GPCRdb

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
	10210629	15536	0	None	2	4	Human	9.9	pIC50	=	9.9	Functional	Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin A receptor of MMQ cells.Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin A receptor of MMQ cells.	ChEMBL	592	15	1	7	5.0	CCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1	10.1021/jm970101g
	CHEMBL109644	15536	0	None	2	4	Human	9.9	pIC50	=	9.9	Functional	Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin A receptor of MMQ cells.Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin A receptor of MMQ cells.	ChEMBL	592	15	1	7	5.0	CCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1	10.1021/jm970101g
	9870830	213493	38	None	-1	5	Human	9.5	pIC50	=	9.5	Functional	Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK	ChEMBL	506	8	1	9	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1	10.1021/jm00008a002
	CHEMBL8981	213493	38	None	-1	5	Human	9.5	pIC50	=	9.5	Functional	Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK	ChEMBL	506	8	1	9	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1	10.1021/jm00008a002
	23670447	9803	2	None	1	4	Human	9.5	pIC50	=	9.5	Functional	Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK	ChEMBL	528	10	0	9	0.1	COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+]	10.1021/jm00008a002
	999	9803	2	None	1	4	Human	9.5	pIC50	=	9.5	Functional	Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK	ChEMBL	528	10	0	9	0.1	COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+]	10.1021/jm00008a002
	CHEMBL1204799	9803	2	None	1	4	Human	9.5	pIC50	=	9.5	Functional	Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK	ChEMBL	528	10	0	9	0.1	COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+]	10.1021/jm00008a002
	CHEMBL25438	9803	2	None	1	4	Human	9.5	pIC50	=	9.5	Functional	Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK	ChEMBL	528	10	0	9	0.1	COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+]	10.1021/jm00008a002
	10187997	116749	0	None	1	4	Human	9.4	pIC50	=	9.4	Functional	Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin A receptor of MMQ cells.Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin A receptor of MMQ cells.	ChEMBL	564	13	1	7	4.2	CCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1	10.1021/jm970101g
	CHEMBL323464	116749	0	None	1	4	Human	9.4	pIC50	=	9.4	Functional	Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin A receptor of MMQ cells.Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin A receptor of MMQ cells.	ChEMBL	564	13	1	7	4.2	CCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1	10.1021/jm970101g
	9916235	16125	1	None	1	4	Human	9.3	pIC50	=	9.3	Functional	Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin A receptor of MMQ cells.Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin A receptor of MMQ cells.	ChEMBL	578	14	1	7	4.6	CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1	10.1021/jm970101g
	CHEMBL111277	16125	1	None	1	4	Human	9.3	pIC50	=	9.3	Functional	Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin A receptor of MMQ cells.Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin A receptor of MMQ cells.	ChEMBL	578	14	1	7	4.6	CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1	10.1021/jm970101g
	10603409	117381	0	None	1	4	Human	9.3	pIC50	=	9.3	Functional	Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin A receptor of MMQ cells.Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin A receptor of MMQ cells.	ChEMBL	584	13	1	7	4.1	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCCl	10.1021/jm970101g
	CHEMBL325581	117381	0	None	1	4	Human	9.3	pIC50	=	9.3	Functional	Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin A receptor of MMQ cells.Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin A receptor of MMQ cells.	ChEMBL	584	13	1	7	4.1	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCCl	10.1021/jm970101g
	443289	7498	47	None	1	4	Human	9.2	pIC50	=	9.2	Functional	Antagonist activity at ETA receptor in human SKNMC cells assessed as inhibition of endothelin-1-mediated Ca2+ mobilization by fura-2/AM dye-based spectrofluorimetric methodAntagonist activity at ETA receptor in human SKNMC cells assessed as inhibition of endothelin-1-mediated Ca2+ mobilization by fura-2/AM dye-based spectrofluorimetric method	ChEMBL		None	None	None		None	10.1016/j.ejmech.2016.06.006
	997	7498	47	None	1	4	Human	9.2	pIC50	=	9.2	Functional	Antagonist activity at ETA receptor in human SKNMC cells assessed as inhibition of endothelin-1-mediated Ca2+ mobilization by fura-2/AM dye-based spectrofluorimetric methodAntagonist activity at ETA receptor in human SKNMC cells assessed as inhibition of endothelin-1-mediated Ca2+ mobilization by fura-2/AM dye-based spectrofluorimetric method	ChEMBL		None	None	None		None	10.1016/j.ejmech.2016.06.006
	CHEMBL314691	7498	47	None	1	4	Human	9.2	pIC50	=	9.2	Functional	Antagonist activity at ETA receptor in human SKNMC cells assessed as inhibition of endothelin-1-mediated Ca2+ mobilization by fura-2/AM dye-based spectrofluorimetric methodAntagonist activity at ETA receptor in human SKNMC cells assessed as inhibition of endothelin-1-mediated Ca2+ mobilization by fura-2/AM dye-based spectrofluorimetric method	ChEMBL		None	None	None		None	10.1016/j.ejmech.2016.06.006
	DB12054	7498	47	None	1	4	Human	9.2	pIC50	=	9.2	Functional	Antagonist activity at ETA receptor in human SKNMC cells assessed as inhibition of endothelin-1-mediated Ca2+ mobilization by fura-2/AM dye-based spectrofluorimetric methodAntagonist activity at ETA receptor in human SKNMC cells assessed as inhibition of endothelin-1-mediated Ca2+ mobilization by fura-2/AM dye-based spectrofluorimetric method	ChEMBL		None	None	None		None	10.1016/j.ejmech.2016.06.006
	CHEMBL3980643	219293	0	None	-6	2	Human	9.2	pIC50	=	9.2	Functional	Agonist activity at ETA receptor in human SKNMC cells assessed as induction of Ca2+ mobilization by fluorimetric methodAgonist activity at ETA receptor in human SKNMC cells assessed as induction of Ca2+ mobilization by fluorimetric method	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)[C@@H](C)CC	10.1016/j.ejmech.2016.06.006
	10230737	119097	0	None	16	2	Human	9.0	pIC50	=	9.0	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	544	7	2	6	4.3	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(F)cccc3F)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL329251	119097	0	None	16	2	Human	9.0	pIC50	=	9.0	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	544	7	2	6	4.3	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(F)cccc3F)c3ccccc32)n1	10.1021/jm031115r
	11318978	174682	0	None	7	2	Human	8.9	pIC50	=	8.9	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	560	7	2	6	4.8	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(F)cccc3Cl)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL431286	174682	0	None	7	2	Human	8.9	pIC50	=	8.9	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	560	7	2	6	4.8	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(F)cccc3Cl)c3ccccc32)n1	10.1021/jm031115r
	10651488	170158	0	None	1	4	Human	8.8	pIC50	=	8.8	Functional	Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin A receptor of MMQ cells.Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin A receptor of MMQ cells.	ChEMBL	618	13	1	7	4.8	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCC(F)(F)F	10.1021/jm970101g
	CHEMBL419367	170158	0	None	1	4	Human	8.8	pIC50	=	8.8	Functional	Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin A receptor of MMQ cells.Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin A receptor of MMQ cells.	ChEMBL	618	13	1	7	4.8	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCC(F)(F)F	10.1021/jm970101g
	CHEMBL412706	219798	0	None	-	1	Pig	8.8	pIC50	=	8.8	Functional	Antagonist activity against ET-A from porcine heart membranesAntagonist activity against ET-A from porcine heart membranes	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/0960-894X(95)00349-X
	9894443	119350	0	None	3	2	Human	8.7	pIC50	=	8.7	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	576	7	2	6	5.3	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(Cl)cccc3Cl)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL330104	119350	0	None	3	2	Human	8.7	pIC50	=	8.7	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	576	7	2	6	5.3	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(Cl)cccc3Cl)c3ccccc32)n1	10.1021/jm031115r
	9955200	16104	0	None	53	3	Human	8.7	pIC50	=	8.7	Functional	Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK	ChEMBL	446	6	1	7	3.8	COc1ccc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc1	10.1021/jm00008a002
	CHEMBL11115	16104	0	None	53	3	Human	8.7	pIC50	=	8.7	Functional	Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK	ChEMBL	446	6	1	7	3.8	COc1ccc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc1	10.1021/jm00008a002
	70690542	82996	0	None	1	2	Human	8.0	pIC50	=	8	Functional	Antagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cellsAntagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cells	ChEMBL	532	9	1	6	6.6	CCCCc1nc2ccc(F)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1016/j.bmc.2012.06.011
	CHEMBL2058375	82996	0	None	1	2	Human	8.0	pIC50	=	8	Functional	Antagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cellsAntagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cells	ChEMBL	532	9	1	6	6.6	CCCCc1nc2ccc(F)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1016/j.bmc.2012.06.011
	70696781	82997	0	None	1	2	Human	8.0	pIC50	=	8	Functional	Antagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cellsAntagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cells	ChEMBL	582	9	1	6	7.5	CCCCc1nc2ccc(C(F)(F)F)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1016/j.bmc.2012.06.011
	CHEMBL2058376	82997	0	None	1	2	Human	8.0	pIC50	=	8	Functional	Antagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cellsAntagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cells	ChEMBL	582	9	1	6	7.5	CCCCc1nc2ccc(C(F)(F)F)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1016/j.bmc.2012.06.011
	11342089	113985	0	None	9	2	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	568	9	2	8	4.0	COc1ccc(CN2C(=O)CN[C@](c3cccc(OC)c3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1	10.1021/jm031115r
	CHEMBL316629	113985	0	None	9	2	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	568	9	2	8	4.0	COc1ccc(CN2C(=O)CN[C@](c3cccc(OC)c3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1	10.1021/jm031115r
	10230703	214638	0	None	4	2	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	542	7	2	6	4.7	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccccc3Cl)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL96472	214638	0	None	4	2	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	542	7	2	6	4.7	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccccc3Cl)c3ccccc32)n1	10.1021/jm031115r
	9957883	105433	0	None	25	2	Human	7.0	pIC50	=	7	Functional	Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin A receptor.Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin A receptor.	ChEMBL	507	7	1	9	5.0	COc1cc2c(Sc3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC	10.1016/0960-894X(96)00232-6
	CHEMBL27732	105433	0	None	25	2	Human	7.0	pIC50	=	7	Functional	Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin A receptor.Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin A receptor.	ChEMBL	507	7	1	9	5.0	COc1cc2c(Sc3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC	10.1016/0960-894X(96)00232-6
	44213651	11070	0	None	-	1	Human	5.0	pIC50	=	5	Functional	Compound was tested for its ability to inhibit Endothelin A receptor induced arachidonic acid release(AARA) in rabbit renal artery vascular smooth muscles.Compound was tested for its ability to inhibit Endothelin A receptor induced arachidonic acid release(AARA) in rabbit renal artery vascular smooth muscles.	ChEMBL	343	3	1	4	4.2	OCC(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12	10.1016/S0960-894X(96)00551-3
	CHEMBL100795	11070	0	None	-	1	Human	5.0	pIC50	=	5	Functional	Compound was tested for its ability to inhibit Endothelin A receptor induced arachidonic acid release(AARA) in rabbit renal artery vascular smooth muscles.Compound was tested for its ability to inhibit Endothelin A receptor induced arachidonic acid release(AARA) in rabbit renal artery vascular smooth muscles.	ChEMBL	343	3	1	4	4.2	OCC(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12	10.1016/S0960-894X(96)00551-3
	11455999	214608	0	None	31	2	Human	7.0	pIC50	=	7	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	580	7	2	4	6.6	O=C(O)[C@@H](Oc1cccc(Cl)c1)[C@@]1(c2ccccc2)NCC(=O)N(Cc2c(Cl)cccc2Cl)c2ccccc21	10.1021/jm031115r
	CHEMBL96325	214608	0	None	31	2	Human	7.0	pIC50	=	7	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	580	7	2	4	6.6	O=C(O)[C@@H](Oc1cccc(Cl)c1)[C@@]1(c2ccccc2)NCC(=O)N(Cc2c(Cl)cccc2Cl)c2ccccc21	10.1021/jm031115r
	11490160	214280	0	None	5	2	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	584	8	2	6	5.7	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL94446	214280	0	None	5	2	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	584	8	2	6	5.7	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)n1	10.1021/jm031115r
	11273181	214645	0	None	-4	2	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	576	7	2	6	5.0	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccccc3C(F)(F)F)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL96506	214645	0	None	-4	2	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	576	7	2	6	5.0	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccccc3C(F)(F)F)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL386778	219169	0	None	-	1	Pig	8.0	pIC50	=	8.0	Functional	Antagonist activity against ET-A from porcine heart membranesAntagonist activity against ET-A from porcine heart membranes	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(95)00349-X
	CHEMBL405337	219336	0	None	-	1	Pig	8.0	pIC50	=	8.0	Functional	Antagonist activity against ET-A from porcine heart membranesAntagonist activity against ET-A from porcine heart membranes	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(95)00349-X
	CHEMBL405916	219364	0	None	-	1	Pig	8.0	pIC50	=	8.0	Functional	Antagonist activity against ET-A from porcine heart membranesAntagonist activity against ET-A from porcine heart membranes	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(95)00349-X
	CHEMBL409180	219529	0	None	-	1	Pig	8.0	pIC50	=	8.0	Functional	Antagonist activity against ET-A from porcine heart membranesAntagonist activity against ET-A from porcine heart membranes	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(95)00349-X
	6450144	129339	8	None	-	1	Rat	8.0	pIC50	=	8.0	Functional	Antagonist activity at endothelin A receptor in rat A7r5 cells assessed as inhibition of ET-1-induced increase in cytosolic free Ca2+ level treated 1 min prior to ET-1 addition by fura-2 dye-based spectrofluorometric analysisAntagonist activity at endothelin A receptor in rat A7r5 cells assessed as inhibition of ET-1-induced increase in cytosolic free Ca2+ level treated 1 min prior to ET-1 addition by fura-2 dye-based spectrofluorometric analysis	ChEMBL	632	5	3	6	8.1	CC1(C)CC[C@]2(C(=O)O)CC[C@]3(COC(=O)/C=C/c4ccc(O)c(O)c4)C(=CC[C@@H]4[C@@]5(C)CCC(=O)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]2C1	10.1016/j.bmc.2015.06.055
	CHEMBL3601500	129339	8	None	-	1	Rat	8.0	pIC50	=	8.0	Functional	Antagonist activity at endothelin A receptor in rat A7r5 cells assessed as inhibition of ET-1-induced increase in cytosolic free Ca2+ level treated 1 min prior to ET-1 addition by fura-2 dye-based spectrofluorometric analysisAntagonist activity at endothelin A receptor in rat A7r5 cells assessed as inhibition of ET-1-induced increase in cytosolic free Ca2+ level treated 1 min prior to ET-1 addition by fura-2 dye-based spectrofluorometric analysis	ChEMBL	632	5	3	6	8.1	CC1(C)CC[C@]2(C(=O)O)CC[C@]3(COC(=O)/C=C/c4ccc(O)c(O)c4)C(=CC[C@@H]4[C@@]5(C)CCC(=O)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]2C1	10.1016/j.bmc.2015.06.055
	70684240	82998	0	None	1	2	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cellsAntagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cells	ChEMBL	559	10	1	8	6.4	CCCCc1nc2ccc([N+](=O)[O-])cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1016/j.bmc.2012.06.011
	CHEMBL2058377	82998	0	None	1	2	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cellsAntagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cells	ChEMBL	559	10	1	8	6.4	CCCCc1nc2ccc([N+](=O)[O-])cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1016/j.bmc.2012.06.011
	11421972	214624	0	None	2	2	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	592	8	2	7	4.9	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cccc(OC(F)(F)F)c3)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL96422	214624	0	None	2	2	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	592	8	2	7	4.9	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cccc(OC(F)(F)F)c3)c3ccccc32)n1	10.1021/jm031115r
	11342005	214328	0	None	2	2	Human	7.9	pIC50	=	7.9	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	562	7	2	6	4.4	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cc(F)c(F)c(F)c3)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL94766	214328	0	None	2	2	Human	7.9	pIC50	=	7.9	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	562	7	2	6	4.4	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cc(F)c(F)c(F)c3)c3ccccc32)n1	10.1021/jm031115r
	11744509	12202	0	None	5	2	Human	7.0	pIC50	=	7.0	Functional	Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK	ChEMBL	450	5	1	6	4.5	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(Cl)cc2)cc1	10.1021/jm00008a002
	CHEMBL10733	12202	0	None	5	2	Human	7.0	pIC50	=	7.0	Functional	Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK	ChEMBL	450	5	1	6	4.5	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(Cl)cc2)cc1	10.1021/jm00008a002
	122194935	130872	0	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at human ETA receptor expressed in CHO cells assessed as inhibition of ET-1-induced Ca2+ efflux from endoplasmic reticulum into cytosol by fluo-4 dye-based FLIPR assayAntagonist activity at human ETA receptor expressed in CHO cells assessed as inhibition of ET-1-induced Ca2+ efflux from endoplasmic reticulum into cytosol by fluo-4 dye-based FLIPR assay	ChEMBL	619	11	2	8	6.8	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(S(F)(F)(F)(F)F)cc2)cc(-c2ncccn2)cc1OCCO	10.1021/acs.jmedchem.5b00258
	CHEMBL3633040	130872	0	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at human ETA receptor expressed in CHO cells assessed as inhibition of ET-1-induced Ca2+ efflux from endoplasmic reticulum into cytosol by fluo-4 dye-based FLIPR assayAntagonist activity at human ETA receptor expressed in CHO cells assessed as inhibition of ET-1-induced Ca2+ efflux from endoplasmic reticulum into cytosol by fluo-4 dye-based FLIPR assay	ChEMBL	619	11	2	8	6.8	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(S(F)(F)(F)(F)F)cc2)cc(-c2ncccn2)cc1OCCO	10.1021/acs.jmedchem.5b00258
	11387205	118338	0	None	-1	2	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	544	8	2	7	4.5	COc1ccc(CN2C(=O)CN[C@](C3CCCCC3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1	10.1021/jm031115r
	CHEMBL328073	118338	0	None	-1	2	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	544	8	2	7	4.5	COc1ccc(CN2C(=O)CN[C@](C3CCCCC3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1	10.1021/jm031115r
	CHEMBL62302	222622	0	None	-	1	Pig	7.9	pIC50	=	7.9	Functional	Antagonist activity against ET-A from porcine heart membranesAntagonist activity against ET-A from porcine heart membranes	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(95)00349-X
	10342643	11929	0	None	144	2	Human	7.9	pIC50	=	7.9	Functional	Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK	ChEMBL	430	5	1	6	4.1	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1C	10.1021/jm00008a002
	CHEMBL10588	11929	0	None	144	2	Human	7.9	pIC50	=	7.9	Functional	Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK	ChEMBL	430	5	1	6	4.1	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1C	10.1021/jm00008a002
	10342643	11929	0	None	144	2	Human	7.9	pIC50	=	7.9	Functional	Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.	ChEMBL	430	5	1	6	4.1	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1C	10.1021/jm00008a002
	CHEMBL10588	11929	0	None	144	2	Human	7.9	pIC50	=	7.9	Functional	Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.	ChEMBL	430	5	1	6	4.1	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1C	10.1021/jm00008a002
	10224745	119467	0	None	15	2	Human	7.9	pIC50	=	7.9	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	432	5	2	6	2.4	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL330425	119467	0	None	15	2	Human	7.9	pIC50	=	7.9	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	432	5	2	6	2.4	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3ccccc32)n1	10.1021/jm031115r
	9865706	104910	0	None	1	2	Human	5.9	pIC50	=	5.9	Functional	Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.	ChEMBL	400	4	1	5	4.1	Cc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1	10.1021/jm00008a002
	CHEMBL273613	104910	0	None	1	2	Human	5.9	pIC50	=	5.9	Functional	Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.	ChEMBL	400	4	1	5	4.1	Cc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1	10.1021/jm00008a002
	10452089	11337	0	None	-	1	Human	4.9	pIC50	=	4.9	Functional	Compound was tested for its ability to inhibit Endothelin A receptor induced arachidonic acid release(AARA) in rabbit renal artery vascular smooth muscles.Compound was tested for its ability to inhibit Endothelin A receptor induced arachidonic acid release(AARA) in rabbit renal artery vascular smooth muscles.	ChEMBL	375	3	0	5	4.1	COC(=O)C(c1ccc2c(c1)OCO2)c1c2c(nc3ccccc13)CCCC2	10.1016/S0960-894X(96)00551-3
	CHEMBL102494	11337	0	None	-	1	Human	4.9	pIC50	=	4.9	Functional	Compound was tested for its ability to inhibit Endothelin A receptor induced arachidonic acid release(AARA) in rabbit renal artery vascular smooth muscles.Compound was tested for its ability to inhibit Endothelin A receptor induced arachidonic acid release(AARA) in rabbit renal artery vascular smooth muscles.	ChEMBL	375	3	0	5	4.1	COC(=O)C(c1ccc2c(c1)OCO2)c1c2c(nc3ccccc13)CCCC2	10.1016/S0960-894X(96)00551-3
	11432855	214633	0	None	28	2	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	552	8	3	7	3.7	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(C(=O)O)cc3)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL96463	214633	0	None	28	2	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	552	8	3	7	3.7	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(C(=O)O)cc3)c3ccccc32)n1	10.1021/jm031115r
	11318559	214581	0	None	5	2	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	531	8	2	8	2.1	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CCN3CCOCC3)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL96193	214581	0	None	5	2	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	531	8	2	8	2.1	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CCN3CCOCC3)c3ccccc32)n1	10.1021/jm031115r
	11238540	214304	0	None	11	2	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	576	8	2	5	5.9	COc1cccc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(Cl)cccc3Cl)c3ccccc32)c1	10.1021/jm031115r
	CHEMBL94602	214304	0	None	11	2	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	576	8	2	5	5.9	COc1cccc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(Cl)cccc3Cl)c3ccccc32)c1	10.1021/jm031115r
	10140418	112978	0	None	43	2	Human	7.9	pIC50	=	7.9	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	476	7	3	7	1.9	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CC(=O)O)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL313867	112978	0	None	43	2	Human	7.9	pIC50	=	7.9	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	476	7	3	7	1.9	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CC(=O)O)c3ccccc32)n1	10.1021/jm031115r
	11308052	119442	0	None	2	2	Human	7.9	pIC50	=	7.9	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	618	10	2	6	5.8	CCCCc1cccc([C@]2([C@H](Oc3nc(C)cc(C)n3)C(=O)O)NCC(=O)N(Cc3c(F)cc(F)cc3F)c3ccccc32)c1	10.1021/jm031115r
	CHEMBL330354	119442	0	None	2	2	Human	7.9	pIC50	=	7.9	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	618	10	2	6	5.8	CCCCc1cccc([C@]2([C@H](Oc3nc(C)cc(C)n3)C(=O)O)NCC(=O)N(Cc3c(F)cc(F)cc3F)c3ccccc32)c1	10.1021/jm031115r
	122194934	130871	0	None	-	1	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at human ETA receptor expressed in CHO cells assessed as inhibition of ET-1-induced Ca2+ efflux from endoplasmic reticulum into cytosol by fluo-4 dye-based FLIPR assayAntagonist activity at human ETA receptor expressed in CHO cells assessed as inhibition of ET-1-induced Ca2+ efflux from endoplasmic reticulum into cytosol by fluo-4 dye-based FLIPR assay	ChEMBL	561	10	2	8	5.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(F)(F)F)cc2)cc(-c2ncccn2)cc1OCCO	10.1021/acs.jmedchem.5b00258
	CHEMBL3633039	130871	0	None	-	1	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at human ETA receptor expressed in CHO cells assessed as inhibition of ET-1-induced Ca2+ efflux from endoplasmic reticulum into cytosol by fluo-4 dye-based FLIPR assayAntagonist activity at human ETA receptor expressed in CHO cells assessed as inhibition of ET-1-induced Ca2+ efflux from endoplasmic reticulum into cytosol by fluo-4 dye-based FLIPR assay	ChEMBL	561	10	2	8	5.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(F)(F)F)cc2)cc(-c2ncccn2)cc1OCCO	10.1021/acs.jmedchem.5b00258
	CHEMBL97470	222704	0	None	-1	2	Human	6.9	pIC50	=	6.9	Functional	Inhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cellsInhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	CHEMBL3143473	218113	0	None	-1071	2	Human	5.9	pIC50	=	5.9	Functional	Antagonistic activity against endothelin A (ETA) receptor using human neuroblastoma cell line.Antagonistic activity against endothelin A (ETA) receptor using human neuroblastoma cell line.	ChEMBL		None	None	None		CCCC[C@@H](NC(=O)[C@@H](Cc1cn(COC)c2ccccc12)NC(=O)[C@H](CC(C)(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1016/0960-894X(95)00084-7
	CHEMBL3305972	218113	0	None	-1071	2	Human	5.9	pIC50	=	5.9	Functional	Antagonistic activity against endothelin A (ETA) receptor using human neuroblastoma cell line.Antagonistic activity against endothelin A (ETA) receptor using human neuroblastoma cell line.	ChEMBL		None	None	None		CCCC[C@@H](NC(=O)[C@@H](Cc1cn(COC)c2ccccc12)NC(=O)[C@H](CC(C)(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1016/0960-894X(95)00084-7
	345351	16131	4	None	24	3	Human	5.9	pIC50	=	5.9	Functional	Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.	ChEMBL	386	4	1	5	3.8	O=C1OC(O)(c2ccccc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2	10.1021/jm00008a002
	CHEMBL11131	16131	4	None	24	3	Human	5.9	pIC50	=	5.9	Functional	Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.	ChEMBL	386	4	1	5	3.8	O=C1OC(O)(c2ccccc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2	10.1021/jm00008a002
	44332623	11538	1	None	-	1	Human	4.9	pIC50	=	4.9	Functional	Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.	ChEMBL	320	3	1	4	2.9	Cc1cc(C(C(N)=O)c2ccc3c(c2)OCO3)c2ccccc2n1	10.1016/S0960-894X(96)00551-3
	CHEMBL103886	11538	1	None	-	1	Human	4.9	pIC50	=	4.9	Functional	Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.	ChEMBL	320	3	1	4	2.9	Cc1cc(C(C(N)=O)c2ccc3c(c2)OCO3)c2ccccc2n1	10.1016/S0960-894X(96)00551-3
	CHEMBL405599	219347	0	None	1	3	Human	7.9	pIC50	=	7.9	Functional	Inhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cellsInhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	11744509	12202	0	None	5	2	Human	6.9	pIC50	=	6.9	Functional	Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.	ChEMBL	450	5	1	6	4.5	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(Cl)cc2)cc1	10.1021/jm00008a002
	CHEMBL10733	12202	0	None	5	2	Human	6.9	pIC50	=	6.9	Functional	Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.	ChEMBL	450	5	1	6	4.5	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(Cl)cc2)cc1	10.1021/jm00008a002
	11386977	214326	0	None	1	2	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	528	8	2	6	4.8	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CCC3CCCCC3)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL94752	214326	0	None	1	2	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	528	8	2	6	4.8	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CCC3CCCCC3)c3ccccc32)n1	10.1021/jm031115r
	11226767	214305	0	None	6	2	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	560	7	2	4	6.2	Cc1ccc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(Cl)cccc3Cl)c3ccccc32)cc1	10.1021/jm031115r
	CHEMBL94606	214305	0	None	6	2	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	560	7	2	4	6.2	Cc1ccc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(Cl)cccc3Cl)c3ccccc32)cc1	10.1021/jm031115r
	11452452	213981	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	404	5	2	6	1.8	CN1C(=O)CN[C@](c2ccccc2)([C@H](Oc2ncccn2)C(=O)O)c2ccccc21	10.1021/jm031115r
	CHEMBL92612	213981	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	404	5	2	6	1.8	CN1C(=O)CN[C@](c2ccccc2)([C@H](Oc2ncccn2)C(=O)O)c2ccccc21	10.1021/jm031115r
	CHEMBL284250	217639	0	None	-19	4	Human	7.8	pIC50	=	7.8	Functional	Functional inhibition of ET-1 induced [Ca2+] increase in human neuroblastoma-derived SK-N-MC cells, which express Endothelin A receptorFunctional inhibition of ET-1 induced [Ca2+] increase in human neuroblastoma-derived SK-N-MC cells, which express Endothelin A receptor	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)[C@@H](NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O	10.1016/0960-894X(95)00237-N
	11331242	114197	0	None	1	2	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	652	8	2	6	7.0	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3cccc(-c4ccccc4)c3)NCC(=O)N(Cc3c(Cl)cccc3Cl)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL318086	114197	0	None	1	2	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	652	8	2	6	7.0	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3cccc(-c4ccccc4)c3)NCC(=O)N(Cc3c(Cl)cccc3Cl)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL265116	217414	0	None	-3	3	Human	6.8	pIC50	=	6.8	Functional	Inhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cellsInhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1021/jm00015a003
	CHEMBL4533479	220765	1	None	-1	2	Human	5.8	pIC50	=	5.8	Functional	Eurofins cellular functional assay - Antagonist (EDNRA)Eurofins cellular functional assay - Antagonist (EDNRA)	ChEMBL		None	None	None		CCCOc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(CC)cccc2CC)cc1	10.6019/CHEMBL4507261
	10166981	213867	0	None	2	2	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	576	7	2	6	5.0	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(C(F)(F)F)cc3)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL91926	213867	0	None	2	2	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	576	7	2	6	5.0	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(C(F)(F)F)cc3)c3ccccc32)n1	10.1021/jm031115r
	11410074	214569	0	None	1	2	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	536	9	2	6	4.4	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CCCc3ccccc3)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL96114	214569	0	None	1	2	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	536	9	2	6	4.4	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CCCc3ccccc3)c3ccccc32)n1	10.1021/jm031115r
	11365059	214574	0	None	1	2	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	564	7	2	6	5.3	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(C(C)(C)C)cc3)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL96154	214574	0	None	1	2	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	564	7	2	6	5.3	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(C(C)(C)C)cc3)c3ccccc32)n1	10.1021/jm031115r
	10347783	214613	0	None	32	2	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	560	7	2	4	5.6	Cc1cc(C)cc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(F)cc(F)cc3F)c3ccccc32)c1	10.1021/jm031115r
	CHEMBL96347	214613	0	None	32	2	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	560	7	2	4	5.6	Cc1cc(C)cc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(F)cc(F)cc3F)c3ccccc32)c1	10.1021/jm031115r
	11753090	112980	0	None	7	2	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	542	7	2	6	4.7	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(Cl)cc3)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL313870	112980	0	None	7	2	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	542	7	2	6	4.7	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(Cl)cc3)c3ccccc32)n1	10.1021/jm031115r
	10412464	15909	0	None	11	2	Human	6.8	pIC50	=	6.8	Functional	Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK	ChEMBL	470	6	1	5	5.4	COc1ccc(CC2=C(c3ccc(Cl)c(Cl)c3)C(=O)OC2(O)c2ccc(OC)cc2)cc1	10.1021/jm00008a002
	CHEMBL10996	15909	0	None	11	2	Human	6.8	pIC50	=	6.8	Functional	Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK	ChEMBL	470	6	1	5	5.4	COc1ccc(CC2=C(c3ccc(Cl)c(Cl)c3)C(=O)OC2(O)c2ccc(OC)cc2)cc1	10.1021/jm00008a002
	44327656	148567	0	None	-1	2	Human	5.8	pIC50	=	5.8	Functional	Inhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cellsInhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cells	ChEMBL	977	25	9	8	4.7	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C(F)(F)F)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	CHEMBL386181	148567	0	None	-1	2	Human	5.8	pIC50	=	5.8	Functional	Inhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cellsInhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cells	ChEMBL	977	25	9	8	4.7	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C(F)(F)F)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	11330923	214601	0	None	-1	2	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	606	10	2	6	6.3	CCCCc1cccc([C@]2([C@H](Oc3nc(C)cc(C)n3)C(=O)O)NCC(=O)N(Cc3c(C)cc(C)cc3C)c3ccccc32)c1	10.1021/jm031115r
	CHEMBL96303	214601	0	None	-1	2	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	606	10	2	6	6.3	CCCCc1cccc([C@]2([C@H](Oc3nc(C)cc(C)n3)C(=O)O)NCC(=O)N(Cc3c(C)cc(C)cc3C)c3ccccc32)c1	10.1021/jm031115r
	11226740	214681	0	None	9	2	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	558	7	2	4	6.0	Cc1cc(C)cc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(F)cccc3Cl)c3ccccc32)c1	10.1021/jm031115r
	CHEMBL96704	214681	0	None	9	2	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	558	7	2	4	6.0	Cc1cc(C)cc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(F)cccc3Cl)c3ccccc32)c1	10.1021/jm031115r
	CHEMBL408574	219501	0	None	-	1	Pig	7.7	pIC50	=	7.7	Functional	Antagonist activity against ET-A from porcine heart membranesAntagonist activity against ET-A from porcine heart membranes	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(95)00349-X
	10410546	16184	0	None	37	2	Human	6.7	pIC50	=	6.7	Functional	Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK	ChEMBL	432	7	1	6	4.1	COc1ccc(CC2=C(c3ccc(OC)cc3)C(=O)OC2(O)c2ccc(OC)cc2)cc1	10.1021/jm00008a002
	CHEMBL11162	16184	0	None	37	2	Human	6.7	pIC50	=	6.7	Functional	Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK	ChEMBL	432	7	1	6	4.1	COc1ccc(CC2=C(c3ccc(OC)cc3)C(=O)OC2(O)c2ccc(OC)cc2)cc1	10.1021/jm00008a002
	CHEMBL319537	217998	0	None	2	2	Human	5.7	pIC50	=	5.7	Functional	Inhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cellsInhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	CHEMBL409808	219565	0	None	-	1	Pig	8.7	pIC50	=	8.7	Functional	Antagonist activity against ET-A from porcine heart membranesAntagonist activity against ET-A from porcine heart membranes	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(95)00349-X
	10120430	214299	0	None	5	2	Human	8.6	pIC50	=	8.6	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	562	7	2	6	4.4	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(F)ccc(F)c3F)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL94580	214299	0	None	5	2	Human	8.6	pIC50	=	8.6	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	562	7	2	6	4.4	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(F)ccc(F)c3F)c3ccccc32)n1	10.1021/jm031115r
	9890440	15026	0	None	301	2	Human	8.6	pIC50	=	8.6	Functional	Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK	ChEMBL	460	6	1	7	4.1	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(OC)c(C)c2)cc1	10.1021/jm00008a002
	CHEMBL10924	15026	0	None	301	2	Human	8.6	pIC50	=	8.6	Functional	Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK	ChEMBL	460	6	1	7	4.1	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(OC)c(C)c2)cc1	10.1021/jm00008a002
	10166543	119139	0	None	33	2	Human	8.6	pIC50	=	8.6	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	562	7	2	6	4.4	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(F)cc(F)cc3F)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL329477	119139	0	None	33	2	Human	8.6	pIC50	=	8.6	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	562	7	2	6	4.4	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(F)cc(F)cc3F)c3ccccc32)n1	10.1021/jm031115r
	10282008	213860	0	None	12	2	Human	8.6	pIC50	=	8.6	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	592	8	2	7	4.9	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(OC(F)(F)F)cc3)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL91873	213860	0	None	12	2	Human	8.6	pIC50	=	8.6	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	592	8	2	7	4.9	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(OC(F)(F)F)cc3)c3ccccc32)n1	10.1021/jm031115r
	11224973	114227	0	None	32	2	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	460	7	2	6	2.9	CCc1cc(CC)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL318270	114227	0	None	32	2	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	460	7	2	6	2.9	CCc1cc(CC)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3ccccc32)n1	10.1021/jm031115r
	11169125	214338	0	None	5	2	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	574	7	2	4	6.5	Cc1cc(C)cc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(Cl)cccc3Cl)c3ccccc32)c1	10.1021/jm031115r
	CHEMBL94802	214338	0	None	5	2	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	574	7	2	4	6.5	Cc1cc(C)cc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(Cl)cccc3Cl)c3ccccc32)c1	10.1021/jm031115r
	CHEMBL263295	217344	0	None	-1	2	Human	6.7	pIC50	=	6.7	Functional	Inhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cellsInhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1021/jm00015a003
	10024044	14611	0	None	-	1	Human	5.7	pIC50	=	5.7	Functional	Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.	ChEMBL	402	6	1	5	4.1	COc1ccc(CC2=C(c3ccccc3)C(=O)OC2(O)c2ccc(OC)cc2)cc1	10.1021/jm00008a002
	CHEMBL10897	14611	0	None	-	1	Human	5.7	pIC50	=	5.7	Functional	Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.	ChEMBL	402	6	1	5	4.1	COc1ccc(CC2=C(c3ccccc3)C(=O)OC2(O)c2ccc(OC)cc2)cc1	10.1021/jm00008a002
	44332577	11478	0	None	-	1	Human	4.7	pIC50	=	4.7	Functional	Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.	ChEMBL	341	3	0	4	4.4	O=CC(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12	10.1016/S0960-894X(96)00551-3
	CHEMBL103484	11478	0	None	-	1	Human	4.7	pIC50	=	4.7	Functional	Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.	ChEMBL	341	3	0	4	4.4	O=CC(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12	10.1016/S0960-894X(96)00551-3
	CHEMBL2373086	217151	0	None	-	1	Pig	7.7	pIC50	=	7.7	Functional	Antagonist activity against ET-A from porcine heart membranesAntagonist activity against ET-A from porcine heart membranes	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)[C@@H](C)CC)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(95)00349-X
	3951	7179	86	None	47	2	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	378	7	1	5	3.5	COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1	10.1021/jm031115r
	4337	7179	86	None	47	2	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	378	7	1	5	3.5	COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1	10.1021/jm031115r
	6918493	7179	86	None	47	2	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	378	7	1	5	3.5	COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1	10.1021/jm031115r
	CHEMBL1111	7179	86	None	47	2	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	378	7	1	5	3.5	COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1	10.1021/jm031115r
	DB06403	7179	86	None	47	2	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	378	7	1	5	3.5	COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1	10.1021/jm031115r
	CHEMBL317099	217977	0	None	-69	2	Human	5.7	pIC50	=	5.7	Functional	Inhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cellsInhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	CHEMBL96822	222699	0	None	-1	2	Human	5.7	pIC50	=	5.7	Functional	Inhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cellsInhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NS(C)(=O)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	11786120	175947	0	None	17	2	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	546	7	2	4	5.9	O=C(O)[C@@H](Oc1ccccc1)[C@@]1(c2ccccc2)NCC(=O)N(Cc2c(Cl)cccc2Cl)c2ccccc21	10.1021/jm031115r
	CHEMBL440507	175947	0	None	17	2	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	546	7	2	4	5.9	O=C(O)[C@@H](Oc1ccccc1)[C@@]1(c2ccccc2)NCC(=O)N(Cc2c(Cl)cccc2Cl)c2ccccc21	10.1021/jm031115r
	70692693	82990	0	None	-1	2	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cellsAntagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cells	ChEMBL	500	8	1	6	6.1	CCCc1nc2ccccc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1016/j.bmc.2012.06.011
	CHEMBL2058369	82990	0	None	-1	2	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cellsAntagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cells	ChEMBL	500	8	1	6	6.1	CCCc1nc2ccccc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1016/j.bmc.2012.06.011
	10385531	119459	0	None	-	1	Human	5.7	pIC50	=	5.7	Functional	Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.	ChEMBL	387	4	0	6	4.4	COC(=O)C(Oc1c2ccccc2nc2ccccc12)c1ccc2c(c1)OCO2	10.1016/S0960-894X(96)00551-3
	CHEMBL330414	119459	0	None	-	1	Human	5.7	pIC50	=	5.7	Functional	Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.	ChEMBL	387	4	0	6	4.4	COC(=O)C(Oc1c2ccccc2nc2ccccc12)c1ccc2c(c1)OCO2	10.1016/S0960-894X(96)00551-3
	10024044	14611	0	None	-	1	Human	5.7	pIC50	=	5.7	Functional	Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK	ChEMBL	402	6	1	5	4.1	COc1ccc(CC2=C(c3ccccc3)C(=O)OC2(O)c2ccc(OC)cc2)cc1	10.1021/jm00008a002
	CHEMBL10897	14611	0	None	-	1	Human	5.7	pIC50	=	5.7	Functional	Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK	ChEMBL	402	6	1	5	4.1	COc1ccc(CC2=C(c3ccccc3)C(=O)OC2(O)c2ccc(OC)cc2)cc1	10.1021/jm00008a002
	10070783	103831	0	None	3	3	Human	5.7	pIC50	=	5.7	Functional	Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.	ChEMBL	420	4	1	5	4.5	O=C1OC(O)(c2ccc(Cl)cc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2	10.1021/jm00008a002
	CHEMBL267094	103831	0	None	3	3	Human	5.7	pIC50	=	5.7	Functional	Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.	ChEMBL	420	4	1	5	4.5	O=C1OC(O)(c2ccc(Cl)cc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2	10.1021/jm00008a002
	11387315	214213	0	None	-1	2	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	552	8	2	7	4.3	COc1ccc(CN2C(=O)CN[C@](c3ccc(C)cc3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1	10.1021/jm031115r
	CHEMBL94091	214213	0	None	-1	2	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	552	8	2	7	4.3	COc1ccc(CN2C(=O)CN[C@](c3ccc(C)cc3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1	10.1021/jm031115r
	11408654	214715	0	None	19	2	Human	7.6	pIC50	=	7.6	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	464	7	2	8	1.8	COc1cc(OC)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL96906	214715	0	None	19	2	Human	7.6	pIC50	=	7.6	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	464	7	2	8	1.8	COc1cc(OC)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3ccccc32)n1	10.1021/jm031115r
	11409474	214339	0	None	1	2	Human	7.6	pIC50	=	7.6	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	502	10	2	6	4.4	CCCCCCN1C(=O)CN[C@](c2ccccc2)([C@H](Oc2nc(C)cc(C)n2)C(=O)O)c2ccccc21	10.1021/jm031115r
	CHEMBL94810	214339	0	None	1	2	Human	7.6	pIC50	=	7.6	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	502	10	2	6	4.4	CCCCCCN1C(=O)CN[C@](c2ccccc2)([C@H](Oc2nc(C)cc(C)n2)C(=O)O)c2ccccc21	10.1021/jm031115r
	44327659	116599	0	None	-1	2	Human	6.6	pIC50	=	6.6	Functional	Inhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cellsInhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cells	ChEMBL	937	26	9	8	4.6	CCC(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC)[C@@H](C)CC)C(c1ccccc1)c1ccccc1	10.1021/jm00015a003
	CHEMBL323331	116599	0	None	-1	2	Human	6.6	pIC50	=	6.6	Functional	Inhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cellsInhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cells	ChEMBL	937	26	9	8	4.6	CCC(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC)[C@@H](C)CC)C(c1ccccc1)c1ccccc1	10.1021/jm00015a003
	CHEMBL263186	217341	0	None	-	1	Pig	7.6	pIC50	=	7.6	Functional	Antagonist activity against ET-A from porcine heart membranesAntagonist activity against ET-A from porcine heart membranes	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(95)00349-X
	9896251	105549	0	None	-1	3	Human	7.6	pIC50	=	7.6	Functional	Antagonist activity at endothelin receptor subtype AAntagonist activity at endothelin receptor subtype A	ChEMBL	682	12	1	9	7.1	CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2	10.1016/j.bmc.2012.06.011
	CHEMBL278176	105549	0	None	-1	3	Human	7.6	pIC50	=	7.6	Functional	Antagonist activity at endothelin receptor subtype AAntagonist activity at endothelin receptor subtype A	ChEMBL	682	12	1	9	7.1	CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2	10.1016/j.bmc.2012.06.011
	11467573	114017	0	None	9	2	Human	7.6	pIC50	=	7.6	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	606	8	2	7	5.0	COc1ccc(CN2C(=O)CN[C@](c3cccc(C(F)(F)F)c3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1	10.1021/jm031115r
	CHEMBL316851	114017	0	None	9	2	Human	7.6	pIC50	=	7.6	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	606	8	2	7	5.0	COc1ccc(CN2C(=O)CN[C@](c3cccc(C(F)(F)F)c3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1	10.1021/jm031115r
	11238500	214603	0	None	3	2	Human	7.6	pIC50	=	7.6	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	572	8	2	7	4.7	COc1ccc(CN2C(=O)CN[C@](c3cccc(Cl)c3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1	10.1021/jm031115r
	CHEMBL96313	214603	0	None	3	2	Human	7.6	pIC50	=	7.6	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	572	8	2	7	4.7	COc1ccc(CN2C(=O)CN[C@](c3cccc(Cl)c3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1	10.1021/jm031115r
	11753582	214367	0	None	4	2	Human	7.6	pIC50	=	7.6	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	586	7	2	6	4.8	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(Br)cc3)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL94962	214367	0	None	4	2	Human	7.6	pIC50	=	7.6	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	586	7	2	6	4.8	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(Br)cc3)c3ccccc32)n1	10.1021/jm031115r
	11397857	214570	0	None	6	2	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	496	7	2	6	3.7	COc1cc(OC)cc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3ccc(Cl)cc32)c1	10.1021/jm031115r
	CHEMBL96125	214570	0	None	6	2	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	496	7	2	6	3.7	COc1cc(OC)cc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3ccc(Cl)cc32)c1	10.1021/jm031115r
	11489946	214126	0	None	2	2	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	566	8	2	7	4.6	COc1ccc(CN2C(=O)CN[C@](c3cc(C)cc(C)c3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1	10.1021/jm031115r
	CHEMBL93612	214126	0	None	2	2	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	566	8	2	7	4.6	COc1ccc(CN2C(=O)CN[C@](c3cc(C)cc(C)c3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1	10.1021/jm031115r
	CHEMBL433406	220419	0	None	-9	2	Human	6.6	pIC50	=	6.6	Functional	Inhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cellsInhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)NC)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	44332803	11479	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.	ChEMBL	335	3	0	5	3.6	COC(=O)C(c1ccc2c(c1)OCO2)c1cc(C)nc2ccccc12	10.1016/S0960-894X(96)00551-3
	CHEMBL103497	11479	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.	ChEMBL	335	3	0	5	3.6	COC(=O)C(c1ccc2c(c1)OCO2)c1cc(C)nc2ccccc12	10.1016/S0960-894X(96)00551-3
	9820754	115339	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.	ChEMBL	371	3	0	5	4.4	COC(=O)C(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12	10.1016/S0960-894X(96)00551-3
	CHEMBL320236	115339	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.	ChEMBL	371	3	0	5	4.4	COC(=O)C(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12	10.1016/S0960-894X(96)00551-3
	11410410	214329	0	None	25	2	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	560	7	2	4	6.2	Cc1cccc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(Cl)cccc3Cl)c3ccccc32)c1	10.1021/jm031115r
	CHEMBL94769	214329	0	None	25	2	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	560	7	2	4	6.2	Cc1cccc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(Cl)cccc3Cl)c3ccccc32)c1	10.1021/jm031115r
	CHEMBL319660	217999	0	None	2	2	Human	7.5	pIC50	=	7.5	Functional	Inhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cellsInhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1021/jm00015a003
	CHEMBL410694	219613	0	None	-	1	Pig	8.5	pIC50	=	8.5	Functional	Antagonist activity against ET-A from porcine heart membranesAntagonist activity against ET-A from porcine heart membranes	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(95)00349-X
	CHEMBL411965	219745	0	None	-	1	Pig	8.5	pIC50	=	8.5	Functional	Antagonist activity against ET-A from porcine heart membranesAntagonist activity against ET-A from porcine heart membranes	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(95)00349-X
	11387934	113954	0	None	28	2	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	614	9	2	7	5.7	COc1ccc(CN2C(=O)CN[C@](c3cccc(-c4ccccc4)c3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1	10.1021/jm031115r
	CHEMBL316453	113954	0	None	28	2	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	614	9	2	7	5.7	COc1ccc(CN2C(=O)CN[C@](c3cccc(-c4ccccc4)c3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1	10.1021/jm031115r
	11353580	214717	0	None	21	2	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	566	9	2	7	4.6	CCc1cccc([C@]2([C@H](Oc3nc(C)cc(C)n3)C(=O)O)NCC(=O)N(Cc3ccc(OC)cc3)c3ccccc32)c1	10.1021/jm031115r
	CHEMBL96932	214717	0	None	21	2	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	566	9	2	7	4.6	CCc1cccc([C@]2([C@H](Oc3nc(C)cc(C)n3)C(=O)O)NCC(=O)N(Cc3ccc(OC)cc3)c3ccccc32)c1	10.1021/jm031115r
	10303258	168654	0	None	3	2	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	564	10	2	6	5.3	CCCCc1ccc(CN2C(=O)CN[C@](c3ccccc3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1	10.1021/jm031115r
	CHEMBL415010	168654	0	None	3	2	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	564	10	2	6	5.3	CCCCc1ccc(CN2C(=O)CN[C@](c3ccccc3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1	10.1021/jm031115r
	11168474	214684	0	None	9	2	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	526	7	2	6	4.1	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccccc3F)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL96723	214684	0	None	9	2	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	526	7	2	6	4.1	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccccc3F)c3ccccc32)n1	10.1021/jm031115r
	11421392	214164	0	None	5	2	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	544	7	2	6	4.3	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cccc(F)c3F)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL93820	214164	0	None	5	2	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	544	7	2	6	4.3	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cccc(F)c3F)c3ccccc32)n1	10.1021/jm031115r
	11489318	214578	0	None	5	2	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	522	8	2	6	4.0	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CCc3ccccc3)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL96171	214578	0	None	5	2	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	522	8	2	6	4.0	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CCc3ccccc3)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL94983	222695	0	None	7	2	Human	7.5	pIC50	=	7.5	Functional	Inhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cellsInhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCN)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	11398818	174710	0	None	2	2	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	556	8	2	7	4.2	COc1ccc(CN2C(=O)CN[C@](c3ccccc3F)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1	10.1021/jm031115r
	CHEMBL431460	174710	0	None	2	2	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	556	8	2	7	4.2	COc1ccc(CN2C(=O)CN[C@](c3ccccc3F)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1	10.1021/jm031115r
	11156692	174655	0	None	2	2	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	522	7	2	6	4.3	Cc1ccc(CN2C(=O)CN[C@](c3ccccc3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1	10.1021/jm031115r
	CHEMBL431087	174655	0	None	2	2	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	522	7	2	6	4.3	Cc1ccc(CN2C(=O)CN[C@](c3ccccc3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1	10.1021/jm031115r
	10412464	15909	0	None	11	2	Human	6.5	pIC50	=	6.5	Functional	Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.	ChEMBL	470	6	1	5	5.4	COc1ccc(CC2=C(c3ccc(Cl)c(Cl)c3)C(=O)OC2(O)c2ccc(OC)cc2)cc1	10.1021/jm00008a002
	CHEMBL10996	15909	0	None	11	2	Human	6.5	pIC50	=	6.5	Functional	Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.	ChEMBL	470	6	1	5	5.4	COc1ccc(CC2=C(c3ccc(Cl)c(Cl)c3)C(=O)OC2(O)c2ccc(OC)cc2)cc1	10.1021/jm00008a002
	10410546	16184	0	None	37	2	Human	6.5	pIC50	=	6.5	Functional	Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.	ChEMBL	432	7	1	6	4.1	COc1ccc(CC2=C(c3ccc(OC)cc3)C(=O)OC2(O)c2ccc(OC)cc2)cc1	10.1021/jm00008a002
	CHEMBL11162	16184	0	None	37	2	Human	6.5	pIC50	=	6.5	Functional	Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.	ChEMBL	432	7	1	6	4.1	COc1ccc(CC2=C(c3ccc(OC)cc3)C(=O)OC2(O)c2ccc(OC)cc2)cc1	10.1021/jm00008a002
	15289330	106578	0	None	18	2	Human	7.5	pIC50	=	7.5	Functional	Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin A receptor.Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin A receptor.	ChEMBL	493	8	1	8	5.3	COc1cccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc(OC)c(OC)cc23)c1	10.1016/0960-894X(96)00232-6
	CHEMBL285368	106578	0	None	18	2	Human	7.5	pIC50	=	7.5	Functional	Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin A receptor.Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin A receptor.	ChEMBL	493	8	1	8	5.3	COc1cccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc(OC)c(OC)cc23)c1	10.1016/0960-894X(96)00232-6
	CHEMBL97431	222703	0	None	2	2	Human	6.5	pIC50	=	6.5	Functional	Inhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cellsInhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1021/jm00015a003
	18995989	107331	0	None	-2	2	Human	5.5	pIC50	=	5.5	Functional	Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin A receptor.Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin A receptor.	ChEMBL	583	9	1	9	6.6	COc1cc2c(Sc3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OCc1ccccc1	10.1016/0960-894X(96)00232-6
	CHEMBL29147	107331	0	None	-2	2	Human	5.5	pIC50	=	5.5	Functional	Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin A receptor.Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin A receptor.	ChEMBL	583	9	1	9	6.6	COc1cc2c(Sc3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OCc1ccccc1	10.1016/0960-894X(96)00232-6
	11307120	119181	0	None	-4	2	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	532	11	2	7	4.5	CCCCC[C@]1([C@H](Oc2nc(C)cc(C)n2)C(=O)O)NCC(=O)N(Cc2ccc(OC)cc2)c2ccccc21	10.1021/jm031115r
	CHEMBL329744	119181	0	None	-4	2	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	532	11	2	7	4.5	CCCCC[C@]1([C@H](Oc2nc(C)cc(C)n2)C(=O)O)NCC(=O)N(Cc2ccc(OC)cc2)c2ccccc21	10.1021/jm031115r
	1009	6982	25	None	-1621	2	Human	5.4	pIC50	=	5.4	Functional	Eurofins cellular functional assay - Antagonist (EDNRA)Eurofins cellular functional assay - Antagonist (EDNRA)	ChEMBL	558	11	2	6	5.8	CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2	10.6019/CHEMBL4507261
	5310991	6982	25	None	-1621	2	Human	5.4	pIC50	=	5.4	Functional	Eurofins cellular functional assay - Antagonist (EDNRA)Eurofins cellular functional assay - Antagonist (EDNRA)	ChEMBL	558	11	2	6	5.8	CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2	10.6019/CHEMBL4507261
	CHEMBL332794	6982	25	None	-1621	2	Human	5.4	pIC50	=	5.4	Functional	Eurofins cellular functional assay - Antagonist (EDNRA)Eurofins cellular functional assay - Antagonist (EDNRA)	ChEMBL	558	11	2	6	5.8	CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2	10.6019/CHEMBL4507261
	11362537	114298	0	None	24	2	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	434	6	2	7	1.8	COc1cnc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3ccccc32)nc1	10.1021/jm031115r
	CHEMBL318683	114298	0	None	24	2	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	434	6	2	7	1.8	COc1cnc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3ccccc32)nc1	10.1021/jm031115r
	11167889	214614	0	None	1	2	Human	5.4	pIC50	=	5.4	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	496	7	2	6	3.7	COc1cc(OC)cc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3cc(Cl)ccc32)c1	10.1021/jm031115r
	CHEMBL96351	214614	0	None	1	2	Human	5.4	pIC50	=	5.4	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	496	7	2	6	3.7	COc1cc(OC)cc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3cc(Cl)ccc32)c1	10.1021/jm031115r
	11752174	179504	0	None	4	2	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	489	8	2	7	2.4	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CCN(C)C)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL450628	179504	0	None	4	2	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	489	8	2	7	2.4	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CCN(C)C)c3ccccc32)n1	10.1021/jm031115r
	70686381	82989	0	None	-1	2	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cellsAntagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cells	ChEMBL	486	7	1	6	5.7	CCc1nc2ccccc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1016/j.bmc.2012.06.011
	CHEMBL2058368	82989	0	None	-1	2	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cellsAntagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cells	ChEMBL	486	7	1	6	5.7	CCc1nc2ccccc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1016/j.bmc.2012.06.011
	11785180	118285	0	None	1	2	Human	5.4	pIC50	=	5.4	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	492	8	2	7	3.1	COc1cc(OC)cc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3cc(OC)ccc32)c1	10.1021/jm031115r
	CHEMBL327823	118285	0	None	1	2	Human	5.4	pIC50	=	5.4	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	492	8	2	7	3.1	COc1cc(OC)cc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3cc(OC)ccc32)c1	10.1021/jm031115r
	CHEMBL1790448	215667	0	None	-	1	Pig	8.4	pIC50	=	8.4	Functional	Antagonist activity against ET-A from porcine heart membranesAntagonist activity against ET-A from porcine heart membranes	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)[C@H](C)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(95)00349-X
	CHEMBL293029	217667	0	None	-	1	Pig	8.4	pIC50	=	8.4	Functional	Antagonist activity against ET-A from porcine heart membranesAntagonist activity against ET-A from porcine heart membranes	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/0960-894X(95)00349-X
	CHEMBL410869	219626	0	None	-	1	Pig	8.4	pIC50	=	8.4	Functional	Antagonist activity against ET-A from porcine heart membranesAntagonist activity against ET-A from porcine heart membranes	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(95)00349-X
	10230546	114024	0	None	4	2	Human	8.3	pIC50	=	8.3	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	538	8	2	7	4.0	COc1ccc(CN2C(=O)CN[C@](c3ccccc3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1	10.1021/jm031115r
	CHEMBL316878	114024	0	None	4	2	Human	8.3	pIC50	=	8.3	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	538	8	2	7	4.0	COc1ccc(CN2C(=O)CN[C@](c3ccccc3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1	10.1021/jm031115r
	9807691	106840	0	None	134	2	Human	8.3	pIC50	=	8.3	Functional	Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin A receptor.Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin A receptor.	ChEMBL	553	10	1	10	5.3	COc1cc2c(Sc3cc(OC)c(OC)c(OC)c3)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC	10.1016/0960-894X(96)00232-6
	CHEMBL287169	106840	0	None	134	2	Human	8.3	pIC50	=	8.3	Functional	Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin A receptor.Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin A receptor.	ChEMBL	553	10	1	10	5.3	COc1cc2c(Sc3cc(OC)c(OC)c(OC)c3)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC	10.1016/0960-894X(96)00232-6
	44304492	103335	0	None	1	4	Human	8.3	pIC50	=	8.3	Functional	Inhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cellsInhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cells	ChEMBL	949	23	9	8	4.3	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	CHEMBL262993	103335	0	None	1	4	Human	8.3	pIC50	=	8.3	Functional	Inhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cellsInhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cells	ChEMBL	949	23	9	8	4.3	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	10027018	105265	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK	ChEMBL	454	4	1	5	5.1	O=C1OC(O)(c2ccc(Cl)c(Cl)c2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2	10.1021/jm00008a002
	CHEMBL275991	105265	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK	ChEMBL	454	4	1	5	5.1	O=C1OC(O)(c2ccc(Cl)c(Cl)c2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2	10.1021/jm00008a002
	CHEMBL94907	222693	0	None	1	2	Human	6.4	pIC50	=	6.4	Functional	Inhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cellsInhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1021/jm00015a003
	10070783	103831	0	None	3	3	Human	6.4	pIC50	=	6.4	Functional	Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK	ChEMBL	420	4	1	5	4.5	O=C1OC(O)(c2ccc(Cl)cc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2	10.1021/jm00008a002
	CHEMBL267094	103831	0	None	3	3	Human	6.4	pIC50	=	6.4	Functional	Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK	ChEMBL	420	4	1	5	4.5	O=C1OC(O)(c2ccc(Cl)cc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2	10.1021/jm00008a002
	CHEMBL2370255	216598	0	None	-13	2	Human	6.4	pIC50	=	6.4	Functional	Inhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cellsInhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	CHEMBL433349	220416	0	None	-1	3	Human	6.4	pIC50	=	6.4	Functional	Inhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cellsInhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	CHEMBL2370254	216597	0	None	2	2	Human	5.4	pIC50	=	5.4	Functional	Inhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cellsInhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	11168401	119081	0	None	18	2	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	522	9	2	8	3.1	COc1cc(OC)cc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3cc(OC)c(OC)cc32)c1	10.1021/jm031115r
	CHEMBL329132	119081	0	None	18	2	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	522	9	2	8	3.1	COc1cc(OC)cc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3cc(OC)c(OC)cc32)c1	10.1021/jm031115r
	11156376	119443	0	None	5	2	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	504	9	3	7	2.7	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CCCC(=O)O)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL330359	119443	0	None	5	2	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	504	9	3	7	2.7	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CCCC(=O)O)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL318020	217988	0	None	8	2	Human	6.4	pIC50	=	6.4	Functional	Inhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cellsInhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1021/jm00015a003
	11330927	214286	0	None	8	2	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	606	9	2	6	5.9	COc1cc(OC)cc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(Cl)cccc3Cl)c3ccccc32)c1	10.1021/jm031115r
	CHEMBL94488	214286	0	None	8	2	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	606	9	2	6	5.9	COc1cc(OC)cc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(Cl)cccc3Cl)c3ccccc32)c1	10.1021/jm031115r
	10385531	119459	0	None	-	1	Human	5.3	pIC50	=	5.3	Functional	Compound was tested for its ability to inhibit Endothelin A receptor induced arachidonic acid release(AARA) in rabbit renal artery vascular smooth muscles.Compound was tested for its ability to inhibit Endothelin A receptor induced arachidonic acid release(AARA) in rabbit renal artery vascular smooth muscles.	ChEMBL	387	4	0	6	4.4	COC(=O)C(Oc1c2ccccc2nc2ccccc12)c1ccc2c(c1)OCO2	10.1016/S0960-894X(96)00551-3
	CHEMBL330414	119459	0	None	-	1	Human	5.3	pIC50	=	5.3	Functional	Compound was tested for its ability to inhibit Endothelin A receptor induced arachidonic acid release(AARA) in rabbit renal artery vascular smooth muscles.Compound was tested for its ability to inhibit Endothelin A receptor induced arachidonic acid release(AARA) in rabbit renal artery vascular smooth muscles.	ChEMBL	387	4	0	6	4.4	COC(=O)C(Oc1c2ccccc2nc2ccccc12)c1ccc2c(c1)OCO2	10.1016/S0960-894X(96)00551-3
	9865706	104910	0	None	1	2	Human	5.3	pIC50	=	5.3	Functional	Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK	ChEMBL	400	4	1	5	4.1	Cc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1	10.1021/jm00008a002
	CHEMBL273613	104910	0	None	1	2	Human	5.3	pIC50	=	5.3	Functional	Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK	ChEMBL	400	4	1	5	4.1	Cc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1	10.1021/jm00008a002
	CHEMBL264330	217391	0	None	-	1	Pig	8.3	pIC50	=	8.3	Functional	Antagonist activity against ET-A from porcine heart membranesAntagonist activity against ET-A from porcine heart membranes	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(C)(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/0960-894X(95)00349-X
	CHEMBL386850	219176	0	None	-	1	Pig	8.3	pIC50	=	8.3	Functional	Antagonist activity against ET-A from porcine heart membranesAntagonist activity against ET-A from porcine heart membranes	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(C)(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/0960-894X(95)00349-X
	11318409	214234	0	None	3	2	Human	8.3	pIC50	=	8.3	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	522	7	2	6	4.3	Cc1cccc(CN2C(=O)CN[C@](c3ccccc3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)c1	10.1021/jm031115r
	CHEMBL94212	214234	0	None	3	2	Human	8.3	pIC50	=	8.3	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	522	7	2	6	4.3	Cc1cccc(CN2C(=O)CN[C@](c3ccccc3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)c1	10.1021/jm031115r
	10187261	118317	0	None	3	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	542	7	2	6	4.7	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cccc(Cl)c3)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL327976	118317	0	None	3	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	542	7	2	6	4.7	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cccc(Cl)c3)c3ccccc32)n1	10.1021/jm031115r
	11785813	113699	0	None	8	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	526	7	2	6	4.1	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(F)cc3)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL314755	113699	0	None	8	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	526	7	2	6	4.1	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(F)cc3)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL408616	219503	0	None	-	1	Pig	7.3	pIC50	=	7.3	Functional	Antagonist activity against ET-A from porcine heart membranesAntagonist activity against ET-A from porcine heart membranes	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(95)00349-X
	9845562	11513	0	None	7	3	Human	7.3	pIC50	=	7.3	Functional	Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.	ChEMBL	430	5	1	6	4.1	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(C)cc2)cc1	10.1021/jm00008a002
	CHEMBL10374	11513	0	None	7	3	Human	7.3	pIC50	=	7.3	Functional	Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.	ChEMBL	430	5	1	6	4.1	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(C)cc2)cc1	10.1021/jm00008a002
	11742628	105011	0	None	25	3	Human	7.3	pIC50	=	7.3	Functional	Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.	ChEMBL	416	5	1	6	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1	10.1021/jm00008a002
	CHEMBL274383	105011	0	None	25	3	Human	7.3	pIC50	=	7.3	Functional	Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.	ChEMBL	416	5	1	6	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1	10.1021/jm00008a002
	9845562	11513	0	None	7	3	Human	7.3	pIC50	=	7.3	Functional	Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK	ChEMBL	430	5	1	6	4.1	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(C)cc2)cc1	10.1021/jm00008a002
	CHEMBL10374	11513	0	None	7	3	Human	7.3	pIC50	=	7.3	Functional	Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK	ChEMBL	430	5	1	6	4.1	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(C)cc2)cc1	10.1021/jm00008a002
	CHEMBL411797	219736	0	None	1	2	Human	6.3	pIC50	=	6.3	Functional	Inhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cellsInhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	10226239	214667	0	None	4	2	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	456	5	2	8	2.9	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCc3nnc(C)n3-c3ccccc32)n1	10.1021/jm031115r
	CHEMBL96614	214667	0	None	4	2	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	456	5	2	8	2.9	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCc3nnc(C)n3-c3ccccc32)n1	10.1021/jm031115r
	10027018	105265	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.	ChEMBL	454	4	1	5	5.1	O=C1OC(O)(c2ccc(Cl)c(Cl)c2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2	10.1021/jm00008a002
	CHEMBL275991	105265	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.	ChEMBL	454	4	1	5	5.1	O=C1OC(O)(c2ccc(Cl)c(Cl)c2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2	10.1021/jm00008a002
	44332578	11087	0	None	-	1	Human	5.3	pIC50	=	5.3	Functional	Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.	ChEMBL	413	3	0	5	5.6	CC(C)(C)OC(=O)C(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12	10.1016/S0960-894X(96)00551-3
	CHEMBL100874	11087	0	None	-	1	Human	5.3	pIC50	=	5.3	Functional	Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.	ChEMBL	413	3	0	5	5.6	CC(C)(C)OC(=O)C(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12	10.1016/S0960-894X(96)00551-3
	122272	103872	31	None	-4	4	Human	6.2	pIC50	=	6.2	Functional	Antagonism of ET-1 induced increase in intracellular Ca+2 in vsm-A10 cellsAntagonism of ET-1 induced increase in intracellular Ca+2 in vsm-A10 cells	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C	10.1021/jm00029a001
	CHEMBL267458	103872	31	None	-4	4	Human	6.2	pIC50	=	6.2	Functional	Antagonism of ET-1 induced increase in intracellular Ca+2 in vsm-A10 cellsAntagonism of ET-1 induced increase in intracellular Ca+2 in vsm-A10 cells	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C	10.1021/jm00029a001
	10047521	15402	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK	ChEMBL	416	6	1	5	4.4	COc1ccc(CC2=C(c3ccc(C)cc3)C(=O)OC2(O)c2ccc(OC)cc2)cc1	10.1021/jm00008a002
	CHEMBL10951	15402	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK	ChEMBL	416	6	1	5	4.4	COc1ccc(CC2=C(c3ccc(C)cc3)C(=O)OC2(O)c2ccc(OC)cc2)cc1	10.1021/jm00008a002
	11156301	85439	0	None	4	2	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	500	7	3	9	2.2	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCc3nnc(CC(=O)O)n3-c3ccccc32)n1	10.1021/jm031115r
	CHEMBL2112377	85439	0	None	4	2	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	500	7	3	9	2.2	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCc3nnc(CC(=O)O)n3-c3ccccc32)n1	10.1021/jm031115r
	9820754	115339	0	None	-	1	Human	5.2	pIC50	=	5.2	Functional	Compound was tested for inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsCompound was tested for inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells	ChEMBL	371	3	0	5	4.4	COC(=O)C(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12	10.1016/S0960-894X(96)00551-3
	CHEMBL320236	115339	0	None	-	1	Human	5.2	pIC50	=	5.2	Functional	Compound was tested for inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsCompound was tested for inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells	ChEMBL	371	3	0	5	4.4	COC(=O)C(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12	10.1016/S0960-894X(96)00551-3
	11203972	113654	0	None	-	1	Human	5.2	pIC50	=	5.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	576	8	2	5	5.9	COc1ccccc1O[C@H](C(=O)O)[C@@]1(c2ccccc2)NCC(=O)N(Cc2c(Cl)cccc2Cl)c2ccccc21	10.1021/jm031115r
	CHEMBL314511	113654	0	None	-	1	Human	5.2	pIC50	=	5.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	576	8	2	5	5.9	COc1ccccc1O[C@H](C(=O)O)[C@@]1(c2ccccc2)NCC(=O)N(Cc2c(Cl)cccc2Cl)c2ccccc21	10.1021/jm031115r
	CHEMBL2373085	217150	0	None	-	1	Pig	8.2	pIC50	=	8.2	Functional	Antagonist activity against ET-A from porcine heart membranesAntagonist activity against ET-A from porcine heart membranes	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(95)00349-X
	CHEMBL433837	220424	0	None	-	1	Pig	8.2	pIC50	=	8.2	Functional	Antagonist activity against ET-A from porcine heart membranesAntagonist activity against ET-A from porcine heart membranes	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(95)00349-X
	CHEMBL62641	222625	0	None	-	1	Pig	8.2	pIC50	=	8.2	Functional	Antagonist activity against ET-A from porcine heart membranesAntagonist activity against ET-A from porcine heart membranes	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(95)00349-X
	10187313	114221	0	None	18	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	544	7	2	6	4.3	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(F)cc3F)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL318247	114221	0	None	18	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	544	7	2	6	4.3	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(F)cc3F)c3ccccc32)n1	10.1021/jm031115r
	9890440	15026	0	None	301	2	Human	8.2	pIC50	=	8.2	Functional	Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.	ChEMBL	460	6	1	7	4.1	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(OC)c(C)c2)cc1	10.1021/jm00008a002
	CHEMBL10924	15026	0	None	301	2	Human	8.2	pIC50	=	8.2	Functional	Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.	ChEMBL	460	6	1	7	4.1	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(OC)c(C)c2)cc1	10.1021/jm00008a002
	11284285	114106	0	None	8	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	552	8	2	7	4.3	COc1ccc(CN2C(=O)CN[C@](c3cccc(C)c3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1	10.1021/jm031115r
	CHEMBL317510	114106	0	None	8	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	552	8	2	7	4.3	COc1ccc(CN2C(=O)CN[C@](c3cccc(C)c3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1	10.1021/jm031115r
	11307805	114118	0	None	3	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	586	7	2	6	4.8	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cccc(Br)c3)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL317589	114118	0	None	3	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	586	7	2	6	4.8	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cccc(Br)c3)c3ccccc32)n1	10.1021/jm031115r
	11283571	214377	0	None	7	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	508	7	2	6	4.0	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccccc3)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL95013	214377	0	None	7	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	508	7	2	6	4.0	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccccc3)c3ccccc32)n1	10.1021/jm031115r
	11364770	170435	0	None	5	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	544	7	2	6	4.3	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(F)c(F)c3)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL420435	170435	0	None	5	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	544	7	2	6	4.3	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(F)c(F)c3)c3ccccc32)n1	10.1021/jm031115r
	10209814	214050	0	None	7	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	562	7	2	6	4.4	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(F)c(F)c3F)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL93084	214050	0	None	7	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	562	7	2	6	4.4	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(F)c(F)c3F)c3ccccc32)n1	10.1021/jm031115r
	10163956	214368	0	None	10	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	500	7	3	9	1.5	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3nn[nH]n3)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL94964	214368	0	None	10	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	500	7	3	9	1.5	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3nn[nH]n3)c3ccccc32)n1	10.1021/jm031115r
	10166139	170123	0	None	2	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	550	7	2	6	4.9	Cc1cc(C)c(CN2C(=O)CN[C@](c3ccccc3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)c(C)c1	10.1021/jm031115r
	CHEMBL419136	170123	0	None	2	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	550	7	2	6	4.9	Cc1cc(C)c(CN2C(=O)CN[C@](c3ccccc3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)c(C)c1	10.1021/jm031115r
	11191999	214278	0	None	4	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	544	7	2	6	4.3	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cc(F)ccc3F)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL94438	214278	0	None	4	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	544	7	2	6	4.3	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cc(F)ccc3F)c3ccccc32)n1	10.1021/jm031115r
	11375934	214692	0	None	3	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	526	7	2	6	4.1	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cccc(F)c3)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL96746	214692	0	None	3	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	526	7	2	6	4.1	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cccc(F)c3)c3ccccc32)n1	10.1021/jm031115r
	11478911	163089	0	None	4	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	598	7	2	6	4.7	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(F)c(F)c(F)c(F)c3F)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL406551	163089	0	None	4	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	598	7	2	6	4.7	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(F)c(F)c(F)c(F)c3F)c3ccccc32)n1	10.1021/jm031115r
	10298354	118783	0	None	15	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	462	7	3	7	1.8	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CCO)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL328878	118783	0	None	15	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	462	7	3	7	1.8	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CCO)c3ccccc32)n1	10.1021/jm031115r
	345351	16131	4	None	24	3	Human	6.2	pIC50	=	6.2	Functional	Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK	ChEMBL	386	4	1	5	3.8	O=C1OC(O)(c2ccccc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2	10.1021/jm00008a002
	CHEMBL11131	16131	4	None	24	3	Human	6.2	pIC50	=	6.2	Functional	Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK	ChEMBL	386	4	1	5	3.8	O=C1OC(O)(c2ccccc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2	10.1021/jm00008a002
	CHEMBL329609	218097	0	None	3	2	Human	5.2	pIC50	=	5.2	Functional	Inhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cellsInhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)[C@@H](C)CC	10.1021/jm00015a003
	11202819	119341	0	None	1	2	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	499	6	3	8	3.2	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCc3c(C(=O)O)nc(C)n3-c3ccccc32)n1	10.1021/jm031115r
	CHEMBL330045	119341	0	None	1	2	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	499	6	3	8	3.2	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCc3c(C(=O)O)nc(C)n3-c3ccccc32)n1	10.1021/jm031115r
	11385689	119573	0	None	10	2	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	462	7	2	6	3.0	COc1cc(OC)cc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3ccccc32)c1	10.1021/jm031115r
	CHEMBL330629	119573	0	None	10	2	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	462	7	2	6	3.0	COc1cc(OC)cc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3ccccc32)c1	10.1021/jm031115r
	44283270	174660	0	None	-2691	4	Human	5.2	pIC50	=	5.2	Functional	Functional inhibition of ET-1 induced [Ca2+] increase in human neuroblastoma-derived SK-N-MC cells, which express Endothelin A receptorFunctional inhibition of ET-1 induced [Ca2+] increase in human neuroblastoma-derived SK-N-MC cells, which express Endothelin A receptor	ChEMBL	580	12	5	5	3.8	CCCC[C@H](NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C)C(=O)O	10.1016/0960-894X(95)00237-N
	CHEMBL431124	174660	0	None	-2691	4	Human	5.2	pIC50	=	5.2	Functional	Functional inhibition of ET-1 induced [Ca2+] increase in human neuroblastoma-derived SK-N-MC cells, which express Endothelin A receptorFunctional inhibition of ET-1 induced [Ca2+] increase in human neuroblastoma-derived SK-N-MC cells, which express Endothelin A receptor	ChEMBL	580	12	5	5	3.8	CCCC[C@H](NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C)C(=O)O	10.1016/0960-894X(95)00237-N
	18995991	107076	0	None	9	2	Human	7.2	pIC50	=	7.2	Functional	Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin A receptor.Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin A receptor.	ChEMBL	537	8	1	10	5.0	COc1cc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc4c(cc23)OCO4)cc(OC)c1OC	10.1016/0960-894X(96)00232-6
	CHEMBL28920	107076	0	None	9	2	Human	7.2	pIC50	=	7.2	Functional	Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin A receptor.Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin A receptor.	ChEMBL	537	8	1	10	5.0	COc1cc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc4c(cc23)OCO4)cc(OC)c1OC	10.1016/0960-894X(96)00232-6
	18995992	106614	0	None	3	2	Human	7.2	pIC50	=	7.2	Functional	Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin A receptor.Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin A receptor.	ChEMBL	507	7	1	9	5.0	COc1ccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc4c(cc23)OCO4)cc1OC	10.1016/0960-894X(96)00232-6
	CHEMBL28563	106614	0	None	3	2	Human	7.2	pIC50	=	7.2	Functional	Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin A receptor.Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin A receptor.	ChEMBL	507	7	1	9	5.0	COc1ccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc4c(cc23)OCO4)cc1OC	10.1016/0960-894X(96)00232-6
	11465096	103540	0	None	-	1	Human	5.2	pIC50	=	5.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	450	6	2	7	2.5	CSc1cnc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3ccccc32)nc1	10.1021/jm031115r
	CHEMBL264625	103540	0	None	-	1	Human	5.2	pIC50	=	5.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	450	6	2	7	2.5	CSc1cnc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3ccccc32)nc1	10.1021/jm031115r
	11235126	214706	0	None	52	2	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	405	5	2	6	2.9	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCCOc3ccccc32)n1	10.1021/jm031115r
	CHEMBL96831	214706	0	None	52	2	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	405	5	2	6	2.9	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCCOc3ccccc32)n1	10.1021/jm031115r
	11478553	170229	0	None	10	2	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	562	7	2	6	4.4	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cc(F)c(F)cc3F)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL419879	170229	0	None	10	2	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	562	7	2	6	4.4	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cc(F)c(F)cc3F)c3ccccc32)n1	10.1021/jm031115r
	11330570	214363	0	None	4	2	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	570	8	2	7	4.5	COc1ccc(CN2C(=O)CN[C@](c3ccc(F)c(C)c3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1	10.1021/jm031115r
	CHEMBL94934	214363	0	None	4	2	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	570	8	2	7	4.5	COc1ccc(CN2C(=O)CN[C@](c3ccc(F)c(C)c3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1	10.1021/jm031115r
	11155687	214606	0	None	12	2	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	472	7	2	6	3.2	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CC3CC3)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL96318	214606	0	None	12	2	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	472	7	2	6	3.2	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CC3CC3)c3ccccc32)n1	10.1021/jm031115r
	10303311	113939	0	None	9	2	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	566	8	2	8	3.8	COC(=O)c1ccc(CN2C(=O)CN[C@](c3ccccc3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1	10.1021/jm031115r
