Biased Signaling Atlas

Ligand source activities (1 row/activity)

Potency
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Ligands					Receptor			Assay information							Chemical information
Sel. page	Common name	GPCRdb ID	#Vendors	Reference ligand	Fold selectivity (Potency)	# tested GPCRs (Potency)	Species	p-value (-log)	Type	Activity Relation	Activity Value	Assay Type	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI
	CHEMBL5093342	213778	0	None	-	1	Human	6.0	pEC50	=	6	Functional	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	213778	0	None	-	1	Human	6.0	pEC50	=	6	Functional	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	84778	0	None	-	1	Guinea pig	5.0	pEC50	=	5	Functional	Agonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contractionAgonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contraction	ChEMBL	450	9	1	5	4.5	O=C(CCCCCN1CCN(c2ccccc2[N+](=O)[O-])CC1)NC1CCCc2ccccc21	10.1021/jm070487n
	CHEMBL225571	84778	0	None	-	1	Guinea pig	5.0	pEC50	=	5	Functional	Agonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contractionAgonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contraction	ChEMBL	450	9	1	5	4.5	O=C(CCCCCN1CCN(c2ccccc2[N+](=O)[O-])CC1)NC1CCCc2ccccc21	10.1021/jm070487n
	CHEMBL5093342	213778	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	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	213778	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	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	66	None	-9	28	Human	7.0	pEC50	=	7.0	Functional	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	66	None	-9	28	Human	7.0	pEC50	=	7.0	Functional	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	66	None	-9	28	Human	7.0	pEC50	=	7.0	Functional	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	66	None	-9	28	Human	7.0	pEC50	=	7.0	Functional	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	147146	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	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	147146	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	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	66	None	-9	28	Human	7.0	pEC50	=	7.0	Functional	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	66	None	-9	28	Human	7.0	pEC50	=	7.0	Functional	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	66	None	-9	28	Human	7.0	pEC50	=	7.0	Functional	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	66	None	-9	28	Human	7.0	pEC50	=	7.0	Functional	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	164272	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay	ChEMBL	248	1	1	3	2.7	Clc1ccc(-c2noc3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	CHEMBL4218801	164272	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay	ChEMBL	248	1	1	3	2.7	Clc1ccc(-c2noc3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	135367816	164272	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay	ChEMBL	248	1	1	3	2.7	Clc1ccc(-c2noc3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	CHEMBL4218801	164272	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay	ChEMBL	248	1	1	3	2.7	Clc1ccc(-c2noc3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	134138168	147146	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	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	147146	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	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	92418	0	None	-	1	Guinea pig	5.9	pEC50	=	5.9	Functional	Agonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contractionAgonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contraction	ChEMBL	448	9	1	4	4.6	CN(C)c1ccccc1N1CCN(CCCCCC(=O)NC2CCCc3ccccc32)CC1	10.1021/jm070487n
	CHEMBL243955	92418	0	None	-	1	Guinea pig	5.9	pEC50	=	5.9	Functional	Agonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contractionAgonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contraction	ChEMBL	448	9	1	4	4.6	CN(C)c1ccccc1N1CCN(CCCCCC(=O)NC2CCCc3ccccc32)CC1	10.1021/jm070487n
	CHEMBL5081379	212964	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	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	212964	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	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	164258	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay	ChEMBL	232	1	1	3	2.2	Fc1ccc(-c2noc3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	CHEMBL4218672	164258	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay	ChEMBL	232	1	1	3	2.2	Fc1ccc(-c2noc3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	135367820	164258	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay	ChEMBL	232	1	1	3	2.2	Fc1ccc(-c2noc3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	CHEMBL4218672	164258	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay	ChEMBL	232	1	1	3	2.2	Fc1ccc(-c2noc3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	CHEMBL5094493	213713	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	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	213713	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	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	150792	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	150792	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	66	None	-9	28	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as increase in cAMP levels by HTRF assayAgonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as increase in cAMP levels by HTRF assay	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1021/jm8014553
	5202	139	66	None	-9	28	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as increase in cAMP levels by HTRF assayAgonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as increase in cAMP levels by HTRF assay	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1021/jm8014553
	CHEMBL39	139	66	None	-9	28	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as increase in cAMP levels by HTRF assayAgonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as increase in cAMP levels by HTRF assay	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1021/jm8014553
	DB08839	139	66	None	-9	28	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as increase in cAMP levels by HTRF assayAgonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as increase in cAMP levels by HTRF assay	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1021/jm8014553
	92042876	150792	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	150792	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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
	67268994	163405	2	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay	ChEMBL	247	1	2	2	2.4	Clc1ccc(-c2n[nH]c3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	CHEMBL4207884	163405	2	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay	ChEMBL	247	1	2	2	2.4	Clc1ccc(-c2n[nH]c3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	67268994	163405	2	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay	ChEMBL	247	1	2	2	2.4	Clc1ccc(-c2n[nH]c3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	CHEMBL4207884	163405	2	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay	ChEMBL	247	1	2	2	2.4	Clc1ccc(-c2n[nH]c3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	135367405	163633	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay	ChEMBL	227	1	2	2	2.1	Cc1ccc(-c2n[nH]c3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	CHEMBL4210782	163633	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay	ChEMBL	227	1	2	2	2.1	Cc1ccc(-c2n[nH]c3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	135367405	163633	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay	ChEMBL	227	1	2	2	2.1	Cc1ccc(-c2n[nH]c3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	CHEMBL4210782	163633	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay	ChEMBL	227	1	2	2	2.1	Cc1ccc(-c2n[nH]c3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	5	139	66	None	-9	28	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human 5-HT7 expressed in HEK-293 cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human 5-HT7 expressed in HEK-293 cells assessed as increase in cAMP level after 45 mins by HTRF assay	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1021/jm500880c
	5202	139	66	None	-9	28	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human 5-HT7 expressed in HEK-293 cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human 5-HT7 expressed in HEK-293 cells assessed as increase in cAMP level after 45 mins by HTRF assay	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1021/jm500880c
	CHEMBL39	139	66	None	-9	28	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human 5-HT7 expressed in HEK-293 cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human 5-HT7 expressed in HEK-293 cells assessed as increase in cAMP level after 45 mins by HTRF assay	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1021/jm500880c
	DB08839	139	66	None	-9	28	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human 5-HT7 expressed in HEK-293 cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human 5-HT7 expressed in HEK-293 cells assessed as increase in cAMP level after 45 mins by HTRF assay	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1021/jm500880c
	11385992	84231	0	None	-	1	Guinea pig	4.8	pEC50	=	4.8	Functional	Agonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contractionAgonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contraction	ChEMBL	439	8	1	3	5.2	O=C(CCCCCN1CCN(c2ccccc2Cl)CC1)NC1CCCc2ccccc21	10.1021/jm070487n
	CHEMBL222477	84231	0	None	-	1	Guinea pig	4.8	pEC50	=	4.8	Functional	Agonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contractionAgonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contraction	ChEMBL	439	8	1	3	5.2	O=C(CCCCCN1CCN(c2ccccc2Cl)CC1)NC1CCCc2ccccc21	10.1021/jm070487n
	23643664	2308	6	None	-	1	Guinea pig	5.8	pEC50	=	5.8	Functional	Agonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contractionAgonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contraction	ChEMBL	481	9	1	3	6.2	O=C(NC1CCCc2c1cccc2)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1	10.1021/jm070487n
	8434	2308	6	None	-	1	Guinea pig	5.8	pEC50	=	5.8	Functional	Agonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contractionAgonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contraction	ChEMBL	481	9	1	3	6.2	O=C(NC1CCCc2c1cccc2)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1	10.1021/jm070487n
	CHEMBL243954	2308	6	None	-	1	Guinea pig	5.8	pEC50	=	5.8	Functional	Agonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contractionAgonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contraction	ChEMBL	481	9	1	3	6.2	O=C(NC1CCCc2c1cccc2)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1	10.1021/jm070487n
	CHEMBL5094234	213787	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	213787	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	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	213787	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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	213787	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	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	84275	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Activity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileumActivity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileum	ChEMBL	419	8	1	3	4.9	Cc1ccccc1N1CCN(CCCCCC(=O)NC2CCCc3ccccc32)CC1	10.1021/jm049702f
	CHEMBL222755	84275	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Activity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileumActivity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileum	ChEMBL	419	8	1	3	4.9	Cc1ccccc1N1CCN(CCCCCC(=O)NC2CCCc3ccccc32)CC1	10.1021/jm049702f
	124247485	163506	7	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay	ChEMBL	231	1	2	2	1.9	Fc1ccc(-c2n[nH]c3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	CHEMBL4209274	163506	7	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay	ChEMBL	231	1	2	2	1.9	Fc1ccc(-c2n[nH]c3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	CHEMBL5084249	213123	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	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	163506	7	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay	ChEMBL	231	1	2	2	1.9	Fc1ccc(-c2n[nH]c3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	CHEMBL4209274	163506	7	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay	ChEMBL	231	1	2	2	1.9	Fc1ccc(-c2n[nH]c3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	CHEMBL5084249	213123	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	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	1490	10	None	-	1	Human	7.7	pEC50	=	7.7	Functional	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	1490	10	None	-	1	Human	7.7	pEC50	=	7.7	Functional	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	1490	10	None	-	1	Human	7.7	pEC50	=	7.7	Functional	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	1490	10	None	-	1	Human	7.7	pEC50	=	7.7	Functional	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	1490	10	None	-	1	Human	7.7	pEC50	=	7.7	Functional	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	1490	10	None	-	1	Human	7.7	pEC50	=	7.7	Functional	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	113031	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human 5-HT7 expressed in HEK-293 cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human 5-HT7 expressed in HEK-293 cells assessed as increase in cAMP level after 45 mins by HTRF assay	ChEMBL	346	6	0	2	4.0	O=C1Cc2ccccc2N1CC/C=C/CCN1CCc2ccccc2C1	10.1021/jm500880c
	CHEMBL3321794	113031	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human 5-HT7 expressed in HEK-293 cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human 5-HT7 expressed in HEK-293 cells assessed as increase in cAMP level after 45 mins by HTRF assay	ChEMBL	346	6	0	2	4.0	O=C1Cc2ccccc2N1CC/C=C/CCN1CCc2ccccc2C1	10.1021/jm500880c
