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Ligand source activities (1 row/activity)

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Ligands (move mouse cursor over ligand name to see structure)					Receptor		Activity									Chemical information
Sel. page	Common name No matches found	GPCRdb ID No matches found	Reference ligand No matches found	Vendors	Species No matches found		Assay Type No matches found	Activity Type No matches found	Activity Relation No matches found	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description No matches found	Source No matches found	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles No matches found	DOI No matches found

Ligands (move mouse cursor over ligand name to see structure)					Receptor	Activity									Chemical information
Sel. page	Common name No matches found	GPCRdb ID No matches found	Reference ligand No matches found	Vendors	Species No matches found	Assay Type No matches found	Activity Type No matches found	Activity Relation No matches found	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description No matches found	Source No matches found	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles No matches found	DOI No matches found
	138697637	184872	None	0	Human	Functional	pEC50	=	11	11.0	3	2	Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	551	10	1	10	4.2	CCCCc1nc(=O)c(S(=O)(=O)c2ccc(-c3cccnc3OC)cc2)c(O)n1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325
	CHEMBL4851100	184872	None	0	Human	Functional	pEC50	=	11	11.0	3	2	Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	551	10	1	10	4.2	CCCCc1nc(=O)c(S(=O)(=O)c2ccc(-c3cccnc3OC)cc2)c(O)n1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325
	138697719	186661	None	0	Human	Functional	pEC50	=	11	11.0	3	2	Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	555	9	1	10	3.9	COc1cccc(OC)c1-n1c(COC(C)C)nc(=O)c(S(=O)(=O)c2ccc(-c3ccc(F)nc3)cc2)c1O	10.1016/j.bmcl.2021.128325
	CHEMBL4878056	186661	None	0	Human	Functional	pEC50	=	11	11.0	3	2	Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	555	9	1	10	3.9	COc1cccc(OC)c1-n1c(COC(C)C)nc(=O)c(S(=O)(=O)c2ccc(-c3ccc(F)nc3)cc2)c1O	10.1016/j.bmcl.2021.128325
	25085173	213673	None	24	Human	Functional	pEC50	=	10.9	10.9	-	1	Agonist activity at APJ receptor in HEK293 cells assessed as inhibition of forskolin-induced cAMP level incubated for 5 mins prior to forskolin challenge measured after 30 mins by TR-FRET assayAgonist activity at APJ receptor in HEK293 cells assessed as inhibition of forskolin-induced cAMP level incubated for 5 mins prior to forskolin challenge measured after 30 mins by TR-FRET assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O	10.1016/j.bmcl.2014.08.045
	CHEMBL3184840	213673	None	24	Human	Functional	pEC50	=	10.9	10.9	-	1	Agonist activity at APJ receptor in HEK293 cells assessed as inhibition of forskolin-induced cAMP level incubated for 5 mins prior to forskolin challenge measured after 30 mins by TR-FRET assayAgonist activity at APJ receptor in HEK293 cells assessed as inhibition of forskolin-induced cAMP level incubated for 5 mins prior to forskolin challenge measured after 30 mins by TR-FRET assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O	10.1016/j.bmcl.2014.08.045
	168274433	190244	None	0	Human	Functional	pEC50	=	10.7	10.7	-	1	Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis	ChEMBL	519	6	1	9	3.1	COc1cccc(OC)c1-n1c(-c2ccn(C)n2)nc(=O)c(C(=O)N2CC[C@H](c3ccccc3F)C2)c1O	10.1021/acs.jmedchem.1c01504
	CHEMBL5173464	190244	None	0	Human	Functional	pEC50	=	10.7	10.7	-	1	Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis	ChEMBL	519	6	1	9	3.1	COc1cccc(OC)c1-n1c(-c2ccn(C)n2)nc(=O)c(C(=O)N2CC[C@H](c3ccccc3F)C2)c1O	10.1021/acs.jmedchem.1c01504