	CHEMBL316301	113939	0	None	9	2	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	566	8	2	8	3.8	COC(=O)c1ccc(CN2C(=O)CN[C@](c3ccccc3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1	10.1021/jm031115r
	11742628	105011	0	None	25	3	Human	8.1	pIC50	=	8.1	Functional	Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK	ChEMBL	416	5	1	6	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1	10.1021/jm00008a002
	CHEMBL274383	105011	0	None	25	3	Human	8.1	pIC50	=	8.1	Functional	Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK	ChEMBL	416	5	1	6	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1	10.1021/jm00008a002
	11477664	174946	0	None	6	2	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	506	10	2	8	2.4	COCCOCN1C(=O)CN[C@](c2ccccc2)([C@H](Oc2nc(C)cc(C)n2)C(=O)O)c2ccccc21	10.1021/jm031115r
	CHEMBL433173	174946	0	None	6	2	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	506	10	2	8	2.4	COCCOCN1C(=O)CN[C@](c2ccccc2)([C@H](Oc2nc(C)cc(C)n2)C(=O)O)c2ccccc21	10.1021/jm031115r
	11204331	119356	0	None	-1	2	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	616	10	2	6	6.1	CCCCc1cccc([C@]2([C@H](Oc3nc(C)cc(C)n3)C(=O)O)NCC(=O)N(Cc3c(F)cccc3Cl)c3ccccc32)c1	10.1021/jm031115r
	CHEMBL330135	119356	0	None	-1	2	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	616	10	2	6	6.1	CCCCc1cccc([C@]2([C@H](Oc3nc(C)cc(C)n3)C(=O)O)NCC(=O)N(Cc3c(F)cccc3Cl)c3ccccc32)c1	10.1021/jm031115r
	11377200	115075	0	None	11	2	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	638	8	2	6	6.1	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3cccc(-c4ccccc4)c3)NCC(=O)N(Cc3c(F)cc(F)cc3F)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL319754	115075	0	None	11	2	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	638	8	2	6	6.1	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3cccc(-c4ccccc4)c3)NCC(=O)N(Cc3c(F)cc(F)cc3F)c3ccccc32)n1	10.1021/jm031115r
	11444738	171658	0	None	4	2	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	594	11	2	7	5.4	CCCCc1cccc([C@]2([C@H](Oc3nc(C)cc(C)n3)C(=O)O)NCC(=O)N(Cc3ccc(OC)cc3)c3ccccc32)c1	10.1021/jm031115r
	CHEMBL422068	171658	0	None	4	2	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	594	11	2	7	5.4	CCCCc1cccc([C@]2([C@H](Oc3nc(C)cc(C)n3)C(=O)O)NCC(=O)N(Cc3ccc(OC)cc3)c3ccccc32)c1	10.1021/jm031115r
	11398658	214378	0	None	1	2	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	544	7	2	6	4.3	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cc(F)cc(F)c3)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL95017	214378	0	None	1	2	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	544	7	2	6	4.3	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cc(F)cc(F)c3)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL319719	218000	0	None	-3	2	Human	7.2	pIC50	=	7.2	Functional	Inhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cellsInhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	CHEMBL328942	218095	0	None	1	4	Human	7.2	pIC50	=	7.2	Functional	Inhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cellsInhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	9980487	12042	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK	ChEMBL	436	6	1	5	4.8	COc1ccc(CC2=C(c3ccc(Cl)cc3)C(=O)OC2(O)c2ccc(OC)cc2)cc1	10.1021/jm00008a002
	CHEMBL10648	12042	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK	ChEMBL	436	6	1	5	4.8	COc1ccc(CC2=C(c3ccc(Cl)cc3)C(=O)OC2(O)c2ccc(OC)cc2)cc1	10.1021/jm00008a002
	10452089	11337	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.	ChEMBL	375	3	0	5	4.1	COC(=O)C(c1ccc2c(c1)OCO2)c1c2c(nc3ccccc13)CCCC2	10.1016/S0960-894X(96)00551-3
	CHEMBL102494	11337	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.	ChEMBL	375	3	0	5	4.1	COC(=O)C(c1ccc2c(c1)OCO2)c1c2c(nc3ccccc13)CCCC2	10.1016/S0960-894X(96)00551-3
	70694736	82988	0	None	-1	2	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cellsAntagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cells	ChEMBL	472	6	1	6	5.5	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(Cn3c(C)nc4ccccc43)cc2)c1C	10.1016/j.bmc.2012.06.011
	CHEMBL2058367	82988	0	None	-1	2	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cellsAntagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cells	ChEMBL	472	6	1	6	5.5	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(Cn3c(C)nc4ccccc43)cc2)c1C	10.1016/j.bmc.2012.06.011
	134136255	149372	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Agonist activity at ETA receptor in human SKNMC cells assessed as induction of Ca2+ mobilization by fluorimetric methodAgonist activity at ETA receptor in human SKNMC cells assessed as induction of Ca2+ mobilization by fluorimetric method	ChEMBL	663	11	2	10	5.2	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(F)(C(F)(F)F)C(F)(F)F)cc2)nc(-c2ncccn2)nc1OCCO	10.1016/j.ejmech.2016.06.006
	CHEMBL3891334	149372	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Agonist activity at ETA receptor in human SKNMC cells assessed as induction of Ca2+ mobilization by fluorimetric methodAgonist activity at ETA receptor in human SKNMC cells assessed as induction of Ca2+ mobilization by fluorimetric method	ChEMBL	663	11	2	10	5.2	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(F)(C(F)(F)F)C(F)(F)F)cc2)nc(-c2ncccn2)nc1OCCO	10.1016/j.ejmech.2016.06.006
	10047521	15402	0	None	-	1	Human	6.1	pIC50	=	6.1	Functional	Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.	ChEMBL	416	6	1	5	4.4	COc1ccc(CC2=C(c3ccc(C)cc3)C(=O)OC2(O)c2ccc(OC)cc2)cc1	10.1021/jm00008a002
	CHEMBL10951	15402	0	None	-	1	Human	6.1	pIC50	=	6.1	Functional	Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.	ChEMBL	416	6	1	5	4.4	COc1ccc(CC2=C(c3ccc(C)cc3)C(=O)OC2(O)c2ccc(OC)cc2)cc1	10.1021/jm00008a002
	44332807	114012	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.	ChEMBL	447	5	0	5	6.0	O=C(OCc1ccccc1)C(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12	10.1016/S0960-894X(96)00551-3
	CHEMBL316792	114012	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.	ChEMBL	447	5	0	5	6.0	O=C(OCc1ccccc1)C(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12	10.1016/S0960-894X(96)00551-3
	44332624	10953	0	None	-	1	Human	4.1	pIC50	=	4.1	Functional	Compound was tested for its ability to inhibit Endothelin A receptor induced arachidonic acid release(AARA) in rabbit renal artery vascular smooth muscles.Compound was tested for its ability to inhibit Endothelin A receptor induced arachidonic acid release(AARA) in rabbit renal artery vascular smooth muscles.	ChEMBL	356	3	1	4	3.7	NC(=O)C(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12	10.1016/S0960-894X(96)00551-3
	CHEMBL100120	10953	0	None	-	1	Human	4.1	pIC50	=	4.1	Functional	Compound was tested for its ability to inhibit Endothelin A receptor induced arachidonic acid release(AARA) in rabbit renal artery vascular smooth muscles.Compound was tested for its ability to inhibit Endothelin A receptor induced arachidonic acid release(AARA) in rabbit renal artery vascular smooth muscles.	ChEMBL	356	3	1	4	3.7	NC(=O)C(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12	10.1016/S0960-894X(96)00551-3
	10336018	108885	0	None	-10	2	Human	5.1	pIC50	=	5.1	Functional	Antagonism of ET1 induced increase in intracellular Ca+2 in rabbit carotid artery ringsAntagonism of ET1 induced increase in intracellular Ca+2 in rabbit carotid artery rings	ChEMBL	318	3	2	5	3.0	Cc1noc(NS(=O)(=O)c2cccc3c(O)cccc23)c1C	10.1021/jm00029a001
	CHEMBL30228	108885	0	None	-10	2	Human	5.1	pIC50	=	5.1	Functional	Antagonism of ET1 induced increase in intracellular Ca+2 in rabbit carotid artery ringsAntagonism of ET1 induced increase in intracellular Ca+2 in rabbit carotid artery rings	ChEMBL	318	3	2	5	3.0	Cc1noc(NS(=O)(=O)c2cccc3c(O)cccc23)c1C	10.1021/jm00029a001
	CHEMBL265614	217435	19	None	-	1	Pig	8.1	pIC50	=	8.1	Functional	Antagonist activity against ET-A from porcine heart membranesAntagonist activity against ET-A from porcine heart membranes	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(95)00349-X
	CHEMBL269189	217561	0	None	-	1	Pig	8.1	pIC50	=	8.1	Functional	Antagonist activity against ET-A from porcine heart membranesAntagonist activity against ET-A from porcine heart membranes	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(95)00349-X
	104865	7493	99	None	-3	5	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cellsAntagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cells	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/j.bmc.2012.06.011
	3494	7493	99	None	-3	5	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cellsAntagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cells	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/j.bmc.2012.06.011
	392	7493	99	None	-3	5	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cellsAntagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cells	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/j.bmc.2012.06.011
	CHEMBL957	7493	99	None	-3	5	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cellsAntagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cells	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/j.bmc.2012.06.011
	DB00559	7493	99	None	-3	5	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cellsAntagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cells	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/j.bmc.2012.06.011
	70694737	82993	0	None	-1	2	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cellsAntagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cells	ChEMBL	544	10	1	7	6.5	CCCCc1nc2ccc(OC)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1016/j.bmc.2012.06.011
	CHEMBL2058372	82993	0	None	-1	2	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cellsAntagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cells	ChEMBL	544	10	1	7	6.5	CCCCc1nc2ccc(OC)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1016/j.bmc.2012.06.011
	11432418	113725	0	None	6	2	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	522	7	2	6	4.3	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccccc3C)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL314946	113725	0	None	6	2	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	522	7	2	6	4.3	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccccc3C)c3ccccc32)n1	10.1021/jm031115r
	44332638	11148	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.	ChEMBL	477	6	0	6	6.0	COc1ccc(COC(=O)C(c2ccc3c(c2)OCO3)c2c3ccccc3nc3ccccc23)cc1	10.1016/S0960-894X(96)00551-3
	CHEMBL101239	11148	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.	ChEMBL	477	6	0	6	6.0	COc1ccc(COC(=O)C(c2ccc3c(c2)OCO3)c2c3ccccc3nc3ccccc23)cc1	10.1016/S0960-894X(96)00551-3
	11489174	119325	0	None	-1	2	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	514	7	2	6	4.4	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CC3CCCCC3)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL329943	119325	0	None	-1	2	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	514	7	2	6	4.4	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CC3CCCCC3)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL216082	216096	0	None	-20	2	Human	6.1	pIC50	=	6.1	Functional	Inhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cellsInhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	44332624	10953	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.	ChEMBL	356	3	1	4	3.7	NC(=O)C(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12	10.1016/S0960-894X(96)00551-3
	CHEMBL100120	10953	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.	ChEMBL	356	3	1	4	3.7	NC(=O)C(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12	10.1016/S0960-894X(96)00551-3
	44332546	113990	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.	ChEMBL	491	5	0	7	5.7	O=C(OCc1ccc2c(c1)OCO2)C(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12	10.1016/S0960-894X(96)00551-3
	CHEMBL316648	113990	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.	ChEMBL	491	5	0	7	5.7	O=C(OCc1ccc2c(c1)OCO2)C(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12	10.1016/S0960-894X(96)00551-3
	9955200	16104	0	None	53	3	Human	8.1	pIC50	=	8.1	Functional	Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.	ChEMBL	446	6	1	7	3.8	COc1ccc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc1	10.1021/jm00008a002
	CHEMBL11115	16104	0	None	53	3	Human	8.1	pIC50	=	8.1	Functional	Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.	ChEMBL	446	6	1	7	3.8	COc1ccc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc1	10.1021/jm00008a002
	11376627	114409	0	None	1	2	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	576	7	2	6	5.0	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cccc(C(F)(F)F)c3)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL319007	114409	0	None	1	2	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	576	7	2	6	5.0	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cccc(C(F)(F)F)c3)c3ccccc32)n1	10.1021/jm031115r
	11307457	214390	0	None	5	2	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	556	8	2	7	4.2	COc1ccc(CN2C(=O)CN[C@](c3cccc(F)c3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1	10.1021/jm031115r
	CHEMBL95095	214390	0	None	5	2	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	556	8	2	7	4.2	COc1ccc(CN2C(=O)CN[C@](c3cccc(F)c3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1	10.1021/jm031115r
	70684239	82992	0	None	-1	2	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cellsAntagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cells	ChEMBL	528	9	1	6	6.8	CCCCc1nc2ccc(C)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1016/j.bmc.2012.06.011
	CHEMBL2058371	82992	0	None	-1	2	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cellsAntagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cells	ChEMBL	528	9	1	6	6.8	CCCCc1nc2ccc(C)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1016/j.bmc.2012.06.011
	70694738	82994	0	None	1	2	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cellsAntagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cells	ChEMBL	548	9	1	6	7.2	CCCCc1nc2ccc(Cl)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1016/j.bmc.2012.06.011
	CHEMBL2058373	82994	0	None	1	2	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cellsAntagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cells	ChEMBL	548	9	1	6	7.2	CCCCc1nc2ccc(Cl)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1016/j.bmc.2012.06.011
	70686382	82991	0	None	1	2	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cellsAntagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cells	ChEMBL	514	9	1	6	6.5	CCCCc1nc2ccccc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1016/j.bmc.2012.06.011
	CHEMBL2058370	82991	0	None	1	2	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cellsAntagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cells	ChEMBL	514	9	1	6	6.5	CCCCc1nc2ccccc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1016/j.bmc.2012.06.011
	70696780	82995	0	None	1	2	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cellsAntagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cells	ChEMBL	592	9	1	6	7.3	CCCCc1nc2ccc(Br)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1016/j.bmc.2012.06.011
	CHEMBL2058374	82995	0	None	1	2	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cellsAntagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cells	ChEMBL	592	9	1	6	7.3	CCCCc1nc2ccc(Br)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1016/j.bmc.2012.06.011
	44213651	11070	0	None	-	1	Human	6.1	pIC50	=	6.1	Functional	Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.	ChEMBL	343	3	1	4	4.2	OCC(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12	10.1016/S0960-894X(96)00551-3
	CHEMBL100795	11070	0	None	-	1	Human	6.1	pIC50	=	6.1	Functional	Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.	ChEMBL	343	3	1	4	4.2	OCC(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12	10.1016/S0960-894X(96)00551-3
	11441050	214610	0	None	85	2	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	403	5	2	5	3.4	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCCCc3ccccc32)n1	10.1021/jm031115r
	CHEMBL96331	214610	0	None	85	2	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	403	5	2	5	3.4	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCCCc3ccccc32)n1	10.1021/jm031115r
	11488556	214648	0	None	10	2	Human	6.0	pIC50	=	6.0	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	482	5	2	6	2.6	CN1C(=O)CN[C@](c2ccccc2)([C@H](Oc2ncc(Br)cn2)C(=O)O)c2ccccc21	10.1021/jm031115r
	CHEMBL96520	214648	0	None	10	2	Human	6.0	pIC50	=	6.0	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	482	5	2	6	2.6	CN1C(=O)CN[C@](c2ccccc2)([C@H](Oc2ncc(Br)cn2)C(=O)O)c2ccccc21	10.1021/jm031115r
	9980487	12042	0	None	-	1	Human	6.0	pIC50	=	6.0	Functional	Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.	ChEMBL	436	6	1	5	4.8	COc1ccc(CC2=C(c3ccc(Cl)cc3)C(=O)OC2(O)c2ccc(OC)cc2)cc1	10.1021/jm00008a002
	CHEMBL10648	12042	0	None	-	1	Human	6.0	pIC50	=	6.0	Functional	Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.	ChEMBL	436	6	1	5	4.8	COc1ccc(CC2=C(c3ccc(Cl)cc3)C(=O)OC2(O)c2ccc(OC)cc2)cc1	10.1021/jm00008a002
	11456110	214618	0	None	-1	2	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	592	8	2	7	4.9	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccccc3OC(F)(F)F)c3ccccc32)n1	10.1021/jm031115r
	CHEMBL96387	214618	0	None	-1	2	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	ChEMBL	592	8	2	7	4.9	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccccc3OC(F)(F)F)c3ccccc32)n1	10.1021/jm031115r
	70686380	82987	0	None	-1	2	Human	7.0	pIC50	=	7	Functional	Antagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cellsAntagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cells	ChEMBL	458	6	1	6	5.2	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(Cn3cnc4ccccc43)cc2)c1C	10.1016/j.bmc.2012.06.011
	CHEMBL2058366	82987	0	None	-1	2	Human	7.0	pIC50	=	7	Functional	Antagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cellsAntagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cells	ChEMBL	458	6	1	6	5.2	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(Cn3cnc4ccccc43)cc2)c1C	10.1016/j.bmc.2012.06.011
	44311232	210886	0	None	-	2	Rat	10.0	pKd	=	10	Functional	Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)	ChEMBL	658	13	2	13	5.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ncccn2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	CHEMBL70293	210886	0	None	-	2	Rat	10.0	pKd	=	10	Functional	Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)	ChEMBL	658	13	2	13	5.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ncccn2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	9939238	210907	0	None	-	2	Rat	9.7	pKd	=	9.7	Functional	Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)	ChEMBL	637	12	2	13	3.6	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	CHEMBL70385	210907	0	None	-	2	Rat	9.7	pKd	=	9.7	Functional	Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)	ChEMBL	637	12	2	13	3.6	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	9809919	211188	0	None	-	2	Rat	9.3	pKd	=	9.3	Functional	Compound was evaluated for in vitro functional inhibitory potency for prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)Compound was evaluated for in vitro functional inhibitory potency for prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)	ChEMBL	665	13	2	13	4.5	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	CHEMBL72037	211188	0	None	-	2	Rat	9.3	pKd	=	9.3	Functional	Compound was evaluated for in vitro functional inhibitory potency for prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)Compound was evaluated for in vitro functional inhibitory potency for prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)	ChEMBL	665	13	2	13	4.5	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	44212539	210872	0	None	-	2	Rat	9.0	pKd	=	9	Functional	Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)	ChEMBL	671	12	2	12	5.9	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	CHEMBL70203	210872	0	None	-	2	Rat	9.0	pKd	=	9	Functional	Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)	ChEMBL	671	12	2	12	5.9	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	44311233	210888	0	None	-	2	Rat	9.0	pKd	=	9	Functional	Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)	ChEMBL	630	12	2	13	4.3	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2ncccn2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	CHEMBL70303	210888	0	None	-	2	Rat	9.0	pKd	=	9	Functional	Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)	ChEMBL	630	12	2	13	4.3	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2ncccn2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	44311516	210897	0	None	-	2	Rat	8.0	pKd	=	8	Functional	Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)	ChEMBL	678	12	2	12	5.2	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	CHEMBL70339	210897	0	None	-	2	Rat	8.0	pKd	=	8	Functional	Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)	ChEMBL	678	12	2	12	5.2	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	44311527	210902	0	None	-	2	Rat	8.0	pKd	=	8	Functional	Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)	ChEMBL	675	12	2	11	7.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2cccs2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	CHEMBL70365	210902	0	None	-	2	Rat	8.0	pKd	=	8	Functional	Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)	ChEMBL	675	12	2	11	7.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2cccs2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	18184234	68983	0	None	-	2	Rat	7.0	pKd	=	7.0	Functional	In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)	ChEMBL	605	15	2	10	4.2	CCS(=O)(=O)NCCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	CHEMBL177802	68983	0	None	-	2	Rat	7.0	pKd	=	7.0	Functional	In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)	ChEMBL	605	15	2	10	4.2	CCS(=O)(=O)NCCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	9807456	67247	0	None	-	2	Rat	7.0	pKd	=	7.0	Functional	Potency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic ringsPotency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic rings	ChEMBL	545	9	1	9	4.8	C#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	CHEMBL175435	67247	0	None	-	2	Rat	7.0	pKd	=	7.0	Functional	Potency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic ringsPotency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic rings	ChEMBL	545	9	1	9	4.8	C#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	44311285	109076	0	None	-	2	Rat	7.9	pKd	=	7.9	Functional	Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)	ChEMBL	635	13	2	10	6.4	CCCc1nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c(Oc2ccccc2OC)c(OCCOC(=O)Nc2ccccn2)n1	10.1016/S0960-894X(97)00400-9
	CHEMBL303428	109076	0	None	-	2	Rat	7.9	pKd	=	7.9	Functional	Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)	ChEMBL	635	13	2	10	6.4	CCCc1nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c(Oc2ccccc2OC)c(OCCOC(=O)Nc2ccccn2)n1	10.1016/S0960-894X(97)00400-9
	9917706	136517	0	None	-	2	Rat	6.9	pKd	=	6.9	Functional	In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)	ChEMBL	659	15	2	11	5.3	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CC2)nc1OCCCNS(=O)(=O)c1cccs1	10.1016/s0960-894x(02)01083-1
	CHEMBL367444	136517	0	None	-	2	Rat	6.9	pKd	=	6.9	Functional	In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)	ChEMBL	659	15	2	11	5.3	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CC2)nc1OCCCNS(=O)(=O)c1cccs1	10.1016/s0960-894x(02)01083-1
	9869444	104021	0	None	120	2	Human	6.9	pKd	=	6.9	Functional	Inhibition of contraction of ET-1 induced rabbit femoral artery, which are known to express predominantly ETA receptorsInhibition of contraction of ET-1 induced rabbit femoral artery, which are known to express predominantly ETA receptors	ChEMBL	473	7	1	7	5.3	CCCOc1ccc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2c1	10.1016/0960-894X(96)00170-9
	CHEMBL268751	104021	0	None	120	2	Human	6.9	pKd	=	6.9	Functional	Inhibition of contraction of ET-1 induced rabbit femoral artery, which are known to express predominantly ETA receptorsInhibition of contraction of ET-1 induced rabbit femoral artery, which are known to express predominantly ETA receptors	ChEMBL	473	7	1	7	5.3	CCCOc1ccc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2c1	10.1016/0960-894X(96)00170-9
	9848132	214356	0	None	120	2	Rat	5.9	pKd	=	5.9	Functional	Compound was evaluated for the antagonism at the Endothelin A receptor in isolated rat aortic ringsCompound was evaluated for the antagonism at the Endothelin A receptor in isolated rat aortic rings	ChEMBL	483	6	1	8	2.8	Cc1cc(C)c(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)n1	10.1016/S0960-894X(96)00617-8
	CHEMBL94918	214356	0	None	120	2	Rat	5.9	pKd	=	5.9	Functional	Compound was evaluated for the antagonism at the Endothelin A receptor in isolated rat aortic ringsCompound was evaluated for the antagonism at the Endothelin A receptor in isolated rat aortic rings	ChEMBL	483	6	1	8	2.8	Cc1cc(C)c(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)n1	10.1016/S0960-894X(96)00617-8
	10281606	136450	0	None	-	2	Rat	6.8	pKd	=	6.8	Functional	Potency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic ringsPotency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic rings	ChEMBL	575	9	2	10	4.2	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCC#CCO	10.1016/s0960-894x(02)01084-3
	CHEMBL367382	136450	0	None	-	2	Rat	6.8	pKd	=	6.8	Functional	Potency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic ringsPotency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic rings	ChEMBL	575	9	2	10	4.2	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCC#CCO	10.1016/s0960-894x(02)01084-3
	44311284	211024	0	None	-	2	Rat	7.8	pKd	=	7.8	Functional	Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)	ChEMBL	635	12	2	10	6.5	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C(C)C)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	CHEMBL71070	211024	0	None	-	2	Rat	7.8	pKd	=	7.8	Functional	Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)	ChEMBL	635	12	2	10	6.5	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C(C)C)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	44311346	109940	0	None	-	2	Rat	6.8	pKd	=	6.8	Functional	Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)	ChEMBL	681	13	2	13	5.2	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCSCC2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	CHEMBL308088	109940	0	None	-	2	Rat	6.8	pKd	=	6.8	Functional	Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)	ChEMBL	681	13	2	13	5.2	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCSCC2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	CHEMBL1790962	215689	0	None	-2	2	Pig	7.7	pKd	=	7.7	Functional	ETA receptor antagonist activity was measured by inhibition of ET-1 induced vasoconstriction in isolated porcine coronary arteryETA receptor antagonist activity was measured by inhibition of ET-1 induced vasoconstriction in isolated porcine coronary artery	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)[C@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1021/jm00077a013
	CHEMBL2373291	217153	0	None	-1	2	Pig	7.7	pKd	=	7.7	Functional	ETA receptor antagonist activity was measured by inhibition of ET-1 induced vasoconstriction in isolated porcine coronary arteryETA receptor antagonist activity was measured by inhibition of ET-1 induced vasoconstriction in isolated porcine coronary artery	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H]2CSSC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1021/jm00077a013
	44311528	210921	0	None	-	2	Rat	7.7	pKd	=	7.7	Functional	Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)	ChEMBL	633	12	2	10	6.3	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C2CC2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	CHEMBL70487	210921	0	None	-	2	Rat	7.7	pKd	=	7.7	Functional	Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)	ChEMBL	633	12	2	10	6.3	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C2CC2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	10122675	105248	0	None	-	2	Rat	7.7	pKd	=	7.7	Functional	Potency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic ringsPotency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic rings	ChEMBL	682	12	2	13	5.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccncc2)nc1OCC#CCOC(=O)Nc1cnccn1	10.1016/s0960-894x(02)01084-3
	CHEMBL275897	105248	0	None	-	2	Rat	7.7	pKd	=	7.7	Functional	Potency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic ringsPotency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic rings	ChEMBL	682	12	2	13	5.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccncc2)nc1OCC#CCOC(=O)Nc1cnccn1	10.1016/s0960-894x(02)01084-3
	10146640	214333	0	None	-	2	Rat	7.7	pKd	=	7.7	Functional	Potency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic ringsPotency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic rings	ChEMBL	689	12	2	13	4.5	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccccn1	10.1016/s0960-894x(02)01084-3
	CHEMBL94786	214333	0	None	-	2	Rat	7.7	pKd	=	7.7	Functional	Potency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic ringsPotency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic rings	ChEMBL	689	12	2	13	4.5	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccccn1	10.1016/s0960-894x(02)01084-3
	10212088	103471	0	None	-	2	Rat	6.7	pKd	=	6.7	Functional	Potency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic ringsPotency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic rings	ChEMBL	688	12	2	12	5.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccccc1	10.1016/s0960-894x(02)01084-3
	CHEMBL264035	103471	0	None	-	2	Rat	6.7	pKd	=	6.7	Functional	Potency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic ringsPotency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic rings	ChEMBL	688	12	2	12	5.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccccc1	10.1016/s0960-894x(02)01084-3
	10211772	63297	0	None	-	2	Rat	6.6	pKd	=	6.6	Functional	Potency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic ringsPotency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic rings	ChEMBL	660	11	2	12	4.2	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccccc1	10.1016/s0960-894x(02)01084-3
	CHEMBL163638	63297	0	None	-	2	Rat	6.6	pKd	=	6.6	Functional	Potency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic ringsPotency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic rings	ChEMBL	660	11	2	12	4.2	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccccc1	10.1016/s0960-894x(02)01084-3
	9917072	68877	0	None	-	2	Rat	6.6	pKd	=	6.6	Functional	In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)	ChEMBL	619	16	2	10	4.6	CCCS(=O)(=O)NCCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	CHEMBL177538	68877	0	None	-	2	Rat	6.6	pKd	=	6.6	Functional	In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)	ChEMBL	619	16	2	10	4.6	CCCS(=O)(=O)NCCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	9809270	138118	0	None	-	2	Rat	6.6	pKd	=	6.6	Functional	In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)	ChEMBL	622	14	2	12	2.3	CCCS(=O)(=O)NCCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	CHEMBL368738	138118	0	None	-	2	Rat	6.6	pKd	=	6.6	Functional	In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)	ChEMBL	622	14	2	12	2.3	CCCS(=O)(=O)NCCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	9870830	213493	38	None	-1	5	Human	7.6	pKd	=	7.6	Functional	Antagonism of ET-1 induced contraction of rabbit femoral artery rings (Endothelin A receptor mediated)Antagonism of ET-1 induced contraction of rabbit femoral artery rings (Endothelin A receptor mediated)	ChEMBL	506	8	1	9	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1	10.1021/jm9606507
	CHEMBL8981	213493	38	None	-1	5	Human	7.6	pKd	=	7.6	Functional	Antagonism of ET-1 induced contraction of rabbit femoral artery rings (Endothelin A receptor mediated)Antagonism of ET-1 induced contraction of rabbit femoral artery rings (Endothelin A receptor mediated)	ChEMBL	506	8	1	9	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1	10.1021/jm9606507
	44311283	109110	0	None	-	2	Rat	7.6	pKd	=	7.6	Functional	Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)	ChEMBL	649	11	2	10	6.7	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C(C)(C)C)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	CHEMBL303649	109110	0	None	-	2	Rat	7.6	pKd	=	7.6	Functional	Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)	ChEMBL	649	11	2	10	6.7	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C(C)(C)C)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	23670447	9803	2	None	1	4	Human	7.6	pKd	=	7.6	Functional	pA2 value towards endothelin receptor A was determined as functional ETA antagonismpA2 value towards endothelin receptor A was determined as functional ETA antagonism	ChEMBL	528	10	0	9	0.1	COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+]	10.1016/s0960-894x(97)10151-2
	999	9803	2	None	1	4	Human	7.6	pKd	=	7.6	Functional	pA2 value towards endothelin receptor A was determined as functional ETA antagonismpA2 value towards endothelin receptor A was determined as functional ETA antagonism	ChEMBL	528	10	0	9	0.1	COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+]	10.1016/s0960-894x(97)10151-2
	CHEMBL1204799	9803	2	None	1	4	Human	7.6	pKd	=	7.6	Functional	pA2 value towards endothelin receptor A was determined as functional ETA antagonismpA2 value towards endothelin receptor A was determined as functional ETA antagonism	ChEMBL	528	10	0	9	0.1	COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+]	10.1016/s0960-894x(97)10151-2
	CHEMBL25438	9803	2	None	1	4	Human	7.6	pKd	=	7.6	Functional	pA2 value towards endothelin receptor A was determined as functional ETA antagonismpA2 value towards endothelin receptor A was determined as functional ETA antagonism	ChEMBL	528	10	0	9	0.1	COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+]	10.1016/s0960-894x(97)10151-2
	44386169	138167	0	None	-	2	Rat	7.6	pKd	=	7.6	Functional	Potency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic ringsPotency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic rings	ChEMBL	690	12	2	14	3.9	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1cnccn1	10.1016/s0960-894x(02)01084-3
	CHEMBL368996	138167	0	None	-	2	Rat	7.6	pKd	=	7.6	Functional	Potency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic ringsPotency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic rings	ChEMBL	690	12	2	14	3.9	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1cnccn1	10.1016/s0960-894x(02)01084-3
	10190108	137476	0	None	-	2	Rat	7.6	pKd	=	7.6	Functional	Potency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic ringsPotency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic rings	ChEMBL	681	12	2	12	5.7	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccncc2)nc1OCC#CCOC(=O)Nc1ccccn1	10.1016/s0960-894x(02)01084-3
	CHEMBL368386	137476	0	None	-	2	Rat	7.6	pKd	=	7.6	Functional	Potency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic ringsPotency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic rings	ChEMBL	681	12	2	12	5.7	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccncc2)nc1OCC#CCOC(=O)Nc1ccccn1	10.1016/s0960-894x(02)01084-3
	10211781	136519	0	None	-	2	Rat	7.6	pKd	=	7.6	Functional	Potency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic ringsPotency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic rings	ChEMBL	661	11	2	13	3.6	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccccn1	10.1016/s0960-894x(02)01084-3
	CHEMBL367453	136519	0	None	-	2	Rat	7.6	pKd	=	7.6	Functional	Potency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic ringsPotency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic rings	ChEMBL	661	11	2	13	3.6	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccccn1	10.1016/s0960-894x(02)01084-3
	18184229	66382	0	None	-	2	Rat	6.5	pKd	=	6.5	Functional	In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)	ChEMBL	605	15	2	10	4.2	CCCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	CHEMBL171950	66382	0	None	-	2	Rat	6.5	pKd	=	6.5	Functional	In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)	ChEMBL	605	15	2	10	4.2	CCCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	9894460	213488	9	None	-158	4	Rat	8.5	pKd	=	8.5	Functional	Compound was evaluated for the antagonism at the Endothelin A receptor (G-protein coupled endothelin A)Compound was evaluated for the antagonism at the Endothelin A receptor (G-protein coupled endothelin A)	ChEMBL	539	10	2	7	4.8	CCCc1cc(C(=O)O)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2	10.1016/S0960-894X(96)00617-8
	CHEMBL313871	213488	9	None	-158	4	Rat	8.5	pKd	=	8.5	Functional	Compound was evaluated for the antagonism at the Endothelin A receptor (G-protein coupled endothelin A)Compound was evaluated for the antagonism at the Endothelin A receptor (G-protein coupled endothelin A)	ChEMBL	539	10	2	7	4.8	CCCc1cc(C(=O)O)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2	10.1016/S0960-894X(96)00617-8
	CHEMBL8978	213488	9	None	-158	4	Rat	8.5	pKd	=	8.5	Functional	Compound was evaluated for the antagonism at the Endothelin A receptor (G-protein coupled endothelin A)Compound was evaluated for the antagonism at the Endothelin A receptor (G-protein coupled endothelin A)	ChEMBL	539	10	2	7	4.8	CCCc1cc(C(=O)O)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2	10.1016/S0960-894X(96)00617-8
	10311570	21402	0	None	-	2	Human	8.5	pKd	=	8.5	Functional	pA2 value towards endothelin receptor A was determined as functional ETA antagonismpA2 value towards endothelin receptor A was determined as functional ETA antagonism	ChEMBL	520	10	1	9	4.7	COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1	10.1016/s0960-894x(97)10151-2
	CHEMBL1205068	21402	0	None	-	2	Human	8.5	pKd	=	8.5	Functional	pA2 value towards endothelin receptor A was determined as functional ETA antagonismpA2 value towards endothelin receptor A was determined as functional ETA antagonism	ChEMBL	520	10	1	9	4.7	COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1	10.1016/s0960-894x(97)10151-2
	CHEMBL48907	21402	0	None	-	2	Human	8.5	pKd	=	8.5	Functional	pA2 value towards endothelin receptor A was determined as functional ETA antagonismpA2 value towards endothelin receptor A was determined as functional ETA antagonism	ChEMBL	520	10	1	9	4.7	COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1	10.1016/s0960-894x(97)10151-2
	9830495	137927	0	None	-	2	Rat	6.5	pKd	=	6.5	Functional	In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)	ChEMBL	618	14	2	9	5.0	CCS(=O)(=O)NCCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	CHEMBL368617	137927	0	None	-	2	Rat	6.5	pKd	=	6.5	Functional	In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)	ChEMBL	618	14	2	9	5.0	CCS(=O)(=O)NCCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	9874557	136516	0	None	-	2	Rat	6.5	pKd	=	6.5	Functional	In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)	ChEMBL	667	15	2	10	5.5	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CC2)nc1OCCCNS(=O)(=O)c1ccc(C)cc1	10.1016/s0960-894x(02)01083-1
	CHEMBL367443	136516	0	None	-	2	Rat	6.5	pKd	=	6.5	Functional	In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)	ChEMBL	667	15	2	10	5.5	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CC2)nc1OCCCNS(=O)(=O)c1ccc(C)cc1	10.1016/s0960-894x(02)01083-1
	9864880	109165	0	None	-	1	Human	7.5	pKd	=	7.5	Functional	pA2 value towards endothelin receptor A was determined as functional ETA antagonismpA2 value towards endothelin receptor A was determined as functional ETA antagonism	ChEMBL	384	4	1	6	3.7	CN(C)c1cccc2c(S(=O)(=O)Nc3ccc4nsnc4c3)cccc12	10.1016/s0960-894x(97)10151-2
	CHEMBL303902	109165	0	None	-	1	Human	7.5	pKd	=	7.5	Functional	pA2 value towards endothelin receptor A was determined as functional ETA antagonismpA2 value towards endothelin receptor A was determined as functional ETA antagonism	ChEMBL	384	4	1	6	3.7	CN(C)c1cccc2c(S(=O)(=O)Nc3ccc4nsnc4c3)cccc12	10.1016/s0960-894x(97)10151-2
	9810571	68160	0	None	-	2	Rat	5.5	pKd	=	5.5	Functional	In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)	ChEMBL	731	18	2	13	5.0	CCCS(=O)(=O)NCCOc1nc(-c2cc(OC)c(OC)c(OC)c2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	CHEMBL176997	68160	0	None	-	2	Rat	5.5	pKd	=	5.5	Functional	In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)	ChEMBL	731	18	2	13	5.0	CCCS(=O)(=O)NCCOc1nc(-c2cc(OC)c(OC)c(OC)c2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	9873255	66408	0	None	-	2	Rat	6.5	pKd	=	6.5	Functional	In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)	ChEMBL	591	14	2	10	3.8	CCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	CHEMBL172071	66408	0	None	-	2	Rat	6.5	pKd	=	6.5	Functional	In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)	ChEMBL	591	14	2	10	3.8	CCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	CHEMBL2373292	217154	0	None	-2	2	Pig	7.4	pKd	=	7.4	Functional	ETA receptor antagonist activity was measured by inhibition of ET-1 induced vasoconstriction in isolated porcine coronary arteryETA receptor antagonist activity was measured by inhibition of ET-1 induced vasoconstriction in isolated porcine coronary artery	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)(C)C)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1021/jm00077a013
	44298982	202399	0	None	-	0	Rat	6.4	pKd	=	6.4	Functional	Functional antagonism against ETA receptor in rat aortic rings expressed as pA2 valueFunctional antagonism against ETA receptor in rat aortic rings expressed as pA2 value	ChEMBL	445	7	1	6	5.2	CCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc(OC)cc1	10.1016/S0960-894X(97)00319-3
	CHEMBL55621	202399	0	None	-	0	Rat	6.4	pKd	=	6.4	Functional	Functional antagonism against ETA receptor in rat aortic rings expressed as pA2 valueFunctional antagonism against ETA receptor in rat aortic rings expressed as pA2 value	ChEMBL	445	7	1	6	5.2	CCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc(OC)cc1	10.1016/S0960-894X(97)00319-3
	10122442	137475	0	None	-	2	Rat	6.4	pKd	=	6.4	Functional	Potency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic ringsPotency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic rings	ChEMBL	660	14	2	11	5.6	CCCCNC(=O)OCC#CCOc1nc(-c2ccncc2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	CHEMBL368383	137475	0	None	-	2	Rat	6.4	pKd	=	6.4	Functional	Potency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic ringsPotency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic rings	ChEMBL	660	14	2	11	5.6	CCCCNC(=O)OCC#CCOc1nc(-c2ccncc2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	18184194	137340	0	None	-	2	Rat	5.3	pKd	=	5.3	Functional	In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)	ChEMBL	712	15	2	12	4.5	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCCNS(=O)(=O)c1ccc(C)cc1	10.1016/s0960-894x(02)01083-1
	CHEMBL368107	137340	0	None	-	2	Rat	5.3	pKd	=	5.3	Functional	In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)	ChEMBL	712	15	2	12	4.5	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCCNS(=O)(=O)c1ccc(C)cc1	10.1016/s0960-894x(02)01083-1
	44311345	210996	0	None	-	2	Rat	8.3	pKd	=	8.3	Functional	Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)	ChEMBL	663	13	3	12	5.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CCNCC2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	CHEMBL70895	210996	0	None	-	2	Rat	8.3	pKd	=	8.3	Functional	Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)	ChEMBL	663	13	3	12	5.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CCNCC2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	104865	7493	99	None	1	5	Rat	7.3	pKd	=	7.3	Functional	Compound was evaluated for in vitro functional inhibitory potency for prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)Compound was evaluated for in vitro functional inhibitory potency for prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/S0960-894X(97)00400-9
	3494	7493	99	None	1	5	Rat	7.3	pKd	=	7.3	Functional	Compound was evaluated for in vitro functional inhibitory potency for prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)Compound was evaluated for in vitro functional inhibitory potency for prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/S0960-894X(97)00400-9
	392	7493	99	None	1	5	Rat	7.3	pKd	=	7.3	Functional	Compound was evaluated for in vitro functional inhibitory potency for prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)Compound was evaluated for in vitro functional inhibitory potency for prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/S0960-894X(97)00400-9
	CHEMBL957	7493	99	None	1	5	Rat	7.3	pKd	=	7.3	Functional	Compound was evaluated for in vitro functional inhibitory potency for prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)Compound was evaluated for in vitro functional inhibitory potency for prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/S0960-894X(97)00400-9
	DB00559	7493	99	None	1	5	Rat	7.3	pKd	=	7.3	Functional	Compound was evaluated for in vitro functional inhibitory potency for prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)Compound was evaluated for in vitro functional inhibitory potency for prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/S0960-894X(97)00400-9
	10005597	126596	0	None	1	2	Rat	6.3	pKd	=	6.3	Functional	In vitro antagonistic activity against endothelin A receptor in isolated rat aortic ringsIn vitro antagonistic activity against endothelin A receptor in isolated rat aortic rings	ChEMBL	485	7	1	7	5.2	COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3cc(OC)ccc3OC)c3c2oc2ccccc23)cc1	10.1016/s0960-894x(99)00040-2
	CHEMBL348407	126596	0	None	1	2	Rat	6.3	pKd	=	6.3	Functional	In vitro antagonistic activity against endothelin A receptor in isolated rat aortic ringsIn vitro antagonistic activity against endothelin A receptor in isolated rat aortic rings	ChEMBL	485	7	1	7	5.2	COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3cc(OC)ccc3OC)c3c2oc2ccccc23)cc1	10.1016/s0960-894x(99)00040-2
	10168597	68111	0	None	-	2	Rat	6.3	pKd	=	6.3	Functional	Potency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic ringsPotency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic rings	ChEMBL	661	11	2	13	3.6	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1cccnc1	10.1016/s0960-894x(02)01084-3
	CHEMBL176741	68111	0	None	-	2	Rat	6.3	pKd	=	6.3	Functional	Potency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic ringsPotency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic rings	ChEMBL	661	11	2	13	3.6	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1cccnc1	10.1016/s0960-894x(02)01084-3
	CHEMBL411171	219646	0	None	-19	2	Pig	5.3	pKd	=	5.3	Functional	ETA receptor antagonist activity was measured by inhibition of ET-1 induced vasoconstriction in isolated porcine coronary arteryETA receptor antagonist activity was measured by inhibition of ET-1 induced vasoconstriction in isolated porcine coronary artery	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00077a013
	10233400	135463	0	None	-	2	Rat	7.3	pKd	=	7.3	Functional	Potency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic ringsPotency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic rings	ChEMBL	661	11	2	13	3.6	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccncc1	10.1016/s0960-894x(02)01084-3
	CHEMBL366885	135463	0	None	-	2	Rat	7.3	pKd	=	7.3	Functional	Potency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic ringsPotency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic rings	ChEMBL	661	11	2	13	3.6	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccncc1	10.1016/s0960-894x(02)01084-3
	10305334	135825	0	None	-	2	Rat	6.3	pKd	=	6.3	Functional	Potency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic ringsPotency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic rings	ChEMBL	680	12	2	11	6.3	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccncc2)nc1OCC#CCOC(=O)Nc1ccccc1	10.1016/s0960-894x(02)01084-3
	CHEMBL367036	135825	0	None	-	2	Rat	6.3	pKd	=	6.3	Functional	Potency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic ringsPotency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic rings	ChEMBL	680	12	2	11	6.3	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccncc2)nc1OCC#CCOC(=O)Nc1ccccc1	10.1016/s0960-894x(02)01084-3
	192311	114051	4	None	-	1	Pig	7.2	pKd	=	7.2	Functional	Antagonistic activity towards ET- l-induced contraction in porcine coronary arteriesAntagonistic activity towards ET- l-induced contraction in porcine coronary arteries	ChEMBL	513	11	5	4	2.8	CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	CHEMBL31702	114051	4	None	-	1	Pig	7.2	pKd	=	7.2	Functional	Antagonistic activity towards ET- l-induced contraction in porcine coronary arteriesAntagonistic activity towards ET- l-induced contraction in porcine coronary arteries	ChEMBL	513	11	5	4	2.8	CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	10457385	119465	0	None	85	2	Rat	6.2	pKd	=	6.2	Functional	Compound was evaluated for the antagonism at the Endothelin A receptor (G-protein coupled endothelin A)Compound was evaluated for the antagonism at the Endothelin A receptor (G-protein coupled endothelin A)	ChEMBL	469	6	1	8	2.5	Cc1ccc(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)n1	10.1016/S0960-894X(96)00617-8
	CHEMBL330424	119465	0	None	85	2	Rat	6.2	pKd	=	6.2	Functional	Compound was evaluated for the antagonism at the Endothelin A receptor (G-protein coupled endothelin A)Compound was evaluated for the antagonism at the Endothelin A receptor (G-protein coupled endothelin A)	ChEMBL	469	6	1	8	2.5	Cc1ccc(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)n1	10.1016/S0960-894X(96)00617-8
	11755275	206788	0	None	-1	2	Rat	5.2	pKd	=	5.2	Functional	Functional antagonism against ETA receptor in rat aortic rings expressed as pA2 valueFunctional antagonism against ETA receptor in rat aortic rings expressed as pA2 value	ChEMBL	489	9	1	7	4.8	CCOc1ccc2c(c1)c(-c1ccc(OC)cc1)c(C(=O)O)c(=O)n2Cc1cc(OC)ccc1OC	10.1016/S0960-894X(97)00319-3
	CHEMBL59537	206788	0	None	-1	2	Rat	5.2	pKd	=	5.2	Functional	Functional antagonism against ETA receptor in rat aortic rings expressed as pA2 valueFunctional antagonism against ETA receptor in rat aortic rings expressed as pA2 value	ChEMBL	489	9	1	7	4.8	CCOc1ccc2c(c1)c(-c1ccc(OC)cc1)c(C(=O)O)c(=O)n2Cc1cc(OC)ccc1OC	10.1016/S0960-894X(97)00319-3
	9831249	66471	0	None	-	2	Rat	6.2	pKd	=	6.2	Functional	In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)	ChEMBL	672	14	2	10	6.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C2CC2)nc1OCCCNS(=O)(=O)c1cccs1	10.1016/s0960-894x(02)01083-1
	CHEMBL172297	66471	0	None	-	2	Rat	6.2	pKd	=	6.2	Functional	In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)	ChEMBL	672	14	2	10	6.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C2CC2)nc1OCCCNS(=O)(=O)c1cccs1	10.1016/s0960-894x(02)01083-1
	10146377	67188	0	None	-	2	Rat	8.1	pKd	=	8.1	Functional	Potency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic ringsPotency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic rings	ChEMBL	662	11	2	14	3.0	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1cnccn1	10.1016/s0960-894x(02)01084-3
	CHEMBL175058	67188	0	None	-	2	Rat	8.1	pKd	=	8.1	Functional	Potency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic ringsPotency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic rings	ChEMBL	662	11	2	14	3.0	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1cnccn1	10.1016/s0960-894x(02)01084-3
	44384715	67136	0	None	-	2	Rat	7.2	pKd	=	7.2	Functional	Potency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic ringsPotency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic rings	ChEMBL	559	9	1	9	5.2	CC#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	CHEMBL174607	67136	0	None	-	2	Rat	7.2	pKd	=	7.2	Functional	Potency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic ringsPotency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic rings	ChEMBL	559	9	1	9	5.2	CC#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	104865	7493	99	None	1	5	Rat	7.1	pKd	=	7.1	Functional	Potency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic ringsPotency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic rings	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/s0960-894x(02)01084-3
	3494	7493	99	None	1	5	Rat	7.1	pKd	=	7.1	Functional	Potency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic ringsPotency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic rings	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/s0960-894x(02)01084-3
	392	7493	99	None	1	5	Rat	7.1	pKd	=	7.1	Functional	Potency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic ringsPotency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic rings	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/s0960-894x(02)01084-3
	CHEMBL957	7493	99	None	1	5	Rat	7.1	pKd	=	7.1	Functional	Potency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic ringsPotency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic rings	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/s0960-894x(02)01084-3
	DB00559	7493	99	None	1	5	Rat	7.1	pKd	=	7.1	Functional	Potency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic ringsPotency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic rings	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/s0960-894x(02)01084-3
	9853077	66401	0	None	-	2	Rat	6.1	pKd	=	6.1	Functional	In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)	ChEMBL	696	13	2	12	5.3	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCNS(=O)(=O)c1cccs1	10.1016/s0960-894x(02)01083-1
	CHEMBL172030	66401	0	None	-	2	Rat	6.1	pKd	=	6.1	Functional	In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)	ChEMBL	696	13	2	12	5.3	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCNS(=O)(=O)c1cccs1	10.1016/s0960-894x(02)01083-1
	9961131	138935	0	None	-	2	Rat	6.1	pKd	=	6.1	Functional	In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)	ChEMBL	650	15	2	12	3.1	CCCS(=O)(=O)NCCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	CHEMBL369676	138935	0	None	-	2	Rat	6.1	pKd	=	6.1	Functional	In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)	ChEMBL	650	15	2	12	3.1	CCCS(=O)(=O)NCCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	9830773	137004	0	None	-	2	Rat	7.0	pKd	=	7.0	Functional	In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)	ChEMBL	636	14	2	12	2.8	CCS(=O)(=O)NCCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	CHEMBL367958	137004	0	None	-	2	Rat	7.0	pKd	=	7.0	Functional	In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)	ChEMBL	636	14	2	12	2.8	CCS(=O)(=O)NCCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	10096179	183799	0	None	-	0	Human	8.7	pKi	=	8.7	Functional	Antagonist activity against human ETA receptor using CHO cellsAntagonist activity against human ETA receptor using CHO cells	ChEMBL	468	9	1	5	5.7	CCOc1ccc(-c2cc(C)nc(OC(C(=O)O)C(C)(c3ccccc3)c3ccccc3)n2)cc1	10.1016/s0960-894x(03)00236-1
	CHEMBL46311	183799	0	None	-	0	Human	8.7	pKi	=	8.7	Functional	Antagonist activity against human ETA receptor using CHO cellsAntagonist activity against human ETA receptor using CHO cells	ChEMBL	468	9	1	5	5.7	CCOc1ccc(-c2cc(C)nc(OC(C(=O)O)C(C)(c3ccccc3)c3ccccc3)n2)cc1	10.1016/s0960-894x(03)00236-1
	10070	7237	47	None	109	2	Human	6.7	pA2	=	6.7	Functional	UnclassifiedUnclassified	Guide to Pharmacology	544	8	2	8	2.5	Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N	18780830
	25099191	7237	47	None	109	2	Human	6.7	pA2	=	6.7	Functional	UnclassifiedUnclassified	Guide to Pharmacology	544	8	2	8	2.5	Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N	18780830
	CHEMBL2165326	7237	47	None	109	2	Human	6.7	pA2	=	6.7	Functional	UnclassifiedUnclassified	Guide to Pharmacology	544	8	2	8	2.5	Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N	18780830
	DB15059	7237	47	None	109	2	Human	6.7	pA2	=	6.7	Functional	UnclassifiedUnclassified	Guide to Pharmacology	544	8	2	8	2.5	Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N	18780830
	3951	7179	86	None	47	2	Human	7.1	pA2	=	7.1	Functional	UnclassifiedUnclassified	Guide to Pharmacology	378	7	1	5	3.5	COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1	15139756
	4337	7179	86	None	47	2	Human	7.1	pA2	=	7.1	Functional	UnclassifiedUnclassified	Guide to Pharmacology	378	7	1	5	3.5	COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1	15139756
	6918493	7179	86	None	47	2	Human	7.1	pA2	=	7.1	Functional	UnclassifiedUnclassified	Guide to Pharmacology	378	7	1	5	3.5	COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1	15139756
	CHEMBL1111	7179	86	None	47	2	Human	7.1	pA2	=	7.1	Functional	UnclassifiedUnclassified	Guide to Pharmacology	378	7	1	5	3.5	COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1	15139756
	DB06403	7179	86	None	47	2	Human	7.1	pA2	=	7.1	Functional	UnclassifiedUnclassified	Guide to Pharmacology	378	7	1	5	3.5	COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1	15139756
	443289	7498	47	None	1	4	Human	7.2	pA2	=	7.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	7647976
	997	7498	47	None	1	4	Human	7.2	pA2	=	7.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	7647976
	CHEMBL314691	7498	47	None	1	4	Human	7.2	pA2	=	7.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	7647976
	DB12054	7498	47	None	1	4	Human	7.2	pA2	=	7.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	7647976
	104865	7493	99	None	1	5	Rat	7.2	pA2	=	7.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	8035319
	3494	7493	99	None	1	5	Rat	7.2	pA2	=	7.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	8035319
	392	7493	99	None	1	5	Rat	7.2	pA2	=	7.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	8035319
	CHEMBL957	7493	99	None	1	5	Rat	7.2	pA2	=	7.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	8035319
	DB00559	7493	99	None	1	5	Rat	7.2	pA2	=	7.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	8035319
	11477084	10382	53	None	58	2	Human	8.0	pA2	=	8	Functional	UnclassifiedUnclassified	Guide to Pharmacology	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	9171878
	216235	10382	53	None	58	2	Human	8.0	pA2	=	8	Functional	UnclassifiedUnclassified	Guide to Pharmacology	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	9171878
	3548	10382	53	None	58	2	Human	8.0	pA2	=	8	Functional	UnclassifiedUnclassified	Guide to Pharmacology	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	9171878
	3950	10382	53	None	58	2	Human	8.0	pA2	=	8	Functional	UnclassifiedUnclassified	Guide to Pharmacology	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	9171878
	CHEMBL282724	10382	53	None	58	2	Human	8.0	pA2	=	8	Functional	UnclassifiedUnclassified	Guide to Pharmacology	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	9171878
	DB06268	10382	53	None	58	2	Human	8.0	pA2	=	8	Functional	UnclassifiedUnclassified	Guide to Pharmacology	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	9171878
	3913	10509	0	None	-1	2	Rat	8.4	pA2	=	8.4	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	7780649
	5311469	10509	0	None	-1	2	Rat	8.4	pA2	=	8.4	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	7780649
	23670447	9803	2	None	1	4	Human	8.7	pA2	=	8.7	Functional	UnclassifiedUnclassified	Guide to Pharmacology	528	10	0	9	0.1	COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+]	10066864
	23670447	9803	2	None	1	4	Human	8.7	pA2	=	8.7	Functional	UnclassifiedUnclassified	Guide to Pharmacology	528	10	0	9	0.1	COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+]	9023329
	999	9803	2	None	1	4	Human	8.7	pA2	=	8.7	Functional	UnclassifiedUnclassified	Guide to Pharmacology	528	10	0	9	0.1	COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+]	10066864
	999	9803	2	None	1	4	Human	8.7	pA2	=	8.7	Functional	UnclassifiedUnclassified	Guide to Pharmacology	528	10	0	9	0.1	COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+]	9023329
	CHEMBL1204799	9803	2	None	1	4	Human	8.7	pA2	=	8.7	Functional	UnclassifiedUnclassified	Guide to Pharmacology	528	10	0	9	0.1	COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+]	10066864
	CHEMBL1204799	9803	2	None	1	4	Human	8.7	pA2	=	8.7	Functional	UnclassifiedUnclassified	Guide to Pharmacology	528	10	0	9	0.1	COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+]	9023329
	CHEMBL25438	9803	2	None	1	4	Human	8.7	pA2	=	8.7	Functional	UnclassifiedUnclassified	Guide to Pharmacology	528	10	0	9	0.1	COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+]	10066864
	CHEMBL25438	9803	2	None	1	4	Human	8.7	pA2	=	8.7	Functional	UnclassifiedUnclassified	Guide to Pharmacology	528	10	0	9	0.1	COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+]	9023329
	159594	7310	45	None	2	4	Human	9.2	pA2	=	9.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	8632312
	3487	7310	45	None	2	4	Human	9.2	pA2	=	9.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	8632312
	CHEMBL9194	7310	45	None	2	4	Human	9.2	pA2	=	9.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	8632312
	DB06199	7310	45	None	2	4	Human	9.2	pA2	=	9.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	8632312
	12286	7735	36	None	234	2	Human	9.5	pA2	=	9.5	Functional	UnclassifiedUnclassified	Guide to Pharmacology	577	11	3	13	2.4	Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC	9399983
	6433095	7735	36	None	234	2	Human	9.5	pA2	=	9.5	Functional	UnclassifiedUnclassified	Guide to Pharmacology	577	11	3	13	2.4	Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC	9399983
	CHEMBL109648	7735	36	None	234	2	Human	9.5	pA2	=	9.5	Functional	UnclassifiedUnclassified	Guide to Pharmacology	577	11	3	13	2.4	Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC	9399983
	DB06677	7735	36	None	234	2	Human	9.5	pA2	=	9.5	Functional	UnclassifiedUnclassified	Guide to Pharmacology	577	11	3	13	2.4	Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC	9399983
	5340	175509	106	None	1	3	Human	8.4	pIC50	=	8.4	Functional	NoneNone	Drug Central	255	3	2	5	1.5	Nc1ccc(S(=O)(=O)Nc2nccs2)cc1	None
	CHEMBL437	175509	106	None	1	3	Human	8.4	pIC50	=	8.4	Functional	NoneNone	Drug Central	255	3	2	5	1.5	Nc1ccc(S(=O)(=O)Nc2nccs2)cc1	None
	5344	180252	101	None	-100	6	Human	8.2	pIC50	=	8.2	Functional	Inhibitory concentration against Endothelin A receptorInhibitory concentration against Endothelin A receptor	Drug Central	267	3	2	5	1.7	Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C	None
	CHEMBL453	180252	101	None	-100	6	Human	8.2	pIC50	=	8.2	Functional	Inhibitory concentration against Endothelin A receptorInhibitory concentration against Endothelin A receptor	Drug Central	267	3	2	5	1.7	Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C	None
	6662	224518	0	None	-1	3	Human	8.2	pIC50	=	8.2	Functional	Inhibitory concentration against Endothelin A receptorInhibitory concentration against Endothelin A receptor	Drug Central	309	3	1	6	1.6	CC(=O)N(C1=C(C)C(C)=NO1)S(=O)(=O)C1=CC=C(N)C=C1	None
	8260	7319	54	None	141	2	Human	7.3	pIC50	=	7.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	479	8	1	9	3.9	COc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cn1)C)c1ccncc1	None
	9912992	7319	54	None	141	2	Human	7.3	pIC50	=	7.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	479	8	1	9	3.9	COc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cn1)C)c1ccncc1	None
	CHEMBL3989834	7319	54	None	141	2	Human	7.3	pIC50	=	7.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	479	8	1	9	3.9	COc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cn1)C)c1ccncc1	None
	107810	8465	30	None	-	1	Human	7.6	pIC50	=	7.6	Functional	UnclassifiedUnclassified	Guide to Pharmacology	604	12	4	6	3.4	CC(C[C@@H](C(=O)N[C@@H](C(=O)N[C@@H](C(=O)O)Cc1ccccn1)Cc1cn(c2c1cccc2)C)NC(=O)N1CCCCCC1)C	7647976
	998	8465	30	None	-	1	Human	7.6	pIC50	=	7.6	Functional	UnclassifiedUnclassified	Guide to Pharmacology	604	12	4	6	3.4	CC(C[C@@H](C(=O)N[C@@H](C(=O)N[C@@H](C(=O)O)Cc1ccccn1)Cc1cn(c2c1cccc2)C)NC(=O)N1CCCCCC1)C	7647976
	CHEMBL352396	8465	30	None	-	1	Human	7.6	pIC50	=	7.6	Functional	UnclassifiedUnclassified	Guide to Pharmacology	604	12	4	6	3.4	CC(C[C@@H](C(=O)N[C@@H](C(=O)N[C@@H](C(=O)O)Cc1ccccn1)Cc1cn(c2c1cccc2)C)NC(=O)N1CCCCCC1)C	7647976
	3951	7179	86	None	47	2	Human	7.7	pIC50	=	7.7	Functional	UnclassifiedUnclassified	Guide to Pharmacology	378	7	1	5	3.5	COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1	15139756
	4337	7179	86	None	47	2	Human	7.7	pIC50	=	7.7	Functional	UnclassifiedUnclassified	Guide to Pharmacology	378	7	1	5	3.5	COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1	15139756
	6918493	7179	86	None	47	2	Human	7.7	pIC50	=	7.7	Functional	UnclassifiedUnclassified	Guide to Pharmacology	378	7	1	5	3.5	COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1	15139756
	CHEMBL1111	7179	86	None	47	2	Human	7.7	pIC50	=	7.7	Functional	UnclassifiedUnclassified	Guide to Pharmacology	378	7	1	5	3.5	COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1	15139756
	DB06403	7179	86	None	47	2	Human	7.7	pIC50	=	7.7	Functional	UnclassifiedUnclassified	Guide to Pharmacology	378	7	1	5	3.5	COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1	15139756
	3539	10913	83	None	-	1	Human	8.3	pIC50	=	8.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	424	6	1	9	2.7	COc1nc(C)cnc1NS(=O)(=O)c1cccnc1c1ccc(cc1)c1nnco1	15956965
	9910224	10913	83	None	-	1	Human	8.3	pIC50	=	8.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	424	6	1	9	2.7	COc1nc(C)cnc1NS(=O)(=O)c1cccnc1c1ccc(cc1)c1nnco1	15956965
	CHEMBL1628688	10913	83	None	-	1	Human	8.3	pIC50	=	8.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	424	6	1	9	2.7	COc1nc(C)cnc1NS(=O)(=O)c1cccnc1c1ccc(cc1)c1nnco1	15956965
	DB06629	10913	83	None	-	1	Human	8.3	pIC50	=	8.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	424	6	1	9	2.7	COc1nc(C)cnc1NS(=O)(=O)c1cccnc1c1ccc(cc1)c1nnco1	15956965
	10070	7237	47	None	109	2	Human	8.5	pIC50	=	8.5	Functional	UnclassifiedUnclassified	Guide to Pharmacology	544	8	2	8	2.5	Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N	18780830
	25099191	7237	47	None	109	2	Human	8.5	pIC50	=	8.5	Functional	UnclassifiedUnclassified	Guide to Pharmacology	544	8	2	8	2.5	Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N	18780830
	CHEMBL2165326	7237	47	None	109	2	Human	8.5	pIC50	=	8.5	Functional	UnclassifiedUnclassified	Guide to Pharmacology	544	8	2	8	2.5	Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N	18780830
	DB15059	7237	47	None	109	2	Human	8.5	pIC50	=	8.5	Functional	UnclassifiedUnclassified	Guide to Pharmacology	544	8	2	8	2.5	Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N	18780830
	1000	10276	0	None	-	1	Human	8.9	pIC50	=	8.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	614	14	2	9	6.1	CCCCn1ncc(c1c1ccc(cc1OCc1ccccc1C(=O)O)OC)/C=C(/C(=O)O)\Cc1cc2OCOc2cc1OC	9694916
	5311425	10276	0	None	-	1	Human	8.9	pIC50	=	8.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	614	14	2	9	6.1	CCCCn1ncc(c1c1ccc(cc1OCc1ccccc1C(=O)O)OC)/C=C(/C(=O)O)\Cc1cc2OCOc2cc1OC	9694916
	CHEMBL1628624	10276	0	None	-	1	Human	8.9	pIC50	=	8.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	614	14	2	9	6.1	CCCCn1ncc(c1c1ccc(cc1OCc1ccccc1C(=O)O)OC)/C=C(/C(=O)O)\Cc1cc2OCOc2cc1OC	9694916
	16004692	9232	91	None	107	2	Human	9.3	pIC50	=	9.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	586	11	2	8	3.6	CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br	22862294
	4809	9232	91	None	107	2	Human	9.3	pIC50	=	9.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	586	11	2	8	3.6	CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br	22862294
	7352	9232	91	None	107	2	Human	9.3	pIC50	=	9.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	586	11	2	8	3.6	CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br	22862294
	CHEMBL2103873	9232	91	None	107	2	Human	9.3	pIC50	=	9.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	586	11	2	8	3.6	CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br	22862294
	DB08932	9232	91	None	107	2	Human	9.3	pIC50	=	9.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	586	11	2	8	3.6	CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br	22862294
	131845706	10245	6	None	-	1	Human	7.8	pIC50	None	7.8	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	7647976
	71308726	10245	6	None	-	1	Human	7.8	pIC50	None	7.8	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	7647976
	995	10245	6	None	-	1	Human	7.8	pIC50	None	7.8	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	7647976
	CHEMBL1222310	10245	6	None	-	1	Human	7.8	pIC50	None	7.8	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	7647976
	CHEMBL4524099	10245	6	None	-	1	Human	7.8	pIC50	None	7.8	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	7647976
	101598716	8343	30	None	-	1	Human	8.2	pIC50	None	8.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	7647976
	16133807	8343	30	None	-	1	Human	8.2	pIC50	None	8.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	7647976
	16212950	8343	30	None	-	1	Human	8.2	pIC50	None	8.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	7647976
	989	8343	30	None	-	1	Human	8.2	pIC50	None	8.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	7647976
	CHEMBL3775234	8343	30	None	-	1	Human	8.2	pIC50	None	8.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	7647976
	16133808	8345	0	None	-	1	Human	8.2	pIC50	None	8.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	7647976
	16219332	8345	0	None	-	1	Human	8.2	pIC50	None	8.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	7647976
	56947103	8345	0	None	-	1	Human	8.2	pIC50	None	8.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	7647976
	990	8345	0	None	-	1	Human	8.2	pIC50	None	8.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	7647976
	CHEMBL3774897	8345	0	None	-	1	Human	8.2	pIC50	None	8.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	7647976
	108002	10267	23	None	-1	2	Rat	9.4	pKB	=	9.4	Functional	UnclassifiedUnclassified	Guide to Pharmacology	520	10	2	7	4.7	CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC	8201588
	3528	10267	23	None	-1	2	Rat	9.4	pKB	=	9.4	Functional	UnclassifiedUnclassified	Guide to Pharmacology	520	10	2	7	4.7	CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC	8201588
	CHEMBL8823	10267	23	None	-1	2	Rat	9.4	pKB	=	9.4	Functional	UnclassifiedUnclassified	Guide to Pharmacology	520	10	2	7	4.7	CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC	8201588

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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
	28230148	212510	97	None	-	0	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	320	3	2	6	0.7	CCn1cc(C(=O)O)c(=O)c2cc(F)c(N3CCNCC3)nc21	10.1038/s41467-023-40064-9
	3229	212510	97	None	-	0	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	320	3	2	6	0.7	CCn1cc(C(=O)O)c(=O)c2cc(F)c(N3CCNCC3)nc21	10.1038/s41467-023-40064-9
	CHEMBL826	212510	97	None	-	0	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	320	3	2	6	0.7	CCn1cc(C(=O)O)c(=O)c2cc(F)c(N3CCNCC3)nc21	10.1038/s41467-023-40064-9
	41684	37995	105	None	-	0	Human	4.9	pAC50	=	4.9	Binding	Binding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	307	4	1	7	2.2	CC(=O)Oc1ccccc1C(=O)Nc1ncc([N+](=O)[O-])s1	10.1038/s41467-023-40064-9
	CHEMBL1401	37995	105	None	-	0	Human	4.9	pAC50	=	4.9	Binding	Binding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	307	4	1	7	2.2	CC(=O)Oc1ccccc1C(=O)Nc1ncc([N+](=O)[O-])s1	10.1038/s41467-023-40064-9
	54677470	207330	115	None	-	29	Human	4.9	pAC50	=	4.9	Binding	Binding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	351	2	2	6	2.0	Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1	10.1038/s41467-023-40064-9
	CHEMBL1256873	207330	115	None	-	29	Human	4.9	pAC50	=	4.9	Binding	Binding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	351	2	2	6	2.0	Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1	10.1038/s41467-023-40064-9
	CHEMBL599	207330	115	None	-	29	Human	4.9	pAC50	=	4.9	Binding	Binding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	351	2	2	6	2.0	Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1	10.1038/s41467-023-40064-9
	4829	206735	108	None	-	0	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	356	7	1	5	3.2	CCc1ccc(CCOc2ccc(CC3SC(=O)NC3=O)cc2)nc1	10.1038/s41467-023-40064-9
	CHEMBL595	206735	108	None	-	0	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	356	7	1	5	3.2	CCc1ccc(CCOc2ccc(CC3SC(=O)NC3=O)cc2)nc1	10.1038/s41467-023-40064-9
	104865	7493	99	None	1	4	Human	7.5	pAC50	=	7.5	Binding	Binding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1038/s41467-023-40064-9
	3494	7493	99	None	1	4	Human	7.5	pAC50	=	7.5	Binding	Binding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1038/s41467-023-40064-9
	392	7493	99	None	1	4	Human	7.5	pAC50	=	7.5	Binding	Binding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1038/s41467-023-40064-9
	CHEMBL957	7493	99	None	1	4	Human	7.5	pAC50	=	7.5	Binding	Binding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1038/s41467-023-40064-9
	DB00559	7493	99	None	1	4	Human	7.5	pAC50	=	7.5	Binding	Binding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1038/s41467-023-40064-9
	1209	8439	75	None	-	32	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	309	6	1	2	4.4	CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F	10.1038/s41467-023-40064-9
	203	8439	75	None	-	32	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	309	6	1	2	4.4	CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F	10.1038/s41467-023-40064-9
	3386	8439	75	None	-	32	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	309	6	1	2	4.4	CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F	10.1038/s41467-023-40064-9
	CHEMBL41	8439	75	None	-	32	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	309	6	1	2	4.4	CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F	10.1038/s41467-023-40064-9
	DB00472	8439	75	None	-	32	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	309	6	1	2	4.4	CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F	10.1038/s41467-023-40064-9
	5329102	201505	86	None	-	0	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	398	7	3	3	3.3	CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C	10.1038/s41467-023-40064-9
	CHEMBL535	201505	86	None	-	0	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	398	7	3	3	3.3	CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C	10.1038/s41467-023-40064-9
	135398513	72893	133	None	-	0	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	225	4	3	8	-0.9	Nc1nc(O)c2ncn(COCCO)c2n1	10.1038/s41467-023-40064-9
	CHEMBL184	72893	133	None	-	0	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	225	4	3	8	-0.9	Nc1nc(O)c2ncn(COCCO)c2n1	10.1038/s41467-023-40064-9
	CHEMBL2370066	216556	0	None	-	0	Human	7.9	pEC50	=	7.9	Binding	Effective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cellsEffective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCN)NC(=O)[C@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00070a001
	CHEMBL315841	217972	0	None	-	0	Human	7.8	pEC50	=	7.8	Binding	Effective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cellsEffective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1021/jm00070a001
	CHEMBL2370067	216557	0	None	-	0	Human	5.7	pEC50	=	5.7	Binding	Effective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cellsEffective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](N)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@H](C=O)Cc1c[nH]c2ccccc12)[C@@H](C)CC	10.1021/jm00070a001
	CHEMBL407269	219430	0	None	-	0	Human	7.6	pEC50	=	7.6	Binding	Effective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cellsEffective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00070a001
	CHEMBL313344	217891	0	None	-	0	Human	5.6	pEC50	=	5.6	Binding	Effective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cellsEffective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)CC	10.1021/jm00070a001
	CHEMBL387200	219187	0	None	-	0	Human	6.2	pEC50	=	6.2	Binding	Effective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cellsEffective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00070a001
	CHEMBL86703	222668	0	None	-	0	Human	5.2	pEC50	=	5.2	Binding	Effective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cellsEffective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)C(C)C	10.1021/jm00070a001
	44284437	106760	0	None	-	0	Human	11.0	pIC50	=	11.0	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	520	9	4	8	3.5	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(O)CO)c1	10.1016/j.bmcl.2004.01.008
	CHEMBL286621	106760	0	None	-	0	Human	11.0	pIC50	=	11.0	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	520	9	4	8	3.5	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(O)CO)c1	10.1016/j.bmcl.2004.01.008
	44284405	107132	0	None	-	0	Human	11.0	pIC50	=	11.0	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	532	10	2	7	5.4	COCC(C)Cc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O	10.1016/j.bmcl.2004.01.008
	CHEMBL289634	107132	0	None	-	0	Human	11.0	pIC50	=	11.0	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	532	10	2	7	5.4	COCC(C)Cc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O	10.1016/j.bmcl.2004.01.008
	44284287	168026	0	None	-	0	Human	11.0	pIC50	=	11.0	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	532	10	3	7	5.2	CCC(CO)Cc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O	10.1016/j.bmcl.2004.01.008
	CHEMBL411925	168026	0	None	-	0	Human	11.0	pIC50	=	11.0	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	532	10	3	7	5.2	CCC(CO)Cc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O	10.1016/j.bmcl.2004.01.008
	11017304	120917	0	None	-	0	Pig	10.9	pIC50	=	10.9	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	579	11	1	9	5.8	CCc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(SC)cn2)cc1	10.1021/jm0102304
	CHEMBL332922	120917	0	None	-	0	Pig	10.9	pIC50	=	10.9	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	579	11	1	9	5.8	CCc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(SC)cn2)cc1	10.1021/jm0102304
	44284288	106911	0	None	-	0	Human	10.9	pIC50	=	10.9	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	559	9	2	7	4.9	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(C)C(=O)N(C)C)c1	10.1016/j.bmcl.2004.01.008
	CHEMBL287683	106911	0	None	-	0	Human	10.9	pIC50	=	10.9	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	559	9	2	7	4.9	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(C)C(=O)N(C)C)c1	10.1016/j.bmcl.2004.01.008
	44284292	174891	0	None	-	0	Human	10.9	pIC50	=	10.9	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	518	8	3	7	4.9	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(C)(C)O)c1	10.1016/j.bmcl.2004.01.008
	CHEMBL432856	174891	0	None	-	0	Human	10.9	pIC50	=	10.9	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	518	8	3	7	4.9	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(C)(C)O)c1	10.1016/j.bmcl.2004.01.008
	9852318	16386	8	None	-	2	Rat	10.8	pIC50	=	10.8	Binding	Displacement of 125I-ET1 from ETA receptor in rat A7R5 cellsDisplacement of 125I-ET1 from ETA receptor in rat A7R5 cells	ChEMBL	613	11	2	9	4.5	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1016/j.bmcl.2016.06.014
	CHEMBL112624	16386	8	None	-	2	Rat	10.8	pIC50	=	10.8	Binding	Displacement of 125I-ET1 from ETA receptor in rat A7R5 cellsDisplacement of 125I-ET1 from ETA receptor in rat A7R5 cells	ChEMBL	613	11	2	9	4.5	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1016/j.bmcl.2016.06.014
	CHEMBL1627022	16386	8	None	-	2	Rat	10.8	pIC50	=	10.8	Binding	Displacement of 125I-ET1 from ETA receptor in rat A7R5 cellsDisplacement of 125I-ET1 from ETA receptor in rat A7R5 cells	ChEMBL	613	11	2	9	4.5	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1016/j.bmcl.2016.06.014
	11082446	16683	0	None	-	0	Pig	10.8	pIC50	=	10.8	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	581	12	1	11	4.6	COc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2Oc2cccc(OC)c2)nc1	10.1021/jm0102304
	CHEMBL114380	16683	0	None	-	0	Pig	10.8	pIC50	=	10.8	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	581	12	1	11	4.6	COc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2Oc2cccc(OC)c2)nc1	10.1021/jm0102304
	10897569	16912	0	None	-	0	Pig	10.7	pIC50	=	10.7	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	645	11	1	10	5.7	COc1ccccc1Sc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)ncnc1OCCOc1ncc(Br)cn1	10.1021/jm0102304
	CHEMBL115724	16912	0	None	-	0	Pig	10.7	pIC50	=	10.7	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	645	11	1	10	5.7	COc1ccccc1Sc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)ncnc1OCCOc1ncc(Br)cn1	10.1021/jm0102304
	10227760	107764	0	None	-	0	Human	10.7	pIC50	=	10.7	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	481	6	2	7	4.9	CC(=O)c1c(C)c(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl	10.1021/jm030528p
	CHEMBL294291	107764	0	None	-	0	Human	10.7	pIC50	=	10.7	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	481	6	2	7	4.9	CC(=O)c1c(C)c(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl	10.1021/jm030528p
	10163017	207560	0	None	-	0	Human	10.7	pIC50	=	10.7	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	482	6	3	8	4.6	C/C(=N\O)c1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl	10.1021/jm030528p
	CHEMBL60058	207560	0	None	-	0	Human	10.7	pIC50	=	10.7	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	482	6	3	8	4.6	C/C(=N\O)c1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl	10.1021/jm030528p
	44284236	129101	0	None	-	0	Human	10.7	pIC50	=	10.7	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	504	9	3	7	4.5	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CCCO)c1	10.1016/j.bmcl.2004.01.008
	CHEMBL35984	129101	0	None	-	0	Human	10.7	pIC50	=	10.7	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	504	9	3	7	4.5	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CCCO)c1	10.1016/j.bmcl.2004.01.008
	72548703	168346	0	None	-	0	Human	10.6	pIC50	=	10.6	Binding	Displacement of [125I]-endothelin-1 from human recombinant ETA receptor after 120 mins by scintillation counting analysisDisplacement of [125I]-endothelin-1 from human recombinant ETA receptor after 120 mins by scintillation counting analysis	ChEMBL	583	8	3	6	5.8	CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12	10.1016/j.bmcl.2018.03.093
	CHEMBL4128926	168346	0	None	-	0	Human	10.6	pIC50	=	10.6	Binding	Displacement of [125I]-endothelin-1 from human recombinant ETA receptor after 120 mins by scintillation counting analysisDisplacement of [125I]-endothelin-1 from human recombinant ETA receptor after 120 mins by scintillation counting analysis	ChEMBL	583	8	3	6	5.8	CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12	10.1016/j.bmcl.2018.03.093
	101598716	8343	30	None	-	0	Human	10.6	pIC50	=	10.6	Binding	Displacement of [125I]Endothelin-1 from human recombinant Endothelin-1 receptor expressed in CHO cellsDisplacement of [125I]Endothelin-1 from human recombinant Endothelin-1 receptor expressed in CHO cells	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.03.006
	16133807	8343	30	None	-	0	Human	10.6	pIC50	=	10.6	Binding	Displacement of [125I]Endothelin-1 from human recombinant Endothelin-1 receptor expressed in CHO cellsDisplacement of [125I]Endothelin-1 from human recombinant Endothelin-1 receptor expressed in CHO cells	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.03.006
	16212950	8343	30	None	-	0	Human	10.6	pIC50	=	10.6	Binding	Displacement of [125I]Endothelin-1 from human recombinant Endothelin-1 receptor expressed in CHO cellsDisplacement of [125I]Endothelin-1 from human recombinant Endothelin-1 receptor expressed in CHO cells	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.03.006
	989	8343	30	None	-	0	Human	10.6	pIC50	=	10.6	Binding	Displacement of [125I]Endothelin-1 from human recombinant Endothelin-1 receptor expressed in CHO cellsDisplacement of [125I]Endothelin-1 from human recombinant Endothelin-1 receptor expressed in CHO cells	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.03.006
	CHEMBL3775234	8343	30	None	-	0	Human	10.6	pIC50	=	10.6	Binding	Displacement of [125I]Endothelin-1 from human recombinant Endothelin-1 receptor expressed in CHO cellsDisplacement of [125I]Endothelin-1 from human recombinant Endothelin-1 receptor expressed in CHO cells	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.03.006
	101598716	8343	30	None	-	0	Human	10.6	pIC50	=	10.6	Binding	Displacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cells measured after 120 mins by scintillation counting method	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.11.014
	16133807	8343	30	None	-	0	Human	10.6	pIC50	=	10.6	Binding	Displacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cells measured after 120 mins by scintillation counting method	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.11.014
	16212950	8343	30	None	-	0	Human	10.6	pIC50	=	10.6	Binding	Displacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cells measured after 120 mins by scintillation counting method	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.11.014
	989	8343	30	None	-	0	Human	10.6	pIC50	=	10.6	Binding	Displacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cells measured after 120 mins by scintillation counting method	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.11.014
	CHEMBL3775234	8343	30	None	-	0	Human	10.6	pIC50	=	10.6	Binding	Displacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cells measured after 120 mins by scintillation counting method	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.11.014
	44284288	106911	0	None	-	0	Human	10.6	pIC50	=	10.6	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	559	9	2	7	4.9	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(C)C(=O)N(C)C)c1	10.1016/j.bmcl.2004.01.008
	CHEMBL287683	106911	0	None	-	0	Human	10.6	pIC50	=	10.6	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	559	9	2	7	4.9	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(C)C(=O)N(C)C)c1	10.1016/j.bmcl.2004.01.008