	11282296	142771	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Activity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileumActivity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileum	ChEMBL	447	9	1	4	4.8	CC(=O)c1ccccc1N1CCN(CCCCCC(=O)NC2CCCc3ccccc32)CC1	10.1021/jm049702f
	CHEMBL389718	142771	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Activity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileumActivity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileum	ChEMBL	447	9	1	4	4.8	CC(=O)c1ccccc1N1CCN(CCCCCC(=O)NC2CCCc3ccccc32)CC1	10.1021/jm049702f
	11224758	2311	3	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Activity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileumActivity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileum	ChEMBL	451	9	1	4	5.3	CSc1ccccc1N1CCN(CC1)CCCCCC(=O)NC1CCCc2c1cccc2	10.1021/jm049702f
	8435	2311	3	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Activity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileumActivity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileum	ChEMBL	451	9	1	4	5.3	CSc1ccccc1N1CCN(CC1)CCCCCC(=O)NC1CCCc2c1cccc2	10.1021/jm049702f
	CHEMBL225284	2311	3	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Activity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileumActivity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileum	ChEMBL	451	9	1	4	5.3	CSc1ccccc1N1CCN(CC1)CCCCCC(=O)NC1CCCc2c1cccc2	10.1021/jm049702f
	5	139	66	None	-9	28	Human	8.4	pEC50	=	8.4	Functional	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	66	None	-9	28	Human	8.4	pEC50	=	8.4	Functional	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	66	None	-9	28	Human	8.4	pEC50	=	8.4	Functional	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	66	None	-9	28	Human	8.4	pEC50	=	8.4	Functional	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	187000	0	None	-	1	Guinea pig	6.5	pEC50	=	6.5	Functional	Agonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAgonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction	ChEMBL	442	10	1	4	4.7	O=C(CCCCCN1CCN(c2ccccc2-c2ccccc2)CC1)NCc1ccncc1	10.1021/jm800615e
	CHEMBL494709	187000	0	None	-	1	Guinea pig	6.5	pEC50	=	6.5	Functional	Agonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAgonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction	ChEMBL	442	10	1	4	4.7	O=C(CCCCCN1CCN(c2ccccc2-c2ccccc2)CC1)NCc1ccncc1	10.1021/jm800615e
	42625440	170236	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as increase in cAMP levels by HTRF assayAgonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as increase in cAMP levels by HTRF assay	ChEMBL	320	5	0	2	3.4	O=C1Cc2ccccc2N1CCCCN1CCc2ccccc2C1	10.1021/jm8014553
	CHEMBL445334	170236	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as increase in cAMP levels by HTRF assayAgonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as increase in cAMP levels by HTRF assay	ChEMBL	320	5	0	2	3.4	O=C1Cc2ccccc2N1CCCCN1CCc2ccccc2C1	10.1021/jm8014553
	92042877	148631	1	None	-	1	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assayAgonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assay	ChEMBL	241	4	1	2	3.4	CNCc1ccc(C)c(-c2ccccc2OC)c1	10.1016/j.ejmech.2016.07.029
	CHEMBL3943658	148631	1	None	-	1	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assayAgonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assay	ChEMBL	241	4	1	2	3.4	CNCc1ccc(C)c(-c2ccccc2OC)c1	10.1016/j.ejmech.2016.07.029
	92042877	148631	1	None	-	1	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assayAgonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assay	ChEMBL	241	4	1	2	3.4	CNCc1ccc(C)c(-c2ccccc2OC)c1	10.1016/j.ejmech.2016.07.029
	CHEMBL3943658	148631	1	None	-	1	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assayAgonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assay	ChEMBL	241	4	1	2	3.4	CNCc1ccc(C)c(-c2ccccc2OC)c1	10.1016/j.ejmech.2016.07.029
	5	139	66	None	-9	28	Human	8.4	pEC50	=	8.4	Functional	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	66	None	-9	28	Human	8.4	pEC50	=	8.4	Functional	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	66	None	-9	28	Human	8.4	pEC50	=	8.4	Functional	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	66	None	-9	28	Human	8.4	pEC50	=	8.4	Functional	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	164041	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay	ChEMBL	228	1	1	3	2.3	Cc1ccc(-c2noc3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	CHEMBL4215875	164041	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay	ChEMBL	228	1	1	3	2.3	Cc1ccc(-c2noc3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	135367857	164041	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay	ChEMBL	228	1	1	3	2.3	Cc1ccc(-c2noc3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	CHEMBL4215875	164041	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay	ChEMBL	228	1	1	3	2.3	Cc1ccc(-c2noc3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	92042876	150792	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	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	150792	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	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	150792	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	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	150792	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	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	66	None	-9	28	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1021/acs.jmedchem.8b00642
	5202	139	66	None	-9	28	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1021/acs.jmedchem.8b00642
	CHEMBL39	139	66	None	-9	28	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1021/acs.jmedchem.8b00642
	DB08839	139	66	None	-9	28	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1021/acs.jmedchem.8b00642
	134138168	147146	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	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	147146	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	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	66	None	-9	28	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1021/acs.jmedchem.8b00642
	5202	139	66	None	-9	28	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1021/acs.jmedchem.8b00642
	CHEMBL39	139	66	None	-9	28	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1021/acs.jmedchem.8b00642
	DB08839	139	66	None	-9	28	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assayAgonist activity at tTA containing TCS cleavage site-fused 5-HT7 receptor (unknown origin) expressed in tTA-dependent luciferase reporter/TEV-fused beta-arrestin2 expressing HTLA cells assessed as induction of beta-arrestin2 recruitment after 22 hrs by Tango assay	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1021/acs.jmedchem.8b00642
	134138168	147146	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	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	147146	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	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	186630	0	None	-	1	Guinea pig	6.3	pEC50	=	6.3	Functional	Agonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAgonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction	ChEMBL	467	8	0	3	5.6	O=C(CCCCCN1CCN(c2ccccc2-c2ccccc2)CC1)N1CCc2ccccc2C1	10.1021/jm800615e
	CHEMBL492480	186630	0	None	-	1	Guinea pig	6.3	pEC50	=	6.3	Functional	Agonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAgonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction	ChEMBL	467	8	0	3	5.6	O=C(CCCCCN1CCN(c2ccccc2-c2ccccc2)CC1)N1CCc2ccccc2C1	10.1021/jm800615e
	1809	134	28	None	-194	9	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human 5HT7 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assayAgonist activity at human 5HT7 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay	ChEMBL	203	3	3	2	0.8	NCCc1c[nH]c2c1cc(cc2)C(=O)N	10.1016/j.ejmech.2020.112709
	4	134	28	None	-194	9	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human 5HT7 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assayAgonist activity at human 5HT7 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay	ChEMBL	203	3	3	2	0.8	NCCc1c[nH]c2c1cc(cc2)C(=O)N	10.1016/j.ejmech.2020.112709
	CHEMBL18840	134	28	None	-194	9	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human 5HT7 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assayAgonist activity at human 5HT7 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay	ChEMBL	203	3	3	2	0.8	NCCc1c[nH]c2c1cc(cc2)C(=O)N	10.1016/j.ejmech.2020.112709
	5	139	66	None	-9	28	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assayAgonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assay	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1016/j.ejmech.2016.07.029
	5202	139	66	None	-9	28	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assayAgonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assay	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1016/j.ejmech.2016.07.029
	CHEMBL39	139	66	None	-9	28	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assayAgonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assay	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1016/j.ejmech.2016.07.029
	DB08839	139	66	None	-9	28	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assayAgonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assay	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1016/j.ejmech.2016.07.029
	5	139	66	None	-9	28	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assayAgonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assay	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1016/j.ejmech.2016.07.029
	5202	139	66	None	-9	28	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assayAgonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assay	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1016/j.ejmech.2016.07.029
	CHEMBL39	139	66	None	-9	28	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assayAgonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assay	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1016/j.ejmech.2016.07.029
	DB08839	139	66	None	-9	28	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assayAgonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assay	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1016/j.ejmech.2016.07.029
	92042876	150792	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assayAgonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assay	ChEMBL	261	4	1	2	3.7	CNCc1ccc(Cl)c(-c2ccccc2OC)c1	10.1016/j.ejmech.2016.07.029
	CHEMBL3961059	150792	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assayAgonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assay	ChEMBL	261	4	1	2	3.7	CNCc1ccc(Cl)c(-c2ccccc2OC)c1	10.1016/j.ejmech.2016.07.029
	92042876	150792	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assayAgonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assay	ChEMBL	261	4	1	2	3.7	CNCc1ccc(Cl)c(-c2ccccc2OC)c1	10.1016/j.ejmech.2016.07.029
	CHEMBL3961059	150792	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assayAgonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assay	ChEMBL	261	4	1	2	3.7	CNCc1ccc(Cl)c(-c2ccccc2OC)c1	10.1016/j.ejmech.2016.07.029
	CHEMBL5074190	212533	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	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	212533	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	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	213091	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	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	133070	23	None	-2818	8	Human	5.3	pEC50	=	5.3	Functional	Activity at 5HT7 receptor expressed in human corneal epithelial CEPI-17-CL4 cells by adenylyl cyclase assayActivity at 5HT7 receptor expressed in human corneal epithelial CEPI-17-CL4 cells by adenylyl cyclase assay	ChEMBL	191	2	2	4	1.1	C[C@H](N)Cn1ncc2ccc(O)cc21	10.1021/jm050663x
	CHEMBL371300	133070	23	None	-2818	8	Human	5.3	pEC50	=	5.3	Functional	Activity at 5HT7 receptor expressed in human corneal epithelial CEPI-17-CL4 cells by adenylyl cyclase assayActivity at 5HT7 receptor expressed in human corneal epithelial CEPI-17-CL4 cells by adenylyl cyclase assay	ChEMBL	191	2	2	4	1.1	C[C@H](N)Cn1ncc2ccc(O)cc21	10.1021/jm050663x
	CHEMBL5083607	213091	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	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	113035	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human 5-HT7 expressed in HEK-293 cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human 5-HT7 expressed in HEK-293 cells assessed as increase in cAMP level after 45 mins by HTRF assay	ChEMBL	352	6	0	2	4.4	O=C1Cc2ccccc2N1CC/C=C/CCN1CC[C@H]2CCCC[C@@H]2C1	10.1021/jm500880c
	CHEMBL3321798	113035	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human 5-HT7 expressed in HEK-293 cells assessed as increase in cAMP level after 45 mins by HTRF assayAgonist activity at human 5-HT7 expressed in HEK-293 cells assessed as increase in cAMP level after 45 mins by HTRF assay	ChEMBL	352	6	0	2	4.4	O=C1Cc2ccccc2N1CC/C=C/CCN1CC[C@H]2CCCC[C@@H]2C1	10.1021/jm500880c
	25107716	2309	35	None	-	1	Guinea pig	6.2	pEC50	=	6.2	Functional	Agonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAgonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction	ChEMBL	466	10	1	4	5.2	N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1	10.1021/jm800615e
	8436	2309	35	None	-	1	Guinea pig	6.2	pEC50	=	6.2	Functional	Agonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAgonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction	ChEMBL	466	10	1	4	5.2	N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1	10.1021/jm800615e
	CHEMBL522691	2309	35	None	-	1	Guinea pig	6.2	pEC50	=	6.2	Functional	Agonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAgonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction	ChEMBL	466	10	1	4	5.2	N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1	10.1021/jm800615e
