
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in HEK293-EBNA cells
ChEMBL 225 1 2 4 2.0 COc1c(Cl)ccc2c1C(C)NC(N)=N2 10.1016/j.bmcl.2007.10.080
CHEMBL258073 95724 None 0 Human Binding pKi = 7.9 7.9 1 5
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in HEK293-EBNA cells
ChEMBL 225 1 2 4 2.0 COc1c(Cl)ccc2c1C(C)NC(N)=N2 10.1016/j.bmcl.2007.10.080
11302161 67299 None 0 Rat Binding pKi = 7.9 7.9 -8 2
Inhibition of [3H]-5-HT binding to rat 5-hydroxytryptamine 7 receptorInhibition of [3H]-5-HT binding to rat 5-hydroxytryptamine 7 receptor
ChEMBL 337 7 0 2 5.3 CCCN(CCC)[C@H]1CCc2c(cccc2-c2ccc(OC)cc2)C1 10.1021/jm0498102
CHEMBL188176 67299 None 0 Rat Binding pKi = 7.9 7.9 -8 2
Inhibition of [3H]-5-HT binding to rat 5-hydroxytryptamine 7 receptorInhibition of [3H]-5-HT binding to rat 5-hydroxytryptamine 7 receptor
ChEMBL 337 7 0 2 5.3 CCCN(CCC)[C@H]1CCc2c(cccc2-c2ccc(OC)cc2)C1 10.1021/jm0498102
44319240 106966 None 0 Human Binding pKi = 7.9 7.9 - 1
Ability to displace the radioligand [3H]5-carboxyamidotryptamine ([3H]5-CT) from human 5-hydroxytryptamine 7 receptor expressed in COS-7 cellsAbility to displace the radioligand [3H]5-carboxyamidotryptamine ([3H]5-CT) from human 5-hydroxytryptamine 7 receptor expressed in COS-7 cells
ChEMBL 374 6 1 2 4.8 O=C1Nc2cccc3c2C1(CCCCCN1CCc2ccccc2C1)CCC3 10.1016/s0960-894x(02)00485-7
CHEMBL314672 106966 None 0 Human Binding pKi = 7.9 7.9 - 1
Ability to displace the radioligand [3H]5-carboxyamidotryptamine ([3H]5-CT) from human 5-hydroxytryptamine 7 receptor expressed in COS-7 cellsAbility to displace the radioligand [3H]5-carboxyamidotryptamine ([3H]5-CT) from human 5-hydroxytryptamine 7 receptor expressed in COS-7 cells
ChEMBL 374 6 1 2 4.8 O=C1Nc2cccc3c2C1(CCCCCN1CCc2ccccc2C1)CCC3 10.1016/s0960-894x(02)00485-7
135398737 958 None 57 Rat Binding pKi = 7.9 7.9 -7 91
Binding affinity towards 5-hydroxytryptamine 7 receptorBinding affinity towards 5-hydroxytryptamine 7 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00166-9
135398737.0 958 None 57 Rat Binding pKi = 7.9 7.9 -7 91
Binding affinity towards 5-hydroxytryptamine 7 receptorBinding affinity towards 5-hydroxytryptamine 7 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00166-9
38 958 None 57 Rat Binding pKi = 7.9 7.9 -7 91
Binding affinity towards 5-hydroxytryptamine 7 receptorBinding affinity towards 5-hydroxytryptamine 7 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00166-9
722 958 None 57 Rat Binding pKi = 7.9 7.9 -7 91
Binding affinity towards 5-hydroxytryptamine 7 receptorBinding affinity towards 5-hydroxytryptamine 7 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00166-9
CHEMBL42 958 None 57 Rat Binding pKi = 7.9 7.9 -7 91
Binding affinity towards 5-hydroxytryptamine 7 receptorBinding affinity towards 5-hydroxytryptamine 7 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00166-9
DB00363 958 None 57 Rat Binding pKi = 7.9 7.9 -7 91
Binding affinity towards 5-hydroxytryptamine 7 receptorBinding affinity towards 5-hydroxytryptamine 7 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00166-9
6540428 184970 None 1 Rat Binding pKi = 7.9 7.9 -7 3
Binding affinity towards 5-hydroxytryptamine 7 receptorBinding affinity towards 5-hydroxytryptamine 7 receptor
ChEMBL 353 4 2 4 1.9 CCC(CO)NC(=O)[C@@H]1C=C2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 10.1016/s0960-894x(00)00166-9
6540428.0 184970 None 1 Rat Binding pKi = 7.9 7.9 -7 3
Binding affinity towards 5-hydroxytryptamine 7 receptorBinding affinity towards 5-hydroxytryptamine 7 receptor
ChEMBL 353 4 2 4 1.9 CCC(CO)NC(=O)[C@@H]1C=C2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 10.1016/s0960-894x(00)00166-9
CHEMBL3989558 184970 None 1 Rat Binding pKi = 7.9 7.9 -7 3
Binding affinity towards 5-hydroxytryptamine 7 receptorBinding affinity towards 5-hydroxytryptamine 7 receptor
ChEMBL 353 4 2 4 1.9 CCC(CO)NC(=O)[C@@H]1C=C2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 10.1016/s0960-894x(00)00166-9
CHEMBL485253 184970 None 1 Rat Binding pKi = 7.9 7.9 -7 3