	44284405	107132	0	None	-	0	Human	10.6	pIC50	=	10.6	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	532	10	2	7	5.4	COCC(C)Cc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O	10.1016/j.bmcl.2004.01.008
	CHEMBL289634	107132	0	None	-	0	Human	10.6	pIC50	=	10.6	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	532	10	2	7	5.4	COCC(C)Cc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O	10.1016/j.bmcl.2004.01.008
	9873636	180603	0	None	-	0	Rat	10.6	pIC50	=	10.6	Binding	Displacement of 125I-ET1 from ETA receptor in rat A7R5 cellsDisplacement of 125I-ET1 from ETA receptor in rat A7R5 cells	ChEMBL	607	10	1	10	6.4	CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2cc3ccccc3s2)nc1	10.1016/j.bmcl.2016.06.014
	CHEMBL4538570	180603	0	None	-	0	Rat	10.6	pIC50	=	10.6	Binding	Displacement of 125I-ET1 from ETA receptor in rat A7R5 cellsDisplacement of 125I-ET1 from ETA receptor in rat A7R5 cells	ChEMBL	607	10	1	10	6.4	CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2cc3ccccc3s2)nc1	10.1016/j.bmcl.2016.06.014
	44381151	66163	0	None	-	0	Pig	10.6	pIC50	=	10.6	Binding	In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.	ChEMBL	671	13	1	10	6.3	CCCc1nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c(Oc2ccccc2OC)c(OCCOc2ncc(Br)cn2)n1	10.1016/s0960-894x(01)00682-5
	CHEMBL170908	66163	0	None	-	0	Pig	10.6	pIC50	=	10.6	Binding	In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.	ChEMBL	671	13	1	10	6.3	CCCc1nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c(Oc2ccccc2OC)c(OCCOc2ncc(Br)cn2)n1	10.1016/s0960-894x(01)00682-5
	44284266	143710	0	None	-	0	Human	10.6	pIC50	=	10.6	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	531	8	2	7	4.6	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CN(C)C(C)=O)c1	10.1016/j.bmcl.2004.01.008
	CHEMBL37427	143710	0	None	-	0	Human	10.6	pIC50	=	10.6	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	531	8	2	7	4.6	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CN(C)C(C)=O)c1	10.1016/j.bmcl.2004.01.008
	11039156	16842	0	None	-	0	Pig	10.6	pIC50	=	10.6	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	581	11	1	10	5.2	COc1cccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(SC)cn2)c1	10.1021/jm0102304
	CHEMBL115333	16842	0	None	-	0	Pig	10.6	pIC50	=	10.6	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	581	11	1	10	5.2	COc1cccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(SC)cn2)c1	10.1021/jm0102304
	10206855	107679	0	None	-	0	Human	10.5	pIC50	=	10.5	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	493	7	2	7	5.0	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)C2CC2)c1	10.1021/jm030528p
	CHEMBL293830	107679	0	None	-	0	Human	10.5	pIC50	=	10.5	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	493	7	2	7	5.0	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)C2CC2)c1	10.1021/jm030528p
	10185556	109433	0	None	-	0	Human	10.5	pIC50	=	10.5	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	503	6	2	8	3.8	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(S(C)(=O)=O)c1	10.1021/jm030528p
	CHEMBL304460	109433	0	None	-	0	Human	10.5	pIC50	=	10.5	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	503	6	2	8	3.8	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(S(C)(=O)=O)c1	10.1021/jm030528p
	10228523	208009	0	None	-	0	Human	10.5	pIC50	=	10.5	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	495	7	2	7	5.3	CCC(=O)c1c(C)c(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl	10.1021/jm030528p
	CHEMBL60367	208009	0	None	-	0	Human	10.5	pIC50	=	10.5	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	495	7	2	7	5.3	CCC(=O)c1c(C)c(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl	10.1021/jm030528p
	44284238	106903	0	None	-	0	Human	10.5	pIC50	=	10.5	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	490	8	3	7	4.2	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CCO)c1	10.1016/j.bmcl.2004.01.008
	CHEMBL287622	106903	0	None	-	0	Human	10.5	pIC50	=	10.5	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	490	8	3	7	4.2	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CCO)c1	10.1016/j.bmcl.2004.01.008
	10152810	21558	2	None	-	0	Rat	10.5	pIC50	=	10.5	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	538	10	1	9	4.8	COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1F	10.1016/s0960-894x(98)00301-1
	CHEMBL1206706	21558	2	None	-	0	Rat	10.5	pIC50	=	10.5	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	538	10	1	9	4.8	COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1F	10.1016/s0960-894x(98)00301-1
	CHEMBL298725	21558	2	None	-	0	Rat	10.5	pIC50	=	10.5	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	538	10	1	9	4.8	COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1F	10.1016/s0960-894x(98)00301-1
	159594	7310	45	None	1	3	Human	10.5	pIC50	=	10.5	Binding	Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm970101g
	3487	7310	45	None	1	3	Human	10.5	pIC50	=	10.5	Binding	Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm970101g
	CHEMBL9194	7310	45	None	1	3	Human	10.5	pIC50	=	10.5	Binding	Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm970101g
	DB06199	7310	45	None	1	3	Human	10.5	pIC50	=	10.5	Binding	Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm970101g
	10962637	16851	0	None	-	0	Rat	10.5	pIC50	=	10.5	Binding	Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane	ChEMBL	549	10	2	9	4.3	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(CO)cn2)cc1	10.1021/jm000538f
	CHEMBL115372	16851	0	None	-	0	Rat	10.5	pIC50	=	10.5	Binding	Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane	ChEMBL	549	10	2	9	4.3	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(CO)cn2)cc1	10.1021/jm000538f
	CHEMBL1627023	16851	0	None	-	0	Rat	10.5	pIC50	=	10.5	Binding	Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane	ChEMBL	549	10	2	9	4.3	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(CO)cn2)cc1	10.1021/jm000538f
	159594	7310	45	None	1	3	Human	10.5	pIC50	=	10.5	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm990171i
	3487	7310	45	None	1	3	Human	10.5	pIC50	=	10.5	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm990171i
	CHEMBL9194	7310	45	None	1	3	Human	10.5	pIC50	=	10.5	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm990171i
	DB06199	7310	45	None	1	3	Human	10.5	pIC50	=	10.5	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm990171i
	11767155	18513	0	None	-	0	Pig	10.4	pIC50	=	10.4	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	596	10	1	9	5.9	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(-c3ccccn3)cn2)cc1	10.1021/jm0102304
	CHEMBL1181545	18513	0	None	-	0	Pig	10.4	pIC50	=	10.4	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	596	10	1	9	5.9	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(-c3ccccn3)cn2)cc1	10.1021/jm0102304
	CHEMBL177173	18513	0	None	-	0	Pig	10.4	pIC50	=	10.4	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	596	10	1	9	5.9	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(-c3ccccn3)cn2)cc1	10.1021/jm0102304
	44284041	107079	0	None	-	0	Human	10.4	pIC50	=	10.4	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	520	9	3	8	4.4	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OC(C)CO)c1	10.1016/j.bmcl.2004.01.008
	CHEMBL289216	107079	0	None	-	0	Human	10.4	pIC50	=	10.4	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	520	9	3	8	4.4	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OC(C)CO)c1	10.1016/j.bmcl.2004.01.008
	9938571	16369	0	None	-	1	Rat	10.4	pIC50	=	10.4	Binding	Ability to inhibit specific binding of [125I]- -ET-1 to rat A 10 cells which express endothelin A receptorAbility to inhibit specific binding of [125I]- -ET-1 to rat A 10 cells which express endothelin A receptor	ChEMBL	597	9	1	8	5.6	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm000538f
	CHEMBL112531	16369	0	None	-	1	Rat	10.4	pIC50	=	10.4	Binding	Ability to inhibit specific binding of [125I]- -ET-1 to rat A 10 cells which express endothelin A receptorAbility to inhibit specific binding of [125I]- -ET-1 to rat A 10 cells which express endothelin A receptor	ChEMBL	597	9	1	8	5.6	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm000538f
	CHEMBL369489	16369	0	None	-	1	Rat	10.4	pIC50	=	10.4	Binding	Ability to inhibit specific binding of [125I]- -ET-1 to rat A 10 cells which express endothelin A receptorAbility to inhibit specific binding of [125I]- -ET-1 to rat A 10 cells which express endothelin A receptor	ChEMBL	597	9	1	8	5.6	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm000538f
	9938571	16369	0	None	-	1	Rat	10.4	pIC50	=	10.4	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	597	9	1	8	5.6	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm0102304
	CHEMBL112531	16369	0	None	-	1	Rat	10.4	pIC50	=	10.4	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	597	9	1	8	5.6	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm0102304
	CHEMBL369489	16369	0	None	-	1	Rat	10.4	pIC50	=	10.4	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	597	9	1	8	5.6	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm0102304
	10187997	116749	0	None	-	0	Rat	10.4	pIC50	=	10.4	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	564	13	1	7	4.2	CCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1	10.1021/jm031041j
	CHEMBL323464	116749	0	None	-	0	Rat	10.4	pIC50	=	10.4	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	564	13	1	7	4.2	CCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1	10.1021/jm031041j
	11828009	16663	0	None	-	0	Pig	10.4	pIC50	=	10.4	Binding	Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane	ChEMBL	581	11	2	10	4.7	CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc(CO)cc2)nc1	10.1021/jm000538f
	CHEMBL114298	16663	0	None	-	0	Pig	10.4	pIC50	=	10.4	Binding	Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane	ChEMBL	581	11	2	10	4.7	CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc(CO)cc2)nc1	10.1021/jm000538f
	11966523	117147	0	None	-	0	Pig	10.4	pIC50	=	10.4	Binding	Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane	ChEMBL	613	10	2	9	4.7	CC(C)(C)c1ccc(S(=O)(=O)Nc2ncnc(OCCOc3ncc(Br)cn3)c2-c2ccc(CO)cc2)cc1	10.1021/jm000538f
	CHEMBL324184	117147	0	None	-	0	Pig	10.4	pIC50	=	10.4	Binding	Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane	ChEMBL	613	10	2	9	4.7	CC(C)(C)c1ccc(S(=O)(=O)Nc2ncnc(OCCOc3ncc(Br)cn3)c2-c2ccc(CO)cc2)cc1	10.1021/jm000538f
	9934302	79419	1	None	-	0	Human	10.4	pIC50	=	10.4	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	467	6	2	7	4.6	CC(=O)c1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl	10.1021/jm030528p
	CHEMBL19950	79419	1	None	-	0	Human	10.4	pIC50	=	10.4	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	467	6	2	7	4.6	CC(=O)c1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl	10.1021/jm030528p
	11752337	169007	0	None	-	0	Human	10.4	pIC50	=	10.4	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	496	7	2	8	4.7	CO/N=C(\C)c1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl	10.1021/jm030528p
	CHEMBL416324	169007	0	None	-	0	Human	10.4	pIC50	=	10.4	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	496	7	2	8	4.7	CO/N=C(\C)c1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl	10.1021/jm030528p
	23445355	207681	0	None	-	0	Human	10.4	pIC50	=	10.4	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	469	6	2	8	3.8	COC(=O)c1cc(C)ccc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl	10.1021/jm030528p
	CHEMBL60149	207681	0	None	-	0	Human	10.4	pIC50	=	10.4	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	469	6	2	8	3.8	COC(=O)c1cc(C)ccc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl	10.1021/jm030528p
	9934302	79419	1	None	-	0	Human	10.4	pIC50	=	10.4	Binding	Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor	ChEMBL	467	6	2	7	4.6	CC(=O)c1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl	10.1021/jm000349x
	CHEMBL19950	79419	1	None	-	0	Human	10.4	pIC50	=	10.4	Binding	Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor	ChEMBL	467	6	2	7	4.6	CC(=O)c1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl	10.1021/jm000349x
	44284115	106971	0	None	-	0	Human	10.4	pIC50	=	10.4	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	518	9	3	7	4.8	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(C)CO)c1	10.1016/j.bmcl.2004.01.008
	CHEMBL288247	106971	0	None	-	0	Human	10.4	pIC50	=	10.4	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	518	9	3	7	4.8	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(C)CO)c1	10.1016/j.bmcl.2004.01.008
	44381125	66063	0	None	-	0	Pig	10.4	pIC50	=	10.4	Binding	In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.	ChEMBL	674	10	1	9	6.6	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)nc(-c3ccccn3)nc2OCCOc2ncc(Br)cn2)cc1	10.1016/s0960-894x(01)00682-5
	CHEMBL170493	66063	0	None	-	0	Pig	10.4	pIC50	=	10.4	Binding	In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.	ChEMBL	674	10	1	9	6.6	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)nc(-c3ccccn3)nc2OCCOc2ncc(Br)cn2)cc1	10.1016/s0960-894x(01)00682-5
	10187997	116749	0	None	-	0	Human	10.4	pIC50	=	10.4	Binding	Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).	ChEMBL	564	13	1	7	4.2	CCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1	10.1021/jm970101g
	CHEMBL323464	116749	0	None	-	0	Human	10.4	pIC50	=	10.4	Binding	Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).	ChEMBL	564	13	1	7	4.2	CCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1	10.1021/jm970101g
	44284287	168026	0	None	-	0	Human	10.4	pIC50	=	10.4	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	532	10	3	7	5.2	CCC(CO)Cc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O	10.1016/j.bmcl.2004.01.008
	CHEMBL411925	168026	0	None	-	0	Human	10.4	pIC50	=	10.4	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	532	10	3	7	5.2	CCC(CO)Cc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O	10.1016/j.bmcl.2004.01.008
	44284481	220504	0	None	-4	5	Human	10.3	pIC50	=	10.3	Binding	Inhibition of ETA receptor in human SK-N-MC cells after 60 mins by scintillation countingInhibition of ETA receptor in human SK-N-MC cells after 60 mins by scintillation counting	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/np900287e
	CHEMBL437472	220504	0	None	-4	5	Human	10.3	pIC50	=	10.3	Binding	Inhibition of ETA receptor in human SK-N-MC cells after 60 mins by scintillation countingInhibition of ETA receptor in human SK-N-MC cells after 60 mins by scintillation counting	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/np900287e
	44284328	134319	0	None	-	0	Human	10.3	pIC50	=	10.3	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	476	7	2	7	4.6	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OC)c1	10.1016/j.bmcl.2004.01.008
	CHEMBL36627	134319	0	None	-	0	Human	10.3	pIC50	=	10.3	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	476	7	2	7	4.6	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OC)c1	10.1016/j.bmcl.2004.01.008
	44284437	106760	0	None	-	0	Human	10.3	pIC50	=	10.3	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	520	9	4	8	3.5	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(O)CO)c1	10.1016/j.bmcl.2004.01.008
	CHEMBL286621	106760	0	None	-	0	Human	10.3	pIC50	=	10.3	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	520	9	4	8	3.5	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(O)CO)c1	10.1016/j.bmcl.2004.01.008
	44386450	69172	0	None	-	0	Rat	10.3	pIC50	=	10.3	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	606	15	1	10	5.1	COC(=O)CCCCOc1cc(C/C(C(=O)c2ccc(OC)cc2)=C(/C(=O)O)c2ccc3c(c2)OCO3)cc(OC)c1OC	10.1021/jm031041j
	CHEMBL177973	69172	0	None	-	0	Rat	10.3	pIC50	=	10.3	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	606	15	1	10	5.1	COC(=O)CCCCOc1cc(C/C(C(=O)c2ccc(OC)cc2)=C(/C(=O)O)c2ccc3c(c2)OCO3)cc(OC)c1OC	10.1021/jm031041j
	44284481	220504	0	None	-4	5	Human	10.3	pIC50	=	10.3	Binding	Binding affinity to human ETA receptor by radioligand displacement assayBinding affinity to human ETA receptor by radioligand displacement assay	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/j.ejmech.2013.01.044
	CHEMBL437472	220504	0	None	-4	5	Human	10.3	pIC50	=	10.3	Binding	Binding affinity to human ETA receptor by radioligand displacement assayBinding affinity to human ETA receptor by radioligand displacement assay	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/j.ejmech.2013.01.044
	10143256	107350	0	None	-	0	Human	10.3	pIC50	=	10.3	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	531	7	2	8	4.6	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(S(=O)(=O)C(C)C)c1	10.1021/jm030528p
	CHEMBL291592	107350	0	None	-	0	Human	10.3	pIC50	=	10.3	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	531	7	2	8	4.6	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(S(=O)(=O)C(C)C)c1	10.1021/jm030528p
	10183338	209565	0	None	-	0	Human	10.3	pIC50	=	10.3	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	464	5	2	7	4.5	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C#N)c1C	10.1021/jm030528p
	CHEMBL62159	209565	0	None	-	0	Human	10.3	pIC50	=	10.3	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	464	5	2	7	4.5	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C#N)c1C	10.1021/jm030528p
	10722385	107275	0	None	-	0	Human	10.3	pIC50	=	10.3	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	606	13	1	11	4.6	COC(=O)CCCCOc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc(OC)c1OC	10.1021/jm980504w
	CHEMBL291058	107275	0	None	-	0	Human	10.3	pIC50	=	10.3	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	606	13	1	11	4.6	COC(=O)CCCCOc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc(OC)c1OC	10.1021/jm980504w
	11006709	16729	0	None	-	0	Pig	10.3	pIC50	=	10.3	Binding	In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membraneIn vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane	ChEMBL	629	11	1	10	5.4	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)c1	10.1016/s0960-894x(01)00682-5
	CHEMBL114700	16729	0	None	-	0	Pig	10.3	pIC50	=	10.3	Binding	In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membraneIn vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane	ChEMBL	629	11	1	10	5.4	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)c1	10.1016/s0960-894x(01)00682-5
	11006709	16729	0	None	-	0	Pig	10.3	pIC50	=	10.3	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	629	11	1	10	5.4	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)c1	10.1021/jm0102304
	CHEMBL114700	16729	0	None	-	0	Pig	10.3	pIC50	=	10.3	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	629	11	1	10	5.4	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)c1	10.1021/jm0102304
	10651488	170158	0	None	-	0	Human	10.3	pIC50	=	10.3	Binding	Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).	ChEMBL	618	13	1	7	4.8	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCC(F)(F)F	10.1021/jm970101g
	CHEMBL419367	170158	0	None	-	0	Human	10.3	pIC50	=	10.3	Binding	Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).	ChEMBL	618	13	1	7	4.8	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCC(F)(F)F	10.1021/jm970101g
	159594	7310	45	None	1	3	Human	10.3	pIC50	=	10.3	Binding	Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membraneDisplacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/acs.jmedchem.5b01781
	3487	7310	45	None	1	3	Human	10.3	pIC50	=	10.3	Binding	Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membraneDisplacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/acs.jmedchem.5b01781
	CHEMBL9194	7310	45	None	1	3	Human	10.3	pIC50	=	10.3	Binding	Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membraneDisplacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/acs.jmedchem.5b01781
	DB06199	7310	45	None	1	3	Human	10.3	pIC50	=	10.3	Binding	Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membraneDisplacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/acs.jmedchem.5b01781
	44284041	107079	0	None	-	0	Human	10.2	pIC50	=	10.2	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	520	9	3	8	4.4	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OC(C)CO)c1	10.1016/j.bmcl.2004.01.008
	CHEMBL289216	107079	0	None	-	0	Human	10.2	pIC50	=	10.2	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	520	9	3	8	4.4	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OC(C)CO)c1	10.1016/j.bmcl.2004.01.008
	11734600	16782	0	None	-	0	Pig	10.2	pIC50	=	10.2	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	585	11	1	10	5.3	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Cl)cn2)c1	10.1021/jm0102304
	CHEMBL114964	16782	0	None	-	0	Pig	10.2	pIC50	=	10.2	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	585	11	1	10	5.3	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Cl)cn2)c1	10.1021/jm0102304
	44284115	106971	0	None	-	0	Human	10.2	pIC50	=	10.2	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	518	9	3	7	4.8	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(C)CO)c1	10.1016/j.bmcl.2004.01.008
	CHEMBL288247	106971	0	None	-	0	Human	10.2	pIC50	=	10.2	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	518	9	3	7	4.8	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(C)CO)c1	10.1016/j.bmcl.2004.01.008
	10119327	209535	0	None	-	0	Human	10.2	pIC50	=	10.2	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	531	8	2	8	4.6	CCCS(=O)(=O)c1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl	10.1021/jm030528p
	CHEMBL62019	209535	0	None	-	0	Human	10.2	pIC50	=	10.2	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	531	8	2	8	4.6	CCCS(=O)(=O)c1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl	10.1021/jm030528p
	10206155	209555	0	None	-	0	Human	10.2	pIC50	=	10.2	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	481	7	2	7	5.0	CCC(=O)c1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl	10.1021/jm030528p
	CHEMBL62112	209555	0	None	-	0	Human	10.2	pIC50	=	10.2	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	481	7	2	7	5.0	CCC(=O)c1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl	10.1021/jm030528p
	10344914	106913	0	None	-	0	Human	10.2	pIC50	=	10.2	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	476	7	3	7	4.1	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CO)c1	10.1016/j.bmcl.2004.01.008
	CHEMBL287711	106913	0	None	-	0	Human	10.2	pIC50	=	10.2	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	476	7	3	7	4.1	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CO)c1	10.1016/j.bmcl.2004.01.008
	44284391	146079	0	None	-	0	Human	10.2	pIC50	=	10.2	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	532	9	3	7	5.3	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CCC(C)(C)O)c1	10.1016/j.bmcl.2004.01.008
	CHEMBL37920	146079	0	None	-	0	Human	10.2	pIC50	=	10.2	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	532	9	3	7	5.3	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CCC(C)(C)O)c1	10.1016/j.bmcl.2004.01.008
	10119177	124243	0	None	-	0	Rat	10.2	pIC50	=	10.2	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	528	12	1	6	4.8	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1	10.1021/jm010237l
	CHEMBL339904	124243	0	None	-	0	Rat	10.2	pIC50	=	10.2	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	528	12	1	6	4.8	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1	10.1021/jm010237l
	10603409	117381	0	None	-	0	Human	10.2	pIC50	=	10.2	Binding	Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).	ChEMBL	584	13	1	7	4.1	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCCl	10.1021/jm970101g
	CHEMBL325581	117381	0	None	-	0	Human	10.2	pIC50	=	10.2	Binding	Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).	ChEMBL	584	13	1	7	4.1	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCCl	10.1021/jm970101g
	10228588	108635	0	None	-	0	Human	10.2	pIC50	=	10.2	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	496	6	2	7	4.1	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)N(C)C)c1	10.1021/jm030528p
	CHEMBL300577	108635	0	None	-	0	Human	10.2	pIC50	=	10.2	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	496	6	2	7	4.1	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)N(C)C)c1	10.1021/jm030528p
	10210629	15536	0	None	-	0	Human	10.1	pIC50	=	10.1	Binding	Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).	ChEMBL	592	15	1	7	5.0	CCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1	10.1021/jm970101g
	CHEMBL109644	15536	0	None	-	0	Human	10.1	pIC50	=	10.1	Binding	Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).	ChEMBL	592	15	1	7	5.0	CCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1	10.1021/jm970101g
	9916235	16125	1	None	-	0	Human	10.1	pIC50	=	10.1	Binding	Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).	ChEMBL	578	14	1	7	4.6	CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1	10.1021/jm970101g
	CHEMBL111277	16125	1	None	-	0	Human	10.1	pIC50	=	10.1	Binding	Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).	ChEMBL	578	14	1	7	4.6	CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1	10.1021/jm970101g
	159594	7310	45	None	1	3	Human	10.1	pIC50	=	10.1	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm990170q
	3487	7310	45	None	1	3	Human	10.1	pIC50	=	10.1	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm990170q
	CHEMBL9194	7310	45	None	1	3	Human	10.1	pIC50	=	10.1	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm990170q
	DB06199	7310	45	None	1	3	Human	10.1	pIC50	=	10.1	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm990170q
	9916235	16125	1	None	-	0	Human	10.1	pIC50	=	10.1	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	578	14	1	7	4.6	CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1	10.1021/jm990170q
	CHEMBL111277	16125	1	None	-	0	Human	10.1	pIC50	=	10.1	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	578	14	1	7	4.6	CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1	10.1021/jm990170q
	10278217	108547	0	None	-	0	Human	10.1	pIC50	=	10.1	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	492	6	2	8	5.0	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(-c2ncco2)c1	10.1021/jm030528p
	CHEMBL299921	108547	0	None	-	0	Human	10.1	pIC50	=	10.1	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	492	6	2	8	5.0	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(-c2ncco2)c1	10.1021/jm030528p
	9911482	174852	20	None	-	0	Human	10.1	pIC50	=	10.1	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	447	6	2	7	4.2	CC(=O)c1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1C	10.1021/jm030528p
	CHEMBL432521	174852	20	None	-	0	Human	10.1	pIC50	=	10.1	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	447	6	2	7	4.2	CC(=O)c1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1C	10.1021/jm030528p
	10114414	205601	0	None	-	0	Human	10.1	pIC50	=	10.1	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	444	5	2	7	4.2	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2C)c(C#N)c1C	10.1021/jm030528p
	CHEMBL58359	205601	0	None	-	0	Human	10.1	pIC50	=	10.1	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	444	5	2	7	4.2	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2C)c(C#N)c1C	10.1021/jm030528p
	11766844	116558	0	None	-	0	Rat	10.1	pIC50	=	10.1	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	553	9	1	8	5.5	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Cl)cn2)cc1	10.1021/jm0102304
	CHEMBL176272	116558	0	None	-	0	Rat	10.1	pIC50	=	10.1	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	553	9	1	8	5.5	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Cl)cn2)cc1	10.1021/jm0102304
	CHEMBL323243	116558	0	None	-	0	Rat	10.1	pIC50	=	10.1	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	553	9	1	8	5.5	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Cl)cn2)cc1	10.1021/jm0102304
	159594	7310	45	None	-1	3	Rat	10.1	pIC50	=	10.1	Binding	Inhibitory activity against human Endothelin A receptorInhibitory activity against human Endothelin A receptor	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm010237l
	3487	7310	45	None	-1	3	Rat	10.1	pIC50	=	10.1	Binding	Inhibitory activity against human Endothelin A receptorInhibitory activity against human Endothelin A receptor	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm010237l
	CHEMBL9194	7310	45	None	-1	3	Rat	10.1	pIC50	=	10.1	Binding	Inhibitory activity against human Endothelin A receptorInhibitory activity against human Endothelin A receptor	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm010237l
	DB06199	7310	45	None	-1	3	Rat	10.1	pIC50	=	10.1	Binding	Inhibitory activity against human Endothelin A receptorInhibitory activity against human Endothelin A receptor	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm010237l
	10115469	107615	0	None	-	0	Human	10.1	pIC50	=	10.1	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	459	5	2	6	5.0	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(Cl)c1	10.1021/jm030528p
	CHEMBL293398	107615	0	None	-	0	Human	10.1	pIC50	=	10.1	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	459	5	2	6	5.0	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(Cl)c1	10.1021/jm030528p
	10627272	210835	0	None	-	0	Human	10.1	pIC50	=	10.1	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	592	12	1	11	4.2	COC(=O)CCCOc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc(OC)c1OC	10.1021/jm980504w
	CHEMBL69986	210835	0	None	-	0	Human	10.1	pIC50	=	10.1	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	592	12	1	11	4.2	COC(=O)CCCOc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc(OC)c1OC	10.1021/jm980504w
	10603409	117381	0	None	-	0	Rat	10.0	pIC50	=	10.0	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	584	13	1	7	4.1	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCCl	10.1021/jm970101g
	CHEMBL325581	117381	0	None	-	0	Rat	10.0	pIC50	=	10.0	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	584	13	1	7	4.1	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCCl	10.1021/jm970101g
	10187997	116749	0	None	-	0	Rat	10.0	pIC50	=	10	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	564	13	1	7	4.2	CCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1	10.1021/jm970101g
	CHEMBL323464	116749	0	None	-	0	Rat	10.0	pIC50	=	10	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	564	13	1	7	4.2	CCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1	10.1021/jm970101g
	21041278	178556	0	None	-	0	Human	10.0	pIC50	=	10	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	554	12	2	9	3.5	CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Br)cc1	10.1016/j.bmcl.2016.06.014
	CHEMBL4467748	178556	0	None	-	0	Human	10.0	pIC50	=	10	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	554	12	2	9	3.5	CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Br)cc1	10.1016/j.bmcl.2016.06.014
	10165963	109626	0	None	-	0	Human	10.0	pIC50	=	10	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	545	8	2	9	3.6	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)CS(C)(=O)=O)c1	10.1021/jm030528p
	CHEMBL305602	109626	0	None	-	0	Human	10.0	pIC50	=	10	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	545	8	2	9	3.6	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)CS(C)(=O)=O)c1	10.1021/jm030528p
	10366278	179243	0	None	-	0	Human	10.0	pIC50	=	10	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	446	6	2	6	4.6	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1	10.1016/s0960-894x(02)00663-7
	CHEMBL448165	179243	0	None	-	0	Human	10.0	pIC50	=	10	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	446	6	2	6	4.6	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1	10.1016/s0960-894x(02)00663-7
	10624511	78513	0	None	-	0	Human	10.0	pIC50	=	10	Binding	Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor	ChEMBL	478	6	2	7	4.7	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2noc(C)c2Cl)c(C)c1CC#N	10.1021/jm000349x
	CHEMBL19661	78513	0	None	-	0	Human	10.0	pIC50	=	10	Binding	Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor	ChEMBL	478	6	2	7	4.7	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2noc(C)c2Cl)c(C)c1CC#N	10.1021/jm000349x
	10210629	15536	0	None	-	0	Rat	10.0	pIC50	=	10.0	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	592	15	1	7	5.0	CCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1	10.1021/jm970101g
	CHEMBL109644	15536	0	None	-	0	Rat	10.0	pIC50	=	10.0	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	592	15	1	7	5.0	CCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1	10.1021/jm970101g
	11827657	26153	1	None	-	0	Rat	10.0	pIC50	=	10.0	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	540	13	1	7	4.7	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(OC)c1	10.1021/jm010237l
	CHEMBL129220	26153	1	None	-	0	Rat	10.0	pIC50	=	10.0	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	540	13	1	7	4.7	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(OC)c1	10.1021/jm010237l
	44284481	220504	0	None	-4	5	Human	10.0	pIC50	=	10.0	Binding	Binding affinity to human ETA receptor by radioligand displacement assayBinding affinity to human ETA receptor by radioligand displacement assay	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/j.bmc.2013.03.016
	CHEMBL437472	220504	0	None	-4	5	Human	10.0	pIC50	=	10.0	Binding	Binding affinity to human ETA receptor by radioligand displacement assayBinding affinity to human ETA receptor by radioligand displacement assay	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/j.bmc.2013.03.016
	44302615	207203	0	None	-	0	Human	10.0	pIC50	=	10.0	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	497	7	2	8	4.6	Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)OC(C)C)c1	10.1021/jm030528p
	CHEMBL59819	207203	0	None	-	0	Human	10.0	pIC50	=	10.0	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	497	7	2	8	4.6	Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)OC(C)C)c1	10.1021/jm030528p
	25211074	25257	0	None	-	0	Human	10.0	pIC50	=	10.0	Binding	Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer	ChEMBL	543	10	2	7	5.1	CCCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2	10.1016/j.bmcl.2010.08.074
	CHEMBL1272244	25257	0	None	-	0	Human	10.0	pIC50	=	10.0	Binding	Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer	ChEMBL	543	10	2	7	5.1	CCCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2	10.1016/j.bmcl.2010.08.074
	11016761	115800	0	None	-	0	Pig	10.0	pIC50	=	10.0	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	519	9	1	8	4.8	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncccn2)cc1	10.1021/jm0102304
	CHEMBL321242	115800	0	None	-	0	Pig	10.0	pIC50	=	10.0	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	519	9	1	8	4.8	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncccn2)cc1	10.1021/jm0102304
	44284329	107188	0	None	-	0	Human	10.0	pIC50	=	10.0	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	504	8	2	7	5.4	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OC(C)C)c1	10.1016/j.bmcl.2004.01.008
	CHEMBL290181	107188	0	None	-	0	Human	10.0	pIC50	=	10.0	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	504	8	2	7	5.4	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OC(C)C)c1	10.1016/j.bmcl.2004.01.008
	9914310	213422	8	None	1995	2	Human	10.0	pIC50	=	10.0	Binding	Radioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cells	ChEMBL	510	12	1	6	4.7	CCCCN(CCCC)C(=O)CN1CC(c2ccc3c(c2)OCO3)C(C(=O)O)C1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL8923	213422	8	None	1995	2	Human	10.0	pIC50	=	10.0	Binding	Radioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cells	ChEMBL	510	12	1	6	4.7	CCCCN(CCCC)C(=O)CN1CC(c2ccc3c(c2)OCO3)C(C(=O)O)C1c1ccc(OC)cc1	10.1021/jm9505369
	10768977	68622	0	None	-	0	Rat	9.9	pIC50	=	9.9	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	548	13	1	8	5.6	CCOc1cc(C/C(C(=O)c2ccc(OC)cc2)=C(/C(=O)O)c2ccc3c(c2)OCO3)cc(OCC)c1OCC	10.1021/jm031041j
	CHEMBL177378	68622	0	None	-	0	Rat	9.9	pIC50	=	9.9	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	548	13	1	8	5.6	CCOc1cc(C/C(C(=O)c2ccc(OC)cc2)=C(/C(=O)O)c2ccc3c(c2)OCO3)cc(OCC)c1OCC	10.1021/jm031041j
	44352079	123319	0	None	-	0	Rat	9.9	pIC50	=	9.9	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	494	11	1	5	5.0	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(C)cc1	10.1021/jm010237l
	CHEMBL336272	123319	0	None	-	0	Rat	9.9	pIC50	=	9.9	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	494	11	1	5	5.0	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(C)cc1	10.1021/jm010237l
	10674176	169479	0	None	-	0	Human	9.9	pIC50	=	9.9	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	548	11	1	9	5.0	CCOc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc(OCC)c1OCC	10.1021/jm9606507
	CHEMBL417067	169479	0	None	-	0	Human	9.9	pIC50	=	9.9	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	548	11	1	9	5.0	CCOc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc(OCC)c1OCC	10.1021/jm9606507
	44334146	174779	0	None	-	0	Human	9.9	pIC50	=	9.9	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	446	7	2	6	4.6	CCCNc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(02)00663-7
	CHEMBL432012	174779	0	None	-	0	Human	9.9	pIC50	=	9.9	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	446	7	2	6	4.6	CCCNc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(02)00663-7
	10163744	105490	0	None	-	0	Human	9.9	pIC50	=	9.9	Binding	Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor	ChEMBL	495	7	2	7	5.2	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)C(C)C)c1	10.1021/jm000349x
	CHEMBL277706	105490	0	None	-	0	Human	9.9	pIC50	=	9.9	Binding	Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor	ChEMBL	495	7	2	7	5.2	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)C(C)C)c1	10.1021/jm000349x
	9916235	16125	1	None	-	0	Rat	9.9	pIC50	=	9.9	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	578	14	1	7	4.6	CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1	10.1021/jm970101g
	CHEMBL111277	16125	1	None	-	0	Rat	9.9	pIC50	=	9.9	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	578	14	1	7	4.6	CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1	10.1021/jm970101g
	11465535	207850	0	None	-	0	Human	9.9	pIC50	=	9.9	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	468	6	3	7	3.5	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(N)=O)c1	10.1021/jm030528p
	CHEMBL60276	207850	0	None	-	0	Human	9.9	pIC50	=	9.9	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	468	6	3	7	3.5	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(N)=O)c1	10.1021/jm030528p
	10277399	73640	0	None	-	0	Human	9.9	pIC50	=	9.9	Binding	Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor	ChEMBL	478	6	2	7	4.7	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1CC#N	10.1021/jm000349x
	CHEMBL18626	73640	0	None	-	0	Human	9.9	pIC50	=	9.9	Binding	Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor	ChEMBL	478	6	2	7	4.7	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1CC#N	10.1021/jm000349x
	10139080	79342	0	None	-	0	Human	9.9	pIC50	=	9.9	Binding	Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor	ChEMBL	454	6	2	7	4.6	Cc1cc(C)c(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1O	10.1021/jm000349x
	CHEMBL19921	79342	0	None	-	0	Human	9.9	pIC50	=	9.9	Binding	Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor	ChEMBL	454	6	2	7	4.6	Cc1cc(C)c(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1O	10.1021/jm000349x
	10717923	105469	0	None	-	0	Human	9.8	pIC50	=	9.8	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	439	5	2	6	4.7	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1	10.1021/jm030528p
	CHEMBL277595	105469	0	None	-	0	Human	9.8	pIC50	=	9.8	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	439	5	2	6	4.7	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1	10.1021/jm030528p
	9810351	64855	0	None	-	0	Pig	9.8	pIC50	=	9.8	Binding	In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.	ChEMBL	705	14	2	12	5.5	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(SCCO)nc1OCCOc1ncc(Br)cn1	10.1016/s0960-894x(01)00682-5
	CHEMBL167314	64855	0	None	-	0	Pig	9.8	pIC50	=	9.8	Binding	In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.	ChEMBL	705	14	2	12	5.5	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(SCCO)nc1OCCOc1ncc(Br)cn1	10.1016/s0960-894x(01)00682-5
	44284481	220504	0	None	-3	5	Pig	9.8	pIC50	=	9.8	Binding	Tested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptorTested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptor	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00077a013
	CHEMBL437472	220504	0	None	-3	5	Pig	9.8	pIC50	=	9.8	Binding	Tested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptorTested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptor	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00077a013
	9936145	25799	2	None	-	1	Human	9.8	pIC50	=	9.8	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	510	11	1	4	5.3	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(C)c(F)c1	10.1021/jm010237l
	CHEMBL128818	25799	2	None	-	1	Human	9.8	pIC50	=	9.8	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	510	11	1	4	5.3	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(C)c(F)c1	10.1021/jm010237l
	44284481	220504	0	None	-4	5	Human	9.8	pIC50	=	9.8	Binding	Displacement of radiolabeled endothelin-1 from human endothelin ETA receptorDisplacement of radiolabeled endothelin-1 from human endothelin ETA receptor	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm8007618
	CHEMBL437472	220504	0	None	-4	5	Human	9.8	pIC50	=	9.8	Binding	Displacement of radiolabeled endothelin-1 from human endothelin ETA receptorDisplacement of radiolabeled endothelin-1 from human endothelin ETA receptor	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm8007618
	11731472	16284	0	None	-	0	Pig	9.8	pIC50	=	9.8	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	571	10	1	10	5.6	CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc(C)s2)nc1	10.1021/jm0102304
	CHEMBL112141	16284	0	None	-	0	Pig	9.8	pIC50	=	9.8	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	571	10	1	10	5.6	CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc(C)s2)nc1	10.1021/jm0102304
	11050163	18516	0	None	-	0	Pig	9.8	pIC50	=	9.8	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	583	10	1	8	5.4	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm0102304
	CHEMBL1181553	18516	0	None	-	0	Pig	9.8	pIC50	=	9.8	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	583	10	1	8	5.4	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm0102304
	CHEMBL177924	18516	0	None	-	0	Pig	9.8	pIC50	=	9.8	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	583	10	1	8	5.4	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm0102304
	44351968	124858	0	None	-	0	Rat	9.8	pIC50	=	9.8	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	508	12	1	5	5.2	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CC)cc1	10.1021/jm010237l
	CHEMBL340575	124858	0	None	-	0	Rat	9.8	pIC50	=	9.8	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	508	12	1	5	5.2	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CC)cc1	10.1021/jm010237l
	10717923	105469	0	None	-	0	Human	9.8	pIC50	=	9.8	Binding	Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor	ChEMBL	439	5	2	6	4.7	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1	10.1021/jm000349x
	CHEMBL277595	105469	0	None	-	0	Human	9.8	pIC50	=	9.8	Binding	Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor	ChEMBL	439	5	2	6	4.7	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1	10.1021/jm000349x
	10623757	105707	0	None	-	0	Human	9.8	pIC50	=	9.8	Binding	Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor	ChEMBL	458	6	2	7	4.4	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2C)c(C)c1CC#N	10.1021/jm000349x
	CHEMBL279471	105707	0	None	-	0	Human	9.8	pIC50	=	9.8	Binding	Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor	ChEMBL	458	6	2	7	4.4	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2C)c(C)c1CC#N	10.1021/jm000349x
	9806559	15922	0	None	-	0	Human	9.8	pIC50	=	9.8	Binding	Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)	ChEMBL	515	13	1	6	3.3	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCN1CCCC1=O	10.1021/jm980217s
	CHEMBL110053	15922	0	None	-	0	Human	9.8	pIC50	=	9.8	Binding	Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)	ChEMBL	515	13	1	6	3.3	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCN1CCCC1=O	10.1021/jm980217s
	9936145	25799	2	None	-	1	Human	9.7	pIC50	=	9.7	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	510	11	1	4	5.3	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(C)c(F)c1	10.1021/jm010237l
	CHEMBL128818	25799	2	None	-	1	Human	9.7	pIC50	=	9.7	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	510	11	1	4	5.3	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(C)c(F)c1	10.1021/jm010237l
	CHEMBL1790959	215687	0	None	-	0	Pig	9.7	pIC50	=	9.7	Binding	Tested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptorTested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptor	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1021/jm00077a013
	9825494	209389	0	None	-	0	Rat	9.7	pIC50	=	9.7	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	460	6	1	6	5.2	COc1ccc(C2=C(C(=O)O)[C@@H](c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1	10.1021/jm031041j
	CHEMBL61211	209389	0	None	-	0	Rat	9.7	pIC50	=	9.7	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	460	6	1	6	5.2	COc1ccc(C2=C(C(=O)O)[C@@H](c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1	10.1021/jm031041j
	9825494	209389	0	None	-	0	Rat	9.7	pIC50	=	9.7	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	460	6	1	6	5.2	COc1ccc(C2=C(C(=O)O)[C@@H](c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1	10.1021/jm010382z
	CHEMBL61211	209389	0	None	-	0	Rat	9.7	pIC50	=	9.7	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	460	6	1	6	5.2	COc1ccc(C2=C(C(=O)O)[C@@H](c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1	10.1021/jm010382z
	9825494	209389	0	None	-	0	Rat	9.7	pIC50	=	9.7	Binding	Displacement of [125I]ET-1 from ET-A receptor in RASMC incubated for 60 minsDisplacement of [125I]ET-1 from ET-A receptor in RASMC incubated for 60 mins	ChEMBL	460	6	1	6	5.2	COc1ccc(C2=C(C(=O)O)[C@@H](c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1	10.1021/acs.jmedchem.5b01781
	CHEMBL61211	209389	0	None	-	0	Rat	9.7	pIC50	=	9.7	Binding	Displacement of [125I]ET-1 from ET-A receptor in RASMC incubated for 60 minsDisplacement of [125I]ET-1 from ET-A receptor in RASMC incubated for 60 mins	ChEMBL	460	6	1	6	5.2	COc1ccc(C2=C(C(=O)O)[C@@H](c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1	10.1021/acs.jmedchem.5b01781
	9868637	105864	1	None	-	0	Human	9.7	pIC50	=	9.7	Binding	Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor	ChEMBL	455	5	3	7	4.4	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1O	10.1021/jm000349x
	CHEMBL280659	105864	1	None	-	0	Human	9.7	pIC50	=	9.7	Binding	Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor	ChEMBL	455	5	3	7	4.4	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1O	10.1021/jm000349x
	CHEMBL1790963	215690	0	None	-	0	Pig	9.7	pIC50	=	9.7	Binding	Tested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptorTested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptor	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)[C@@H](C)O)[C@@H](C)CC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1021/jm00077a013
	11757759	181225	0	None	-	0	Human	9.7	pIC50	=	9.7	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	570	13	2	10	2.8	COCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Br)cc1	10.1016/j.bmcl.2016.06.014
	CHEMBL4553625	181225	0	None	-	0	Human	9.7	pIC50	=	9.7	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	570	13	2	10	2.8	COCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Br)cc1	10.1016/j.bmcl.2016.06.014
	18931096	65521	0	None	-	0	Pig	9.7	pIC50	=	9.7	Binding	In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.	ChEMBL	689	14	2	12	4.8	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(OCCO)nc1OCCOc1ncc(Br)cn1	10.1016/s0960-894x(01)00682-5
	CHEMBL168604	65521	0	None	-	0	Pig	9.7	pIC50	=	9.7	Binding	In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.	ChEMBL	689	14	2	12	4.8	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(OCCO)nc1OCCOc1ncc(Br)cn1	10.1016/s0960-894x(01)00682-5
	44284481	220504	0	None	-4	5	Human	9.7	pIC50	=	9.7	Binding	Inhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cellsInhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00095a029
	CHEMBL437472	220504	0	None	-4	5	Human	9.7	pIC50	=	9.7	Binding	Inhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cellsInhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00095a029
	10722371	109005	0	None	-	0	Human	9.7	pIC50	=	9.7	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	605	11	1	11	3.6	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCN3CCOCC3)c2)cc1	10.1021/jm980504w
	CHEMBL302974	109005	0	None	-	0	Human	9.7	pIC50	=	9.7	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	605	11	1	11	3.6	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCN3CCOCC3)c2)cc1	10.1021/jm980504w
	10578853	110369	0	None	-	0	Human	9.7	pIC50	=	9.7	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	564	10	1	11	3.4	COC(=O)COc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc(OC)c1OC	10.1021/jm980504w
	CHEMBL308646	110369	0	None	-	0	Human	9.7	pIC50	=	9.7	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	564	10	1	11	3.4	COC(=O)COc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc(OC)c1OC	10.1021/jm980504w
	44334128	11178	0	None	-	0	Human	9.7	pIC50	=	9.7	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	443	7	1	5	4.9	C=CCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(02)00663-7
	CHEMBL101424	11178	0	None	-	0	Human	9.7	pIC50	=	9.7	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	443	7	1	5	4.9	C=CCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(02)00663-7
	9939238	210907	0	None	-	1	Human	9.7	pIC50	=	9.7	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	637	12	2	13	3.6	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	CHEMBL70385	210907	0	None	-	1	Human	9.7	pIC50	=	9.7	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	637	12	2	13	3.6	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	44284481	220504	0	None	-4	5	Human	9.7	pIC50	=	9.7	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(97)00400-9
	CHEMBL437472	220504	0	None	-4	5	Human	9.7	pIC50	=	9.7	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(97)00400-9
	CHEMBL1790960	215688	0	None	-	0	Pig	9.7	pIC50	=	9.7	Binding	Tested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptorTested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptor	ChEMBL		None	None	None		CCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)[C@@H](C)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00077a013
	10120499	116533	0	None	-	0	Rat	9.7	pIC50	=	9.7	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	564	12	1	7	4.1	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CC(C)C	10.1021/jm970101g
	CHEMBL323055	116533	0	None	-	0	Rat	9.7	pIC50	=	9.7	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	564	12	1	7	4.1	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CC(C)C	10.1021/jm970101g
	11113541	210047	0	None	-	0	Rat	9.7	pIC50	=	9.7	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	476	7	1	7	5.2	COc1ccc(OC2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1	10.1021/jm010382z
	CHEMBL64632	210047	0	None	-	0	Rat	9.7	pIC50	=	9.7	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	476	7	1	7	5.2	COc1ccc(OC2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1	10.1021/jm010382z
	10299555	107810	0	None	-	0	Human	9.7	pIC50	=	9.7	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	481	6	2	7	4.9	CC(=O)c1cc(C)cc(C)c1NC(=O)c1sc(C)cc1S(=O)(=O)Nc1onc(C)c1Cl	10.1021/jm030528p
	CHEMBL294563	107810	0	None	-	0	Human	9.7	pIC50	=	9.7	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	481	6	2	7	4.9	CC(=O)c1cc(C)cc(C)c1NC(=O)c1sc(C)cc1S(=O)(=O)Nc1onc(C)c1Cl	10.1021/jm030528p
	10321290	11408	0	None	-	0	Human	9.7	pIC50	=	9.7	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	445	7	1	5	5.1	CCCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(02)00663-7
	CHEMBL102969	11408	0	None	-	0	Human	9.7	pIC50	=	9.7	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	445	7	1	5	5.1	CCCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(02)00663-7
	10651488	170158	0	None	-	0	Rat	9.7	pIC50	=	9.7	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	618	13	1	7	4.8	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCC(F)(F)F	10.1021/jm970101g
	CHEMBL419367	170158	0	None	-	0	Rat	9.7	pIC50	=	9.7	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	618	13	1	7	4.8	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCC(F)(F)F	10.1021/jm970101g
	44284381	135287	0	None	-	0	Human	9.7	pIC50	=	9.7	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	462	6	3	7	4.3	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(O)c1	10.1016/j.bmcl.2004.01.008
	CHEMBL36671	135287	0	None	-	0	Human	9.7	pIC50	=	9.7	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	462	6	3	7	4.3	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(O)c1	10.1016/j.bmcl.2004.01.008
	10648937	214085	0	None	-	0	Rat	9.7	pIC50	=	9.7	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	496	11	1	6	4.3	CCCCN(CCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL9334	214085	0	None	-	0	Rat	9.7	pIC50	=	9.7	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	496	11	1	6	4.3	CCCCN(CCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	44284481	220504	0	None	-4	5	Human	9.6	pIC50	=	9.6	Binding	Displacement of [125I]Endothelin-1 from human recombinant ETA receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Endothelin-1 from human recombinant ETA receptor expressed in CHOK1 cells after 2 hrs	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/j.bmcl.2013.01.025
	CHEMBL437472	220504	0	None	-4	5	Human	9.6	pIC50	=	9.6	Binding	Displacement of [125I]Endothelin-1 from human recombinant ETA receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Endothelin-1 from human recombinant ETA receptor expressed in CHOK1 cells after 2 hrs	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/j.bmcl.2013.01.025
	123883	21416	1	None	-	0	Human	9.6	pIC50	=	9.6	Binding	Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor	ChEMBL	927	12	9	11	0.8	CC(C)C[C@@H]1NC(=O)[C@@H](c2cccs2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)N2CCN(c3ccccc3)CC2)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm970101g
	CHEMBL1205177	21416	1	None	-	0	Human	9.6	pIC50	=	9.6	Binding	Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor	ChEMBL	927	12	9	11	0.8	CC(C)C[C@@H]1NC(=O)[C@@H](c2cccs2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)N2CCN(c3ccccc3)CC2)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm970101g
	CHEMBL61425	21416	1	None	-	0	Human	9.6	pIC50	=	9.6	Binding	Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor	ChEMBL	927	12	9	11	0.8	CC(C)C[C@@H]1NC(=O)[C@@H](c2cccs2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)N2CCN(c3ccccc3)CC2)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm970101g
	123883	21416	1	None	-	0	Human	9.6	pIC50	=	9.6	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	927	12	9	11	0.8	CC(C)C[C@@H]1NC(=O)[C@@H](c2cccs2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)N2CCN(c3ccccc3)CC2)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm030528p
	CHEMBL1205177	21416	1	None	-	0	Human	9.6	pIC50	=	9.6	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	927	12	9	11	0.8	CC(C)C[C@@H]1NC(=O)[C@@H](c2cccs2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)N2CCN(c3ccccc3)CC2)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm030528p
	CHEMBL61425	21416	1	None	-	0	Human	9.6	pIC50	=	9.6	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	927	12	9	11	0.8	CC(C)C[C@@H]1NC(=O)[C@@H](c2cccs2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)N2CCN(c3ccccc3)CC2)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm030528p
	11006532	19015	0	None	-	0	Rat	9.6	pIC50	=	9.6	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	601	10	1	9	6.5	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(-c3cccs3)cn2)cc1	10.1021/jm0102304
	CHEMBL1184515	19015	0	None	-	0	Rat	9.6	pIC50	=	9.6	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	601	10	1	9	6.5	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(-c3cccs3)cn2)cc1	10.1021/jm0102304
	CHEMBL367445	19015	0	None	-	0	Rat	9.6	pIC50	=	9.6	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	601	10	1	9	6.5	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(-c3cccs3)cn2)cc1	10.1021/jm0102304
	9894460	213488	9	None	24	3	Human	9.6	pIC50	=	9.6	Binding	Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor	ChEMBL	539	10	2	7	4.8	CCCc1cc(C(=O)O)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2	10.1021/jm970101g
	CHEMBL313871	213488	9	None	24	3	Human	9.6	pIC50	=	9.6	Binding	Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor	ChEMBL	539	10	2	7	4.8	CCCc1cc(C(=O)O)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2	10.1021/jm970101g
	CHEMBL8978	213488	9	None	24	3	Human	9.6	pIC50	=	9.6	Binding	Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor	ChEMBL	539	10	2	7	4.8	CCCc1cc(C(=O)O)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2	10.1021/jm970101g
	22004774	107586	0	None	-	0	Rat	9.6	pIC50	=	9.6	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	442	8	1	6	5.7	CCCCSC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	CHEMBL293192	107586	0	None	-	0	Rat	9.6	pIC50	=	9.6	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	442	8	1	6	5.7	CCCCSC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	CHEMBL2304284	216267	0	None	-	0	Human	9.5	pIC50	=	9.5	Binding	Inhibition of ETA receptor in human SK-N-MC cells after 60 mins by scintillation countingInhibition of ETA receptor in human SK-N-MC cells after 60 mins by scintillation counting	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/np900287e
	44387242	127181	0	None	-	0	Rat	9.5	pIC50	=	9.5	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	502	15	1	5	5.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCCCC(C)C	10.1021/jm031041j
	CHEMBL353560	127181	0	None	-	0	Rat	9.5	pIC50	=	9.5	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	502	15	1	5	5.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCCCC(C)C	10.1021/jm031041j
	11093237	17179	0	None	-	0	Pig	9.5	pIC50	=	9.5	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	601	10	1	9	6.4	CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc3ccccc3c2)nc1	10.1021/jm0102304
	CHEMBL116281	17179	0	None	-	0	Pig	9.5	pIC50	=	9.5	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	601	10	1	9	6.4	CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc3ccccc3c2)nc1	10.1021/jm0102304
	10769526	109477	0	None	-	0	Human	9.5	pIC50	=	9.5	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	578	12	2	10	4.1	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCC(=O)O)c2)cc1	10.1021/jm980504w
	CHEMBL304762	109477	0	None	-	0	Human	9.5	pIC50	=	9.5	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	578	12	2	10	4.1	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCC(=O)O)c2)cc1	10.1021/jm980504w
	9870959	15689	0	None	-	0	Human	9.5	pIC50	=	9.5	Binding	Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)	ChEMBL	509	13	1	6	4.3	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1ccccn1	10.1021/jm980217s
	CHEMBL109778	15689	0	None	-	0	Human	9.5	pIC50	=	9.5	Binding	Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)	ChEMBL	509	13	1	6	4.3	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1ccccn1	10.1021/jm980217s
	44339655	15878	0	None	-	0	Human	9.5	pIC50	=	9.5	Binding	Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)	ChEMBL	530	14	1	6	5.3	C/C=C\C(C)(C)C[C@H]1[C@H](C(=O)O)[C@@H](c2cc(OC)c3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC	10.1021/jm980217s
	CHEMBL109926	15878	0	None	-	0	Human	9.5	pIC50	=	9.5	Binding	Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)	ChEMBL	530	14	1	6	5.3	C/C=C\C(C)(C)C[C@H]1[C@H](C(=O)O)[C@@H](c2cc(OC)c3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC	10.1021/jm980217s
	10278777	174911	0	None	-	0	Human	9.5	pIC50	=	9.5	Binding	Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)	ChEMBL	502	14	1	5	5.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC	10.1021/jm980217s
	CHEMBL432974	174911	0	None	-	0	Human	9.5	pIC50	=	9.5	Binding	Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)	ChEMBL	502	14	1	5	5.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC	10.1021/jm980217s
	9870830	213493	38	None	66	2	Human	9.5	pIC50	=	9.5	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	506	8	1	9	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1	10.1021/jm9606507
	CHEMBL8981	213493	38	None	66	2	Human	9.5	pIC50	=	9.5	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	506	8	1	9	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1	10.1021/jm9606507
	9939238	210907	0	None	-	1	Human	9.5	pIC50	=	9.5	Binding	Displacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cellsDisplacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cells	ChEMBL	637	12	2	13	3.6	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1	10.1016/j.bmcl.2016.06.014
	CHEMBL70385	210907	0	None	-	1	Human	9.5	pIC50	=	9.5	Binding	Displacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cellsDisplacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cells	ChEMBL	637	12	2	13	3.6	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1	10.1016/j.bmcl.2016.06.014
	21041284	177716	0	None	-	0	Human	9.5	pIC50	=	9.5	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	568	13	2	9	3.9	CCCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Br)cc1	10.1016/j.bmcl.2016.06.014
	CHEMBL4455360	177716	0	None	-	0	Human	9.5	pIC50	=	9.5	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	568	13	2	9	3.9	CCCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Br)cc1	10.1016/j.bmcl.2016.06.014
	58688006	177895	0	None	-	0	Human	9.5	pIC50	=	9.5	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	524	13	2	9	3.8	CCCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Cl)cc1	10.1016/j.bmcl.2016.06.014
	CHEMBL4458005	177895	0	None	-	0	Human	9.5	pIC50	=	9.5	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	524	13	2	9	3.8	CCCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Cl)cc1	10.1016/j.bmcl.2016.06.014
	9870830	213493	38	None	-	2	Mouse	9.5	pIC50	=	9.5	Binding	Displacement of [125I]ET1 from endothelin A receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin A receptor in DBA mouse microsomes	ChEMBL	506	8	1	9	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1	10.1016/j.bmc.2009.08.058
	CHEMBL8981	213493	38	None	-	2	Mouse	9.5	pIC50	=	9.5	Binding	Displacement of [125I]ET1 from endothelin A receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin A receptor in DBA mouse microsomes	ChEMBL	506	8	1	9	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1	10.1016/j.bmc.2009.08.058
	21041264	88786	1	None	-	0	Human	9.5	pIC50	=	9.5	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	600	12	2	8	4.0	CCCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1	10.1021/jm3009103
	CHEMBL2165339	88786	1	None	-	0	Human	9.5	pIC50	=	9.5	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	600	12	2	8	4.0	CCCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1	10.1021/jm3009103
	10311570	21402	0	None	-	1	Rat	9.5	pIC50	=	9.5	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	520	10	1	9	4.7	COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1	10.1016/s0960-894x(98)00301-1
	CHEMBL1205068	21402	0	None	-	1	Rat	9.5	pIC50	=	9.5	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	520	10	1	9	4.7	COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1	10.1016/s0960-894x(98)00301-1
	CHEMBL48907	21402	0	None	-	1	Rat	9.5	pIC50	=	9.5	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	520	10	1	9	4.7	COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1	10.1016/s0960-894x(98)00301-1
	10555424	210815	0	None	-	0	Human	9.5	pIC50	=	9.5	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	592	13	2	10	4.5	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCCC(=O)O)c2)cc1	10.1021/jm980504w
	CHEMBL69832	210815	0	None	-	0	Human	9.5	pIC50	=	9.5	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	592	13	2	10	4.5	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCCC(=O)O)c2)cc1	10.1021/jm980504w
	9870830	213493	38	None	66	2	Human	9.5	pIC50	=	9.5	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	506	8	1	9	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1	10.1021/jm980504w
	CHEMBL8981	213493	38	None	66	2	Human	9.5	pIC50	=	9.5	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	506	8	1	9	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1	10.1021/jm980504w
	9871348	210806	0	None	-	0	Rat	9.5	pIC50	=	9.5	Binding	Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor	ChEMBL	520	8	1	10	4.1	COc1ccc(C2(O)OC(=O)C(c3ccc4nsnc4c3)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1	10.1016/s0960-894x(97)10151-2
	CHEMBL69741	210806	0	None	-	0	Rat	9.5	pIC50	=	9.5	Binding	Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor	ChEMBL	520	8	1	10	4.1	COc1ccc(C2(O)OC(=O)C(c3ccc4nsnc4c3)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1	10.1016/s0960-894x(97)10151-2
	9809919	211188	0	None	-	2	Human	9.5	pIC50	=	9.5	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	665	13	2	13	4.5	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	CHEMBL72037	211188	0	None	-	2	Human	9.5	pIC50	=	9.5	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	665	13	2	13	4.5	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	44284481	220504	0	None	-4	5	Human	9.5	pIC50	=	9.5	Binding	Receptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cellsReceptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(97)00400-9
	CHEMBL437472	220504	0	None	-4	5	Human	9.5	pIC50	=	9.5	Binding	Receptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cellsReceptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(97)00400-9
	159594	7310	45	None	-1	3	Rat	9.5	pIC50	=	9.5	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm031041j
	3487	7310	45	None	-1	3	Rat	9.5	pIC50	=	9.5	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm031041j
	CHEMBL9194	7310	45	None	-1	3	Rat	9.5	pIC50	=	9.5	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm031041j
	DB06199	7310	45	None	-1	3	Rat	9.5	pIC50	=	9.5	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm031041j
	159594	7310	45	None	1	3	Human	9.5	pIC50	=	9.5	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm030528p
	3487	7310	45	None	1	3	Human	9.5	pIC50	=	9.5	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm030528p
	CHEMBL9194	7310	45	None	1	3	Human	9.5	pIC50	=	9.5	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm030528p
	DB06199	7310	45	None	1	3	Human	9.5	pIC50	=	9.5	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm030528p
	159594	7310	45	None	-1	3	Rat	9.5	pIC50	=	9.5	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm9505369
	3487	7310	45	None	-1	3	Rat	9.5	pIC50	=	9.5	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm9505369
	CHEMBL9194	7310	45	None	-1	3	Rat	9.5	pIC50	=	9.5	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm9505369
	DB06199	7310	45	None	-1	3	Rat	9.5	pIC50	=	9.5	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm9505369
	11144344	209791	0	None	-	0	Rat	9.5	pIC50	=	9.5	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	424	8	1	5	5.8	CCCCCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	CHEMBL63267	209791	0	None	-	0	Rat	9.5	pIC50	=	9.5	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	424	8	1	5	5.8	CCCCCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	44334150	11306	0	None	-	0	Human	9.5	pIC50	=	9.5	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	445	6	1	5	5.0	COc1ccc([C@@H]2c3nc(CC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1	10.1016/s0960-894x(02)00663-7
	CHEMBL102314	11306	0	None	-	0	Human	9.5	pIC50	=	9.5	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	445	6	1	5	5.0	COc1ccc([C@@H]2c3nc(CC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1	10.1016/s0960-894x(02)00663-7
	9852318	16386	8	None	-	2	Rat	9.5	pIC50	=	9.5	Binding	Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane	ChEMBL	613	11	2	9	4.5	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm000538f
	CHEMBL112624	16386	8	None	-	2	Rat	9.5	pIC50	=	9.5	Binding	Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane	ChEMBL	613	11	2	9	4.5	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm000538f
	CHEMBL1627022	16386	8	None	-	2	Rat	9.5	pIC50	=	9.5	Binding	Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane	ChEMBL	613	11	2	9	4.5	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm000538f
	11102201	210002	0	None	-	0	Rat	9.5	pIC50	=	9.5	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	438	9	1	6	5.1	C=CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	CHEMBL64447	210002	0	None	-	0	Rat	9.5	pIC50	=	9.5	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	438	9	1	6	5.1	C=CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	44266903	21358	0	None	-	0	Human	9.5	pIC50	=	9.5	Binding	Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells	ChEMBL	536	11	1	9	4.4	COc1ccc(C(=O)/C(Cc2ccc(OC)c(OC)c2OC)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1	10.1021/jm9606507
	CHEMBL10862	21358	0	None	-	0	Human	9.5	pIC50	=	9.5	Binding	Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells	ChEMBL	536	11	1	9	4.4	COc1ccc(C(=O)/C(Cc2ccc(OC)c(OC)c2OC)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1	10.1021/jm9606507
	CHEMBL1204672	21358	0	None	-	0	Human	9.5	pIC50	=	9.5	Binding	Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells	ChEMBL	536	11	1	9	4.4	COc1ccc(C(=O)/C(Cc2ccc(OC)c(OC)c2OC)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1	10.1021/jm9606507
	9960931	114798	0	None	-	0	Human	9.5	pIC50	=	9.5	Binding	Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells	ChEMBL	635	12	1	12	4.1	CCOC(=O)CNC(=O)OC1(c2ccc(OC)cc2)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1cc(OC)c(OC)c(OC)c1	10.1016/S0960-894X(97)00002-4
	CHEMBL319452	114798	0	None	-	0	Human	9.5	pIC50	=	9.5	Binding	Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells	ChEMBL	635	12	1	12	4.1	CCOC(=O)CNC(=O)OC1(c2ccc(OC)cc2)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1cc(OC)c(OC)c(OC)c1	10.1016/S0960-894X(97)00002-4
	159594	7310	45	None	-1	3	Rat	9.4	pIC50	=	9.4	Binding	Binding affinity against Endothelin A receptor in MMQ cells in ratBinding affinity against Endothelin A receptor in MMQ cells in rat	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm010237l
	3487	7310	45	None	-1	3	Rat	9.4	pIC50	=	9.4	Binding	Binding affinity against Endothelin A receptor in MMQ cells in ratBinding affinity against Endothelin A receptor in MMQ cells in rat	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm010237l
	CHEMBL9194	7310	45	None	-1	3	Rat	9.4	pIC50	=	9.4	Binding	Binding affinity against Endothelin A receptor in MMQ cells in ratBinding affinity against Endothelin A receptor in MMQ cells in rat	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm010237l
	DB06199	7310	45	None	-1	3	Rat	9.4	pIC50	=	9.4	Binding	Binding affinity against Endothelin A receptor in MMQ cells in ratBinding affinity against Endothelin A receptor in MMQ cells in rat	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm010237l
	9914310	213422	8	None	-	2	Rat	9.4	pIC50	=	9.4	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	510	12	1	6	4.7	CCCCN(CCCC)C(=O)CN1CC(c2ccc3c(c2)OCO3)C(C(=O)O)C1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL8923	213422	8	None	-	2	Rat	9.4	pIC50	=	9.4	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	510	12	1	6	4.7	CCCCN(CCCC)C(=O)CN1CC(c2ccc3c(c2)OCO3)C(C(=O)O)C1c1ccc(OC)cc1	10.1021/jm9505369
	9870830	213493	38	None	66	2	Human	9.4	pIC50	=	9.4	Binding	Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells	ChEMBL	506	8	1	9	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1	10.1016/S0960-894X(97)00002-4
	CHEMBL8981	213493	38	None	66	2	Human	9.4	pIC50	=	9.4	Binding	Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells	ChEMBL	506	8	1	9	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1	10.1016/S0960-894X(97)00002-4
	11017436	16722	0	None	-	0	Pig	9.4	pIC50	=	9.4	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	597	12	1	11	5.3	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)ncnc1OCCOc1ncc(SC)cn1	10.1021/jm0102304
	CHEMBL114660	16722	0	None	-	0	Pig	9.4	pIC50	=	9.4	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	597	12	1	11	5.3	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)ncnc1OCCOc1ncc(SC)cn1	10.1021/jm0102304
	44333913	11873	0	None	-	0	Human	9.4	pIC50	=	9.4	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	431	6	1	5	4.8	CCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(02)00663-7
	CHEMBL105591	11873	0	None	-	0	Human	9.4	pIC50	=	9.4	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	431	6	1	5	4.8	CCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(02)00663-7
	9870959	15689	0	None	-	0	Rat	9.4	pIC50	=	9.4	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	509	13	1	6	4.3	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1ccccn1	10.1021/jm980217s
	CHEMBL109778	15689	0	None	-	0	Rat	9.4	pIC50	=	9.4	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	509	13	1	6	4.3	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1ccccn1	10.1021/jm980217s
	9809526	21631	0	None	-	0	Human	9.4	pIC50	=	9.4	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	614	12	2	11	3.5	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCS(=O)(=O)O)c2)cc1	10.1021/jm980504w
	CHEMBL1207463	21631	0	None	-	0	Human	9.4	pIC50	=	9.4	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	614	12	2	11	3.5	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCS(=O)(=O)O)c2)cc1	10.1021/jm980504w
	CHEMBL408055	21631	0	None	-	0	Human	9.4	pIC50	=	9.4	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	614	12	2	11	3.5	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCS(=O)(=O)O)c2)cc1	10.1021/jm980504w
	44284481	220504	0	None	-4	5	Human	9.4	pIC50	=	9.4	Binding	Inhibition of human ETA receptorInhibition of human ETA receptor	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm701575k
	CHEMBL437472	220504	0	None	-4	5	Human	9.4	pIC50	=	9.4	Binding	Inhibition of human ETA receptorInhibition of human ETA receptor	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm701575k
	10208674	108630	0	None	-	0	Human	9.4	pIC50	=	9.4	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	529	7	2	7	5.6	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)c2ccccc2)c1	10.1021/jm030528p
	CHEMBL300547	108630	0	None	-	0	Human	9.4	pIC50	=	9.4	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	529	7	2	7	5.6	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)c2ccccc2)c1	10.1021/jm030528p
	10603409	117381	0	None	-	0	Rat	9.4	pIC50	=	9.4	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	584	13	1	7	4.1	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCCl	10.1021/jm970101g
	CHEMBL325581	117381	0	None	-	0	Rat	9.4	pIC50	=	9.4	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	584	13	1	7	4.1	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCCl	10.1021/jm970101g
	9852318	16386	8	None	2691	2	Human	9.4	pIC50	=	9.4	Binding	Antagonist activity at ET-A receptor (unknown origin)Antagonist activity at ET-A receptor (unknown origin)	ChEMBL	613	11	2	9	4.5	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/acs.jmedchem.5b01781
	CHEMBL112624	16386	8	None	2691	2	Human	9.4	pIC50	=	9.4	Binding	Antagonist activity at ET-A receptor (unknown origin)Antagonist activity at ET-A receptor (unknown origin)	ChEMBL	613	11	2	9	4.5	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/acs.jmedchem.5b01781
	CHEMBL1627022	16386	8	None	2691	2	Human	9.4	pIC50	=	9.4	Binding	Antagonist activity at ET-A receptor (unknown origin)Antagonist activity at ET-A receptor (unknown origin)	ChEMBL	613	11	2	9	4.5	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/acs.jmedchem.5b01781
	44332735	179481	0	None	-	0	Human	9.4	pIC50	=	9.4	Binding	Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells	ChEMBL	649	13	1	12	4.5	CCOC(=O)CCNC(=O)OC1(c2ccc(OC)cc2)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1cc(OC)c(OC)c(OC)c1	10.1016/S0960-894X(97)00002-4
	CHEMBL450337	179481	0	None	-	0	Human	9.4	pIC50	=	9.4	Binding	Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells	ChEMBL	649	13	1	12	4.5	CCOC(=O)CCNC(=O)OC1(c2ccc(OC)cc2)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1cc(OC)c(OC)c(OC)c1	10.1016/S0960-894X(97)00002-4
	159594	7310	45	None	-1	3	Rat	9.4	pIC50	=	9.4	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm960077r
	3487	7310	45	None	-1	3	Rat	9.4	pIC50	=	9.4	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm960077r
	CHEMBL9194	7310	45	None	-1	3	Rat	9.4	pIC50	=	9.4	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm960077r
	DB06199	7310	45	None	-1	3	Rat	9.4	pIC50	=	9.4	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm960077r
	9852318	16386	8	None	2691	2	Human	9.4	pIC50	=	9.4	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	613	11	2	9	4.5	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm3009103
	CHEMBL112624	16386	8	None	2691	2	Human	9.4	pIC50	=	9.4	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	613	11	2	9	4.5	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm3009103
	CHEMBL1627022	16386	8	None	2691	2	Human	9.4	pIC50	=	9.4	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	613	11	2	9	4.5	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm3009103
	71462245	88441	0	None	-	0	Human	9.4	pIC50	=	9.4	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	588	13	2	10	3.6	CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1Oc1cc(OC)ccc1Cl	10.1021/jm3009103
	CHEMBL2163692	88441	0	None	-	0	Human	9.4	pIC50	=	9.4	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	588	13	2	10	3.6	CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1Oc1cc(OC)ccc1Cl	10.1021/jm3009103
	44386169	138167	0	None	-	1	Human	9.4	pIC50	=	9.4	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	690	12	2	14	3.9	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1cnccn1	10.1016/s0960-894x(02)01084-3
	CHEMBL368996	138167	0	None	-	1	Human	9.4	pIC50	=	9.4	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	690	12	2	14	3.9	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1cnccn1	10.1016/s0960-894x(02)01084-3
	11122784	169701	0	None	-	0	Rat	9.4	pIC50	=	9.4	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	426	8	1	6	4.9	CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	CHEMBL417413	169701	0	None	-	0	Rat	9.4	pIC50	=	9.4	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	426	8	1	6	4.9	CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	44339655	15878	0	None	-	0	Rat	9.4	pIC50	=	9.4	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	530	14	1	6	5.3	C/C=C\C(C)(C)C[C@H]1[C@H](C(=O)O)[C@@H](c2cc(OC)c3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC	10.1021/jm980217s
	CHEMBL109926	15878	0	None	-	0	Rat	9.4	pIC50	=	9.4	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	530	14	1	6	5.3	C/C=C\C(C)(C)C[C@H]1[C@H](C(=O)O)[C@@H](c2cc(OC)c3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC	10.1021/jm980217s
	44284196	107299	0	None	-	0	Human	9.4	pIC50	=	9.4	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	504	9	2	7	5.4	CCCOc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O	10.1016/j.bmcl.2004.01.008
	CHEMBL291247	107299	0	None	-	0	Human	9.4	pIC50	=	9.4	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	504	9	2	7	5.4	CCCOc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O	10.1016/j.bmcl.2004.01.008
	10364227	209578	0	None	-	0	Rat	9.4	pIC50	=	9.4	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	410	7	1	5	5.4	CCCCC1=C(C(=O)O)[C@@H](c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm031041j
	CHEMBL62264	209578	0	None	-	0	Rat	9.4	pIC50	=	9.4	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	410	7	1	5	5.4	CCCCC1=C(C(=O)O)[C@@H](c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm031041j
	10364227	209578	0	None	-	0	Rat	9.4	pIC50	=	9.4	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	410	7	1	5	5.4	CCCCC1=C(C(=O)O)[C@@H](c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	CHEMBL62264	209578	0	None	-	0	Rat	9.4	pIC50	=	9.4	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	410	7	1	5	5.4	CCCCC1=C(C(=O)O)[C@@H](c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	9806559	15922	0	None	-	0	Rat	9.4	pIC50	=	9.4	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	515	13	1	6	3.3	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCN1CCCC1=O	10.1021/jm980217s
	CHEMBL110053	15922	0	None	-	0	Rat	9.4	pIC50	=	9.4	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	515	13	1	6	3.3	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCN1CCCC1=O	10.1021/jm980217s
	11827880	16998	0	None	-	0	Rat	9.4	pIC50	=	9.4	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	565	10	1	9	5.5	CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc(C)cc2)nc1	10.1021/jm0102304
	CHEMBL116046	16998	0	None	-	0	Rat	9.4	pIC50	=	9.4	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	565	10	1	9	5.5	CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc(C)cc2)nc1	10.1021/jm0102304
	CHEMBL177979	16998	0	None	-	0	Rat	9.4	pIC50	=	9.4	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	565	10	1	9	5.5	CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc(C)cc2)nc1	10.1021/jm0102304
	CHEMBL1790962	215689	0	None	-	1	Pig	9.4	pIC50	=	9.4	Binding	Tested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptorTested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptor	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)[C@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1021/jm00077a013
	10303555	170160	0	None	-	0	Rat	9.4	pIC50	=	9.4	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	574	15	1	7	4.9	CCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm970101g
	CHEMBL419383	170160	0	None	-	0	Rat	9.4	pIC50	=	9.4	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	574	15	1	7	4.9	CCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm970101g
	10578320	104085	0	None	-	0	Rat	9.4	pIC50	=	9.4	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	538	12	1	6	5.2	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(CCC(C)C)CCC(C)C)cc1	10.1021/jm9505369
	CHEMBL269141	104085	0	None	-	0	Rat	9.4	pIC50	=	9.4	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	538	12	1	6	5.2	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(CCC(C)C)CCC(C)C)cc1	10.1021/jm9505369
	10182624	106329	0	None	-	0	Human	9.4	pIC50	=	9.4	Binding	Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor	ChEMBL	453	6	2	6	4.9	CCc1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl	10.1021/jm000349x
	CHEMBL283582	106329	0	None	-	0	Human	9.4	pIC50	=	9.4	Binding	Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor	ChEMBL	453	6	2	6	4.9	CCc1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl	10.1021/jm000349x
	9870830	213493	38	None	-	2	Rat	9.4	pIC50	=	9.4	Binding	Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor	ChEMBL	506	8	1	9	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1	10.1016/s0960-894x(97)10151-2
	CHEMBL8981	213493	38	None	-	2	Rat	9.4	pIC50	=	9.4	Binding	Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor	ChEMBL	506	8	1	9	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1	10.1016/s0960-894x(97)10151-2
	9825494	209389	0	None	-	0	Human	9.4	pIC50	=	9.4	Binding	Binding affinity at human Endothelin A receptorBinding affinity at human Endothelin A receptor	ChEMBL	460	6	1	6	5.2	COc1ccc(C2=C(C(=O)O)[C@@H](c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1	10.1021/jm010382z
	CHEMBL61211	209389	0	None	-	0	Human	9.4	pIC50	=	9.4	Binding	Binding affinity at human Endothelin A receptorBinding affinity at human Endothelin A receptor	ChEMBL	460	6	1	6	5.2	COc1ccc(C2=C(C(=O)O)[C@@H](c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1	10.1021/jm010382z
	44380648	127291	0	None	-	0	Pig	9.4	pIC50	=	9.4	Binding	In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.	ChEMBL	727	12	1	12	5.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(N2CCN(C)CC2)nc1OCCOc1ncc(Br)cn1	10.1016/s0960-894x(01)00682-5
	CHEMBL354528	127291	0	None	-	0	Pig	9.4	pIC50	=	9.4	Binding	In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.	ChEMBL	727	12	1	12	5.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(N2CCN(C)CC2)nc1OCCOc1ncc(Br)cn1	10.1016/s0960-894x(01)00682-5
	10210629	15536	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	592	15	1	7	5.0	CCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1	10.1021/jm970101g
	CHEMBL109644	15536	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	592	15	1	7	5.0	CCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1	10.1021/jm970101g
	10167052	116416	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	578	13	1	7	4.5	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCC(C)C	10.1021/jm970101g
	CHEMBL322297	116416	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	578	13	1	7	4.5	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCC(C)C	10.1021/jm970101g
	44265870	214350	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	524	12	1	6	5.1	CCCCN(CCCC)C(=O)C(C)N1CC(c2ccc3c(c2)OCO3)C(C(=O)O)C1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL9488	214350	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	524	12	1	6	5.1	CCCCN(CCCC)C(=O)C(C)N1CC(c2ccc3c(c2)OCO3)C(C(=O)O)C1c1ccc(OC)cc1	10.1021/jm9505369
	10391487	16433	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	506	12	1	5	5.7	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3occc3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm010237l
	CHEMBL112832	16433	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	506	12	1	5	5.7	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3occc3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm010237l