	1809	134	28	None	-194	9	Human	6.2	pEC50	=	6.2	Functional	Activity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileumActivity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileum	ChEMBL	203	3	3	2	0.8	NCCc1c[nH]c2c1cc(cc2)C(=O)N	10.1021/jm049702f
	4	134	28	None	-194	9	Human	6.2	pEC50	=	6.2	Functional	Activity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileumActivity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileum	ChEMBL	203	3	3	2	0.8	NCCc1c[nH]c2c1cc(cc2)C(=O)N	10.1021/jm049702f
	CHEMBL18840	134	28	None	-194	9	Human	6.2	pEC50	=	6.2	Functional	Activity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileumActivity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileum	ChEMBL	203	3	3	2	0.8	NCCc1c[nH]c2c1cc(cc2)C(=O)N	10.1021/jm049702f
	1809	134	28	None	-2137	9	Guinea pig	6.2	pEC50	=	6.2	Functional	Agonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAgonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction	ChEMBL	203	3	3	2	0.8	NCCc1c[nH]c2c1cc(cc2)C(=O)N	10.1021/jm800615e
	4	134	28	None	-2137	9	Guinea pig	6.2	pEC50	=	6.2	Functional	Agonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAgonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction	ChEMBL	203	3	3	2	0.8	NCCc1c[nH]c2c1cc(cc2)C(=O)N	10.1021/jm800615e
	CHEMBL18840	134	28	None	-2137	9	Guinea pig	6.2	pEC50	=	6.2	Functional	Agonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contractionAgonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction	ChEMBL	203	3	3	2	0.8	NCCc1c[nH]c2c1cc(cc2)C(=O)N	10.1021/jm800615e
	1809	134	28	None	-2137	9	Guinea pig	6.2	pEC50	=	6.2	Functional	Agonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contractionAgonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contraction	ChEMBL	203	3	3	2	0.8	NCCc1c[nH]c2c1cc(cc2)C(=O)N	10.1021/jm070487n
	4	134	28	None	-2137	9	Guinea pig	6.2	pEC50	=	6.2	Functional	Agonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contractionAgonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contraction	ChEMBL	203	3	3	2	0.8	NCCc1c[nH]c2c1cc(cc2)C(=O)N	10.1021/jm070487n
	CHEMBL18840	134	28	None	-2137	9	Guinea pig	6.2	pEC50	=	6.2	Functional	Agonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contractionAgonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contraction	ChEMBL	203	3	3	2	0.8	NCCc1c[nH]c2c1cc(cc2)C(=O)N	10.1021/jm070487n
	11432177	84684	0	None	-	1	Human	5.2	pEC50	=	5.2	Functional	Activity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileumActivity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileum	ChEMBL	435	9	1	4	4.6	COc1ccccc1N1CCN(CCCCCC(=O)NC2CCCc3ccccc32)CC1	10.1021/jm049702f
	CHEMBL224820	84684	0	None	-	1	Human	5.2	pEC50	=	5.2	Functional	Activity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileumActivity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileum	ChEMBL	435	9	1	4	4.6	COc1ccccc1N1CCN(CCCCCC(=O)NC2CCCc3ccccc32)CC1	10.1021/jm049702f
	CHEMBL5083607	213091	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	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	213091	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	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	66	None	-9	28	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as increase in serotonin-induced cAMP level after 1 hr by TR-FRET assayAgonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as increase in serotonin-induced cAMP level after 1 hr by TR-FRET assay	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1016/j.bmcl.2018.04.059
	5202	139	66	None	-9	28	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as increase in serotonin-induced cAMP level after 1 hr by TR-FRET assayAgonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as increase in serotonin-induced cAMP level after 1 hr by TR-FRET assay	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1016/j.bmcl.2018.04.059
	CHEMBL39	139	66	None	-9	28	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as increase in serotonin-induced cAMP level after 1 hr by TR-FRET assayAgonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as increase in serotonin-induced cAMP level after 1 hr by TR-FRET assay	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1016/j.bmcl.2018.04.059
	DB08839	139	66	None	-9	28	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as increase in serotonin-induced cAMP level after 1 hr by TR-FRET assayAgonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as increase in serotonin-induced cAMP level after 1 hr by TR-FRET assay	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1016/j.bmcl.2018.04.059
	5	139	66	None	-9	28	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell incubated for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysisAgonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell incubated for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysis	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1016/j.bmc.2020.115578
	5202	139	66	None	-9	28	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell incubated for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysisAgonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell incubated for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysis	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1016/j.bmc.2020.115578
	CHEMBL39	139	66	None	-9	28	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell incubated for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysisAgonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell incubated for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysis	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1016/j.bmc.2020.115578
	DB08839	139	66	None	-9	28	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell incubated for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysisAgonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell incubated for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysis	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1016/j.bmc.2020.115578
	CHEMBL5091373	213781	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	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	213781	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	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	213781	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	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	213781	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	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	213781	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	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	213781	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	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	213781	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	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	213781	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	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	212710	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	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	212710	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	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	212558	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	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	212558	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	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	84188	0	None	-	1	Guinea pig	5.1	pEC50	=	5.1	Functional	Agonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contractionAgonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contraction	ChEMBL	405	8	1	3	4.6	O=C(CCCCCN1CCN(c2ccccc2)CC1)NC1CCCc2ccccc21	10.1021/jm070487n
	CHEMBL222188	84188	0	None	-	1	Guinea pig	5.1	pEC50	=	5.1	Functional	Agonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contractionAgonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contraction	ChEMBL	405	8	1	3	4.6	O=C(CCCCCN1CCN(c2ccccc2)CC1)NC1CCCc2ccccc21	10.1021/jm070487n
	24825775	1490	10	None	-	1	Human	7.1	pEC50	=	7.1	Functional	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	1490	10	None	-	1	Human	7.1	pEC50	=	7.1	Functional	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	1490	10	None	-	1	Human	7.1	pEC50	=	7.1	Functional	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	1490	10	None	-	1	Human	7.1	pEC50	=	7.1	Functional	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	1490	10	None	-	1	Human	7.1	pEC50	=	7.1	Functional	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	1490	10	None	-	1	Human	7.1	pEC50	=	7.1	Functional	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	212533	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	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	212533	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	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	66	None	-9	28	Human	8.0	pEC50	=	8.0	Functional	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	66	None	-9	28	Human	8.0	pEC50	=	8.0	Functional	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	66	None	-9	28	Human	8.0	pEC50	=	8.0	Functional	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	66	None	-9	28	Human	8.0	pEC50	=	8.0	Functional	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	92398	0	None	-	1	Guinea pig	6.1	pEC50	=	6.1	Functional	Agonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contractionAgonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contraction	ChEMBL	447	9	1	3	5.7	CC(C)c1ccccc1N1CCN(CCCCCC(=O)NC2CCCc3ccccc32)CC1	10.1021/jm070487n
	CHEMBL243744	92398	0	None	-	1	Guinea pig	6.1	pEC50	=	6.1	Functional	Agonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contractionAgonist activity at 5HT7 receptor in guinea pig ileum assessed as relaxation of substance P-induced contraction	ChEMBL	447	9	1	3	5.7	CC(C)c1ccccc1N1CCN(CCCCCC(=O)NC2CCCc3ccccc32)CC1	10.1021/jm070487n
	CHEMBL5077293	212710	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	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	212710	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	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	3443	40	None	8511	2	Human	9.3	pIC50	=	9.3	Functional	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	3443	40	None	8511	2	Human	9.3	pIC50	=	9.3	Functional	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	3443	40	None	8511	2	Human	9.3	pIC50	=	9.3	Functional	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	3443	40	None	8511	2	Human	9.3	pIC50	=	9.3	Functional	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	3443	40	None	8511	2	Human	9.3	pIC50	=	9.3	Functional	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	2456	16	None	-7	7	Human	9.1	pIC50	=	9.1	Functional	Antagonist activity at 5HT7R receptor (unknown origin) assessed as forskolin-mediated cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by TR-FRET analysisAntagonist activity at 5HT7R receptor (unknown origin) assessed as forskolin-mediated cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by TR-FRET analysis	ChEMBL	356	2	0	4	4.4	CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C	10.1016/j.bmcl.2019.126703
	5358812	2456	16	None	-7	7	Human	9.1	pIC50	=	9.1	Functional	Antagonist activity at 5HT7R receptor (unknown origin) assessed as forskolin-mediated cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by TR-FRET analysisAntagonist activity at 5HT7R receptor (unknown origin) assessed as forskolin-mediated cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by TR-FRET analysis	ChEMBL	356	2	0	4	4.4	CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C	10.1016/j.bmcl.2019.126703
	89	2456	16	None	-7	7	Human	9.1	pIC50	=	9.1	Functional	Antagonist activity at 5HT7R receptor (unknown origin) assessed as forskolin-mediated cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by TR-FRET analysisAntagonist activity at 5HT7R receptor (unknown origin) assessed as forskolin-mediated cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by TR-FRET analysis	ChEMBL	356	2	0	4	4.4	CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C	10.1016/j.bmcl.2019.126703
	CHEMBL93240	2456	16	None	-7	7	Human	9.1	pIC50	=	9.1	Functional	Antagonist activity at 5HT7R receptor (unknown origin) assessed as forskolin-mediated cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by TR-FRET analysisAntagonist activity at 5HT7R receptor (unknown origin) assessed as forskolin-mediated cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by TR-FRET analysis	ChEMBL	356	2	0	4	4.4	CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C	10.1016/j.bmcl.2019.126703
	3233	3443	40	None	8511	2	Human	9.1	pIC50	=	9.1	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay	ChEMBL	352	5	1	4	2.7	CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O	10.1021/acs.jmedchem.8b00642
	3247	3443	40	None	8511	2	Human	9.1	pIC50	=	9.1	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay	ChEMBL	352	5	1	4	2.7	CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O	10.1021/acs.jmedchem.8b00642
	6604889	3443	40	None	8511	2	Human	9.1	pIC50	=	9.1	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay	ChEMBL	352	5	1	4	2.7	CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O	10.1021/acs.jmedchem.8b00642
	CHEMBL282199	3443	40	None	8511	2	Human	9.1	pIC50	=	9.1	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay	ChEMBL	352	5	1	4	2.7	CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O	10.1021/acs.jmedchem.8b00642
	DB13988	3443	40	None	8511	2	Human	9.1	pIC50	=	9.1	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay	ChEMBL	352	5	1	4	2.7	CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O	10.1021/acs.jmedchem.8b00642
	3233	3443	40	None	8511	2	Human	9.0	pIC50	=	9.0	Functional	Antagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assayAntagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assay	ChEMBL	352	5	1	4	2.7	CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O	10.1016/j.bmcl.2018.04.059
	3247	3443	40	None	8511	2	Human	9.0	pIC50	=	9.0	Functional	Antagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assayAntagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assay	ChEMBL	352	5	1	4	2.7	CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O	10.1016/j.bmcl.2018.04.059