Binding affinity towards 5-hydroxytryptamine 7 receptorBinding affinity towards 5-hydroxytryptamine 7 receptor
ChEMBL 353 4 2 4 1.9 CCC(CO)NC(=O)[C@@H]1C=C2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 10.1016/s0960-894x(00)00166-9
DB00247 184970 None 1 Rat Binding pKi = 7.9 7.9 -7 3
Binding affinity towards 5-hydroxytryptamine 7 receptorBinding affinity towards 5-hydroxytryptamine 7 receptor
ChEMBL 353 4 2 4 1.9 CCC(CO)NC(=O)[C@@H]1C=C2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 10.1016/s0960-894x(00)00166-9
10571274 99513 None 0 Rat Binding pKi = 7.9 7.9 42 3
Binding affinity towards cloned rat 5-hydroxytryptamine 7 receptor was determined using [3H]5-HT as radioligandBinding affinity towards cloned rat 5-hydroxytryptamine 7 receptor was determined using [3H]5-HT as radioligand
ChEMBL 371 3 0 3 5.1 COc1cccc(OC)c1-c1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm030841r
CHEMBL283065 99513 None 0 Rat Binding pKi = 7.9 7.9 42 3
Binding affinity towards cloned rat 5-hydroxytryptamine 7 receptor was determined using [3H]5-HT as radioligandBinding affinity towards cloned rat 5-hydroxytryptamine 7 receptor was determined using [3H]5-HT as radioligand
ChEMBL 371 3 0 3 5.1 COc1cccc(OC)c1-c1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm030841r
135398737 958 None 57 Human Binding pKi = 7.9 7.9 -13 91
Non-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptorNon-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030841r
135398737.0 958 None 57 Human Binding pKi = 7.9 7.9 -13 91
Non-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptorNon-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030841r
38 958 None 57 Human Binding pKi = 7.9 7.9 -13 91
Non-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptorNon-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030841r
722 958 None 57 Human Binding pKi = 7.9 7.9 -13 91
Non-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptorNon-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030841r
CHEMBL42 958 None 57 Human Binding pKi = 7.9 7.9 -13 91
Non-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptorNon-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030841r
DB00363 958 None 57 Human Binding pKi = 7.9 7.9 -13 91
Non-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptorNon-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030841r
6540428 184970 None 1 Human Binding pKi = 7.9 7.9 -7 3
Non-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptorNon-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptor
ChEMBL 353 4 2 4 1.9 CCC(CO)NC(=O)[C@@H]1C=C2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 10.1021/jm030841r
6540428.0 184970 None 1 Human Binding pKi = 7.9 7.9 -7 3
Non-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptorNon-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptor
ChEMBL 353 4 2 4 1.9 CCC(CO)NC(=O)[C@@H]1C=C2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 10.1021/jm030841r
CHEMBL3989558 184970 None 1 Human Binding pKi = 7.9 7.9 -7 3
Non-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptorNon-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptor
ChEMBL 353 4 2 4 1.9 CCC(CO)NC(=O)[C@@H]1C=C2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 10.1021/jm030841r
CHEMBL485253 184970 None 1 Human Binding pKi = 7.9 7.9 -7 3
Non-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptorNon-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptor
ChEMBL 353 4 2 4 1.9 CCC(CO)NC(=O)[C@@H]1C=C2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 10.1021/jm030841r
DB00247 184970 None 1 Human Binding pKi = 7.9 7.9 -7 3
Non-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptorNon-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptor
ChEMBL 353 4 2 4 1.9 CCC(CO)NC(=O)[C@@H]1C=C2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 10.1021/jm030841r
11151958 66992 None 0 Rat Binding pKi = 7.9 7.9 -9 3
Inhibition of [3H]-5-HT binding to rat 5-hydroxytryptamine 7 receptorInhibition of [3H]-5-HT binding to rat 5-hydroxytryptamine 7 receptor