	10983045	209685	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	440	9	1	6	5.3	CCCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	CHEMBL62762	209685	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	440	9	1	6	5.3	CCCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	11050177	17031	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	585	10	1	9	6.1	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(-c3ccco3)cn2)cc1	10.1021/jm0102304
	CHEMBL116108	17031	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	585	10	1	9	6.1	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(-c3ccco3)cn2)cc1	10.1021/jm0102304
	CHEMBL175501	17031	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	585	10	1	9	6.1	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(-c3ccco3)cn2)cc1	10.1021/jm0102304
	9915028	16183	18	None	28183	2	Human	9.3	pIC50	=	9.3	Binding	Inhibitory activity against human endothelin A receptorInhibitory activity against human endothelin A receptor	ChEMBL	532	15	1	6	5.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC	10.1021/jm010237l
	CHEMBL111612	16183	18	None	28183	2	Human	9.3	pIC50	=	9.3	Binding	Inhibitory activity against human endothelin A receptorInhibitory activity against human endothelin A receptor	ChEMBL	532	15	1	6	5.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC	10.1021/jm010237l
	CHEMBL4761843	16183	18	None	28183	2	Human	9.3	pIC50	=	9.3	Binding	Inhibitory activity against human endothelin A receptorInhibitory activity against human endothelin A receptor	ChEMBL	532	15	1	6	5.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC	10.1021/jm010237l
	10391487	16433	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	506	12	1	5	5.7	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3occc3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm031041j
	CHEMBL112832	16433	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	506	12	1	5	5.7	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3occc3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm031041j
	10840068	67131	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	536	11	1	9	4.4	COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1	10.1021/jm031041j
	CHEMBL174573	67131	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	536	11	1	9	4.4	COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1	10.1021/jm031041j
	44387124	137669	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	524	13	1	6	5.1	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](CC(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm031041j
	CHEMBL368558	137669	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	524	13	1	6	5.1	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](CC(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm031041j
	10530409	12478	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	536	9	1	10	3.9	COc1ccc(C2(O)OC(=O)C(c3cc(OC)c4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1	10.1021/jm9606507
	CHEMBL10781	12478	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	536	9	1	10	3.9	COc1ccc(C2(O)OC(=O)C(c3cc(OC)c4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1	10.1021/jm9606507
	10815823	16569	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	520	8	1	9	4.2	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1C	10.1021/jm9606507
	CHEMBL11369	16569	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	520	8	1	9	4.2	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1C	10.1021/jm9606507
	15411009	113967	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells	ChEMBL	691	14	1	12	5.6	CCOC(=O)C(CC(C)C)NC(=O)OC1(c2ccc(OC)cc2)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1cc(OC)c(OC)c(OC)c1	10.1016/S0960-894X(97)00002-4
	CHEMBL316523	113967	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells	ChEMBL	691	14	1	12	5.6	CCOC(=O)C(CC(C)C)NC(=O)OC1(c2ccc(OC)cc2)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1cc(OC)c(OC)c(OC)c1	10.1016/S0960-894X(97)00002-4
	10391487	16433	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	506	12	1	5	5.7	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3occc3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	CHEMBL112832	16433	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	506	12	1	5	5.7	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3occc3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	16004692	9232	91	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	586	11	2	8	3.6	CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br	10.1016/j.bmcl.2016.06.014
	4809	9232	91	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	586	11	2	8	3.6	CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br	10.1016/j.bmcl.2016.06.014
	7352	9232	91	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	586	11	2	8	3.6	CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br	10.1016/j.bmcl.2016.06.014
	CHEMBL2103873	9232	91	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	586	11	2	8	3.6	CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br	10.1016/j.bmcl.2016.06.014
	DB08932	9232	91	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	586	11	2	8	3.6	CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br	10.1016/j.bmcl.2016.06.014
	157574	85165	11	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	517	4	1	5	5.0	CCc1cc(C2=C(C(=O)O)N(c3ccccc3C(F)(F)F)S(=O)(=O)c3ccccc32)cc2c1OCO2	10.1016/j.bmcl.2016.06.014
	CHEMBL2110610	85165	11	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	517	4	1	5	5.0	CCc1cc(C2=C(C(=O)O)N(c3ccccc3C(F)(F)F)S(=O)(=O)c3ccccc32)cc2c1OCO2	10.1016/j.bmcl.2016.06.014
	21041283	179926	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	552	13	2	9	3.2	CCCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(OC)cn2)c1-c1ccc(Br)cc1	10.1016/j.bmcl.2016.06.014
	CHEMBL4521348	179926	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	552	13	2	9	3.2	CCCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(OC)cn2)c1-c1ccc(Br)cc1	10.1016/j.bmcl.2016.06.014
	155544917	180193	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	540	13	2	10	3.4	CCCNS(=O)(=O)Nc1ncnc(OCCOc2cc(OC)ccc2Cl)c1-c1ncc(SC)cn1	10.1016/j.bmcl.2016.06.014
	CHEMBL4528516	180193	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	540	13	2	10	3.4	CCCNS(=O)(=O)Nc1ncnc(OCCOc2cc(OC)ccc2Cl)c1-c1ncc(SC)cn1	10.1016/j.bmcl.2016.06.014
	16004692	9232	91	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	586	11	2	8	3.6	CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br	10.1021/jm3009103
	4809	9232	91	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	586	11	2	8	3.6	CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br	10.1021/jm3009103
	7352	9232	91	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	586	11	2	8	3.6	CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br	10.1021/jm3009103
	CHEMBL2103873	9232	91	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	586	11	2	8	3.6	CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br	10.1021/jm3009103
	DB08932	9232	91	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	586	11	2	8	3.6	CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br	10.1021/jm3009103
	44279554	106102	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors	ChEMBL	512	11	2	7	3.8	COCCNC(=O)c1cccc(S(=O)(=O)Nc2ncc(C)nc2OC)c1-c1ccc(CC(C)C)cc1	10.1016/S0960-894X(97)00228-X
	CHEMBL282187	106102	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors	ChEMBL	512	11	2	7	3.8	COCCNC(=O)c1cccc(S(=O)(=O)Nc2ncc(C)nc2OC)c1-c1ccc(CC(C)C)cc1	10.1016/S0960-894X(97)00228-X
	11754394	115405	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors	ChEMBL	468	8	2	6	3.8	CNC(=O)c1cccc(S(=O)(=O)Nc2ncc(C)nc2OC)c1-c1ccc(CC(C)C)cc1	10.1016/S0960-894X(97)00228-X
	CHEMBL32066	115405	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors	ChEMBL	468	8	2	6	3.8	CNC(=O)c1cccc(S(=O)(=O)Nc2ncc(C)nc2OC)c1-c1ccc(CC(C)C)cc1	10.1016/S0960-894X(97)00228-X
	9933950	209605	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	460	6	1	6	5.2	COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1	10.1021/jm010382z
	CHEMBL62395	209605	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	460	6	1	6	5.2	COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1	10.1021/jm010382z
	10553384	116445	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	498	13	1	7	3.6	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCn1cccn1	10.1021/jm980217s
	CHEMBL322537	116445	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	498	13	1	7	3.6	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCn1cccn1	10.1021/jm980217s
	44333721	174572	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	447	7	1	6	4.3	CCOCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(02)00663-7
	CHEMBL430506	174572	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	447	7	1	6	4.3	CCOCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(02)00663-7
	9916235	16125	1	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	578	14	1	7	4.6	CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1	10.1021/jm970101g
	CHEMBL111277	16125	1	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	578	14	1	7	4.6	CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1	10.1021/jm970101g
	10994374	210195	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	474	7	1	6	5.4	COc1ccc(CC2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1	10.1021/jm010382z
	CHEMBL65619	210195	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	474	7	1	6	5.4	COc1ccc(CC2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1	10.1021/jm010382z
	10651146	115641	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	596	12	1	8	4.4	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)c1ccc(OC)cc1	10.1021/jm970101g
	CHEMBL321035	115641	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	596	12	1	8	4.4	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)c1ccc(OC)cc1	10.1021/jm970101g
	10982740	210162	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	422	5	1	5	5.4	CC(C)Oc1ccc2c(c1)C(C1CCCC1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	CHEMBL65353	210162	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	422	5	1	5	5.4	CC(C)Oc1ccc2c(c1)C(C1CCCC1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	10187997	116749	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	564	13	1	7	4.2	CCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1	10.1021/jm970101g
	CHEMBL323464	116749	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	564	13	1	7	4.2	CCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1	10.1021/jm970101g
	10651488	170158	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	618	13	1	7	4.8	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCC(F)(F)F	10.1021/jm970101g
	CHEMBL419367	170158	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	618	13	1	7	4.8	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCC(F)(F)F	10.1021/jm970101g
	9915510	91930	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	549	8	2	8	3.4	CCOc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12	10.1016/s0960-894x(01)00660-6
	CHEMBL22513	91930	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	549	8	2	8	3.4	CCOc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12	10.1016/s0960-894x(01)00660-6
	9915510	91930	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells	ChEMBL	549	8	2	8	3.4	CCOc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12	10.1007/s00044-004-0021-y
	CHEMBL22513	91930	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells	ChEMBL	549	8	2	8	3.4	CCOc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12	10.1007/s00044-004-0021-y
	44334097	116846	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	447	7	2	6	3.7	COc1ccc([C@@H]2c3nc(CCCO)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1	10.1016/s0960-894x(02)00663-7
	CHEMBL323561	116846	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	447	7	2	6	3.7	COc1ccc([C@@H]2c3nc(CCCO)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1	10.1016/s0960-894x(02)00663-7
	10719598	213769	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Radioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cells	ChEMBL	482	10	1	6	3.9	CCCN(CCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL9139	213769	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Radioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cells	ChEMBL	482	10	1	6	3.9	CCCN(CCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	9915028	16183	18	None	-	2	Rat	9.3	pIC50	=	9.3	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	532	15	1	6	5.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC	10.1021/jm980217s
	CHEMBL111612	16183	18	None	-	2	Rat	9.3	pIC50	=	9.3	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	532	15	1	6	5.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC	10.1021/jm980217s
	CHEMBL4761843	16183	18	None	-	2	Rat	9.3	pIC50	=	9.3	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	532	15	1	6	5.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC	10.1021/jm980217s
	10886132	16581	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	549	10	1	9	4.8	COc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc(C)cc2)nc1	10.1021/jm0102304
	CHEMBL113757	16581	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	549	10	1	9	4.8	COc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc(C)cc2)nc1	10.1021/jm0102304
	CHEMBL368796	16581	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	549	10	1	9	4.8	COc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc(C)cc2)nc1	10.1021/jm0102304
	10744973	214055	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	538	14	1	6	5.5	CCCCCN(CCCCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL9313	214055	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	538	14	1	6	5.5	CCCCCN(CCCCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	10209779	170210	0	None	-	0	Rat	9.2	pIC50	=	9.2	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	560	14	1	7	4.5	CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm970101g
	CHEMBL419749	170210	0	None	-	0	Rat	9.2	pIC50	=	9.2	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	560	14	1	7	4.5	CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm970101g
	11015826	210310	0	None	-	0	Rat	9.2	pIC50	=	9.2	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	450	6	1	5	6.1	CC(C)Oc1ccc2c(c1)C(CC1CCCCC1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	CHEMBL66426	210310	0	None	-	0	Rat	9.2	pIC50	=	9.2	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	450	6	1	5	6.1	CC(C)Oc1ccc2c(c1)C(CC1CCCCC1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	9915028	16183	18	None	28183	2	Human	9.2	pIC50	=	9.2	Binding	Affinity On-target Cellular interaction (Endothelin-1-evoked phosphatidylinositol hydrolysis in MMQ cells) EUB0000348aPTSA EDNRAAffinity On-target Cellular interaction (Endothelin-1-evoked phosphatidylinositol hydrolysis in MMQ cells) EUB0000348aPTSA EDNRA	ChEMBL	532	15	1	6	5.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC	10.6019/CHEMBL5210121
	CHEMBL111612	16183	18	None	28183	2	Human	9.2	pIC50	=	9.2	Binding	Affinity On-target Cellular interaction (Endothelin-1-evoked phosphatidylinositol hydrolysis in MMQ cells) EUB0000348aPTSA EDNRAAffinity On-target Cellular interaction (Endothelin-1-evoked phosphatidylinositol hydrolysis in MMQ cells) EUB0000348aPTSA EDNRA	ChEMBL	532	15	1	6	5.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC	10.6019/CHEMBL5210121
	CHEMBL4761843	16183	18	None	28183	2	Human	9.2	pIC50	=	9.2	Binding	Affinity On-target Cellular interaction (Endothelin-1-evoked phosphatidylinositol hydrolysis in MMQ cells) EUB0000348aPTSA EDNRAAffinity On-target Cellular interaction (Endothelin-1-evoked phosphatidylinositol hydrolysis in MMQ cells) EUB0000348aPTSA EDNRA	ChEMBL	532	15	1	6	5.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC	10.6019/CHEMBL5210121
	10346184	15968	0	None	-	0	Rat	9.2	pIC50	=	9.2	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	508	12	1	5	4.9	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm010237l
	CHEMBL110366	15968	0	None	-	0	Rat	9.2	pIC50	=	9.2	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	508	12	1	5	4.9	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm010237l
	15411005	11532	0	None	-	0	Human	9.2	pIC50	=	9.2	Binding	Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells	ChEMBL	677	13	1	12	5.2	CCOC(=O)C(NC(=O)OC1(c2ccc(OC)cc2)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1cc(OC)c(OC)c(OC)c1)C(C)C	10.1016/S0960-894X(97)00002-4
	CHEMBL103846	11532	0	None	-	0	Human	9.2	pIC50	=	9.2	Binding	Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells	ChEMBL	677	13	1	12	5.2	CCOC(=O)C(NC(=O)OC1(c2ccc(OC)cc2)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1cc(OC)c(OC)c(OC)c1)C(C)C	10.1016/S0960-894X(97)00002-4
	10346184	15968	0	None	-	0	Rat	9.2	pIC50	=	9.2	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	508	12	1	5	4.9	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	CHEMBL110366	15968	0	None	-	0	Rat	9.2	pIC50	=	9.2	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	508	12	1	5	4.9	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	CHEMBL2373291	217153	0	None	-	1	Pig	9.2	pIC50	=	9.2	Binding	Tested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptorTested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptor	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H]2CSSC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1021/jm00077a013
	10579303	16203	0	None	-	0	Rat	9.2	pIC50	=	9.2	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	590	16	1	8	4.5	CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCOC)cc1	10.1021/jm970101g
	CHEMBL111712	16203	0	None	-	0	Rat	9.2	pIC50	=	9.2	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	590	16	1	8	4.5	CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCOC)cc1	10.1021/jm970101g
	11015645	209966	0	None	-	0	Rat	9.2	pIC50	=	9.2	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	438	9	1	5	6.1	CCCCCCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	CHEMBL64282	209966	0	None	-	0	Rat	9.2	pIC50	=	9.2	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	438	9	1	5	6.1	CCCCCCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	10938122	169785	0	None	-	0	Rat	9.2	pIC50	=	9.2	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	396	5	1	5	4.8	CC(C)Oc1ccc2c(c1)C(C(C)C)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	CHEMBL417555	169785	0	None	-	0	Rat	9.2	pIC50	=	9.2	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	396	5	1	5	4.8	CC(C)Oc1ccc2c(c1)C(C(C)C)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	10503921	108253	0	None	-	0	Human	9.2	pIC50	=	9.2	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	454	6	1	8	4.0	Cc1cc2c(cc1CC(=O)c1sccc1S(=O)(=O)Nc1noc(C)c1Cl)OCO2	10.1021/jm9700068
	CHEMBL297783	108253	0	None	-	0	Human	9.2	pIC50	=	9.2	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	454	6	1	8	4.0	Cc1cc2c(cc1CC(=O)c1sccc1S(=O)(=O)Nc1noc(C)c1Cl)OCO2	10.1021/jm9700068
	44279141	113800	0	None	-	0	Human	9.2	pIC50	=	9.2	Binding	In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors	ChEMBL	498	10	3	7	3.2	COc1nc(C)cnc1NS(=O)(=O)c1cccc(C(=O)NCCO)c1-c1ccc(CC(C)C)cc1	10.1016/S0960-894X(97)00228-X
	CHEMBL31544	113800	0	None	-	0	Human	9.2	pIC50	=	9.2	Binding	In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors	ChEMBL	498	10	3	7	3.2	COc1nc(C)cnc1NS(=O)(=O)c1cccc(C(=O)NCCO)c1-c1ccc(CC(C)C)cc1	10.1016/S0960-894X(97)00228-X
	10552883	116781	0	None	-	0	Rat	9.2	pIC50	=	9.2	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	484	13	1	5	4.8	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC=C1CC1	10.1021/jm980217s
	CHEMBL323485	116781	0	None	-	0	Rat	9.2	pIC50	=	9.2	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	484	13	1	5	4.8	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC=C1CC1	10.1021/jm980217s
	10974047	16289	0	None	-	0	Pig	9.2	pIC50	=	9.2	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	601	11	1	10	4.3	COc1ccc(S(=O)(=O)Nc2ncnc(OCCOc3ncc(Br)cn3)c2-c2ccc(C)cc2)cc1OC	10.1021/jm0102304
	CHEMBL112162	16289	0	None	-	0	Pig	9.2	pIC50	=	9.2	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	601	11	1	10	4.3	COc1ccc(S(=O)(=O)Nc2ncnc(OCCOc3ncc(Br)cn3)c2-c2ccc(C)cc2)cc1OC	10.1021/jm0102304
	10745942	16083	0	None	-	0	Rat	9.2	pIC50	=	9.2	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	588	13	1	8	4.3	CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc2c(c1)OCCO2	10.1021/jm970101g
	CHEMBL111010	16083	0	None	-	0	Rat	9.2	pIC50	=	9.2	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	588	13	1	8	4.3	CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc2c(c1)OCCO2	10.1021/jm970101g
	11080933	210191	0	None	-	0	Rat	9.2	pIC50	=	9.2	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	454	10	1	6	5.7	CCCCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	CHEMBL65599	210191	0	None	-	0	Rat	9.2	pIC50	=	9.2	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	454	10	1	6	5.7	CCCCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	10166223	209490	0	None	-	0	Human	9.2	pIC50	=	9.2	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	552	7	2	7	5.5	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)N(C)CC(C)(C)C)c1	10.1021/jm030528p
	CHEMBL61711	209490	0	None	-	0	Human	9.2	pIC50	=	9.2	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	552	7	2	7	5.5	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)N(C)CC(C)(C)C)c1	10.1021/jm030528p
	10076527	21387	0	None	-	0	Human	9.2	pIC50	=	9.2	Binding	Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer	ChEMBL	485	7	2	6	4.3	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3ccccc31)OCO2	10.1016/j.bmcl.2010.08.074
	CHEMBL1204990	21387	0	None	-	0	Human	9.2	pIC50	=	9.2	Binding	Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer	ChEMBL	485	7	2	6	4.3	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3ccccc31)OCO2	10.1016/j.bmcl.2010.08.074
	10720982	134595	0	None	-	0	Rat	9.2	pIC50	=	9.2	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	530	9	2	6	4.8	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)C)cc1	10.1021/jm031041j
	CHEMBL121647	134595	0	None	-	0	Rat	9.2	pIC50	=	9.2	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	530	9	2	6	4.8	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)C)cc1	10.1021/jm031041j
	CHEMBL366441	134595	0	None	-	0	Rat	9.2	pIC50	=	9.2	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	530	9	2	6	4.8	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)C)cc1	10.1021/jm031041j
	71462320	88779	0	None	-	0	Human	9.2	pIC50	=	9.2	Binding	Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)	ChEMBL	570	11	2	8	3.9	Cc1ccc(-c2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1016/j.bmcl.2016.06.014
	CHEMBL2165332	88779	0	None	-	0	Human	9.2	pIC50	=	9.2	Binding	Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)	ChEMBL	570	11	2	8	3.9	Cc1ccc(-c2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1016/j.bmcl.2016.06.014
	10720982	134595	0	None	-	0	Human	9.2	pIC50	=	9.2	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	530	9	2	6	4.8	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)C)cc1	10.1021/jm990171i
	CHEMBL121647	134595	0	None	-	0	Human	9.2	pIC50	=	9.2	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	530	9	2	6	4.8	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)C)cc1	10.1021/jm990171i
	CHEMBL366441	134595	0	None	-	0	Human	9.2	pIC50	=	9.2	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	530	9	2	6	4.8	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)C)cc1	10.1021/jm990171i
	10649266	16404	0	None	-	0	Rat	9.2	pIC50	=	9.2	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	506	12	1	5	5.7	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3ccoc3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	CHEMBL112685	16404	0	None	-	0	Rat	9.2	pIC50	=	9.2	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	506	12	1	5	5.7	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3ccoc3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	11505449	178263	0	None	-	0	Human	9.2	pIC50	=	9.2	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	616	12	3	9	2.6	O=C(O)CCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1	10.1016/j.bmcl.2016.06.014
	CHEMBL4463633	178263	0	None	-	0	Human	9.2	pIC50	=	9.2	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	616	12	3	9	2.6	O=C(O)CCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1	10.1016/j.bmcl.2016.06.014
	58688005	181739	1	None	-	0	Human	9.2	pIC50	=	9.2	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	540	11	2	9	3.1	CCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Br)cc1	10.1016/j.bmcl.2016.06.014
	CHEMBL4565926	181739	1	None	-	0	Human	9.2	pIC50	=	9.2	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	540	11	2	9	3.1	CCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Br)cc1	10.1016/j.bmcl.2016.06.014
	71462320	88779	0	None	-	0	Human	9.2	pIC50	=	9.2	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	570	11	2	8	3.9	Cc1ccc(-c2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm3009103
	CHEMBL2165332	88779	0	None	-	0	Human	9.2	pIC50	=	9.2	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	570	11	2	8	3.9	Cc1ccc(-c2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm3009103
	10746431	109083	0	None	-	0	Human	9.2	pIC50	=	9.2	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	619	12	1	11	3.9	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCN3CCOCC3)c2)cc1	10.1021/jm980504w
	CHEMBL303484	109083	0	None	-	0	Human	9.2	pIC50	=	9.2	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	619	12	1	11	3.9	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCN3CCOCC3)c2)cc1	10.1021/jm980504w
	9809919	211188	0	None	-	2	Human	9.2	pIC50	=	9.2	Binding	Receptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cellsReceptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cells	ChEMBL	665	13	2	13	4.5	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	CHEMBL72037	211188	0	None	-	2	Human	9.2	pIC50	=	9.2	Binding	Receptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cellsReceptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cells	ChEMBL	665	13	2	13	4.5	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	CHEMBL2373292	217154	0	None	-	1	Pig	9.2	pIC50	=	9.2	Binding	Tested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptorTested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptor	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)(C)C)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1021/jm00077a013
	9870959	15689	0	None	-	0	Rat	9.1	pIC50	=	9.1	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	509	13	1	6	4.3	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1ccccn1	10.1021/jm980217s
	CHEMBL109778	15689	0	None	-	0	Rat	9.1	pIC50	=	9.1	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	509	13	1	6	4.3	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1ccccn1	10.1021/jm980217s
	10916597	210094	0	None	-	0	Rat	9.1	pIC50	=	9.1	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	410	7	1	5	5.4	CCCCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	CHEMBL64832	210094	0	None	-	0	Rat	9.1	pIC50	=	9.1	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	410	7	1	5	5.4	CCCCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	44284184	146778	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	490	8	2	7	5.0	CCOc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O	10.1016/j.bmcl.2004.01.008
	CHEMBL38000	146778	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	490	8	2	7	5.0	CCOc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O	10.1016/j.bmcl.2004.01.008
	CHEMBL427748	220151	0	None	-	0	Pig	9.1	pIC50	=	9.1	Binding	Tested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptorTested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptor	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1021/jm00077a013
	11827489	123764	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	524	12	1	4	5.6	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CC)c(F)c1	10.1021/jm010237l
	CHEMBL338754	123764	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	524	12	1	4	5.6	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CC)c(F)c1	10.1021/jm010237l
	10984671	16245	0	None	-	0	Pig	9.1	pIC50	=	9.1	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	571	10	1	9	4.3	COc1ccc(S(=O)(=O)Nc2ncnc(OCCOc3ncc(Br)cn3)c2-c2ccc(C)cc2)cc1	10.1021/jm0102304
	CHEMBL111934	16245	0	None	-	0	Pig	9.1	pIC50	=	9.1	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	571	10	1	9	4.3	COc1ccc(S(=O)(=O)Nc2ncnc(OCCOc3ncc(Br)cn3)c2-c2ccc(C)cc2)cc1	10.1021/jm0102304
	10648006	168445	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	468	6	1	6	4.7	Cc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1	10.1021/jm9700068
	CHEMBL413093	168445	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	468	6	1	6	4.7	Cc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1	10.1021/jm9700068
	10648135	16114	0	None	-	0	Rat	9.1	pIC50	=	9.1	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	472	13	1	5	4.7	C/C=C/CC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC	10.1021/jm031041j
	CHEMBL111218	16114	0	None	-	0	Rat	9.1	pIC50	=	9.1	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	472	13	1	5	4.7	C/C=C/CC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC	10.1021/jm031041j
	10209320	16057	0	None	-	0	Rat	9.1	pIC50	=	9.1	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	546	12	1	7	4.0	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CC(C)C	10.1021/jm970101g
	CHEMBL110899	16057	0	None	-	0	Rat	9.1	pIC50	=	9.1	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	546	12	1	7	4.0	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CC(C)C	10.1021/jm970101g
	11038320	25645	0	None	-	0	Rat	9.1	pIC50	=	9.1	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	492	11	1	4	5.2	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(C)cc1	10.1021/jm010237l
	CHEMBL128240	25645	0	None	-	0	Rat	9.1	pIC50	=	9.1	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	492	11	1	4	5.2	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(C)cc1	10.1021/jm010237l
	44340049	117108	0	None	-	0	Rat	9.1	pIC50	=	9.1	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	500	13	1	5	5.3	C/C=C\C(C)(C)C[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC	10.1021/jm980217s
	CHEMBL323951	117108	0	None	-	0	Rat	9.1	pIC50	=	9.1	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	500	13	1	5	5.3	C/C=C\C(C)(C)C[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC	10.1021/jm980217s
	10552413	117445	0	None	-	0	Rat	9.1	pIC50	=	9.1	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	472	13	1	5	4.7	C/C=C\CC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC	10.1021/jm980217s
	CHEMBL325935	117445	0	None	-	0	Rat	9.1	pIC50	=	9.1	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	472	13	1	5	4.7	C/C=C\CC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC	10.1021/jm980217s
	44266851	21357	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells	ChEMBL	550	11	1	9	4.7	COc1ccc(C(=O)/C(Cc2ccc(OC)c(OC)c2OC)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1C	10.1021/jm9606507
	CHEMBL10847	21357	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells	ChEMBL	550	11	1	9	4.7	COc1ccc(C(=O)/C(Cc2ccc(OC)c(OC)c2OC)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1C	10.1021/jm9606507
	CHEMBL1204671	21357	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells	ChEMBL	550	11	1	9	4.7	COc1ccc(C(=O)/C(Cc2ccc(OC)c(OC)c2OC)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1C	10.1021/jm9606507
	44279316	114123	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors	ChEMBL	518	8	2	6	4.0	COc1nc(Br)cnc1NS(=O)(=O)c1cccc(C(N)=O)c1-c1ccc(CC(C)C)cc1	10.1016/S0960-894X(97)00228-X
	CHEMBL31763	114123	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors	ChEMBL	518	8	2	6	4.0	COc1nc(Br)cnc1NS(=O)(=O)c1cccc(C(N)=O)c1-c1ccc(CC(C)C)cc1	10.1016/S0960-894X(97)00228-X
	137649592	164189	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	567	10	2	9	4.6	CCCOc1ccc2c(c1)c(=O)c(Cc1cccc(-c3nnn[nH]3)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2	10.1016/j.bmcl.2017.04.049
	CHEMBL4078537	164189	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	567	10	2	9	4.6	CCCOc1ccc2c(c1)c(=O)c(Cc1cccc(-c3nnn[nH]3)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2	10.1016/j.bmcl.2017.04.049
	15411003	115497	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells	ChEMBL	589	11	1	10	4.8	C=CCNC(=O)OC1(c2ccc(OC)cc2)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1cc(OC)c(OC)c(OC)c1	10.1016/S0960-894X(97)00002-4
	CHEMBL320839	115497	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells	ChEMBL	589	11	1	10	4.8	C=CCNC(=O)OC1(c2ccc(OC)cc2)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1cc(OC)c(OC)c(OC)c1	10.1016/S0960-894X(97)00002-4
	10673644	16554	0	None	-	0	Rat	9.1	pIC50	=	9.1	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	524	12	1	6	4.7	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	CHEMBL113611	16554	0	None	-	0	Rat	9.1	pIC50	=	9.1	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	524	12	1	6	4.7	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	177236	8107	45	None	2	3	Human	9.1	pIC50	=	9.1	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	410	9	1	7	2.9	COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1	10.1016/s0960-894x(01)00660-6
	3508	8107	45	None	2	3	Human	9.1	pIC50	=	9.1	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	410	9	1	7	2.9	COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1	10.1016/s0960-894x(01)00660-6
	CHEMBL23261	8107	45	None	2	3	Human	9.1	pIC50	=	9.1	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	410	9	1	7	2.9	COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1	10.1016/s0960-894x(01)00660-6
	DB04883	8107	45	None	2	3	Human	9.1	pIC50	=	9.1	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	410	9	1	7	2.9	COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1	10.1016/s0960-894x(01)00660-6
	71462322	88785	11	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	572	10	2	8	3.2	CCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1	10.1021/jm3009103
	CHEMBL2165338	88785	11	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	572	10	2	8	3.2	CCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1	10.1021/jm3009103
	44284199	106886	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	552	9	2	7	6.2	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OCc2ccccc2)c1	10.1016/j.bmcl.2004.01.008
	CHEMBL287517	106886	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	552	9	2	7	6.2	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OCc2ccccc2)c1	10.1016/j.bmcl.2004.01.008
	10993320	209759	0	None	-	0	Rat	9.1	pIC50	=	9.1	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	412	6	1	6	4.6	CC(C)OC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	CHEMBL63067	209759	0	None	-	0	Rat	9.1	pIC50	=	9.1	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	412	6	1	6	4.6	CC(C)OC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	10097589	213060	0	None	-	0	Rat	9.1	pIC50	=	9.1	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	502	7	2	7	5.2	O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2cccs2)nn1CC1CCC(C(=O)O)CC1	10.1016/s0960-894x(00)00513-8
	CHEMBL86965	213060	0	None	-	0	Rat	9.1	pIC50	=	9.1	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	502	7	2	7	5.2	O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2cccs2)nn1CC1CCC(C(=O)O)CC1	10.1016/s0960-894x(00)00513-8
	10792319	214013	0	None	-	0	Rat	9.1	pIC50	=	9.1	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	530	10	1	6	5.1	CCCCN(C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1)c1ccccc1	10.1021/jm9505369
	CHEMBL9283	214013	0	None	-	0	Rat	9.1	pIC50	=	9.1	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	530	10	1	6	5.1	CCCCN(C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1)c1ccccc1	10.1021/jm9505369
	10648937	214085	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Radioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cells	ChEMBL	496	11	1	6	4.3	CCCCN(CCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL9334	214085	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Radioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cells	ChEMBL	496	11	1	6	4.3	CCCCN(CCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	10673644	16554	0	None	-	0	Rat	9.1	pIC50	=	9.1	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	524	12	1	6	4.7	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm010237l
	CHEMBL113611	16554	0	None	-	0	Rat	9.1	pIC50	=	9.1	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	524	12	1	6	4.7	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm010237l
	10814655	214379	0	None	-	0	Rat	9.1	pIC50	=	9.1	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	482	10	1	6	3.9	CCCCN(CC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL9502	214379	0	None	-	0	Rat	9.1	pIC50	=	9.1	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	482	10	1	6	3.9	CCCCN(CC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	44339714	118085	0	None	-	0	Rat	9.1	pIC50	=	9.1	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	500	14	1	5	5.4	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC/C=C(/C)CC	10.1021/jm980217s
	CHEMBL326685	118085	0	None	-	0	Rat	9.1	pIC50	=	9.1	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	500	14	1	5	5.4	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC/C=C(/C)CC	10.1021/jm980217s
	10984617	16780	0	None	-	0	Pig	9.1	pIC50	=	9.1	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	565	11	1	10	4.9	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(C)cn2)c1	10.1021/jm0102304
	CHEMBL114933	16780	0	None	-	0	Pig	9.1	pIC50	=	9.1	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	565	11	1	10	4.9	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(C)cn2)c1	10.1021/jm0102304
	44284183	146353	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	518	9	2	7	5.7	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OCC(C)C)c1	10.1016/j.bmcl.2004.01.008
	CHEMBL37973	146353	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor	ChEMBL	518	9	2	7	5.7	COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OCC(C)C)c1	10.1016/j.bmcl.2004.01.008
	11027946	25685	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	540	12	1	5	5.4	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CC)c(F)c1	10.1021/jm010237l
	CHEMBL128479	25685	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	540	12	1	5	5.4	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CC)c(F)c1	10.1021/jm010237l
	11006213	176048	0	None	-	0	Pig	9.1	pIC50	=	9.1	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	557	10	1	10	5.3	CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2cccs2)nc1	10.1021/jm0102304
	CHEMBL441277	176048	0	None	-	0	Pig	9.1	pIC50	=	9.1	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	557	10	1	10	5.3	CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2cccs2)nc1	10.1021/jm0102304
	10602743	13929	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	550	9	1	10	4.2	COc1ccc(C2(O)OC(=O)C(c3cc(OC)c4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1C	10.1021/jm9606507
	CHEMBL10854	13929	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	550	9	1	10	4.2	COc1ccc(C2(O)OC(=O)C(c3cc(OC)c4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1C	10.1021/jm9606507
	10983992	26233	0	None	-	0	Rat	9.0	pIC50	=	9.0	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	506	12	1	4	5.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CC)cc1	10.1021/jm010237l
	CHEMBL129740	26233	0	None	-	0	Rat	9.0	pIC50	=	9.0	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	506	12	1	4	5.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CC)cc1	10.1021/jm010237l
	44333598	115967	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	447	7	1	6	4.6	CCCOc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(02)00663-7
	CHEMBL321520	115967	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	447	7	1	6	4.6	CCCOc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(02)00663-7
	11037806	209603	0	None	-	0	Rat	9.0	pIC50	=	9.0	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	456	10	2	7	4.3	CC(C)Oc1ccc2c(c1)C(OCCCCCO)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	CHEMBL62376	209603	0	None	-	0	Rat	9.0	pIC50	=	9.0	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	456	10	2	7	4.3	CC(C)Oc1ccc2c(c1)C(OCCCCCO)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	10788494	177402	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	424	6	1	6	4.5	Cc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1	10.1021/jm9700068
	CHEMBL445101	177402	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	424	6	1	6	4.5	Cc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1	10.1021/jm9700068
	10768294	21360	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells	ChEMBL	520	10	1	8	4.7	COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1C	10.1021/jm9606507
	CHEMBL10922	21360	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells	ChEMBL	520	10	1	8	4.7	COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1C	10.1021/jm9606507
	CHEMBL1204674	21360	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells	ChEMBL	520	10	1	8	4.7	COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1C	10.1021/jm9606507
	10625694	18218	0	None	-	0	Human	9.0	pIC50	=	9	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	516	9	2	6	4.5	CCC(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1	10.1021/jm990171i
	CHEMBL1180344	18218	0	None	-	0	Human	9.0	pIC50	=	9	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	516	9	2	6	4.5	CCC(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1	10.1021/jm990171i
	CHEMBL123107	18218	0	None	-	0	Human	9.0	pIC50	=	9	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	516	9	2	6	4.5	CCC(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1	10.1021/jm990171i
	9868379	107560	0	None	-	0	Rat	9.0	pIC50	=	9	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	450	5	1	6	5.6	Cc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)s1	10.1021/jm010382z
	CHEMBL293012	107560	0	None	-	0	Rat	9.0	pIC50	=	9	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	450	5	1	6	5.6	Cc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)s1	10.1021/jm010382z
	44332842	116498	0	None	-	0	Human	9.0	pIC50	=	9	Binding	Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells	ChEMBL	703	11	1	10	7.5	COc1ccc(C2(OC(=O)N[C@@H](C)c3cccc4ccccc34)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1	10.1016/S0960-894X(97)00002-4
	CHEMBL322920	116498	0	None	-	0	Human	9.0	pIC50	=	9	Binding	Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells	ChEMBL	703	11	1	10	7.5	COc1ccc(C2(OC(=O)N[C@@H](C)c3cccc4ccccc34)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1	10.1016/S0960-894X(97)00002-4
	44314904	109924	0	None	-	0	Pig	9.0	pIC50	=	9	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	585	12	5	5	3.6	CSCCC(NC(=O)[C@@H](Cc1c(C)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O	10.1021/jm9600914
	CHEMBL307936	109924	0	None	-	0	Pig	9.0	pIC50	=	9	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	585	12	5	5	3.6	CSCCC(NC(=O)[C@@H](Cc1c(C)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O	10.1021/jm9600914
	10649321	117723	0	None	-	0	Rat	9.0	pIC50	=	9	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	508	12	1	5	4.9	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	CHEMBL326191	117723	0	None	-	0	Rat	9.0	pIC50	=	9	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	508	12	1	5	4.9	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	3951	7179	86	None	-1	2	Human	9.0	pIC50	=	9	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	378	7	1	5	3.5	COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1	10.1016/j.bmcl.2016.06.014
	4337	7179	86	None	-1	2	Human	9.0	pIC50	=	9	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	378	7	1	5	3.5	COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1	10.1016/j.bmcl.2016.06.014
	6918493	7179	86	None	-1	2	Human	9.0	pIC50	=	9	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	378	7	1	5	3.5	COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1	10.1016/j.bmcl.2016.06.014
	CHEMBL1111	7179	86	None	-1	2	Human	9.0	pIC50	=	9	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	378	7	1	5	3.5	COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1	10.1016/j.bmcl.2016.06.014
	DB06403	7179	86	None	-1	2	Human	9.0	pIC50	=	9	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	378	7	1	5	3.5	COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1	10.1016/j.bmcl.2016.06.014
	9868379	107560	0	None	-	0	Human	9.0	pIC50	=	9	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	450	5	1	6	5.6	Cc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)s1	10.1016/j.bmcl.2016.06.014
	CHEMBL293012	107560	0	None	-	0	Human	9.0	pIC50	=	9	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	450	5	1	6	5.6	Cc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)s1	10.1016/j.bmcl.2016.06.014
	155519384	177197	0	None	-	1	Human	9.0	pIC50	=	9	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	674	12	1	13	4.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)c1ccccn1	10.1016/j.bmcl.2016.06.014
	CHEMBL4448273	177197	0	None	-	1	Human	9.0	pIC50	=	9	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	674	12	1	13	4.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)c1ccccn1	10.1016/j.bmcl.2016.06.014
	155551580	180772	0	None	-	0	Human	9.0	pIC50	=	9	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	526	12	2	10	3.0	CCNS(=O)(=O)Nc1ncnc(OCCOc2cc(OC)ccc2Cl)c1-c1ncc(SC)cn1	10.1016/j.bmcl.2016.06.014
	CHEMBL4542394	180772	0	None	-	0	Human	9.0	pIC50	=	9	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	526	12	2	10	3.0	CCNS(=O)(=O)Nc1ncnc(OCCOc2cc(OC)ccc2Cl)c1-c1ncc(SC)cn1	10.1016/j.bmcl.2016.06.014
	10146305	181050	0	None	-	0	Human	9.0	pIC50	=	9	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	656	14	2	13	4.2	COc1ccccc1Oc1c(NS(=O)(=O)CCc2cccs2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1	10.1016/j.bmcl.2016.06.014
	CHEMBL4549357	181050	0	None	-	0	Human	9.0	pIC50	=	9	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	656	14	2	13	4.2	COc1ccccc1Oc1c(NS(=O)(=O)CCc2cccs2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1	10.1016/j.bmcl.2016.06.014
	44439102	97074	0	None	-	0	Human	9.0	pIC50	=	9	Binding	Displacement of [125I]ET1 from human ETA receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETA receptor expressed in CHO cells	ChEMBL	508	8	1	7	5.2	CN(Cc1cc(-c2ncco2)ccc1-c1ccccc1S(=O)(=O)Nc1ccno1)C(=O)CC(C)(C)C	10.1016/j.bmcl.2006.10.009
	CHEMBL238539	97074	0	None	-	0	Human	9.0	pIC50	=	9	Binding	Displacement of [125I]ET1 from human ETA receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETA receptor expressed in CHO cells	ChEMBL	508	8	1	7	5.2	CN(Cc1cc(-c2ncco2)ccc1-c1ccccc1S(=O)(=O)Nc1ccno1)C(=O)CC(C)(C)C	10.1016/j.bmcl.2006.10.009
	71460621	88776	0	None	-	0	Human	9.0	pIC50	=	9	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	602	13	2	10	3.7	COc1cccc(Oc2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)c1	10.1021/jm3009103
	CHEMBL2165329	88776	0	None	-	0	Human	9.0	pIC50	=	9	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	602	13	2	10	3.7	COc1cccc(Oc2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)c1	10.1021/jm3009103
	44295173	21405	0	None	-	0	Rat	9.0	pIC50	=	9	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	554	10	1	9	5.3	COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1Cl	10.1016/s0960-894x(98)00301-1
	CHEMBL1205090	21405	0	None	-	0	Rat	9.0	pIC50	=	9	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	554	10	1	9	5.3	COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1Cl	10.1016/s0960-894x(98)00301-1
	CHEMBL51234	21405	0	None	-	0	Rat	9.0	pIC50	=	9	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	554	10	1	9	5.3	COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1Cl	10.1016/s0960-894x(98)00301-1
	44279398	106665	0	None	-	0	Human	9.0	pIC50	=	9	Binding	In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors	ChEMBL	454	8	2	6	3.6	COc1nc(C)cnc1NS(=O)(=O)c1cccc(C(N)=O)c1-c1ccc(CC(C)C)cc1	10.1016/S0960-894X(97)00228-X
	CHEMBL285976	106665	0	None	-	0	Human	9.0	pIC50	=	9	Binding	In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors	ChEMBL	454	8	2	6	3.6	COc1nc(C)cnc1NS(=O)(=O)c1cccc(C(N)=O)c1-c1ccc(CC(C)C)cc1	10.1016/S0960-894X(97)00228-X
	44279294	106672	0	None	-	0	Human	9.0	pIC50	=	9	Binding	In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors	ChEMBL	546	8	1	6	4.6	COc1nc(Br)cnc1NS(=O)(=O)c1cccc(C(=O)N(C)C)c1-c1ccc(CC(C)C)cc1	10.1016/S0960-894X(97)00228-X
	CHEMBL286014	106672	0	None	-	0	Human	9.0	pIC50	=	9	Binding	In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors	ChEMBL	546	8	1	6	4.6	COc1nc(Br)cnc1NS(=O)(=O)c1cccc(C(=O)N(C)C)c1-c1ccc(CC(C)C)cc1	10.1016/S0960-894X(97)00228-X
	10897248	16281	0	None	-	0	Pig	9.0	pIC50	=	9	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	591	9	1	8	5.4	Cc1ccc(-c2c(NS(=O)(=O)c3ccc4ccccc4c3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm0102304
	CHEMBL112134	16281	0	None	-	0	Pig	9.0	pIC50	=	9	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	591	9	1	8	5.4	Cc1ccc(-c2c(NS(=O)(=O)c3ccc4ccccc4c3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm0102304
	11136124	17142	0	None	-	0	Pig	9.0	pIC50	=	9	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	667	9	1	8	4.9	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(I)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm0102304
	CHEMBL116220	17142	0	None	-	0	Pig	9.0	pIC50	=	9	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	667	9	1	8	4.9	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(I)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm0102304
	10211781	136519	0	None	-	1	Human	9.0	pIC50	=	9	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	661	11	2	13	3.6	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccccn1	10.1016/s0960-894x(02)01084-3
	CHEMBL367453	136519	0	None	-	1	Human	9.0	pIC50	=	9	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	661	11	2	13	3.6	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccccn1	10.1016/s0960-894x(02)01084-3
	10146640	214333	0	None	-	1	Human	9.0	pIC50	=	9	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	689	12	2	13	4.5	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccccn1	10.1016/s0960-894x(02)01084-3
	CHEMBL94786	214333	0	None	-	1	Human	9.0	pIC50	=	9	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	689	12	2	13	4.5	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccccn1	10.1016/s0960-894x(02)01084-3
	10555191	210571	0	None	-	0	Human	9.0	pIC50	=	9	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	577	12	1	10	4.2	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCN(C)C)c2)cc1	10.1021/jm980504w
	CHEMBL68269	210571	0	None	-	0	Human	9.0	pIC50	=	9	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	577	12	1	10	4.2	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCN(C)C)c2)cc1	10.1021/jm980504w
	CHEMBL1790519	215672	0	None	-	0	Human	9.0	pIC50	=	9	Binding	Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N(C)[C@@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@H](C)CC	10.1021/jm970161m
	44311346	109940	0	None	-	1	Human	9.0	pIC50	=	9	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	681	13	2	13	5.2	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCSCC2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	CHEMBL308088	109940	0	None	-	1	Human	9.0	pIC50	=	9	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	681	13	2	13	5.2	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCSCC2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	44340049	117108	0	None	-	0	Human	9.0	pIC50	=	9	Binding	Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)	ChEMBL	500	13	1	5	5.3	C/C=C\C(C)(C)C[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC	10.1021/jm980217s
	CHEMBL323951	117108	0	None	-	0	Human	9.0	pIC50	=	9	Binding	Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)	ChEMBL	500	13	1	5	5.3	C/C=C\C(C)(C)C[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC	10.1021/jm980217s
	44339662	16624	0	None	-	0	Rat	9.0	pIC50	=	9.0	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	527	13	1	7	4.6	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1nc(C)c(C)o1	10.1021/jm980217s
	CHEMBL114074	16624	0	None	-	0	Rat	9.0	pIC50	=	9.0	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	527	13	1	7	4.6	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1nc(C)c(C)o1	10.1021/jm980217s
	44351961	25608	0	None	-	0	Rat	9.0	pIC50	=	9.0	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	522	13	1	5	5.6	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CCC)cc1	10.1021/jm010237l
	CHEMBL128061	25608	0	None	-	0	Rat	9.0	pIC50	=	9.0	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	522	13	1	5	5.6	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CCC)cc1	10.1021/jm010237l
	10553384	116445	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)	ChEMBL	498	13	1	7	3.6	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCn1cccn1	10.1021/jm980217s
	CHEMBL322537	116445	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)	ChEMBL	498	13	1	7	3.6	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCn1cccn1	10.1021/jm980217s
	9909467	212290	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	409	4	1	5	3.8	Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1Br	10.1016/0960-894X(96)00441-6
	CHEMBL80782	212290	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	409	4	1	5	3.8	Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1Br	10.1016/0960-894X(96)00441-6
	9827093	180203	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	494	9	2	7	5.1	CCCc1nc(SC2CCC(CC(=O)O)CC2)c(C(=O)O)n1Cc1cc2c(cc1Cl)OCO2	10.1016/j.bmcl.2016.06.014
	CHEMBL4528664	180203	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	494	9	2	7	5.1	CCCc1nc(SC2CCC(CC(=O)O)CC2)c(C(=O)O)n1Cc1cc2c(cc1Cl)OCO2	10.1016/j.bmcl.2016.06.014
	10347080	92002	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	535	7	2	8	3.0	COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12	10.1016/s0960-894x(01)00660-6
	CHEMBL22562	92002	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	535	7	2	8	3.0	COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12	10.1016/s0960-894x(01)00660-6
	10347080	92002	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells	ChEMBL	535	7	2	8	3.0	COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12	10.1007/s00044-004-0021-y
	CHEMBL22562	92002	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells	ChEMBL	535	7	2	8	3.0	COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12	10.1007/s00044-004-0021-y
	71449713	88443	27	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	585	11	1	8	4.5	CCCCS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1	10.1021/jm3009103
	CHEMBL2163694	88443	27	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	585	11	1	8	4.5	CCCCS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1	10.1021/jm3009103
	71458719	88453	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	647	15	1	13	4.7	COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(SC)cn1	10.1021/jm3009103
	CHEMBL2163704	88453	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	647	15	1	13	4.7	COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(SC)cn1	10.1021/jm3009103
	17885918	112750	0	None	-	0	Rat	9.0	pIC50	=	9.0	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	458	6	1	6	5.9	O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccsc2)nn1CC1CCCCC1	10.1016/s0960-894x(00)00513-8
	CHEMBL313044	112750	0	None	-	0	Rat	9.0	pIC50	=	9.0	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	458	6	1	6	5.9	O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccsc2)nn1CC1CCCCC1	10.1016/s0960-894x(00)00513-8
	9846994	112766	0	None	-	0	Rat	9.0	pIC50	=	9.0	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	458	6	1	6	5.9	O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2cccs2)nn1CC1CCCCC1	10.1016/s0960-894x(00)00513-8
	CHEMBL313153	112766	0	None	-	0	Rat	9.0	pIC50	=	9.0	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	458	6	1	6	5.9	O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2cccs2)nn1CC1CCCCC1	10.1016/s0960-894x(00)00513-8
	44380976	172405	0	None	-	0	Pig	9.0	pIC50	=	9.0	Binding	In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.	ChEMBL	639	10	1	8	6.7	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)nc(C(C)C)nc2OCCOc2ncc(Br)cn2)cc1	10.1016/s0960-894x(01)00682-5
	CHEMBL424358	172405	0	None	-	0	Pig	9.0	pIC50	=	9.0	Binding	In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.	ChEMBL	639	10	1	8	6.7	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)nc(C(C)C)nc2OCCOc2ncc(Br)cn2)cc1	10.1016/s0960-894x(01)00682-5
	10505755	21356	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells	ChEMBL	506	10	1	8	4.4	COc1ccc(C(=O)/C(Cc2ccc(OC)c(OC)c2OC)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1	10.1021/jm9606507
	CHEMBL10832	21356	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells	ChEMBL	506	10	1	8	4.4	COc1ccc(C(=O)/C(Cc2ccc(OC)c(OC)c2OC)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1	10.1021/jm9606507
	CHEMBL1204670	21356	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells	ChEMBL	506	10	1	8	4.4	COc1ccc(C(=O)/C(Cc2ccc(OC)c(OC)c2OC)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1	10.1021/jm9606507
	9870830	213493	38	None	66	2	Human	9.0	pIC50	=	9.0	Binding	Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells	ChEMBL	506	8	1	9	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1	10.1021/jm9606507
	CHEMBL8981	213493	38	None	66	2	Human	9.0	pIC50	=	9.0	Binding	Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells	ChEMBL	506	8	1	9	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1	10.1021/jm9606507
	10142669	16216	0	None	-	0	Rat	8.9	pIC50	=	8.9	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	518	11	1	7	3.3	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CC	10.1021/jm970101g
	CHEMBL111769	16216	0	None	-	0	Rat	8.9	pIC50	=	8.9	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	518	11	1	7	3.3	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CC	10.1021/jm970101g
	137637038	162720	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	581	11	2	9	5.0	CCCCOc1ccc2c(c1)c(=O)c(Cc1cccc(-c3nnn[nH]3)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2	10.1016/j.bmcl.2017.04.049
	CHEMBL4061110	162720	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	581	11	2	9	5.0	CCCCOc1ccc2c(c1)c(=O)c(Cc1cccc(-c3nnn[nH]3)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2	10.1016/j.bmcl.2017.04.049
	10649321	117723	0	None	-	0	Rat	8.9	pIC50	=	8.9	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	508	12	1	5	4.9	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm010237l
	CHEMBL326191	117723	0	None	-	0	Rat	8.9	pIC50	=	8.9	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	508	12	1	5	4.9	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm010237l
	10576427	12142	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	473	6	2	7	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(NC(C)=O)cc2)cc1	10.1021/jm9606507
	CHEMBL10697	12142	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	473	6	2	7	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(NC(C)=O)cc2)cc1	10.1021/jm9606507
	21041324	88439	5	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	542	11	2	8	3.5	CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Cl)cc1	10.1021/jm3009103
	CHEMBL2163690	88439	5	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	542	11	2	8	3.5	CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Cl)cc1	10.1021/jm3009103
	11093167	16825	0	None	-	0	Pig	8.9	pIC50	=	8.9	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	593	11	1	9	6.3	CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc(C(C)C)cc2)nc1	10.1021/jm0102304
	CHEMBL115230	16825	0	None	-	0	Pig	8.9	pIC50	=	8.9	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	593	11	1	9	6.3	CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc(C(C)C)cc2)nc1	10.1021/jm0102304
	11813644	117154	0	None	-	0	Pig	8.9	pIC50	=	8.9	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	551	11	1	10	4.6	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ccncn2)c1	10.1021/jm0102304
	CHEMBL324246	117154	0	None	-	0	Pig	8.9	pIC50	=	8.9	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	551	11	1	10	4.6	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ccncn2)c1	10.1021/jm0102304
	CHEMBL414165	219894	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Inhibitory effect against Human ET-A receptorInhibitory effect against Human ET-A receptor	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](c2cccs2)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	10719598	213769	0	None	-	0	Rat	8.9	pIC50	=	8.9	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	482	10	1	6	3.9	CCCN(CCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL9139	213769	0	None	-	0	Rat	8.9	pIC50	=	8.9	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	482	10	1	6	3.9	CCCN(CCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	44279296	117407	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors	ChEMBL	532	8	2	6	4.3	CNC(=O)c1cccc(S(=O)(=O)Nc2ncc(Br)nc2OC)c1-c1ccc(CC(C)C)cc1	10.1016/S0960-894X(97)00228-X
	CHEMBL32572	117407	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors	ChEMBL	532	8	2	6	4.3	CNC(=O)c1cccc(S(=O)(=O)Nc2ncc(Br)nc2OC)c1-c1ccc(CC(C)C)cc1	10.1016/S0960-894X(97)00228-X
	10206812	206414	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	492	6	2	8	5.0	Cc1cc(-c2ncco2)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl	10.1021/jm030528p
	CHEMBL59288	206414	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	492	6	2	8	5.0	Cc1cc(-c2ncco2)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl	10.1021/jm030528p
	11102609	175349	0	None	-	0	Rat	8.9	pIC50	=	8.9	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	462	6	1	6	5.2	COc1ccc([C@@H]2c3cc(OC(C)C)ccc3O[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1	10.1021/jm031041j
	CHEMBL435773	175349	0	None	-	0	Rat	8.9	pIC50	=	8.9	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	462	6	1	6	5.2	COc1ccc([C@@H]2c3cc(OC(C)C)ccc3O[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1	10.1021/jm031041j
	10603546	117224	0	None	-	0	Rat	8.9	pIC50	=	8.9	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	592	15	1	7	5.0	CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCC)c(F)c1	10.1021/jm970101g
	CHEMBL324639	117224	0	None	-	0	Rat	8.9	pIC50	=	8.9	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	592	15	1	7	5.0	CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCC)c(F)c1	10.1021/jm970101g
	11102609	175349	0	None	-	0	Rat	8.9	pIC50	=	8.9	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	462	6	1	6	5.2	COc1ccc([C@@H]2c3cc(OC(C)C)ccc3O[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1	10.1021/jm010382z
	CHEMBL435773	175349	0	None	-	0	Rat	8.9	pIC50	=	8.9	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	462	6	1	6	5.2	COc1ccc([C@@H]2c3cc(OC(C)C)ccc3O[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1	10.1021/jm010382z
	10576910	115316	0	None	-	0	Rat	8.9	pIC50	=	8.9	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	486	13	1	5	5.1	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC=C(C)C	10.1021/jm980217s
	CHEMBL320124	115316	0	None	-	0	Rat	8.9	pIC50	=	8.9	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	486	13	1	5	5.1	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC=C(C)C	10.1021/jm980217s
	10278777	174911	0	None	-	0	Rat	8.9	pIC50	=	8.9	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	502	14	1	5	5.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC	10.1021/jm980217s
	CHEMBL432974	174911	0	None	-	0	Rat	8.9	pIC50	=	8.9	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	502	14	1	5	5.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC	10.1021/jm980217s
	10767586	16541	0	None	-	0	Rat	8.9	pIC50	=	8.9	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	496	13	1	5	5.0	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc(OC)cc2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	CHEMBL113529	16541	0	None	-	0	Rat	8.9	pIC50	=	8.9	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	496	13	1	5	5.0	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc(OC)cc2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	58688008	182081	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	496	11	2	9	3.0	CCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Cl)cc1	10.1016/j.bmcl.2016.06.014
	CHEMBL4573273	182081	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	496	11	2	9	3.0	CCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Cl)cc1	10.1016/j.bmcl.2016.06.014
	23670447	9803	2	None	-	2	Rat	8.9	pIC50	=	8.9	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	528	10	0	9	0.1	COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+]	10.1016/s0960-894x(98)00301-1
	999	9803	2	None	-	2	Rat	8.9	pIC50	=	8.9	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	528	10	0	9	0.1	COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+]	10.1016/s0960-894x(98)00301-1
	CHEMBL1204799	9803	2	None	-	2	Rat	8.9	pIC50	=	8.9	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	528	10	0	9	0.1	COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+]	10.1016/s0960-894x(98)00301-1
	CHEMBL25438	9803	2	None	-	2	Rat	8.9	pIC50	=	8.9	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	528	10	0	9	0.1	COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+]	10.1016/s0960-894x(98)00301-1
	44320480	112735	0	None	-	0	Rat	8.9	pIC50	=	8.9	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	442	6	1	6	5.4	O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccco2)nn1CC1CCCCC1	10.1016/s0960-894x(00)00513-8
	CHEMBL312979	112735	0	None	-	0	Rat	8.9	pIC50	=	8.9	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	442	6	1	6	5.4	O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccco2)nn1CC1CCCCC1	10.1016/s0960-894x(00)00513-8
	17885920	213220	0	None	-	0	Rat	8.9	pIC50	=	8.9	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	502	7	2	7	5.2	O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2cccs2)nn1CC1CCCC(C(=O)O)C1	10.1016/s0960-894x(00)00513-8
	CHEMBL88011	213220	0	None	-	0	Rat	8.9	pIC50	=	8.9	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	502	7	2	7	5.2	O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2cccs2)nn1CC1CCCC(C(=O)O)C1	10.1016/s0960-894x(00)00513-8
	44291775	107944	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	506	6	1	10	4.1	CC#N.Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Cc2cc3c(cc2C#N)OCO3)c1Cl	10.1021/jm9700068
	CHEMBL295557	107944	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	506	6	1	10	4.1	CC#N.Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Cc2cc3c(cc2C#N)OCO3)c1Cl	10.1021/jm9700068
	10280278	107620	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	535	7	2	7	6.1	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)C2CCCCC2)c1	10.1021/jm030528p
	CHEMBL293421	107620	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	535	7	2	7	6.1	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)C2CCCCC2)c1	10.1021/jm030528p
	11071347	124584	0	None	-	0	Rat	8.9	pIC50	=	8.9	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	516	11	1	5	5.0	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(F)c(F)c1	10.1021/jm010237l
	CHEMBL340190	124584	0	None	-	0	Rat	8.9	pIC50	=	8.9	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	516	11	1	5	5.0	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(F)c(F)c1	10.1021/jm010237l
	10745564	12997	0	None	-	0	Rat	8.9	pIC50	=	8.9	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	566	11	1	7	4.4	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)c1ccccc1	10.1021/jm970101g
	CHEMBL108142	12997	0	None	-	0	Rat	8.9	pIC50	=	8.9	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	566	11	1	7	4.4	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)c1ccccc1	10.1021/jm970101g
	11125029	16811	0	None	-	0	Pig	8.9	pIC50	=	8.9	Binding	Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane	ChEMBL	627	11	2	9	4.6	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C(=O)O)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm000538f
	CHEMBL115147	16811	0	None	-	0	Pig	8.9	pIC50	=	8.9	Binding	Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane	ChEMBL	627	11	2	9	4.6	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C(=O)O)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm000538f
	15453177	212300	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	392	4	1	4	4.2	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2)c1Br	10.1016/0960-894X(96)00441-6
	CHEMBL80857	212300	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	392	4	1	4	4.2	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2)c1Br	10.1016/0960-894X(96)00441-6
	10790757	103988	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	476	7	1	8	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(OC)c(OC)c2)cc1	10.1021/jm9606507
	CHEMBL268480	103988	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	476	7	1	8	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(OC)c(OC)c2)cc1	10.1021/jm9606507
	10554273	16182	0	None	-	0	Rat	8.9	pIC50	=	8.9	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	532	13	1	7	4.1	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)C1OCCO1	10.1021/jm980217s
	CHEMBL111611	16182	0	None	-	0	Rat	8.9	pIC50	=	8.9	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	532	13	1	7	4.1	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)C1OCCO1	10.1021/jm980217s
	8260	7319	54	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cellsDisplacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cells	ChEMBL	479	8	1	9	3.9	COc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cn1)C)c1ccncc1	10.1016/j.bmcl.2016.06.014
	9912992	7319	54	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cellsDisplacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cells	ChEMBL	479	8	1	9	3.9	COc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cn1)C)c1ccncc1	10.1016/j.bmcl.2016.06.014
	CHEMBL3989834	7319	54	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cellsDisplacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cells	ChEMBL	479	8	1	9	3.9	COc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cn1)C)c1ccncc1	10.1016/j.bmcl.2016.06.014
	18630945	177771	1	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cellsDisplacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cells	ChEMBL	507	9	1	9	4.7	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccncc2)nc1OC	10.1016/j.bmcl.2016.06.014
	CHEMBL4456288	177771	1	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cellsDisplacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cells	ChEMBL	507	9	1	9	4.7	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccncc2)nc1OC	10.1016/j.bmcl.2016.06.014
	155542285	179856	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	522	14	2	11	2.9	CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1Oc1cccc(OC)c1	10.1016/j.bmcl.2016.06.014
	CHEMBL4519822	179856	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	522	14	2	11	2.9	CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1Oc1cccc(OC)c1	10.1016/j.bmcl.2016.06.014
	11477084	10382	53	None	1	2	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	10.1021/jm030528p
	216235	10382	53	None	1	2	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	10.1021/jm030528p
	3548	10382	53	None	1	2	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	10.1021/jm030528p
	3950	10382	53	None	1	2	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	10.1021/jm030528p
	CHEMBL282724	10382	53	None	1	2	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	10.1021/jm030528p
	DB06268	10382	53	None	1	2	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	10.1021/jm030528p
	22467234	92128	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells	ChEMBL	534	7	1	8	4.1	COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(C)=O)ccc12	10.1007/s00044-004-0021-y
	CHEMBL2261599	92128	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells	ChEMBL	534	7	1	8	4.1	COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(C)=O)ccc12	10.1007/s00044-004-0021-y
	21041372	88475	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	687	14	2	12	3.6	COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(N2CCOCC2)nc1OCCOc1ncc(Br)cn1	10.1021/jm3009103
	CHEMBL2163725	88475	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	687	14	2	12	3.6	COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(N2CCOCC2)nc1OCCOc1ncc(Br)cn1	10.1021/jm3009103
	21041370	88777	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	636	13	2	10	4.4	COc1ccc(Cl)c(Oc2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)c1	10.1021/jm3009103
	CHEMBL2165330	88777	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	636	13	2	10	4.4	COc1ccc(Cl)c(Oc2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)c1	10.1021/jm3009103
	21979593	88780	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	590	11	2	8	4.3	O=S(=O)(NCc1ccccc1)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Cl)cc1	10.1021/jm3009103
	CHEMBL2165333	88780	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	590	11	2	8	4.3	O=S(=O)(NCc1ccccc1)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Cl)cc1	10.1021/jm3009103
	44295177	21553	0	None	-	0	Rat	8.9	pIC50	=	8.9	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	534	10	1	9	5.0	COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1C	10.1016/s0960-894x(98)00301-1
	CHEMBL1206680	21553	0	None	-	0	Rat	8.9	pIC50	=	8.9	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	534	10	1	9	5.0	COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1C	10.1016/s0960-894x(98)00301-1
	CHEMBL295483	21553	0	None	-	0	Rat	8.9	pIC50	=	8.9	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	534	10	1	9	5.0	COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1C	10.1016/s0960-894x(98)00301-1
	104865	7493	99	None	-1	4	Rat	8.9	pIC50	=	8.9	Binding	In vitro for specific binding of [125I]ET1 to A10 cell expressed in endothelin A receptorIn vitro for specific binding of [125I]ET1 to A10 cell expressed in endothelin A receptor	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm0102304
	3494	7493	99	None	-1	4	Rat	8.9	pIC50	=	8.9	Binding	In vitro for specific binding of [125I]ET1 to A10 cell expressed in endothelin A receptorIn vitro for specific binding of [125I]ET1 to A10 cell expressed in endothelin A receptor	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm0102304
	392	7493	99	None	-1	4	Rat	8.9	pIC50	=	8.9	Binding	In vitro for specific binding of [125I]ET1 to A10 cell expressed in endothelin A receptorIn vitro for specific binding of [125I]ET1 to A10 cell expressed in endothelin A receptor	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm0102304
	CHEMBL957	7493	99	None	-1	4	Rat	8.9	pIC50	=	8.9	Binding	In vitro for specific binding of [125I]ET1 to A10 cell expressed in endothelin A receptorIn vitro for specific binding of [125I]ET1 to A10 cell expressed in endothelin A receptor	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm0102304
	DB00559	7493	99	None	-1	4	Rat	8.9	pIC50	=	8.9	Binding	In vitro for specific binding of [125I]ET1 to A10 cell expressed in endothelin A receptorIn vitro for specific binding of [125I]ET1 to A10 cell expressed in endothelin A receptor	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm0102304
	10952199	16795	0	None	-	0	Pig	8.9	pIC50	=	8.9	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	609	9	1	8	5.3	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(F)(F)F)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm0102304
	CHEMBL115017	16795	0	None	-	0	Pig	8.9	pIC50	=	8.9	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	609	9	1	8	5.3	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(F)(F)F)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm0102304
	11477084	10382	53	None	1	2	Human	8.9	pIC50	=	8.9	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	10.1021/jm9700068
	216235	10382	53	None	1	2	Human	8.9	pIC50	=	8.9	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	10.1021/jm9700068
	3548	10382	53	None	1	2	Human	8.9	pIC50	=	8.9	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	10.1021/jm9700068
	3950	10382	53	None	1	2	Human	8.9	pIC50	=	8.9	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	10.1021/jm9700068
	CHEMBL282724	10382	53	None	1	2	Human	8.9	pIC50	=	8.9	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	10.1021/jm9700068
	DB06268	10382	53	None	1	2	Human	8.9	pIC50	=	8.9	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	10.1021/jm9700068
	11477084	10382	53	None	1	2	Human	8.9	pIC50	=	8.9	Binding	Inhibitory concentration towards Endothelin A receptor in humanInhibitory concentration towards Endothelin A receptor in human	ChEMBL	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	10.1021/jm030528p
	216235	10382	53	None	1	2	Human	8.9	pIC50	=	8.9	Binding	Inhibitory concentration towards Endothelin A receptor in humanInhibitory concentration towards Endothelin A receptor in human	ChEMBL	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	10.1021/jm030528p
	3548	10382	53	None	1	2	Human	8.9	pIC50	=	8.9	Binding	Inhibitory concentration towards Endothelin A receptor in humanInhibitory concentration towards Endothelin A receptor in human	ChEMBL	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	10.1021/jm030528p
	3950	10382	53	None	1	2	Human	8.9	pIC50	=	8.9	Binding	Inhibitory concentration towards Endothelin A receptor in humanInhibitory concentration towards Endothelin A receptor in human	ChEMBL	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	10.1021/jm030528p
	CHEMBL282724	10382	53	None	1	2	Human	8.9	pIC50	=	8.9	Binding	Inhibitory concentration towards Endothelin A receptor in humanInhibitory concentration towards Endothelin A receptor in human	ChEMBL	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	10.1021/jm030528p
	DB06268	10382	53	None	1	2	Human	8.9	pIC50	=	8.9	Binding	Inhibitory concentration towards Endothelin A receptor in humanInhibitory concentration towards Endothelin A receptor in human	ChEMBL	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	10.1021/jm030528p
	11477084	10382	53	None	1	2	Human	8.9	pIC50	=	8.9	Binding	Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor	ChEMBL	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	10.1021/jm000349x
	216235	10382	53	None	1	2	Human	8.9	pIC50	=	8.9	Binding	Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor	ChEMBL	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	10.1021/jm000349x
	3548	10382	53	None	1	2	Human	8.9	pIC50	=	8.9	Binding	Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor	ChEMBL	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	10.1021/jm000349x
	3950	10382	53	None	1	2	Human	8.9	pIC50	=	8.9	Binding	Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor	ChEMBL	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	10.1021/jm000349x
	CHEMBL282724	10382	53	None	1	2	Human	8.9	pIC50	=	8.9	Binding	Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor	ChEMBL	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	10.1021/jm000349x
	DB06268	10382	53	None	1	2	Human	8.9	pIC50	=	8.9	Binding	Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor	ChEMBL	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	10.1021/jm000349x
	42630655	25179	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer	ChEMBL	557	11	2	7	5.5	CCCCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2	10.1016/j.bmcl.2010.08.074
	CHEMBL1271586	25179	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer	ChEMBL	557	11	2	7	5.5	CCCCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2	10.1016/j.bmcl.2010.08.074
	11409462	205467	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	501	6	2	6	6.0	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(-c2ccccc2)c1	10.1021/jm030528p
	CHEMBL58058	205467	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	501	6	2	6	6.0	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(-c2ccccc2)c1	10.1021/jm030528p
	10505771	170135	0	None	-	0	Rat	8.8	pIC50	=	8.8	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	506	12	1	4	5.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm010237l
	CHEMBL419211	170135	0	None	-	0	Rat	8.8	pIC50	=	8.8	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	506	12	1	4	5.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm010237l
	11026025	209664	0	None	-	0	Rat	8.8	pIC50	=	8.8	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	412	7	1	6	4.6	CCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	CHEMBL62669	209664	0	None	-	0	Rat	8.8	pIC50	=	8.8	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	412	7	1	6	4.6	CCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	10649122	16511	0	None	-	0	Rat	8.8	pIC50	=	8.8	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	502	12	1	4	5.2	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc(F)c(F)c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	CHEMBL113400	16511	0	None	-	0	Rat	8.8	pIC50	=	8.8	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	502	12	1	4	5.2	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc(F)c(F)c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	10505771	170135	0	None	-	0	Rat	8.8	pIC50	=	8.8	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	506	12	1	4	5.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	CHEMBL419211	170135	0	None	-	0	Rat	8.8	pIC50	=	8.8	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	506	12	1	4	5.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	21041297	176386	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	510	12	2	9	3.4	CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Cl)cc1	10.1016/j.bmcl.2016.06.014
	CHEMBL4436531	176386	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	510	12	2	9	3.4	CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Cl)cc1	10.1016/j.bmcl.2016.06.014
	71453357	88457	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	707	12	1	12	5.8	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1	10.1021/jm3009103
	CHEMBL2163708	88457	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	707	12	1	12	5.8	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1	10.1021/jm3009103
	159594	7310	45	None	-1	3	Rat	8.8	pIC50	=	8.8	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1016/s0960-894x(98)00301-1
	3487	7310	45	None	-1	3	Rat	8.8	pIC50	=	8.8	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1016/s0960-894x(98)00301-1
	CHEMBL9194	7310	45	None	-1	3	Rat	8.8	pIC50	=	8.8	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1016/s0960-894x(98)00301-1
	DB06199	7310	45	None	-1	3	Rat	8.8	pIC50	=	8.8	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1016/s0960-894x(98)00301-1
	44279303	113873	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors	ChEMBL	576	11	2	7	4.3	COCCNC(=O)c1cccc(S(=O)(=O)Nc2ncc(Br)nc2OC)c1-c1ccc(CC(C)C)cc1	10.1016/S0960-894X(97)00228-X
	CHEMBL31592	113873	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors	ChEMBL	576	11	2	7	4.3	COCCNC(=O)c1cccc(S(=O)(=O)Nc2ncc(Br)nc2OC)c1-c1ccc(CC(C)C)cc1	10.1016/S0960-894X(97)00228-X
	10302092	118114	0	None	-	0	Rat	8.8	pIC50	=	8.8	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	532	12	1	7	3.7	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CCC	10.1021/jm970101g
	CHEMBL326861	118114	0	None	-	0	Rat	8.8	pIC50	=	8.8	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	532	12	1	7	3.7	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CCC	10.1021/jm970101g
	10768903	18906	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	544	11	2	6	5.3	CCCCC(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1	10.1021/jm990171i
	CHEMBL1184133	18906	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	544	11	2	6	5.3	CCCCC(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1	10.1021/jm990171i
	CHEMBL334076	18906	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	544	11	2	6	5.3	CCCCC(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1	10.1021/jm990171i
	11733231	209623	0	None	-	0	Rat	8.8	pIC50	=	8.8	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	460	6	1	6	5.2	COc1cccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)c1	10.1021/jm010382z
	CHEMBL62465	209623	0	None	-	0	Rat	8.8	pIC50	=	8.8	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	460	6	1	6	5.2	COc1cccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)c1	10.1021/jm010382z
	9872534	182802	0	None	-	0	Rat	8.8	pIC50	=	8.8	Binding	Displacement of 125I-ET1 from ETA receptor in rat A7R5 cellsDisplacement of 125I-ET1 from ETA receptor in rat A7R5 cells	ChEMBL	521	11	2	10	3.5	COc1ccccc1Oc1c(NS(=O)(=O)/C=C/c2ccccc2)nc(-c2ncccn2)nc1OCCO	10.1016/j.bmcl.2016.06.014
	CHEMBL4590018	182802	0	None	-	0	Rat	8.8	pIC50	=	8.8	Binding	Displacement of 125I-ET1 from ETA receptor in rat A7R5 cellsDisplacement of 125I-ET1 from ETA receptor in rat A7R5 cells	ChEMBL	521	11	2	10	3.5	COc1ccccc1Oc1c(NS(=O)(=O)/C=C/c2ccccc2)nc(-c2ncccn2)nc1OCCO	10.1016/j.bmcl.2016.06.014
	44439103	98726	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Displacement of [125I]ET1 from human ETA receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETA receptor expressed in CHO cells	ChEMBL	859	27	2	14	5.3	CC(=O)CC(=O)CCc1ccc(NC(=O)CCOCCOCCOCCOCC(=O)N(C)Cc2cc(-c3ncco3)ccc2-c2ccccc2S(=O)(=O)Nc2ccno2)cc1	10.1016/j.bmcl.2006.10.009
	CHEMBL241460	98726	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Displacement of [125I]ET1 from human ETA receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETA receptor expressed in CHO cells	ChEMBL	859	27	2	14	5.3	CC(=O)CC(=O)CCc1ccc(NC(=O)CCOCCOCCOCCOCC(=O)N(C)Cc2cc(-c3ncco3)ccc2-c2ccccc2S(=O)(=O)Nc2ccno2)cc1	10.1016/j.bmcl.2006.10.009