	6604889	3443	40	None	8511	2	Human	9.0	pIC50	=	9.0	Functional	Antagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assayAntagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assay	ChEMBL	352	5	1	4	2.7	CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O	10.1016/j.bmcl.2018.04.059
	CHEMBL282199	3443	40	None	8511	2	Human	9.0	pIC50	=	9.0	Functional	Antagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assayAntagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assay	ChEMBL	352	5	1	4	2.7	CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O	10.1016/j.bmcl.2018.04.059
	DB13988	3443	40	None	8511	2	Human	9.0	pIC50	=	9.0	Functional	Antagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assayAntagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assay	ChEMBL	352	5	1	4	2.7	CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O	10.1016/j.bmcl.2018.04.059
	3233	3443	40	None	8511	2	Human	9.0	pIC50	=	9.0	Functional	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	3443	40	None	8511	2	Human	9.0	pIC50	=	9.0	Functional	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	3443	40	None	8511	2	Human	9.0	pIC50	=	9.0	Functional	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	3443	40	None	8511	2	Human	9.0	pIC50	=	9.0	Functional	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	3443	40	None	8511	2	Human	9.0	pIC50	=	9.0	Functional	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	3443	40	None	8511	2	Human	9.0	pIC50	=	9.0	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay	ChEMBL	352	5	1	4	2.7	CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O	10.1021/acs.jmedchem.8b00642
	3247	3443	40	None	8511	2	Human	9.0	pIC50	=	9.0	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay	ChEMBL	352	5	1	4	2.7	CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O	10.1021/acs.jmedchem.8b00642
	6604889	3443	40	None	8511	2	Human	9.0	pIC50	=	9.0	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay	ChEMBL	352	5	1	4	2.7	CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O	10.1021/acs.jmedchem.8b00642
	CHEMBL282199	3443	40	None	8511	2	Human	9.0	pIC50	=	9.0	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay	ChEMBL	352	5	1	4	2.7	CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O	10.1021/acs.jmedchem.8b00642
	DB13988	3443	40	None	8511	2	Human	9.0	pIC50	=	9.0	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay	ChEMBL	352	5	1	4	2.7	CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O	10.1021/acs.jmedchem.8b00642
	4106	2456	16	None	-7	7	Human	8.8	pIC50	=	8.8	Functional	Antagonist activity at human recombinant 5-HT7 receptor assessed as inhibition of serotonin-induced cAMP accumulationAntagonist activity at human recombinant 5-HT7 receptor assessed as inhibition of serotonin-induced cAMP accumulation	ChEMBL	356	2	0	4	4.4	CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C	10.1021/jm401895u
	5358812	2456	16	None	-7	7	Human	8.8	pIC50	=	8.8	Functional	Antagonist activity at human recombinant 5-HT7 receptor assessed as inhibition of serotonin-induced cAMP accumulationAntagonist activity at human recombinant 5-HT7 receptor assessed as inhibition of serotonin-induced cAMP accumulation	ChEMBL	356	2	0	4	4.4	CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C	10.1021/jm401895u
	89	2456	16	None	-7	7	Human	8.8	pIC50	=	8.8	Functional	Antagonist activity at human recombinant 5-HT7 receptor assessed as inhibition of serotonin-induced cAMP accumulationAntagonist activity at human recombinant 5-HT7 receptor assessed as inhibition of serotonin-induced cAMP accumulation	ChEMBL	356	2	0	4	4.4	CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C	10.1021/jm401895u
	CHEMBL93240	2456	16	None	-7	7	Human	8.8	pIC50	=	8.8	Functional	Antagonist activity at human recombinant 5-HT7 receptor assessed as inhibition of serotonin-induced cAMP accumulationAntagonist activity at human recombinant 5-HT7 receptor assessed as inhibition of serotonin-induced cAMP accumulation	ChEMBL	356	2	0	4	4.4	CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C	10.1021/jm401895u
	164609529	183872	0	None	-36	2	Human	7.0	pIC50	=	7	Functional	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	183872	0	None	-36	2	Human	7.0	pIC50	=	7	Functional	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	179933	0	None	-	1	Human	7.0	pIC50	=	7	Functional	Inverse agonist activity at 5-HT7 receptor (unknown origin) by cAMP functional assayInverse agonist activity at 5-HT7 receptor (unknown origin) by cAMP functional assay	ChEMBL	273	2	1	3	3.0	CC(C)n1nc2c(c1-c1ccc(F)cc1)CCNCC2	10.1016/j.bmcl.2020.127669
	CHEMBL4753511	179933	0	None	-	1	Human	7.0	pIC50	=	7	Functional	Inverse agonist activity at 5-HT7 receptor (unknown origin) by cAMP functional assayInverse agonist activity at 5-HT7 receptor (unknown origin) by cAMP functional assay	ChEMBL	273	2	1	3	3.0	CC(C)n1nc2c(c1-c1ccc(F)cc1)CCNCC2	10.1016/j.bmcl.2020.127669
	127028798	137643	0	None	-	1	Human	6.0	pIC50	=	6	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay	ChEMBL	454	6	2	5	2.4	Cc1ccc(C)c(N2CCN(CC(O)CN3C(=O)NC(C)(c4ccc(F)cc4)C3=O)CC2)c1	10.1016/j.ejmech.2016.02.024
	CHEMBL3769612	137643	0	None	-	1	Human	6.0	pIC50	=	6	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay	ChEMBL	454	6	2	5	2.4	Cc1ccc(C)c(N2CCN(CC(O)CN3C(=O)NC(C)(c4ccc(F)cc4)C3=O)CC2)c1	10.1016/j.ejmech.2016.02.024
	142601335	185829	0	None	-	1	Human	6.0	pIC50	=	6.0	Functional	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	185829	0	None	-	1	Human	6.0	pIC50	=	6.0	Functional	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	167025	0	None	-144	3	Human	6.0	pIC50	=	6.0	Functional	Antagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assayAntagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assay	ChEMBL	354	7	0	4	3.9	COc1ccccc1N1CCN(CCCOc2ccc(C)cc2C)CC1	10.1016/j.bmcl.2018.04.059
	CHEMBL4209888	167025	0	None	-144	3	Human	6.0	pIC50	=	6.0	Functional	Antagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assayAntagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assay	ChEMBL	354	7	0	4	3.9	COc1ccccc1N1CCN(CCCOc2ccc(C)cc2C)CC1	10.1016/j.bmcl.2018.04.059
	CHEMBL4300899	167025	0	None	-144	3	Human	6.0	pIC50	=	6.0	Functional	Antagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assayAntagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assay	ChEMBL	354	7	0	4	3.9	COc1ccccc1N1CCN(CCCOc2ccc(C)cc2C)CC1	10.1016/j.bmcl.2018.04.059
	142601335	185829	0	None	-	1	Human	6.0	pIC50	=	6.0	Functional	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	185829	0	None	-	1	Human	6.0	pIC50	=	6.0	Functional	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	2456	16	None	-7	7	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human 5HT7 receptor expressed in CHO-K1 cells assessed as inhibition of 5CT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5CT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT7 receptor expressed in CHO-K1 cells assessed as inhibition of 5CT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5CT addition by calcium 4 dye based FLIPR assay	ChEMBL	356	2	0	4	4.4	CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C	10.1016/j.ejmech.2020.112709
	5358812	2456	16	None	-7	7	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human 5HT7 receptor expressed in CHO-K1 cells assessed as inhibition of 5CT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5CT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT7 receptor expressed in CHO-K1 cells assessed as inhibition of 5CT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5CT addition by calcium 4 dye based FLIPR assay	ChEMBL	356	2	0	4	4.4	CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C	10.1016/j.ejmech.2020.112709
	89	2456	16	None	-7	7	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human 5HT7 receptor expressed in CHO-K1 cells assessed as inhibition of 5CT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5CT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT7 receptor expressed in CHO-K1 cells assessed as inhibition of 5CT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5CT addition by calcium 4 dye based FLIPR assay	ChEMBL	356	2	0	4	4.4	CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C	10.1016/j.ejmech.2020.112709
	CHEMBL93240	2456	16	None	-7	7	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human 5HT7 receptor expressed in CHO-K1 cells assessed as inhibition of 5CT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5CT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT7 receptor expressed in CHO-K1 cells assessed as inhibition of 5CT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5CT addition by calcium 4 dye based FLIPR assay	ChEMBL	356	2	0	4	4.4	CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C	10.1016/j.ejmech.2020.112709
	117209912	184745	1	None	-	1	Human	5.9	pIC50	=	5.9	Functional	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	184745	1	None	-	1	Human	5.9	pIC50	=	5.9	Functional	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	184745	1	None	-	1	Human	5.9	pIC50	=	5.9	Functional	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	184745	1	None	-	1	Human	5.9	pIC50	=	5.9	Functional	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	180892	0	None	-1	5	Human	7.9	pIC50	=	7.9	Functional	Antagonist activity at human 5HT7 receptor expressed in CHO-K1 cells assessed as inhibition of 5CT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5CT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT7 receptor expressed in CHO-K1 cells assessed as inhibition of 5CT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5CT addition by calcium 4 dye based FLIPR assay	ChEMBL	437	6	0	5	4.2	CN1CCc2ccc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc2C1=O	10.1016/j.ejmech.2020.112709
	CHEMBL4764679	180892	0	None	-1	5	Human	7.9	pIC50	=	7.9	Functional	Antagonist activity at human 5HT7 receptor expressed in CHO-K1 cells assessed as inhibition of 5CT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5CT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT7 receptor expressed in CHO-K1 cells assessed as inhibition of 5CT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5CT addition by calcium 4 dye based FLIPR assay	ChEMBL	437	6	0	5	4.2	CN1CCc2ccc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc2C1=O	10.1016/j.ejmech.2020.112709
	206	2447	10	None	-97	3	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as inhibition of serotonon-induced increase in cAMP levels by HTRF assay relative to untreated controlAntagonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as inhibition of serotonon-induced increase in cAMP levels by HTRF assay relative to untreated control	ChEMBL	362	3	1	4	1.3	CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C	10.1021/jm8014553
	68848	2447	10	None	-97	3	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as inhibition of serotonon-induced increase in cAMP levels by HTRF assay relative to untreated controlAntagonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as inhibition of serotonon-induced increase in cAMP levels by HTRF assay relative to untreated control	ChEMBL	362	3	1	4	1.3	CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C	10.1021/jm8014553
	CHEMBL12314	2447	10	None	-97	3	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as inhibition of serotonon-induced increase in cAMP levels by HTRF assay relative to untreated controlAntagonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as inhibition of serotonon-induced increase in cAMP levels by HTRF assay relative to untreated control	ChEMBL	362	3	1	4	1.3	CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C	10.1021/jm8014553
	156013673	176677	0	None	-	1	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell preincubated for 30 mins followed by incubation with agonist for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysisAntagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell preincubated for 30 mins followed by incubation with agonist for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysis	ChEMBL	293	1	2	2	2.9	CN1CCc2cccc3c2C1Cc1ccc(NC(N)=O)cc1-3	10.1016/j.bmc.2020.115578
	CHEMBL4636148	176677	0	None	-	1	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell preincubated for 30 mins followed by incubation with agonist for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysisAntagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell preincubated for 30 mins followed by incubation with agonist for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysis	ChEMBL	293	1	2	2	2.9	CN1CCc2cccc3c2C1Cc1ccc(NC(N)=O)cc1-3	10.1016/j.bmc.2020.115578
	127028797	137792	0	None	-	1	Human	5.9	pIC50	=	5.9	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay	ChEMBL	494	6	2	5	3.1	CC1(c2ccc(F)cc2)NC(=O)N(CC(O)CN2CCN(c3cccc(Cl)c3Cl)CC2)C1=O	10.1016/j.ejmech.2016.02.024
	CHEMBL3771309	137792	0	None	-	1	Human	5.9	pIC50	=	5.9	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay	ChEMBL	494	6	2	5	3.1	CC1(c2ccc(F)cc2)NC(=O)N(CC(O)CN2CCN(c3cccc(Cl)c3Cl)CC2)C1=O	10.1016/j.ejmech.2016.02.024
	11536844	114611	0	None	2	2	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human 5-HT7 receptor expressed in CHO cells assessed as cAMP production by EIA systemAntagonist activity at human 5-HT7 receptor expressed in CHO cells assessed as cAMP production by EIA system	ChEMBL	307	1	2	2	2.1	NC(N)=NC(=O)c1ccc2c(c1)[C@]1(CCCO1)c1ccccc1-2	10.1016/j.bmc.2014.09.005
	CHEMBL3343672	114611	0	None	2	2	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human 5-HT7 receptor expressed in CHO cells assessed as cAMP production by EIA systemAntagonist activity at human 5-HT7 receptor expressed in CHO cells assessed as cAMP production by EIA system	ChEMBL	307	1	2	2	2.1	NC(N)=NC(=O)c1ccc2c(c1)[C@]1(CCCO1)c1ccccc1-2	10.1016/j.bmc.2014.09.005