	137197922	191471	None	0	Human	Functional	pEC50	=	10.7	10.7	-	1	Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis	ChEMBL	537	6	1	9	3.3	COc1cccc(OC)c1-n1c(-c2cnn(C)c2)nc(=O)c(C(=O)N2CCC(c3ccc(F)cc3F)C2)c1O	10.1021/acs.jmedchem.1c01504
	CHEMBL5192130	191471	None	0	Human	Functional	pEC50	=	10.7	10.7	-	1	Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis	ChEMBL	537	6	1	9	3.3	COc1cccc(OC)c1-n1c(-c2cnn(C)c2)nc(=O)c(C(=O)N2CCC(c3ccc(F)cc3F)C2)c1O	10.1021/acs.jmedchem.1c01504
	137198123	191558	None	0	Human	Functional	pEC50	=	10.7	10.7	-	1	Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis	ChEMBL	533	6	1	7	4.4	CCc1cccc(CC)c1-n1c(-c2ccn(C)n2)nc(=O)c(C(=O)N2CCC(c3c(F)cccc3F)C2)c1O	10.1021/acs.jmedchem.1c01504
	CHEMBL5193130	191558	None	0	Human	Functional	pEC50	=	10.7	10.7	-	1	Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis	ChEMBL	533	6	1	7	4.4	CCc1cccc(CC)c1-n1c(-c2ccn(C)n2)nc(=O)c(C(=O)N2CCC(c3c(F)cccc3F)C2)c1O	10.1021/acs.jmedchem.1c01504
	168293355	192177	None	0	Human	Functional	pEC50	=	10.7	10.7	-	1	Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis	ChEMBL	534	6	1	8	3.8	CCc1cccc(CC)c1-n1c(-c2ccn(C)n2)nc(=O)c(C(=O)N2CC[C@@H](c3ncc(F)cc3F)C2)c1O	10.1021/acs.jmedchem.1c01504
	CHEMBL5202635	192177	None	0	Human	Functional	pEC50	=	10.7	10.7	-	1	Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis	ChEMBL	534	6	1	8	3.8	CCc1cccc(CC)c1-n1c(-c2ccn(C)n2)nc(=O)c(C(=O)N2CC[C@@H](c3ncc(F)cc3F)C2)c1O	10.1021/acs.jmedchem.1c01504
	137198148	192369	None	0	Human	Functional	pEC50	=	10.7	10.7	-	1	Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis	ChEMBL	515	8	1	8	3.4	CCOCc1nc(=O)c(C(=O)N2CCC(c3ccc(F)cc3F)C2)c(O)n1-c1c(OC)cccc1OC	10.1021/acs.jmedchem.1c01504
	CHEMBL5205562	192369	None	0	Human	Functional	pEC50	=	10.7	10.7	-	1	Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis	ChEMBL	515	8	1	8	3.4	CCOCc1nc(=O)c(C(=O)N2CCC(c3ccc(F)cc3F)C2)c(O)n1-c1c(OC)cccc1OC	10.1021/acs.jmedchem.1c01504
	137198156	192529	None	0	Human	Functional	pEC50	=	10.7	10.7	-	1	Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis	ChEMBL	537	6	1	9	3.3	COc1cccc(OC)c1-n1c(-c2ccn(C)n2)nc(=O)c(C(=O)N2CCC(c3ccc(F)cc3F)C2)c1O	10.1021/acs.jmedchem.1c01504
	CHEMBL5208127	192529	None	0	Human	Functional	pEC50	=	10.7	10.7	-	1	Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis	ChEMBL	537	6	1	9	3.3	COc1cccc(OC)c1-n1c(-c2ccn(C)n2)nc(=O)c(C(=O)N2CCC(c3ccc(F)cc3F)C2)c1O	10.1021/acs.jmedchem.1c01504
	137250580	185753	None	0	Human	Functional	pEC50	=	10.7	10.7	1	2	Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	484	9	1	8	4.0	CCCCc1nc(=O)c(S(=O)(=O)c2ccc(C3CC3)cc2)c(O)n1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325
	CHEMBL4864542	185753	None	0	Human	Functional	pEC50	=	10.7	10.7	1	2	Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	484	9	1	8	4.0	CCCCc1nc(=O)c(S(=O)(=O)c2ccc(C3CC3)cc2)c(O)n1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325
	138697675	186259	None	0	Human	Functional	pEC50	=	10.7	10.7	1	2	Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	537	9	1	10	3.3	CCCCc1nc(=O)c(S(=O)(=O)c2ccc(-n3ccccc3=O)cc2)c(O)n1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325
	CHEMBL4872345	186259	None	0	Human	Functional	pEC50	=	10.7	10.7	1	2	Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	537	9	1	10	3.3	CCCCc1nc(=O)c(S(=O)(=O)c2ccc(-n3ccccc3=O)cc2)c(O)n1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325
	11838	687	None	16	Human	Functional	pEC50	=	10.6	10.6	-15	2	Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	498	9	2	9	4.0	CCOCc1c(c(c(c(=O)[nH]1)c1nnc(o1)Cc1ncc(cc1)Cl)O)c1c(cccc1OC)OC	10.1016/j.bmcl.2021.128325
	137106310	687	None	16	Human	Functional	pEC50	=	10.6	10.6	-15	2	Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	498	9	2	9	4.0	CCOCc1c(c(c(c(=O)[nH]1)c1nnc(o1)Cc1ncc(cc1)Cl)O)c1c(cccc1OC)OC	10.1016/j.bmcl.2021.128325