	67952994	88781	14	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	634	11	2	8	4.4	O=S(=O)(NCc1ccccc1)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1	10.1021/jm3009103
	CHEMBL2165334	88781	14	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	634	11	2	8	4.4	O=S(=O)(NCc1ccccc1)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1	10.1021/jm3009103
	19689505	65688	0	None	-	0	Pig	8.8	pIC50	=	8.8	Binding	In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.	ChEMBL	639	11	1	8	6.5	CCCc1nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c(-c2ccc(C)cc2)c(OCCOc2ncc(Br)cn2)n1	10.1016/s0960-894x(01)00682-5
	CHEMBL168904	65688	0	None	-	0	Pig	8.8	pIC50	=	8.8	Binding	In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.	ChEMBL	639	11	1	8	6.5	CCCc1nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c(-c2ccc(C)cc2)c(OCCOc2ncc(Br)cn2)n1	10.1016/s0960-894x(01)00682-5
	44334065	174601	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	429	5	1	5	4.7	COc1ccc([C@@H]2c3nc(C4CC4)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1	10.1016/s0960-894x(02)00663-7
	CHEMBL430695	174601	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	429	5	1	5	4.7	COc1ccc([C@@H]2c3nc(C4CC4)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1	10.1016/s0960-894x(02)00663-7
	10719367	105006	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	476	7	1	8	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)cc(OC)c2)cc1	10.1021/jm9606507
	CHEMBL274359	105006	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	476	7	1	8	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)cc(OC)c2)cc1	10.1021/jm9606507
	12286	7735	36	None	1348	2	Human	8.8	pIC50	=	8.8	Binding	Displacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cellsDisplacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cells	ChEMBL	577	11	3	13	2.4	Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC	10.1016/j.bmcl.2016.06.014
	6433095	7735	36	None	1348	2	Human	8.8	pIC50	=	8.8	Binding	Displacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cellsDisplacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cells	ChEMBL	577	11	3	13	2.4	Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC	10.1016/j.bmcl.2016.06.014
	CHEMBL109648	7735	36	None	1348	2	Human	8.8	pIC50	=	8.8	Binding	Displacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cellsDisplacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cells	ChEMBL	577	11	3	13	2.4	Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC	10.1016/j.bmcl.2016.06.014
	DB06677	7735	36	None	1348	2	Human	8.8	pIC50	=	8.8	Binding	Displacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cellsDisplacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cells	ChEMBL	577	11	3	13	2.4	Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC	10.1016/j.bmcl.2016.06.014
	22467237	92118	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells	ChEMBL	549	8	3	8	2.3	Cn1cc(C(C(=O)NS(=O)(=O)c2ccc(CC(=O)O)cc2)c2ccc3c(c2)OCO3)c2ccc(C(N)=O)cc21	10.1007/s00044-004-0021-y
	CHEMBL2261357	92118	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells	ChEMBL	549	8	3	8	2.3	Cn1cc(C(C(=O)NS(=O)(=O)c2ccc(CC(=O)O)cc2)c2ccc3c(c2)OCO3)c2ccc(C(N)=O)cc21	10.1007/s00044-004-0021-y
	71455063	88470	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	646	15	2	12	3.8	CCCCNS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC	10.1021/jm3009103
	CHEMBL2163720	88470	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	646	15	2	12	3.8	CCCCNS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC	10.1021/jm3009103
	21041267	88784	13	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	558	9	2	8	2.8	CNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1	10.1021/jm3009103
	CHEMBL2165337	88784	13	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	558	9	2	8	2.8	CNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1	10.1021/jm3009103
	10813261	67201	0	None	-	0	Rat	8.7	pIC50	=	8.7	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	446	8	1	6	4.4	COc1ccc(C/C(C(=O)c2ccc(OC)cc2)=C(/C(=O)O)c2ccc3c(c2)OCO3)cc1	10.1021/jm031041j
	CHEMBL175129	67201	0	None	-	0	Rat	8.7	pIC50	=	8.7	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	446	8	1	6	4.4	COc1ccc(C/C(C(=O)c2ccc(OC)cc2)=C(/C(=O)O)c2ccc3c(c2)OCO3)cc1	10.1021/jm031041j
	9955200	16104	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	446	6	1	7	3.8	COc1ccc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc1	10.1021/jm9606507
	CHEMBL11115	16104	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	446	6	1	7	3.8	COc1ccc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc1	10.1021/jm9606507
	10601668	105222	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	506	8	1	9	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)cc2OC)cc1	10.1021/jm9606507
	CHEMBL275701	105222	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	506	8	1	9	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)cc2OC)cc1	10.1021/jm9606507
	10973523	209640	0	None	-	0	Rat	8.7	pIC50	=	8.7	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	537	7	1	8	4.2	COc1ccc(C2=C(C(=O)NS(C)(=O)=O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1	10.1021/jm010382z
	CHEMBL62578	209640	0	None	-	0	Rat	8.7	pIC50	=	8.7	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	537	7	1	8	4.2	COc1ccc(C2=C(C(=O)NS(C)(=O)=O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1	10.1021/jm010382z
	11122785	209754	0	None	-	0	Rat	8.7	pIC50	=	8.7	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	426	8	1	6	4.6	COCCCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	CHEMBL63057	209754	0	None	-	0	Rat	8.7	pIC50	=	8.7	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	426	8	1	6	4.6	COCCCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	10649546	115391	0	None	-	0	Rat	8.7	pIC50	=	8.7	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	516	13	1	6	4.7	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1CCCCO1	10.1021/jm980217s
	CHEMBL320569	115391	0	None	-	0	Rat	8.7	pIC50	=	8.7	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	516	13	1	6	4.7	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1CCCCO1	10.1021/jm980217s
	CHEMBL2304015	216250	0	None	-	0	Pig	8.7	pIC50	=	8.7	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		Cc1[nH]c2ccccc2c1C[C@@H]1NC(=O)[C@@H](C2CC2)NC(=O)[C@H](C2CCCC2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC1=O	10.1021/jm9600914
	10029171	105541	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	505	6	2	7	3.0	Cc1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(C(N)=O)ccc23)cc1	10.1016/s0960-894x(01)00660-6
	CHEMBL278109	105541	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	505	6	2	7	3.0	Cc1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(C(N)=O)ccc23)cc1	10.1016/s0960-894x(01)00660-6
	11800804	168615	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor	ChEMBL	550	10	4	5	4.7	Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N(C)C2CCCCC2)nc1C(=O)O	10.1021/jm9505932
	CHEMBL414605	168615	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor	ChEMBL	550	10	4	5	4.7	Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N(C)C2CCCCC2)nc1C(=O)O	10.1021/jm9505932
	42630655	25179	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	557	11	2	7	5.5	CCCCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2	10.1016/j.bmcl.2017.04.049
	CHEMBL1271586	25179	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	557	11	2	7	5.5	CCCCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2	10.1016/j.bmcl.2017.04.049
	10504475	213731	0	None	-	0	Rat	8.7	pIC50	=	8.7	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	468	8	1	6	3.4	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(C)CC(C)C)cc1	10.1021/jm9505369
	CHEMBL9119	213731	0	None	-	0	Rat	8.7	pIC50	=	8.7	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	468	8	1	6	3.4	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(C)CC(C)C)cc1	10.1021/jm9505369
	71456863	88465	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)	ChEMBL	680	14	2	12	4.2	COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1	10.1016/j.bmcl.2016.06.014
	CHEMBL2163716	88465	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)	ChEMBL	680	14	2	12	4.2	COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1	10.1016/j.bmcl.2016.06.014
	10971938	209755	0	None	-	0	Rat	8.7	pIC50	=	8.7	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	424	7	1	5	5.6	CC(C)CCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	CHEMBL63058	209755	0	None	-	0	Rat	8.7	pIC50	=	8.7	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	424	7	1	5	5.6	CC(C)CCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	44315008	109608	0	None	-	0	Pig	8.7	pIC50	=	8.7	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	665	13	5	5	4.7	CCSCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1021/jm9600914
	CHEMBL305524	109608	0	None	-	0	Pig	8.7	pIC50	=	8.7	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	665	13	5	5	4.7	CCSCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1021/jm9600914
	71453356	88440	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	554	13	2	10	2.9	CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1Oc1cccc(OC)c1	10.1021/jm3009103
	CHEMBL2163691	88440	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	554	13	2	10	2.9	CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1Oc1cccc(OC)c1	10.1021/jm3009103
	71456863	88465	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	680	14	2	12	4.2	COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1	10.1021/jm3009103
	CHEMBL2163716	88465	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	680	14	2	12	4.2	COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1	10.1021/jm3009103
	11827768	16647	0	None	-	0	Pig	8.7	pIC50	=	8.7	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	551	11	1	10	4.6	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncccn2)c1	10.1021/jm0102304
	CHEMBL114201	16647	0	None	-	0	Pig	8.7	pIC50	=	8.7	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	551	11	1	10	4.6	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncccn2)c1	10.1021/jm0102304
	44387543	67336	0	None	-	0	Pig	8.7	pIC50	=	8.7	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	759	9	1	9	8.1	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(Cl)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1.O=C1C2=C(CCCC2)c2ccccc21	10.1021/jm0102304
	CHEMBL175931	67336	0	None	-	0	Pig	8.7	pIC50	=	8.7	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	759	9	1	9	8.1	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(Cl)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1.O=C1C2=C(CCCC2)c2ccccc21	10.1021/jm0102304
	44334129	115331	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	459	8	1	5	5.5	CCCCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(02)00663-7
	CHEMBL320208	115331	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	459	8	1	5	5.5	CCCCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(02)00663-7
	10507467	15272	0	None	-	0	Rat	8.0	pIC50	=	8	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	580	12	1	7	4.5	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)Cc1ccccc1	10.1021/jm970101g
	CHEMBL109408	15272	0	None	-	0	Rat	8.0	pIC50	=	8	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	580	12	1	7	4.5	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)Cc1ccccc1	10.1021/jm970101g
	10118046	16208	0	None	-	0	Rat	8.0	pIC50	=	8	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	504	10	1	7	2.9	CCCS(=O)(=O)N(C)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm970101g
	CHEMBL111728	16208	0	None	-	0	Rat	8.0	pIC50	=	8	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	504	10	1	7	2.9	CCCS(=O)(=O)N(C)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm970101g
	10597575	13668	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	408	5	1	6	4.2	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2CC2CCCC2)cc1	10.1021/jm9606507
	CHEMBL10843	13668	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	408	5	1	6	4.2	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2CC2CCCC2)cc1	10.1021/jm9606507
	10671928	14048	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	467	5	1	7	4.4	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2nccc3ccccc23)cc1	10.1021/jm9606507
	CHEMBL10860	14048	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	467	5	1	7	4.4	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2nccc3ccccc23)cc1	10.1021/jm9606507
	10791988	15355	0	None	-	0	Rat	8.0	pIC50	=	8	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	516	13	1	6	4.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1CCOCC1	10.1021/jm980217s
	CHEMBL109474	15355	0	None	-	0	Rat	8.0	pIC50	=	8	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	516	13	1	6	4.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1CCOCC1	10.1021/jm980217s
	10792934	170692	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	558	10	2	6	5.6	CCc1cc(CC)c(NC(=O)CN2C[C@H](c3ccc4c(c3)OCO4)[C@@H](C(=O)O)[C@@H]2c2ccc(OC)cc2)c(CC)c1	10.1021/jm990170q
	CHEMBL420729	170692	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	558	10	2	6	5.6	CCc1cc(CC)c(NC(=O)CN2C[C@H](c3ccc4c(c3)OCO4)[C@@H](C(=O)O)[C@@H]2c2ccc(OC)cc2)c(CC)c1	10.1021/jm990170q
	9939960	182354	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Displacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cellsDisplacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cells	ChEMBL	704	13	2	11	5.2	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)cc(C(=O)N2CCN(C)CC2)cc1OCCOC(=O)Nc1ccccn1	10.1016/j.bmcl.2016.06.014
	CHEMBL4579445	182354	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Displacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cellsDisplacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cells	ChEMBL	704	13	2	11	5.2	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)cc(C(=O)N2CCN(C)CC2)cc1OCCOC(=O)Nc1ccccn1	10.1016/j.bmcl.2016.06.014
	127035070	143250	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	647	11	2	7	7.3	CCCc1nc2c(C)cc(C(=O)NCc3ccccc3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	CHEMBL3735931	143250	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	647	11	2	7	7.3	CCCc1nc2c(C)cc(C(=O)NCc3ccccc3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	127036865	144202	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes	ChEMBL	584	10	3	7	5.7	CCCc1nc2c(C)cc(C(=O)NCc3ccccc3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1	10.1039/C5MD00169B
	CHEMBL3753406	144202	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes	ChEMBL	584	10	3	7	5.7	CCCc1nc2c(C)cc(C(=O)NCc3ccccc3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1	10.1039/C5MD00169B
	9875246	127087	0	None	-	0	Pig	8.0	pIC50	=	8	Binding	In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.	ChEMBL	733	15	2	12	6.0	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(SCCC(=O)O)nc1OCCOc1ncc(Br)cn1	10.1016/s0960-894x(01)00682-5
	CHEMBL352775	127087	0	None	-	0	Pig	8.0	pIC50	=	8	Binding	In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.	ChEMBL	733	15	2	12	6.0	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(SCCC(=O)O)nc1OCCOc1ncc(Br)cn1	10.1016/s0960-894x(01)00682-5
	10696210	106324	0	None	-	0	Human	8.0	pIC50	=	8	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	483	6	2	9	3.7	CC(=O)c1cc2c(cc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2	10.1021/jm9608366
	CHEMBL283535	106324	0	None	-	0	Human	8.0	pIC50	=	8	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	483	6	2	9	3.7	CC(=O)c1cc2c(cc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2	10.1021/jm9608366
	44291884	179677	0	None	-	0	Human	8.0	pIC50	=	8	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	483	6	2	9	3.7	CC(=O)c1c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)ccc2c1OCO2	10.1021/jm9700068
	CHEMBL45160	179677	0	None	-	0	Human	8.0	pIC50	=	8	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	483	6	2	9	3.7	CC(=O)c1c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)ccc2c1OCO2	10.1021/jm9700068
	10671037	138222	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells	ChEMBL	446	8	1	6	4.4	COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1	10.1021/jm9606507
	CHEMBL273660	138222	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells	ChEMBL	446	8	1	6	4.4	COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1	10.1021/jm9606507
	CHEMBL369085	138222	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells	ChEMBL	446	8	1	6	4.4	COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1	10.1021/jm9606507
	10673756	210241	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	529	9	1	8	4.3	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OCCN3CCCC3)c2)cc1	10.1021/jm980504w
	CHEMBL65939	210241	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	529	9	1	8	4.3	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OCCN3CCCC3)c2)cc1	10.1021/jm980504w
	10475644	209911	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	392	5	1	6	3.2	COc1nc(Cl)cnc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12	10.1021/jm9604585
	CHEMBL6412	209911	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	392	5	1	6	3.2	COc1nc(Cl)cnc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12	10.1021/jm9604585
	10696210	106324	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor	ChEMBL	483	6	2	9	3.7	CC(=O)c1cc2c(cc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2	10.1021/jm000349x
	CHEMBL283535	106324	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor	ChEMBL	483	6	2	9	3.7	CC(=O)c1cc2c(cc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2	10.1021/jm000349x
	71456862	88458	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	651	12	1	12	4.5	COc1ccccc1Oc1c(NS(=O)(=O)c2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1	10.1021/jm3009103
	CHEMBL2163709	88458	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	651	12	1	12	4.5	COc1ccccc1Oc1c(NS(=O)(=O)c2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1	10.1021/jm3009103
	44291583	108167	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	500	8	3	9	2.9	COc1cc(OC)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(N)=O)c1	10.1021/jm9608366
	CHEMBL297215	108167	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	500	8	3	9	2.9	COc1cc(OC)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(N)=O)c1	10.1021/jm9608366
	44278215	106334	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.	ChEMBL	491	5	1	9	4.7	O=C(O)c1c(Sc2ccc3c(c2)OCO3)c2cc3c(cc2n1Cc1ccc2c(c1)OCO2)OCO3	10.1016/0960-894X(96)00232-6
	CHEMBL283598	106334	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.	ChEMBL	491	5	1	9	4.7	O=C(O)c1c(Sc2ccc3c(c2)OCO3)c2cc3c(cc2n1Cc1ccc2c(c1)OCO2)OCO3	10.1016/0960-894X(96)00232-6
	10841576	18215	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	620	11	2	6	6.3	CCc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1CC	10.1021/jm990171i
	CHEMBL1180336	18215	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	620	11	2	6	6.3	CCc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1CC	10.1021/jm990171i
	CHEMBL122673	18215	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	620	11	2	6	6.3	CCc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1CC	10.1021/jm990171i
	CHEMBL94907	222693	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1021/jm00015a003
	CHEMBL2304010	216245	0	None	-	0	Pig	7.0	pIC50	=	7	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CSC(C)(C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc2c(Cl)[nH]c3ccccc23)NC(=O)[C@@H](C(C)C)NC1=O	10.1021/jm9600914
	10792316	175261	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	530	8	2	6	5.3	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(C)cccc2C(C)C)cc1	10.1021/jm990170q
	CHEMBL435185	175261	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	530	8	2	6	5.3	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(C)cccc2C(C)C)cc1	10.1021/jm990170q
	18738890	105923	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	548	7	1	8	4.5	COC(=O)c1ccc2c(C(C(=O)NS(=O)(=O)c3ccc(C(C)C)cc3)c3ccc4c(c3)OCO4)cn(C)c2c1	10.1016/s0960-894x(01)00660-6
	CHEMBL281121	105923	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	548	7	1	8	4.5	COC(=O)c1ccc2c(C(C(=O)NS(=O)(=O)c3ccc(C(C)C)cc3)c3ccc4c(c3)OCO4)cn(C)c2c1	10.1016/s0960-894x(01)00660-6
	23445498	213479	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	426	4	1	5	4.9	Cc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1	10.1016/S0960-894X(96)00496-9
	CHEMBL89688	213479	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	426	4	1	5	4.9	Cc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1	10.1016/S0960-894X(96)00496-9
	10265127	103611	2	None	-	0	Rat	6.0	pIC50	=	6	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	270	3	1	4	2.2	Cc1noc(NS(=O)(=O)c2ccc(F)cc2)c1C	10.1021/jm00008a013
	CHEMBL26522	103611	2	None	-	0	Rat	6.0	pIC50	=	6	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	270	3	1	4	2.2	Cc1noc(NS(=O)(=O)c2ccc(F)cc2)c1C	10.1021/jm00008a013
	CHEMBL315047	217965	0	None	-	0	Human	6.0	pIC50	=	6	Binding	Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00070a001
	44327659	116599	0	None	-	0	Human	6.0	pIC50	=	6	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL	937	26	9	8	4.6	CCC(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC)[C@@H](C)CC)C(c1ccccc1)c1ccccc1	10.1021/jm00015a003
	CHEMBL323331	116599	0	None	-	0	Human	6.0	pIC50	=	6	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL	937	26	9	8	4.6	CCC(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC)[C@@H](C)CC)C(c1ccccc1)c1ccccc1	10.1021/jm00015a003
	CHEMBL318020	217988	0	None	-	0	Human	6.0	pIC50	=	6	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1021/jm00015a003
	44316685	211827	1	None	-	0	Human	6.0	pIC50	=	6	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	266	3	1	4	2.4	Cc1ccccc1S(=O)(=O)Nc1onc(C)c1C	10.1016/0960-894X(96)00441-6
	CHEMBL77090	211827	1	None	-	0	Human	6.0	pIC50	=	6	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	266	3	1	4	2.4	Cc1ccccc1S(=O)(=O)Nc1onc(C)c1C	10.1016/0960-894X(96)00441-6
	10022291	118805	0	None	-	0	Rat	6.0	pIC50	=	6	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	374	9	1	3	5.1	O=C(O)CCC(C(=O)c1cccc(OCc2ccccc2)c1)c1ccccc1	10.1021/jm970847e
	CHEMBL328964	118805	0	None	-	0	Rat	6.0	pIC50	=	6	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	374	9	1	3	5.1	O=C(O)CCC(C(=O)c1cccc(OCc2ccccc2)c1)c1ccccc1	10.1021/jm970847e
	12060119	117168	0	None	-	0	Human	6.0	pIC50	=	6	Binding	Displacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cellsDisplacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cells	ChEMBL	441	7	2	6	3.9	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCO)cc1	10.1016/j.bmcl.2016.06.014
	CHEMBL324304	117168	0	None	-	0	Human	6.0	pIC50	=	6	Binding	Displacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cellsDisplacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cells	ChEMBL	441	7	2	6	3.9	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCO)cc1	10.1016/j.bmcl.2016.06.014
	4568158	118184	1	None	-	0	Rat	6.0	pIC50	=	6	Binding	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	ChEMBL	400	8	2	4	4.9	O=C(O)c1cc(-c2ccc(OCc3ccccc3)cc2OCc2ccccc2)[nH]n1	10.1021/jm9707131
	CHEMBL327247	118184	1	None	-	0	Rat	6.0	pIC50	=	6	Binding	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	ChEMBL	400	8	2	4	4.9	O=C(O)c1cc(-c2ccc(OCc3ccccc3)cc2OCc2ccccc2)[nH]n1	10.1021/jm9707131
	CHEMBL315047	217965	0	None	-	0	Human	6.0	pIC50	=	6	Binding	Inhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cellsInhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00095a029
	10568280	209882	0	None	-	0	Human	6.0	pIC50	=	6	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	328	4	1	5	2.5	CN(C)c1cccc2c(S(=O)(=O)Nc3cnccn3)cccc12	10.1021/jm9604585
	CHEMBL6399	209882	0	None	-	0	Human	6.0	pIC50	=	6	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	328	4	1	5	2.5	CN(C)c1cccc2c(S(=O)(=O)Nc3cnccn3)cccc12	10.1021/jm9604585
	10553319	67842	0	None	-	0	Rat	6.0	pIC50	=	6	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	496	11	5	4	3.8	CCN(CC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(C)[nH]1	10.1021/jm950592+
	CHEMBL176430	67842	0	None	-	0	Rat	6.0	pIC50	=	6	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	496	11	5	4	3.8	CCN(CC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(C)[nH]1	10.1021/jm950592+
	10006086	127840	0	None	-	0	Pig	5.0	pIC50	=	5	Binding	Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.	ChEMBL	498	9	2	5	4.6	COc1ccc(CN(C(=O)/C=C/c2ccc3c(c2)OCO3)C(Cc2c[nH]c3ccccc23)C(=O)O)cc1	10.1016/s0960-894x(01)00009-9
	CHEMBL356916	127840	0	None	-	0	Pig	5.0	pIC50	=	5	Binding	Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.	ChEMBL	498	9	2	5	4.6	COc1ccc(CN(C(=O)/C=C/c2ccc3c(c2)OCO3)C(Cc2c[nH]c3ccccc23)C(=O)O)cc1	10.1016/s0960-894x(01)00009-9
	10381122	105973	0	None	-	0	Rat	5.0	pIC50	=	5	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	317	3	2	5	2.8	Cc1noc(NS(=O)(=O)c2ccc3ccc(N)cc3c2)c1C	10.1021/jm00008a013
	CHEMBL281427	105973	0	None	-	0	Rat	5.0	pIC50	=	5	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	317	3	2	5	2.8	Cc1noc(NS(=O)(=O)c2ccc3ccc(N)cc3c2)c1C	10.1021/jm00008a013
	44327466	103226	0	None	-	0	Human	5.0	pIC50	=	5	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL	966	25	9	8	5.2	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C(C)(C)C)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	CHEMBL262229	103226	0	None	-	0	Human	5.0	pIC50	=	5	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL	966	25	9	8	5.2	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C(C)(C)C)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	18617385	211991	0	None	-	0	Human	5.0	pIC50	=	5	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	286	3	1	4	2.7	Cc1noc(NS(=O)(=O)c2ccc(Cl)cc2)c1C	10.1016/0960-894X(96)00441-6
	CHEMBL78601	211991	0	None	-	0	Human	5.0	pIC50	=	5	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	286	3	1	4	2.7	Cc1noc(NS(=O)(=O)c2ccc(Cl)cc2)c1C	10.1016/0960-894X(96)00441-6
	127029201	144036	0	None	-	0	Human	5.0	pIC50	=	5	Binding	Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes	ChEMBL	644	12	3	9	5.7	CCCc1nc2c(C)cc(C(=O)NCc3ccc(OC)c(OC)c3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1	10.1039/C5MD00169B
	CHEMBL3751994	144036	0	None	-	0	Human	5.0	pIC50	=	5	Binding	Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes	ChEMBL	644	12	3	9	5.7	CCCc1nc2c(C)cc(C(=O)NCc3ccc(OC)c(OC)c3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1	10.1039/C5MD00169B
	3080568	185624	33	None	-	0	Rat	5.0	pIC50	=	5	Binding	Displacement of endothelin-1 from ETA receptor in rat A10 cellsDisplacement of endothelin-1 from ETA receptor in rat A10 cells	ChEMBL	348	5	3	7	2.7	COC(=O)c1cc(O)cc(OC)c1Oc1cc(C)cc(O)c1C(=O)O	10.1021/np0102758
	CHEMBL469424	185624	33	None	-	0	Rat	5.0	pIC50	=	5	Binding	Displacement of endothelin-1 from ETA receptor in rat A10 cellsDisplacement of endothelin-1 from ETA receptor in rat A10 cells	ChEMBL	348	5	3	7	2.7	COC(=O)c1cc(O)cc(OC)c1Oc1cc(C)cc(O)c1C(=O)O	10.1021/np0102758
	9846065	177698	0	None	-	0	Human	5.0	pIC50	=	5	Binding	Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes	ChEMBL	439	7	2	6	3.6	O=S(=O)(Nc1ncnc(OCCO)c1-c1ccc(Cl)cc1)c1ccc(Cl)cc1	10.1016/j.bmcl.2016.06.014
	CHEMBL4455096	177698	0	None	-	0	Human	5.0	pIC50	=	5	Binding	Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes	ChEMBL	439	7	2	6	3.6	O=S(=O)(Nc1ncnc(OCCO)c1-c1ccc(Cl)cc1)c1ccc(Cl)cc1	10.1016/j.bmcl.2016.06.014
	44276947	113628	0	None	-	0	Rat	5.0	pIC50	=	5	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	430	5	1	3	5.2	COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc(Cl)c(Cl)c3)c2=O)c1	10.1016/s0960-894x(00)00232-8
	CHEMBL3144803	113628	0	None	-	0	Rat	5.0	pIC50	=	5	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	430	5	1	3	5.2	COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc(Cl)c(Cl)c3)c2=O)c1	10.1016/s0960-894x(00)00232-8
	44276907	113632	0	None	-	0	Rat	5.0	pIC50	=	5	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	376	4	1	4	3.6	O=c1c(Cc2ccc3c(c2)OCO3)c(C(F)(F)F)[nH]n1Cc1ccccc1	10.1016/s0960-894x(00)00232-8
	CHEMBL3144845	113632	0	None	-	0	Rat	5.0	pIC50	=	5	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	376	4	1	4	3.6	O=c1c(Cc2ccc3c(c2)OCO3)c(C(F)(F)F)[nH]n1Cc1ccccc1	10.1016/s0960-894x(00)00232-8
	10381122	105973	0	None	-	0	Rat	5.0	pIC50	=	5	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	317	3	2	5	2.8	Cc1noc(NS(=O)(=O)c2ccc3ccc(N)cc3c2)c1C	10.1021/jm00004a012
	CHEMBL281427	105973	0	None	-	0	Rat	5.0	pIC50	=	5	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	317	3	2	5	2.8	Cc1noc(NS(=O)(=O)c2ccc3ccc(N)cc3c2)c1C	10.1021/jm00004a012
	3765218	210200	1	None	-	0	Human	5.0	pIC50	=	5	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	419	4	1	4	4.2	Cc1nc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)ccc1Br	10.1021/jm9604585
	CHEMBL6566	210200	1	None	-	0	Human	5.0	pIC50	=	5	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	419	4	1	4	4.2	Cc1nc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)ccc1Br	10.1021/jm9604585
	44266649	104886	0	None	-	0	Human	5.0	pIC50	=	5	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	391	3	1	4	5.4	O=C(O)c1c(-c2ccc3c(c2)OCO3)c2cc(Cl)ccc2n1-c1ccccc1	10.1016/0960-894X(96)00170-9
	CHEMBL273488	104886	0	None	-	0	Human	5.0	pIC50	=	5	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	391	3	1	4	5.4	O=C(O)c1c(-c2ccc3c(c2)OCO3)c2cc(Cl)ccc2n1-c1ccccc1	10.1016/0960-894X(96)00170-9
	23445421	66704	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	454	6	1	5	5.0	Cc1ccc(CCc2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1	10.1016/S0960-894X(97)00133-9
	CHEMBL173189	66704	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	454	6	1	5	5.0	Cc1ccc(CCc2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1	10.1016/S0960-894X(97)00133-9
	10832763	175218	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	366	4	2	6	2.3	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)O)c1Br	10.1016/S0960-894X(97)00367-3
	CHEMBL434983	175218	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	366	4	2	6	2.3	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)O)c1Br	10.1016/S0960-894X(97)00367-3
	137649809	164166	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	583	10	2	7	5.9	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC4CCCC4)ccc31)OCO2	10.1016/j.bmcl.2017.04.049
	CHEMBL4078297	164166	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	583	10	2	7	5.9	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC4CCCC4)ccc31)OCO2	10.1016/j.bmcl.2017.04.049
	10527774	190467	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	455	5	2	6	4.2	Cc1cccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c1	10.1021/jm9608366
	CHEMBL48031	190467	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	455	5	2	6	4.2	Cc1cccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c1	10.1021/jm9608366
	22998456	66568	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor	ChEMBL	514	8	1	8	4.9	CCCc1cc2c(cc1OCc1sccc1S(=O)(=O)Nc1onc(C)c1Br)OCO2	10.1016/S0960-894X(97)00132-7
	CHEMBL172666	66568	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor	ChEMBL	514	8	1	8	4.9	CCCc1cc2c(cc1OCc1sccc1S(=O)(=O)Nc1onc(C)c1Br)OCO2	10.1016/S0960-894X(97)00132-7
	9874379	67220	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	653	14	2	10	5.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CC2)nc1OCCNS(=O)(=O)c1ccc(C)cc1	10.1016/s0960-894x(02)01083-1
	CHEMBL175268	67220	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	653	14	2	10	5.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CC2)nc1OCCNS(=O)(=O)c1ccc(C)cc1	10.1016/s0960-894x(02)01083-1
	10718385	213590	0	None	-	0	Rat	7.0	pIC50	=	7.0	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	450	7	1	6	2.4	C#CCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL9040	213590	0	None	-	0	Rat	7.0	pIC50	=	7.0	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	450	7	1	6	2.4	C#CCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	23445593	67009	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	440	6	1	5	4.7	Cc1ccc(CCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1	10.1016/S0960-894X(97)00133-9
	CHEMBL174086	67009	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	440	6	1	5	4.7	Cc1ccc(CCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1	10.1016/S0960-894X(97)00133-9
	10805820	210496	60	None	-	0	Human	6.0	pIC50	=	6.0	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	322	4	2	6	2.2	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)O)c1Cl	10.1016/S0960-894X(97)00367-3
	CHEMBL67664	210496	60	None	-	0	Human	6.0	pIC50	=	6.0	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	322	4	2	6	2.2	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)O)c1Cl	10.1016/S0960-894X(97)00367-3
	10812400	105155	0	None	-	0	Rat	7.0	pIC50	=	7.0	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	427	9	1	6	3.7	CCCOCCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL275306	105155	0	None	-	0	Rat	7.0	pIC50	=	7.0	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	427	9	1	6	3.7	CCCOCCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	44265853	213181	0	None	-	0	Rat	6.0	pIC50	=	6.0	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	454	4	1	6	2.7	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2C(=O)N2CCOCC2)cc1	10.1021/jm9505369
	CHEMBL8776	213181	0	None	-	0	Rat	6.0	pIC50	=	6.0	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	454	4	1	6	2.7	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2C(=O)N2CCOCC2)cc1	10.1021/jm9505369
	10854399	209779	41	None	-	0	Human	6.0	pIC50	=	6.0	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	336	4	1	7	2.3	COC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl	10.1016/S0960-894X(97)00367-3
	CHEMBL63169	209779	41	None	-	0	Human	6.0	pIC50	=	6.0	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	336	4	1	7	2.3	COC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl	10.1016/S0960-894X(97)00367-3
	10647020	68069	0	None	-	0	Rat	8.0	pIC50	=	8.0	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	446	8	1	6	4.4	COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1OC	10.1021/jm031041j
	CHEMBL176696	68069	0	None	-	0	Rat	8.0	pIC50	=	8.0	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	446	8	1	6	4.4	COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1OC	10.1021/jm031041j
	10647021	13746	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	446	6	1	7	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1OC	10.1021/jm9606507
	CHEMBL10846	13746	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	446	6	1	7	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1OC	10.1021/jm9606507
	10552548	105298	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	476	7	1	8	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OC)c2OC)cc1	10.1021/jm9606507
	CHEMBL276252	105298	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	476	7	1	8	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OC)c2OC)cc1	10.1021/jm9606507
	9934580	169709	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	474	6	1	8	3.6	COC(=O)c1ccc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc1	10.1021/jm9606507
	CHEMBL417428	169709	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	474	6	1	8	3.6	COC(=O)c1ccc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc1	10.1021/jm9606507
	127035757	143283	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	591	10	1	8	6.2	CCCCc1nn(-c2ccccc2Cl)c(=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	CHEMBL3736242	143283	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	591	10	1	8	6.2	CCCCc1nn(-c2ccccc2Cl)c(=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	76308472	92129	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells	ChEMBL	517	6	1	8	3.7	COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C#N)ccc12	10.1007/s00044-004-0021-y
	CHEMBL2261600	92129	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells	ChEMBL	517	6	1	8	3.7	COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C#N)ccc12	10.1007/s00044-004-0021-y
	44320338	113751	0	None	-	0	Rat	8.0	pIC50	=	8.0	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	490	7	2	6	5.0	O=C(O)c1ccc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)cc1	10.1016/s0960-894x(00)00513-8
	CHEMBL315087	113751	0	None	-	0	Rat	8.0	pIC50	=	8.0	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	490	7	2	6	5.0	O=C(O)c1ccc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)cc1	10.1016/s0960-894x(00)00513-8
	44385162	68155	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	533	10	2	10	3.3	C#CCOc1nc(-c2ccnc(CO)c2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	CHEMBL176963	68155	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	533	10	2	10	3.3	C#CCOc1nc(-c2ccnc(CO)c2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	10697633	67108	0	None	-	0	Rat	8.0	pIC50	=	8.0	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	536	10	5	5	4.4	Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)nc1C(=O)O	10.1021/jm950592+
	CHEMBL174448	67108	0	None	-	0	Rat	8.0	pIC50	=	8.0	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	536	10	5	5	4.4	Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)nc1C(=O)O	10.1021/jm950592+
	10697633	67108	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor	ChEMBL	536	10	5	5	4.4	Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)nc1C(=O)O	10.1021/jm9505932
	CHEMBL174448	67108	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor	ChEMBL	536	10	5	5	4.4	Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)nc1C(=O)O	10.1021/jm9505932
	10551548	134596	0	None	-	0	Rat	7.0	pIC50	=	7.0	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	450	7	1	5	5.0	COc1ccc(C(=O)/C(Cc2ccc(Cl)cc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1	10.1021/jm031041j
	CHEMBL366442	134596	0	None	-	0	Rat	7.0	pIC50	=	7.0	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	450	7	1	5	5.0	COc1ccc(C(=O)/C(Cc2ccc(Cl)cc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1	10.1021/jm031041j
	11732966	209950	0	None	-	0	Rat	7.0	pIC50	=	7.0	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	444	5	1	5	5.6	COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(C(C)C)cc32)cc1	10.1021/jm031041j
	CHEMBL64244	209950	0	None	-	0	Rat	7.0	pIC50	=	7.0	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	444	5	1	5	5.6	COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(C(C)C)cc32)cc1	10.1021/jm031041j
	CHEMBL302776	217694	0	None	-	0	Pig	7.0	pIC50	=	7.0	Binding	Binding activity against Endothelin A receptor of Porcine aortic smooth muscle membranesBinding activity against Endothelin A receptor of Porcine aortic smooth muscle membranes	ChEMBL		None	None	None		CC(C)C[C@@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00089a028
	22616262	212318	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	366	3	1	4	3.7	Cc1noc(NS(=O)(=O)c2cccc3ccccc23)c1Br	10.1016/0960-894X(96)00441-6
	CHEMBL80980	212318	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	366	3	1	4	3.7	Cc1noc(NS(=O)(=O)c2cccc3ccccc23)c1Br	10.1016/0960-894X(96)00441-6
	18617351	110886	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	384	3	1	4	3.9	Cc1noc(NS(=O)(=O)c2cc(Cl)ccc2Cl)c1Br	10.1016/0960-894X(96)00441-6
	CHEMBL309397	110886	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	384	3	1	4	3.9	Cc1noc(NS(=O)(=O)c2cc(Cl)ccc2Cl)c1Br	10.1016/0960-894X(96)00441-6
	10433234	212226	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	436	5	1	4	4.3	CCCc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1Br	10.1016/0960-894X(96)00441-6
	CHEMBL80342	212226	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	436	5	1	4	4.3	CCCc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1Br	10.1016/0960-894X(96)00441-6
	11744509	12202	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	450	5	1	6	4.5	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(Cl)cc2)cc1	10.1021/jm9606507
	CHEMBL10733	12202	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	450	5	1	6	4.5	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(Cl)cc2)cc1	10.1021/jm9606507
	11732966	209950	0	None	-	0	Rat	7.0	pIC50	=	7.0	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	444	5	1	5	5.6	COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(C(C)C)cc32)cc1	10.1021/jm010382z
	CHEMBL64244	209950	0	None	-	0	Rat	7.0	pIC50	=	7.0	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	444	5	1	5	5.6	COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(C(C)C)cc32)cc1	10.1021/jm010382z
	54587165	67083	0	None	-	0	Pig	7.0	pIC50	=	7.0	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	675	15	5	4	5.9	CCCCCC[C@@H](NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1021/jm9600914
	CHEMBL1744023	67083	0	None	-	0	Pig	7.0	pIC50	=	7.0	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	675	15	5	4	5.9	CCCCCC[C@@H](NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1021/jm9600914
	44293932	169925	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	521	10	2	8	3.9	CCOc1ccc2c(c1)[C@H](c1cccc(OC)c1OCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	CHEMBL417903	169925	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	521	10	2	8	3.9	CCOc1ccc2c(c1)[C@H](c1cccc(OC)c1OCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	15304942	171209	0	None	-	0	Rat	7.0	pIC50	=	7.0	Binding	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	ChEMBL	394	9	1	4	5.5	Cc1ccccc1C(CCC(=O)O)C(=O)c1cccc(OCc2ccsc2)c1	10.1021/jm9707131
	CHEMBL421365	171209	0	None	-	0	Rat	7.0	pIC50	=	7.0	Binding	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	ChEMBL	394	9	1	4	5.5	Cc1ccccc1C(CCC(=O)O)C(=O)c1cccc(OCc2ccsc2)c1	10.1021/jm9707131
	44213279	113625	0	None	-	0	Rat	7.0	pIC50	=	7.0	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	456	6	1	5	4.2	COc1cccc(Cn2[nH]c(C(F)(F)C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2=O)c1	10.1016/s0960-894x(00)00232-8
	CHEMBL3144737	113625	0	None	-	0	Rat	7.0	pIC50	=	7.0	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	456	6	1	5	4.2	COc1cccc(Cn2[nH]c(C(F)(F)C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2=O)c1	10.1016/s0960-894x(00)00232-8
	10554748	66848	0	None	-	0	Rat	7.0	pIC50	=	7.0	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	552	10	6	6	3.3	Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCC(O)CC2)nc1C(=O)O	10.1021/jm950592+
	CHEMBL173826	66848	0	None	-	0	Rat	7.0	pIC50	=	7.0	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	552	10	6	6	3.3	Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCC(O)CC2)nc1C(=O)O	10.1021/jm950592+
	CHEMBL335143	218325	0	None	-	0	Pig	7.0	pIC50	=	7.0	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	44382975	127111	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.	ChEMBL	596	11	4	7	3.7	CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1cn(C)c2ccccc12)C(=O)NCc1nc(C(=O)O)cs1	10.1016/0960-894X(95)00144-I
	CHEMBL352929	127111	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.	ChEMBL	596	11	4	7	3.7	CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1cn(C)c2ccccc12)C(=O)NCc1nc(C(=O)O)cs1	10.1016/0960-894X(95)00144-I
	10440821	214317	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL	918	24	9	8	4.1	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c(C)c(C)c(C)c(C)c1C)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	CHEMBL94689	214317	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL	918	24	9	8	4.1	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c(C)c(C)c(C)c(C)c1C)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	10620470	118296	0	None	-	0	Rat	6.0	pIC50	=	6.0	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	391	7	1	5	4.8	COc1cccc(/C(=C\c2cc(OCc3ccsc3)ccc2C#N)C(=O)O)c1	10.1021/jm970847e
	CHEMBL327861	118296	0	None	-	0	Rat	6.0	pIC50	=	6.0	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	391	7	1	5	4.8	COc1cccc(/C(=C\c2cc(OCc3ccsc3)ccc2C#N)C(=O)O)c1	10.1021/jm970847e
	44293915	199325	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	507	9	1	8	4.4	CCOc1ccc2c(c1)[C@H](c1cc(OC)c(OC)c(OC)c1)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	CHEMBL52110	199325	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	507	9	1	8	4.4	CCOc1ccc2c(c1)[C@H](c1cc(OC)c(OC)c(OC)c1)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	44291495	18005	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	455	6	2	9	3.6	Cc1noc(NS(=O)(=O)c2ccsc2/C(Cc2ccc3c(c2)OCO3)=N\O)c1Cl	10.1021/jm9700068
	CHEMBL1178832	18005	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	455	6	2	9	3.6	Cc1noc(NS(=O)(=O)c2ccsc2/C(Cc2ccc3c(c2)OCO3)=N\O)c1Cl	10.1021/jm9700068
	CHEMBL45351	18005	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	455	6	2	9	3.6	Cc1noc(NS(=O)(=O)c2ccsc2/C(Cc2ccc3c(c2)OCO3)=N\O)c1Cl	10.1021/jm9700068
	44266565	105010	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	417	5	1	6	4.7	COc1ccc(-c2c(C(=O)O)n(-c3ccc4c(c3)OCO4)c3ccc(OC)cc23)cc1	10.1016/0960-894X(96)00170-9
	CHEMBL274370	105010	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	417	5	1	6	4.7	COc1ccc(-c2c(C(=O)O)n(-c3ccc4c(c3)OCO4)c3ccc(OC)cc23)cc1	10.1016/0960-894X(96)00170-9
	44311225	211486	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	581	11	1	10	5.5	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCOC(=O)c1ccoc1	10.1016/S0960-894X(97)00400-9
	CHEMBL74118	211486	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	581	11	1	10	5.5	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCOC(=O)c1ccoc1	10.1016/S0960-894X(97)00400-9
	13044638	92613	22	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)	ChEMBL	206	2	1	3	2.4	COc1cccc2oc(C(=O)O)c(C)c12	10.1007/s00044-013-0542-3
	CHEMBL2296888	92613	22	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)	ChEMBL	206	2	1	3	2.4	COc1cccc2oc(C(=O)O)c(C)c12	10.1007/s00044-013-0542-3
	CHEMBL269428	217566	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)C(c1ccccc1)(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	10769177	119689	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	558	11	2	6	5.2	CCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CCOC)cc1	10.1021/jm990170q
	CHEMBL331066	119689	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	558	11	2	6	5.2	CCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CCOC)cc1	10.1021/jm990170q
	127026338	144182	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes	ChEMBL	616	11	3	7	5.9	CCCc1nc2c(C)cc(C(=O)NCCc3ccccc3F)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1	10.1039/C5MD00169B
	CHEMBL3753277	144182	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes	ChEMBL	616	11	3	7	5.9	CCCc1nc2c(C)cc(C(=O)NCCc3ccccc3F)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1	10.1039/C5MD00169B
	120533	108407	9	None	-	0	Rat	5.0	pIC50	=	5.0	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	379	3	2	5	2.0	Cc1onc(NS(=O)(=O)c2ccc(N)cc2)c1I	10.1016/s0960-894x(00)00366-8
	CHEMBL298976	108407	9	None	-	0	Rat	5.0	pIC50	=	5.0	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	379	3	2	5	2.0	Cc1onc(NS(=O)(=O)c2ccc(N)cc2)c1I	10.1016/s0960-894x(00)00366-8
	10674532	175367	0	None	-	0	Rat	5.0	pIC50	=	5.0	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	567	10	4	5	5.8	CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(C(C)C)s1	10.1021/jm950591h
	CHEMBL435894	175367	0	None	-	0	Rat	5.0	pIC50	=	5.0	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	567	10	4	5	5.8	CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(C(C)C)s1	10.1021/jm950591h
	10452089	11337	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells	ChEMBL	375	3	0	5	4.1	COC(=O)C(c1ccc2c(c1)OCO2)c1c2c(nc3ccccc13)CCCC2	10.1016/S0960-894X(96)00551-3
	CHEMBL102494	11337	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells	ChEMBL	375	3	0	5	4.1	COC(=O)C(c1ccc2c(c1)OCO2)c1c2c(nc3ccccc13)CCCC2	10.1016/S0960-894X(96)00551-3
	10095637	56741	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells	ChEMBL	457	9	1	5	5.8	CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)O)c1ccccc1	10.1016/0960-894X(95)00186-W
	CHEMBL15689	56741	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells	ChEMBL	457	9	1	5	5.8	CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)O)c1ccccc1	10.1016/0960-894X(95)00186-W
	19385674	105365	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells	ChEMBL	715	13	1	7	8.3	CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)O)c1cc(Br)c(OC)c(OC)c1Br	10.1016/0960-894X(95)00186-W
	CHEMBL276819	105365	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells	ChEMBL	715	13	1	7	8.3	CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)O)c1cc(Br)c(OC)c(OC)c1Br	10.1016/0960-894X(95)00186-W
	19385674	105365	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Inhibitory concentration against endothelin receptor type AInhibitory concentration against endothelin receptor type A	ChEMBL	715	13	1	7	8.3	CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)O)c1cc(Br)c(OC)c(OC)c1Br	10.1021/jm058225d
	CHEMBL276819	105365	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Inhibitory concentration against endothelin receptor type AInhibitory concentration against endothelin receptor type A	ChEMBL	715	13	1	7	8.3	CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)O)c1cc(Br)c(OC)c(OC)c1Br	10.1021/jm058225d
	44266538	12237	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	371	4	1	4	4.8	O=C(O)c1c(-c2ccc3c(c2)OCO3)c2ccccc2n1Cc1ccccc1	10.1016/0960-894X(96)00170-9
	CHEMBL10750	12237	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	371	4	1	4	4.8	O=C(O)c1c(-c2ccc3c(c2)OCO3)c2ccccc2n1Cc1ccccc1	10.1016/0960-894X(96)00170-9
	11798999	214364	0	None	-	0	Rat	7.0	pIC50	=	7.0	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	482	7	1	6	3.8	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(C)CC(C)(C)C)cc1	10.1021/jm9505369
	CHEMBL9495	214364	0	None	-	0	Rat	7.0	pIC50	=	7.0	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	482	7	1	6	3.8	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(C)CC(C)(C)C)cc1	10.1021/jm9505369
	71460536	88461	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	589	11	1	12	3.1	COc1ccccc1Oc1c(NS(C)(=O)=O)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1	10.1021/jm3009103
	CHEMBL2163712	88461	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	589	11	1	12	3.1	COc1ccccc1Oc1c(NS(C)(=O)=O)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1	10.1021/jm3009103
	10669120	214224	0	None	-	0	Rat	7.0	pIC50	=	7.0	Binding	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	ChEMBL	407	9	1	5	5.5	Cc1ccccc1[C@H](CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1C#N	10.1021/jm9707131
	CHEMBL94141	214224	0	None	-	0	Rat	7.0	pIC50	=	7.0	Binding	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	ChEMBL	407	9	1	5	5.5	Cc1ccccc1[C@H](CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1C#N	10.1021/jm9707131
	CHEMBL444274	220710	0	None	-	0	Mouse	6.9	pIC50	=	6.9	Binding	Inhibition of [125I]ET1 binding to Endothelin A receptor of murine 3T3 cellsInhibition of [125I]ET1 binding to Endothelin A receptor of murine 3T3 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H](NC(=O)[C@H](CCc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCN)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/S0960-894X(01)81219-1
	23445366	112960	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	482	7	1	5	6.2	Cc1cc(CCC(C)C)ccc1-c1ccsc1S(=O)(=O)Nc1onc(C)c1Br	10.1016/S0960-894X(96)00496-9
	CHEMBL313801	112960	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	482	7	1	5	6.2	Cc1cc(CCC(C)C)ccc1-c1ccsc1S(=O)(=O)Nc1onc(C)c1Br	10.1016/S0960-894X(96)00496-9
	52949197	25196	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer	ChEMBL	555	10	2	7	5.1	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC4CC4)ccc31)OCO2	10.1016/j.bmcl.2010.08.074
	CHEMBL1271746	25196	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer	ChEMBL	555	10	2	7	5.1	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC4CC4)ccc31)OCO2	10.1016/j.bmcl.2010.08.074
	10694591	15998	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	444	6	1	6	4.6	CC(C)Oc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1	10.1021/jm9606507
	CHEMBL11064	15998	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	444	6	1	6	4.6	CC(C)Oc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1	10.1021/jm9606507
	18184194	137340	0	None	-	2	Human	6.9	pIC50	=	6.9	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	712	15	2	12	4.5	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCCNS(=O)(=O)c1ccc(C)cc1	10.1016/s0960-894x(02)01083-1
	CHEMBL368107	137340	0	None	-	2	Human	6.9	pIC50	=	6.9	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	712	15	2	12	4.5	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCCNS(=O)(=O)c1ccc(C)cc1	10.1016/s0960-894x(02)01083-1
	9998577	104878	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	359	5	1	5	3.6	CCc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C	10.1021/jm00008a013
	CHEMBL27344	104878	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	359	5	1	5	3.6	CCc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C	10.1021/jm00008a013
	CHEMBL327350	218069	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cellsDisplacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)81215-4
	18184228	68127	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	604	13	2	9	4.6	CCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	CHEMBL176749	68127	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	604	13	2	9	4.6	CCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	10342643	11929	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	430	5	1	6	4.1	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1C	10.1021/jm9606507
	CHEMBL10588	11929	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	430	5	1	6	4.1	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1C	10.1021/jm9606507
	10791694	104976	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	506	8	1	9	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(OC)c(OC)c2OC)cc1	10.1021/jm9606507
	CHEMBL274175	104976	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	506	8	1	9	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(OC)c(OC)c2OC)cc1	10.1021/jm9606507
	11058202	209602	0	None	-	0	Rat	7.9	pIC50	=	7.9	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	388	4	1	5	4.4	CC(C)Oc1ccc2c(c1)C(Cl)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	CHEMBL62374	209602	0	None	-	0	Rat	7.9	pIC50	=	7.9	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	388	4	1	5	4.4	CC(C)Oc1ccc2c(c1)C(Cl)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	11799636	116041	0	None	-	0	Rat	7.9	pIC50	=	7.9	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	502	13	1	6	4.3	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1CCCO1	10.1021/jm980217s
	CHEMBL321831	116041	0	None	-	0	Rat	7.9	pIC50	=	7.9	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	502	13	1	6	4.3	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1CCCO1	10.1021/jm980217s
	10626646	23218	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	558	11	2	6	5.8	CCCc1cccc(CCC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm990170q
	CHEMBL123305	23218	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	558	11	2	6	5.8	CCCc1cccc(CCC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm990170q
	10224745	119467	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	432	5	2	6	2.4	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3ccccc32)n1	10.1016/j.bmcl.2016.06.014
	CHEMBL330425	119467	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	432	5	2	6	2.4	Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3ccccc32)n1	10.1016/j.bmcl.2016.06.014
	44459272	98015	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	491	6	2	7	2.6	Cn1cc(C(C(=O)NS(=O)(=O)c2ccccc2)c2ccc3c(c2)OCO3)c2ccc(C(N)=O)cc21	10.1016/s0960-894x(01)00660-6
	CHEMBL24015	98015	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	491	6	2	7	2.6	Cn1cc(C(C(=O)NS(=O)(=O)c2ccccc2)c2ccc3c(c2)OCO3)c2ccc(C(N)=O)cc21	10.1016/s0960-894x(01)00660-6
	22010352	124404	0	None	-	0	Rat	7.9	pIC50	=	7.9	Binding	Displacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry method	ChEMBL	404	10	1	4	5.5	CC(=O)c1ccc(OCc2ccccc2)cc1OC(CCC(=O)O)c1ccccc1	10.1016/j.bmc.2015.01.003
	CHEMBL3400984	124404	0	None	-	0	Rat	7.9	pIC50	=	7.9	Binding	Displacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry method	ChEMBL	404	10	1	4	5.5	CC(=O)c1ccc(OCc2ccccc2)cc1OC(CCC(=O)O)c1ccccc1	10.1016/j.bmc.2015.01.003
	10693270	66843	1	None	-	0	Rat	7.9	pIC50	=	7.9	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	417	7	1	6	4.4	Cc1ccccc1C(Oc1cc(OCc2ccc3c(c2)OCO3)ccc1C#N)C(=O)O	10.1021/jm990378b
	CHEMBL172144	66843	1	None	-	0	Rat	7.9	pIC50	=	7.9	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	417	7	1	6	4.4	Cc1ccccc1C(Oc1cc(OCc2ccc3c(c2)OCO3)ccc1C#N)C(=O)O	10.1021/jm990378b
	CHEMBL173792	66843	1	None	-	0	Rat	7.9	pIC50	=	7.9	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	417	7	1	6	4.4	Cc1ccccc1C(Oc1cc(OCc2ccc3c(c2)OCO3)ccc1C#N)C(=O)O	10.1021/jm990378b
	44295257	21400	0	None	-	0	Rat	7.9	pIC50	=	7.9	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	538	10	1	9	4.8	COc1cc(F)ccc1C(=O)/C(Cc1cc(OC)c(OC)c(OC)c1)=C(\C(=O)O)c1ccc2nsnc2c1	10.1016/s0960-894x(98)00301-1
	CHEMBL1205063	21400	0	None	-	0	Rat	7.9	pIC50	=	7.9	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	538	10	1	9	4.8	COc1cc(F)ccc1C(=O)/C(Cc1cc(OC)c(OC)c(OC)c1)=C(\C(=O)O)c1ccc2nsnc2c1	10.1016/s0960-894x(98)00301-1
	CHEMBL48458	21400	0	None	-	0	Rat	7.9	pIC50	=	7.9	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	538	10	1	9	4.8	COc1cc(F)ccc1C(=O)/C(Cc1cc(OC)c(OC)c(OC)c1)=C(\C(=O)O)c1ccc2nsnc2c1	10.1016/s0960-894x(98)00301-1
	9915095	108307	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	535	8	2	8	3.4	CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCC(=O)O)N(C(=O)C(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	CHEMBL298212	108307	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	535	8	2	8	3.4	CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCC(=O)O)N(C(=O)C(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	10864618	120099	0	None	-	0	Pig	7.9	pIC50	=	7.9	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	556	11	1	10	5.3	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2nccs2)c1	10.1021/jm0102304
	CHEMBL331580	120099	0	None	-	0	Pig	7.9	pIC50	=	7.9	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	556	11	1	10	5.3	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2nccs2)c1	10.1021/jm0102304
	10599879	108053	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	455	5	2	6	4.2	Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1	10.1021/jm9608366
	CHEMBL296326	108053	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	455	5	2	6	4.2	Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1	10.1021/jm9608366
	10233400	135463	0	None	-	1	Human	7.9	pIC50	=	7.9	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	661	11	2	13	3.6	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccncc1	10.1016/s0960-894x(02)01084-3
	CHEMBL366885	135463	0	None	-	1	Human	7.9	pIC50	=	7.9	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	661	11	2	13	3.6	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccncc1	10.1016/s0960-894x(02)01084-3
	10304227	136786	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	603	10	2	13	4.2	C#CCOc1nc(-c2ccnc(-c3noc(S)n3)c2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	CHEMBL367686	136786	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	603	10	2	13	4.2	C#CCOc1nc(-c2ccnc(-c3noc(S)n3)c2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	10745668	211156	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	572	10	1	9	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OCCCN3CCN(C)CC3)c2)cc1	10.1021/jm980504w
	CHEMBL71787	211156	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	572	10	1	9	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OCCCN3CCN(C)CC3)c2)cc1	10.1021/jm980504w
	CHEMBL148751	215563	0	None	-	0	Mouse	7.9	pIC50	=	7.9	Binding	Inhibition of [125I]ET1 binding to Endothelin A receptor of murine 3T3 cellsInhibition of [125I]ET1 binding to Endothelin A receptor of murine 3T3 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)CN(Cc1ccccc1)C(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@H](C)CC	10.1016/S0960-894X(01)81219-1
	CHEMBL137659	215525	0	None	-	0	Pig	7.9	pIC50	=	7.9	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC1=O	10.1021/jm00021a021
	44302513	109495	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	553	9	3	9	5.1	CCCc1c(O)c(C(C)=O)cc(C(C)=O)c1NC(=O)c1sc(C)cc1S(=O)(=O)Nc1onc(C)c1Cl	10.1021/jm030528p
	CHEMBL304860	109495	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	553	9	3	9	5.1	CCCc1c(O)c(C(C)=O)cc(C(C)=O)c1NC(=O)c1sc(C)cc1S(=O)(=O)Nc1onc(C)c1Cl	10.1021/jm030528p
	10623465	210526	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Inhibition of specific binding of [125-I] ET-1 to human Endothelin A receptorInhibition of specific binding of [125-I] ET-1 to human Endothelin A receptor	ChEMBL	450	6	1	6	3.7	CCN(C)c1cccc2c(S(=O)(=O)Nc3ncc(Br)nc3OC)cccc12	10.1021/jm9604585
	CHEMBL6785	210526	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Inhibition of specific binding of [125-I] ET-1 to human Endothelin A receptorInhibition of specific binding of [125-I] ET-1 to human Endothelin A receptor	ChEMBL	450	6	1	6	3.7	CCN(C)c1cccc2c(S(=O)(=O)Nc3ncc(Br)nc3OC)cccc12	10.1021/jm9604585
	18617303	112572	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	330	3	1	4	2.9	Cc1cccc(S(=O)(=O)Nc2onc(C)c2Br)c1	10.1016/0960-894X(96)00441-6
	CHEMBL312685	112572	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	330	3	1	4	2.9	Cc1cccc(S(=O)(=O)Nc2onc(C)c2Br)c1	10.1016/0960-894X(96)00441-6
	15453179	212260	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	392	4	1	4	4.2	Cc1noc(NS(=O)(=O)c2cccc(-c3ccccc3)c2)c1Br	10.1016/0960-894X(96)00441-6
	CHEMBL80538	212260	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	392	4	1	4	4.2	Cc1noc(NS(=O)(=O)c2cccc(-c3ccccc3)c2)c1Br	10.1016/0960-894X(96)00441-6
	44293866	108399	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	461	8	1	6	4.8	CCCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	CHEMBL298922	108399	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	461	8	1	6	4.8	CCCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	CHEMBL292901	217666	0	None	-	0	Pig	6.9	pIC50	=	6.9	Binding	Inhibition of endothelin (ET-A) binding to porcine heart membranes Inhibition of endothelin (ET-A) binding to porcine heart membranes	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/0960-894X(95)00349-X
	10627333	67157	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	595	11	4	8	4.2	COC(=O)C1(NC(=O)N[C@@H](CC(C)C)C(=O)N[C@H](Cc2cn(C)c3ccccc23)c2nc(C(=O)O)c(C)o2)CCCCC1	10.1021/jm950592+
	CHEMBL174818	67157	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	595	11	4	8	4.2	COC(=O)C1(NC(=O)N[C@@H](CC(C)C)C(=O)N[C@H](Cc2cn(C)c3ccccc23)c2nc(C(=O)O)c(C)o2)CCCCC1	10.1021/jm950592+
	CHEMBL335416	218326	0	None	-	0	Pig	6.9	pIC50	=	6.9	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC1=O	10.1021/jm00021a021
	10961510	209614	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	458	7	1	4	6.6	COc1ccc(C2=C(C(=O)O)C(c3ccc(C(C)C)cc3)Oc3ccc(OC(C)C)cc32)cc1	10.1021/jm031041j
	CHEMBL62425	209614	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	458	7	1	4	6.6	COc1ccc(C2=C(C(=O)O)C(c3ccc(C(C)C)cc3)Oc3ccc(OC(C)C)cc32)cc1	10.1021/jm031041j
	44371449	56152	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes	ChEMBL	485	7	1	7	5.2	COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2ccccc23)c(OC)c1	10.1016/s0960-894x(99)00040-2
	CHEMBL156404	56152	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes	ChEMBL	485	7	1	7	5.2	COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2ccccc23)c(OC)c1	10.1016/s0960-894x(99)00040-2
	44371460	56304	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes	ChEMBL	469	5	1	7	4.9	COc1ccccc1Cn1c(=O)c(C(=O)O)c(-c2ccc3c(c2)OCO3)c2oc3ccccc3c21	10.1016/s0960-894x(99)00040-2
	CHEMBL156539	56304	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes	ChEMBL	469	5	1	7	4.9	COc1ccccc1Cn1c(=O)c(C(=O)O)c(-c2ccc3c(c2)OCO3)c2oc3ccccc3c21	10.1016/s0960-894x(99)00040-2
	10961510	209614	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	458	7	1	4	6.6	COc1ccc(C2=C(C(=O)O)C(c3ccc(C(C)C)cc3)Oc3ccc(OC(C)C)cc32)cc1	10.1021/jm010382z
	CHEMBL62425	209614	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	458	7	1	4	6.6	COc1ccc(C2=C(C(=O)O)C(c3ccc(C(C)C)cc3)Oc3ccc(OC(C)C)cc32)cc1	10.1021/jm010382z
	11733232	209643	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	460	7	1	6	5.2	CCCOc1cccc2c1C(c1ccc(OC)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	CHEMBL62586	209643	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	460	7	1	6	5.2	CCCOc1cccc2c1C(c1ccc(OC)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	CHEMBL412460	219770	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	In vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricleIn vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricle	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)80156-6
	23445317	107322	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	456	5	1	7	4.1	Cc1cccc(OC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c1	10.1016/S0960-894X(97)00367-3
	CHEMBL291404	107322	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	456	5	1	7	4.1	Cc1cccc(OC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c1	10.1016/S0960-894X(97)00367-3
	23445507	66534	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor	ChEMBL	442	6	1	6	4.5	Cc1ccc(OCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1	10.1016/S0960-894X(97)00132-7
	CHEMBL172538	66534	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor	ChEMBL	442	6	1	6	4.5	Cc1ccc(OCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1	10.1016/S0960-894X(97)00132-7
	44298956	202459	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)	ChEMBL	489	9	1	7	4.8	CCOc1ccc2c(c1)c(-c1ccc(OC)cc1OC)c(C(=O)O)c(=O)n2Cc1ccccc1OC	10.1016/S0960-894X(97)00319-3
	CHEMBL55666	202459	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)	ChEMBL	489	9	1	7	4.8	CCOc1ccc2c(c1)c(-c1ccc(OC)cc1OC)c(C(=O)O)c(=O)n2Cc1ccccc1OC	10.1016/S0960-894X(97)00319-3
	10041979	106148	0	None	-	0	Rat	4.9	pIC50	=	4.9	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	325	6	3	6	1.6	Cc1noc(NS(=O)(=O)c2ccc(NCC(=O)O)cc2)c1C	10.1021/jm00008a013
	CHEMBL282557	106148	0	None	-	0	Rat	4.9	pIC50	=	4.9	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	325	6	3	6	1.6	Cc1noc(NS(=O)(=O)c2ccc(NCC(=O)O)cc2)c1C	10.1021/jm00008a013
	44266654	104848	0	None	-	0	Human	4.9	pIC50	=	4.9	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	387	4	1	5	4.7	COc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2-c1ccccc1	10.1016/0960-894X(96)00170-9
	CHEMBL273258	104848	0	None	-	0	Human	4.9	pIC50	=	4.9	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	387	4	1	5	4.7	COc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2-c1ccccc1	10.1016/0960-894X(96)00170-9
	44385576	138155	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	539	10	1	10	3.4	C#CCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	CHEMBL368929	138155	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	539	10	1	10	3.4	C#CCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	11799440	213755	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	496	11	1	6	4.3	CCCN(CCC)C(=O)CCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL9132	213755	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	496	11	1	6	4.3	CCCN(CCC)C(=O)CCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	52949197	25196	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	555	10	2	7	5.1	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC4CC4)ccc31)OCO2	10.1016/j.bmcl.2017.04.049
	CHEMBL1271746	25196	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	555	10	2	7	5.1	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC4CC4)ccc31)OCO2	10.1016/j.bmcl.2017.04.049
	10531506	18888	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	592	9	2	6	5.8	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)c2cc(C)ccc2C)cc1	10.1021/jm990171i
	CHEMBL1184076	18888	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	592	9	2	6	5.8	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)c2cc(C)ccc2C)cc1	10.1021/jm990171i
	CHEMBL331548	18888	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	592	9	2	6	5.8	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)c2cc(C)ccc2C)cc1	10.1021/jm990171i
	10650546	18892	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	562	7	2	6	5.2	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC2c3ccccc3-c3ccccc32)cc1	10.1021/jm990171i
	CHEMBL1184091	18892	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	562	7	2	6	5.2	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC2c3ccccc3-c3ccccc32)cc1	10.1021/jm990171i
	CHEMBL332144	18892	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	562	7	2	6	5.2	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC2c3ccccc3-c3ccccc32)cc1	10.1021/jm990171i
	10814743	186150	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	484	6	1	9	3.7	Cc1noc(NS(=O)(=O)c2ccsc2C2(Cc3ccc4c(c3)OCO4)OCCO2)c1Cl	10.1021/jm9700068
	CHEMBL47383	186150	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	484	6	1	9	3.7	Cc1noc(NS(=O)(=O)c2ccsc2C2(Cc3ccc4c(c3)OCO4)OCCO2)c1Cl	10.1021/jm9700068
	10623888	169937	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	461	8	1	6	3.4	CCCCS(=O)(=O)N1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL417971	169937	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	461	8	1	6	3.4	CCCCS(=O)(=O)N1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	10281573	66749	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	574	9	2	9	4.8	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ccncc2)nc1OCC#CCO	10.1016/s0960-894x(02)01084-3
	CHEMBL173358	66749	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	574	9	2	9	4.8	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ccncc2)nc1OCC#CCO	10.1016/s0960-894x(02)01084-3
	44385586	68436	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	531	10	1	9	4.7	C#CCOc1nc(-c2ccncc2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	CHEMBL177143	68436	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	531	10	1	9	4.7	C#CCOc1nc(-c2ccncc2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	10645066	103969	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	406	4	1	5	3.3	CN(C)c1cccc2c(S(=O)(=O)Nc3cnc(Br)cn3)cccc12	10.1021/jm9604585
	CHEMBL268339	103969	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	406	4	1	5	3.3	CN(C)c1cccc2c(S(=O)(=O)Nc3cnc(Br)cn3)cccc12	10.1021/jm9604585
	11792960	168694	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	361	4	1	4	3.8	CN(C)c1cccc2c(S(=O)(=O)Nc3ccc(Cl)nc3)cccc12	10.1021/jm9604585
	CHEMBL415292	168694	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	361	4	1	4	3.8	CN(C)c1cccc2c(S(=O)(=O)Nc3ccc(Cl)nc3)cccc12	10.1021/jm9604585
	10593411	210226	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	342	4	1	5	2.8	Cc1cnc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)cn1	10.1021/jm9604585
	CHEMBL6583	210226	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	342	4	1	5	2.8	Cc1cnc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)cn1	10.1021/jm9604585
	127029202	144106	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes	ChEMBL	598	11	3	7	5.8	CCCc1nc2c(C)cc(C(=O)NCCc3ccccc3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1	10.1039/C5MD00169B
	CHEMBL3752680	144106	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes	ChEMBL	598	11	3	7	5.8	CCCc1nc2c(C)cc(C(=O)NCCc3ccccc3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1	10.1039/C5MD00169B
	10122495	37644	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	665	12	1	10	6.4	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCC#CCOCc1ccccc1	10.1016/s0960-894x(02)01084-3
	CHEMBL139734	37644	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	665	12	1	10	6.4	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCC#CCOCc1ccccc1	10.1016/s0960-894x(02)01084-3
	44384177	127071	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor	ChEMBL	506	6	1	8	4.6	Cc1noc(NS(=O)(=O)c2ccsc2COc2cc3c(cc2Cl)OCO3)c1Br	10.1016/S0960-894X(97)00132-7
	CHEMBL352657	127071	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor	ChEMBL	506	6	1	8	4.6	Cc1noc(NS(=O)(=O)c2ccsc2COc2cc3c(cc2Cl)OCO3)c1Br	10.1016/S0960-894X(97)00132-7
	10550033	108144	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	419	5	2	9	2.9	Cc1nnc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)s1	10.1021/jm9608366
	CHEMBL297048	108144	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	419	5	2	9	2.9	Cc1nnc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)s1	10.1021/jm9608366
	10626521	66849	0	None	-	0	Rat	4.9	pIC50	=	4.9	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	551	11	4	6	5.1	CCn1cc(C[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)c2nc(C(=O)O)c(C)o2)c2ccccc21	10.1021/jm950592+
	CHEMBL173833	66849	0	None	-	0	Rat	4.9	pIC50	=	4.9	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	551	11	4	6	5.1	CCn1cc(C[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)c2nc(C(=O)O)c(C)o2)c2ccccc21	10.1021/jm950592+
	CHEMBL94983	222695	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCN)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	10671036	13429	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	446	6	1	7	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)c(OC)c1	10.1021/jm9606507
	CHEMBL10834	13429	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	446	6	1	7	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)c(OC)c1	10.1021/jm9606507
	9932004	104953	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	422	5	1	6	4.6	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2CC2CCCCC2)cc1	10.1021/jm9606507
	CHEMBL273948	104953	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	422	5	1	6	4.6	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2CC2CCCCC2)cc1	10.1021/jm9606507
	10816110	115343	0	None	-	0	Rat	7.9	pIC50	=	7.9	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	532	13	1	7	4.2	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1OC(C)C(C)O1	10.1021/jm980217s
	CHEMBL320254	115343	0	None	-	0	Rat	7.9	pIC50	=	7.9	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	532	13	1	7	4.2	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1OC(C)C(C)O1	10.1021/jm980217s
	44314619	211465	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranesBinding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranes	ChEMBL	631	12	5	4	4.5	CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O	10.1021/jm9600914
	CHEMBL73925	211465	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranesBinding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranes	ChEMBL	631	12	5	4	4.5	CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O	10.1021/jm9600914
	10209324	21262	0	None	-	1	Human	7.9	pIC50	=	7.9	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	546	8	1	7	6.2	CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(C)c1)C(=O)CCCC2	10.1039/C4MD00499J
	CHEMBL12013	21262	0	None	-	1	Human	7.9	pIC50	=	7.9	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	546	8	1	7	6.2	CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(C)c1)C(=O)CCCC2	10.1039/C4MD00499J
	10740439	179527	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	412	5	2	7	3.5	Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)nc1	10.1021/jm9608366
	CHEMBL45087	179527	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	412	5	2	7	3.5	Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)nc1	10.1021/jm9608366
	135415889	66043	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	587	10	2	13	3.6	C#CCOc1nc(-c2ccnc(-c3noc(O)n3)c2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	CHEMBL170401	66043	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	587	10	2	13	3.6	C#CCOc1nc(-c2ccnc(-c3noc(O)n3)c2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	10281943	66838	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	589	10	1	10	4.9	COCC#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	CHEMBL173743	66838	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	589	10	1	10	4.9	COCC#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	10212088	103471	0	None	-	1	Human	7.9	pIC50	=	7.9	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	688	12	2	12	5.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccccc1	10.1016/s0960-894x(02)01084-3
	CHEMBL264035	103471	0	None	-	1	Human	7.9	pIC50	=	7.9	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	688	12	2	12	5.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccccc1	10.1016/s0960-894x(02)01084-3
	CHEMBL2370830	216708	0	None	-	0	Pig	7.9	pIC50	=	7.9	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	42630531	25260	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer	ChEMBL	543	9	2	7	5.1	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OC(C)C)ccc31)OCO2	10.1016/j.bmcl.2010.08.074
	CHEMBL1272299	25260	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer	ChEMBL	543	9	2	7	5.1	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OC(C)C)ccc31)OCO2	10.1016/j.bmcl.2010.08.074
	10768904	18902	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	544	10	2	6	5.2	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(CC(C)C)c2ccccc2)cc1	10.1021/jm990171i
	CHEMBL1184117	18902	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	544	10	2	6	5.2	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(CC(C)C)c2ccccc2)cc1	10.1021/jm990171i
	CHEMBL333034	18902	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	544	10	2	6	5.2	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(CC(C)C)c2ccccc2)cc1	10.1021/jm990171i
	10385400	102982	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	385	4	1	5	3.4	Cc1noc(NS(=O)(=O)c2cccc3c(N4CCCC4=O)cccc23)c1C	10.1021/jm00008a013
	CHEMBL26079	102982	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	385	4	1	5	3.4	Cc1noc(NS(=O)(=O)c2cccc3c(N4CCCC4=O)cccc23)c1C	10.1021/jm00008a013
	10426828	104921	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	331	4	2	5	3.3	CNc1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12	10.1021/jm00008a013
	CHEMBL27370	104921	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	331	4	2	5	3.3	CNc1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12	10.1021/jm00008a013
	10361993	106342	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	373	5	1	5	4.1	Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C(C)C)cccc23)c1C	10.1021/jm00008a013
	CHEMBL283652	106342	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	373	5	1	5	4.1	Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C(C)C)cccc23)c1C	10.1021/jm00008a013
	11103224	209432	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	510	14	1	6	7.3	CCCCCCCCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	CHEMBL61406	209432	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	510	14	1	6	7.3	CCCCCCCCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	11826847	209698	1	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	474	8	1	6	5.6	CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccccc1OC)O2	10.1021/jm010382z
	CHEMBL62814	209698	1	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	474	8	1	6	5.6	CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccccc1OC)O2	10.1021/jm010382z
	10837347	15641	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	452	8	1	5	3.3	CCCN(C)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	CHEMBL109736	15641	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	452	8	1	5	3.3	CCCN(C)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	10298764	16626	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	468	8	1	6	3.2	CCCN(C)C(=O)CN1C[C@H](c2ccc3c(c2)OCCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	CHEMBL114084	16626	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	468	8	1	6	3.2	CCCN(C)C(=O)CN1C[C@H](c2ccc3c(c2)OCCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	CHEMBL317064	217976	15	None	-	1	Human	6.9	pIC50	=	6.9	Binding	Inhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cellsInhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00095a029
	44266552	11285	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	473	7	1	7	5.3	CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2c(c1)OCO2	10.1016/0960-894X(96)00170-9
	CHEMBL10218	11285	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	473	7	1	7	5.3	CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2c(c1)OCO2	10.1016/0960-894X(96)00170-9
	CHEMBL337567	218377	0	None	-	0	Pig	6.9	pIC50	=	6.9	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CSCC[C@H]1NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](C(C)C)NC1=O	10.1021/jm00021a021
	CHEMBL150719	215570	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	The inhibitory constant was evaluated against Endothelin A receptor in rabbit renal artery tissueThe inhibitory constant was evaluated against Endothelin A receptor in rabbit renal artery tissue	ChEMBL		None	None	None		CC[C@@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@H](C)CC	10.1016/S0960-894X(01)81219-1
	44371421	58209	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes	ChEMBL	459	5	1	5	5.8	COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3Cl)c3c2oc2ccccc23)cc1	10.1016/s0960-894x(99)00040-2
	CHEMBL158204	58209	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes	ChEMBL	459	5	1	5	5.8	COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3Cl)c3c2oc2ccccc23)cc1	10.1016/s0960-894x(99)00040-2
	10067008	104576	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	359	4	2	5	3.2	CC(=O)Nc1ccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc2c1	10.1021/jm00008a013
	CHEMBL27187	104576	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	359	4	2	5	3.2	CC(=O)Nc1ccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc2c1	10.1021/jm00008a013
	10423091	106747	3	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	267	3	2	5	1.7	Cc1noc(NS(=O)(=O)c2cccc(N)c2)c1C	10.1021/jm00008a013
	CHEMBL286521	106747	3	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	267	3	2	5	1.7	Cc1noc(NS(=O)(=O)c2cccc(N)c2)c1C	10.1021/jm00008a013
	10552007	13095	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	462	8	1	7	4.1	COc1ccc(C2(O)OC(=O)C(c3cc(OC)c(OC)c(OC)c3)=C2Cc2ccccc2)cc1	10.1021/jm9606507
	CHEMBL10819	13095	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	462	8	1	7	4.1	COc1ccc(C2(O)OC(=O)C(c3cc(OC)c(OC)c(OC)c3)=C2Cc2ccccc2)cc1	10.1021/jm9606507
	10961720	210263	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	472	6	1	5	6.3	CC(C)Oc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc(C(C)C)cc1)O2	10.1021/jm010382z
	CHEMBL66094	210263	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	472	6	1	5	6.3	CC(C)Oc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc(C(C)C)cc1)O2	10.1021/jm010382z
	10577405	16424	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	502	14	1	5	5.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1C(C)(C)CCCC	10.1021/jm980217s
	CHEMBL112777	16424	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	502	14	1	5	5.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1C(C)(C)CCCC	10.1021/jm980217s
	10573912	118399	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	415	7	1	5	5.5	O=C(O)/C(=C/c1cc(OCc2ccsc2)ccc1[N+](=O)[O-])c1ccccc1Cl	10.1021/jm970847e
	CHEMBL328444	118399	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	415	7	1	5	5.5	O=C(O)/C(=C/c1cc(OCc2ccsc2)ccc1[N+](=O)[O-])c1ccccc1Cl	10.1021/jm970847e
	10524954	213839	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	399	6	1	5	4.5	N#Cc1ccc(OCc2ccc3c(c2)OCO3)cc1/C=C(/C(=O)O)c1ccccc1	10.1021/jm970847e
	CHEMBL91741	213839	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	399	6	1	5	4.5	N#Cc1ccc(OCc2ccc3c(c2)OCO3)cc1/C=C(/C(=O)O)c1ccccc1	10.1021/jm970847e
	44298343	108570	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	485	9	1	7	5.8	COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCC#N)c1	10.1016/s0960-894x(00)00366-8
	CHEMBL300066	108570	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	485	9	1	7	5.8	COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCC#N)c1	10.1016/s0960-894x(00)00366-8
	44298279	201730	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	502	10	1	7	5.8	COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCC(C)=O)c1	10.1016/s0960-894x(00)00366-8
	CHEMBL54274	201730	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	502	10	1	7	5.8	COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCC(C)=O)c1	10.1016/s0960-894x(00)00366-8
	155560344	183282	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of [125I]ET-1 from ET-A receptor in human SK-N-MC cells incubated for 4 hrs by gamma counting methodDisplacement of [125I]ET-1 from ET-A receptor in human SK-N-MC cells incubated for 4 hrs by gamma counting method	ChEMBL	641	12	4	7	4.8	CCCC[C@H](NC(=O)[C@@H](Cc1cn(C(=O)OC)c2ccccc12)NC(=O)[C@@H](CC(C)(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1021/acs.jmedchem.5b01781
	CHEMBL4568795	183282	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of [125I]ET-1 from ET-A receptor in human SK-N-MC cells incubated for 4 hrs by gamma counting methodDisplacement of [125I]ET-1 from ET-A receptor in human SK-N-MC cells incubated for 4 hrs by gamma counting method	ChEMBL	641	12	4	7	4.8	CCCC[C@H](NC(=O)[C@@H](Cc1cn(C(=O)OC)c2ccccc12)NC(=O)[C@@H](CC(C)(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1021/acs.jmedchem.5b01781
	CHEMBL4596821	183282	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of [125I]ET-1 from ET-A receptor in human SK-N-MC cells incubated for 4 hrs by gamma counting methodDisplacement of [125I]ET-1 from ET-A receptor in human SK-N-MC cells incubated for 4 hrs by gamma counting method	ChEMBL	641	12	4	7	4.8	CCCC[C@H](NC(=O)[C@@H](Cc1cn(C(=O)OC)c2ccccc12)NC(=O)[C@@H](CC(C)(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1021/acs.jmedchem.5b01781