	213046	2343	55	None	-	1	Human	7.8	pIC50	=	7.8	Functional	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	2343	55	None	-	1	Human	7.8	pIC50	=	7.8	Functional	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	2343	55	None	-	1	Human	7.8	pIC50	=	7.8	Functional	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	2343	55	None	-	1	Human	7.8	pIC50	=	7.8	Functional	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	2343	55	None	-	1	Human	7.8	pIC50	=	7.8	Functional	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	184953	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	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	184953	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	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	184953	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	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	184953	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	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	120057	0	None	3	2	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human 5-HT7 receptor expressed in CHO cells assessed as cAMP production by EIA systemAntagonist activity at human 5-HT7 receptor expressed in CHO cells assessed as cAMP production by EIA system	ChEMBL	307	1	2	2	2.1	NC(N)=NC(=O)c1ccc2c(c1)C1(CCCO1)c1ccccc1-2	10.1016/j.bmc.2014.09.005
	CHEMBL3343670	120057	0	None	3	2	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human 5-HT7 receptor expressed in CHO cells assessed as cAMP production by EIA systemAntagonist activity at human 5-HT7 receptor expressed in CHO cells assessed as cAMP production by EIA system	ChEMBL	307	1	2	2	2.1	NC(N)=NC(=O)c1ccc2c(c1)C1(CCCO1)c1ccccc1-2	10.1016/j.bmc.2014.09.005
	CHEMBL3545812	120057	0	None	3	2	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human 5-HT7 receptor expressed in CHO cells assessed as cAMP production by EIA systemAntagonist activity at human 5-HT7 receptor expressed in CHO cells assessed as cAMP production by EIA system	ChEMBL	307	1	2	2	2.1	NC(N)=NC(=O)c1ccc2c(c1)C1(CCCO1)c1ccccc1-2	10.1016/j.bmc.2014.09.005
	117209962	184276	1	None	-	1	Human	5.8	pIC50	=	5.8	Functional	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	184276	1	None	-	1	Human	5.8	pIC50	=	5.8	Functional	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	184276	1	None	-	1	Human	5.8	pIC50	=	5.8	Functional	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	184276	1	None	-	1	Human	5.8	pIC50	=	5.8	Functional	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	185011	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	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	185011	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	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	185011	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	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	185011	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	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	137787	0	None	-	1	Human	5.7	pIC50	=	5.7	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay	ChEMBL	516	8	2	5	3.4	CC1(c2ccc(F)cc2)NC(=O)N(CC(O)CN2CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O	10.1016/j.ejmech.2016.02.024
	CHEMBL3771222	137787	0	None	-	1	Human	5.7	pIC50	=	5.7	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay	ChEMBL	516	8	2	5	3.4	CC1(c2ccc(F)cc2)NC(=O)N(CC(O)CN2CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O	10.1016/j.ejmech.2016.02.024
	145947937	167151	0	None	-32	4	Human	5.7	pIC50	=	5.7	Functional	Antagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assayAntagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assay	ChEMBL	398	9	0	5	3.8	COc1ccccc1N1CCN(CCOCCOc2c(C)cc(C)cc2C)CC1	10.1016/j.bmcl.2018.04.059
	CHEMBL4207653	167151	0	None	-32	4	Human	5.7	pIC50	=	5.7	Functional	Antagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assayAntagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assay	ChEMBL	398	9	0	5	3.8	COc1ccccc1N1CCN(CCOCCOc2c(C)cc(C)cc2C)CC1	10.1016/j.bmcl.2018.04.059
	CHEMBL4302655	167151	0	None	-32	4	Human	5.7	pIC50	=	5.7	Functional	Antagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assayAntagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assay	ChEMBL	398	9	0	5	3.8	COc1ccccc1N1CCN(CCOCCOc2c(C)cc(C)cc2C)CC1	10.1016/j.bmcl.2018.04.059
	134141985	146631	0	None	-	1	Human	4.7	pIC50	=	4.7	Functional	Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay	ChEMBL	432	6	0	6	4.4	COc1ccccc1-c1cc(CN2CCN(c3ccccc3OC)CC2)cc2c1OCO2	10.1016/j.ejmech.2016.07.029
	CHEMBL3927929	146631	0	None	-	1	Human	4.7	pIC50	=	4.7	Functional	Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay	ChEMBL	432	6	0	6	4.4	COc1ccccc1-c1cc(CN2CCN(c3ccccc3OC)CC2)cc2c1OCO2	10.1016/j.ejmech.2016.07.029
	134141985	146631	0	None	-	1	Human	4.7	pIC50	=	4.7	Functional	Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay	ChEMBL	432	6	0	6	4.4	COc1ccccc1-c1cc(CN2CCN(c3ccccc3OC)CC2)cc2c1OCO2	10.1016/j.ejmech.2016.07.029
	CHEMBL3927929	146631	0	None	-	1	Human	4.7	pIC50	=	4.7	Functional	Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay	ChEMBL	432	6	0	6	4.4	COc1ccccc1-c1cc(CN2CCN(c3ccccc3OC)CC2)cc2c1OCO2	10.1016/j.ejmech.2016.07.029
	44348383	16112	0	None	-	1	Human	8.7	pIC50	=	8.7	Functional	Antagonist activity at human 5HT7 receptor expressed in HEK293 assessed as inhibition of 5HT-induced cAMP accumulationAntagonist activity at human 5HT7 receptor expressed in HEK293 assessed as inhibition of 5HT-induced cAMP accumulation	ChEMBL	205	3	1	2	2.7	CSc1ccc2c(c1)C(CCN)=CC2	10.1016/j.ejmech.2012.11.042
	CHEMBL122536	16112	0	None	-	1	Human	8.7	pIC50	=	8.7	Functional	Antagonist activity at human 5HT7 receptor expressed in HEK293 assessed as inhibition of 5HT-induced cAMP accumulationAntagonist activity at human 5HT7 receptor expressed in HEK293 assessed as inhibition of 5HT-induced cAMP accumulation	ChEMBL	205	3	1	2	2.7	CSc1ccc2c(c1)C(CCN)=CC2	10.1016/j.ejmech.2012.11.042
	4106	2456	16	None	-7	7	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay	ChEMBL	356	2	0	4	4.4	CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C	10.1016/j.ejmech.2016.02.024
	5358812	2456	16	None	-7	7	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay	ChEMBL	356	2	0	4	4.4	CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C	10.1016/j.ejmech.2016.02.024
	89	2456	16	None	-7	7	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay	ChEMBL	356	2	0	4	4.4	CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C	10.1016/j.ejmech.2016.02.024
	CHEMBL93240	2456	16	None	-7	7	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay	ChEMBL	356	2	0	4	4.4	CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C	10.1016/j.ejmech.2016.02.024
	102364516	113031	0	None	-	1	Human	5.7	pIC50	=	5.7	Functional	Antagonist activity at human 5-HT7 expressed in HEK-293 cells assessed as inhibition in serotonin-induced increase in cAMP level after 45 mins by HTRF assayAntagonist activity at human 5-HT7 expressed in HEK-293 cells assessed as inhibition in serotonin-induced increase in cAMP level after 45 mins by HTRF assay	ChEMBL	346	6	0	2	4.0	O=C1Cc2ccccc2N1CC/C=C/CCN1CCc2ccccc2C1	10.1021/jm500880c
	CHEMBL3321794	113031	0	None	-	1	Human	5.7	pIC50	=	5.7	Functional	Antagonist activity at human 5-HT7 expressed in HEK-293 cells assessed as inhibition in serotonin-induced increase in cAMP level after 45 mins by HTRF assayAntagonist activity at human 5-HT7 expressed in HEK-293 cells assessed as inhibition in serotonin-induced increase in cAMP level after 45 mins by HTRF assay	ChEMBL	346	6	0	2	4.0	O=C1Cc2ccccc2N1CC/C=C/CCN1CCc2ccccc2C1	10.1021/jm500880c
	134157289	153535	0	None	-	1	Human	4.6	pIC50	=	4.6	Functional	Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay	ChEMBL	422	6	0	4	5.3	COc1ccccc1-c1cc(CN2CCN(c3ccccc3OC)CC2)ccc1Cl	10.1016/j.ejmech.2016.07.029
	CHEMBL3984812	153535	0	None	-	1	Human	4.6	pIC50	=	4.6	Functional	Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay	ChEMBL	422	6	0	4	5.3	COc1ccccc1-c1cc(CN2CCN(c3ccccc3OC)CC2)ccc1Cl	10.1016/j.ejmech.2016.07.029
	118709756	113035	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at human 5-HT7 expressed in HEK-293 cells assessed as inhibition in serotonin-induced increase in cAMP level after 45 mins by HTRF assayAntagonist activity at human 5-HT7 expressed in HEK-293 cells assessed as inhibition in serotonin-induced increase in cAMP level after 45 mins by HTRF assay	ChEMBL	352	6	0	2	4.4	O=C1Cc2ccccc2N1CC/C=C/CCN1CC[C@H]2CCCC[C@@H]2C1	10.1021/jm500880c
	CHEMBL3321798	113035	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at human 5-HT7 expressed in HEK-293 cells assessed as inhibition in serotonin-induced increase in cAMP level after 45 mins by HTRF assayAntagonist activity at human 5-HT7 expressed in HEK-293 cells assessed as inhibition in serotonin-induced increase in cAMP level after 45 mins by HTRF assay	ChEMBL	352	6	0	2	4.4	O=C1Cc2ccccc2N1CC/C=C/CCN1CC[C@H]2CCCC[C@@H]2C1	10.1021/jm500880c
	134157289	153535	0	None	-	1	Human	4.6	pIC50	=	4.6	Functional	Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay	ChEMBL	422	6	0	4	5.3	COc1ccccc1-c1cc(CN2CCN(c3ccccc3OC)CC2)ccc1Cl	10.1016/j.ejmech.2016.07.029
	CHEMBL3984812	153535	0	None	-	1	Human	4.6	pIC50	=	4.6	Functional	Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay	ChEMBL	422	6	0	4	5.3	COc1ccccc1-c1cc(CN2CCN(c3ccccc3OC)CC2)ccc1Cl	10.1016/j.ejmech.2016.07.029
	117209857	184545	1	None	-	1	Human	5.6	pIC50	=	5.6	Functional	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	184545	1	None	-	1	Human	5.6	pIC50	=	5.6	Functional	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	184410	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	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	184410	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	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	166986	0	None	-30	4	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assayAntagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assay	ChEMBL	398	9	0	5	3.8	COc1ccccc1N1CCN(CCOCCOc2cc(C)cc(C)c2C)CC1	10.1016/j.bmcl.2018.04.059
	CHEMBL4213352	166986	0	None	-30	4	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assayAntagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assay	ChEMBL	398	9	0	5	3.8	COc1ccccc1N1CCN(CCOCCOc2cc(C)cc(C)c2C)CC1	10.1016/j.bmcl.2018.04.059
	CHEMBL4300399	166986	0	None	-30	4	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assayAntagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assay	ChEMBL	398	9	0	5	3.8	COc1ccccc1N1CCN(CCOCCOc2cc(C)cc(C)c2C)CC1	10.1016/j.bmcl.2018.04.059
	142601328	184410	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	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	184410	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	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	184545	1	None	-	1	Human	5.6	pIC50	=	5.6	Functional	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	184545	1	None	-	1	Human	5.6	pIC50	=	5.6	Functional	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	137725	0	None	-	1	Human	4.6	pIC50	=	4.6	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay	ChEMBL	494	6	2	5	3.1	CC1(c2ccc(F)cc2)NC(=O)N(CC(O)CN2CCN(c3ccc(Cl)c(Cl)c3)CC2)C1=O	10.1016/j.ejmech.2016.02.024
	CHEMBL3770581	137725	0	None	-	1	Human	4.6	pIC50	=	4.6	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay	ChEMBL	494	6	2	5	3.1	CC1(c2ccc(F)cc2)NC(=O)N(CC(O)CN2CCN(c3ccc(Cl)c(Cl)c3)CC2)C1=O	10.1016/j.ejmech.2016.02.024
	142601333	185171	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	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	185171	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	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	184410	0	None	-	1	Human	4.6	pIC50	=	4.6	Functional	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	184410	0	None	-	1	Human	4.6	pIC50	=	4.6	Functional	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	164258	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay	ChEMBL	232	1	1	3	2.2	Fc1ccc(-c2noc3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	CHEMBL4218672	164258	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay	ChEMBL	232	1	1	3	2.2	Fc1ccc(-c2noc3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	142601333	185171	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	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	185171	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	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	184410	0	None	-	1	Human	4.6	pIC50	=	4.6	Functional	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	184410	0	None	-	1	Human	4.6	pIC50	=	4.6	Functional	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	164258	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay	ChEMBL	232	1	1	3	2.2	Fc1ccc(-c2noc3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	CHEMBL4218672	164258	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay	ChEMBL	232	1	1	3	2.2	Fc1ccc(-c2noc3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	135367405	163633	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay	ChEMBL	227	1	2	2	2.1	Cc1ccc(-c2n[nH]c3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	CHEMBL4210782	163633	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay	ChEMBL	227	1	2	2	2.1	Cc1ccc(-c2n[nH]c3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	135367405	163633	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay	ChEMBL	227	1	2	2	2.1	Cc1ccc(-c2n[nH]c3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	CHEMBL4210782	163633	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay	ChEMBL	227	1	2	2	2.1	Cc1ccc(-c2n[nH]c3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	156010865	176547	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell preincubated for 30 mins followed by incubation with agonist for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysisAntagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell preincubated for 30 mins followed by incubation with agonist for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysis	ChEMBL	307	0	1	4	3.6	CN1CCc2cccc3c2C1Cc1cc2sc(N)nc2cc1-3	10.1016/j.bmc.2020.115578