	CHEMBL4873876	687	None	16	Human	Functional	pEC50	=	10.6	10.6	-15	2	Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	498	9	2	9	4.0	CCOCc1c(c(c(c(=O)[nH]1)c1nnc(o1)Cc1ncc(cc1)Cl)O)c1c(cccc1OC)OC	10.1016/j.bmcl.2021.128325
	164619102	185570	None	0	Human	Functional	pEC50	=	10.6	10.6	-	1	Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay	ChEMBL	478	9	2	9	3.6	CCOCc1[nH]c(=O)c(-c2nnc(Cc3ccc(C)cn3)o2)c(O)c1-c1c(OC)cccc1OC	10.1021/acsmedchemlett.1c00385
	CHEMBL4861895	185570	None	0	Human	Functional	pEC50	=	10.6	10.6	-	1	Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay	ChEMBL	478	9	2	9	3.6	CCOCc1[nH]c(=O)c(-c2nnc(Cc3ccc(C)cn3)o2)c(O)c1-c1c(OC)cccc1OC	10.1021/acsmedchemlett.1c00385
	11838	687	None	16	Human	Functional	pEC50	=	10.6	10.6	-15	2	Agonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assayAgonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assay	ChEMBL	498	9	2	9	4.0	CCOCc1c(c(c(c(=O)[nH]1)c1nnc(o1)Cc1ncc(cc1)Cl)O)c1c(cccc1OC)OC	10.1021/acs.jmedchem.0c01878
	137106310	687	None	16	Human	Functional	pEC50	=	10.6	10.6	-15	2	Agonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assayAgonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assay	ChEMBL	498	9	2	9	4.0	CCOCc1c(c(c(c(=O)[nH]1)c1nnc(o1)Cc1ncc(cc1)Cl)O)c1c(cccc1OC)OC	10.1021/acs.jmedchem.0c01878
	CHEMBL4873876	687	None	16	Human	Functional	pEC50	=	10.6	10.6	-15	2	Agonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assayAgonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assay	ChEMBL	498	9	2	9	4.0	CCOCc1c(c(c(c(=O)[nH]1)c1nnc(o1)Cc1ncc(cc1)Cl)O)c1c(cccc1OC)OC	10.1021/acs.jmedchem.0c01878
	11837	986	None	4	Human	Functional	pEC50	=	10.6	10.6	-2	2	Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay	ChEMBL	512	8	1	8	4.0	C(CCC)c1n(c(c(c(=O)n1)C(=O)N1C[C@@H](CC1)c1ncc(cc1)Cl)O)c1c(cccc1OC)OC	10.1021/acsmedchemlett.1c00385
	162679533	986	None	4	Human	Functional	pEC50	=	10.6	10.6	-2	2	Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay	ChEMBL	512	8	1	8	4.0	C(CCC)c1n(c(c(c(=O)n1)C(=O)N1C[C@@H](CC1)c1ncc(cc1)Cl)O)c1c(cccc1OC)OC	10.1021/acsmedchemlett.1c00385
	CHEMBL4854412	986	None	4	Human	Functional	pEC50	=	10.6	10.6	-2	2	Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay	ChEMBL	512	8	1	8	4.0	C(CCC)c1n(c(c(c(=O)n1)C(=O)N1C[C@@H](CC1)c1ncc(cc1)Cl)O)c1c(cccc1OC)OC	10.1021/acsmedchemlett.1c00385
	137198078	190367	None	0	Human	Functional	pEC50	=	10.5	10.5	-	1	Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis	ChEMBL	516	6	1	8	3.6	CCc1cccc(CC)c1-n1c(-c2ccn(C)n2)nc(=O)c(C(=O)N2CCC(c3ncccc3F)C2)c1O	10.1021/acs.jmedchem.1c01504
	CHEMBL5175424	190367	None	0	Human	Functional	pEC50	=	10.5	10.5	-	1	Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis	ChEMBL	516	6	1	8	3.6	CCc1cccc(CC)c1-n1c(-c2ccn(C)n2)nc(=O)c(C(=O)N2CCC(c3ncccc3F)C2)c1O	10.1021/acs.jmedchem.1c01504
	137197999	192152	None	0	Human	Functional	pEC50	=	10.5	10.5	-	1	Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis	ChEMBL	554	6	1	9	4.3	COc1cccc(OC)c1-n1c(-c2csc(C)n2)nc(=O)c(C(=O)N2CCC(c3ccc(F)cc3F)C2)c1O	10.1021/acs.jmedchem.1c01504
	CHEMBL5202233	192152	None	0	Human	Functional	pEC50	=	10.5	10.5	-	1	Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis	ChEMBL	554	6	1	9	4.3	COc1cccc(OC)c1-n1c(-c2csc(C)n2)nc(=O)c(C(=O)N2CCC(c3ccc(F)cc3F)C2)c1O	10.1021/acs.jmedchem.1c01504
	146222276	184670	None	0	Human	Functional	pEC50	=	10.5	10.5	6	2	Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	550	10	2	8	5.0	CCCCc1[nH]c(=O)c(S(=O)(=O)c2ccc(-c3cccnc3OC)cc2)c(O)c1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325
	CHEMBL4848436	184670	None	0	Human	Functional	pEC50	=	10.5	10.5	6	2	Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	550	10	2	8	5.0	CCCCc1[nH]c(=O)c(S(=O)(=O)c2ccc(-c3cccnc3OC)cc2)c(O)c1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325