ChEMBL 339 7 0 3 4.8 CCCN(CCC)[C@H]1COc2c(cccc2-c2ccc(OC)cc2)C1 10.1021/jm0498102
CHEMBL186758 66992 None 0 Rat Binding pKi = 7.9 7.9 -9 3
Inhibition of [3H]-5-HT binding to rat 5-hydroxytryptamine 7 receptorInhibition of [3H]-5-HT binding to rat 5-hydroxytryptamine 7 receptor
ChEMBL 339 7 0 3 4.8 CCCN(CCC)[C@H]1COc2c(cccc2-c2ccc(OC)cc2)C1 10.1021/jm0498102
71062123 93170 None 0 Human Binding pKi = 7.9 7.9 6 2
Displacement of [3H]5-CT from human 5HT7 receptor transfected in HEK293 cells after 60 minsDisplacement of [3H]5-CT from human 5HT7 receptor transfected in HEK293 cells after 60 mins
ChEMBL 472 11 1 5 4.8 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)NCc3cccnc3)CC2)cc1 10.1016/j.bmc.2014.01.016
CHEMBL2442995 93170 None 0 Human Binding pKi = 7.9 7.9 6 2
Displacement of [3H]5-CT from human 5HT7 receptor transfected in HEK293 cells after 60 minsDisplacement of [3H]5-CT from human 5HT7 receptor transfected in HEK293 cells after 60 mins
ChEMBL 472 11 1 5 4.8 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)NCc3cccnc3)CC2)cc1 10.1016/j.bmc.2014.01.016
71062123 93170 None 0 Human Binding pKi = 7.9 7.9 6 2
Displacement of [3H]5-CT from human 5HT7A receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]5-CT from human 5HT7A receptor expressed in HEK293 cells after 60 mins
ChEMBL 472 11 1 5 4.8 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)NCc3cccnc3)CC2)cc1 10.1016/j.bmcl.2013.09.025
CHEMBL2442995 93170 None 0 Human Binding pKi = 7.9 7.9 6 2
Displacement of [3H]5-CT from human 5HT7A receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]5-CT from human 5HT7A receptor expressed in HEK293 cells after 60 mins
ChEMBL 472 11 1 5 4.8 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)NCc3cccnc3)CC2)cc1 10.1016/j.bmcl.2013.09.025
76284453 105062 None 0 Human Binding pKi = 7.9 7.9 67 2
Displacement of [3H]5-CT from human 5HT7 receptor transfected in HEK293 cells after 60 minsDisplacement of [3H]5-CT from human 5HT7 receptor transfected in HEK293 cells after 60 mins
ChEMBL 476 10 1 5 4.0 Cc1ccccc1-c1ccccc1N1CCN(CCOCCC(=O)NCc2ccc(F)nc2)CC1 10.1016/j.bmc.2014.01.016
CHEMBL3113595 105062 None 0 Human Binding pKi = 7.9 7.9 67 2
Displacement of [3H]5-CT from human 5HT7 receptor transfected in HEK293 cells after 60 minsDisplacement of [3H]5-CT from human 5HT7 receptor transfected in HEK293 cells after 60 mins
ChEMBL 476 10 1 5 4.0 Cc1ccccc1-c1ccccc1N1CCN(CCOCCC(=O)NCc2ccc(F)nc2)CC1 10.1016/j.bmc.2014.01.016
90656713 111032 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in HEK293 cells after 30 mins by microbeta counting analysisDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in HEK293 cells after 30 mins by microbeta counting analysis
ChEMBL 385 4 2 3 4.7 Cc1[nH]c2ccc(O)cc2c1CCN1CCN(c2cccc3ccccc23)CC1 10.1016/j.ejmech.2014.04.034
CHEMBL3262394 111032 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in HEK293 cells after 30 mins by microbeta counting analysisDisplacement of [3H]5-HT from human 5-HT7 receptor expressed in HEK293 cells after 30 mins by microbeta counting analysis
ChEMBL 385 4 2 3 4.7 Cc1[nH]c2ccc(O)cc2c1CCN1CCN(c2cccc3ccccc23)CC1 10.1016/j.ejmech.2014.04.034
162662399 182035 None 0 Human Binding pKi = 7.9 7.9 -12 4
Displacement of [3H]-LSD from recombinant human 5HT7 receptor expressed in CHOK1 cell membranes measured after 120 mins by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT7 receptor expressed in CHOK1 cell membranes measured after 120 mins by microbeta counting method
ChEMBL 399 7 1 5 3.1 Cc1cccc(S(=O)(=O)N[C@H]2CCN(CCCc3noc4ccccc34)C2)c1 10.1016/j.ejmech.2020.112149
CHEMBL4779739 182035 None 0 Human Binding pKi = 7.9 7.9 -12 4
Displacement of [3H]-LSD from recombinant human 5HT7 receptor expressed in CHOK1 cell membranes measured after 120 mins by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT7 receptor expressed in CHOK1 cell membranes measured after 120 mins by microbeta counting method
ChEMBL 399 7 1 5 3.1 Cc1cccc(S(=O)(=O)N[C@H]2CCN(CCCc3noc4ccccc34)C2)c1 10.1016/j.ejmech.2020.112149
11948707 166262 None 0 Human Binding pKi = 7.9 7.9 -158 13