	CHEMBL4633786	176547	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell preincubated for 30 mins followed by incubation with agonist for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysisAntagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell preincubated for 30 mins followed by incubation with agonist for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysis	ChEMBL	307	0	1	4	3.6	CN1CCc2cccc3c2C1Cc1cc2sc(N)nc2cc1-3	10.1016/j.bmc.2020.115578
	71574210	85842	0	None	2	2	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at human 5HT7 receptor expressed in HEK293 assessed as inhibition of 5HT-induced cAMP accumulationAntagonist activity at human 5HT7 receptor expressed in HEK293 assessed as inhibition of 5HT-induced cAMP accumulation	ChEMBL	478	7	1	5	4.0	O=S(=O)(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2cccnc2c1	10.1016/j.ejmech.2012.11.042
	CHEMBL2312934	85842	0	None	2	2	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at human 5HT7 receptor expressed in HEK293 assessed as inhibition of 5HT-induced cAMP accumulationAntagonist activity at human 5HT7 receptor expressed in HEK293 assessed as inhibition of 5HT-induced cAMP accumulation	ChEMBL	478	7	1	5	4.0	O=S(=O)(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2cccnc2c1	10.1016/j.ejmech.2012.11.042
	206	2447	10	None	-97	3	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human 5-HT7 expressed in HEK-293 cells assessed as inhibition in serotonin-induced increase in cAMP level after 45 mins by HTRF assayAntagonist activity at human 5-HT7 expressed in HEK-293 cells assessed as inhibition in serotonin-induced increase in cAMP level after 45 mins by HTRF assay	ChEMBL	362	3	1	4	1.3	CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C	10.1021/jm500880c
	68848	2447	10	None	-97	3	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human 5-HT7 expressed in HEK-293 cells assessed as inhibition in serotonin-induced increase in cAMP level after 45 mins by HTRF assayAntagonist activity at human 5-HT7 expressed in HEK-293 cells assessed as inhibition in serotonin-induced increase in cAMP level after 45 mins by HTRF assay	ChEMBL	362	3	1	4	1.3	CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C	10.1021/jm500880c
	CHEMBL12314	2447	10	None	-97	3	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human 5-HT7 expressed in HEK-293 cells assessed as inhibition in serotonin-induced increase in cAMP level after 45 mins by HTRF assayAntagonist activity at human 5-HT7 expressed in HEK-293 cells assessed as inhibition in serotonin-induced increase in cAMP level after 45 mins by HTRF assay	ChEMBL	362	3	1	4	1.3	CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C	10.1021/jm500880c
	3233	3443	40	None	8511	2	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay	ChEMBL	352	5	1	4	2.7	CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O	10.1016/j.ejmech.2016.07.029
	3247	3443	40	None	8511	2	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay	ChEMBL	352	5	1	4	2.7	CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O	10.1016/j.ejmech.2016.07.029
	6604889	3443	40	None	8511	2	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay	ChEMBL	352	5	1	4	2.7	CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O	10.1016/j.ejmech.2016.07.029
	CHEMBL282199	3443	40	None	8511	2	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay	ChEMBL	352	5	1	4	2.7	CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O	10.1016/j.ejmech.2016.07.029
	DB13988	3443	40	None	8511	2	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay	ChEMBL	352	5	1	4	2.7	CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O	10.1016/j.ejmech.2016.07.029
	3233	3443	40	None	8511	2	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay	ChEMBL	352	5	1	4	2.7	CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O	10.1016/j.ejmech.2016.07.029
	3247	3443	40	None	8511	2	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay	ChEMBL	352	5	1	4	2.7	CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O	10.1016/j.ejmech.2016.07.029
	6604889	3443	40	None	8511	2	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay	ChEMBL	352	5	1	4	2.7	CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O	10.1016/j.ejmech.2016.07.029
	CHEMBL282199	3443	40	None	8511	2	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay	ChEMBL	352	5	1	4	2.7	CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O	10.1016/j.ejmech.2016.07.029
	DB13988	3443	40	None	8511	2	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay	ChEMBL	352	5	1	4	2.7	CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O	10.1016/j.ejmech.2016.07.029
	2470	3583	46	None	-5128	11	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell preincubated for 30 mins followed by incubation with agonist for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysisAntagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell preincubated for 30 mins followed by incubation with agonist for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysis	ChEMBL	395	6	1	4	3.2	Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1016/j.bmc.2020.115578
	3300	3583	46	None	-5128	11	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell preincubated for 30 mins followed by incubation with agonist for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysisAntagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell preincubated for 30 mins followed by incubation with agonist for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysis	ChEMBL	395	6	1	4	3.2	Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1016/j.bmc.2020.115578
	5265	3583	46	None	-5128	11	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell preincubated for 30 mins followed by incubation with agonist for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysisAntagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell preincubated for 30 mins followed by incubation with agonist for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysis	ChEMBL	395	6	1	4	3.2	Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1016/j.bmc.2020.115578
	99	3583	46	None	-5128	11	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell preincubated for 30 mins followed by incubation with agonist for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysisAntagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell preincubated for 30 mins followed by incubation with agonist for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysis	ChEMBL	395	6	1	4	3.2	Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1016/j.bmc.2020.115578
	CHEMBL267930	3583	46	None	-5128	11	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell preincubated for 30 mins followed by incubation with agonist for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysisAntagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell preincubated for 30 mins followed by incubation with agonist for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysis	ChEMBL	395	6	1	4	3.2	Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1016/j.bmc.2020.115578
	127028473	137732	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay	ChEMBL	451	6	2	6	1.6	CC1(c2ccc(F)cc2)NC(=O)N(CC(O)CN2CCN(c3ccccc3C#N)CC2)C1=O	10.1016/j.ejmech.2016.02.024
	CHEMBL3770639	137732	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay	ChEMBL	451	6	2	6	1.6	CC1(c2ccc(F)cc2)NC(=O)N(CC(O)CN2CCN(c3ccccc3C#N)CC2)C1=O	10.1016/j.ejmech.2016.02.024
	86288948	112116	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay	ChEMBL	456	7	2	6	1.8	COc1ccccc1N1CCN(CC(O)CN2C(=O)NC(C)(c3ccc(F)cc3)C2=O)CC1	10.1016/j.ejmech.2016.02.024
	CHEMBL3233679	112116	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay	ChEMBL	456	7	2	6	1.8	COc1ccccc1N1CCN(CC(O)CN2C(=O)NC(C)(c3ccc(F)cc3)C2=O)CC1	10.1016/j.ejmech.2016.02.024
	CHEMBL3302600	112116	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay	ChEMBL	456	7	2	6	1.8	COc1ccccc1N1CCN(CC(O)CN2C(=O)NC(C)(c3ccc(F)cc3)C2=O)CC1	10.1016/j.ejmech.2016.02.024
	71574302	85823	0	None	-4	2	Human	5.4	pIC50	=	5.4	Functional	Antagonist activity at human 5HT7 receptor expressed in HEK293 assessed as inhibition of 5HT-induced cAMP accumulationAntagonist activity at human 5HT7 receptor expressed in HEK293 assessed as inhibition of 5HT-induced cAMP accumulation	ChEMBL	492	8	1	5	4.4	O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2cccnc2c1	10.1016/j.ejmech.2012.11.042
	CHEMBL2312637	85823	0	None	-4	2	Human	5.4	pIC50	=	5.4	Functional	Antagonist activity at human 5HT7 receptor expressed in HEK293 assessed as inhibition of 5HT-induced cAMP accumulationAntagonist activity at human 5HT7 receptor expressed in HEK293 assessed as inhibition of 5HT-induced cAMP accumulation	ChEMBL	492	8	1	5	4.4	O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2cccnc2c1	10.1016/j.ejmech.2012.11.042
	142601323	185249	0	None	-	1	Human	5.4	pIC50	=	5.4	Functional	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	185249	0	None	-	1	Human	5.4	pIC50	=	5.4	Functional	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	164272	0	None	-	1	Human	5.4	pIC50	=	5.4	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay	ChEMBL	248	1	1	3	2.7	Clc1ccc(-c2noc3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	CHEMBL4218801	164272	0	None	-	1	Human	5.4	pIC50	=	5.4	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay	ChEMBL	248	1	1	3	2.7	Clc1ccc(-c2noc3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	117209971	185893	1	None	-	1	Human	5.4	pIC50	=	5.4	Functional	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	185893	1	None	-	1	Human	5.4	pIC50	=	5.4	Functional	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	164272	0	None	-	1	Human	5.4	pIC50	=	5.4	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay	ChEMBL	248	1	1	3	2.7	Clc1ccc(-c2noc3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	CHEMBL4218801	164272	0	None	-	1	Human	5.4	pIC50	=	5.4	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay	ChEMBL	248	1	1	3	2.7	Clc1ccc(-c2noc3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	142601323	185249	0	None	-	1	Human	5.4	pIC50	=	5.4	Functional	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	185249	0	None	-	1	Human	5.4	pIC50	=	5.4	Functional	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	185893	1	None	-	1	Human	5.4	pIC50	=	5.4	Functional	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	185893	1	None	-	1	Human	5.4	pIC50	=	5.4	Functional	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	185818	1	None	-	1	Human	5.4	pIC50	=	5.4	Functional	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	185818	1	None	-	1	Human	5.4	pIC50	=	5.4	Functional	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	185818	1	None	-	1	Human	5.4	pIC50	=	5.4	Functional	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	185818	1	None	-	1	Human	5.4	pIC50	=	5.4	Functional	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	114612	0	None	1	2	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human 5-HT7 receptor expressed in CHO cells assessed as cAMP production by EIA systemAntagonist activity at human 5-HT7 receptor expressed in CHO cells assessed as cAMP production by EIA system	ChEMBL	307	1	2	2	2.1	NC(N)=NC(=O)c1ccc2c(c1)[C@@]1(CCCO1)c1ccccc1-2	10.1016/j.bmc.2014.09.005
	CHEMBL3343673	114612	0	None	1	2	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human 5-HT7 receptor expressed in CHO cells assessed as cAMP production by EIA systemAntagonist activity at human 5-HT7 receptor expressed in CHO cells assessed as cAMP production by EIA system	ChEMBL	307	1	2	2	2.1	NC(N)=NC(=O)c1ccc2c(c1)[C@@]1(CCCO1)c1ccccc1-2	10.1016/j.bmc.2014.09.005
	22001618	81387	6	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at human 5HT7A receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation by ELISAAntagonist activity at human 5HT7A receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation by ELISA	ChEMBL	268	3	1	3	2.8	COc1ccc(-c2ccccc2N2CCNCC2)cc1	10.1021/jm3003679
	CHEMBL2164336	81387	6	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at human 5HT7A receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation by ELISAAntagonist activity at human 5HT7A receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation by ELISA	ChEMBL	268	3	1	3	2.8	COc1ccc(-c2ccccc2N2CCNCC2)cc1	10.1021/jm3003679
	59511191	184931	3	None	-	1	Human	5.3	pIC50	=	5.3	Functional	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	184931	3	None	-	1	Human	5.3	pIC50	=	5.3	Functional	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	184931	3	None	-	1	Human	5.3	pIC50	=	5.3	Functional	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	184931	3	None	-	1	Human	5.3	pIC50	=	5.3	Functional	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	186993	23	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human 5HT7A receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation by ELISAAntagonist activity at human 5HT7A receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation by ELISA	ChEMBL	238	2	1	2	2.8	c1ccc(-c2ccccc2N2CCNCC2)cc1	10.1021/jm3003679
	CHEMBL494675	186993	23	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human 5HT7A receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation by ELISAAntagonist activity at human 5HT7A receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation by ELISA	ChEMBL	238	2	1	2	2.8	c1ccc(-c2ccccc2N2CCNCC2)cc1	10.1021/jm3003679
	90656694	110493	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	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	110493	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	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	185737	1	None	-	1	Human	5.3	pIC50	=	5.3	Functional	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	185737	1	None	-	1	Human	5.3	pIC50	=	5.3	Functional	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	185737	1	None	-	1	Human	5.3	pIC50	=	5.3	Functional	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	185737	1	None	-	1	Human	5.3	pIC50	=	5.3	Functional	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	152184	0	None	-	1	Human	5.3	pIC50	=	5.3	Functional	Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay	ChEMBL	418	7	0	5	4.7	COc1ccccc1-c1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OC	10.1016/j.ejmech.2016.07.029