	132248099	186246	None	0	Human	Functional	pEC50	=	10.5	10.5	3	2	Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	570	9	2	8	4.7	CCCCc1[nH]c(=O)c(S(=O)(=O)c2ccc(-n3cc(Cl)ccc3=O)cc2)c(O)c1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325
	CHEMBL4872192	186246	None	0	Human	Functional	pEC50	=	10.5	10.5	3	2	Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	570	9	2	8	4.7	CCCCc1[nH]c(=O)c(S(=O)(=O)c2ccc(-n3cc(Cl)ccc3=O)cc2)c(O)c1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325
	139292739	186278	None	0	Human	Functional	pEC50	=	10.5	10.5	1	2	Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	604	11	2	10	4.5	CCCCc1nc(=O)c(S(=O)(=O)c2ccc(-c3ccnc(NC(=O)C4CC4)c3)cc2)c(O)n1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325
	CHEMBL4872583	186278	None	0	Human	Functional	pEC50	=	10.5	10.5	1	2	Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	604	11	2	10	4.5	CCCCc1nc(=O)c(S(=O)(=O)c2ccc(-c3ccnc(NC(=O)C4CC4)c3)cc2)c(O)n1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325
	164624169	185922	None	0	Human	Functional	pEC50	=	10.5	10.5	-	1	Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay	ChEMBL	512	8	1	8	4.0	CCCCc1nc(=O)c(C(=O)N2CC[C@H](c3ccc(Cl)cn3)C2)c(O)n1-c1c(OC)cccc1OC	10.1021/acsmedchemlett.1c00385
	CHEMBL4867145	185922	None	0	Human	Functional	pEC50	=	10.5	10.5	-	1	Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay	ChEMBL	512	8	1	8	4.0	CCCCc1nc(=O)c(C(=O)N2CC[C@H](c3ccc(Cl)cn3)C2)c(O)n1-c1c(OC)cccc1OC	10.1021/acsmedchemlett.1c00385
	168287693	191856	None	0	Human	Functional	pEC50	=	10.4	10.4	-	1	Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis	ChEMBL	515	6	1	7	4.2	CCc1cccc(CC)c1-n1c(-c2ccn(C)n2)nc(=O)c(C(=O)N2CC[C@H](c3ccccc3F)C2)c1O	10.1021/acs.jmedchem.1c01504
	CHEMBL5197398	191856	None	0	Human	Functional	pEC50	=	10.4	10.4	-	1	Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis	ChEMBL	515	6	1	7	4.2	CCc1cccc(CC)c1-n1c(-c2ccn(C)n2)nc(=O)c(C(=O)N2CC[C@H](c3ccccc3F)C2)c1O	10.1021/acs.jmedchem.1c01504
	145419550	185688	None	0	Human	Functional	pEC50	=	10.4	10.4	2	2	Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	534	9	2	7	5.3	CCCCc1[nH]c(=O)c(S(=O)(=O)c2ccc(-c3ccncc3C)cc2)c(O)c1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325
	CHEMBL4863554	185688	None	0	Human	Functional	pEC50	=	10.4	10.4	2	2	Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	534	9	2	7	5.3	CCCCc1[nH]c(=O)c(S(=O)(=O)c2ccc(-c3ccncc3C)cc2)c(O)c1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325
	164620375	186323	None	0	Human	Functional	pEC50	=	10.4	10.4	1	2	Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	521	9	1	9	4.2	CCCCc1nc(=O)c(S(=O)(=O)c2ccc(-c3cccnc3)cc2)c(O)n1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325

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Ligands (move mouse cursor over ligand name to see structure)					Receptor		Activity									Chemical information
Sel. page	Common name No matches found	GPCRdb ID No matches found	Reference ligand No matches found	Vendors	Species No matches found		Assay Type No matches found	Activity Type No matches found	Activity Relation No matches found	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description No matches found	Source No matches found	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles No matches found	DOI No matches found

Ligands (move mouse cursor over ligand name to see structure)					Receptor	Activity									Chemical information
Sel. page	Common name No matches found	GPCRdb ID No matches found	Reference ligand No matches found	Vendors	Species No matches found	Assay Type No matches found	Activity Type No matches found	Activity Relation No matches found	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description No matches found	Source No matches found	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles No matches found	DOI No matches found