	155535325	178788	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes	ChEMBL	549	10	2	8	5.4	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)cc(-c2ncccn2)cc1OCCO	10.1016/j.bmcl.2016.06.014
	CHEMBL4471434	178788	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes	ChEMBL	549	10	2	8	5.4	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)cc(-c2ncccn2)cc1OCCO	10.1016/j.bmcl.2016.06.014
	44276946	113623	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	440	5	1	5	4.2	COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3cc(Cl)c4c(c3)OCO4)c2=O)c1	10.1016/s0960-894x(00)00232-8
	CHEMBL3144735	113623	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	440	5	1	5	4.2	COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3cc(Cl)c4c(c3)OCO4)c2=O)c1	10.1016/s0960-894x(00)00232-8
	44309897	211410	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor	ChEMBL	469	5	1	7	4.9	COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccc4c(c3)OCO4)c3c2oc2ccccc23)cc1	10.1016/s0960-894x(97)10151-2
	CHEMBL73506	211410	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor	ChEMBL	469	5	1	7	4.9	COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccc4c(c3)OCO4)c3c2oc2ccccc23)cc1	10.1016/s0960-894x(97)10151-2
	44298988	107495	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)	ChEMBL	459	8	1	6	4.8	CCOc1ccc2c(c1)c(-c1ccc(OC)cc1)c(C(=O)O)c(=O)n2Cc1ccccc1OC	10.1016/S0960-894X(97)00319-3
	CHEMBL292580	107495	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)	ChEMBL	459	8	1	6	4.8	CCOc1ccc2c(c1)c(-c1ccc(OC)cc1)c(C(=O)O)c(=O)n2Cc1ccccc1OC	10.1016/S0960-894X(97)00319-3
	10067008	104576	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	359	4	2	5	3.2	CC(=O)Nc1ccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc2c1	10.1021/jm00004a012
	CHEMBL27187	104576	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	359	4	2	5	3.2	CC(=O)Nc1ccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc2c1	10.1021/jm00004a012
	10423091	106747	3	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	267	3	2	5	1.7	Cc1noc(NS(=O)(=O)c2cccc(N)c2)c1C	10.1021/jm00004a012
	CHEMBL286521	106747	3	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	267	3	2	5	1.7	Cc1noc(NS(=O)(=O)c2cccc(N)c2)c1C	10.1021/jm00004a012
	44266595	11165	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	507	6	1	7	6.0	O=C(O)c1c(-c2ccc3c(c2)OCO3)c2cc(OCc3ccccc3)ccc2n1-c1ccc2c(c1)OCO2	10.1016/0960-894X(96)00170-9
	CHEMBL10136	11165	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	507	6	1	7	6.0	O=C(O)c1c(-c2ccc3c(c2)OCO3)c2cc(OCc3ccccc3)ccc2n1-c1ccc2c(c1)OCO2	10.1016/0960-894X(96)00170-9
	10337668	108914	0	None	-	0	Human	4.9	pIC50	=	4.9	Binding	Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells	ChEMBL	346	4	2	5	2.9	Cc1noc(NS(=O)(=O)c2cccc3c(C(=O)O)cccc23)c1C	10.1021/jm00029a001
	CHEMBL30246	108914	0	None	-	0	Human	4.9	pIC50	=	4.9	Binding	Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells	ChEMBL	346	4	2	5	2.9	Cc1noc(NS(=O)(=O)c2cccc3c(C(=O)O)cccc23)c1C	10.1021/jm00029a001
	10337668	108914	0	None	-	0	Rat	4.9	pIC50	=	4.9	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	346	4	2	5	2.9	Cc1noc(NS(=O)(=O)c2cccc3c(C(=O)O)cccc23)c1C	10.1021/jm00008a013
	CHEMBL30246	108914	0	None	-	0	Rat	4.9	pIC50	=	4.9	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	346	4	2	5	2.9	Cc1noc(NS(=O)(=O)c2cccc3c(C(=O)O)cccc23)c1C	10.1021/jm00008a013
	160743	211269	23	None	-	0	Rat	4.9	pIC50	=	4.9	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	309	4	2	5	2.1	CC(=O)Nc1ccc(S(=O)(=O)Nc2onc(C)c2C)cc1	10.1021/jm00008a013
	CHEMBL725	211269	23	None	-	0	Rat	4.9	pIC50	=	4.9	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	309	4	2	5	2.1	CC(=O)Nc1ccc(S(=O)(=O)Nc2onc(C)c2C)cc1	10.1021/jm00008a013
	18617314	212011	0	None	-	0	Human	4.9	pIC50	=	4.9	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	334	3	1	4	2.7	Cc1noc(NS(=O)(=O)c2ccc(F)cc2)c1Br	10.1016/0960-894X(96)00441-6
	CHEMBL78734	212011	0	None	-	0	Human	4.9	pIC50	=	4.9	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	334	3	1	4	2.7	Cc1noc(NS(=O)(=O)c2ccc(F)cc2)c1Br	10.1016/0960-894X(96)00441-6
	CHEMBL38071	219051	0	None	-	0	Rat	4.9	pIC50	=	4.9	Binding	Compound was evaluated for the binding affinity to endothelin receptor in the rat heart ventricle.Compound was evaluated for the binding affinity to endothelin receptor in the rat heart ventricle.	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O)C(=O)N[C@@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00087a001
	44213959	177147	0	None	-	0	Human	4.9	pIC50	=	4.9	Binding	Displacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cellsDisplacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cells	ChEMBL	592	11	3	9	5.0	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C(=O)Nc2ccccc2)nc1OCCO	10.1016/j.bmcl.2016.06.014
	CHEMBL4447655	177147	0	None	-	0	Human	4.9	pIC50	=	4.9	Binding	Displacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cellsDisplacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cells	ChEMBL	592	11	3	9	5.0	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C(=O)Nc2ccccc2)nc1OCCO	10.1016/j.bmcl.2016.06.014
	127026027	144051	0	None	-	0	Human	4.9	pIC50	=	4.9	Binding	Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes	ChEMBL	628	12	3	8	5.8	CCCc1nc2c(C)cc(C(=O)NCCc3ccc(OC)cc3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1	10.1039/C5MD00169B
	CHEMBL3752145	144051	0	None	-	0	Human	4.9	pIC50	=	4.9	Binding	Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes	ChEMBL	628	12	3	8	5.8	CCCc1nc2c(C)cc(C(=O)NCCc3ccc(OC)cc3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1	10.1039/C5MD00169B
	CHEMBL1791280	215699	0	None	-	0	Human	4.9	pIC50	=	4.9	Binding	Inhibition of [125I]endothelin-1 [ET-1] binding to endothelin A receptor (ETA) of rabbit renal artery vascular smooth muscle cellsInhibition of [125I]endothelin-1 [ET-1] binding to endothelin A receptor (ETA) of rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(95)00152-J
	10816667	18216	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	558	9	2	6	5.6	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(CC(C)(C)C)c2ccccc2)cc1	10.1021/jm990171i
	CHEMBL1180341	18216	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	558	9	2	6	5.6	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(CC(C)(C)C)c2ccccc2)cc1	10.1021/jm990171i
	CHEMBL122933	18216	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	558	9	2	6	5.6	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(CC(C)(C)C)c2ccccc2)cc1	10.1021/jm990171i
	9853680	105424	0	None	-	1	Human	5.9	pIC50	=	5.9	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	771	17	2	14	5.7	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2cc(OC)c(OC)c(OC)c2)nc1OCCNS(=O)(=O)c1cccs1	10.1016/s0960-894x(02)01083-1
	CHEMBL277275	105424	0	None	-	1	Human	5.9	pIC50	=	5.9	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	771	17	2	14	5.7	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2cc(OC)c(OC)c(OC)c2)nc1OCCNS(=O)(=O)c1cccs1	10.1016/s0960-894x(02)01083-1
	10576378	107900	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	471	6	2	7	3.9	COc1ccccc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Br	10.1021/jm9608366
	CHEMBL295207	107900	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	471	6	2	7	3.9	COc1ccccc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Br	10.1021/jm9608366
	CHEMBL170229	215621	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)[C@@H](Cc1cn(C)c2ccccc12)NC(=O)[C@H](CC(C)C)NC(=O)N1CCCCCC1)C(=O)O	10.1016/0960-894X(95)00144-I
	23445219	119252	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	428	5	1	6	4.3	COc1cccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c1	10.1016/S0960-894X(96)00496-9
	CHEMBL329861	119252	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	428	5	1	6	4.3	COc1cccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c1	10.1016/S0960-894X(96)00496-9
	44386163	67154	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	577	14	2	10	3.4	CCCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	CHEMBL174781	67154	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	577	14	2	10	3.4	CCCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	23445537	67919	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor	ChEMBL	514	8	1	8	4.9	CCCc1cc2c(cc1OCc1ccsc1S(=O)(=O)Nc1onc(C)c1Br)OCO2	10.1016/S0960-894X(97)00132-7
	CHEMBL176538	67919	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor	ChEMBL	514	8	1	8	4.9	CCCc1cc2c(cc1OCc1ccsc1S(=O)(=O)Nc1onc(C)c1Br)OCO2	10.1016/S0960-894X(97)00132-7
	10766067	16510	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	452	8	1	5	3.3	CCCN(C)C(=O)CN1C[C@H](c2ccc3c(c2)OCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	CHEMBL113379	16510	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	452	8	1	5	3.3	CCCN(C)C(=O)CN1C[C@H](c2ccc3c(c2)OCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	127035069	143177	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	663	11	2	8	7.7	CCCc1nc2c(C)cc(C(=O)Nc3ccccc3OC)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	CHEMBL3735300	143177	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	663	11	2	8	7.7	CCCc1nc2c(C)cc(C(=O)Nc3ccccc3OC)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	10792785	173502	0	None	-	0	Rat	4.9	pIC50	=	4.9	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	551	10	3	6	5.0	CCOC(=O)c1nc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)oc1C	10.1021/jm950592+
	CHEMBL428298	173502	0	None	-	0	Rat	4.9	pIC50	=	4.9	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	551	10	3	6	5.0	CCOC(=O)c1nc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)oc1C	10.1021/jm950592+
	9831527	136260	0	None	-	1	Human	5.9	pIC50	=	5.9	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	698	14	2	12	4.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCNS(=O)(=O)c1ccc(C)cc1	10.1016/s0960-894x(02)01083-1
	CHEMBL367274	136260	0	None	-	1	Human	5.9	pIC50	=	5.9	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	698	14	2	12	4.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCNS(=O)(=O)c1ccc(C)cc1	10.1016/s0960-894x(02)01083-1
	10189776	66831	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	651	11	1	10	6.3	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCC#CCOc1ccccc1	10.1016/s0960-894x(02)01084-3
	CHEMBL173689	66831	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	651	11	1	10	6.3	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCC#CCOc1ccccc1	10.1016/s0960-894x(02)01084-3
	10743478	116045	0	None	-	0	Rat	7.9	pIC50	=	7.9	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	484	12	1	4	5.1	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc(F)cc2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm031041j
	CHEMBL321852	116045	0	None	-	0	Rat	7.9	pIC50	=	7.9	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	484	12	1	4	5.1	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc(F)cc2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm031041j
	10504389	137452	0	None	-	0	Rat	7.9	pIC50	=	7.9	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	466	7	1	5	5.5	COc1ccc(C(=O)/C(Cc2cccc3ccccc23)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1	10.1021/jm031041j
	CHEMBL368270	137452	0	None	-	0	Rat	7.9	pIC50	=	7.9	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	466	7	1	5	5.5	COc1ccc(C(=O)/C(Cc2cccc3ccccc23)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1	10.1021/jm031041j
	10505209	16089	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	490	6	1	9	3.6	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c3c(c2)OCO3)cc1	10.1021/jm9606507
	CHEMBL11106	16089	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	490	6	1	9	3.6	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c3c(c2)OCO3)cc1	10.1021/jm9606507
	10742841	104124	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	466	5	1	6	5.0	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc3ccccc3c2)cc1	10.1021/jm9606507
	CHEMBL269453	104124	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	466	5	1	6	5.0	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc3ccccc3c2)cc1	10.1021/jm9606507
	44314645	179451	0	None	-	0	Pig	7.9	pIC50	=	7.9	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	601	13	5	4	4.7	CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(CC1CC1)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1021/jm9600914
	CHEMBL449962	179451	0	None	-	0	Pig	7.9	pIC50	=	7.9	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	601	13	5	4	4.7	CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(CC1CC1)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1021/jm9600914
	10743478	116045	0	None	-	0	Rat	7.9	pIC50	=	7.9	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	484	12	1	4	5.1	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc(F)cc2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	CHEMBL321852	116045	0	None	-	0	Rat	7.9	pIC50	=	7.9	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	484	12	1	4	5.1	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc(F)cc2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	10166561	16836	0	None	-	1	Human	7.9	pIC50	=	7.9	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	562	9	2	8	5.4	CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(CO)c1)C(=O)CCCC2	10.1039/C4MD00499J
	CHEMBL11528	16836	0	None	-	1	Human	7.9	pIC50	=	7.9	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	562	9	2	8	5.4	CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(CO)c1)C(=O)CCCC2	10.1039/C4MD00499J
	44214320	92125	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells	ChEMBL	510	6	1	7	4.0	COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(F)ccc12	10.1007/s00044-004-0021-y
	CHEMBL2261364	92125	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells	ChEMBL	510	6	1	7	4.0	COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(F)ccc12	10.1007/s00044-004-0021-y
	10240093	88462	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	603	12	1	12	3.5	CCS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC	10.1021/jm3009103
	CHEMBL2163713	88462	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	603	12	1	12	3.5	CCS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC	10.1021/jm3009103
	71458721	88476	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	642	14	2	10	4.6	COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(C2CC2)nc1OCCOc1ncc(Br)cn1	10.1021/jm3009103
	CHEMBL2163726	88476	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	642	14	2	10	4.6	COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(C2CC2)nc1OCCOc1ncc(Br)cn1	10.1021/jm3009103
	10812894	127054	0	None	-	0	Rat	7.9	pIC50	=	7.9	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	437	7	1	6	4.7	N#Cc1ccc(OCc2ccc3c(c2)OCO3)cc1OC(C(=O)O)c1ccccc1Cl	10.1021/jm990378b
	CHEMBL352536	127054	0	None	-	0	Rat	7.9	pIC50	=	7.9	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	437	7	1	6	4.7	N#Cc1ccc(OCc2ccc3c(c2)OCO3)cc1OC(C(=O)O)c1ccccc1Cl	10.1021/jm990378b
	17869371	21561	0	None	-	0	Rat	7.9	pIC50	=	7.9	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	478	8	1	7	4.8	COc1ccc(C(=O)/C(Cc2ccc(OC)c(F)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1	10.1016/s0960-894x(98)00301-1
	CHEMBL1206716	21561	0	None	-	0	Rat	7.9	pIC50	=	7.9	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	478	8	1	7	4.8	COc1ccc(C(=O)/C(Cc2ccc(OC)c(F)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1	10.1016/s0960-894x(98)00301-1
	CHEMBL299521	21561	0	None	-	0	Rat	7.9	pIC50	=	7.9	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	478	8	1	7	4.8	COc1ccc(C(=O)/C(Cc2ccc(OC)c(F)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1	10.1016/s0960-894x(98)00301-1
	44293417	194115	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	563	11	2	8	4.9	CCOc1ccc2c(c1)[C@H](c1ccc(OC)cc1OCC(C)(C)C(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	CHEMBL49312	194115	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	563	11	2	8	4.9	CCOc1ccc2c(c1)[C@H](c1ccc(OC)cc1OCC(C)(C)C(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	443289	7498	47	None	-2	3	Rat	7.9	pIC50	=	7.9	Binding	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	ChEMBL		None	None	None		None	10.1021/jm9707131
	997	7498	47	None	-2	3	Rat	7.9	pIC50	=	7.9	Binding	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	ChEMBL		None	None	None		None	10.1021/jm9707131
	CHEMBL314691	7498	47	None	-2	3	Rat	7.9	pIC50	=	7.9	Binding	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	ChEMBL		None	None	None		None	10.1021/jm9707131
	DB12054	7498	47	None	-2	3	Rat	7.9	pIC50	=	7.9	Binding	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	ChEMBL		None	None	None		None	10.1021/jm9707131
	10814746	188373	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	484	6	1	8	3.8	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Cc2ccc3c(c2)OCO3)c1Br	10.1021/jm9700068
	CHEMBL47706	188373	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	484	6	1	8	3.8	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Cc2ccc3c(c2)OCO3)c1Br	10.1021/jm9700068
	10122675	105248	0	None	-	1	Human	7.9	pIC50	=	7.9	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	682	12	2	13	5.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccncc2)nc1OCC#CCOC(=O)Nc1cnccn1	10.1016/s0960-894x(02)01084-3
	CHEMBL275897	105248	0	None	-	1	Human	7.9	pIC50	=	7.9	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	682	12	2	13	5.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccncc2)nc1OCC#CCOC(=O)Nc1cnccn1	10.1016/s0960-894x(02)01084-3
	CHEMBL1791271	215695	2	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Inhibition of [125I]endothelin-1 [ET-1] binding to endothelin A receptor (ETA) of rabbit renal artery vascular smooth muscle cellsInhibition of [125I]endothelin-1 [ET-1] binding to endothelin A receptor (ETA) of rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)[C@H](C)CC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/0960-894X(95)00152-J
	9831249	66471	0	None	-	2	Human	7.9	pIC50	=	7.9	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	672	14	2	10	6.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C2CC2)nc1OCCCNS(=O)(=O)c1cccs1	10.1016/s0960-894x(02)01083-1
	CHEMBL172297	66471	0	None	-	2	Human	7.9	pIC50	=	7.9	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	672	14	2	10	6.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C2CC2)nc1OCCCNS(=O)(=O)c1cccs1	10.1016/s0960-894x(02)01083-1
	44311283	109110	0	None	-	1	Human	7.9	pIC50	=	7.9	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	649	11	2	10	6.7	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C(C)(C)C)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	CHEMBL303649	109110	0	None	-	1	Human	7.9	pIC50	=	7.9	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	649	11	2	10	6.7	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C(C)(C)C)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	44320590	113338	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	556	10	2	9	4.8	COc1ccc(Cn2nc(-c3cccs3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)c(OCC(=O)O)c1	10.1016/s0960-894x(00)00513-8
	CHEMBL314206	113338	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	556	10	2	9	4.8	COc1ccc(Cn2nc(-c3cccs3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)c(OCC(=O)O)c1	10.1016/s0960-894x(00)00513-8
	CHEMBL1788127	217895	8	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00070a001
	CHEMBL313760	217895	8	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00070a001
	44382933	171878	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.	ChEMBL	541	12	4	5	3.2	CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1cn(C)c2ccccc12)C(=O)NCCCC(=O)O	10.1016/0960-894X(95)00144-I
	CHEMBL422720	171878	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.	ChEMBL	541	12	4	5	3.2	CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1cn(C)c2ccccc12)C(=O)NCCCC(=O)O	10.1016/0960-894X(95)00144-I
	CHEMBL330144	218106	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)C(C)C	10.1021/jm00015a003
	22616257	211793	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	272	3	1	4	2.4	Cc1noc(NS(=O)(=O)c2ccccc2)c1Cl	10.1016/0960-894X(96)00441-6
	CHEMBL76860	211793	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	272	3	1	4	2.4	Cc1noc(NS(=O)(=O)c2ccccc2)c1Cl	10.1016/0960-894X(96)00441-6
	44317109	111669	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	472	3	1	4	4.1	Cc1noc(NS(=O)(=O)c2cc(Br)ccc2Br)c1Br	10.1016/0960-894X(96)00441-6
	CHEMBL311216	111669	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	472	3	1	4	4.1	Cc1noc(NS(=O)(=O)c2cc(Br)ccc2Br)c1Br	10.1016/0960-894X(96)00441-6
	18617327	212035	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	330	3	1	4	2.9	Cc1ccccc1S(=O)(=O)Nc1onc(C)c1Br	10.1016/0960-894X(96)00441-6
	CHEMBL78929	212035	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	330	3	1	4	2.9	Cc1ccccc1S(=O)(=O)Nc1onc(C)c1Br	10.1016/0960-894X(96)00441-6
	44276969	113616	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	506	7	1	5	4.8	COc1cccc(Cn2[nH]c(C(F)(F)C(F)(F)C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2=O)c1	10.1016/s0960-894x(00)00232-8
	CHEMBL3144607	113616	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	506	7	1	5	4.8	COc1cccc(Cn2[nH]c(C(F)(F)C(F)(F)C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2=O)c1	10.1016/s0960-894x(00)00232-8
	9961131	138935	0	None	-	2	Human	6.9	pIC50	=	6.9	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	650	15	2	12	3.1	CCCS(=O)(=O)NCCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	CHEMBL369676	138935	0	None	-	2	Human	6.9	pIC50	=	6.9	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	650	15	2	12	3.1	CCCS(=O)(=O)NCCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	CHEMBL342617	218455	0	None	-	0	Pig	6.9	pIC50	=	6.9	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	CHEMBL407639	219451	0	None	-	0	Pig	6.9	pIC50	=	6.9	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H](CS(=O)(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	10381121	103008	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	317	3	2	5	2.8	Cc1noc(NS(=O)(=O)c2cccc3ccc(N)cc23)c1C	10.1021/jm00008a013
	CHEMBL26090	103008	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	317	3	2	5	2.8	Cc1noc(NS(=O)(=O)c2cccc3ccc(N)cc23)c1C	10.1021/jm00008a013
	9974856	106129	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2ccc3ccc(N(C)C)cc3c2)c1C	10.1021/jm00008a013
	CHEMBL282401	106129	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2ccc3ccc(N(C)C)cc3c2)c1C	10.1021/jm00008a013
	CHEMBL1790499	215671	0	None	-	0	Pig	5.9	pIC50	=	5.9	Binding	Binding activity against Endothelin A receptor of Porcine aortic smooth muscle membranesBinding activity against Endothelin A receptor of Porcine aortic smooth muscle membranes	ChEMBL		None	None	None		CC[C@@H](C)[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC1=O	10.1021/jm00089a028
	CHEMBL327350	218069	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00070a001
	18617355	211733	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	330	3	1	4	2.9	Cc1ccc(S(=O)(=O)Nc2onc(C)c2Br)cc1	10.1016/0960-894X(96)00441-6
	CHEMBL76438	211733	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	330	3	1	4	2.9	Cc1ccc(S(=O)(=O)Nc2onc(C)c2Br)cc1	10.1016/0960-894X(96)00441-6
	CHEMBL432683	220413	0	None	-	0	Pig	5.9	pIC50	=	5.9	Binding	Compound was evaluated for the binding affinity to Endothelin A receptor in the porcine aortic smooth muscleCompound was evaluated for the binding affinity to Endothelin A receptor in the porcine aortic smooth muscle	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00087a001
	10618969	214121	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	367	7	1	5	4.8	O=[N+]([O-])c1ccc(OCc2ccsc2)cc1/C=C(/CO)c1ccccc1	10.1021/jm970847e
	CHEMBL93596	214121	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	367	7	1	5	4.8	O=[N+]([O-])c1ccc(OCc2ccsc2)cc1/C=C(/CO)c1ccccc1	10.1021/jm970847e
	127034901	143256	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	670	12	2	9	5.5	CCCc1nc2c(C)cc(C(=O)NCCN3CCOCC3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	CHEMBL3736037	143256	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	670	12	2	9	5.5	CCCc1nc2c(C)cc(C(=O)NCCN3CCOCC3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	44298382	201891	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	502	11	1	7	5.8	COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCCC=O)c1	10.1016/s0960-894x(00)00366-8
	CHEMBL54998	201891	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	502	11	1	7	5.8	COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCCC=O)c1	10.1016/s0960-894x(00)00366-8
	9974856	106129	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2ccc3ccc(N(C)C)cc3c2)c1C	10.1021/jm00004a012
	CHEMBL282401	106129	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2ccc3ccc(N(C)C)cc3c2)c1C	10.1021/jm00004a012
	CHEMBL343379	218478	0	None	-	0	Pig	5.9	pIC50	=	5.9	Binding	Inhibitory effect against porcine Endothelin A receptorInhibitory effect against porcine Endothelin A receptor	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC1=O	10.1021/jm00021a021
	CHEMBL343379	218478	0	None	-	0	Pig	5.9	pIC50	=	5.9	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC1=O	10.1021/jm00021a021
	CHEMBL315780	217971	0	None	-	0	Human	4.9	pIC50	=	4.9	Binding	Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@H](C(=O)O)c1csc2ccccc12)[C@@H](C)CC	10.1021/jm00070a001
	10334781	102785	0	None	-	0	Human	4.9	pIC50	=	4.9	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	297	4	1	6	2.0	Cc1noc(NS(=O)(=O)c2cccc([N+](=O)[O-])c2)c1C	10.1016/0960-894X(96)00441-6
	CHEMBL25970	102785	0	None	-	0	Human	4.9	pIC50	=	4.9	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	297	4	1	6	2.0	Cc1noc(NS(=O)(=O)c2cccc([N+](=O)[O-])c2)c1C	10.1016/0960-894X(96)00441-6
	18617299	212053	0	None	-	0	Human	4.9	pIC50	=	4.9	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	320	3	1	4	3.4	Cc1noc(NS(=O)(=O)c2ccc(Cl)cc2Cl)c1C	10.1016/0960-894X(96)00441-6
	CHEMBL79054	212053	0	None	-	0	Human	4.9	pIC50	=	4.9	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	320	3	1	4	3.4	Cc1noc(NS(=O)(=O)c2ccc(Cl)cc2Cl)c1C	10.1016/0960-894X(96)00441-6
	127028930	144082	0	None	-	0	Human	4.9	pIC50	=	4.9	Binding	Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes	ChEMBL	570	9	3	7	6.0	CCCc1nc2c(C)cc(C(=O)Nc3ccccc3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1	10.1039/C5MD00169B
	CHEMBL3752444	144082	0	None	-	0	Human	4.9	pIC50	=	4.9	Binding	Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes	ChEMBL	570	9	3	7	6.0	CCCc1nc2c(C)cc(C(=O)Nc3ccccc3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1	10.1039/C5MD00169B
	10769025	67044	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	550	10	5	5	4.6	Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCC(C)CC2)nc1C(=O)O	10.1021/jm950592+
	CHEMBL174171	67044	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	550	10	5	5	4.6	Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCC(C)CC2)nc1C(=O)O	10.1021/jm950592+
	44384656	136873	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	468	5	1	7	4.5	Cc1noc(NS(=O)(=O)c2ccsc2/C=C/c2ccc3c(c2)OCO3)c1Br	10.1016/S0960-894X(97)00133-9
	CHEMBL367763	136873	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	468	5	1	7	4.5	Cc1noc(NS(=O)(=O)c2ccsc2/C=C/c2ccc3c(c2)OCO3)c1Br	10.1016/S0960-894X(97)00133-9
	10577111	213676	0	None	-	0	Rat	4.9	pIC50	=	4.9	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	493	7	1	6	4.0	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2C(=O)COc2ccc(F)cc2)cc1	10.1021/jm9505369
	CHEMBL9084	213676	0	None	-	0	Rat	4.9	pIC50	=	4.9	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	493	7	1	6	4.0	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2C(=O)COc2ccc(F)cc2)cc1	10.1021/jm9505369
	10723203	18222	0	None	-	0	Human	4.9	pIC50	=	4.9	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	678	14	2	7	6.8	CCc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC(C)C)cc1)c1ccccc1C	10.1021/jm990171i
	CHEMBL1180350	18222	0	None	-	0	Human	4.9	pIC50	=	4.9	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	678	14	2	7	6.8	CCc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC(C)C)cc1)c1ccccc1C	10.1021/jm990171i
	CHEMBL123206	18222	0	None	-	0	Human	4.9	pIC50	=	4.9	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	678	14	2	7	6.8	CCc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC(C)C)cc1)c1ccccc1C	10.1021/jm990171i
	44291584	108011	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	501	8	3	9	3.5	COc1cc(OC)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)O)c1	10.1021/jm9608366
	CHEMBL296074	108011	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	501	8	3	9	3.5	COc1cc(OC)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)O)c1	10.1021/jm9608366
	10625875	136426	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	523	9	4	5	4.6	Cc1oc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O	10.1021/jm950591h
	CHEMBL367313	136426	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	523	9	4	5	4.6	Cc1oc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O	10.1021/jm950591h
	10625875	136426	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	523	9	4	5	4.6	Cc1oc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O	10.1021/jm950592+
	CHEMBL367313	136426	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	523	9	4	5	4.6	Cc1oc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O	10.1021/jm950592+
	22998447	213454	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	414	5	1	6	4.4	Cc1noc(NS(=O)(=O)c2sccc2Oc2ccccc2)c1Br	10.1016/S0960-894X(96)00496-9
	CHEMBL89457	213454	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	414	5	1	6	4.4	Cc1noc(NS(=O)(=O)c2sccc2Oc2ccccc2)c1Br	10.1016/S0960-894X(96)00496-9
	10381121	103008	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	317	3	2	5	2.8	Cc1noc(NS(=O)(=O)c2cccc3ccc(N)cc23)c1C	10.1021/jm00004a012
	CHEMBL26090	103008	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	317	3	2	5	2.8	Cc1noc(NS(=O)(=O)c2cccc3ccc(N)cc23)c1C	10.1021/jm00004a012
	10718688	190405	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	457	5	3	7	3.6	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cccc(O)c2)c1Br	10.1021/jm9608366
	CHEMBL48024	190405	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	457	5	3	7	3.6	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cccc(O)c2)c1Br	10.1021/jm9608366
	23445325	210166	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	397	5	2	6	3.8	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccccc2)c1Cl	10.1016/S0960-894X(97)00367-3
	CHEMBL65407	210166	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	397	5	2	6	3.8	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccccc2)c1Cl	10.1016/S0960-894X(97)00367-3
	10961546	103534	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	460	6	1	6	5.2	COc1ccc(C2=C(C(=O)O)[C@H](c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1	10.1021/jm031041j
	CHEMBL264543	103534	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	460	6	1	6	5.2	COc1ccc(C2=C(C(=O)O)[C@H](c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1	10.1021/jm031041j
	122272	103872	31	None	-1	2	Rat	7.8	pIC50	=	7.8	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C	10.1021/jm00008a013
	CHEMBL267458	103872	31	None	-1	2	Rat	7.8	pIC50	=	7.8	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C	10.1021/jm00008a013
	10961546	103534	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	460	6	1	6	5.2	COc1ccc(C2=C(C(=O)O)[C@H](c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1	10.1021/jm010382z
	CHEMBL264543	103534	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	460	6	1	6	5.2	COc1ccc(C2=C(C(=O)O)[C@H](c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1	10.1021/jm010382z
	44314751	168134	0	None	-	0	Pig	7.8	pIC50	=	7.8	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	603	13	5	4	5.0	CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1021/jm9600914
	CHEMBL412602	168134	0	None	-	0	Pig	7.8	pIC50	=	7.8	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	603	13	5	4	5.0	CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1021/jm9600914
	10602620	23363	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	544	10	2	6	5.4	CCCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm990170q
	CHEMBL123997	23363	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	544	10	2	6	5.4	CCCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm990170q
	10529868	170970	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	516	8	2	6	4.8	CCc1cccc(C)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm990170q
	CHEMBL421073	170970	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	516	8	2	6	4.8	CCc1cccc(C)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm990170q
	127035410	143163	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	557	8	1	8	5.7	CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(C#N)c1)C(=O)CCCC2	10.1039/C4MD00499J
	CHEMBL3735155	143163	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	557	8	1	8	5.7	CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(C#N)c1)C(=O)CCCC2	10.1039/C4MD00499J
	44320474	113845	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	440	8	1	5	5.7	CCC(CC)Cn1nc(-c2ccccc2)c(Cc2cc3c(cc2Cl)OCO3)c1C(=O)O	10.1016/s0960-894x(00)00513-8
	CHEMBL315752	113845	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	440	8	1	5	5.7	CCC(CC)Cn1nc(-c2ccccc2)c(Cc2cc3c(cc2Cl)OCO3)c1C(=O)O	10.1016/s0960-894x(00)00513-8
	10575845	18001	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	457	7	2	8	3.8	COc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(OC)c1	10.1021/jm9608366
	CHEMBL1178807	18001	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	457	7	2	8	3.8	COc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(OC)c1	10.1021/jm9608366
	CHEMBL43788	18001	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	457	7	2	8	3.8	COc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(OC)c1	10.1021/jm9608366
	10811595	105543	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	411	5	2	6	4.1	Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)cc1	10.1021/jm9608366
	10811595	105543	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	411	5	2	6	4.1	Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)cc1	10.1021/jm9700068
	CHEMBL278114	105543	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	411	5	2	6	4.1	Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)cc1	10.1021/jm9608366
	CHEMBL278114	105543	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	411	5	2	6	4.1	Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)cc1	10.1021/jm9700068
	CHEMBL328942	218095	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cellsInhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00095a029
	CHEMBL150719	215570	0	None	-	0	Mouse	7.8	pIC50	=	7.8	Binding	Inhibition of [125I]ET1 binding to Endothelin A receptor of murine 3T3 cellsInhibition of [125I]ET1 binding to Endothelin A receptor of murine 3T3 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@H](C)CC	10.1016/S0960-894X(01)81219-1
	10360201	102461	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	345	4	1	5	3.3	Cc1onc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C	10.1021/jm00004a012
	CHEMBL25816	102461	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	345	4	1	5	3.3	Cc1onc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C	10.1021/jm00004a012
	122272	103872	31	None	-1	2	Rat	7.8	pIC50	=	7.8	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C	10.1021/jm00004a012
	CHEMBL267458	103872	31	None	-1	2	Rat	7.8	pIC50	=	7.8	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C	10.1021/jm00004a012
	44283349	107102	0	None	-	0	Pig	7.8	pIC50	=	7.8	Binding	Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	603	13	5	4	5.0	CCCC[C@H](NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1016/0960-894X(95)00237-N
	CHEMBL289410	107102	0	None	-	0	Pig	7.8	pIC50	=	7.8	Binding	Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	603	13	5	4	5.0	CCCC[C@H](NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1016/0960-894X(95)00237-N
	44334053	11323	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	465	5	1	5	5.5	COc1ccc([C@@H]2c3nc(-c4ccccc4)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1	10.1016/s0960-894x(02)00663-7
	CHEMBL102411	11323	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	465	5	1	5	5.5	COc1ccc([C@@H]2c3nc(-c4ccccc4)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1	10.1016/s0960-894x(02)00663-7
	10811595	105543	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor	ChEMBL	411	5	2	6	4.1	Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)cc1	10.1021/jm000349x
	CHEMBL278114	105543	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor	ChEMBL	411	5	2	6	4.1	Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)cc1	10.1021/jm000349x
	CHEMBL336563	218363	0	None	-	0	Pig	7.8	pIC50	=	7.8	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C(C)(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	CHEMBL347948	218493	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	The inhibitory constant was evaluated against Endothelin A receptorThe inhibitory constant was evaluated against Endothelin A receptor	ChEMBL		None	None	None		CC[C@H](C)[C@@H](NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)81219-1
	11072080	18876	0	None	-	0	Pig	7.8	pIC50	=	7.8	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	600	11	1	9	6.4	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ccc3ccccc3n2)c1	10.1021/jm0102304
	CHEMBL1183970	18876	0	None	-	0	Pig	7.8	pIC50	=	7.8	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	600	11	1	9	6.4	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ccc3ccccc3n2)c1	10.1021/jm0102304
	CHEMBL326160	18876	0	None	-	0	Pig	7.8	pIC50	=	7.8	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	600	11	1	9	6.4	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ccc3ccccc3n2)c1	10.1021/jm0102304
	155562688	181959	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	554	13	2	10	2.9	CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC	10.1016/j.bmcl.2016.06.014
	CHEMBL4570529	181959	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	554	13	2	10	2.9	CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC	10.1016/j.bmcl.2016.06.014
	22616258	112183	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	372	5	1	4	3.8	CCCc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1C	10.1016/0960-894X(96)00441-6
	CHEMBL311781	112183	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	372	5	1	4	3.8	CCCc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1C	10.1016/0960-894X(96)00441-6
	10740943	210185	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	422	5	2	6	3.2	CNc1cccc2c(S(=O)(=O)Nc3ncc(Br)nc3OC)cccc12	10.1021/jm9604585
	CHEMBL6555	210185	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	422	5	2	6	3.2	CNc1cccc2c(S(=O)(=O)Nc3ncc(Br)nc3OC)cccc12	10.1021/jm9604585
	CHEMBL67074	210393	0	None	-	0	Pig	7.8	pIC50	=	7.8	Binding	Tested for its ability to inhibit the binding of [125I]ET1 to the Endothelin A receptor in porcine thoracic aorta membranes.Tested for its ability to inhibit the binding of [125I]ET1 to the Endothelin A receptor in porcine thoracic aorta membranes.	ChEMBL	646	8	2	13	5.8	COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC(=O)C2=C(C)N=C(C)/C(=C(/O)OC)[C@@H]2c2cccc([N+](=O)[O-])c2)[C@@H]1c1cccc([N+](=O)[O-])c1	10.1016/S0960-894X(01)81025-8
	122272	103872	31	None	1	2	Human	6.8	pIC50	=	6.8	Binding	Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C	10.1021/jm00029a001
	CHEMBL267458	103872	31	None	1	2	Human	6.8	pIC50	=	6.8	Binding	Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C	10.1021/jm00029a001
	10095393	104334	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	452	5	3	5	5.3	Cc1noc(NS(=O)(=O)c2cccc3c(N/C(S)=N/c4ccccc4)cccc23)c1C	10.1021/jm00008a013
	CHEMBL27063	104334	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	452	5	3	5	5.3	Cc1noc(NS(=O)(=O)c2cccc3c(N/C(S)=N/c4ccccc4)cccc23)c1C	10.1021/jm00008a013
	10576863	15060	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	484	5	1	6	5.1	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(Cl)c(Cl)c2)cc1	10.1021/jm9606507
	CHEMBL10926	15060	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	484	5	1	6	5.1	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(Cl)c(Cl)c2)cc1	10.1021/jm9606507
	44279338	113471	0	None	-	0	Pig	6.8	pIC50	=	6.8	Binding	Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	487	11	6	4	2.3	CC(C)C[C@H](NC(=O)NC(C)(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	CHEMBL31436	113471	0	None	-	0	Pig	6.8	pIC50	=	6.8	Binding	Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	487	11	6	4	2.3	CC(C)C[C@H](NC(=O)NC(C)(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	44279309	168596	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor	ChEMBL	412	3	2	3	4.5	Cc1ccc(-c2ccc3c(c2)C(=O)c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@H]32)cc1	10.1016/0960-894X(95)00230-Q
	CHEMBL414408	168596	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor	ChEMBL	412	3	2	3	4.5	Cc1ccc(-c2ccc3c(c2)C(=O)c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@H]32)cc1	10.1016/0960-894X(95)00230-Q
	10641986	214014	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	356	6	1	4	4.2	N#Cc1ccc(OCc2cccnc2)cc1/C=C(/C(=O)O)c1ccccc1	10.1021/jm970847e
	CHEMBL92842	214014	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	356	6	1	4	4.2	N#Cc1ccc(OCc2cccnc2)cc1/C=C(/C(=O)O)c1ccccc1	10.1021/jm970847e
	44266646	105341	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor	ChEMBL	475	6	1	8	4.5	COc1cc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC	10.1016/s0960-894x(97)10151-2
	CHEMBL276638	105341	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor	ChEMBL	475	6	1	8	4.5	COc1cc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC	10.1016/s0960-894x(97)10151-2
	10087191	108614	1	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	317	3	2	5	2.8	Cc1noc(NS(=O)(=O)c2cccc3c(N)cccc23)c1C	10.1021/jm00004a012
	CHEMBL30039	108614	1	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	317	3	2	5	2.8	Cc1noc(NS(=O)(=O)c2cccc3c(N)cccc23)c1C	10.1021/jm00004a012
	CHEMBL424227	220101	0	None	-	0	Pig	6.8	pIC50	=	6.8	Binding	Inhibition of endothelin (ET-A) binding to porcine heart membranes Inhibition of endothelin (ET-A) binding to porcine heart membranes	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)CNC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/0960-894X(95)00349-X
	44334084	116430	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	461	7	2	6	3.8	COc1ccc([C@@H]2c3nc(CCC(=O)O)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1	10.1016/s0960-894x(02)00663-7
	CHEMBL322434	116430	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	461	7	2	6	3.8	COc1ccc([C@@H]2c3nc(CCC(=O)O)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1	10.1016/s0960-894x(02)00663-7
	122272	103872	31	None	1	2	Human	6.8	pIC50	=	6.8	Binding	Inhibitory concentration against Endothelin A receptorInhibitory concentration against Endothelin A receptor	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C	10.1021/jm030480f
	CHEMBL267458	103872	31	None	1	2	Human	6.8	pIC50	=	6.8	Binding	Inhibitory concentration against Endothelin A receptorInhibitory concentration against Endothelin A receptor	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C	10.1021/jm030480f
	44266646	105341	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Potency at Endothelin A receptor was determinedPotency at Endothelin A receptor was determined	ChEMBL	475	6	1	8	4.5	COc1cc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC	10.1021/jm0300429
	CHEMBL276638	105341	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Potency at Endothelin A receptor was determinedPotency at Endothelin A receptor was determined	ChEMBL	475	6	1	8	4.5	COc1cc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC	10.1021/jm0300429
	CHEMBL137671	215526	0	None	-	0	Pig	6.8	pIC50	=	6.8	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	CHEMBL335128	218324	0	None	-	0	Pig	6.8	pIC50	=	6.8	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	44371429	55674	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes	ChEMBL	455	6	1	6	5.2	COc1cccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2ccccc23)c1	10.1016/s0960-894x(99)00040-2
	CHEMBL155973	55674	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes	ChEMBL	455	6	1	6	5.2	COc1cccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2ccccc23)c1	10.1016/s0960-894x(99)00040-2
	44316993	211718	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	286	3	1	4	2.7	Cc1noc(NS(=O)(=O)c2cccc(Cl)c2)c1C	10.1016/0960-894X(96)00441-6
	CHEMBL76360	211718	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	286	3	1	4	2.7	Cc1noc(NS(=O)(=O)c2cccc(Cl)c2)c1C	10.1016/0960-894X(96)00441-6
	10983585	180053	0	None	-	1	Human	5.8	pIC50	=	5.8	Binding	Binding affinity to recombinant human ETABinding affinity to recombinant human ETA	ChEMBL	473	9	2	8	3.7	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)ncnc1OCCO	10.1021/acs.jmedchem.0c01093
	CHEMBL4525321	180053	0	None	-	1	Human	5.8	pIC50	=	5.8	Binding	Binding affinity to recombinant human ETABinding affinity to recombinant human ETA	ChEMBL	473	9	2	8	3.7	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)ncnc1OCCO	10.1021/acs.jmedchem.0c01093
	10650477	121026	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	558	10	2	6	5.8	CCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC(C)C)cc1	10.1021/jm990170q
	CHEMBL333009	121026	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	558	10	2	6	5.8	CCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC(C)C)cc1	10.1021/jm990170q
	44298356	201764	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	503	10	2	8	5.7	COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCC/C=N/O)c1	10.1016/s0960-894x(00)00366-8
	CHEMBL54703	201764	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	503	10	2	8	5.7	COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCC/C=N/O)c1	10.1016/s0960-894x(00)00366-8
	10983585	180053	0	None	-	1	Human	5.8	pIC50	=	5.8	Binding	Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes	ChEMBL	473	9	2	8	3.7	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)ncnc1OCCO	10.1016/j.bmcl.2016.06.014
	CHEMBL4525321	180053	0	None	-	1	Human	5.8	pIC50	=	5.8	Binding	Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes	ChEMBL	473	9	2	8	3.7	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)ncnc1OCCO	10.1016/j.bmcl.2016.06.014
	66875612	182051	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes	ChEMBL	495	10	2	10	2.9	COc1ccccc1Oc1c(NS(=O)(=O)c2ccccc2)nc(-c2ncccn2)nc1OCCO	10.1016/j.bmcl.2016.06.014
	CHEMBL4572634	182051	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes	ChEMBL	495	10	2	10	2.9	COc1ccccc1Oc1c(NS(=O)(=O)c2ccccc2)nc(-c2ncccn2)nc1OCCO	10.1016/j.bmcl.2016.06.014
	10693981	66324	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	431	7	1	6	4.4	Cc1ccccc1C(Oc1cc(OCc2ccc3c(c2)OCCO3)ccc1C#N)C(=O)O	10.1021/jm990378b
	CHEMBL171702	66324	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	431	7	1	6	4.4	Cc1ccccc1C(Oc1cc(OCc2ccc3c(c2)OCCO3)ccc1C#N)C(=O)O	10.1021/jm990378b
	15340612	113609	1	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	406	5	1	5	3.6	COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2=O)c1	10.1016/s0960-894x(00)00232-8
	CHEMBL3144599	113609	1	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	406	5	1	5	3.6	COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2=O)c1	10.1016/s0960-894x(00)00232-8
	10744921	66827	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	536	10	5	4	4.6	CCc1[nH]c([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O	10.1021/jm950591h
	CHEMBL173666	66827	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	536	10	5	4	4.6	CCc1[nH]c([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O	10.1021/jm950591h
	44299023	203277	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)	ChEMBL	457	6	1	6	4.7	CCc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)c(=O)n2Cc1ccccc1OC	10.1016/S0960-894X(97)00319-3
	CHEMBL56343	203277	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)	ChEMBL	457	6	1	6	4.7	CCc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)c(=O)n2Cc1ccccc1OC	10.1016/S0960-894X(97)00319-3
	44332577	11478	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells	ChEMBL	341	3	0	4	4.4	O=CC(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12	10.1016/S0960-894X(96)00551-3
	CHEMBL103484	11478	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells	ChEMBL	341	3	0	4	4.4	O=CC(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12	10.1016/S0960-894X(96)00551-3
	44266540	11677	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	447	6	1	7	4.8	COc1ccc2c(c1)c(-c1ccc(OC)c(OC)c1)c(C(=O)O)n2-c1ccc2c(c1)OCO2	10.1016/0960-894X(96)00170-9
	CHEMBL10457	11677	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	447	6	1	7	4.8	COc1ccc2c(c1)c(-c1ccc(OC)c(OC)c1)c(C(=O)O)n2-c1ccc2c(c1)OCO2	10.1016/0960-894X(96)00170-9
	44266549	169146	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	415	4	1	6	4.5	O=C(O)c1c(-c2ccc3c(c2)OCO3)c2ccccc2n1Cc1ccc2c(c1)OCO2	10.1016/0960-894X(96)00170-9
	CHEMBL416518	169146	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	415	4	1	6	4.5	O=C(O)c1c(-c2ccc3c(c2)OCO3)c2ccccc2n1Cc1ccc2c(c1)OCO2	10.1016/0960-894X(96)00170-9
	19432649	211267	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	487	9	2	8	4.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCO	10.1016/S0960-894X(97)00400-9
	CHEMBL72473	211267	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	487	9	2	8	4.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCO	10.1016/S0960-894X(97)00400-9
	CHEMBL342215	218442	0	None	-	0	Pig	5.8	pIC50	=	5.8	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2cn(C(=O)OC(C)(C)C)c3ccccc23)NC1=O	10.1021/jm00021a021
	44279349	174926	0	None	-	0	Human	4.8	pIC50	=	4.8	Binding	Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor	ChEMBL	448	3	2	3	5.3	O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(-c3cccc4ccccc34)cc21	10.1016/0960-894X(95)00230-Q
	CHEMBL433039	174926	0	None	-	0	Human	4.8	pIC50	=	4.8	Binding	Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor	ChEMBL	448	3	2	3	5.3	O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(-c3cccc4ccccc34)cc21	10.1016/0960-894X(95)00230-Q
	CHEMBL336087	218356	0	None	-	0	Pig	4.8	pIC50	=	4.8	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O	10.1021/jm00021a021
	44386537	134588	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	532	10	4	7	4.2	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2cccnc2)nc1C(=O)O	10.1021/jm950592+
	CHEMBL366391	134588	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	532	10	4	7	4.2	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2cccnc2)nc1C(=O)O	10.1021/jm950592+
	10188517	68540	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	582	9	2	10	3.6	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(N2CCOCC2)nc1OCC#CCO	10.1016/s0960-894x(02)01084-3
	CHEMBL177203	68540	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	582	9	2	10	3.6	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(N2CCOCC2)nc1OCC#CCO	10.1016/s0960-894x(02)01084-3
	10122442	137475	0	None	-	1	Human	6.8	pIC50	=	6.8	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	660	14	2	11	5.6	CCCCNC(=O)OCC#CCOc1nc(-c2ccncc2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	CHEMBL368383	137475	0	None	-	1	Human	6.8	pIC50	=	6.8	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	660	14	2	11	5.6	CCCCNC(=O)OCC#CCOc1nc(-c2ccncc2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	10832511	210183	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	362	4	1	5	3.2	CN(C)c1cccc2c(S(=O)(=O)Nc3cnc(Cl)cn3)cccc12	10.1021/jm9604585
	CHEMBL6553	210183	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	362	4	1	5	3.2	CN(C)c1cccc2c(S(=O)(=O)Nc3cnc(Cl)cn3)cccc12	10.1021/jm9604585
	104865	7493	99	None	1	4	Human	5.8	pIC50	=	5.8	Binding	Antagonist activity at ETA receptor (unknown origin) assessed as increase in G protein-mediated vasoconstrictionAntagonist activity at ETA receptor (unknown origin) assessed as increase in G protein-mediated vasoconstriction	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/acs.jmedchem.8b00435
	3494	7493	99	None	1	4	Human	5.8	pIC50	=	5.8	Binding	Antagonist activity at ETA receptor (unknown origin) assessed as increase in G protein-mediated vasoconstrictionAntagonist activity at ETA receptor (unknown origin) assessed as increase in G protein-mediated vasoconstriction	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/acs.jmedchem.8b00435
	392	7493	99	None	1	4	Human	5.8	pIC50	=	5.8	Binding	Antagonist activity at ETA receptor (unknown origin) assessed as increase in G protein-mediated vasoconstrictionAntagonist activity at ETA receptor (unknown origin) assessed as increase in G protein-mediated vasoconstriction	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/acs.jmedchem.8b00435
	CHEMBL957	7493	99	None	1	4	Human	5.8	pIC50	=	5.8	Binding	Antagonist activity at ETA receptor (unknown origin) assessed as increase in G protein-mediated vasoconstrictionAntagonist activity at ETA receptor (unknown origin) assessed as increase in G protein-mediated vasoconstriction	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/acs.jmedchem.8b00435
	DB00559	7493	99	None	1	4	Human	5.8	pIC50	=	5.8	Binding	Antagonist activity at ETA receptor (unknown origin) assessed as increase in G protein-mediated vasoconstrictionAntagonist activity at ETA receptor (unknown origin) assessed as increase in G protein-mediated vasoconstriction	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/acs.jmedchem.8b00435
	10569313	103978	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	342	4	1	5	2.8	Cc1ccc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)nn1	10.1021/jm9604585
	CHEMBL268387	103978	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	342	4	1	5	2.8	Cc1ccc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)nn1	10.1021/jm9604585
	5018984	209909	2	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	405	4	1	4	3.9	CN(C)c1cccc2c(S(=O)(=O)Nc3ccc(Br)cn3)cccc12	10.1021/jm9604585
	CHEMBL6411	209909	2	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	405	4	1	4	3.9	CN(C)c1cccc2c(S(=O)(=O)Nc3ccc(Br)cn3)cccc12	10.1021/jm9604585
	10690058	209976	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	362	4	1	5	3.2	CN(C)c1cccc2c(S(=O)(=O)Nc3ncc(Cl)cn3)cccc12	10.1021/jm9604585
	CHEMBL6433	209976	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	362	4	1	5	3.2	CN(C)c1cccc2c(S(=O)(=O)Nc3ncc(Cl)cn3)cccc12	10.1021/jm9604585
	5017966	210045	2	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	341	4	1	4	3.4	Cc1ccc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)nc1	10.1021/jm9604585
	CHEMBL6463	210045	2	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	341	4	1	4	3.4	Cc1ccc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)nc1	10.1021/jm9604585
	23445285	119154	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	454	7	1	5	5.6	CCCCc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1	10.1016/S0960-894X(96)00496-9
	CHEMBL329560	119154	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	454	7	1	5	5.6	CCCCc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1	10.1016/S0960-894X(96)00496-9
	10250826	105881	0	None	-	0	Rat	4.8	pIC50	=	4.8	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	407	5	1	5	4.7	Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1-c1ccccc1	10.1021/jm00008a013
	CHEMBL280823	105881	0	None	-	0	Rat	4.8	pIC50	=	4.8	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	407	5	1	5	4.7	Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1-c1ccccc1	10.1021/jm00008a013
	9980084	108910	0	None	-	0	Rat	4.8	pIC50	=	4.8	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	429	10	1	5	5.7	CCCCN(CCCC)c1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12	10.1021/jm00008a013
	CHEMBL30245	108910	0	None	-	0	Rat	4.8	pIC50	=	4.8	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	429	10	1	5	5.7	CCCCN(CCCC)c1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12	10.1021/jm00008a013
	9852624	135459	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	656	14	2	11	4.5	CCS(=O)(=O)NCCCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	CHEMBL366872	135459	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	656	14	2	11	4.5	CCS(=O)(=O)NCCCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	10744040	120346	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	502	7	2	6	4.5	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2cccc(C)c2C)cc1	10.1021/jm031041j
	CHEMBL332231	120346	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	502	7	2	6	4.5	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2cccc(C)c2C)cc1	10.1021/jm031041j
	10815726	18220	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	516	8	2	6	4.5	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(C)c2ccccc2C)cc1	10.1021/jm990171i
	CHEMBL1180348	18220	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	516	8	2	6	4.5	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(C)c2ccccc2C)cc1	10.1021/jm990171i
	CHEMBL123146	18220	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	516	8	2	6	4.5	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(C)c2ccccc2C)cc1	10.1021/jm990171i
	10671649	105342	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	460	5	1	8	3.6	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc3c(c2)OCO3)cc1	10.1021/jm9606507
	CHEMBL276639	105342	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	460	5	1	8	3.6	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc3c(c2)OCO3)cc1	10.1021/jm9606507
	10299975	117031	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	488	14	1	5	5.1	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC(C)CC	10.1021/jm980217s
	CHEMBL323791	117031	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	488	14	1	5	5.1	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC(C)CC	10.1021/jm980217s
	10816152	23105	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	534	9	2	8	3.9	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(OC)cccc2OC)cc1	10.1021/jm990170q
	CHEMBL122832	23105	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	534	9	2	8	3.9	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(OC)cccc2OC)cc1	10.1021/jm990170q
	10744040	120346	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	502	7	2	6	4.5	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2cccc(C)c2C)cc1	10.1021/jm990170q
	CHEMBL332231	120346	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	502	7	2	6	4.5	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2cccc(C)c2C)cc1	10.1021/jm990170q
	10552344	65989	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	471	7	1	6	5.1	N#Cc1ccc(OCc2ccc3c(c2)OCO3)cc1OC(C(=O)O)c1ccccc1C(F)(F)F	10.1021/jm990378b
	CHEMBL170202	65989	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	471	7	1	6	5.1	N#Cc1ccc(OCc2ccc3c(c2)OCO3)cc1OC(C(=O)O)c1ccccc1C(F)(F)F	10.1021/jm990378b
	44295156	21399	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	520	10	1	9	4.7	COc1ccccc1C(=O)/C(Cc1cc(OC)c(OC)c(OC)c1)=C(\C(=O)O)c1ccc2nsnc2c1	10.1016/s0960-894x(98)00301-1
	CHEMBL1205062	21399	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	520	10	1	9	4.7	COc1ccccc1C(=O)/C(Cc1cc(OC)c(OC)c(OC)c1)=C(\C(=O)O)c1ccc2nsnc2c1	10.1016/s0960-894x(98)00301-1
	CHEMBL48411	21399	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	520	10	1	9	4.7	COc1ccccc1C(=O)/C(Cc1cc(OC)c(OC)c(OC)c1)=C(\C(=O)O)c1ccc2nsnc2c1	10.1016/s0960-894x(98)00301-1
	10231591	138138	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	569	10	2	11	2.8	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCO	10.1016/s0960-894x(02)01084-3
	CHEMBL368828	138138	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	569	10	2	11	2.8	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCO	10.1016/s0960-894x(02)01084-3
	10338502	126253	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	359	4	2	5	3.2	CC(=O)Nc1cccc2c(S(=O)(=O)Nc3noc(C)c3C)cccc12	10.1021/jm00004a012
	CHEMBL345247	126253	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	359	4	2	5	3.2	CC(=O)Nc1cccc2c(S(=O)(=O)Nc3noc(C)c3C)cccc12	10.1021/jm00004a012
	44386370	67189	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	531	10	4	6	4.8	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2ccccc2)nc1C(=O)O	10.1021/jm950592+
	CHEMBL175066	67189	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	531	10	4	6	4.8	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2ccccc2)nc1C(=O)O	10.1021/jm950592+
	15453177	212300	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	392	4	1	4	4.2	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2)c1Br	10.1016/S0960-894X(96)00496-9
	CHEMBL80857	212300	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	392	4	1	4	4.2	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2)c1Br	10.1016/S0960-894X(96)00496-9
	10601795	103747	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	510	10	1	6	4.4	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(CC(C)C)CC(C)C)cc1	10.1021/jm9505369
	CHEMBL266354	103747	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	510	10	1	6	4.4	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(CC(C)C)CC(C)C)cc1	10.1021/jm9505369
	44265869	104037	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	466	7	2	6	3.3	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC2CCCC2)cc1	10.1021/jm9505369
	CHEMBL268864	104037	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	466	7	2	6	3.3	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC2CCCC2)cc1	10.1021/jm9505369
	44278003	106044	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.	ChEMBL	449	8	1	6	5.6	COc1cccc(Sc2c(C(=O)O)n(Cc3ccccc3)c3cc(OC)c(OC)cc23)c1	10.1016/0960-894X(96)00232-6
	CHEMBL28188	106044	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.	ChEMBL	449	8	1	6	5.6	COc1cccc(Sc2c(C(=O)O)n(Cc3ccccc3)c3cc(OC)c(OC)cc23)c1	10.1016/0960-894X(96)00232-6
	18617302	111193	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	334	3	1	4	2.7	Cc1noc(NS(=O)(=O)c2ccccc2F)c1Br	10.1016/0960-894X(96)00441-6
	CHEMBL310361	111193	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	334	3	1	4	2.7	Cc1noc(NS(=O)(=O)c2ccccc2F)c1Br	10.1016/0960-894X(96)00441-6
	15453180	112002	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	348	4	1	4	4.1	Cc1noc(NS(=O)(=O)c2cccc(-c3ccccc3)c2)c1Cl	10.1016/0960-894X(96)00441-6
	CHEMBL311510	112002	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	348	4	1	4	4.1	Cc1noc(NS(=O)(=O)c2cccc(-c3ccccc3)c2)c1Cl	10.1016/0960-894X(96)00441-6
	10951244	209732	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	504	9	1	7	5.6	CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1cc(OC)ccc1OC)O2	10.1021/jm010382z
	CHEMBL62962	209732	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	504	9	1	7	5.6	CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1cc(OC)ccc1OC)O2	10.1021/jm010382z
	11100307	209980	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	354	5	1	5	3.8	CCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21	10.1021/jm010382z
	CHEMBL64340	209980	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	354	5	1	5	3.8	CCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21	10.1021/jm010382z
	44314461	211558	0	None	-	0	Pig	6.8	pIC50	=	6.8	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	605	13	5	4	3.9	CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1CCCC1)C(=O)O	10.1021/jm9600914
	CHEMBL74837	211558	0	None	-	0	Pig	6.8	pIC50	=	6.8	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	605	13	5	4	3.9	CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1CCCC1)C(=O)O	10.1021/jm9600914
	10767778	23174	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	502	7	2	6	4.5	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2cc(C)cc(C)c2)cc1	10.1021/jm990170q
	CHEMBL123077	23174	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	502	7	2	6	4.5	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2cc(C)cc(C)c2)cc1	10.1021/jm990170q
	44295114	21652	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	556	11	1	9	5.3	COc1cc(C/C(C(=O)c2ccc(OC(F)F)cc2)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC	10.1016/s0960-894x(98)00301-1
	CHEMBL1207717	21652	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	556	11	1	9	5.3	COc1cc(C/C(C(=O)c2ccc(OC(F)F)cc2)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC	10.1016/s0960-894x(98)00301-1
	CHEMBL433090	21652	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	556	11	1	9	5.3	COc1cc(C/C(C(=O)c2ccc(OC(F)F)cc2)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC	10.1016/s0960-894x(98)00301-1
	122044	16945	51	None	-	0	Pig	6.8	pIC50	=	6.8	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	473	9	2	8	3.7	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCO)c1	10.1021/jm0102304
	CHEMBL115951	16945	51	None	-	0	Pig	6.8	pIC50	=	6.8	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	473	9	2	8	3.7	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCO)c1	10.1021/jm0102304
	44309814	109783	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor	ChEMBL	487	8	1	7	6.2	CCCOc1ccc2c(c1)c(-c1ccc(OC)cc1)c(C(=O)O)n2Cc1cc2nsnc2cc1C	10.1016/s0960-894x(97)10151-2
	CHEMBL306863	109783	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor	ChEMBL	487	8	1	7	6.2	CCCOc1ccc2c(c1)c(-c1ccc(OC)cc1)c(C(=O)O)n2Cc1cc2nsnc2cc1C	10.1016/s0960-894x(97)10151-2
	44327380	118381	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	457	6	1	9	1.4	COc1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)n2nc(C)ccc2=O)cc1	10.1016/S0960-894X(96)00617-8
	CHEMBL328311	118381	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	457	6	1	9	1.4	COc1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)n2nc(C)ccc2=O)cc1	10.1016/S0960-894X(96)00617-8
	CHEMBL136634	215519	0	None	-	0	Pig	6.8	pIC50	=	6.8	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](C(C)C)NC1=O	10.1021/jm00021a021
	CHEMBL337031	218369	0	None	-	0	Pig	6.8	pIC50	=	6.8	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)CNC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	CHEMBL342840	218473	0	None	-	0	Pig	6.8	pIC50	=	6.8	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	10926281	109535	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	354	4	1	5	3.8	CC(C)Oc1ccc2c(c1)C=C(C(=O)O)[C@H](c1ccc3c(c1)OCO3)O2	10.1021/jm031041j
	CHEMBL305117	109535	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	354	4	1	5	3.8	CC(C)Oc1ccc2c(c1)C=C(C(=O)O)[C@H](c1ccc3c(c1)OCO3)O2	10.1021/jm031041j
	10926281	109535	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	354	4	1	5	3.8	CC(C)Oc1ccc2c(c1)C=C(C(=O)O)[C@H](c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	CHEMBL305117	109535	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	354	4	1	5	3.8	CC(C)Oc1ccc2c(c1)C=C(C(=O)O)[C@H](c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	11026419	209961	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	432	5	1	6	4.5	COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3c(OC)cccc32)cc1	10.1021/jm010382z
	CHEMBL64266	209961	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	432	5	1	6	4.5	COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3c(OC)cccc32)cc1	10.1021/jm010382z
	44368819	175671	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	In vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricleIn vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricle	ChEMBL	1637	31	19	20	1.7	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)NCCCCCCCC(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)80156-6
	77282140	175671	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	In vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricleIn vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricle	ChEMBL	1637	31	19	20	1.7	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)NCCCCCCCC(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)80156-6
	CHEMBL438380	175671	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	In vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricleIn vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricle	ChEMBL	1637	31	19	20	1.7	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)NCCCCCCCC(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)80156-6
	44270524	104983	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells	ChEMBL	682	13	1	9	6.9	CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)NS(=O)(=O)c1ccccc1)c1ccc2c(c1)OCO2	10.1016/0960-894X(95)00186-W
	CHEMBL274243	104983	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells	ChEMBL	682	13	1	9	6.9	CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)NS(=O)(=O)c1ccccc1)c1ccc2c(c1)OCO2	10.1016/0960-894X(95)00186-W
	44267002	105335	0	None	-	0	Human	4.8	pIC50	=	4.8	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	546	5	1	7	5.2	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc3c2CCc2ccccc2C3=O)cc1	10.1021/jm9606507
	CHEMBL276601	105335	0	None	-	0	Human	4.8	pIC50	=	4.8	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	546	5	1	7	5.2	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc3c2CCc2ccccc2C3=O)cc1	10.1021/jm9606507
	10627398	137465	0	None	-	0	Rat	4.8	pIC50	=	4.8	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	599	11	4	5	5.8	CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(Cc2ccccc2)o1	10.1021/jm950591h
	CHEMBL368339	137465	0	None	-	0	Rat	4.8	pIC50	=	4.8	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	599	11	4	5	5.8	CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(Cc2ccccc2)o1	10.1021/jm950591h
	10841170	18891	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	592	9	2	6	5.8	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2C)c2ccccc2C)cc1	10.1021/jm990171i
	CHEMBL1184090	18891	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	592	9	2	6	5.8	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2C)c2ccccc2C)cc1	10.1021/jm990171i
	CHEMBL332109	18891	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	592	9	2	6	5.8	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2C)c2ccccc2C)cc1	10.1021/jm990171i
	10579647	175257	0	None	-	0	Rat	4.8	pIC50	=	4.8	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	612	11	4	5	5.8	Cc1c(C(=O)O)nc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)n1Cc1ccccc1	10.1021/jm950592+
	CHEMBL435156	175257	0	None	-	0	Rat	4.8	pIC50	=	4.8	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	612	11	4	5	5.8	Cc1c(C(=O)O)nc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)n1Cc1ccccc1	10.1021/jm950592+
	10575061	213672	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	439	9	1	6	4.0	CCCCC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL9082	213672	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	439	9	1	6	4.0	CCCCC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	10646637	213827	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	437	8	1	5	4.9	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2C/C=C/CC(C)C)cc1	10.1021/jm9505369
	CHEMBL9168	213827	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	437	8	1	5	4.9	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2C/C=C/CC(C)C)cc1	10.1021/jm9505369
	44368416	51466	0	None	-	0	Pig	4.8	pIC50	=	4.8	Binding	Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.	ChEMBL	540	8	2	6	5.6	O=C(O)C(Cc1c[nH]c2ccccc12)N(Cc1cc2c(cc1Cl)OCO2)Cc1cc2c(cc1Cl)OCO2	10.1016/s0960-894x(01)00009-9
	CHEMBL152098	51466	0	None	-	0	Pig	4.8	pIC50	=	4.8	Binding	Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.	ChEMBL	540	8	2	6	5.6	O=C(O)C(Cc1c[nH]c2ccccc12)N(Cc1cc2c(cc1Cl)OCO2)Cc1cc2c(cc1Cl)OCO2	10.1016/s0960-894x(01)00009-9
	10478562	138576	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor	ChEMBL	442	6	1	6	4.5	Cc1ccc(OCc2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1	10.1016/S0960-894X(97)00132-7
	CHEMBL369359	138576	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor	ChEMBL	442	6	1	6	4.5	Cc1ccc(OCc2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1	10.1016/S0960-894X(97)00132-7
	127026043	144131	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes	ChEMBL	607	11	3	9	3.8	CCCc1nc2c(C)cc(C(=O)NCCN3CCOCC3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1	10.1039/C5MD00169B
	CHEMBL3752947	144131	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes	ChEMBL	607	11	3	9	3.8	CCCc1nc2c(C)cc(C(=O)NCCN3CCOCC3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1	10.1039/C5MD00169B
	44386162	67183	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	575	11	1	9	6.2	CC/C=C/COc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	CHEMBL175005	67183	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	575	11	1	9	6.2	CC/C=C/COc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	10503334	180123	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	441	5	2	6	3.9	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccccc2)c1Br	10.1016/S0960-894X(97)00367-3
	CHEMBL45269	180123	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	441	5	2	6	3.9	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccccc2)c1Br	10.1016/S0960-894X(97)00367-3
	10503334	180123	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	441	5	2	6	3.9	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccccc2)c1Br	10.1021/jm9608366
	CHEMBL45269	180123	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	441	5	2	6	3.9	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccccc2)c1Br	10.1021/jm9608366
	10140871	66025	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	484	9	2	9	3.0	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)ncnc1OCC#CCO	10.1016/s0960-894x(02)01084-3
	CHEMBL170342	66025	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	484	9	2	9	3.0	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)ncnc1OCC#CCO	10.1016/s0960-894x(02)01084-3
	44383754	66657	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	452	5	1	5	5.4	Cc1ccc(/C=C/c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1	10.1016/S0960-894X(97)00133-9
	CHEMBL172987	66657	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	452	5	1	5	5.4	Cc1ccc(/C=C/c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1	10.1016/S0960-894X(97)00133-9
	CHEMBL319660	217999	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1021/jm00015a003
	11005243	210160	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	474	8	1	6	5.6	CCCCOc1ccc2c(c1)C(c1ccc(OC)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	CHEMBL65337	210160	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	474	8	1	6	5.6	CCCCOc1ccc2c(c1)C(c1ccc(OC)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	9801093	66010	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	399	7	1	5	5.1	N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1ccccc1Cl	10.1021/jm990378b
	CHEMBL170296	66010	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	399	7	1	5	5.1	N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1ccccc1Cl	10.1021/jm990378b
	44295089	21404	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	476	8	1	7	5.4	COc1ccc(C(=O)/C(Cc2ccc(SC)cc2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1	10.1016/s0960-894x(98)00301-1
	CHEMBL1205088	21404	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	476	8	1	7	5.4	COc1ccc(C(=O)/C(Cc2ccc(SC)cc2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1	10.1016/s0960-894x(98)00301-1
	CHEMBL51030	21404	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	476	8	1	7	5.4	COc1ccc(C(=O)/C(Cc2ccc(SC)cc2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1	10.1016/s0960-894x(98)00301-1
	44320192	113833	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	480	6	1	5	5.9	O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1Cc1cccc(Cl)c1	10.1016/s0960-894x(00)00513-8
	CHEMBL315622	113833	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	480	6	1	5	5.9	O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1Cc1cccc(Cl)c1	10.1016/s0960-894x(00)00513-8
	10504542	186342	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	469	6	2	6	4.4	CCc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1	10.1021/jm9608366
	CHEMBL47418	186342	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	469	6	2	6	4.4	CCc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1	10.1021/jm9608366
	44386536	137491	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	549	10	4	6	4.9	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2ccccc2F)nc1C(=O)O	10.1021/jm950592+
	CHEMBL368461	137491	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	549	10	4	6	4.9	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2ccccc2F)nc1C(=O)O	10.1021/jm950592+
	10626245	137940	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor	ChEMBL	539	10	2	8	5.5	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)OC(=O)OC2CCCCC2)nc1C(=O)O	10.1021/jm9505932
	CHEMBL368629	137940	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor	ChEMBL	539	10	2	8	5.5	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)OC(=O)OC2CCCCC2)nc1C(=O)O	10.1021/jm9505932
	44311516	210897	0	None	-	1	Human	7.8	pIC50	=	7.8	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	678	12	2	12	5.2	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	CHEMBL70339	210897	0	None	-	1	Human	7.8	pIC50	=	7.8	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	678	12	2	12	5.2	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	137633242	163259	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	569	10	2	10	3.8	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(OCOC)ccc31)OCO2	10.1016/j.bmcl.2017.04.049
	CHEMBL4067475	163259	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	569	10	2	10	3.8	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(OCOC)ccc31)OCO2	10.1016/j.bmcl.2017.04.049
	10599230	213774	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	440	8	2	6	2.8	CCCNC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL9141	213774	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	440	8	2	6	2.8	CCCNC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	71458718	88449	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	615	14	1	12	4.3	COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(C)cn1	10.1021/jm3009103
	CHEMBL2163700	88449	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	615	14	1	12	4.3	COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(C)cn1	10.1021/jm3009103
	44320783	113470	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	453	6	1	6	5.2	O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2cccnc2)nn1CC1CCCCC1	10.1016/s0960-894x(00)00513-8
	CHEMBL314357	113470	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	453	6	1	6	5.2	O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2cccnc2)nn1CC1CCCCC1	10.1016/s0960-894x(00)00513-8
	18995986	106357	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.	ChEMBL	537	8	1	10	5.0	COc1ccc(Sc2c(C(=O)O)n(Cc3cc(OC)c4c(c3)OCO4)c3cc4c(cc23)OCO4)cc1OC	10.1016/0960-894X(96)00232-6
	CHEMBL283858	106357	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.	ChEMBL	537	8	1	10	5.0	COc1ccc(Sc2c(C(=O)O)n(Cc3cc(OC)c4c(c3)OCO4)c3cc4c(cc23)OCO4)cc1OC	10.1016/0960-894X(96)00232-6
	18617379	212003	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	364	3	1	4	3.5	Cc1noc(NS(=O)(=O)c2cccc(Cl)c2C)c1Br	10.1016/0960-894X(96)00441-6
	CHEMBL78669	212003	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	364	3	1	4	3.5	Cc1noc(NS(=O)(=O)c2cccc(Cl)c2C)c1Br	10.1016/0960-894X(96)00441-6
	10622616	14830	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	432	5	1	6	4.5	CSc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1	10.1021/jm9606507
	CHEMBL10911	14830	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	432	5	1	6	4.5	CSc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1	10.1021/jm9606507
	10412464	15909	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	470	6	1	5	5.4	COc1ccc(CC2=C(c3ccc(Cl)c(Cl)c3)C(=O)OC2(O)c2ccc(OC)cc2)cc1	10.1021/jm9606507
	CHEMBL10996	15909	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	470	6	1	5	5.4	COc1ccc(CC2=C(c3ccc(Cl)c(Cl)c3)C(=O)OC2(O)c2ccc(OC)cc2)cc1	10.1021/jm9606507
	11826883	206930	1	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	476	8	1	6	5.5	COc1ccc(C2=C(C(=O)O)C(c3ccc(OC)c(OC)c3)Oc3ccc(OC(C)C)cc32)cc1	10.1021/jm010382z
	CHEMBL59635	206930	1	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	476	8	1	6	5.5	COc1ccc(C2=C(C(=O)O)C(c3ccc(OC)c(OC)c3)Oc3ccc(OC(C)C)cc32)cc1	10.1021/jm010382z
	11017198	115790	0	None	-	0	Pig	6.8	pIC50	=	6.8	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	563	12	1	8	6.0	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOCc2ccccc2)c1	10.1021/jm0102304
	CHEMBL321226	115790	0	None	-	0	Pig	6.8	pIC50	=	6.8	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	563	12	1	8	6.0	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOCc2ccccc2)c1	10.1021/jm0102304
	10765567	118131	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	440	9	1	5	3.4	CCCN(C)C(=O)CN1C[C@H](c2cccc(OC)c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	CHEMBL326951	118131	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	440	9	1	5	3.4	CCCN(C)C(=O)CN1C[C@H](c2cccc(OC)c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	9870117	201665	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	Displacement of 125I-ET1 from ETA receptor in rat A7R5 cellsDisplacement of 125I-ET1 from ETA receptor in rat A7R5 cells	ChEMBL	488	10	1	7	5.5	COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCC=O)c1	10.1016/j.bmcl.2016.06.014
	CHEMBL54057	201665	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	Displacement of 125I-ET1 from ETA receptor in rat A7R5 cellsDisplacement of 125I-ET1 from ETA receptor in rat A7R5 cells	ChEMBL	488	10	1	7	5.5	COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCC=O)c1	10.1016/j.bmcl.2016.06.014
	9870117	201665	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	488	10	1	7	5.5	COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCC=O)c1	10.1016/s0960-894x(00)00366-8
	CHEMBL54057	201665	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	488	10	1	7	5.5	COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCC=O)c1	10.1016/s0960-894x(00)00366-8
	44277367	113615	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	392	4	2	5	3.3	O=c1c(Cc2ccc3c(c2)OCO3)c(C(F)(F)F)[nH]n1Cc1cccc(O)c1	10.1016/s0960-894x(00)00232-8
	CHEMBL3144606	113615	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	392	4	2	5	3.3	O=c1c(Cc2ccc3c(c2)OCO3)c(C(F)(F)F)[nH]n1Cc1cccc(O)c1	10.1016/s0960-894x(00)00232-8
	44387128	175368	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	558	12	2	10	3.8	CNCC(=O)OCCOc1nc(C)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/S0960-894X(97)00400-9
	CHEMBL435895	175368	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	558	12	2	10	3.8	CNCC(=O)OCCOc1nc(C)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/S0960-894X(97)00400-9
	CHEMBL422464	220066	0	None	-	0	Pig	5.8	pIC50	=	5.8	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CCO)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	5310990	173609	11	None	-	1	Rat	6.8	pIC50	=	6.8	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	510	12	1	6	4.7	CCCCN(CCCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL428504	173609	11	None	-	1	Rat	6.8	pIC50	=	6.8	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	510	12	1	6	4.7	CCCCN(CCCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	23445506	119335	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	428	5	1	6	4.3	COc1ccccc1-c1ccsc1S(=O)(=O)Nc1onc(C)c1Br	10.1016/S0960-894X(96)00496-9
	CHEMBL330003	119335	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	428	5	1	6	4.3	COc1ccccc1-c1ccsc1S(=O)(=O)Nc1onc(C)c1Br	10.1016/S0960-894X(96)00496-9
	10452145	104980	0	None	-	0	Rat	4.8	pIC50	=	4.8	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	376	5	1	7	2.9	Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1[N+](=O)[O-]	10.1021/jm00008a013
	CHEMBL27420	104980	0	None	-	0	Rat	4.8	pIC50	=	4.8	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	376	5	1	7	2.9	Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1[N+](=O)[O-]	10.1021/jm00008a013
	10813007	120097	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	440	9	1	5	3.4	CCCN(C)C(=O)CN1C[C@H](c2ccc(OC)cc2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	CHEMBL331577	120097	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	440	9	1	5	3.4	CCCN(C)C(=O)CN1C[C@H](c2ccc(OC)cc2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	44384852	67014	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	544	9	1	8	5.5	C#CCOc1nc(-c2ccncc2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	CHEMBL174094	67014	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	544	9	1	8	5.5	C#CCOc1nc(-c2ccncc2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	10362674	104558	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	385	4	1	5	4.2	Cc1noc(NS(=O)(=O)c2cccc3c(N4CCCCC4)cccc23)c1C	10.1021/jm00008a013
	CHEMBL27178	104558	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	385	4	1	5	4.2	Cc1noc(NS(=O)(=O)c2cccc3c(N4CCCCC4)cccc23)c1C	10.1021/jm00008a013
	10742446	213791	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	456	9	2	7	2.0	COCCNC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL9147	213791	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	456	9	2	7	2.0	COCCNC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	10650638	15956	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	566	13	1	6	4.8	CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(F)c(F)c1	10.1021/jm970101g
	CHEMBL110305	15956	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	566	13	1	6	4.8	CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(F)c(F)c1	10.1021/jm970101g