	CHEMBL3973160	152184	0	None	-	1	Human	5.3	pIC50	=	5.3	Functional	Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay	ChEMBL	418	7	0	5	4.7	COc1ccccc1-c1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OC	10.1016/j.ejmech.2016.07.029
	71574306	85825	0	None	2	2	Human	5.3	pIC50	=	5.3	Functional	Antagonist activity at human 5HT7 receptor expressed in HEK293 assessed as inhibition of 5HT-induced cAMP accumulationAntagonist activity at human 5HT7 receptor expressed in HEK293 assessed as inhibition of 5HT-induced cAMP accumulation	ChEMBL	492	8	1	5	4.4	O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2cn1	10.1016/j.ejmech.2012.11.042
	CHEMBL2312639	85825	0	None	2	2	Human	5.3	pIC50	=	5.3	Functional	Antagonist activity at human 5HT7 receptor expressed in HEK293 assessed as inhibition of 5HT-induced cAMP accumulationAntagonist activity at human 5HT7 receptor expressed in HEK293 assessed as inhibition of 5HT-induced cAMP accumulation	ChEMBL	492	8	1	5	4.4	O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2cn1	10.1016/j.ejmech.2012.11.042
	134154531	152184	0	None	-	1	Human	5.3	pIC50	=	5.3	Functional	Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay	ChEMBL	418	7	0	5	4.7	COc1ccccc1-c1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OC	10.1016/j.ejmech.2016.07.029
	CHEMBL3973160	152184	0	None	-	1	Human	5.3	pIC50	=	5.3	Functional	Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay	ChEMBL	418	7	0	5	4.7	COc1ccccc1-c1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OC	10.1016/j.ejmech.2016.07.029
	145947560	167136	0	None	-19	4	Human	5.2	pIC50	=	5.2	Functional	Antagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assayAntagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assay	ChEMBL	344	6	0	3	4.2	Cc1cc(OCCCN2CCN(c3ccccc3)CC2)ccc1Cl	10.1016/j.bmcl.2018.04.059
	CHEMBL4212812	167136	0	None	-19	4	Human	5.2	pIC50	=	5.2	Functional	Antagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assayAntagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assay	ChEMBL	344	6	0	3	4.2	Cc1cc(OCCCN2CCN(c3ccccc3)CC2)ccc1Cl	10.1016/j.bmcl.2018.04.059
	CHEMBL4302457	167136	0	None	-19	4	Human	5.2	pIC50	=	5.2	Functional	Antagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assayAntagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assay	ChEMBL	344	6	0	3	4.2	Cc1cc(OCCCN2CCN(c3ccccc3)CC2)ccc1Cl	10.1016/j.bmcl.2018.04.059
	11694810	120015	0	None	-1	2	Human	7.2	pIC50	=	7.2	Functional	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	120015	0	None	-1	2	Human	7.2	pIC50	=	7.2	Functional	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	120015	0	None	-1	2	Human	7.2	pIC50	=	7.2	Functional	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	137622	0	None	-	1	Human	5.2	pIC50	=	5.2	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay	ChEMBL	456	7	2	6	1.8	COc1cccc(N2CCN(CC(O)CN3C(=O)NC(C)(c4ccc(F)cc4)C3=O)CC2)c1	10.1016/j.ejmech.2016.02.024
	CHEMBL3769441	137622	0	None	-	1	Human	5.2	pIC50	=	5.2	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay	ChEMBL	456	7	2	6	1.8	COc1cccc(N2CCN(CC(O)CN3C(=O)NC(C)(c4ccc(F)cc4)C3=O)CC2)c1	10.1016/j.ejmech.2016.02.024
	142601325	185277	0	None	-	1	Human	5.2	pIC50	=	5.2	Functional	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	185277	0	None	-	1	Human	5.2	pIC50	=	5.2	Functional	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	185277	0	None	-	1	Human	5.2	pIC50	=	5.2	Functional	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	185277	0	None	-	1	Human	5.2	pIC50	=	5.2	Functional	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	185542	1	None	-	1	Human	5.2	pIC50	=	5.2	Functional	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	185542	1	None	-	1	Human	5.2	pIC50	=	5.2	Functional	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	142148	0	None	-	1	Human	5.2	pIC50	=	5.2	Functional	Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay	ChEMBL	402	6	0	4	5.0	COc1ccccc1-c1cc(CN2CCN(c3ccccc3OC)CC2)ccc1C	10.1016/j.ejmech.2016.07.029
	CHEMBL3892079	142148	0	None	-	1	Human	5.2	pIC50	=	5.2	Functional	Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay	ChEMBL	402	6	0	4	5.0	COc1ccccc1-c1cc(CN2CCN(c3ccccc3OC)CC2)ccc1C	10.1016/j.ejmech.2016.07.029
	134137104	142148	0	None	-	1	Human	5.2	pIC50	=	5.2	Functional	Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay	ChEMBL	402	6	0	4	5.0	COc1ccccc1-c1cc(CN2CCN(c3ccccc3OC)CC2)ccc1C	10.1016/j.ejmech.2016.07.029
	CHEMBL3892079	142148	0	None	-	1	Human	5.2	pIC50	=	5.2	Functional	Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assayAntagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay	ChEMBL	402	6	0	4	5.0	COc1ccccc1-c1cc(CN2CCN(c3ccccc3OC)CC2)ccc1C	10.1016/j.ejmech.2016.07.029
	117209964	185542	1	None	-	1	Human	5.2	pIC50	=	5.2	Functional	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	185542	1	None	-	1	Human	5.2	pIC50	=	5.2	Functional	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	168942	0	None	1	2	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at 5HT7R receptor (unknown origin) assessed as forskolin-mediated cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by TR-FRET analysisAntagonist activity at 5HT7R receptor (unknown origin) assessed as forskolin-mediated cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by TR-FRET analysis	ChEMBL	430	6	1	1	6.9	Fc1ccc(C2CCN(CCCc3c[nH]c4ccc(F)cc34)CC2)c(-c2ccccc2)c1	10.1016/j.bmcl.2019.126703
	CHEMBL4434876	168942	0	None	1	2	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at 5HT7R receptor (unknown origin) assessed as forskolin-mediated cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by TR-FRET analysisAntagonist activity at 5HT7R receptor (unknown origin) assessed as forskolin-mediated cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by TR-FRET analysis	ChEMBL	430	6	1	1	6.9	Fc1ccc(C2CCN(CCCc3c[nH]c4ccc(F)cc34)CC2)c(-c2ccccc2)c1	10.1016/j.bmcl.2019.126703
	142601329	185925	3	None	-	1	Human	6.2	pIC50	=	6.2	Functional	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	185925	3	None	-	1	Human	6.2	pIC50	=	6.2	Functional	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	185925	3	None	-	1	Human	6.2	pIC50	=	6.2	Functional	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	185925	3	None	-	1	Human	6.2	pIC50	=	6.2	Functional	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	163506	7	None	-	1	Human	5.2	pIC50	=	5.2	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay	ChEMBL	231	1	2	2	1.9	Fc1ccc(-c2n[nH]c3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	CHEMBL4209274	163506	7	None	-	1	Human	5.2	pIC50	=	5.2	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay	ChEMBL	231	1	2	2	1.9	Fc1ccc(-c2n[nH]c3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	124247485	163506	7	None	-	1	Human	5.2	pIC50	=	5.2	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay	ChEMBL	231	1	2	2	1.9	Fc1ccc(-c2n[nH]c3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	CHEMBL4209274	163506	7	None	-	1	Human	5.2	pIC50	=	5.2	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay	ChEMBL	231	1	2	2	1.9	Fc1ccc(-c2n[nH]c3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	142601337	185378	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	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	185378	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	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	185378	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	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	185378	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	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	185829	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	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	185829	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	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	185829	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	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	185829	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	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	163405	2	None	-	1	Human	5.1	pIC50	=	5.1	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay	ChEMBL	247	1	2	2	2.4	Clc1ccc(-c2n[nH]c3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	CHEMBL4207884	163405	2	None	-	1	Human	5.1	pIC50	=	5.1	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay	ChEMBL	247	1	2	2	2.4	Clc1ccc(-c2n[nH]c3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	67268994	163405	2	None	-	1	Human	5.1	pIC50	=	5.1	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay	ChEMBL	247	1	2	2	2.4	Clc1ccc(-c2n[nH]c3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	CHEMBL4207884	163405	2	None	-	1	Human	5.1	pIC50	=	5.1	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay	ChEMBL	247	1	2	2	2.4	Clc1ccc(-c2n[nH]c3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	71574212	85843	0	None	-4	2	Human	5.1	pIC50	=	5.1	Functional	Antagonist activity at human 5HT7 receptor expressed in HEK293 assessed as inhibition of 5HT-induced cAMP accumulationAntagonist activity at human 5HT7 receptor expressed in HEK293 assessed as inhibition of 5HT-induced cAMP accumulation	ChEMBL	492	8	1	5	4.4	O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cnc2ccccc2c1	10.1016/j.ejmech.2012.11.042
	CHEMBL2312935	85843	0	None	-4	2	Human	5.1	pIC50	=	5.1	Functional	Antagonist activity at human 5HT7 receptor expressed in HEK293 assessed as inhibition of 5HT-induced cAMP accumulationAntagonist activity at human 5HT7 receptor expressed in HEK293 assessed as inhibition of 5HT-induced cAMP accumulation	ChEMBL	492	8	1	5	4.4	O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cnc2ccccc2c1	10.1016/j.ejmech.2012.11.042
	127028472	137630	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay	ChEMBL	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	137630	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay	ChEMBL	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	85826	0	None	18	2	Human	6.1	pIC50	=	6.1	Functional	Antagonist activity at human 5HT7 receptor expressed in HEK293 assessed as inhibition of 5HT-induced cAMP accumulationAntagonist activity at human 5HT7 receptor expressed in HEK293 assessed as inhibition of 5HT-induced cAMP accumulation	ChEMBL	492	8	1	5	4.4	O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cncc2ccccc12	10.1016/j.ejmech.2012.11.042
	CHEMBL2312640	85826	0	None	18	2	Human	6.1	pIC50	=	6.1	Functional	Antagonist activity at human 5HT7 receptor expressed in HEK293 assessed as inhibition of 5HT-induced cAMP accumulationAntagonist activity at human 5HT7 receptor expressed in HEK293 assessed as inhibition of 5HT-induced cAMP accumulation	ChEMBL	492	8	1	5	4.4	O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cncc2ccccc12	10.1016/j.ejmech.2012.11.042
	135367857	164041	0	None	-	1	Human	6.1	pIC50	=	6.1	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay	ChEMBL	228	1	1	3	2.3	Cc1ccc(-c2noc3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	CHEMBL4215875	164041	0	None	-	1	Human	6.1	pIC50	=	6.1	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay	ChEMBL	228	1	1	3	2.3	Cc1ccc(-c2noc3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	135367857	164041	0	None	-	1	Human	6.1	pIC50	=	6.1	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay	ChEMBL	228	1	1	3	2.3	Cc1ccc(-c2noc3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	CHEMBL4215875	164041	0	None	-	1	Human	6.1	pIC50	=	6.1	Functional	Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assayAntagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay	ChEMBL	228	1	1	3	2.3	Cc1ccc(-c2noc3c2CCNCC3)cc1	10.1021/acs.jmedchem.8b00642
	117209864	185442	1	None	-	1	Human	5.1	pIC50	=	5.1	Functional	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	185442	1	None	-	1	Human	5.1	pIC50	=	5.1	Functional	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	185442	1	None	-	1	Human	5.1	pIC50	=	5.1	Functional	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	185442	1	None	-	1	Human	5.1	pIC50	=	5.1	Functional	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	184655	1	None	-	1	Human	6.1	pIC50	=	6.1	Functional	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	184655	1	None	-	1	Human	6.1	pIC50	=	6.1	Functional	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	184780	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	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	184780	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	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	184655	1	None	-	1	Human	6.1	pIC50	=	6.1	Functional	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	184655	1	None	-	1	Human	6.1	pIC50	=	6.1	Functional	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	184780	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	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	184780	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	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	183961	1	None	-	1	Human	6.0	pIC50	=	6.0	Functional	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	183961	1	None	-	1	Human	6.0	pIC50	=	6.0	Functional	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	183961	1	None	-	1	Human	6.0	pIC50	=	6.0	Functional	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	183961	1	None	-	1	Human	6.0	pIC50	=	6.0	Functional	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	3443	40	None	-	2	Guinea pig	8.0	pKd	=	8.0	Functional	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	3443	40	None	-	2	Guinea pig	8.0	pKd	=	8.0	Functional	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	3443	40	None	-	2	Guinea pig	8.0	pKd	=	8.0	Functional	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	3443	40	None	-	2	Guinea pig	8.0	pKd	=	8.0	Functional	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	3443	40	None	-	2	Guinea pig	8.0	pKd	=	8.0	Functional	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	3443	40	None	-	2	Guinea pig	7.9	pKd	=	7.9	Functional	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	3443	40	None	-	2	Guinea pig	7.9	pKd	=	7.9	Functional	