	137250573	184852	None	0	Mouse	Binding	pEC50	=	10.7	10.7	-	0	Agonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	571	9	1	10	3.9	CCCCc1nc(=O)c(S(=O)(=O)c2ccc(-n3cc(Cl)ccc3=O)cc2)c(O)n1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325
	CHEMBL4850818	184852	None	0	Mouse	Binding	pEC50	=	10.7	10.7	-	0	Agonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	571	9	1	10	3.9	CCCCc1nc(=O)c(S(=O)(=O)c2ccc(-n3cc(Cl)ccc3=O)cc2)c(O)n1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325
	138697624	185128	None	0	Mouse	Binding	pEC50	=	10.7	10.7	-	0	Agonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	539	9	1	9	4.3	CCCCc1nc(=O)c(S(=O)(=O)c2ccc(-c3ccc(F)nc3)cc2)c(O)n1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325
	CHEMBL4855004	185128	None	0	Mouse	Binding	pEC50	=	10.7	10.7	-	0	Agonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	539	9	1	9	4.3	CCCCc1nc(=O)c(S(=O)(=O)c2ccc(-c3ccc(F)nc3)cc2)c(O)n1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325
	11838	687	None	16	Mouse	Binding	pEC50	=	10.6	10.6	-	1	Agonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	498	9	2	9	4.0	CCOCc1c(c(c(c(=O)[nH]1)c1nnc(o1)Cc1ncc(cc1)Cl)O)c1c(cccc1OC)OC	10.1016/j.bmcl.2021.128325
	137106310	687	None	16	Mouse	Binding	pEC50	=	10.6	10.6	-	1	Agonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	498	9	2	9	4.0	CCOCc1c(c(c(c(=O)[nH]1)c1nnc(o1)Cc1ncc(cc1)Cl)O)c1c(cccc1OC)OC	10.1016/j.bmcl.2021.128325
	CHEMBL4873876	687	None	16	Mouse	Binding	pEC50	=	10.6	10.6	-	1	Agonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	498	9	2	9	4.0	CCOCc1c(c(c(c(=O)[nH]1)c1nnc(o1)Cc1ncc(cc1)Cl)O)c1c(cccc1OC)OC	10.1016/j.bmcl.2021.128325
	138697637	184872	None	0	Mouse	Binding	pEC50	=	10.5	10.5	-	0	Agonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	551	10	1	10	4.2	CCCCc1nc(=O)c(S(=O)(=O)c2ccc(-c3cccnc3OC)cc2)c(O)n1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325
	CHEMBL4851100	184872	None	0	Mouse	Binding	pEC50	=	10.5	10.5	-	0	Agonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	551	10	1	10	4.2	CCCCc1nc(=O)c(S(=O)(=O)c2ccc(-c3cccnc3OC)cc2)c(O)n1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325
	137250580	185753	None	0	Mouse	Binding	pEC50	=	10.5	10.5	-	0	Agonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	484	9	1	8	4.0	CCCCc1nc(=O)c(S(=O)(=O)c2ccc(C3CC3)cc2)c(O)n1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325
	CHEMBL4864542	185753	None	0	Mouse	Binding	pEC50	=	10.5	10.5	-	0	Agonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	484	9	1	8	4.0	CCCCc1nc(=O)c(S(=O)(=O)c2ccc(C3CC3)cc2)c(O)n1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325
	138697675	186259	None	0	Mouse	Binding	pEC50	=	10.5	10.5	-	0	Agonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	537	9	1	10	3.3	CCCCc1nc(=O)c(S(=O)(=O)c2ccc(-n3ccccc3=O)cc2)c(O)n1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325
	CHEMBL4872345	186259	None	0	Mouse	Binding	pEC50	=	10.5	10.5	-	0	Agonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	537	9	1	10	3.3	CCCCc1nc(=O)c(S(=O)(=O)c2ccc(-n3ccccc3=O)cc2)c(O)n1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325
	138697719	186661	None	0	Mouse	Binding	pEC50	=	10.5	10.5	-	0	Agonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	555	9	1	10	3.9	COc1cccc(OC)c1-n1c(COC(C)C)nc(=O)c(S(=O)(=O)c2ccc(-c3ccc(F)nc3)cc2)c1O	10.1016/j.bmcl.2021.128325
	CHEMBL4878056	186661	None	0	Mouse	Binding	pEC50	=	10.5	10.5	-	0	Agonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	555	9	1	10	3.9	COc1cccc(OC)c1-n1c(COC(C)C)nc(=O)c(S(=O)(=O)c2ccc(-c3ccc(F)nc3)cc2)c1O	10.1016/j.bmcl.2021.128325
	139292739	186278	None	0	Mouse	Binding	pEC50	=	10.4	10.4	-	0	Agonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	604	11	2	10	4.5	CCCCc1nc(=O)c(S(=O)(=O)c2ccc(-c3ccnc(NC(=O)C4CC4)c3)cc2)c(O)n1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325