	10647898	104121	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	466	5	1	6	5.0	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc3ccccc23)cc1	10.1021/jm9606507
	CHEMBL269409	104121	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	466	5	1	6	5.0	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc3ccccc23)cc1	10.1021/jm9606507
	10993781	208128	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	434	7	1	7	5.0	CCCCC1=C(c2nnn[nH]2)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	CHEMBL60440	208128	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	434	7	1	7	5.0	CCCCC1=C(c2nnn[nH]2)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	10896412	209583	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	504	9	1	7	5.6	CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc(OC)cc1OC)O2	10.1021/jm010382z
	CHEMBL62277	209583	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	504	9	1	7	5.6	CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc(OC)cc1OC)O2	10.1021/jm010382z
	15410997	11480	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells	ChEMBL	563	8	1	7	6.3	COc1ccc(C2(OC(=O)N[C@@H](C)c3ccccc3)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1	10.1016/S0960-894X(97)00002-4
	CHEMBL103501	11480	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells	ChEMBL	563	8	1	7	6.3	COc1ccc(C2(OC(=O)N[C@@H](C)c3ccccc3)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1	10.1016/S0960-894X(97)00002-4
	CHEMBL2370534	216648	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1CCCCNC(=O)CC[C@@H](NC(=O)[C@H](CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](N)Cc2ccccc2)C(C)C)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](C)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(N)=O)[C@@H](C)CC)[C@@H](C)CC	10.1021/jm990170q
	151174	209499	45	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cellsDisplacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cells	ChEMBL	605	12	3	13	3.2	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccnc(-c3nn[nH]n3)c2)nc1OCCO	10.1016/j.bmcl.2016.06.014
	CHEMBL61780	209499	45	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cellsDisplacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cells	ChEMBL	605	12	3	13	3.2	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccnc(-c3nn[nH]n3)c2)nc1OCCO	10.1016/j.bmcl.2016.06.014
	76319370	92131	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells	ChEMBL	564	8	1	9	4.0	CCOC(=O)c1ccc2c(C(C(=O)NS(=O)(=O)c3ccc(C)cc3OC)c3ccc4c(c3)OCO4)cn(C)c2c1	10.1007/s00044-004-0021-y
	CHEMBL2261602	92131	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells	ChEMBL	564	8	1	9	4.0	CCOC(=O)c1ccc2c(C(C(=O)NS(=O)(=O)c3ccc(C)cc3OC)c3ccc4c(c3)OCO4)cn(C)c2c1	10.1007/s00044-004-0021-y
	10050696	103553	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	476	7	1	6	5.3	COc1cccc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)c1	10.1016/s0960-894x(00)00513-8
	CHEMBL26474	103553	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	476	7	1	6	5.3	COc1cccc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)c1	10.1016/s0960-894x(00)00513-8
	10050696	103553	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	476	7	1	6	5.3	COc1cccc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)c1	10.1016/s0960-894x(00)00232-8
	CHEMBL26474	103553	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	476	7	1	6	5.3	COc1cccc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)c1	10.1016/s0960-894x(00)00232-8
	10138169	106137	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	440	6	1	8	3.7	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Cc2ccc3c(c2)OCO3)c1Cl	10.1021/jm9700068
	CHEMBL282470	106137	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	440	6	1	8	3.7	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Cc2ccc3c(c2)OCO3)c1Cl	10.1021/jm9700068
	10211772	63297	0	None	-	1	Human	7.8	pIC50	=	7.8	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	660	11	2	12	4.2	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccccc1	10.1016/s0960-894x(02)01084-3
	CHEMBL163638	63297	0	None	-	1	Human	7.8	pIC50	=	7.8	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	660	11	2	12	4.2	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccccc1	10.1016/s0960-894x(02)01084-3
	10165809	138577	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	541	9	2	11	2.0	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCO	10.1016/s0960-894x(02)01084-3
	CHEMBL369362	138577	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	541	9	2	11	2.0	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCO	10.1016/s0960-894x(02)01084-3
	CHEMBL61900	222620	0	None	-	0	Pig	7.8	pIC50	=	7.8	Binding	Inhibition of endothelin (ET-A) binding to porcine heart membranes Inhibition of endothelin (ET-A) binding to porcine heart membranes	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)CNC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/0960-894X(95)00349-X
	44327412	214360	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	497	5	1	8	3.0	Cc1cc(C)c(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c2ccc3c(c2)OCO3)n1	10.1016/S0960-894X(96)00617-8
	CHEMBL94929	214360	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	497	5	1	8	3.0	Cc1cc(C)c(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c2ccc3c(c2)OCO3)n1	10.1016/S0960-894X(96)00617-8
	44385621	134974	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	550	10	5	5	4.6	Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2C)nc1C(=O)O	10.1021/jm950592+
	CHEMBL366544	134974	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	550	10	5	5	4.6	Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2C)nc1C(=O)O	10.1021/jm950592+
	44356917	126019	0	None	-	0	Pig	7.8	pIC50	=	7.8	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL	638	8	5	8	0.3	CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2cn(C=O)c3ccccc23)NC1=O	10.1021/jm00021a021
	CHEMBL343516	126019	0	None	-	0	Pig	7.8	pIC50	=	7.8	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL	638	8	5	8	0.3	CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2cn(C=O)c3ccccc23)NC1=O	10.1021/jm00021a021
	CHEMBL2370825	216707	0	None	-	0	Pig	7.8	pIC50	=	7.8	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2C[C@@H](O)CN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	11091217	107844	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	426	9	1	6	5.0	CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2cc(OCCC)ccc21	10.1021/jm010382z
	CHEMBL294787	107844	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	426	9	1	6	5.0	CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2cc(OCCC)ccc21	10.1021/jm010382z
	44314722	162530	0	None	-	0	Pig	6.8	pIC50	=	6.8	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	597	14	5	4	4.9	CCCCC(NC(=O)[C@@H](Cc1c(CC)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1021/jm9600914
	CHEMBL405724	162530	0	None	-	0	Pig	6.8	pIC50	=	6.8	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	597	14	5	4	4.9	CCCCC(NC(=O)[C@@H](Cc1c(CC)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1021/jm9600914
	CHEMBL293216	217668	0	None	-	0	Pig	6.8	pIC50	=	6.8	Binding	Inhibition of endothelin (ET-A) binding to porcine heart membranes Inhibition of endothelin (ET-A) binding to porcine heart membranes	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/0960-894X(95)00349-X
	44283421	106933	0	None	-	0	Pig	6.8	pIC50	=	6.8	Binding	Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	597	14	5	4	4.9	CCCC[C@H](NC(=O)[C@@H](Cc1c(CC)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1016/0960-894X(95)00237-N
	CHEMBL287888	106933	0	None	-	0	Pig	6.8	pIC50	=	6.8	Binding	Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	597	14	5	4	4.9	CCCC[C@H](NC(=O)[C@@H](Cc1c(CC)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1016/0960-894X(95)00237-N
	44383742	175284	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	452	5	1	5	5.4	Cc1ccc(/C=C/c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1	10.1016/S0960-894X(97)00133-9
	CHEMBL435346	175284	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	452	5	1	5	5.4	Cc1ccc(/C=C/c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1	10.1016/S0960-894X(97)00133-9
	CHEMBL137361	215523	0	None	-	0	Pig	6.8	pIC50	=	6.8	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	CHEMBL313382	217892	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00070a001
	CHEMBL86814	222671	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00070a001
	44368819	175671	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)	ChEMBL	1637	31	19	20	1.7	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)NCCCCCCCC(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)80156-6
	77282140	175671	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)	ChEMBL	1637	31	19	20	1.7	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)NCCCCCCCC(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)80156-6
	CHEMBL438380	175671	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)	ChEMBL	1637	31	19	20	1.7	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)NCCCCCCCC(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)80156-6
	44316973	212384	2	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	330	3	1	4	2.9	Cc1noc(NS(=O)(=O)c2cccc(Br)c2)c1C	10.1016/0960-894X(96)00441-6
	CHEMBL81593	212384	2	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	330	3	1	4	2.9	Cc1noc(NS(=O)(=O)c2cccc(Br)c2)c1C	10.1016/0960-894X(96)00441-6
	127035067	143170	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	683	12	2	9	5.4	CCCc1nc2c(C)cc(C(=O)NCCN3CCN(C)CC3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	CHEMBL3735236	143170	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	683	12	2	9	5.4	CCCc1nc2c(C)cc(C(=O)NCCN3CCN(C)CC3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	44368824	103602	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	In vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricleIn vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricle	ChEMBL	1595	31	19	20	0.6	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)NCCCCC(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)80156-6
	77282142	103602	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	In vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricleIn vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricle	ChEMBL	1595	31	19	20	0.6	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)NCCCCC(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)80156-6
	CHEMBL265164	103602	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	In vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricleIn vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricle	ChEMBL	1595	31	19	20	0.6	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)NCCCCC(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)80156-6
	CHEMBL436899	220473	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	In vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricleIn vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricle	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)80156-6
	44277034	113620	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	406	5	1	5	3.6	COc1ccccc1Cn1[nH]c(C(F)(F)F)c(Cc2ccc3c(c2)OCO3)c1=O	10.1016/s0960-894x(00)00232-8
	CHEMBL3144729	113620	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	406	5	1	5	3.6	COc1ccccc1Cn1[nH]c(C(F)(F)F)c(Cc2ccc3c(c2)OCO3)c1=O	10.1016/s0960-894x(00)00232-8
	CHEMBL1791279	215698	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Inhibition of [125I]endothelin-1 [ET-1] binding to endothelin A receptor (ETA) of rabbit renal artery vascular smooth muscle cellsInhibition of [125I]endothelin-1 [ET-1] binding to endothelin A receptor (ETA) of rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)[C@H](C)CC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/0960-894X(95)00152-J
	CHEMBL5272983	200522	0	None	-	0	Human	4.8	pIC50	=	4.8	Binding	Binding affinity to recombinant human ETABinding affinity to recombinant human ETA	ChEMBL	439	7	2	6	3.3	O=S(=O)(Nc1ncnc(OCCO)c1-c1ccccc1)c1ccc(C(F)(F)F)cc1	10.1021/acs.jmedchem.0c01093
	19735343	182830	0	None	-	1	Human	4.8	pIC50	=	4.8	Binding	Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes	ChEMBL	473	7	2	6	4.0	O=S(=O)(Nc1ncnc(OCCO)c1-c1ccc(Cl)cc1)c1ccc(C(F)(F)F)cc1	10.1016/j.bmcl.2016.06.014
	CHEMBL4590568	182830	0	None	-	1	Human	4.8	pIC50	=	4.8	Binding	Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes	ChEMBL	473	7	2	6	4.0	O=S(=O)(Nc1ncnc(OCCO)c1-c1ccc(Cl)cc1)c1ccc(C(F)(F)F)cc1	10.1016/j.bmcl.2016.06.014
	23445516	113405	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	468	7	1	5	5.9	Cc1noc(NS(=O)(=O)c2sccc2-c2ccc(CCC(C)C)cc2)c1Br	10.1016/S0960-894X(96)00496-9
	CHEMBL314307	113405	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	468	7	1	5	5.9	Cc1noc(NS(=O)(=O)c2sccc2-c2ccc(CCC(C)C)cc2)c1Br	10.1016/S0960-894X(96)00496-9
	23445354	213414	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	426	5	1	5	4.8	CCc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1	10.1016/S0960-894X(96)00496-9
	CHEMBL89203	213414	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	426	5	1	5	4.8	CCc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1	10.1016/S0960-894X(96)00496-9
	CHEMBL273391	217588	0	None	-	0	Human	4.7	pIC50	=	4.7	Binding	Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00070a001
	CHEMBL273391	217588	0	None	-	0	Human	4.7	pIC50	=	4.7	Binding	Displacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cellsDisplacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)81215-4
	18184206	67106	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	600	13	2	11	3.2	CCS(=O)(=O)NCCOc1nc(-c2ccncc2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	CHEMBL174413	67106	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	600	13	2	11	3.2	CCS(=O)(=O)NCCOc1nc(-c2ccncc2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	44385792	67125	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	617	13	2	11	4.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(C2CC2)nc1OCCNS(=O)(=O)c1cccs1	10.1016/s0960-894x(02)01083-1
	CHEMBL174547	67125	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	617	13	2	11	4.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(C2CC2)nc1OCCNS(=O)(=O)c1cccs1	10.1016/s0960-894x(02)01083-1
	44384966	66771	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	545	9	1	9	4.8	C#CCOc1nc(-c2cnccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	CHEMBL173465	66771	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	545	9	1	9	4.8	C#CCOc1nc(-c2cnccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	71460537	88472	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	660	12	1	13	2.7	COc1ccccc1Oc1c(NS(=O)(=O)N2CCOCC2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1	10.1021/jm3009103
	CHEMBL2163722	88472	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	660	12	1	13	2.7	COc1ccccc1Oc1c(NS(=O)(=O)N2CCOCC2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1	10.1021/jm3009103
	10765057	169939	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	430	4	1	7	3.5	O=C1OC(O)(c2ccc3c(c2)OCO3)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2	10.1021/jm9606507
	CHEMBL417978	169939	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	430	4	1	7	3.5	O=C1OC(O)(c2ccc3c(c2)OCO3)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2	10.1021/jm9606507
	CHEMBL2304012	216247	0	None	-	0	Pig	7.7	pIC50	=	7.7	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)[C@H]1NC(=O)[C@H](C2CCCC2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc2c(Br)[nH]c3ccccc23)NC1=O	10.1021/jm9600914
	44458399	105768	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	520	7	2	7	4.2	CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(CO)ccc23)cc1	10.1016/s0960-894x(01)00660-6
	CHEMBL279947	105768	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	520	7	2	7	4.2	CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(CO)ccc23)cc1	10.1016/s0960-894x(01)00660-6
	73669992	124409	0	None	-	0	Rat	7.7	pIC50	=	7.7	Binding	Displacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry method	ChEMBL	387	9	1	4	5.4	N#CCCC(Oc1cc(OCc2ccccc2)ccc1C(=O)O)c1ccccc1	10.1016/j.bmc.2015.01.003
	CHEMBL3400998	124409	0	None	-	0	Rat	7.7	pIC50	=	7.7	Binding	Displacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry method	ChEMBL	387	9	1	4	5.4	N#CCCC(Oc1cc(OCc2ccccc2)ccc1C(=O)O)c1ccccc1	10.1016/j.bmc.2015.01.003
	10814776	106249	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	485	5	2	8	3.6	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc3c(c2)OCO3)c1Br	10.1021/jm9608366
	10814776	106249	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	485	5	2	8	3.6	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc3c(c2)OCO3)c1Br	10.1021/jm9700068
	CHEMBL283136	106249	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	485	5	2	8	3.6	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc3c(c2)OCO3)c1Br	10.1021/jm9608366
	CHEMBL283136	106249	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	485	5	2	8	3.6	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc3c(c2)OCO3)c1Br	10.1021/jm9700068
	44387111	172961	0	None	-	0	Rat	7.7	pIC50	=	7.7	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	548	10	5	5	4.2	Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CC3CCC2C3)nc1C(=O)O	10.1021/jm950592+
	CHEMBL426413	172961	0	None	-	0	Rat	7.7	pIC50	=	7.7	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	548	10	5	5	4.2	Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CC3CCC2C3)nc1C(=O)O	10.1021/jm950592+
	9830773	137004	0	None	-	2	Human	7.7	pIC50	=	7.7	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	636	14	2	12	2.8	CCS(=O)(=O)NCCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	CHEMBL367958	137004	0	None	-	2	Human	7.7	pIC50	=	7.7	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	636	14	2	12	2.8	CCS(=O)(=O)NCCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	10814776	106249	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor	ChEMBL	485	5	2	8	3.6	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc3c(c2)OCO3)c1Br	10.1021/jm000349x
	CHEMBL283136	106249	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor	ChEMBL	485	5	2	8	3.6	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc3c(c2)OCO3)c1Br	10.1021/jm000349x
	CHEMBL341994	218440	0	None	-	0	Pig	7.7	pIC50	=	7.7	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C2=CCC=CC2)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	10410546	16184	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	432	7	1	6	4.1	COc1ccc(CC2=C(c3ccc(OC)cc3)C(=O)OC2(O)c2ccc(OC)cc2)cc1	10.1021/jm9606507
	CHEMBL11162	16184	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	432	7	1	6	4.1	COc1ccc(CC2=C(c3ccc(OC)cc3)C(=O)OC2(O)c2ccc(OC)cc2)cc1	10.1021/jm9606507
	44279481	119160	0	None	-	0	Pig	6.7	pIC50	=	6.7	Binding	Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	555	11	5	4	4.0	CC(C)C[C@H](NC(=O)N1C(C)(C)CCCC1(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	CHEMBL32959	119160	0	None	-	0	Pig	6.7	pIC50	=	6.7	Binding	Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	555	11	5	4	4.0	CC(C)C[C@H](NC(=O)N1C(C)(C)CCCC1(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	10674095	120290	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	544	9	1	6	5.1	CCc1cccc(CC)c1N(C)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm990170q
	CHEMBL332093	120290	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	544	9	1	6	5.1	CCc1cccc(CC)c1N(C)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm990170q
	CHEMBL135906	215513	0	None	-	0	Pig	6.7	pIC50	=	6.7	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	44316983	111573	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	312	5	1	6	2.1	COc1ccc(S(=O)(=O)Nc2onc(C)c2C)cc1OC	10.1016/0960-894X(96)00441-6
	CHEMBL310944	111573	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	312	5	1	6	2.1	COc1ccc(S(=O)(=O)Nc2onc(C)c2C)cc1OC	10.1016/0960-894X(96)00441-6
	44371670	148441	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Binding affinity in LtK cells stably transfected with human endothelin A (ETA) receptorBinding affinity in LtK cells stably transfected with human endothelin A (ETA) receptor	ChEMBL	1082	23	11	10	3.7	CC(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)C1c2ccccc2CCc2ccccc21	10.1016/0960-894X(95)00084-7
	CHEMBL385405	148441	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Binding affinity in LtK cells stably transfected with human endothelin A (ETA) receptorBinding affinity in LtK cells stably transfected with human endothelin A (ETA) receptor	ChEMBL	1082	23	11	10	3.7	CC(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)C1c2ccccc2CCc2ccccc21	10.1016/0960-894X(95)00084-7
	44277035	113629	0	None	-	0	Rat	5.7	pIC50	=	5.7	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	410	4	1	4	4.2	O=c1c(Cc2ccc3c(c2)OCO3)c(C(F)(F)F)[nH]n1Cc1cccc(Cl)c1	10.1016/s0960-894x(00)00232-8
	CHEMBL3144806	113629	0	None	-	0	Rat	5.7	pIC50	=	5.7	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	410	4	1	4	4.2	O=c1c(Cc2ccc3c(c2)OCO3)c(C(F)(F)F)[nH]n1Cc1cccc(Cl)c1	10.1016/s0960-894x(00)00232-8
	10554385	66989	0	None	-	0	Rat	5.7	pIC50	=	5.7	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	537	10	4	5	4.8	CCc1oc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O	10.1021/jm950591h
	CHEMBL174000	66989	0	None	-	0	Rat	5.7	pIC50	=	5.7	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	537	10	4	5	4.8	CCc1oc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O	10.1021/jm950591h
	10721963	67333	0	None	-	0	Rat	5.7	pIC50	=	5.7	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	580	11	5	6	3.7	Cc1oc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)NCC(=O)O	10.1021/jm950592+
	CHEMBL175924	67333	0	None	-	0	Rat	5.7	pIC50	=	5.7	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	580	11	5	6	3.7	Cc1oc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)NCC(=O)O	10.1021/jm950592+
	44386620	177384	0	None	-	0	Rat	5.7	pIC50	=	5.7	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	549	10	4	6	4.9	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2ccc(F)cc2)nc1C(=O)O	10.1021/jm950592+
	CHEMBL445076	177384	0	None	-	0	Rat	5.7	pIC50	=	5.7	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	549	10	4	6	4.9	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2ccc(F)cc2)nc1C(=O)O	10.1021/jm950592+
	44311218	109904	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	607	11	2	10	5.7	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCOC(=O)Nc1ccncc1	10.1016/S0960-894X(97)00400-9
	CHEMBL307803	109904	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	607	11	2	10	5.7	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCOC(=O)Nc1ccncc1	10.1016/S0960-894X(97)00400-9
	18617344	212057	0	None	-	0	Human	4.7	pIC50	=	4.7	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	361	4	1	6	2.5	Cc1noc(NS(=O)(=O)c2ccc([N+](=O)[O-])cc2)c1Br	10.1016/0960-894X(96)00441-6
	CHEMBL79080	212057	0	None	-	0	Human	4.7	pIC50	=	4.7	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	361	4	1	6	2.5	Cc1noc(NS(=O)(=O)c2ccc([N+](=O)[O-])cc2)c1Br	10.1016/0960-894X(96)00441-6
	15342056	213792	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	322	3	1	5	2.6	Cc1noc(NS(=O)(=O)c2cccs2)c1Br	10.1016/S0960-894X(96)00496-9
	CHEMBL91470	213792	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	322	3	1	5	2.6	Cc1noc(NS(=O)(=O)c2cccs2)c1Br	10.1016/S0960-894X(96)00496-9
	10503976	18010	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	455	5	1	6	3.9	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)N(C)c2ccccc2)c1Br	10.1021/jm9608366
	CHEMBL1178874	18010	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	455	5	1	6	3.9	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)N(C)c2ccccc2)c1Br	10.1021/jm9608366
	CHEMBL47536	18010	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	455	5	1	6	3.9	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)N(C)c2ccccc2)c1Br	10.1021/jm9608366
	10211543	138163	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	640	13	2	12	3.5	CCCCNC(=O)OCC#CCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	CHEMBL368989	138163	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	640	13	2	12	3.5	CCCCNC(=O)OCC#CCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	10341117	169976	1	None	-	0	Rat	5.7	pIC50	=	5.7	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	403	8	3	6	3.5	Cc1noc(NS(=O)(=O)c2cccc3c(NCCCC(=O)O)cccc23)c1C	10.1021/jm00008a013
	CHEMBL418202	169976	1	None	-	0	Rat	5.7	pIC50	=	5.7	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	403	8	3	6	3.5	Cc1noc(NS(=O)(=O)c2cccc3c(NCCCC(=O)O)cccc23)c1C	10.1021/jm00008a013
	10554085	108064	0	None	-	0	Human	4.7	pIC50	=	4.7	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	524	6	1	9	3.2	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)N2CCN(Cc3ccc4c(c3)OCO4)CC2)c1Cl	10.1021/jm9700068
	CHEMBL296427	108064	0	None	-	0	Human	4.7	pIC50	=	4.7	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	524	6	1	9	3.2	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)N2CCN(Cc3ccc4c(c3)OCO4)CC2)c1Cl	10.1021/jm9700068
	10817024	18900	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	578	10	2	6	5.2	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NCC(c2ccccc2)c2ccccc2)cc1	10.1021/jm990171i
	CHEMBL1184112	18900	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	578	10	2	6	5.2	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NCC(c2ccccc2)c2ccccc2)cc1	10.1021/jm990171i
	CHEMBL332808	18900	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	578	10	2	6	5.2	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NCC(c2ccccc2)c2ccccc2)cc1	10.1021/jm990171i
	44279140	117409	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors	ChEMBL	588	12	2	6	5.8	CCCCCNC(=O)c1cccc(S(=O)(=O)Nc2ncc(Br)nc2OC)c1-c1ccc(CC(C)C)cc1	10.1016/S0960-894X(97)00228-X
	CHEMBL32574	117409	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors	ChEMBL	588	12	2	6	5.8	CCCCCNC(=O)c1cccc(S(=O)(=O)Nc2ncc(Br)nc2OC)c1-c1ccc(CC(C)C)cc1	10.1016/S0960-894X(97)00228-X
	11793037	210486	3	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	362	4	1	5	3.2	CN(C)c1cccc2c(S(=O)(=O)Nc3ccc(Cl)nn3)cccc12	10.1021/jm9604585
	CHEMBL6761	210486	3	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	362	4	1	5	3.2	CN(C)c1cccc2c(S(=O)(=O)Nc3ccc(Cl)nn3)cccc12	10.1021/jm9604585
	9885296	103744	1	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	361	4	1	4	3.8	CN(C)c1cccc2c(S(=O)(=O)Nc3ccc(Cl)cn3)cccc12	10.1021/jm9604585
	CHEMBL266315	103744	1	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	361	4	1	4	3.8	CN(C)c1cccc2c(S(=O)(=O)Nc3ccc(Cl)cn3)cccc12	10.1021/jm9604585
	10786783	210214	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	393	4	1	5	3.2	COc1nc(Br)cnc1NS(=O)(=O)c1cccc2ccccc12	10.1021/jm9604585
	CHEMBL6576	210214	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	393	4	1	5	3.2	COc1nc(Br)cnc1NS(=O)(=O)c1cccc2ccccc12	10.1021/jm9604585
	10740137	210292	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	406	4	1	5	3.3	CN(C)c1cccc2c(S(=O)(=O)Nc3ncc(Br)cn3)cccc12	10.1021/jm9604585
	CHEMBL6630	210292	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	406	4	1	5	3.3	CN(C)c1cccc2c(S(=O)(=O)Nc3ncc(Br)cn3)cccc12	10.1021/jm9604585
	10230836	15681	0	None	-	0	Rat	8.7	pIC50	=	8.7	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	546	13	1	7	4.1	CCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm970101g
	CHEMBL109765	15681	0	None	-	0	Rat	8.7	pIC50	=	8.7	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	546	13	1	7	4.1	CCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm970101g
	10209319	16142	0	None	-	0	Rat	8.7	pIC50	=	8.7	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	546	13	1	7	4.1	CCCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CCC	10.1021/jm970101g
	CHEMBL111355	16142	0	None	-	0	Rat	8.7	pIC50	=	8.7	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	546	13	1	7	4.1	CCCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CCC	10.1021/jm970101g
	10507211	117148	0	None	-	0	Rat	8.7	pIC50	=	8.7	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	566	13	1	7	3.9	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CCCCl	10.1021/jm970101g
	CHEMBL324214	117148	0	None	-	0	Rat	8.7	pIC50	=	8.7	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	566	13	1	7	3.9	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CCCCl	10.1021/jm970101g
	9807691	106840	0	None	-	1	Human	8.7	pIC50	=	8.7	Binding	Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.	ChEMBL	553	10	1	10	5.3	COc1cc2c(Sc3cc(OC)c(OC)c(OC)c3)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC	10.1016/0960-894X(96)00232-6
	CHEMBL287169	106840	0	None	-	1	Human	8.7	pIC50	=	8.7	Binding	Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.	ChEMBL	553	10	1	10	5.3	COc1cc2c(Sc3cc(OC)c(OC)c(OC)c3)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC	10.1016/0960-894X(96)00232-6
	11732669	209896	0	None	-	0	Rat	8.7	pIC50	=	8.7	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	426	9	1	6	5.0	CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OCCC)cc21	10.1021/jm010382z
	CHEMBL64039	209896	0	None	-	0	Rat	8.7	pIC50	=	8.7	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	426	9	1	6	5.0	CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OCCC)cc21	10.1021/jm010382z
	10602267	15359	0	None	-	0	Rat	8.7	pIC50	=	8.7	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	529	13	1	6	3.7	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCN1CCCCC1=O	10.1021/jm980217s
	CHEMBL109478	15359	0	None	-	0	Rat	8.7	pIC50	=	8.7	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	529	13	1	6	3.7	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCN1CCCCC1=O	10.1021/jm980217s
	44332842	116498	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells	ChEMBL	703	11	1	10	7.5	COc1ccc(C2(OC(=O)N[C@@H](C)c3cccc4ccccc34)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1	10.1016/S0960-894X(97)00002-4
	CHEMBL322920	116498	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells	ChEMBL	703	11	1	10	7.5	COc1ccc(C2(OC(=O)N[C@@H](C)c3cccc4ccccc34)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1	10.1016/S0960-894X(97)00002-4
	44315009	109983	0	None	-	0	Pig	8.7	pIC50	=	8.7	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	665	13	5	5	4.7	CSCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1021/jm9600914
	CHEMBL308403	109983	0	None	-	0	Pig	8.7	pIC50	=	8.7	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	665	13	5	5	4.7	CSCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1021/jm9600914
	10791702	202595	0	None	-	0	Rat	8.7	pIC50	=	8.7	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	506	12	1	5	5.7	CCCCN(CCCC)C(=O)CN1C[C@H](c2cccc3occc23)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	CHEMBL558148	202595	0	None	-	0	Rat	8.7	pIC50	=	8.7	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	506	12	1	5	5.7	CCCCN(CCCC)C(=O)CN1C[C@H](c2cccc3occc23)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	9895957	17445	18	None	3	3	Human	8.7	pIC50	=	8.7	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	659	11	1	7	6.8	CCCCC1=NC2(CCCC2)C(=O)N1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(CN2CCC(C)(C)C2=O)c1	10.1039/C4MD00499J
	CHEMBL11706	17445	18	None	3	3	Human	8.7	pIC50	=	8.7	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	659	11	1	7	6.8	CCCCC1=NC2(CCCC2)C(=O)N1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(CN2CCC(C)(C)C2=O)c1	10.1039/C4MD00499J
	21041288	180705	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	526	10	2	9	2.8	CNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Br)cc1	10.1016/j.bmcl.2016.06.014
	CHEMBL4540866	180705	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	526	10	2	9	2.8	CNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Br)cc1	10.1016/j.bmcl.2016.06.014
	155563100	182055	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	619	13	2	10	4.6	COc1cnc(OCCOc2nc(-c3ccncc3)nc(NS(=O)(=O)NCc3ccccc3)c2-c2ccc(Cl)cc2)nc1	10.1016/j.bmcl.2016.06.014
	CHEMBL4572734	182055	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	619	13	2	10	4.6	COc1cnc(OCCOc2nc(-c3ccncc3)nc(NS(=O)(=O)NCc3ccccc3)c2-c2ccc(Cl)cc2)nc1	10.1016/j.bmcl.2016.06.014
	9829478	182104	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	567	10	1	8	4.9	Cc1ccc(-c2c(NS(=O)(=O)/C=C/c3ccccc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1016/j.bmcl.2016.06.014
	CHEMBL4573806	182104	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	567	10	1	8	4.9	Cc1ccc(-c2c(NS(=O)(=O)/C=C/c3ccccc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1016/j.bmcl.2016.06.014
	10146377	67188	0	None	-	1	Human	8.7	pIC50	=	8.7	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	662	11	2	14	3.0	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1cnccn1	10.1016/s0960-894x(02)01084-3
	CHEMBL175058	67188	0	None	-	1	Human	8.7	pIC50	=	8.7	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	662	11	2	14	3.0	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1cnccn1	10.1016/s0960-894x(02)01084-3
	10816682	108918	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	559	10	1	9	3.9	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OCCCN3CCOCC3)c2)cc1	10.1021/jm980504w
	CHEMBL302493	108918	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	559	10	1	9	3.9	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OCCCN3CCOCC3)c2)cc1	10.1021/jm980504w
	10579885	109484	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	632	12	1	11	3.9	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCN3CCN(C)CC3)c2)cc1	10.1021/jm980504w
	CHEMBL304802	109484	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	632	12	1	11	3.9	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCN3CCN(C)CC3)c2)cc1	10.1021/jm980504w
	10814440	104923	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	476	7	1	8	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)ccc2OC)cc1	10.1021/jm9606507
	CHEMBL273723	104923	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	476	7	1	8	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)ccc2OC)cc1	10.1021/jm9606507
	71462247	88473	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	680	14	2	12	4.2	COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(-c2cnccn2)nc1OCCOc1ncc(Br)cn1	10.1021/jm3009103
	CHEMBL2163723	88473	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	680	14	2	12	4.2	COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(-c2cnccn2)nc1OCCOc1ncc(Br)cn1	10.1021/jm3009103
	23548253	88451	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)	ChEMBL	679	14	1	12	4.7	COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1	10.1016/j.bmcl.2016.06.014
	CHEMBL2163702	88451	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)	ChEMBL	679	14	1	12	4.7	COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1	10.1016/j.bmcl.2016.06.014
	11014820	209691	0	None	-	0	Rat	8.7	pIC50	=	8.7	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	398	6	1	6	4.2	CCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	CHEMBL62780	209691	0	None	-	0	Rat	8.7	pIC50	=	8.7	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	398	6	1	6	4.2	CCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	10602183	16011	0	None	-	0	Rat	8.7	pIC50	=	8.7	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	525	13	1	7	3.6	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCn1ccccc1=O	10.1021/jm980217s
	CHEMBL110695	16011	0	None	-	0	Rat	8.7	pIC50	=	8.7	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	525	13	1	7	3.6	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCn1ccccc1=O	10.1021/jm980217s
	10625152	117236	0	None	-	0	Rat	8.7	pIC50	=	8.7	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	498	13	1	6	4.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1ccoc1	10.1021/jm980217s
	CHEMBL324685	117236	0	None	-	0	Rat	8.7	pIC50	=	8.7	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	498	13	1	6	4.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1ccoc1	10.1021/jm980217s
	90766557	177307	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	528	10	2	8	3.1	CCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Cl)cc1	10.1016/j.bmcl.2016.06.014
	CHEMBL4449731	177307	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	528	10	2	8	3.1	CCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Cl)cc1	10.1016/j.bmcl.2016.06.014
	76312118	92122	0	None	691	2	Human	8.7	pIC50	=	8.7	Binding	Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells	ChEMBL	522	7	2	8	3.4	COc1cc(C)ccc1S(=O)(=O)NC(=O)[C@@H](c1ccc2c(c1)OCO2)c1cn(C)c2cc(CO)ccc12	10.1007/s00044-004-0021-y
	CHEMBL2261361	92122	0	None	691	2	Human	8.7	pIC50	=	8.7	Binding	Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells	ChEMBL	522	7	2	8	3.4	COc1cc(C)ccc1S(=O)(=O)NC(=O)[C@@H](c1ccc2c(c1)OCO2)c1cn(C)c2cc(CO)ccc12	10.1007/s00044-004-0021-y
	9916121	88442	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	571	10	1	8	4.1	CCCS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1	10.1021/jm3009103
	CHEMBL2163693	88442	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	571	10	1	8	4.1	CCCS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1	10.1021/jm3009103
	23548253	88451	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	679	14	1	12	4.7	COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1	10.1021/jm3009103
	CHEMBL2163702	88451	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	679	14	1	12	4.7	COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1	10.1021/jm3009103
	44334130	11281	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	458	5	1	6	4.4	COc1ccc([C@@H]2c3nc(N4CCCC4)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1	10.1016/s0960-894x(02)00663-7
	CHEMBL102173	11281	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	458	5	1	6	4.4	COc1ccc([C@@H]2c3nc(N4CCCC4)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1	10.1016/s0960-894x(02)00663-7
	9808602	115986	0	None	-	0	Rat	8.6	pIC50	=	8.6	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	590	15	1	8	4.5	CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(OC)c1	10.1021/jm970101g
	CHEMBL321673	115986	0	None	-	0	Rat	8.6	pIC50	=	8.6	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	590	15	1	8	4.5	CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(OC)c1	10.1021/jm970101g
	11826062	209768	0	None	-	0	Rat	8.6	pIC50	=	8.6	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	426	8	2	6	4.3	CC(C)Oc1ccc2c(c1)C(CCCCO)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	CHEMBL63113	209768	0	None	-	0	Rat	8.6	pIC50	=	8.6	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	426	8	2	6	4.3	CC(C)Oc1ccc2c(c1)C(CCCCO)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	10696876	117113	0	None	-	0	Rat	8.6	pIC50	=	8.6	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	504	13	1	7	3.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1OCCO1	10.1021/jm980217s
	CHEMBL323989	117113	0	None	-	0	Rat	8.6	pIC50	=	8.6	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	504	13	1	7	3.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1OCCO1	10.1021/jm980217s
	22467235	103300	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	533	7	2	7	3.8	CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(C(N)=O)ccc23)cc1	10.1016/s0960-894x(01)00660-6
	CHEMBL262784	103300	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	533	7	2	7	3.8	CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(C(N)=O)ccc23)cc1	10.1016/s0960-894x(01)00660-6
	22467235	103300	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells	ChEMBL	533	7	2	7	3.8	CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(C(N)=O)ccc23)cc1	10.1007/s00044-004-0021-y
	CHEMBL262784	103300	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells	ChEMBL	533	7	2	7	3.8	CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(C(N)=O)ccc23)cc1	10.1007/s00044-004-0021-y
	71462321	88782	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	584	12	2	8	4.2	CCc1ccc(-c2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm3009103
	CHEMBL2165335	88782	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	584	12	2	8	4.2	CCc1ccc(-c2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm3009103
	9890440	15026	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	460	6	1	7	4.1	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(OC)c(C)c2)cc1	10.1021/jm9606507
	CHEMBL10924	15026	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	460	6	1	7	4.1	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(OC)c(C)c2)cc1	10.1021/jm9606507
	10577306	116465	0	None	-	0	Rat	8.6	pIC50	=	8.6	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	499	13	1	7	3.9	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1ncco1	10.1021/jm980217s
	CHEMBL322732	116465	0	None	-	0	Rat	8.6	pIC50	=	8.6	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	499	13	1	7	3.9	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1ncco1	10.1021/jm980217s
	44315007	211327	0	None	-	0	Pig	8.6	pIC50	=	8.6	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	679	14	5	5	5.1	CCCSCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1021/jm9600914
	CHEMBL72891	211327	0	None	-	0	Pig	8.6	pIC50	=	8.6	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	679	14	5	5	5.1	CCCSCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1021/jm9600914
	21041273	180527	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	538	12	2	9	2.8	CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(OC)cn2)c1-c1ccc(Br)cc1	10.1016/j.bmcl.2016.06.014
	CHEMBL4536769	180527	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	538	12	2	9	2.8	CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(OC)cn2)c1-c1ccc(Br)cc1	10.1016/j.bmcl.2016.06.014
	9821701	11384	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	389	4	1	5	3.8	COc1ccc([C@@H]2c3ncccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1	10.1016/s0960-894x(02)00663-7
	CHEMBL102825	11384	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	389	4	1	5	3.8	COc1ccc([C@@H]2c3ncccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1	10.1016/s0960-894x(02)00663-7
	10698065	18885	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	558	11	2	6	5.6	CCC(CC)C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1	10.1021/jm990171i
	CHEMBL1184065	18885	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	558	11	2	6	5.6	CCC(CC)C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1	10.1021/jm990171i
	CHEMBL330895	18885	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	558	11	2	6	5.6	CCC(CC)C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1	10.1021/jm990171i
	CHEMBL171198	215625	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1cn(C)c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)O	10.1016/0960-894X(95)00144-I
	10529742	14964	0	None	-	0	Rat	8.6	pIC50	=	8.6	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	511	13	1	6	4.3	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1cccn1C	10.1021/jm980217s
	CHEMBL109206	14964	0	None	-	0	Rat	8.6	pIC50	=	8.6	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	511	13	1	6	4.3	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1cccn1C	10.1021/jm980217s
	10116355	15038	0	None	-	0	Rat	8.6	pIC50	=	8.6	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	474	14	1	5	4.9	CCCCC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC	10.1021/jm980217s
	CHEMBL109248	15038	0	None	-	0	Rat	8.6	pIC50	=	8.6	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	474	14	1	5	4.9	CCCCC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC	10.1021/jm980217s
	10648715	116446	0	None	-	0	Rat	8.6	pIC50	=	8.6	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	488	14	1	5	5.1	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCCC(C)C	10.1021/jm980217s
	CHEMBL322547	116446	0	None	-	0	Rat	8.6	pIC50	=	8.6	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	488	14	1	5	5.1	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCCC(C)C	10.1021/jm980217s
	44320291	112715	0	None	-	0	Rat	8.6	pIC50	=	8.6	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	548	7	2	8	4.8	O=C(O)c1cc2c(c(Cn3nc(-c4ccccc4)c(Cc4cc5c(cc4Cl)OCO5)c3C(=O)O)c1)OCOC2	10.1016/s0960-894x(00)00513-8
	CHEMBL312854	112715	0	None	-	0	Rat	8.6	pIC50	=	8.6	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	548	7	2	8	4.8	O=C(O)c1cc2c(c(Cn3nc(-c4ccccc4)c(Cc4cc5c(cc4Cl)OCO5)c3C(=O)O)c1)OCOC2	10.1016/s0960-894x(00)00513-8
	17885912	113876	0	None	-	0	Rat	8.6	pIC50	=	8.6	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	496	7	2	6	5.1	O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1CC1CCCC(C(=O)O)C1	10.1016/s0960-894x(00)00513-8
	CHEMBL315936	113876	0	None	-	0	Rat	8.6	pIC50	=	8.6	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	496	7	2	6	5.1	O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1CC1CCCC(C(=O)O)C1	10.1016/s0960-894x(00)00513-8
	44279295	112779	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors	ChEMBL	482	8	1	6	4.2	COc1nc(C)cnc1NS(=O)(=O)c1cccc(C(=O)N(C)C)c1-c1ccc(CC(C)C)cc1	10.1016/S0960-894X(97)00228-X
	CHEMBL31324	112779	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors	ChEMBL	482	8	1	6	4.2	COc1nc(C)cnc1NS(=O)(=O)c1cccc(C(=O)N(C)C)c1-c1ccc(CC(C)C)cc1	10.1016/S0960-894X(97)00228-X
	10670600	103351	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	436	6	2	6	3.6	CCNc1cccc2c(S(=O)(=O)Nc3ncc(Br)nc3OC)cccc12	10.1021/jm9604585
	CHEMBL263079	103351	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	436	6	2	6	3.6	CCNc1cccc2c(S(=O)(=O)Nc3ncc(Br)nc3OC)cccc12	10.1021/jm9604585
	10646831	190699	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	441	6	2	7	4.1	COc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1	10.1021/jm9608366
	10646831	190699	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	441	6	2	7	4.1	COc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1	10.1021/jm9700068
	CHEMBL48134	190699	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	441	6	2	7	4.1	COc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1	10.1021/jm9608366
	CHEMBL48134	190699	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	441	6	2	7	4.1	COc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1	10.1021/jm9700068
	11751754	109138	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	469	6	3	7	4.1	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)O)c1	10.1021/jm030528p
	CHEMBL303806	109138	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	469	6	3	7	4.1	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)O)c1	10.1021/jm030528p
	10555516	16013	0	None	-	0	Rat	8.6	pIC50	=	8.6	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	598	12	1	7	4.6	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)Cc1ccccc1	10.1021/jm970101g
	CHEMBL110700	16013	0	None	-	0	Rat	8.6	pIC50	=	8.6	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	598	12	1	7	4.6	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)Cc1ccccc1	10.1021/jm970101g
	11799503	16525	0	None	-	0	Rat	8.6	pIC50	=	8.6	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	498	13	1	6	4.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1ccco1	10.1021/jm980217s
	CHEMBL113472	16525	0	None	-	0	Rat	8.6	pIC50	=	8.6	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	498	13	1	6	4.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1ccco1	10.1021/jm980217s
	10289311	117212	0	None	-	0	Rat	8.6	pIC50	=	8.6	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	514	13	1	5	5.7	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)C=C(C)C	10.1021/jm980217s
	CHEMBL324586	117212	0	None	-	0	Rat	8.6	pIC50	=	8.6	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	514	13	1	5	5.7	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)C=C(C)C	10.1021/jm980217s
	CHEMBL2304007	216242	0	None	-	0	Pig	8.6	pIC50	=	8.6	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		Cc1[nH]c2ccccc2c1C[C@@H]1NC(=O)[C@@H](C(C)C)NC(=O)[C@H](C2CCCC2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC1=O	10.1021/jm9600914
	44380954	64451	0	None	-	0	Pig	8.6	pIC50	=	8.6	Binding	In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.	ChEMBL	643	11	1	10	5.7	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCOc1ncc(Br)cn1	10.1016/s0960-894x(01)00682-5
	CHEMBL166875	64451	0	None	-	0	Pig	8.6	pIC50	=	8.6	Binding	In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.	ChEMBL	643	11	1	10	5.7	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCOc1ncc(Br)cn1	10.1016/s0960-894x(01)00682-5
	10525281	189629	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	404	6	1	6	4.2	Cc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2C)c(C)c1	10.1021/jm9700068
	CHEMBL47915	189629	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	404	6	1	6	4.2	Cc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2C)c(C)c1	10.1021/jm9700068
	9888574	110953	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	422	4	1	4	3.9	CCc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1Br	10.1016/0960-894X(96)00441-6
	CHEMBL309692	110953	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	422	4	1	4	3.9	CCc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1Br	10.1016/0960-894X(96)00441-6
	11102844	210020	0	None	-	0	Rat	8.6	pIC50	=	8.6	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	476	7	2	7	4.2	COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)CO)cc32)cc1	10.1021/jm010382z
	CHEMBL64536	210020	0	None	-	0	Rat	8.6	pIC50	=	8.6	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	476	7	2	7	4.2	COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)CO)cc32)cc1	10.1021/jm010382z
	44314906	110355	0	None	-	0	Pig	8.6	pIC50	=	8.6	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	607	12	6	5	3.4	Cc1[nH]c2ccccc2c1C[C@@H](NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)NC(Cc1c[nH]cn1)C(=O)O	10.1021/jm9600914
	CHEMBL308621	110355	0	None	-	0	Pig	8.6	pIC50	=	8.6	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	607	12	6	5	3.4	Cc1[nH]c2ccccc2c1C[C@@H](NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)NC(Cc1c[nH]cn1)C(=O)O	10.1021/jm9600914
	44458670	105828	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	521	7	2	8	2.7	COc1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(C(N)=O)ccc23)cc1	10.1016/s0960-894x(01)00660-6
	CHEMBL280379	105828	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	521	7	2	8	2.7	COc1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(C(N)=O)ccc23)cc1	10.1016/s0960-894x(01)00660-6
	71455060	88438	1	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	614	9	1	9	2.9	O=S(=O)(Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1)N1CCOCC1	10.1021/jm3009103
	CHEMBL2163689	88438	1	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	614	9	1	9	2.9	O=S(=O)(Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1)N1CCOCC1	10.1021/jm3009103
	71451526	88450	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	635	14	1	12	4.6	COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Cl)cn1	10.1021/jm3009103
	CHEMBL2163701	88450	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	635	14	1	12	4.6	COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Cl)cn1	10.1021/jm3009103
	10875868	121739	0	None	-	0	Pig	8.6	pIC50	=	8.6	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	619	9	1	8	5.0	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(Br)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm0102304
	CHEMBL334263	121739	0	None	-	0	Pig	8.6	pIC50	=	8.6	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	619	9	1	8	5.0	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(Br)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm0102304
	9810190	109843	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	563	11	1	10	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCN(C)C)c2)cc1	10.1021/jm980504w
	CHEMBL307330	109843	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	563	11	1	10	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCN(C)C)c2)cc1	10.1021/jm980504w
	CHEMBL2304015	216250	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Binding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranesBinding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranes	ChEMBL		None	None	None		Cc1[nH]c2ccccc2c1C[C@@H]1NC(=O)[C@@H](C2CC2)NC(=O)[C@H](C2CCCC2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC1=O	10.1021/jm9600914
	10875239	16359	0	None	-	0	Pig	8.5	pIC50	=	8.5	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	541	10	1	10	4.8	CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccco2)nc1	10.1021/jm0102304
	CHEMBL112502	16359	0	None	-	0	Pig	8.5	pIC50	=	8.5	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	541	10	1	10	4.8	CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccco2)nc1	10.1021/jm0102304
	10791823	16221	0	None	-	0	Rat	7.7	pIC50	=	7.7	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	510	12	1	6	4.7	CCCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)C(=O)CCC	10.1021/jm970101g
	CHEMBL111783	16221	0	None	-	0	Rat	7.7	pIC50	=	7.7	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	510	12	1	6	4.7	CCCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)C(=O)CCC	10.1021/jm970101g
	15289330	106578	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.	ChEMBL	493	8	1	8	5.3	COc1cccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc(OC)c(OC)cc23)c1	10.1016/0960-894X(96)00232-6
	CHEMBL285368	106578	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.	ChEMBL	493	8	1	8	5.3	COc1cccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc(OC)c(OC)cc23)c1	10.1016/0960-894X(96)00232-6
	10361107	168827	0	None	-	0	Rat	7.7	pIC50	=	7.7	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	359	5	2	5	4.1	Cc1noc(NS(=O)(=O)c2cccc3c(NC(C)C)cccc23)c1C	10.1021/jm00008a013
	CHEMBL416026	168827	0	None	-	0	Rat	7.7	pIC50	=	7.7	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	359	5	2	5	4.1	Cc1noc(NS(=O)(=O)c2cccc3c(NC(C)C)cccc23)c1C	10.1021/jm00008a013
	44314658	211947	0	None	-	0	Pig	7.7	pIC50	=	7.7	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	589	13	5	4	4.7	CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(CCC)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1021/jm9600914
	CHEMBL78230	211947	0	None	-	0	Pig	7.7	pIC50	=	7.7	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	589	13	5	4	4.7	CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(CCC)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1021/jm9600914
	9951753	173116	0	None	-	0	Rat	7.7	pIC50	=	7.7	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	379	7	1	5	4.7	Cc1ccccc1C(Oc1cc(OCc2ccsc2)ccc1C#N)C(=O)O	10.1021/jm990378b
	CHEMBL427294	173116	0	None	-	0	Rat	7.7	pIC50	=	7.7	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	379	7	1	5	4.7	Cc1ccccc1C(Oc1cc(OCc2ccsc2)ccc1C#N)C(=O)O	10.1021/jm990378b
	11797717	213840	0	None	-	0	Rat	7.7	pIC50	=	7.7	Binding	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	ChEMBL	448	10	2	5	6.0	Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1-c1cc[nH]n1	10.1021/jm9707131
	CHEMBL91753	213840	0	None	-	0	Rat	7.7	pIC50	=	7.7	Binding	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	ChEMBL	448	10	2	5	6.0	Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1-c1cc[nH]n1	10.1021/jm9707131
	10668808	213940	0	None	-	0	Rat	7.7	pIC50	=	7.7	Binding	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	ChEMBL	402	9	1	5	4.8	Cc1ccccc1[C@@H](CCC(=O)O)Oc1cc(OCc2ccncc2)ccc1C#N	10.1021/jm9707131
	CHEMBL92353	213940	0	None	-	0	Rat	7.7	pIC50	=	7.7	Binding	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	ChEMBL	402	9	1	5	4.8	Cc1ccccc1[C@@H](CCC(=O)O)Oc1cc(OCc2ccncc2)ccc1C#N	10.1021/jm9707131
	10694804	214599	0	None	-	0	Rat	7.7	pIC50	=	7.7	Binding	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	ChEMBL	449	10	1	6	6.3	Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1-c1ncco1	10.1021/jm9707131
	CHEMBL96301	214599	0	None	-	0	Rat	7.7	pIC50	=	7.7	Binding	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	ChEMBL	449	10	1	6	6.3	Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1-c1ncco1	10.1021/jm9707131
	10695071	107935	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	454	6	1	6	4.3	Cc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1	10.1021/jm9700068
	CHEMBL295477	107935	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	454	6	1	6	4.3	Cc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1	10.1021/jm9700068
	10672494	186332	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	483	6	2	6	5.0	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc(C(C)C)cc2)c1Br	10.1021/jm9608366
	CHEMBL47417	186332	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	483	6	2	6	5.0	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc(C(C)C)cc2)c1Br	10.1021/jm9608366
	44327412	214360	0	None	-	0	Rat	7.7	pIC50	=	7.7	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	497	5	1	8	3.0	Cc1cc(C)c(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c2ccc3c(c2)OCO3)n1	10.1016/S0960-894X(96)00617-8
	CHEMBL94929	214360	0	None	-	0	Rat	7.7	pIC50	=	7.7	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	497	5	1	8	3.0	Cc1cc(C)c(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c2ccc3c(c2)OCO3)n1	10.1016/S0960-894X(96)00617-8
	CHEMBL343062	218475	0	None	-	0	Pig	7.7	pIC50	=	7.7	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CSCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	443289	7498	47	None	2	3	Human	7.7	pIC50	=	7.7	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL		None	None	None		None	10.1021/jm3009103
	997	7498	47	None	2	3	Human	7.7	pIC50	=	7.7	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL		None	None	None		None	10.1021/jm3009103
	CHEMBL314691	7498	47	None	2	3	Human	7.7	pIC50	=	7.7	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL		None	None	None		None	10.1021/jm3009103
	DB12054	7498	47	None	2	3	Human	7.7	pIC50	=	7.7	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL		None	None	None		None	10.1021/jm3009103
	44320431	113733	0	None	-	0	Rat	7.7	pIC50	=	7.7	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	526	9	2	7	4.9	O=C(O)COC1CCCCC1Cn1nc(-c2ccccc2)c(Cc2cc3c(cc2Cl)OCO3)c1C(=O)O	10.1016/s0960-894x(00)00513-8
	CHEMBL314973	113733	0	None	-	0	Rat	7.7	pIC50	=	7.7	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	526	9	2	7	4.9	O=C(O)COC1CCCCC1Cn1nc(-c2ccccc2)c(Cc2cc3c(cc2Cl)OCO3)c1C(=O)O	10.1016/s0960-894x(00)00513-8
	10767442	138001	0	None	-	0	Rat	6.7	pIC50	=	6.7	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	492	8	1	5	6.1	COc1ccc(C(=O)/C(Cc2ccc(-c3ccccc3)cc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1	10.1021/jm031041j
	CHEMBL368668	138001	0	None	-	0	Rat	6.7	pIC50	=	6.7	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	492	8	1	5	6.1	COc1ccc(C(=O)/C(Cc2ccc(-c3ccccc3)cc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1	10.1021/jm031041j
	CHEMBL313984	217902	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00070a001
	CHEMBL265116	217414	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1021/jm00015a003
	10815005	16520	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	492	6	1	6	5.5	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(-c3ccccc3)cc2)cc1	10.1021/jm9606507
	CHEMBL11345	16520	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	492	6	1	6	5.5	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(-c3ccccc3)cc2)cc1	10.1021/jm9606507
	10506430	120567	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	532	9	2	7	4.5	CCc1cccc(OC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm990170q
	CHEMBL332387	120567	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	532	9	2	7	4.5	CCc1cccc(OC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm990170q
	10669001	119399	0	None	-	0	Rat	6.7	pIC50	=	6.7	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	405	6	1	6	4.6	N#Cc1ccc(OCc2ccsc2)cc1/C=C(/C(=O)O)c1ccc2c(c1)OCO2	10.1021/jm970847e
	CHEMBL330255	119399	0	None	-	0	Rat	6.7	pIC50	=	6.7	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	405	6	1	6	4.6	N#Cc1ccc(OCc2ccsc2)cc1/C=C(/C(=O)O)c1ccc2c(c1)OCO2	10.1021/jm970847e
	10692108	174949	0	None	-	0	Rat	6.7	pIC50	=	6.7	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	395	6	1	4	5.5	N#Cc1ccc(OCc2ccsc2)cc1/C=C(/C(=O)O)c1ccccc1Cl	10.1021/jm970847e
	CHEMBL433201	174949	0	None	-	0	Rat	6.7	pIC50	=	6.7	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	395	6	1	4	5.5	N#Cc1ccc(OCc2ccsc2)cc1/C=C(/C(=O)O)c1ccccc1Cl	10.1021/jm970847e
	CHEMBL313984	217902	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cellsDisplacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)81215-4
	10577255	182198	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	497	8	2	6	5.2	CCCCc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1	10.1021/jm9608366
	CHEMBL45760	182198	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	497	8	2	6	5.2	CCCCc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1	10.1021/jm9608366
	CHEMBL1793926	215709	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm970161m
	10769045	137995	0	None	-	0	Rat	6.7	pIC50	=	6.7	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	551	10	4	6	5.0	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2(C)CCCCC2)nc1C(=O)O	10.1021/jm950592+
	CHEMBL368641	137995	0	None	-	0	Rat	6.7	pIC50	=	6.7	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	551	10	4	6	5.0	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2(C)CCCCC2)nc1C(=O)O	10.1021/jm950592+
	CHEMBL134562	215509	0	None	-	0	Pig	6.7	pIC50	=	6.7	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	CHEMBL436899	220473	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)80156-6
	CHEMBL407933	219473	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)NC1CCCCC1)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	18617284	211987	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	350	3	1	4	3.2	Cc1noc(NS(=O)(=O)c2ccc(Cl)cc2)c1Br	10.1016/0960-894X(96)00441-6
	CHEMBL78552	211987	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	350	3	1	4	3.2	Cc1noc(NS(=O)(=O)c2ccc(Cl)cc2)c1Br	10.1016/0960-894X(96)00441-6
	44314579	109694	0	None	-	0	Pig	5.7	pIC50	=	5.7	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	580	12	5	5	3.8	CCCCC(NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C)C(=O)O	10.1021/jm9600914
	CHEMBL306123	109694	0	None	-	0	Pig	5.7	pIC50	=	5.7	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	580	12	5	5	3.8	CCCCC(NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C)C(=O)O	10.1021/jm9600914
	10549516	117167	0	None	-	0	Rat	5.7	pIC50	=	5.7	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	410	8	1	4	3.4	CCCN(C)C(=O)CN1C[C@H](c2ccccc2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	CHEMBL324301	117167	0	None	-	0	Rat	5.7	pIC50	=	5.7	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	410	8	1	4	3.4	CCCN(C)C(=O)CN1C[C@H](c2ccccc2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	22010208	213874	0	None	-	0	Rat	5.7	pIC50	=	5.7	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	362	9	1	3	5.3	O=C(O)CCC(Oc1cccc(OCc2ccccc2)c1)c1ccccc1	10.1021/jm970847e
	CHEMBL91965	213874	0	None	-	0	Rat	5.7	pIC50	=	5.7	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	362	9	1	3	5.3	O=C(O)CCC(Oc1cccc(OCc2ccccc2)c1)c1ccccc1	10.1021/jm970847e
	10717670	213974	0	None	-	0	Rat	5.7	pIC50	=	5.7	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	433	7	1	5	5.7	O=C(O)/C(=C/c1cc(OCc2ccsc2)ccc1[N+](=O)[O-])c1c(F)cccc1Cl	10.1021/jm970847e
	CHEMBL92570	213974	0	None	-	0	Rat	5.7	pIC50	=	5.7	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	433	7	1	5	5.7	O=C(O)/C(=C/c1cc(OCc2ccsc2)ccc1[N+](=O)[O-])c1c(F)cccc1Cl	10.1021/jm970847e
	19735404	182600	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Displacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cellsDisplacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cells	ChEMBL	471	9	2	7	3.5	COc1ccccc1Cc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)ncnc1OCCO	10.1016/j.bmcl.2016.06.014
	CHEMBL4584753	182600	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Displacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cellsDisplacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cells	ChEMBL	471	9	2	7	3.5	COc1ccccc1Cc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)ncnc1OCCO	10.1016/j.bmcl.2016.06.014
	10528383	18007	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	470	5	1	8	3.6	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)c2ccc3c(c2)OCO3)c1Br	10.1021/jm9700068
	CHEMBL1178854	18007	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	470	5	1	8	3.6	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)c2ccc3c(c2)OCO3)c1Br	10.1021/jm9700068
	CHEMBL46357	18007	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	470	5	1	8	3.6	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)c2ccc3c(c2)OCO3)c1Br	10.1021/jm9700068
	10604797	109121	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	704	14	1	13	3.3	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OCCN3CCOCC3)c(OC)c(OCCN3CCOCC3)c2)cc1	10.1021/jm980504w
	CHEMBL303712	109121	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	704	14	1	13	3.3	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OCCN3CCOCC3)c(OC)c(OCCN3CCOCC3)c2)cc1	10.1021/jm980504w
	10238141	202630	0	None	-	0	Rat	5.7	pIC50	=	5.7	Binding	Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)	ChEMBL	429	5	1	6	4.2	COc1ccccc1Cn1c(=O)c(C(=O)O)c(-c2ccc3c(c2)OCO3)c2ccccc21	10.1016/S0960-894X(97)00319-3
	CHEMBL55853	202630	0	None	-	0	Rat	5.7	pIC50	=	5.7	Binding	Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)	ChEMBL	429	5	1	6	4.2	COc1ccccc1Cn1c(=O)c(C(=O)O)c(-c2ccc3c(c2)OCO3)c2ccccc21	10.1016/S0960-894X(97)00319-3
	44283270	174660	0	None	-	0	Pig	5.7	pIC50	=	5.7	Binding	Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	580	12	5	5	3.8	CCCC[C@H](NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C)C(=O)O	10.1016/0960-894X(95)00237-N
	CHEMBL431124	174660	0	None	-	0	Pig	5.7	pIC50	=	5.7	Binding	Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	580	12	5	5	3.8	CCCC[C@H](NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C)C(=O)O	10.1016/0960-894X(95)00237-N
	10357554	104340	1	None	-	0	Human	4.7	pIC50	=	4.7	Binding	Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells	ChEMBL	302	3	1	4	3.2	Cc1noc(NS(=O)(=O)c2cccc3ccccc23)c1C	10.1021/jm00029a001
	CHEMBL27065	104340	1	None	-	0	Human	4.7	pIC50	=	4.7	Binding	Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells	ChEMBL	302	3	1	4	3.2	Cc1noc(NS(=O)(=O)c2cccc3ccccc23)c1C	10.1021/jm00029a001
	44278161	106580	0	None	-	0	Human	4.7	pIC50	=	4.7	Binding	Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.	ChEMBL	569	10	1	8	6.9	COc1cccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc(OCc4ccccc4)c(OC)cc23)c1	10.1016/0960-894X(96)00232-6
	CHEMBL285380	106580	0	None	-	0	Human	4.7	pIC50	=	4.7	Binding	Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.	ChEMBL	569	10	1	8	6.9	COc1cccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc(OCc4ccccc4)c(OC)cc23)c1	10.1016/0960-894X(96)00232-6
	10357554	104340	1	None	-	0	Rat	4.7	pIC50	=	4.7	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	302	3	1	4	3.2	Cc1noc(NS(=O)(=O)c2cccc3ccccc23)c1C	10.1021/jm00008a013
	CHEMBL27065	104340	1	None	-	0	Rat	4.7	pIC50	=	4.7	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	302	3	1	4	3.2	Cc1noc(NS(=O)(=O)c2cccc3ccccc23)c1C	10.1021/jm00008a013
	10495634	214707	0	None	-	0	Rat	4.7	pIC50	=	4.7	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	316	6	1	2	4.8	OC/C(=C/c1cccc(OCc2ccccc2)c1)c1ccccc1	10.1021/jm970847e
	CHEMBL96836	214707	0	None	-	0	Rat	4.7	pIC50	=	4.7	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	316	6	1	2	4.8	OC/C(=C/c1cccc(OCc2ccccc2)c1)c1ccccc1	10.1021/jm970847e
	44276966	113633	0	None	-	0	Rat	4.7	pIC50	=	4.7	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	352	5	1	5	2.9	COc1cccc(Cn2[nH]c(C)c(Cc3ccc4c(c3)OCO4)c2=O)c1	10.1016/s0960-894x(00)00232-8
	CHEMBL3144846	113633	0	None	-	0	Rat	4.7	pIC50	=	4.7	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	352	5	1	5	2.9	COc1cccc(Cn2[nH]c(C)c(Cc3ccc4c(c3)OCO4)c2=O)c1	10.1016/s0960-894x(00)00232-8
	44386894	69255	0	None	-	0	Rat	5.7	pIC50	=	5.7	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	412	7	2	6	2.1	COc1ccc([C@@H]2[C@@H](CC(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(N)=O)cc1	10.1021/jm031041j
	CHEMBL177999	69255	0	None	-	0	Rat	5.7	pIC50	=	5.7	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	412	7	2	6	2.1	COc1ccc([C@@H]2[C@@H](CC(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(N)=O)cc1	10.1021/jm031041j
	11795139	173316	0	None	-	0	Rat	5.7	pIC50	=	5.7	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	398	6	2	6	1.8	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(N)=O)cc1	10.1021/jm9505369
	CHEMBL427935	173316	0	None	-	0	Rat	5.7	pIC50	=	5.7	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	398	6	2	6	1.8	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(N)=O)cc1	10.1021/jm9505369
	10212163	136874	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	696	11	2	13	5.3	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCC#CCOC(=O)Nc1cnccn1	10.1016/s0960-894x(02)01084-3
	CHEMBL367767	136874	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	696	11	2	13	5.3	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCC#CCOC(=O)Nc1cnccn1	10.1016/s0960-894x(02)01084-3
	23445256	66963	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	470	6	1	7	4.1	Cc1noc(NS(=O)(=O)c2ccsc2CCc2ccc3c(c2)OCO3)c1Br	10.1016/S0960-894X(97)00133-9
	CHEMBL173982	66963	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	470	6	1	7	4.1	Cc1noc(NS(=O)(=O)c2ccsc2CCc2ccc3c(c2)OCO3)c1Br	10.1016/S0960-894X(97)00133-9
	10604119	18229	0	None	-	0	Human	4.7	pIC50	=	4.7	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	636	12	2	7	5.8	COCCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2C)c2ccccc2C)cc1	10.1021/jm990171i
	CHEMBL1180361	18229	0	None	-	0	Human	4.7	pIC50	=	4.7	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	636	12	2	7	5.8	COCCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2C)c2ccccc2C)cc1	10.1021/jm990171i
	CHEMBL123654	18229	0	None	-	0	Human	4.7	pIC50	=	4.7	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	636	12	2	7	5.8	COCCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2C)c2ccccc2C)cc1	10.1021/jm990171i
	44325305	214246	0	None	-	0	Rat	6.7	pIC50	=	6.7	Binding	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	ChEMBL	426	10	2	5	5.3	Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1C(=O)O	10.1021/jm9707131
	CHEMBL94279	214246	0	None	-	0	Rat	6.7	pIC50	=	6.7	Binding	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	ChEMBL	426	10	2	5	5.3	Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1C(=O)O	10.1021/jm9707131
	10005597	126596	0	None	-	1	Rat	7.7	pIC50	=	7.7	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	485	7	1	7	5.2	COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3cc(OC)ccc3OC)c3c2oc2ccccc23)cc1	10.1021/jm031041j
	CHEMBL348407	126596	0	None	-	1	Rat	7.7	pIC50	=	7.7	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	485	7	1	7	5.2	COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3cc(OC)ccc3OC)c3c2oc2ccccc23)cc1	10.1021/jm031041j
	10005597	126596	0	None	-	1	Rat	7.7	pIC50	=	7.7	Binding	Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes	ChEMBL	485	7	1	7	5.2	COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3cc(OC)ccc3OC)c3c2oc2ccccc23)cc1	10.1016/s0960-894x(99)00040-2
	CHEMBL348407	126596	0	None	-	1	Rat	7.7	pIC50	=	7.7	Binding	Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes	ChEMBL	485	7	1	7	5.2	COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3cc(OC)ccc3OC)c3c2oc2ccccc23)cc1	10.1016/s0960-894x(99)00040-2
	CHEMBL433349	220416	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	44314890	111853	0	None	-	0	Pig	7.7	pIC50	=	7.7	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	647	12	5	4	5.0	CC(C)CC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1021/jm9600914
	CHEMBL311384	111853	0	None	-	0	Pig	7.7	pIC50	=	7.7	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	647	12	5	4	5.0	CC(C)CC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1021/jm9600914
	3539	10913	83	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	424	6	1	9	2.7	COc1nc(C)cnc1NS(=O)(=O)c1cccnc1c1ccc(cc1)c1nnco1	10.1016/j.bmcl.2016.06.014
	9910224	10913	83	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	424	6	1	9	2.7	COc1nc(C)cnc1NS(=O)(=O)c1cccnc1c1ccc(cc1)c1nnco1	10.1016/j.bmcl.2016.06.014
	CHEMBL1628688	10913	83	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	424	6	1	9	2.7	COc1nc(C)cnc1NS(=O)(=O)c1cccnc1c1ccc(cc1)c1nnco1	10.1016/j.bmcl.2016.06.014
	DB06629	10913	83	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	424	6	1	9	2.7	COc1nc(C)cnc1NS(=O)(=O)c1cccnc1c1ccc(cc1)c1nnco1	10.1016/j.bmcl.2016.06.014
	10168597	68111	0	None	-	1	Human	7.7	pIC50	=	7.7	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	661	11	2	13	3.6	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1cccnc1	10.1016/s0960-894x(02)01084-3
	CHEMBL176741	68111	0	None	-	1	Human	7.7	pIC50	=	7.7	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	661	11	2	13	3.6	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1cccnc1	10.1016/s0960-894x(02)01084-3
	10673969	68879	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor	ChEMBL	538	10	3	7	5.0	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)OC(=O)NC2CCCCC2)nc1C(=O)O	10.1021/jm9505932
	CHEMBL177546	68879	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor	ChEMBL	538	10	3	7	5.0	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)OC(=O)NC2CCCCC2)nc1C(=O)O	10.1021/jm9505932
	10138169	106137	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor	ChEMBL	440	6	1	8	3.7	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Cc2ccc3c(c2)OCO3)c1Cl	10.1021/jm000349x
	CHEMBL282470	106137	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor	ChEMBL	440	6	1	8	3.7	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Cc2ccc3c(c2)OCO3)c1Cl	10.1021/jm000349x
	CHEMBL342615	218454	0	None	-	0	Pig	7.7	pIC50	=	7.7	Binding	Inhibitory effect against porcine Endothelin A receptorInhibitory effect against porcine Endothelin A receptor	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CS(=O)(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	CHEMBL342615	218454	0	None	-	0	Pig	7.7	pIC50	=	7.7	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CS(=O)(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	10527706	103776	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Radioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cells	ChEMBL	454	8	1	6	3.1	CCCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL266594	103776	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Radioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cells	ChEMBL	454	8	1	6	3.1	CCCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	44439114	168409	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I]ET1 from human ETA receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETA receptor expressed in CHO cells	ChEMBL	993	32	2	15	7.3	CC(=O)CC(=O)CCc1ccc(NC(=O)CCOCCOCCOCCOCCOc2ccc(CCC(=O)N(C)Cc3cc(-c4ncco4)ccc3-c3ccccc3S(=O)(=O)Nc3ccno3)cc2)cc1	10.1016/j.bmcl.2006.10.009
	CHEMBL413001	168409	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I]ET1 from human ETA receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETA receptor expressed in CHO cells	ChEMBL	993	32	2	15	7.3	CC(=O)CC(=O)CCc1ccc(NC(=O)CCOCCOCCOCCOCCOc2ccc(CCC(=O)N(C)Cc3cc(-c4ncco4)ccc3-c3ccccc3S(=O)(=O)Nc3ccno3)cc2)cc1	10.1016/j.bmcl.2006.10.009
	18738889	94741	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	562	8	1	8	4.9	CCn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c2ccc(C(=O)OC)cc21	10.1016/s0960-894x(01)00660-6
	CHEMBL23418	94741	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	562	8	1	8	4.9	CCn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c2ccc(C(=O)OC)cc21	10.1016/s0960-894x(01)00660-6
	10310877	210668	0	None	-	0	Rat	6.7	pIC50	=	6.7	Binding	Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor	ChEMBL	473	8	1	7	5.9	CCCOc1ccc2c(c1)c(-c1ccc(OC)cc1)c(C(=O)O)n2Cc1ccc2nsnc2c1	10.1016/s0960-894x(97)10151-2
	CHEMBL68896	210668	0	None	-	0	Rat	6.7	pIC50	=	6.7	Binding	Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor	ChEMBL	473	8	1	7	5.9	CCCOc1ccc2c(c1)c(-c1ccc(OC)cc1)c(C(=O)O)n2Cc1ccc2nsnc2c1	10.1016/s0960-894x(97)10151-2
	CHEMBL136210	215516	0	None	-	0	Pig	6.7	pIC50	=	6.7	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	21462927	127020	0	None	-	0	Rat	5.7	pIC50	=	5.7	Binding	Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes	ChEMBL	500	7	1	8	5.1	COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2cc([N+](=O)[O-])ccc23)cc1	10.1016/s0960-894x(99)00040-2
	CHEMBL352241	127020	0	None	-	0	Rat	5.7	pIC50	=	5.7	Binding	Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes	ChEMBL	500	7	1	8	5.1	COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2cc([N+](=O)[O-])ccc23)cc1	10.1016/s0960-894x(99)00040-2
	10086660	105936	0	None	-	0	Rat	5.7	pIC50	=	5.7	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	309	6	2	5	2.9	CCCNc1cccc(S(=O)(=O)Nc2onc(C)c2C)c1	10.1021/jm00008a013
	CHEMBL281199	105936	0	None	-	0	Rat	5.7	pIC50	=	5.7	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	309	6	2	5	2.9	CCCNc1cccc(S(=O)(=O)Nc2onc(C)c2C)c1	10.1021/jm00008a013
	44279308	106909	0	None	-	0	Pig	5.7	pIC50	=	5.7	Binding	Binding affinity against ETA receptor in porcine aortic smooth muscle membraneBinding affinity against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	521	12	6	4	3.3	Cc1cccc(NC(=O)N[C@@H](CC(C)C)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NCCC(=O)O)c1	10.1016/0960-894X(95)00221-E
	CHEMBL287676	106909	0	None	-	0	Pig	5.7	pIC50	=	5.7	Binding	Binding affinity against ETA receptor in porcine aortic smooth muscle membraneBinding affinity against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	521	12	6	4	3.3	Cc1cccc(NC(=O)N[C@@H](CC(C)C)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NCCC(=O)O)c1	10.1016/0960-894X(95)00221-E
	44279307	114791	0	None	-	0	Pig	5.7	pIC50	=	5.7	Binding	Binding affinity against ETA receptor in porcine aortic smooth muscle membraneBinding affinity against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	541	12	6	4	3.7	CC(C)C[C@H](NC(=O)Nc1cccc(Cl)c1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	CHEMBL31944	114791	0	None	-	0	Pig	5.7	pIC50	=	5.7	Binding	Binding affinity against ETA receptor in porcine aortic smooth muscle membraneBinding affinity against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	541	12	6	4	3.7	CC(C)C[C@H](NC(=O)Nc1cccc(Cl)c1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	CHEMBL319537	217998	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	10621049	214022	0	None	-	0	Rat	5.7	pIC50	=	5.7	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	400	6	1	3	5.6	OC/C(=C/c1cc(OCc2ccsc2)ccc1Br)c1ccccc1	10.1021/jm970847e
	CHEMBL92876	214022	0	None	-	0	Rat	5.7	pIC50	=	5.7	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	400	6	1	3	5.6	OC/C(=C/c1cc(OCc2ccsc2)ccc1Br)c1ccccc1	10.1021/jm970847e
	44213278	113626	0	None	-	0	Rat	5.7	pIC50	=	5.7	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	406	5	1	5	3.6	COc1ccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2=O)cc1	10.1016/s0960-894x(00)00232-8
	CHEMBL3144799	113626	0	None	-	0	Rat	5.7	pIC50	=	5.7	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	406	5	1	5	3.6	COc1ccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2=O)cc1	10.1016/s0960-894x(00)00232-8
	10719007	18013	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	465	6	1	9	3.7	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)C(C#N)c2ccc3c(c2)OCO3)c1Cl	10.1021/jm9700068
	CHEMBL1178895	18013	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	465	6	1	9	3.7	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)C(C#N)c2ccc3c(c2)OCO3)c1Cl	10.1021/jm9700068
	CHEMBL48448	18013	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	465	6	1	9	3.7	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)C(C#N)c2ccc3c(c2)OCO3)c1Cl	10.1021/jm9700068
	10626054	138126	0	None	-	0	Rat	5.7	pIC50	=	5.7	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	530	11	6	4	4.2	Cc1[nH]c([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NCc2ccccc2)nc1C(=O)O	10.1021/jm950592+
	CHEMBL368788	138126	0	None	-	0	Rat	5.7	pIC50	=	5.7	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	530	11	6	4	4.2	Cc1[nH]c([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NCc2ccccc2)nc1C(=O)O	10.1021/jm950592+
	CHEMBL1206645	215387	0	None	-	0	Pig	4.7	pIC50	=	4.7	Binding	Compound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranesCompound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranes	ChEMBL		None	None	None		CC(C)C[C@@H](NC(=O)N1CCCCCC1)C(=O)N(C)[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)O	10.1021/jm00087a001
	CHEMBL290454	215387	0	None	-	0	Pig	4.7	pIC50	=	4.7	Binding	Compound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranesCompound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranes	ChEMBL		None	None	None		CC(C)C[C@@H](NC(=O)N1CCCCCC1)C(=O)N(C)[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)O	10.1021/jm00087a001
	10742968	19133	0	None	-	0	Human	4.7	pIC50	=	4.7	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	469	7	1	8	4.1	Cc1noc(NS(=O)(=O)c2ccsc2C(Cc2ccc3c(c2)OCO3)N(C)C)c1Cl	10.1021/jm9700068
	CHEMBL1185472	19133	0	None	-	0	Human	4.7	pIC50	=	4.7	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	469	7	1	8	4.1	Cc1noc(NS(=O)(=O)c2ccsc2C(Cc2ccc3c(c2)OCO3)N(C)C)c1Cl	10.1021/jm9700068
	CHEMBL416453	19133	0	None	-	0	Human	4.7	pIC50	=	4.7	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	469	7	1	8	4.1	Cc1noc(NS(=O)(=O)c2ccsc2C(Cc2ccc3c(c2)OCO3)N(C)C)c1Cl	10.1021/jm9700068
	44368481	128298	0	None	-	0	Pig	4.7	pIC50	=	4.7	Binding	Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.	ChEMBL	435	9	2	7	2.8	CCOC(=O)CN(Cc1cc2c(cc1Cl)OCO2)C(Cc1ccc(O)cc1)C(=O)O	10.1016/s0960-894x(01)00009-9
	CHEMBL358444	128298	0	None	-	0	Pig	4.7	pIC50	=	4.7	Binding	Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.	ChEMBL	435	9	2	7	2.8	CCOC(=O)CN(Cc1cc2c(cc1Cl)OCO2)C(Cc1ccc(O)cc1)C(=O)O	10.1016/s0960-894x(01)00009-9
	10576888	177624	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	485	6	3	7	3.6	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccccc2C(=O)O)c1Br	10.1021/jm9608366
	CHEMBL44539	177624	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	485	6	3	7	3.6	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccccc2C(=O)O)c1Br	10.1021/jm9608366
	23445284	119579	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	440	5	1	5	5.4	Cc1noc(NS(=O)(=O)c2sccc2-c2ccc(C(C)C)cc2)c1Br	10.1016/S0960-894X(96)00496-9
	CHEMBL330674	119579	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	440	5	1	5	5.4	Cc1noc(NS(=O)(=O)c2sccc2-c2ccc(C(C)C)cc2)c1Br	10.1016/S0960-894X(96)00496-9
	23445458	67074	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	468	5	1	7	4.5	Cc1noc(NS(=O)(=O)c2sccc2/C=C/c2ccc3c(c2)OCO3)c1Br	10.1016/S0960-894X(97)00133-9
	CHEMBL174363	67074	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	468	5	1	7	4.5	Cc1noc(NS(=O)(=O)c2sccc2/C=C/c2ccc3c(c2)OCO3)c1Br	10.1016/S0960-894X(97)00133-9
	5344	180252	101	None	-	1	Human	4.7	pIC50	=	4.7	Binding	DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)	ChEMBL	267	3	2	5	1.7	Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C	nan
	CHEMBL453	180252	101	None	-	1	Human	4.7	pIC50	=	4.7	Binding	DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)	ChEMBL	267	3	2	5	1.7	Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C	nan
	44385412	138156	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	711	14	2	13	4.5	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(Cc2ccc3c(c2)OCO3)nc1OCCNS(=O)(=O)c1cccs1	10.1016/s0960-894x(02)01083-1
	CHEMBL368945	138156	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	711	14	2	13	4.5	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(Cc2ccc3c(c2)OCO3)nc1OCCNS(=O)(=O)c1cccs1	10.1016/s0960-894x(02)01083-1
	18184249	135250	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	662	13	2	11	4.5	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2ccncc2)nc1OCCNS(=O)(=O)c1ccc(C)cc1	10.1016/s0960-894x(02)01083-1
	CHEMBL366628	135250	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	662	13	2	11	4.5	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2ccncc2)nc1OCCNS(=O)(=O)c1ccc(C)cc1	10.1016/s0960-894x(02)01083-1
	CHEMBL303185	217696	0	None	-	0	Pig	7.7	pIC50	=	7.7	Binding	Binding activity against Endothelin A receptor of Porcine aortic smooth muscle membranesBinding activity against Endothelin A receptor of Porcine aortic smooth muscle membranes	ChEMBL		None	None	None		CC(C)C[C@@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00089a028
	10696818	16422	0	None	-	0	Rat	7.7	pIC50	=	7.7	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	502	15	1	5	5.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC(CC)CC	10.1021/jm980217s
	CHEMBL112770	16422	0	None	-	0	Rat	7.7	pIC50	=	7.7	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	502	15	1	5	5.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC(CC)CC	10.1021/jm980217s
	CHEMBL303185	217696	0	None	-	0	Pig	7.7	pIC50	=	7.7	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm9600914
	10792711	121569	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	548	9	2	6	5.2	CCc1cc(F)cc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm990170q
	CHEMBL333972	121569	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	548	9	2	6	5.2	CCc1cc(F)cc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm990170q
	9917706	136517	0	None	-	2	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	659	15	2	11	5.3	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CC2)nc1OCCCNS(=O)(=O)c1cccs1	10.1016/j.bmcl.2016.06.014