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	3443	40	None	-	2	Guinea pig	7.9	pKd	=	7.9	Functional	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	3443	40	None	-	2	Guinea pig	7.9	pKd	=	7.9	Functional	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	3443	40	None	-	2	Guinea pig	7.9	pKd	=	7.9	Functional	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	3443	40	None	-	2	Guinea pig	7.8	pKd	=	7.8	Functional	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	3443	40	None	-	2	Guinea pig	7.8	pKd	=	7.8	Functional	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	3443	40	None	-	2	Guinea pig	7.8	pKd	=	7.8	Functional	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	3443	40	None	-	2	Guinea pig	7.8	pKd	=	7.8	Functional	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	3443	40	None	-	2	Guinea pig	7.8	pKd	=	7.8	Functional	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	3443	40	None	-	2	Guinea pig	7.8	pKd	=	7.8	Functional	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	3443	40	None	-	2	Guinea pig	7.8	pKd	=	7.8	Functional	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	3443	40	None	-	2	Guinea pig	7.8	pKd	=	7.8	Functional	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	3443	40	None	-	2	Guinea pig	7.8	pKd	=	7.8	Functional	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	3443	40	None	-	2	Guinea pig	7.8	pKd	=	7.8	Functional	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	3443	40	None	-	2	Guinea pig	7.8	pKd	=	7.8	Functional	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	3443	40	None	-	2	Guinea pig	7.8	pKd	=	7.8	Functional	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	3443	40	None	-	2	Guinea pig	7.8	pKd	=	7.8	Functional	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	3443	40	None	-	2	Guinea pig	7.8	pKd	=	7.8	Functional	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	3443	40	None	-	2	Guinea pig	7.8	pKd	=	7.8	Functional	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	92561	0	None	-	0	Guinea pig	7.7	pKd	=	7.7	Functional	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	92561	0	None	-	0	Guinea pig	7.7	pKd	=	7.7	Functional	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	3443	40	None	-	2	Guinea pig	7.7	pKd	=	7.7	Functional	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	3443	40	None	-	2	Guinea pig	7.7	pKd	=	7.7	Functional	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	3443	40	None	-	2	Guinea pig	7.7	pKd	=	7.7	Functional	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	3443	40	None	-	2	Guinea pig	7.7	pKd	=	7.7	Functional	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	3443	40	None	-	2	Guinea pig	7.7	pKd	=	7.7	Functional	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	3443	40	None	-	2	Guinea pig	8.4	pKd	=	8.4	Functional	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	3443	40	None	-	2	Guinea pig	8.4	pKd	=	8.4	Functional	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	3443	40	None	-	2	Guinea pig	8.4	pKd	=	8.4	Functional	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	3443	40	None	-	2	Guinea pig	8.4	pKd	=	8.4	Functional	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	3443	40	None	-	2	Guinea pig	8.4	pKd	=	8.4	Functional	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	3443	40	None	-	2	Guinea pig	7.5	pKd	=	7.5	Functional	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	3443	40	None	-	2	Guinea pig	7.5	pKd	=	7.5	Functional	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	3443	40	None	-	2	Guinea pig	7.5	pKd	=	7.5	Functional	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	3443	40	None	-	2	Guinea pig	7.5	pKd	=	7.5	Functional	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	3443	40	None	-	2	Guinea pig	7.5	pKd	=	7.5	Functional	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	3443	40	None	-	2	Guinea pig	7.5	pKd	=	7.5	Functional	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	3443	40	None	-	2	Guinea pig	7.5	pKd	=	7.5	Functional	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	3443	40	None	-	2	Guinea pig	7.5	pKd	=	7.5	Functional	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	3443	40	None	-	2	Guinea pig	7.5	pKd	=	7.5	Functional	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	3443	40	None	-	2	Guinea pig	7.5	pKd	=	7.5	Functional	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	3443	40	None	-	2	Guinea pig	8.2	pKd	=	8.2	Functional	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	3443	40	None	-	2	Guinea pig	8.2	pKd	=	8.2	Functional	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	3443	40	None	-	2	Guinea pig	8.2	pKd	=	8.2	Functional	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	3443	40	None	-	2	Guinea pig	8.2	pKd	=	8.2	Functional	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	3443	40	None	-	2	Guinea pig	8.2	pKd	=	8.2	Functional	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	3443	40	None	-	2	Guinea pig	8.1	pKd	=	8.1	Functional	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	3443	40	None	-	2	Guinea pig	8.1	pKd	=	8.1	Functional	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	3443	40	None	-	2	Guinea pig	8.1	pKd	=	8.1	Functional	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	3443	40	None	-	2	Guinea pig	8.1	pKd	=	8.1	Functional	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	3443	40	None	-	2	Guinea pig	8.1	pKd	=	8.1	Functional	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	3443	40	None	-	2	Guinea pig	8.1	pKd	=	8.1	Functional	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	3443	40	None	-	2	Guinea pig	8.1	pKd	=	8.1	Functional	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	3443	40	None	-	2	Guinea pig	8.1	pKd	=	8.1	Functional	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	3443	40	None	-	2	Guinea pig	8.1	pKd	=	8.1	Functional	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	3443	40	None	-	2	Guinea pig	8.1	pKd	=	8.1	Functional	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	117676	0	None	-	0	Human	7.7	pKi	=	7.7	Functional	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	117676	0	None	-	0	Human	7.7	pKi	=	7.7	Functional	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	3933	85	None	-	3	Human	6.4	pKi	=	6.4	Functional	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	3933	85	None	-	3	Human	6.4	pKi	=	6.4	Functional	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	3933	85	None	-	3	Human	6.4	pKi	=	6.4	Functional	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	3933	85	None	-	3	Human	6.4	pKi	=	6.4	Functional	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	3933	85	None	-	3	Human	6.4	pKi	=	6.4	Functional	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	117672	0	None	-	0	Human	8.2	pKi	=	8.2	Functional	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	117672	0	None	-	0	Human	8.2	pKi	=	8.2	Functional	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	117676	0	None	-	0	Human	7.0	pKi	=	7.0	Functional	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	117676	0	None	-	0	Human	7.0	pKi	=	7.0	Functional	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	117672	0	None	-	0	Human	7.0	pKi	=	7.0	Functional	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	117672	0	None	-	0	Human	7.0	pKi	=	7.0	Functional	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	929	39	None	-1	18	Human	8.2	pEC50	=	8.2	Functional	NoneNone	Drug Central	465	9	2	6	3.4	COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N	None
	2769	929	39	None	-1	18	Human	8.2	pEC50	=	8.2	Functional	NoneNone	Drug Central	465	9	2	6	3.4	COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N	None
	44279790	929	39	None	-1	18	Human	8.2	pEC50	=	8.2	Functional	NoneNone	Drug Central	465	9	2	6	3.4	COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N	None
	660	929	39	None	-1	18	Human	8.2	pEC50	=	8.2	Functional	NoneNone	Drug Central	465	9	2	6	3.4	COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N	None
	CHEMBL1729	929	39	None	-1	18	Human	8.2	pEC50	=	8.2	Functional	NoneNone	Drug Central	465	9	2	6	3.4	COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N	None
	CHEMBL560739	929	39	None	-1	18	Human	8.2	pEC50	=	8.2	Functional	NoneNone	Drug Central	465	9	2	6	3.4	COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N	None
	DB00604	929	39	None	-1	18	Human	8.2	pEC50	=	8.2	Functional	NoneNone	Drug Central	465	9	2	6	3.4	COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N	None
	4223	3917	88	None	-562	16	Rat	8.3	pIC50	=	8.3	Functional	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	3917	88	None	-562	16	Rat	8.3	pIC50	=	8.3	Functional	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	3917	88	None	-562	16	Rat	8.3	pIC50	=	8.3	Functional	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	3917	88	None	-562	16	Rat	8.3	pIC50	=	8.3	Functional	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	3917	88	None	-562	16	Rat	8.3	pIC50	=	8.3	Functional	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					Receptor			Assay information							Chemical information
Sel. page	Common name	GPCRdb ID	#Vendors	Reference ligand	Fold selectivity (Affinity)	# tested GPCRs (Affinity)	Species	p-value (-log)	Type	Activity Relation	Activity Value	Assay Type	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI
	4106	2456	16	None	-4	34	Human	9.2	pEC50	=	9.2	Binding	Displacement of [3H]lysergic acid from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]lysergic acid from human recombinant 5HT7 receptor expressed in CHO cells	ChEMBL	356	2	0	4	4.4	CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C	10.1021/np058114h
	5358812	2456	16	None	-4	34	Human	9.2	pEC50	=	9.2	Binding	Displacement of [3H]lysergic acid from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]lysergic acid from human recombinant 5HT7 receptor expressed in CHO cells	ChEMBL	356	2	0	4	4.4	CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C	10.1021/np058114h
	89	2456	16	None	-4	34	Human	9.2	pEC50	=	9.2	Binding	Displacement of [3H]lysergic acid from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]lysergic acid from human recombinant 5HT7 receptor expressed in CHO cells	ChEMBL	356	2	0	4	4.4	CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C	10.1021/np058114h
	CHEMBL93240	2456	16	None	-4	34	Human	9.2	pEC50	=	9.2	Binding	Displacement of [3H]lysergic acid from human recombinant 5HT7 receptor expressed in CHO cellsDisplacement of [3H]lysergic acid from human recombinant 5HT7 receptor expressed in CHO cells	ChEMBL	356	2	0	4	4.4	CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C	10.1021/np058114h
	5	139	66	None	-3	55	Human	8.3	pEC50	=	8.3	Binding	Agonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells by LANCE TR-FRET assayAgonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells by LANCE TR-FRET assay	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1016/j.bmc.2019.07.046
	5202	139	66	None	-3	55	Human	8.3	pEC50	=	8.3	Binding	Agonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells by LANCE TR-FRET assayAgonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells by LANCE TR-FRET assay	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1016/j.bmc.2019.07.046
	CHEMBL39	139	66	None	-3	55	Human	8.3	pEC50	=	8.3	Binding	Agonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells by LANCE TR-FRET assayAgonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells by LANCE TR-FRET assay	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1016/j.bmc.2019.07.046
	DB08839	139	66	None	-3	55	Human	8.3	pEC50	=	8.3	Binding	Agonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells by LANCE TR-FRET assayAgonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells by LANCE TR-FRET assay	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1016/j.bmc.2019.07.046
	5	139	66	None	-3	55	Human	8.2	pEC50	=	8.2	Binding	Agonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells by LANCE TR-FRET assayAgonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells by LANCE TR-FRET assay	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1016/j.bmc.2019.07.046
	5202	139	66	None	-3	55	Human	8.2	pEC50	=	8.2	Binding	Agonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells by LANCE TR-FRET assayAgonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells by LANCE TR-FRET assay	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1016/j.bmc.2019.07.046
	CHEMBL39	139	66	None	-3	55	Human	8.2	pEC50	=	8.2	Binding	Agonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells by LANCE TR-FRET assayAgonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells by LANCE TR-FRET assay	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1016/j.bmc.2019.07.046
	DB08839	139	66	None	-3	55	Human	8.2	pEC50	=	8.2	Binding	Agonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells by LANCE TR-FRET assayAgonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells by LANCE TR-FRET assay	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1016/j.bmc.2019.07.046
	5	139	66	None	-3	55	Human	9.6	pIC50	=	9.6	Binding	Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO cells	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1016/j.bmc.2016.03.006
	5202	139	66	None	-3	55	Human	9.6	pIC50	=	9.6	Binding	Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO cells	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1016/j.bmc.2016.03.006
	CHEMBL39	139	66	None	-3	55	Human	9.6	pIC50	=	9.6	Binding	Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO cells	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1016/j.bmc.2016.03.006
	DB08839	139	66	None	-3	55	Human	9.6	pIC50	=	9.6	Binding	Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in CHO cells	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1016/j.bmc.2016.03.006
	5	139	66	None	-3	55	Human	9.6	pIC50	=	9.6	Binding	Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells measured after 120 mins by scintillation counting method	ChEMBL	176	2	3	2	1.4	NCCc1c[nH]c2c1cc(O)cc2	10.1016/j.bmc.2016.11.014
	5202	139	66	None	-3

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Ligand source activities (1 row/activity)