	CHEMBL4872583	186278	None	0	Mouse	Binding	pEC50	=	10.4	10.4	-	0	Agonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	604	11	2	10	4.5	CCCCc1nc(=O)c(S(=O)(=O)c2ccc(-c3ccnc(NC(=O)C4CC4)c3)cc2)c(O)n1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325
	138698137	185191	None	0	Mouse	Binding	pEC50	=	10.3	10.3	-	0	Agonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	553	9	1	9	4.6	COc1cccc(OC)c1-n1c(CCC(C)C)nc(=O)c(S(=O)(=O)c2ccc(-c3ccc(F)nc3)cc2)c1O	10.1016/j.bmcl.2021.128325
	CHEMBL4855918	185191	None	0	Mouse	Binding	pEC50	=	10.3	10.3	-	0	Agonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	553	9	1	9	4.6	COc1cccc(OC)c1-n1c(CCC(C)C)nc(=O)c(S(=O)(=O)c2ccc(-c3ccc(F)nc3)cc2)c1O	10.1016/j.bmcl.2021.128325
	164620375	186323	None	0	Mouse	Binding	pEC50	=	10.3	10.3	-	0	Agonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	521	9	1	9	4.2	CCCCc1nc(=O)c(S(=O)(=O)c2ccc(-c3cccnc3)cc2)c(O)n1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325
	CHEMBL4873216	186323	None	0	Mouse	Binding	pEC50	=	10.3	10.3	-	0	Agonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	521	9	1	9	4.2	CCCCc1nc(=O)c(S(=O)(=O)c2ccc(-c3cccnc3)cc2)c(O)n1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325
	145419550	185688	None	0	Mouse	Binding	pEC50	=	10	10.0	-	0	Agonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	534	9	2	7	5.3	CCCCc1[nH]c(=O)c(S(=O)(=O)c2ccc(-c3ccncc3C)cc2)c(O)c1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325
	CHEMBL4863554	185688	None	0	Mouse	Binding	pEC50	=	10	10.0	-	0	Agonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	534	9	2	7	5.3	CCCCc1[nH]c(=O)c(S(=O)(=O)c2ccc(-c3ccncc3C)cc2)c(O)c1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325
	132248099	186246	None	0	Mouse	Binding	pEC50	=	10	10.0	-	0	Agonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	570	9	2	8	4.7	CCCCc1[nH]c(=O)c(S(=O)(=O)c2ccc(-n3cc(Cl)ccc3=O)cc2)c(O)c1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325
	CHEMBL4872192	186246	None	0	Mouse	Binding	pEC50	=	10	10.0	-	0	Agonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	570	9	2	8	4.7	CCCCc1[nH]c(=O)c(S(=O)(=O)c2ccc(-n3cc(Cl)ccc3=O)cc2)c(O)c1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325
	137250546	186404	None	0	Mouse	Binding	pEC50	=	10	10.0	-	0	Agonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	538	9	1	8	4.9	CCCCc1nc(=O)c(S(=O)(=O)c2ccc(-c3ccc(F)cc3)cc2)c(O)n1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325
	CHEMBL4874447	186404	None	0	Mouse	Binding	pEC50	=	10	10.0	-	0	Agonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	538	9	1	8	4.9	CCCCc1nc(=O)c(S(=O)(=O)c2ccc(-c3ccc(F)cc3)cc2)c(O)n1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325
	127043374	140580	None	0	Human	Binding	pEC50	=	9.9	9.9	-	1	Agonist activity at human APJ receptor by saphenous vein contraction assayAgonist activity at human APJ receptor by saphenous vein contraction assay	ChEMBL	1533	44	20	20	-5.0	CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)C1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O	10.1021/acs.jmedchem.8b00435
	CHEMBL3809818	140580	None	0	Human	Binding	pEC50	=	9.9	9.9	-	1	Agonist activity at human APJ receptor by saphenous vein contraction assayAgonist activity at human APJ receptor by saphenous vein contraction assay	ChEMBL	1533	44	20	20	-5.0	CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)C1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O	10.1021/acs.jmedchem.8b00435
	146222276	184670	None	0	Mouse	Binding	pEC50	=	9.7	9.7	-	0	Agonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	550	10	2	8	5.0	CCCCc1[nH]c(=O)c(S(=O)(=O)c2ccc(-c3cccnc3OC)cc2)c(O)c1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325