Binding affinity to 5-HT7 receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT7 receptor (unknown origin) assessed as inhibition constant
ChEMBL 373 7 0 8 0.6 COc1cccc(N2CCN(CCCCn3ncc(=O)n(C)c3=O)CC2)c1 10.1021/acs.jmedchem.2c00633
CHEMBL426317 166262 None 0 Human Binding pKi = 7.9 7.9 -158 13
Binding affinity to 5-HT7 receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT7 receptor (unknown origin) assessed as inhibition constant
ChEMBL 373 7 0 8 0.6 COc1cccc(N2CCN(CCCCn3ncc(=O)n(C)c3=O)CC2)c1 10.1021/acs.jmedchem.2c00633
21830793 91869 None 12 Human Binding pKi = 7.9 7.9 -85 44
Binding affinity to 5HT7 receptor (unknown origin)Binding affinity to 5HT7 receptor (unknown origin)
ChEMBL 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 10.1016/j.bmc.2013.05.050
CHEMBL2413154 91869 None 12 Human Binding pKi = 7.9 7.9 -85 44
Binding affinity to 5HT7 receptor (unknown origin)Binding affinity to 5HT7 receptor (unknown origin)
ChEMBL 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 10.1016/j.bmc.2013.05.050
118728524 117783 None 0 Human Binding pKi = 7.9 7.9 3 2
Displacement of [3H]-8-OH-DPAT from human 5-HT7 receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-8-OH-DPAT from human 5-HT7 receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysis
ChEMBL 410 7 0 5 4.0 O=c1c2ccccc2ncn1CCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2015.02.042
CHEMBL3401487 117783 None 0 Human Binding pKi = 7.9 7.9 3 2
Displacement of [3H]-8-OH-DPAT from human 5-HT7 receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-8-OH-DPAT from human 5-HT7 receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysis
ChEMBL 410 7 0 5 4.0 O=c1c2ccccc2ncn1CCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2015.02.042
145990586 166939 None 0 Human Binding pKi = 6.9 6.9 -9 11
Binding affinity to 5-HT7 receptor (unknown origin) assessed as inhibition of radioligand binding by radioligand competition binding assayBinding affinity to 5-HT7 receptor (unknown origin) assessed as inhibition of radioligand binding by radioligand competition binding assay
ChEMBL 297 2 2 4 2.6 COc1cc2c3c(c1OC)-c1ccccc1[C@@H](O)[C@@H]3NCC2 10.1039/C7MD00656J
CHEMBL4285281 166939 None 0 Human Binding pKi = 6.9 6.9 -9 11
Binding affinity to 5-HT7 receptor (unknown origin) assessed as inhibition of radioligand binding by radioligand competition binding assayBinding affinity to 5-HT7 receptor (unknown origin) assessed as inhibition of radioligand binding by radioligand competition binding assay
ChEMBL 297 2 2 4 2.6 COc1cc2c3c(c1OC)-c1ccccc1[C@@H](O)[C@@H]3NCC2 10.1039/C7MD00656J
66801425 157278 None 0 Human Binding pKi = 6.9 6.9 -39 4
Displacement of [3H]-LSD from human 5-HT7 receptor expressed in CHO-K1 cell membranes after 120 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT7 receptor expressed in CHO-K1 cell membranes after 120 mins by scintillation counting
ChEMBL 441 8 2 3 4.5 Cc1cccc(S(=O)(=O)NCCCCN2CC=C(c3c[nH]c4ccc(F)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4075673 157278 None 0 Human Binding pKi = 6.9 6.9 -39 4
Displacement of [3H]-LSD from human 5-HT7 receptor expressed in CHO-K1 cell membranes after 120 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT7 receptor expressed in CHO-K1 cell membranes after 120 mins by scintillation counting
ChEMBL 441 8 2 3 4.5 Cc1cccc(S(=O)(=O)NCCCCN2CC=C(c3c[nH]c4ccc(F)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
66801354 112146 None 0 Human Binding pKi = 6.9 6.9 -1 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 450 7 1 6 3.5 O=S(=O)(NCCCN1CCN(c2noc3ccccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
CHEMBL3289977 112146 None 0 Human Binding pKi = 6.9 6.9 -1 4
Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO-K1 cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 450 7 1 6 3.5 O=S(=O)(NCCCN1CCN(c2noc3ccccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
44437329 151689 None 0 Rat Binding pKi = 6.9 6.9 -8 2
Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells
ChEMBL 692 18 0 8