	CHEMBL4848436	184670	None	0	Mouse	Binding	pEC50	=	9.7	9.7	-	0	Agonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	550	10	2	8	5.0	CCCCc1[nH]c(=O)c(S(=O)(=O)c2ccc(-c3cccnc3OC)cc2)c(O)c1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325
	134828250	2581	None	16	Human	Binding	pEC50	=	9.5	9.5	-	0	Agonist activity at human APJ receptor by saphenous vein contraction assayAgonist activity at human APJ receptor by saphenous vein contraction assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00435
	8523	2581	None	16	Human	Binding	pEC50	=	9.5	9.5	-	0	Agonist activity at human APJ receptor by saphenous vein contraction assayAgonist activity at human APJ receptor by saphenous vein contraction assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00435
	CHEMBL4475589	2581	None	16	Human	Binding	pEC50	=	9.5	9.5	-	0	Agonist activity at human APJ receptor by saphenous vein contraction assayAgonist activity at human APJ receptor by saphenous vein contraction assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00435
	138698343	185835	None	0	Mouse	Binding	pEC50	=	9.5	9.5	-	0	Agonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	458	8	1	8	3.4	CCCCc1nc(=O)c(S(=O)(=O)c2ccc(C)cc2)c(O)n1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325
	CHEMBL4865954	185835	None	0	Mouse	Binding	pEC50	=	9.5	9.5	-	0	Agonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	458	8	1	8	3.4	CCCCc1nc(=O)c(S(=O)(=O)c2ccc(C)cc2)c(O)n1-c1c(OC)cccc1OC	10.1016/j.bmcl.2021.128325
	137649320	157400	None	0	Human	Binding	pEC50	=	9.4	9.4	-	1	Activity at human APJ receptor expressed in HEK293 cells assessed as dissociation of Galphai1 from Gbetagamma subunit after 5 mins by BRET assayActivity at human APJ receptor expressed in HEK293 cells assessed as dissociation of Galphai1 from Gbetagamma subunit after 5 mins by BRET assay	ChEMBL	1485	46	20	19	-4.4	C=CC[C@H](N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC=C)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCC)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O	10.1021/acs.jmedchem.7b01353
	CHEMBL4077162	157400	None	0	Human	Binding	pEC50	=	9.4	9.4	-	1	Activity at human APJ receptor expressed in HEK293 cells assessed as dissociation of Galphai1 from Gbetagamma subunit after 5 mins by BRET assayActivity at human APJ receptor expressed in HEK293 cells assessed as dissociation of Galphai1 from Gbetagamma subunit after 5 mins by BRET assay	ChEMBL	1485	46	20	19	-4.4	C=CC[C@H](N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC=C)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCC)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O	10.1021/acs.jmedchem.7b01353
	138697975	185811	None	0	Mouse	Binding	pEC50	=	9.4	9.4	-	0	Agonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	496	7	1	8	4.3	COc1cccc(OC)c1-n1c(C2CCCC2)nc(=O)c(S(=O)(=O)c2ccc(C3CC3)cc2)c1O	10.1016/j.bmcl.2021.128325
	CHEMBL4865532	185811	None	0	Mouse	Binding	pEC50	=	9.4	9.4	-	0	Agonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at mouse APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay	ChEMBL	496	7	1	8	4.3	COc1cccc(OC)c1-n1c(C2CCCC2)nc(=O)c(S(=O)(=O)c2ccc(C3CC3)cc2)c1O	10.1016/j.bmcl.2021.128325
	CHEMBL3417291	214103	None	0	Human	Binding	pEC50	=	9.3	9.3	-	1	Agonist activity at human APJ receptor expressed in HEK293 cells assessed as induction of Galphai1 subunit dissociation incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as induction of Galphai1 subunit dissociation incubated for 5 mins by BRET assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O	10.1021/jm501916k
	CHEMBL3417379	214108	None	0	Human	Binding	pEC50	=	9.1	9.1	-	1	Agonist activity at human APJ receptor expressed in HEK293 cells assessed as induction of Galphai1 subunit dissociation incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as induction of Galphai1 subunit dissociation incubated for 5 mins by BRET assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccncc1)C(=O)O	10.1021/jm501916k
	137639006	157030	None	0	Human	Binding	pEC50	=	9.1	9.1	-	1	Activity at human APJ receptor expressed in HEK293 cells assessed as dissociation of Galphai1 from Gbetagamma subunit after 5 mins by BRET assayActivity at human APJ receptor expressed in HEK293 cells assessed as dissociation of Galphai1 from Gbetagamma subunit after 5 mins by BRET assay	ChEMBL	1484	45	20	18	-4.1	C=CC[C@H](NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC=C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O	10.1021/acs.jmedchem.7b01353
	CHEMBL4072606	157030	None	0	Human	Binding	pEC50	=	9.1	9.1	-	1	Activity at human APJ receptor expressed in HEK293 cells assessed as dissociation of Galphai1 from Gbetagamma subunit after 5 mins by BRET assayActivity at human APJ receptor expressed in HEK293 cells assessed as dissociation of Galphai1 from Gbetagamma subunit after 5 mins by BRET assay	ChEMBL	1484	45	20	18	-4.1	C=CC[C@H](NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC=C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O	10.1021/acs.jmedchem.7b01353
	25085173	213673	None	24	Human	Binding	pEC50	=	9.1	9.1	8	2	Agonist activity at human APJ receptor expressed in HEK293 cells assessed as induction of Galphai1 subunit dissociation incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as induction of Galphai1 subunit dissociation incubated for 5 mins by BRET assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O	10.1021/jm501916k
	CHEMBL3184840	213673	None	24	Human	Binding	pEC50	=	9.1	9.1	8	2	Agonist activity at human APJ receptor expressed in HEK293 cells assessed as induction of Galphai1 subunit dissociation incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as induction of Galphai1 subunit dissociation incubated for 5 mins by BRET assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O	10.1021/jm501916k
	CHEMBL3417385	214114	None	0	Human	Binding	pEC50	=	9.0	9.0	-	1	Agonist activity at human APJ receptor expressed in HEK293 cells assessed as induction of Galphai1 subunit dissociation incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as induction of Galphai1 subunit dissociation incubated for 5 mins by BRET assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccc(C(=O)c2ccccc2)cc1)C(=O)O	10.1021/jm501916k
	137650464	157354	None	0	Human	Binding	pEC50	=	9	9.0	-	1	Activity at human APJ receptor expressed in HEK293 cells assessed as dissociation of Galphai1 from Gbetagamma subunit after 5 mins by BRET assayActivity at human APJ receptor expressed in HEK293 cells assessed as dissociation of Galphai1 from Gbetagamma subunit after 5 mins by BRET assay	ChEMBL	1459	43	19	18	-4.6	C=CC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CC=C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O	10.1021/acs.jmedchem.7b01353
	CHEMBL4076652	157354	None	0	Human	Binding	pEC50	=	9	9.0	-	1	Activity at human APJ receptor expressed in HEK293 cells assessed as dissociation of Galphai1 from Gbetagamma subunit after 5 mins by BRET assayActivity at human APJ receptor expressed in HEK293 cells assessed as dissociation of Galphai1 from Gbetagamma subunit after 5 mins by BRET assay	ChEMBL	1459	43	19	18	-4.6	C=CC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CC=C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O	10.1021/acs.jmedchem.7b01353
	127043374	140580	None	0	Human	Binding	pEC50	=	9	9.0	-	1	Agonist activity at human APJ receptor assessed as Gi activationAgonist activity at human APJ receptor assessed as Gi activation	ChEMBL	1533	44	20	20	-5.0	CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)C1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O	10.1021/acs.jmedchem.8b00435

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Ligand source activities (1 row/activity)