	CHEMBL367444	136517	0	None	-	2	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	659	15	2	11	5.3	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CC2)nc1OCCCNS(=O)(=O)c1cccs1	10.1016/j.bmcl.2016.06.014
	18738881	86358	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	534	7	2	7	4.4	CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(C(=O)O)ccc23)cc1	10.1016/s0960-894x(01)00660-6
	CHEMBL2114305	86358	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	534	7	2	7	4.4	CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(C(=O)O)ccc23)cc1	10.1016/s0960-894x(01)00660-6
	443289	7498	47	None	2	3	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL		None	None	None		None	10.1021/jm030528p
	997	7498	47	None	2	3	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL		None	None	None		None	10.1021/jm030528p
	CHEMBL314691	7498	47	None	2	3	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL		None	None	None		None	10.1021/jm030528p
	DB12054	7498	47	None	2	3	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL		None	None	None		None	10.1021/jm030528p
	9886303	66311	0	None	-	0	Rat	7.7	pIC50	=	7.7	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	383	7	1	5	4.5	N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1ccccc1F	10.1021/jm990378b
	CHEMBL171638	66311	0	None	-	0	Rat	7.7	pIC50	=	7.7	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	383	7	1	5	4.5	N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1ccccc1F	10.1021/jm990378b
	44293761	175993	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	549	12	2	8	4.6	CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCCCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	CHEMBL440853	175993	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	549	12	2	8	4.6	CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCCCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	10908075	18515	0	None	-	0	Pig	7.7	pIC50	=	7.7	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	591	9	1	8	5.4	Cc1ccc(-c2c(NS(=O)(=O)c3cccc4ccccc34)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm0102304
	CHEMBL1181549	18515	0	None	-	0	Pig	7.7	pIC50	=	7.7	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	591	9	1	8	5.4	Cc1ccc(-c2c(NS(=O)(=O)c3cccc4ccccc34)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm0102304
	CHEMBL177373	18515	0	None	-	0	Pig	7.7	pIC50	=	7.7	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	591	9	1	8	5.4	Cc1ccc(-c2c(NS(=O)(=O)c3cccc4ccccc34)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm0102304
	10302118	67198	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	533	9	2	10	3.2	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2ccncc2)nc1OCC#CCO	10.1016/s0960-894x(02)01084-3
	CHEMBL175111	67198	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	533	9	2	10	3.2	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2ccncc2)nc1OCC#CCO	10.1016/s0960-894x(02)01084-3
	135512539	135252	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	615	11	2	13	4.4	C#CCOc1nc(-c2ccnc(-c3noc(O)n3)c2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	CHEMBL366652	135252	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	615	11	2	13	4.4	C#CCOc1nc(-c2ccnc(-c3noc(O)n3)c2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	9864880	109165	0	None	-	1	Rat	7.7	pIC50	=	7.7	Binding	Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor	ChEMBL	384	4	1	6	3.7	CN(C)c1cccc2c(S(=O)(=O)Nc3ccc4nsnc4c3)cccc12	10.1016/s0960-894x(97)10151-2
	CHEMBL303902	109165	0	None	-	1	Rat	7.7	pIC50	=	7.7	Binding	Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor	ChEMBL	384	4	1	6	3.7	CN(C)c1cccc2c(S(=O)(=O)Nc3ccc4nsnc4c3)cccc12	10.1016/s0960-894x(97)10151-2
	443289	7498	47	None	-	3	Pig	7.7	pIC50	=	7.7	Binding	Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		None	10.1016/0960-894X(95)00237-N
	997	7498	47	None	-	3	Pig	7.7	pIC50	=	7.7	Binding	Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		None	10.1016/0960-894X(95)00237-N
	CHEMBL314691	7498	47	None	-	3	Pig	7.7	pIC50	=	7.7	Binding	Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		None	10.1016/0960-894X(95)00237-N
	DB12054	7498	47	None	-	3	Pig	7.7	pIC50	=	7.7	Binding	Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		None	10.1016/0960-894X(95)00237-N
	10578601	135823	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor	ChEMBL	550	10	4	5	4.7	Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)N(C)C(=O)NC2CCCCC2)nc1C(=O)O	10.1021/jm9505932
	CHEMBL367033	135823	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor	ChEMBL	550	10	4	5	4.7	Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)N(C)C(=O)NC2CCCCC2)nc1C(=O)O	10.1021/jm9505932
	9917706	136517	0	None	-	2	Human	7.7	pIC50	=	7.7	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	659	15	2	11	5.3	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CC2)nc1OCCCNS(=O)(=O)c1cccs1	10.1016/s0960-894x(02)01083-1
	CHEMBL367444	136517	0	None	-	2	Human	7.7	pIC50	=	7.7	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	659	15	2	11	5.3	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CC2)nc1OCCCNS(=O)(=O)c1cccs1	10.1016/s0960-894x(02)01083-1
	CHEMBL336033	218353	1	None	-	0	Pig	7.7	pIC50	=	7.7	Binding	Inhibitory effect against porcine Endothelin A receptorInhibitory effect against porcine Endothelin A receptor	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	CHEMBL336033	218353	1	None	-	0	Pig	7.7	pIC50	=	7.7	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	CHEMBL170121	215620	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1cn(C)c2ccccc12)C(=O)NCC(=O)O	10.1016/0960-894X(95)00144-I
	11070564	210179	0	None	-	0	Rat	6.7	pIC50	=	6.7	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	460	7	1	6	5.2	CCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc(OC)cc1)O2	10.1021/jm010382z
	CHEMBL65494	210179	0	None	-	0	Rat	6.7	pIC50	=	6.7	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	460	7	1	6	5.2	CCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc(OC)cc1)O2	10.1021/jm010382z
	122044	16945	51	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of 125I-ET1 from human smooth muscle ETA receptor expressed in fall armyworm sf9 cell membranesDisplacement of 125I-ET1 from human smooth muscle ETA receptor expressed in fall armyworm sf9 cell membranes	ChEMBL	473	9	2	8	3.7	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCO)c1	10.1016/j.bmcl.2016.06.014
	CHEMBL115951	16945	51	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of 125I-ET1 from human smooth muscle ETA receptor expressed in fall armyworm sf9 cell membranesDisplacement of 125I-ET1 from human smooth muscle ETA receptor expressed in fall armyworm sf9 cell membranes	ChEMBL	473	9	2	8	3.7	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCO)c1	10.1016/j.bmcl.2016.06.014
	10571812	135426	0	None	-	0	Rat	6.7	pIC50	=	6.7	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	380	7	1	6	4.1	Cc1ccccc1C(Oc1cc(OCc2ccsn2)ccc1C#N)C(=O)O	10.1021/jm990378b
	CHEMBL366788	135426	0	None	-	0	Rat	6.7	pIC50	=	6.7	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	380	7	1	6	4.1	Cc1ccccc1C(Oc1cc(OCc2ccsn2)ccc1C#N)C(=O)O	10.1021/jm990378b
	2802888	67331	10	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Inhibition of [125]ET-1 binding to human Endothelin A receptor expressed in vero cellsInhibition of [125]ET-1 binding to human Endothelin A receptor expressed in vero cells	ChEMBL	414	9	4	5	2.5	CC(C)C(NC(=O)OCc1ccccc1)C(=O)NC(Cc1ccc(O)cc1)C(=O)O	10.1021/jm031041j
	CHEMBL175916	67331	10	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Inhibition of [125]ET-1 binding to human Endothelin A receptor expressed in vero cellsInhibition of [125]ET-1 binding to human Endothelin A receptor expressed in vero cells	ChEMBL	414	9	4	5	2.5	CC(C)C(NC(=O)OCc1ccccc1)C(=O)NC(Cc1ccc(O)cc1)C(=O)O	10.1021/jm031041j
	10789279	213344	0	None	-	0	Rat	6.7	pIC50	=	6.7	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	441	10	1	6	4.1	CCCCOCCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL8878	213344	0	None	-	0	Rat	6.7	pIC50	=	6.7	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	441	10	1	6	4.1	CCCCOCCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	10554384	176024	0	None	-	0	Rat	6.7	pIC50	=	6.7	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	537	10	4	6	4.6	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)nc1C(=O)O	10.1021/jm950592+
	CHEMBL441112	176024	0	None	-	0	Rat	6.7	pIC50	=	6.7	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	537	10	4	6	4.6	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)nc1C(=O)O	10.1021/jm950592+
	10554384	176024	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor	ChEMBL	537	10	4	6	4.6	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)nc1C(=O)O	10.1021/jm9505932
	CHEMBL441112	176024	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor	ChEMBL	537	10	4	6	4.6	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)nc1C(=O)O	10.1021/jm9505932
	CHEMBL2370254	216597	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	10024044	14611	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	402	6	1	5	4.1	COc1ccc(CC2=C(c3ccccc3)C(=O)OC2(O)c2ccc(OC)cc2)cc1	10.1021/jm9606507
	CHEMBL10897	14611	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	402	6	1	5	4.1	COc1ccc(CC2=C(c3ccccc3)C(=O)OC2(O)c2ccc(OC)cc2)cc1	10.1021/jm9606507
	11732155	209445	0	None	-	0	Rat	5.7	pIC50	=	5.7	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	402	4	1	5	4.4	COc1ccccc1C1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21	10.1021/jm010382z
	CHEMBL61460	209445	0	None	-	0	Rat	5.7	pIC50	=	5.7	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	402	4	1	5	4.4	COc1ccccc1C1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21	10.1021/jm010382z
	CHEMBL2304014	216249	0	None	-	0	Pig	5.7	pIC50	=	5.7	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc2c(C#N)[nH]c3ccccc23)NC(=O)[C@@H](C(C)C)NC1=O	10.1021/jm9600914
	443289	7498	47	None	-	3	Pig	4.7	pIC50	=	4.7	Binding	Compound was evaluated for the binding affinity to Endothelin A receptor in the porcine aortic smooth muscleCompound was evaluated for the binding affinity to Endothelin A receptor in the porcine aortic smooth muscle	ChEMBL		None	None	None		None	10.1021/jm00087a001
	997	7498	47	None	-	3	Pig	4.7	pIC50	=	4.7	Binding	Compound was evaluated for the binding affinity to Endothelin A receptor in the porcine aortic smooth muscleCompound was evaluated for the binding affinity to Endothelin A receptor in the porcine aortic smooth muscle	ChEMBL		None	None	None		None	10.1021/jm00087a001
	CHEMBL314691	7498	47	None	-	3	Pig	4.7	pIC50	=	4.7	Binding	Compound was evaluated for the binding affinity to Endothelin A receptor in the porcine aortic smooth muscleCompound was evaluated for the binding affinity to Endothelin A receptor in the porcine aortic smooth muscle	ChEMBL		None	None	None		None	10.1021/jm00087a001
	DB12054	7498	47	None	-	3	Pig	4.7	pIC50	=	4.7	Binding	Compound was evaluated for the binding affinity to Endothelin A receptor in the porcine aortic smooth muscleCompound was evaluated for the binding affinity to Endothelin A receptor in the porcine aortic smooth muscle	ChEMBL		None	None	None		None	10.1021/jm00087a001
	10647488	183701	0	None	-	0	Human	4.7	pIC50	=	4.7	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	456	6	2	8	3.7	Cc1noc(NS(=O)(=O)c2ccsc2C(C)(O)Cc2ccc3c(c2)OCO3)c1Cl	10.1021/jm9700068
	CHEMBL46195	183701	0	None	-	0	Human	4.7	pIC50	=	4.7	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	456	6	2	8	3.7	Cc1noc(NS(=O)(=O)c2ccsc2C(C)(O)Cc2ccc3c(c2)OCO3)c1Cl	10.1021/jm9700068
	44320488	113762	0	None	-	0	Rat	6.7	pIC50	=	6.7	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	438	5	1	5	5.7	O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1C1CCCCC1	10.1016/s0960-894x(00)00513-8
	CHEMBL315175	113762	0	None	-	0	Rat	6.7	pIC50	=	6.7	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	438	5	1	5	5.7	O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1C1CCCCC1	10.1016/s0960-894x(00)00513-8
	10766198	169664	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	455	6	2	6	3.5	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)NCc2ccccc2)c1Br	10.1021/jm9608366
	CHEMBL417358	169664	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	455	6	2	6	3.5	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)NCc2ccccc2)c1Br	10.1021/jm9608366
	76324075	92615	0	None	-	0	Rat	7.6	pIC50	=	7.6	Binding	Displacement of [125I]ET-1 from ETA receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hrDisplacement of [125I]ET-1 from ETA receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hr	ChEMBL	340	4	1	6	4.0	Cc1c(C(=O)O)oc2cccc(OCc3ccc4nsnc4c3)c12	10.1007/s00044-013-0542-3
	CHEMBL2296899	92615	0	None	-	0	Rat	7.6	pIC50	=	7.6	Binding	Displacement of [125I]ET-1 from ETA receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hrDisplacement of [125I]ET-1 from ETA receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hr	ChEMBL	340	4	1	6	4.0	Cc1c(C(=O)O)oc2cccc(OCc3ccc4nsnc4c3)c12	10.1007/s00044-013-0542-3
	151174	209499	45	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	605	12	3	13	3.2	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccnc(-c3nn[nH]n3)c2)nc1OCCO	10.1021/jm030528p
	CHEMBL61780	209499	45	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor	ChEMBL	605	12	3	13	3.2	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccnc(-c3nn[nH]n3)c2)nc1OCCO	10.1021/jm030528p
	10810505	66285	0	None	-	0	Rat	7.6	pIC50	=	7.6	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	392	7	1	5	4.2	Cc1ccccc1C(Oc1cc(OCc2ccnc(F)c2)ccc1C#N)C(=O)O	10.1021/jm990378b
	CHEMBL171513	66285	0	None	-	0	Rat	7.6	pIC50	=	7.6	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	392	7	1	5	4.2	Cc1ccccc1C(Oc1cc(OCc2ccnc(F)c2)ccc1C#N)C(=O)O	10.1021/jm990378b
	10282163	67187	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	599	11	2	12	3.9	C#CCOc1nc(-c2ccnc(-c3nn[nH]n3)c2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	CHEMBL175057	67187	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	599	11	2	12	3.9	C#CCOc1nc(-c2ccnc(-c3nn[nH]n3)c2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	10838921	213125	0	None	-	0	Rat	7.6	pIC50	=	7.6	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	494	7	1	6	4.1	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(C)C2CCCCC2)cc1	10.1021/jm9505369
	CHEMBL8736	213125	0	None	-	0	Rat	7.6	pIC50	=	7.6	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	494	7	1	6	4.1	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(C)C2CCCCC2)cc1	10.1021/jm9505369
	44279338	113471	0	None	-	0	Pig	6.6	pIC50	=	6.6	Binding	Binding affinity against ETA receptor in porcine aortic smooth muscle membraneBinding affinity against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	487	11	6	4	2.3	CC(C)C[C@H](NC(=O)NC(C)(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	CHEMBL31436	113471	0	None	-	0	Pig	6.6	pIC50	=	6.6	Binding	Binding affinity against ETA receptor in porcine aortic smooth muscle membraneBinding affinity against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	487	11	6	4	2.3	CC(C)C[C@H](NC(=O)NC(C)(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	CHEMBL97431	222703	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1021/jm00015a003
	18617403	212052	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	394	3	1	4	3.3	Cc1noc(NS(=O)(=O)c2cccc(Br)c2)c1Br	10.1016/0960-894X(96)00441-6
	CHEMBL79031	212052	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	394	3	1	4	3.3	Cc1noc(NS(=O)(=O)c2cccc(Br)c2)c1Br	10.1016/0960-894X(96)00441-6
	18617374	212295	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	350	3	1	4	3.2	Cc1noc(NS(=O)(=O)c2cccc(Cl)c2)c1Br	10.1016/0960-894X(96)00441-6
	CHEMBL80808	212295	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	350	3	1	4	3.2	Cc1noc(NS(=O)(=O)c2cccc(Cl)c2)c1Br	10.1016/0960-894X(96)00441-6
	CHEMBL262782	217329	0	None	-	0	Mouse	6.6	pIC50	=	6.6	Binding	Binding affinity for Endothelin A receptor was determined in murine 3T3 cellsBinding affinity for Endothelin A receptor was determined in murine 3T3 cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)CCCNC(=O)[C@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(00)80326-1
	122044	16945	51	None	-	0	Rat	6.6	pIC50	=	6.6	Binding	In vitro for specific binding of [125I]ET1 to A10 cell expressed in endothelin A receptorIn vitro for specific binding of [125I]ET1 to A10 cell expressed in endothelin A receptor	ChEMBL	473	9	2	8	3.7	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCO)c1	10.1021/jm0102304
	CHEMBL115951	16945	51	None	-	0	Rat	6.6	pIC50	=	6.6	Binding	In vitro for specific binding of [125I]ET1 to A10 cell expressed in endothelin A receptorIn vitro for specific binding of [125I]ET1 to A10 cell expressed in endothelin A receptor	ChEMBL	473	9	2	8	3.7	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCO)c1	10.1021/jm0102304
	44327728	214674	0	None	-	0	Rat	6.6	pIC50	=	6.6	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	505	5	1	8	2.1	Cc1ccc(=O)n(C(C(=O)NS(=O)(=O)c2ccc(Br)cc2)c2ccc3c(c2)OCO3)n1	10.1016/S0960-894X(96)00617-8
	CHEMBL96662	214674	0	None	-	0	Rat	6.6	pIC50	=	6.6	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	505	5	1	8	2.1	Cc1ccc(=O)n(C(C(=O)NS(=O)(=O)c2ccc(Br)cc2)c2ccc3c(c2)OCO3)n1	10.1016/S0960-894X(96)00617-8
	44327354	214835	0	None	-	0	Rat	6.6	pIC50	=	6.6	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	427	5	1	8	1.4	Cc1ccc(=O)n(C(C(=O)NS(=O)(=O)c2ccccc2)c2ccc3c(c2)OCO3)n1	10.1016/S0960-894X(96)00617-8
	CHEMBL97595	214835	0	None	-	0	Rat	6.6	pIC50	=	6.6	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	427	5	1	8	1.4	Cc1ccc(=O)n(C(C(=O)NS(=O)(=O)c2ccccc2)c2ccc3c(c2)OCO3)n1	10.1016/S0960-894X(96)00617-8
	10579210	175370	0	None	-	0	Rat	6.6	pIC50	=	6.6	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	585	10	4	6	5.4	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCc3ccccc32)nc1C(=O)O	10.1021/jm950592+
	CHEMBL435901	175370	0	None	-	0	Rat	6.6	pIC50	=	6.6	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	585	10	4	6	5.4	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCc3ccccc32)nc1C(=O)O	10.1021/jm950592+
	CHEMBL1791007	215692	0	None	-	0	Pig	6.6	pIC50	=	6.6	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	CHEMBL423941	220100	0	None	-	0	Mouse	6.6	pIC50	=	6.6	Binding	The compound was tested for the binding affinity against eEndothelin A receptor in murine 3T3 cells using [125I]ET1 as a radioligandThe compound was tested for the binding affinity against eEndothelin A receptor in murine 3T3 cells using [125I]ET1 as a radioligand	ChEMBL		None	None	None		CC[C@@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCN)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@H](C)CC	10.1016/S0960-894X(01)81219-1
	21462925	126717	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes	ChEMBL	470	6	2	7	4.8	COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2cc(N)ccc23)cc1	10.1016/s0960-894x(99)00040-2
	CHEMBL349556	126717	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes	ChEMBL	470	6	2	7	4.8	COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2cc(N)ccc23)cc1	10.1016/s0960-894x(99)00040-2
	10766396	117356	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	460	8	1	4	4.6	CCCN(C)C(=O)CN1C[C@H](c2ccc3ccccc3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	CHEMBL325418	117356	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	460	8	1	4	4.6	CCCN(C)C(=O)CN1C[C@H](c2ccc3ccccc3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	10837666	176667	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	460	8	1	4	4.6	CCCN(C)C(=O)CN1C[C@H](c2cccc3ccccc23)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	CHEMBL444061	176667	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	460	8	1	4	4.6	CCCN(C)C(=O)CN1C[C@H](c2cccc3ccccc23)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	44284290	19719	0	None	-	0	Pig	5.6	pIC50	=	5.6	Binding	Compound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranesCompound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranes	ChEMBL	589	13	4	5	3.9	CC(C)C[C@@H](NC(=O)C1CCCCC1)C(=O)N(C)[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccn1)C(=O)O	10.1021/jm00087a001
	CHEMBL1189291	19719	0	None	-	0	Pig	5.6	pIC50	=	5.6	Binding	Compound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranesCompound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranes	ChEMBL	589	13	4	5	3.9	CC(C)C[C@@H](NC(=O)C1CCCCC1)C(=O)N(C)[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccn1)C(=O)O	10.1021/jm00087a001
	CHEMBL538475	19719	0	None	-	0	Pig	5.6	pIC50	=	5.6	Binding	Compound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranesCompound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranes	ChEMBL	589	13	4	5	3.9	CC(C)C[C@@H](NC(=O)C1CCCCC1)C(=O)N(C)[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccn1)C(=O)O	10.1021/jm00087a001
	44320782	113849	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	482	7	1	6	5.8	COc1ccc(-c2nn(CC3CCCCC3)c(C(=O)O)c2Cc2cc3c(cc2Cl)OCO3)cc1	10.1016/s0960-894x(00)00513-8
	CHEMBL315788	113849	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	482	7	1	6	5.8	COc1ccc(-c2nn(CC3CCCCC3)c(C(=O)O)c2Cc2cc3c(cc2Cl)OCO3)cc1	10.1016/s0960-894x(00)00513-8
	44266629	11191	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	387	4	1	5	4.7	COc1ccc(-n2c(C(=O)O)c(-c3ccc4c(c3)OCO4)c3ccccc32)cc1	10.1016/0960-894X(96)00170-9
	CHEMBL10151	11191	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	387	4	1	5	4.7	COc1ccc(-n2c(C(=O)O)c(-c3ccc4c(c3)OCO4)c3ccccc32)cc1	10.1016/0960-894X(96)00170-9
	CHEMBL2304017	216252	0	None	-	0	Pig	4.6	pIC50	=	4.6	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CSC(C)(C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc2c(C#N)[nH]c3ccccc23)NC(=O)[C@@H](C(C)C)NC1=O	10.1021/jm9600914
	44278270	168822	0	None	-	0	Human	4.6	pIC50	=	4.6	Binding	Compound was evaluated for the receptor binding activity in rabbit artery vascular smooth muscle cells expressing Endothelin A receptorCompound was evaluated for the receptor binding activity in rabbit artery vascular smooth muscle cells expressing Endothelin A receptor	ChEMBL	300	4	1	4	4.3	COc1cccc(Sc2c(C(=O)O)oc3ccccc23)c1	10.1016/0960-894X(96)00232-6
	CHEMBL416019	168822	0	None	-	0	Human	4.6	pIC50	=	4.6	Binding	Compound was evaluated for the receptor binding activity in rabbit artery vascular smooth muscle cells expressing Endothelin A receptorCompound was evaluated for the receptor binding activity in rabbit artery vascular smooth muscle cells expressing Endothelin A receptor	ChEMBL	300	4	1	4	4.3	COc1cccc(Sc2c(C(=O)O)oc3ccccc23)c1	10.1016/0960-894X(96)00232-6
	23445430	67840	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	438	5	1	5	5.1	Cc1ccc(/C=C/c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1	10.1016/S0960-894X(97)00133-9
	CHEMBL176422	67840	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	438	5	1	5	5.1	Cc1ccc(/C=C/c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1	10.1016/S0960-894X(97)00133-9
	10530424	68864	0	None	-	0	Rat	4.6	pIC50	=	4.6	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	536	9	4	5	4.3	Cc1c(C(=O)O)nc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)n1C	10.1021/jm950592+
	CHEMBL177502	68864	0	None	-	0	Rat	4.6	pIC50	=	4.6	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	536	9	4	5	4.3	Cc1c(C(=O)O)nc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)n1C	10.1021/jm950592+
	23445438	68273	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	470	6	1	7	4.1	Cc1noc(NS(=O)(=O)c2sccc2CCc2ccc3c(c2)OCO3)c1Br	10.1016/S0960-894X(97)00133-9
	CHEMBL177070	68273	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	470	6	1	7	4.1	Cc1noc(NS(=O)(=O)c2sccc2CCc2ccc3c(c2)OCO3)c1Br	10.1016/S0960-894X(97)00133-9
	44384826	66750	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	561	10	1	9	5.8	C/C=C/COc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	CHEMBL173366	66750	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	561	10	1	9	5.8	C/C=C/COc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	9896251	105549	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Compound was evaluated for inhibitory activity against human Endothelin A receptor (ETA)Compound was evaluated for inhibitory activity against human Endothelin A receptor (ETA)	ChEMBL	682	12	1	9	7.1	CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2	10.1021/jm020138n
	CHEMBL278176	105549	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Compound was evaluated for inhibitory activity against human Endothelin A receptor (ETA)Compound was evaluated for inhibitory activity against human Endothelin A receptor (ETA)	ChEMBL	682	12	1	9	7.1	CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2	10.1021/jm020138n
	127034758	143148	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	681	12	1	8	7.7	CCCc1cc(Cn2c(CC)nc3c(C)cc(C)cc32)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2	10.1039/C4MD00499J
	CHEMBL3734968	143148	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	681	12	1	8	7.7	CCCc1cc(Cn2c(CC)nc3c(C)cc(C)cc32)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2	10.1039/C4MD00499J
	10576379	108048	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	471	6	2	7	3.9	COc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1	10.1021/jm9608366
	CHEMBL296291	108048	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	471	6	2	7	3.9	COc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1	10.1021/jm9608366
	10281192	67851	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	561	11	2	10	4.2	C#CCOc1nc(-c2ccnc(CO)c2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	CHEMBL176482	67851	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	561	11	2	10	4.2	C#CCOc1nc(-c2ccnc(CO)c2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	9896251	105549	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells	ChEMBL	682	12	1	9	7.1	CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2	10.1016/0960-894X(95)00186-W
	CHEMBL278176	105549	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells	ChEMBL	682	12	1	9	7.1	CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2	10.1016/0960-894X(95)00186-W
	44404967	142196	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibitory concentration against endothelin receptor type AInhibitory concentration against endothelin receptor type A	ChEMBL	680	12	1	8	7.3	CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCC2	10.1021/jm058225d
	CHEMBL372814	142196	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibitory concentration against endothelin receptor type AInhibitory concentration against endothelin receptor type A	ChEMBL	680	12	1	8	7.3	CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCC2	10.1021/jm058225d
	CHEMBL343582	218480	0	None	-	0	Pig	7.6	pIC50	=	7.6	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](c2ccccc2)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	42630654	25176	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	545	10	2	8	4.3	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCOC)ccc31)OCO2	10.1016/j.bmcl.2017.04.049
	CHEMBL1271531	25176	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	545	10	2	8	4.3	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCOC)ccc31)OCO2	10.1016/j.bmcl.2017.04.049
	42630654	25176	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer	ChEMBL	545	10	2	8	4.3	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCOC)ccc31)OCO2	10.1016/j.bmcl.2010.08.074
	CHEMBL1271531	25176	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer	ChEMBL	545	10	2	8	4.3	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCOC)ccc31)OCO2	10.1016/j.bmcl.2010.08.074
	11763363	117284	0	None	-	0	Pig	7.6	pIC50	=	7.6	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	551	11	1	10	4.6	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2cnccn2)c1	10.1021/jm0102304
	CHEMBL324943	117284	0	None	-	0	Pig	7.6	pIC50	=	7.6	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	551	11	1	10	4.6	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2cnccn2)c1	10.1021/jm0102304
	443289	7498	47	None	2	3	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer	ChEMBL		None	None	None		None	10.1016/j.bmcl.2010.08.074
	997	7498	47	None	2	3	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer	ChEMBL		None	None	None		None	10.1016/j.bmcl.2010.08.074
	CHEMBL314691	7498	47	None	2	3	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer	ChEMBL		None	None	None		None	10.1016/j.bmcl.2010.08.074
	DB12054	7498	47	None	2	3	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer	ChEMBL		None	None	None		None	10.1016/j.bmcl.2010.08.074
	10915215	107580	0	None	-	0	Rat	6.6	pIC50	=	6.6	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	354	4	1	5	3.8	CC(C)Oc1ccc2c(c1)C=C(C(=O)O)[C@@H](c1ccc3c(c1)OCO3)O2	10.1021/jm031041j
	CHEMBL293161	107580	0	None	-	0	Rat	6.6	pIC50	=	6.6	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	354	4	1	5	3.8	CC(C)Oc1ccc2c(c1)C=C(C(=O)O)[C@@H](c1ccc3c(c1)OCO3)O2	10.1021/jm031041j
	18617389	170257	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	408	3	1	4	3.6	Cc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1Br	10.1016/0960-894X(96)00441-6
	CHEMBL420029	170257	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	408	3	1	4	3.6	Cc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1Br	10.1016/0960-894X(96)00441-6
	10646375	103832	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	432	7	1	6	4.1	COc1ccc(C2(O)OC(=O)C(c3cc(OC)ccc3OC)=C2Cc2ccccc2)cc1	10.1021/jm9606507
	CHEMBL267096	103832	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	432	7	1	6	4.1	COc1ccc(C2(O)OC(=O)C(c3cc(OC)ccc3OC)=C2Cc2ccccc2)cc1	10.1021/jm9606507
	10915215	107580	0	None	-	0	Rat	6.6	pIC50	=	6.6	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	354	4	1	5	3.8	CC(C)Oc1ccc2c(c1)C=C(C(=O)O)[C@@H](c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	CHEMBL293161	107580	0	None	-	0	Rat	6.6	pIC50	=	6.6	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	354	4	1	5	3.8	CC(C)Oc1ccc2c(c1)C=C(C(=O)O)[C@@H](c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	44327727	174976	0	None	-	0	Rat	6.6	pIC50	=	6.6	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	503	6	1	8	3.0	Cc1ccc(=O)n(C(C(=O)NS(=O)(=O)c2ccc(-c3ccccc3)cc2)c2ccc3c(c2)OCO3)n1	10.1016/S0960-894X(96)00617-8
	CHEMBL433373	174976	0	None	-	0	Rat	6.6	pIC50	=	6.6	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	503	6	1	8	3.0	Cc1ccc(=O)n(C(C(=O)NS(=O)(=O)c2ccc(-c3ccccc3)cc2)c2ccc3c(c2)OCO3)n1	10.1016/S0960-894X(96)00617-8
	44266640	104893	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	459	4	1	8	4.2	O=C(O)c1c(-c2ccc3c(c2)OCO3)c2cc3c(cc2n1Cc1ccc2c(c1)OCO2)OCO3	10.1016/0960-894X(96)00170-9
	CHEMBL273529	104893	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	459	4	1	8	4.2	O=C(O)c1c(-c2ccc3c(c2)OCO3)c2cc3c(cc2n1Cc1ccc2c(c1)OCO2)OCO3	10.1016/0960-894X(96)00170-9
	CHEMBL335780	218341	0	None	-	0	Pig	6.6	pIC50	=	6.6	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	CHEMBL343768	218481	0	None	-	0	Pig	6.6	pIC50	=	6.6	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	10448516	105988	1	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	317	3	2	5	2.8	Cc1noc(NS(=O)(=O)c2cccc3cc(N)ccc23)c1C	10.1021/jm00008a013
	CHEMBL281511	105988	1	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	317	3	2	5	2.8	Cc1noc(NS(=O)(=O)c2cccc3cc(N)ccc23)c1C	10.1021/jm00008a013
	CHEMBL413880	219873	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Binding affinity in LtK cells stably transfected with human endothelin A (ETA) receptorBinding affinity in LtK cells stably transfected with human endothelin A (ETA) receptor	ChEMBL		None	None	None		NC(=O)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)N[C@H](Cc1c[nH]c2ccccc12)C(=O)O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/0960-894X(95)00084-7
	44314579	109694	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Binding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranesBinding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranes	ChEMBL	580	12	5	5	3.8	CCCCC(NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C)C(=O)O	10.1021/jm9600914
	CHEMBL306123	109694	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Binding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranesBinding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranes	ChEMBL	580	12	5	5	3.8	CCCCC(NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C)C(=O)O	10.1021/jm9600914
	10618166	66625	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	355	7	1	6	4.0	N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1ccco1	10.1021/jm990378b
	CHEMBL172880	66625	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	355	7	1	6	4.0	N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1ccco1	10.1021/jm990378b
	10151203	107577	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)	ChEMBL	429	5	1	6	4.2	COc1ccc(Cn2c(=O)c(C(=O)O)c(-c3ccc4c(c3)OCO4)c3ccccc32)cc1	10.1016/S0960-894X(97)00319-3
	CHEMBL293151	107577	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)	ChEMBL	429	5	1	6	4.2	COc1ccc(Cn2c(=O)c(C(=O)O)c(-c3ccc4c(c3)OCO4)c3ccccc32)cc1	10.1016/S0960-894X(97)00319-3
	10448516	105988	1	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	317	3	2	5	2.8	Cc1noc(NS(=O)(=O)c2cccc3cc(N)ccc23)c1C	10.1021/jm00004a012
	CHEMBL281511	105988	1	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	317	3	2	5	2.8	Cc1noc(NS(=O)(=O)c2cccc3cc(N)ccc23)c1C	10.1021/jm00004a012
	44266568	104873	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	493	7	1	6	6.3	COc1ccc(-c2c(C(=O)O)n(-c3ccc4c(c3)OCO4)c3ccc(OCc4ccccc4)cc23)cc1	10.1016/0960-894X(96)00170-9
	CHEMBL273410	104873	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	493	7	1	6	6.3	COc1ccc(-c2c(C(=O)O)n(-c3ccc4c(c3)OCO4)c3ccc(OCc4ccccc4)cc23)cc1	10.1016/0960-894X(96)00170-9
	10313743	102321	0	None	-	0	Rat	4.6	pIC50	=	4.6	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	317	3	2	5	2.8	Cc1noc(NS(=O)(=O)c2ccc3c(N)cccc3c2)c1C	10.1021/jm00008a013
	CHEMBL25756	102321	0	None	-	0	Rat	4.6	pIC50	=	4.6	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	317	3	2	5	2.8	Cc1noc(NS(=O)(=O)c2ccc3c(N)cccc3c2)c1C	10.1021/jm00008a013
	10314989	106637	1	None	-	0	Rat	4.6	pIC50	=	4.6	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	336	3	1	4	3.9	Cc1noc(NS(=O)(=O)c2cccc3c(Cl)cccc23)c1C	10.1021/jm00008a013
	CHEMBL285814	106637	1	None	-	0	Rat	4.6	pIC50	=	4.6	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	336	3	1	4	3.9	Cc1noc(NS(=O)(=O)c2cccc3c(Cl)cccc23)c1C	10.1021/jm00008a013
	127035379	143285	0	None	-	0	Human	4.6	pIC50	=	4.6	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	691	13	2	8	7.4	CCCc1nc2c(C)cc(C(=O)NCCc3cccc(OC)c3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	CHEMBL3736248	143285	0	None	-	0	Human	4.6	pIC50	=	4.6	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	691	13	2	8	7.4	CCCc1nc2c(C)cc(C(=O)NCCc3cccc(OC)c3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	10507191	135570	0	None	-	0	Rat	4.6	pIC50	=	4.6	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	565	10	4	5	5.6	CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(C2CC2)s1	10.1021/jm950591h
	CHEMBL366911	135570	0	None	-	0	Rat	4.6	pIC50	=	4.6	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	565	10	4	5	5.6	CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(C2CC2)s1	10.1021/jm950591h
	CHEMBL2369710	216432	0	None	-	0	Human	4.6	pIC50	=	4.6	Binding	Inhibition of [125I]endothelin-1 [ET-1] binding to endothelin A receptor (ETA) of rabbit renal artery vascular smooth muscle cellsInhibition of [125I]endothelin-1 [ET-1] binding to endothelin A receptor (ETA) of rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/0960-894X(95)00152-J
	10313743	102321	0	None	-	0	Rat	4.6	pIC50	=	4.6	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	317	3	2	5	2.8	Cc1noc(NS(=O)(=O)c2ccc3c(N)cccc3c2)c1C	10.1021/jm00004a012
	CHEMBL25756	102321	0	None	-	0	Rat	4.6	pIC50	=	4.6	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	317	3	2	5	2.8	Cc1noc(NS(=O)(=O)c2ccc3c(N)cccc3c2)c1C	10.1021/jm00004a012
	10813822	103745	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	460	5	2	5	4.5	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2C(=O)Nc2ccccc2)cc1	10.1021/jm9505369
	CHEMBL266336	103745	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	460	5	2	5	4.5	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2C(=O)Nc2ccccc2)cc1	10.1021/jm9505369
	9915028	16183	18	None	28183	2	Human	4.6	pIC50	=	4.6	Binding	Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)	ChEMBL	532	15	1	6	5.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC	10.1021/jm980217s
	CHEMBL111612	16183	18	None	28183	2	Human	4.6	pIC50	=	4.6	Binding	Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)	ChEMBL	532	15	1	6	5.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC	10.1021/jm980217s
	CHEMBL4761843	16183	18	None	28183	2	Human	4.6	pIC50	=	4.6	Binding	Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)	ChEMBL	532	15	1	6	5.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC	10.1021/jm980217s
	10218058	88444	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)	ChEMBL	523	12	2	10	3.1	COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCO	10.1016/j.bmcl.2016.06.014
	CHEMBL2163695	88444	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)	ChEMBL	523	12	2	10	3.1	COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCO	10.1016/j.bmcl.2016.06.014
	CHEMBL97470	222704	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	10600668	11930	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	476	7	1	8	3.8	COc1cc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc(OC)c1OC	10.1021/jm9606507
	CHEMBL10589	11930	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	476	7	1	8	3.8	COc1cc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc(OC)c1OC	10.1021/jm9606507
	10625269	21228	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	502	7	2	6	4.5	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2ccc(C)cc2C)cc1	10.1021/jm990170q
	CHEMBL120106	21228	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	502	7	2	6	4.5	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2ccc(C)cc2C)cc1	10.1021/jm990170q
	10792783	67150	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor	ChEMBL	551	10	3	6	5.0	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N(C)C2CCCCC2)nc1C(=O)O	10.1021/jm9505932
	CHEMBL174699	67150	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor	ChEMBL	551	10	3	6	5.0	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N(C)C2CCCCC2)nc1C(=O)O	10.1021/jm9505932
	10218058	88444	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	523	12	2	10	3.1	COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCO	10.1021/jm3009103
	CHEMBL2163695	88444	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	523	12	2	10	3.1	COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCO	10.1021/jm3009103
	10951918	117650	0	None	-	0	Pig	7.6	pIC50	=	7.6	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	567	11	1	10	5.3	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2SCCOc2ncccn2)c1	10.1021/jm0102304
	CHEMBL326105	117650	0	None	-	0	Pig	7.6	pIC50	=	7.6	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	567	11	1	10	5.3	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2SCCOc2ncccn2)c1	10.1021/jm0102304
	44327656	148567	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL	977	25	9	8	4.7	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C(F)(F)F)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	CHEMBL386181	148567	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL	977	25	9	8	4.7	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C(F)(F)F)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	CHEMBL21253	216054	0	None	-	0	Mouse	6.6	pIC50	=	6.6	Binding	Binding affinity for Endothelin A receptor was determined in murine 3T3 cellsBinding affinity for Endothelin A receptor was determined in murine 3T3 cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](N)CCCNC(=O)[C@H](Cc1ccccc1)NC(C)=O)[C@@H](C)CC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/S0960-894X(00)80326-1
	10862228	209740	0	None	-	0	Rat	6.6	pIC50	=	6.6	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	398	7	1	6	4.2	CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC)cc21	10.1021/jm010382z
	CHEMBL63000	209740	0	None	-	0	Rat	6.6	pIC50	=	6.6	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	398	7	1	6	4.2	CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC)cc21	10.1021/jm010382z
	CHEMBL405677	219353	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Binding affinity in LtK cells stably transfected with human endothelin A (ETA) receptorBinding affinity in LtK cells stably transfected with human endothelin A (ETA) receptor	ChEMBL		None	None	None		CC(=O)[C@@H](Cc1c[nH]c2ccccc12)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/0960-894X(95)00084-7
	44266552	11285	0	None	-	0	Rat	6.6	pIC50	=	6.6	Binding	Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor	ChEMBL	473	7	1	7	5.3	CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2c(c1)OCO2	10.1016/s0960-894x(97)10151-2
	CHEMBL10218	11285	0	None	-	0	Rat	6.6	pIC50	=	6.6	Binding	Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor	ChEMBL	473	7	1	7	5.3	CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2c(c1)OCO2	10.1016/s0960-894x(97)10151-2
	56671734	70103	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells	ChEMBL	937	26	9	9	3.6	CC[C@H](C)[C@H](NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)NCC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)[C@@H](C)CC	10.1021/jm970161m
	CHEMBL1793932	70103	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells	ChEMBL	937	26	9	9	3.6	CC[C@H](C)[C@H](NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)NCC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)[C@@H](C)CC	10.1021/jm970161m
	44266552	11285	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Potency at Endothelin A receptor was determinedPotency at Endothelin A receptor was determined	ChEMBL	473	7	1	7	5.3	CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2c(c1)OCO2	10.1021/jm0300429
	CHEMBL10218	11285	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Potency at Endothelin A receptor was determinedPotency at Endothelin A receptor was determined	ChEMBL	473	7	1	7	5.3	CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2c(c1)OCO2	10.1021/jm0300429
	CHEMBL341443	218419	0	None	-	0	Pig	6.6	pIC50	=	6.6	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H](CCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	44368824	103602	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)	ChEMBL	1595	31	19	20	0.6	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)NCCCCC(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)80156-6
	77282142	103602	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)	ChEMBL	1595	31	19	20	0.6	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)NCCCCC(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)80156-6
	CHEMBL265164	103602	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)	ChEMBL	1595	31	19	20	0.6	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)NCCCCC(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)80156-6
	CHEMBL412460	219770	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)80156-6
	18617363	171339	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	384	3	1	4	3.9	Cc1noc(NS(=O)(=O)c2ccc(Cl)cc2Cl)c1Br	10.1016/0960-894X(96)00441-6
	CHEMBL421523	171339	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	384	3	1	4	3.9	Cc1noc(NS(=O)(=O)c2ccc(Cl)cc2Cl)c1Br	10.1016/0960-894X(96)00441-6
	CHEMBL37860	219041	0	None	-	0	Pig	5.6	pIC50	=	5.6	Binding	Compound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranesCompound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranes	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N(C)[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccn1)C(=O)O	10.1021/jm00087a001
	44368905	168601	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	In vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricleIn vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricle	ChEMBL	1623	31	19	20	1.3	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)NCCCCCCC(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)80156-6
	77282145	168601	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	In vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricleIn vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricle	ChEMBL	1623	31	19	20	1.3	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)NCCCCCCC(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)80156-6
	CHEMBL414448	168601	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	In vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricleIn vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricle	ChEMBL	1623	31	19	20	1.3	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)NCCCCCCC(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)80156-6
	10792784	66369	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	551	10	4	5	5.4	CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(C(C)C)o1	10.1021/jm950591h
	CHEMBL171910	66369	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	551	10	4	5	5.4	CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(C(C)C)o1	10.1021/jm950591h
	44309488	210788	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor	ChEMBL	471	7	1	8	5.1	CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2nonc2c1	10.1016/s0960-894x(97)10151-2
	CHEMBL69664	210788	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor	ChEMBL	471	7	1	8	5.1	CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2nonc2c1	10.1016/s0960-894x(97)10151-2
	44327726	214671	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	495	6	1	8	2.7	CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)n2nc3c(cc2=O)CCC3)cc1	10.1016/S0960-894X(96)00617-8
	CHEMBL96644	214671	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	495	6	1	8	2.7	CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)n2nc3c(cc2=O)CCC3)cc1	10.1016/S0960-894X(96)00617-8
	44309488	210788	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Potency at Endothelin A receptor was determinedPotency at Endothelin A receptor was determined	ChEMBL	471	7	1	8	5.1	CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2nonc2c1	10.1021/jm0300429
	CHEMBL69664	210788	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Potency at Endothelin A receptor was determinedPotency at Endothelin A receptor was determined	ChEMBL	471	7	1	8	5.1	CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2nonc2c1	10.1021/jm0300429
	10038537	66747	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Tested for binding affinity towards human Endothelin A receptorTested for binding affinity towards human Endothelin A receptor	ChEMBL	266	3	2	5	0.8	C/C=C/C=C/C(=O)O[C@@H]1C=C2COC(O)[C@]2(O)CC1	10.1016/s0960-894x(00)00136-0
	CHEMBL173336	66747	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Tested for binding affinity towards human Endothelin A receptorTested for binding affinity towards human Endothelin A receptor	ChEMBL	266	3	2	5	0.8	C/C=C/C=C/C(=O)O[C@@H]1C=C2COC(O)[C@]2(O)CC1	10.1016/s0960-894x(00)00136-0
	44279479	106063	1	None	-	0	Pig	4.6	pIC50	=	4.6	Binding	Binding affinity against ETA receptor in porcine aortic smooth muscle membrane was determinedBinding affinity against ETA receptor in porcine aortic smooth muscle membrane was determined	ChEMBL	516	14	6	5	1.8	CC(C)CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CC(=O)O)C(=O)O	10.1016/0960-894X(95)00221-E
	CHEMBL281963	106063	1	None	-	0	Pig	4.6	pIC50	=	4.6	Binding	Binding affinity against ETA receptor in porcine aortic smooth muscle membrane was determinedBinding affinity against ETA receptor in porcine aortic smooth muscle membrane was determined	ChEMBL	516	14	6	5	1.8	CC(C)CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CC(=O)O)C(=O)O	10.1016/0960-894X(95)00221-E
	44279439	114155	0	None	-	0	Human	4.6	pIC50	=	4.6	Binding	Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor	ChEMBL	534	3	2	3	6.2	O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(-c3ccc(C(F)(F)F)cc3C(F)(F)F)cc21	10.1016/0960-894X(95)00230-Q
	CHEMBL31781	114155	0	None	-	0	Human	4.6	pIC50	=	4.6	Binding	Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor	ChEMBL	534	3	2	3	6.2	O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(-c3ccc(C(F)(F)F)cc3C(F)(F)F)cc21	10.1016/0960-894X(95)00230-Q
	CHEMBL137569	215524	0	None	-	0	Pig	4.6	pIC50	=	4.6	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CCCC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	10787482	103736	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	405	4	1	4	3.9	CN(C)c1cccc2c(S(=O)(=O)Nc3ccc(Br)nc3)cccc12	10.1021/jm9604585
	CHEMBL266277	103736	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	405	4	1	4	3.9	CN(C)c1cccc2c(S(=O)(=O)Nc3ccc(Br)nc3)cccc12	10.1021/jm9604585
	10740139	209734	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	406	4	1	5	3.3	CN(C)c1cccc2c(S(=O)(=O)Nc3ccc(Br)nn3)cccc12	10.1021/jm9604585
	CHEMBL6297	209734	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	406	4	1	5	3.3	CN(C)c1cccc2c(S(=O)(=O)Nc3ccc(Br)nn3)cccc12	10.1021/jm9604585
	18617288	211925	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	316	3	1	4	2.5	Cc1noc(NS(=O)(=O)c2ccccc2)c1Br	10.1016/S0960-894X(96)00496-9
	CHEMBL78080	211925	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	316	3	1	4	2.5	Cc1noc(NS(=O)(=O)c2ccccc2)c1Br	10.1016/S0960-894X(96)00496-9
	10646522	210171	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	434	5	1	5	3.8	CCc1nc(Br)cnc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12	10.1021/jm9604585
	CHEMBL6543	210171	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	434	5	1	5	3.8	CCc1nc(Br)cnc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12	10.1021/jm9604585
	22998439	209875	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	392	5	1	7	3.7	Cc1ccc(OC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1016/S0960-894X(97)00367-3
	CHEMBL63938	209875	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	392	5	1	7	3.7	Cc1ccc(OC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1016/S0960-894X(97)00367-3
	10650368	67141	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	553	10	5	7	3.6	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCC(O)CC2)nc1C(=O)O	10.1021/jm950592+
	CHEMBL174635	67141	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	553	10	5	7	3.6	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCC(O)CC2)nc1C(=O)O	10.1021/jm950592+
	10789715	119875	0	None	-	0	Rat	6.6	pIC50	=	6.6	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	450	8	1	5	4.2	CCCN(C)C(=O)CN1C[C@H](c2cccc3occc23)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	CHEMBL331375	119875	0	None	-	0	Rat	6.6	pIC50	=	6.6	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	450	8	1	5	4.2	CCCN(C)C(=O)CN1C[C@H](c2cccc3occc23)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	10575552	118086	0	None	-	0	Rat	6.6	pIC50	=	6.6	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	450	8	1	5	4.2	CCCN(C)C(=O)CN1C[C@H](c2ccc3ccoc3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	CHEMBL326690	118086	0	None	-	0	Rat	6.6	pIC50	=	6.6	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	450	8	1	5	4.2	CCCN(C)C(=O)CN1C[C@H](c2ccc3ccoc3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	9871561	181579	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)	ChEMBL	527	10	2	8	4.6	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cc2)nc(C(F)(F)F)nc1OCCO	10.1016/j.bmcl.2016.06.014
	CHEMBL4562189	181579	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)	ChEMBL	527	10	2	8	4.6	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cc2)nc(C(F)(F)F)nc1OCCO	10.1016/j.bmcl.2016.06.014
	44314657	109980	0	None	-	0	Pig	7.6	pIC50	=	7.6	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	619	13	5	4	4.3	CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1CCCCC1)C(=O)O	10.1021/jm9600914
	CHEMBL308383	109980	0	None	-	0	Pig	7.6	pIC50	=	7.6	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	619	13	5	4	4.3	CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1CCCCC1)C(=O)O	10.1021/jm9600914
	10288020	21401	0	None	-	0	Rat	7.6	pIC50	=	7.6	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	430	7	1	6	4.7	COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1	10.1016/s0960-894x(98)00301-1
	CHEMBL1205067	21401	0	None	-	0	Rat	7.6	pIC50	=	7.6	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	430	7	1	6	4.7	COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1	10.1016/s0960-894x(98)00301-1
	CHEMBL48881	21401	0	None	-	0	Rat	7.6	pIC50	=	7.6	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	430	7	1	6	4.7	COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1	10.1016/s0960-894x(98)00301-1
	11796594	214157	0	None	-	0	Rat	7.6	pIC50	=	7.6	Binding	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	ChEMBL	424	10	1	5	5.8	CC(=O)c1ccc(OCc2ccsc2)cc1OC(CCC(=O)O)c1ccccc1C	10.1021/jm9707131
	CHEMBL93776	214157	0	None	-	0	Rat	7.6	pIC50	=	7.6	Binding	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	ChEMBL	424	10	1	5	5.8	CC(=O)c1ccc(OCc2ccsc2)cc1OC(CCC(=O)O)c1ccccc1C	10.1021/jm9707131
	10144334	137442	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	561	10	2	10	4.0	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccncc2)nc1OCC#CCO	10.1016/s0960-894x(02)01084-3
	CHEMBL368211	137442	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	561	10	2	10	4.0	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccncc2)nc1OCC#CCO	10.1016/s0960-894x(02)01084-3
	CHEMBL147510	215557	0	None	-	0	Mouse	7.6	pIC50	=	7.6	Binding	Inhibition of [125I]ET1 binding to Endothelin A receptor of murine 3T3 cellsInhibition of [125I]ET1 binding to Endothelin A receptor of murine 3T3 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCN)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@H](C)CC	10.1016/S0960-894X(01)81219-1
	44385941	137454	0	None	-	0	Rat	7.6	pIC50	=	7.6	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	550	10	5	5	4.6	Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCC(C)C2)nc1C(=O)O	10.1021/jm950592+
	CHEMBL368286	137454	0	None	-	0	Rat	7.6	pIC50	=	7.6	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	550	10	5	5	4.6	Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCC(C)C2)nc1C(=O)O	10.1021/jm950592+
	31771	103741	37	None	-	0	Rat	6.6	pIC50	=	6.6	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	267	3	2	5	1.7	Cc1onc(NS(=O)(=O)c2ccc(N)cc2)c1C	10.1021/jm00008a013
	CHEMBL26630	103741	37	None	-	0	Rat	6.6	pIC50	=	6.6	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	267	3	2	5	1.7	Cc1onc(NS(=O)(=O)c2ccc(N)cc2)c1C	10.1021/jm00008a013
	11755275	206788	0	None	-	1	Rat	6.6	pIC50	=	6.6	Binding	Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)	ChEMBL	489	9	1	7	4.8	CCOc1ccc2c(c1)c(-c1ccc(OC)cc1)c(C(=O)O)c(=O)n2Cc1cc(OC)ccc1OC	10.1016/S0960-894X(97)00319-3
	CHEMBL59537	206788	0	None	-	1	Rat	6.6	pIC50	=	6.6	Binding	Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)	ChEMBL	489	9	1	7	4.8	CCOc1ccc2c(c1)c(-c1ccc(OC)cc1)c(C(=O)O)c(=O)n2Cc1cc(OC)ccc1OC	10.1016/S0960-894X(97)00319-3
	31771	103741	37	None	-	0	Rat	6.6	pIC50	=	6.6	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	267	3	2	5	1.7	Cc1onc(NS(=O)(=O)c2ccc(N)cc2)c1C	10.1021/jm00004a012
	CHEMBL26630	103741	37	None	-	0	Rat	6.6	pIC50	=	6.6	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	267	3	2	5	1.7	Cc1onc(NS(=O)(=O)c2ccc(N)cc2)c1C	10.1021/jm00004a012
	56657875	70099	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells	ChEMBL	937	26	9	9	3.6	CC[C@H](C)[C@H](NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)[C@@H](C)CC	10.1021/jm970161m
	CHEMBL1793925	70099	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells	ChEMBL	937	26	9	9	3.6	CC[C@H](C)[C@H](NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)[C@@H](C)CC	10.1021/jm970161m
	56681798	70102	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells	ChEMBL	937	26	9	9	3.6	CC[C@@H](C)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)CNC(=O)[C@H](NC(=O)[C@H](N)Cc1c[nH]c2ccccc12)[C@H](C)CC	10.1021/jm970161m
	CHEMBL1793929	70102	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells	ChEMBL	937	26	9	9	3.6	CC[C@@H](C)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)CNC(=O)[C@H](NC(=O)[C@H](N)Cc1c[nH]c2ccccc12)[C@H](C)CC	10.1021/jm970161m
	44327252	214312	0	None	-	0	Rat	6.6	pIC50	=	6.6	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	495	7	1	8	3.1	CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)n2nc(C3CC3)ccc2=O)cc1	10.1016/S0960-894X(96)00617-8
	CHEMBL94654	214312	0	None	-	0	Rat	6.6	pIC50	=	6.6	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	495	7	1	8	3.1	CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)n2nc(C3CC3)ccc2=O)cc1	10.1016/S0960-894X(96)00617-8
	44266592	12147	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	431	4	1	7	4.5	COc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2-c1ccc2c(c1)OCO2	10.1016/0960-894X(96)00170-9
	CHEMBL10699	12147	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	431	4	1	7	4.5	COc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2-c1ccc2c(c1)OCO2	10.1016/0960-894X(96)00170-9
	CHEMBL137754	215528	0	None	-	0	Pig	6.6	pIC50	=	6.6	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	CHEMBL436884	220469	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)80156-6
	44328019	162483	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL	1000	26	9	8	5.4	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	CHEMBL405178	162483	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL	1000	26	9	8	5.4	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	44327348	168686	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL	1076	28	9	8	7.0	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	CHEMBL415238	168686	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL	1076	28	9	8	7.0	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	10216862	203191	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)	ChEMBL	443	4	1	7	3.9	O=C(O)c1c(-c2ccc3c(c2)OCO3)c2ccccc2n(Cc2ccc3c(c2)OCO3)c1=O	10.1016/S0960-894X(97)00319-3
	CHEMBL56286	203191	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)	ChEMBL	443	4	1	7	3.9	O=C(O)c1c(-c2ccc3c(c2)OCO3)c2ccccc2n(Cc2ccc3c(c2)OCO3)c1=O	10.1016/S0960-894X(97)00319-3
	44327412	214360	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	497	5	1	8	3.0	Cc1cc(C)c(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c2ccc3c(c2)OCO3)n1	10.1016/S0960-894X(96)00617-8
	CHEMBL94929	214360	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	497	5	1	8	3.0	Cc1cc(C)c(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c2ccc3c(c2)OCO3)n1	10.1016/S0960-894X(96)00617-8
	44327114	214587	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	533	7	1	7	4.1	CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)N2N=C(c3ccccc3)CCC2=O)cc1	10.1016/S0960-894X(96)00617-8
	CHEMBL96234	214587	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	533	7	1	7	4.1	CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)N2N=C(c3ccccc3)CCC2=O)cc1	10.1016/S0960-894X(96)00617-8
	10244529	66056	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Tested for binding affinity towards human Endothelin A receptorTested for binding affinity towards human Endothelin A receptor	ChEMBL	264	3	1	5	1.0	C/C=C/C=C/C(=O)O[C@@H]1C=C2COC(=O)[C@]2(O)CC1	10.1016/s0960-894x(00)00136-0
	CHEMBL170450	66056	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Tested for binding affinity towards human Endothelin A receptorTested for binding affinity towards human Endothelin A receptor	ChEMBL	264	3	1	5	1.0	C/C=C/C=C/C(=O)O[C@@H]1C=C2COC(=O)[C@]2(O)CC1	10.1016/s0960-894x(00)00136-0
	44279371	106700	0	None	-	0	Human	4.6	pIC50	=	4.6	Binding	Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor	ChEMBL	466	3	2	3	5.5	O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(-c3cc(Cl)cc(Cl)c3)cc21	10.1016/0960-894X(95)00230-Q
	CHEMBL286214	106700	0	None	-	0	Human	4.6	pIC50	=	4.6	Binding	Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor	ChEMBL	466	3	2	3	5.5	O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(-c3cc(Cl)cc(Cl)c3)cc21	10.1016/0960-894X(95)00230-Q
	6426756	157488	40	None	-	0	Human	4.6	pIC50	=	4.6	Binding	Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes	ChEMBL	537	9	3	10	3.9	CC(C)(C)c1ccc(S(=O)(=O)Nc2nc(-c3ncccn3)nc(OCCO)c2Oc2ccccc2O)cc1	10.1016/j.bmcl.2016.06.014
	CHEMBL3956076	157488	40	None	-	0	Human	4.6	pIC50	=	4.6	Binding	Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes	ChEMBL	537	9	3	10	3.9	CC(C)(C)c1ccc(S(=O)(=O)Nc2nc(-c3ncccn3)nc(OCCO)c2Oc2ccccc2O)cc1	10.1016/j.bmcl.2016.06.014
	23445254	213934	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	412	5	1	5	4.2	Cc1noc(NS(=O)(=O)c2sccc2Cc2ccccc2)c1Br	10.1016/S0960-894X(96)00496-9
	CHEMBL92318	213934	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	412	5	1	5	4.2	Cc1noc(NS(=O)(=O)c2sccc2Cc2ccccc2)c1Br	10.1016/S0960-894X(96)00496-9
	9810571	68160	0	None	-	2	Human	6.6	pIC50	=	6.6	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	731	18	2	13	5.0	CCCS(=O)(=O)NCCOc1nc(-c2cc(OC)c(OC)c(OC)c2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	CHEMBL176997	68160	0	None	-	2	Human	6.6	pIC50	=	6.6	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	731	18	2	13	5.0	CCCS(=O)(=O)NCCOc1nc(-c2cc(OC)c(OC)c(OC)c2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	127034756	143131	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	679	12	2	7	7.5	CCCc1nc2c(C)cc(C(=O)NCCc3ccccc3F)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	CHEMBL3734829	143131	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	679	12	2	7	7.5	CCCc1nc2c(C)cc(C(=O)NCCc3ccccc3F)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	176	7186	66	None	-7	31	Human	4.6	pIC50	=	4.6	Binding	DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
	2157	7186	66	None	-7	31	Human	4.6	pIC50	=	4.6	Binding	DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
	2566	7186	66	None	-7	31	Human	4.6	pIC50	=	4.6	Binding	DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
	CHEMBL633	7186	66	None	-7	31	Human	4.6	pIC50	=	4.6	Binding	DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
	DB01118	7186	66	None	-7	31	Human	4.6	pIC50	=	4.6	Binding	DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
	18617393	212056	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	308	5	1	4	3.2	CCc1ccc(CC)c(S(=O)(=O)Nc2onc(C)c2C)c1	10.1016/0960-894X(96)00441-6
	CHEMBL79066	212056	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	308	5	1	4	3.2	CCc1ccc(CC)c(S(=O)(=O)Nc2onc(C)c2C)c1	10.1016/0960-894X(96)00441-6
	44314647	211864	0	None	-	0	Pig	7.6	pIC50	=	7.6	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	647	13	5	4	5.1	CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1CCCCCCC1)C(=O)O	10.1021/jm9600914
	CHEMBL77468	211864	0	None	-	0	Pig	7.6	pIC50	=	7.6	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	647	13	5	4	5.1	CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1CCCCCCC1)C(=O)O	10.1021/jm9600914
	CHEMBL2304016	216251	0	None	-	0	Pig	7.6	pIC50	=	7.6	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)[C@H]1NC(=O)[C@H](C(C)(C)C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc2c(Cl)[nH]c3ccccc23)NC1=O	10.1021/jm9600914
	10502226	108305	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	420	6	1	8	3.3	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Cc2ccc3c(c2)OCO3)c1C	10.1021/jm9700068
	CHEMBL298203	108305	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	420	6	1	8	3.3	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Cc2ccc3c(c2)OCO3)c1C	10.1021/jm9700068
	10715441	182705	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	390	6	1	6	3.9	Cc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1021/jm9700068
	CHEMBL45875	182705	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	390	6	1	6	3.9	Cc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1021/jm9700068
	10575755	186596	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	455	5	2	6	4.2	Cc1ccccc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Br	10.1021/jm9608366
	CHEMBL47450	186596	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	455	5	2	6	4.2	Cc1ccccc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Br	10.1021/jm9608366
	10168195	68161	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	631	11	2	13	5.0	C#CCOc1nc(-c2ccnc(-c3noc(S)n3)c2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	CHEMBL176999	68161	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	631	11	2	13	5.0	C#CCOc1nc(-c2ccnc(-c3noc(S)n3)c2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	10744085	109647	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	503	9	1	8	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OCCN(C)C)c2)cc1	10.1021/jm980504w
	CHEMBL305777	109647	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	503	9	1	8	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OCCN(C)C)c2)cc1	10.1021/jm980504w
	10318748	106407	0	None	-	0	Rat	6.6	pIC50	=	6.6	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	399	4	1	5	3.8	Cc1noc(NS(=O)(=O)c2cccc3c(N4CCCCC4=O)cccc23)c1C	10.1021/jm00008a013
	CHEMBL284177	106407	0	None	-	0	Rat	6.6	pIC50	=	6.6	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	399	4	1	5	3.8	Cc1noc(NS(=O)(=O)c2cccc3c(N4CCCCC4=O)cccc23)c1C	10.1021/jm00008a013
	44316527	212259	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	280	3	1	4	2.7	Cc1ccc(C)c(S(=O)(=O)Nc2onc(C)c2C)c1	10.1016/0960-894X(96)00441-6
	CHEMBL80532	212259	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	280	3	1	4	2.7	Cc1ccc(C)c(S(=O)(=O)Nc2onc(C)c2C)c1	10.1016/0960-894X(96)00441-6
	44316831	212294	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	358	4	1	4	3.4	CCc1ccc(Br)c(S(=O)(=O)Nc2onc(C)c2C)c1	10.1016/0960-894X(96)00441-6
	CHEMBL80807	212294	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	358	4	1	4	3.4	CCc1ccc(Br)c(S(=O)(=O)Nc2onc(C)c2C)c1	10.1016/0960-894X(96)00441-6
	15296635	106331	0	None	-	0	Pig	6.6	pIC50	=	6.6	Binding	Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	488	11	5	5	2.7	CC(C)C[C@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	CHEMBL283591	106331	0	None	-	0	Pig	6.6	pIC50	=	6.6	Binding	Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	488	11	5	5	2.7	CC(C)C[C@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	23445224	210177	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	406	5	1	7	4.0	Cc1ccc(OC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2C)c(C)c1	10.1016/S0960-894X(97)00367-3
	CHEMBL65488	210177	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	406	5	1	7	4.0	Cc1ccc(OC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2C)c(C)c1	10.1016/S0960-894X(97)00367-3
	CHEMBL356864	218521	0	None	-	0	Mouse	6.6	pIC50	=	6.6	Binding	Inhibition of [125I]ET1 binding to Endothelin A receptor of murine 3T3 cellsInhibition of [125I]ET1 binding to Endothelin A receptor of murine 3T3 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@H](C)CC	10.1016/S0960-894X(01)81219-1
	CHEMBL1791006	215691	0	None	-	0	Pig	6.6	pIC50	=	6.6	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H]([C@H](C)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	44371396	56292	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes	ChEMBL	471	6	1	6	5.9	COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3SC)c3c2oc2ccccc23)cc1	10.1016/s0960-894x(99)00040-2
	CHEMBL156532	56292	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes	ChEMBL	471	6	1	6	5.9	COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3SC)c3c2oc2ccccc23)cc1	10.1016/s0960-894x(99)00040-2
	44371532	58249	1	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes	ChEMBL	455	6	1	6	5.2	COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3cccc(OC)c3)c3c2oc2ccccc23)cc1	10.1016/s0960-894x(99)00040-2
	CHEMBL158239	58249	1	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes	ChEMBL	455	6	1	6	5.2	COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3cccc(OC)c3)c3c2oc2ccccc23)cc1	10.1016/s0960-894x(99)00040-2
	44371571	126267	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes	ChEMBL	425	5	1	5	5.2	COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3)c3c2oc2ccccc23)cc1	10.1016/s0960-894x(99)00040-2
	CHEMBL345380	126267	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes	ChEMBL	425	5	1	5	5.2	COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3)c3c2oc2ccccc23)cc1	10.1016/s0960-894x(99)00040-2
	10473627	108666	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	359	4	2	5	3.2	CC(=O)Nc1cccc2cc(S(=O)(=O)Nc3onc(C)c3C)ccc12	10.1021/jm00008a013
	CHEMBL30077	108666	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	359	4	2	5	3.2	CC(=O)Nc1cccc2cc(S(=O)(=O)Nc3onc(C)c3C)ccc12	10.1021/jm00008a013
	18617395	212051	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	361	4	1	6	2.5	Cc1noc(NS(=O)(=O)c2cccc([N+](=O)[O-])c2)c1Br	10.1016/0960-894X(96)00441-6
	CHEMBL79030	212051	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	361	4	1	6	2.5	Cc1noc(NS(=O)(=O)c2cccc([N+](=O)[O-])c2)c1Br	10.1016/0960-894X(96)00441-6
	10473627	108666	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	359	4	2	5	3.2	CC(=O)Nc1cccc2cc(S(=O)(=O)Nc3onc(C)c3C)ccc12	10.1021/jm00004a012
	CHEMBL30077	108666	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	359	4	2	5	3.2	CC(=O)Nc1cccc2cc(S(=O)(=O)Nc3onc(C)c3C)ccc12	10.1021/jm00004a012
	56681797	70098	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells	ChEMBL	937	26	9	9	3.6	CC[C@H](C)[C@H](NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)[C@H](C)CC	10.1021/jm970161m
	CHEMBL1793924	70098	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells	ChEMBL	937	26	9	9	3.6	CC[C@H](C)[C@H](NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)[C@H](C)CC	10.1021/jm970161m
	44213924	214275	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	567	7	1	7	4.8	CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)N2N=C(c3ccc(Cl)cc3)CCC2=O)cc1	10.1016/S0960-894X(96)00617-8
	CHEMBL94426	214275	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	567	7	1	7	4.8	CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)N2N=C(c3ccc(Cl)cc3)CCC2=O)cc1	10.1016/S0960-894X(96)00617-8
	44266537	11100	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	507	8	1	6	6.4	COc1ccc(Cn2c(C(=O)O)c(-c3ccc4c(c3)OCO4)c3cc(OCc4ccccc4)ccc32)cc1	10.1016/0960-894X(96)00170-9
	CHEMBL10092	11100	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	507	8	1	6	6.4	COc1ccc(Cn2c(C(=O)O)c(-c3ccc4c(c3)OCO4)c3cc(OCc4ccccc4)ccc32)cc1	10.1016/0960-894X(96)00170-9
	44368414	128065	0	None	-	0	Pig	4.6	pIC50	=	4.6	Binding	Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.	ChEMBL	459	9	1	5	4.2	COc1ccc(CN(C(=O)/C=C/c2ccc3c(c2)OCO3)C(Cc2ccccc2)C(=O)O)cc1	10.1016/s0960-894x(01)00009-9
	CHEMBL357978	128065	0	None	-	0	Pig	4.6	pIC50	=	4.6	Binding	Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.	ChEMBL	459	9	1	5	4.2	COc1ccc(CN(C(=O)/C=C/c2ccc3c(c2)OCO3)C(Cc2ccccc2)C(=O)O)cc1	10.1016/s0960-894x(01)00009-9
	10470588	106768	2	None	-	0	Human	4.6	pIC50	=	4.6	Binding	Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells	ChEMBL	309	6	2	5	2.9	CCCNc1ccc(S(=O)(=O)Nc2onc(C)c2C)cc1	10.1021/jm00029a001
	CHEMBL286682	106768	2	None	-	0	Human	4.6	pIC50	=	4.6	Binding	Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells	ChEMBL	309	6	2	5	2.9	CCCNc1ccc(S(=O)(=O)Nc2onc(C)c2C)cc1	10.1021/jm00029a001
	10470588	106768	2	None	-	0	Rat	4.6	pIC50	=	4.6	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	309	6	2	5	2.9	CCCNc1ccc(S(=O)(=O)Nc2onc(C)c2C)cc1	10.1021/jm00008a013
	CHEMBL286682	106768	2	None	-	0	Rat	4.6	pIC50	=	4.6	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	309	6	2	5	2.9	CCCNc1ccc(S(=O)(=O)Nc2onc(C)c2C)cc1	10.1021/jm00008a013
	127035068	143151	0	None	-	0	Human	4.6	pIC50	=	4.6	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	633	10	2	7	7.7	CCCc1nc2c(C)cc(C(=O)Nc3ccccc3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	CHEMBL3735036	143151	0	None	-	0	Human	4.6	pIC50	=	4.6	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	633	10	2	7	7.7	CCCc1nc2c(C)cc(C(=O)Nc3ccccc3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	10604119	18229	0	None	-	0	Human	4.6	pIC50	=	4.6	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	636	12	2	7	5.8	COCCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2C)c2ccccc2C)cc1	10.1021/jm990171i
	CHEMBL1180361	18229	0	None	-	0	Human	4.6	pIC50	=	4.6	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	636	12	2	7	5.8	COCCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2C)c2ccccc2C)cc1	10.1021/jm990171i
	CHEMBL123654	18229	0	None	-	0	Human	4.6	pIC50	=	4.6	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	636	12	2	7	5.8	COCCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2C)c2ccccc2C)cc1	10.1021/jm990171i
	23445241	109425	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	442	5	1	7	3.8	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Oc2ccccc2)c1Br	10.1016/S0960-894X(97)00367-3
	CHEMBL304406	109425	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	442	5	1	7	3.8	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Oc2ccccc2)c1Br	10.1016/S0960-894X(97)00367-3
	10554724	68539	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	551	10	4	6	4.9	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCC(C)CC2)nc1C(=O)O	10.1021/jm950592+
	CHEMBL177195	68539	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	551	10	4	6	4.9	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCC(C)CC2)nc1C(=O)O	10.1021/jm950592+
	12146375	103624	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	322	3	1	5	2.6	Cc1noc(NS(=O)(=O)c2ccsc2)c1Br	10.1016/S0960-894X(96)00496-9
	CHEMBL265290	103624	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	322	3	1	5	2.6	Cc1noc(NS(=O)(=O)c2ccsc2)c1Br	10.1016/S0960-894X(96)00496-9
	9975719	102800	0	None	-	0	Rat	4.6	pIC50	=	4.6	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	359	4	2	5	3.2	CC(=O)Nc1cccc2ccc(S(=O)(=O)Nc3onc(C)c3C)cc12	10.1021/jm00008a013
	CHEMBL25977	102800	0	None	-	0	Rat	4.6	pIC50	=	4.6	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	359	4	2	5	3.2	CC(=O)Nc1cccc2ccc(S(=O)(=O)Nc3onc(C)c3C)cc12	10.1021/jm00008a013
	9975719	102800	0	None	-	0	Rat	4.6	pIC50	=	4.6	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	359	4	2	5	3.2	CC(=O)Nc1cccc2ccc(S(=O)(=O)Nc3onc(C)c3C)cc12	10.1021/jm00004a012
	CHEMBL25977	102800	0	None	-	0	Rat	4.6	pIC50	=	4.6	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	359	4	2	5	3.2	CC(=O)Nc1cccc2ccc(S(=O)(=O)Nc3onc(C)c3C)cc12	10.1021/jm00004a012
	127034919	143293	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	599	10	2	7	6.6	CCCc1nc2c(C)cc(C(=O)NC(C)C)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	CHEMBL3736310	143293	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	599	10	2	7	6.6	CCCc1nc2c(C)cc(C(=O)NC(C)C)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	44384610	135249	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	743	16	2	14	4.9	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2cc(OC)c(OC)c(OC)c2)nc1OCCNS(=O)(=O)c1cccs1	10.1016/s0960-894x(02)01083-1
	CHEMBL366627	135249	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	743	16	2	14	4.9	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2cc(OC)c(OC)c(OC)c2)nc1OCCNS(=O)(=O)c1cccs1	10.1016/s0960-894x(02)01083-1
	137633653	163376	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	593	10	2	9	5.0	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(OCC4CCC4)ccc31)OCO2	10.1016/j.bmcl.2017.04.049
	CHEMBL4068786	163376	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	593	10	2	9	5.0	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(OCC4CCC4)ccc31)OCO2	10.1016/j.bmcl.2017.04.049
	9868822	15363	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	459	6	1	7	3.9	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(N(C)C)cc2)cc1	10.1021/jm9606507
	CHEMBL10948	15363	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	459	6	1	7	3.9	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(N(C)C)cc2)cc1	10.1021/jm9606507
	CHEMBL2304013	216248	0	None	-	0	Pig	7.6	pIC50	=	7.6	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)[C@H]1NC(=O)[C@H](C(C)(C)C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc2c(Br)[nH]c3ccccc23)NC1=O	10.1021/jm9600914
	443289	7498	47	None	-2	3	Rat	7.6	pIC50	=	7.6	Binding	Displacement of [125I]ET-1 from ETA receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hrDisplacement of [125I]ET-1 from ETA receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hr	ChEMBL		None	None	None		None	10.1007/s00044-013-0542-3
	997	7498	47	None	-2	3	Rat	7.6	pIC50	=	7.6	Binding	Displacement of [125I]ET-1 from ETA receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hrDisplacement of [125I]ET-1 from ETA receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hr	ChEMBL		None	None	None		None	10.1007/s00044-013-0542-3
	CHEMBL314691	7498	47	None	-2	3	Rat	7.6	pIC50	=	7.6	Binding	Displacement of [125I]ET-1 from ETA receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hrDisplacement of [125I]ET-1 from ETA receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hr	ChEMBL		None	None	None		None	10.1007/s00044-013-0542-3
	DB12054	7498	47	None	-2	3	Rat	7.6	pIC50	=	7.6	Binding	Displacement of [125I]ET-1 from ETA receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hrDisplacement of [125I]ET-1 from ETA receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hr	ChEMBL		None	None	None		None	10.1007/s00044-013-0542-3
	CHEMBL336033	218353	1	None	-	0	Rat	7.6	pIC50	=	7.6	Binding	Displacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry method	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmc.2015.01.003
	44295224	21403	0	None	-	0	Rat	7.6	pIC50	=	7.6	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	532	9	1	9	4.6	COc1cc(C/C(C(=O)c2ccc3c(c2)CCO3)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC	10.1016/s0960-894x(98)00301-1
	CHEMBL1205077	21403	0	None	-	0	Rat	7.6	pIC50	=	7.6	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	532	9	1	9	4.6	COc1cc(C/C(C(=O)c2ccc3c(c2)CCO3)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC	10.1016/s0960-894x(98)00301-1
	CHEMBL49675	21403	0	None	-	0	Rat	7.6	pIC50	=	7.6	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	532	9	1	9	4.6	COc1cc(C/C(C(=O)c2ccc3c(c2)CCO3)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC	10.1016/s0960-894x(98)00301-1
	44294929	21566	0	None	-	0	Rat	7.6	pIC50	=	7.6	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	460	8	1	7	4.7	COc1ccc(C/C(C(=O)c2ccc(OC)cc2)=C(/C(=O)O)c2ccc3nsnc3c2)cc1	10.1016/s0960-894x(98)00301-1
	CHEMBL1206731	21566	0	None	-	0	Rat	7.6	pIC50	=	7.6	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	460	8	1	7	4.7	COc1ccc(C/C(C(=O)c2ccc(OC)cc2)=C(/C(=O)O)c2ccc3nsnc3c2)cc1	10.1016/s0960-894x(98)00301-1
	CHEMBL301971	21566	0	None	-	0	Rat	7.6	pIC50	=	7.6	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	460	8	1	7	4.7	COc1ccc(C/C(C(=O)c2ccc(OC)cc2)=C(/C(=O)O)c2ccc3nsnc3c2)cc1	10.1016/s0960-894x(98)00301-1
	44320375	113922	0	None	-	0	Rat	7.6	pIC50	=	7.6	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	506	8	1	7	5.3	COc1cc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)cc(OC)c1	10.1016/s0960-894x(00)00513-8
	CHEMBL316187	113922	0	None	-	0	Rat	7.6	pIC50	=	7.6	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	506	8	1	7	5.3	COc1cc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)cc(OC)c1	10.1016/s0960-894x(00)00513-8
	10252787	106042	0	None	-	0	Rat	7.6	pIC50	=	7.6	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	442	7	1	6	4.6	COc1cccc(Cn2nc(-c3ccccc3)c(Cc3ccc4c(c3)OCO4)c2C(=O)O)c1	10.1016/s0960-894x(00)00232-8
	CHEMBL281865	106042	0	None	-	0	Rat	7.6	pIC50	=	7.6	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	442	7	1	6	4.6	COc1cccc(Cn2nc(-c3ccccc3)c(Cc3ccc4c(c3)OCO4)c2C(=O)O)c1	10.1016/s0960-894x(00)00232-8
	10839618	210353	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	517	10	1	8	4.2	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OCCCN(C)C)c2)cc1	10.1021/jm980504w
	CHEMBL66762	210353	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	517	10	1	8	4.2	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OCCCN(C)C)c2)cc1	10.1021/jm980504w
	17885919	213189	0	None	-	0	Rat	7.6	pIC50	=	7.6	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	526	9	2	8	4.8	O=C(O)COc1ccccc1Cn1nc(-c2cccs2)c(Cc2cc3c(cc2Cl)OCO3)c1C(=O)O	10.1016/s0960-894x(00)00513-8
	CHEMBL87801	213189	0	None	-	0	Rat	7.6	pIC50	=	7.6	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	526	9	2	8	4.8	O=C(O)COc1ccccc1Cn1nc(-c2cccs2)c(Cc2cc3c(cc2Cl)OCO3)c1C(=O)O	10.1016/s0960-894x(00)00513-8
	3795752	111979	1	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	320	3	1	4	3.4	Cc1noc(NS(=O)(=O)c2cc(Cl)ccc2Cl)c1C	10.1016/0960-894X(96)00441-6
	CHEMBL311455	111979	1	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	320	3	1	4	3.4	Cc1noc(NS(=O)(=O)c2cc(Cl)ccc2Cl)c1C	10.1016/0960-894X(96)00441-6
	44283453	145555	0	None	-	0	Pig	6.6	pIC50	=	6.6	Binding	Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	641	12	4	7	4.8	CCCC[C@H](NC(=O)[C@@H](Cc1cn(C(=O)OC)c2ccccc12)NC(=O)C(CC(C)(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1016/0960-894X(95)00237-N
	CHEMBL37807	145555	0	None	-	0	Pig	6.6	pIC50	=	6.6	Binding	Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	641	12	4	7	4.8	CCCC[C@H](NC(=O)[C@@H](Cc1cn(C(=O)OC)c2ccccc12)NC(=O)C(CC(C)(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1016/0960-894X(95)00237-N
	10721106	68180	0	None	-	0	Rat	6.6	pIC50	=	6.6	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	536	9	4	5	4.3	Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O	10.1021/jm950592+
	CHEMBL177023	68180	0	None	-	0	Rat	6.6	pIC50	=	6.6	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	536	9	4	5	4.3	Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O	10.1021/jm950592+
	10247887	105139	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells	ChEMBL	359	5	1	5	3.3	Cc1noc(NS(=O)(=O)c2cccc3c(CN(C)C)cccc23)c1C	10.1021/jm00029a001
	CHEMBL27525	105139	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells	ChEMBL	359	5	1	5	3.3	Cc1noc(NS(=O)(=O)c2cccc3c(CN(C)C)cccc23)c1C	10.1021/jm00029a001
	10247887	105139	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	359	5	1	5	3.3	Cc1noc(NS(=O)(=O)c2cccc3c(CN(C)C)cccc23)c1C	10.1021/jm00008a013
	CHEMBL27525	105139	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	359	5	1	5	3.3	Cc1noc(NS(=O)(=O)c2cccc3c(CN(C)C)cccc23)c1C	10.1021/jm00008a013
	CHEMBL86814	222671	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Displacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cellsDisplacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)81215-4
	CHEMBL408141	219482	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	In vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricleIn vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricle	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)80156-6
	CHEMBL86814	222671	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Inhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cellsInhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00095a029
	CHEMBL344473	218485	0	None	-	0	Pig	5.6	pIC50	=	5.6	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)[C@@H]1NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](C)NC1=O	10.1021/jm00021a021
	10444974	106375	24	None	-	0	Human	4.6	pIC50	=	4.6	Binding	Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells	ChEMBL	253	3	2	5	1.4	Cc1cc(NS(=O)(=O)c2ccc(N)cc2)on1	10.1021/jm00029a001
	CHEMBL283941	106375	24	None	-	0	Human	4.6	pIC50	=	4.6	Binding	Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells	ChEMBL	253	3	2	5	1.4	Cc1cc(NS(=O)(=O)c2ccc(N)cc2)on1	10.1021/jm00029a001
	10444974	106375	24	None	-	0	Rat	4.6	pIC50	=	4.6	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	253	3	2	5	1.4	Cc1cc(NS(=O)(=O)c2ccc(N)cc2)on1	10.1021/jm00008a013
	CHEMBL283941	106375	24	None	-	0	Rat	4.6	pIC50	=	4.6	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	253	3	2	5	1.4	Cc1cc(NS(=O)(=O)c2ccc(N)cc2)on1	10.1021/jm00008a013
	127035084	143161	0	None	-	0	Human	4.6	pIC50	=	4.6	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	707	13	2	9	7.4	CCCc1nc2c(C)cc(C(=O)NCc3ccc(OC)c(OC)c3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	CHEMBL3735151	143161	0	None	-	0	Human	4.6	pIC50	=	4.6	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	707	13	2	9	7.4	CCCc1nc2c(C)cc(C(=O)NCc3ccc(OC)c(OC)c3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	44298395	107462	0	None	-	0	Rat	4.6	pIC50	=	4.6	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	308	3	1	4	3.4	Cc1onc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1C	10.1016/s0960-894x(00)00366-8
	CHEMBL292355	107462	0	None	-	0	Rat	4.6	pIC50	=	4.6	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	308	3	1	4	3.4	Cc1onc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1C	10.1016/s0960-894x(00)00366-8
	44298342	108534	0	None	-	0	Rat	4.6	pIC50	=	4.6	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	283	3	2	5	2.1	Cc1snc(NS(=O)(=O)c2ccc(N)cc2)c1C	10.1016/s0960-894x(00)00366-8
	CHEMBL299831	108534	0	None	-	0	Rat	4.6	pIC50	=	4.6	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	283	3	2	5	2.1	Cc1snc(NS(=O)(=O)c2ccc(N)cc2)c1C	10.1016/s0960-894x(00)00366-8
	18184179	135800	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	654	13	2	12	4.3	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2ccncc2)nc1OCCNS(=O)(=O)c1cccs1	10.1016/s0960-894x(02)01083-1
	CHEMBL367017	135800	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	654	13	2	12	4.3	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2ccncc2)nc1OCCNS(=O)(=O)c1cccs1	10.1016/s0960-894x(02)01083-1
	52950137	25206	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer	ChEMBL	559	10	3	8	3.8	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC(=O)O)ccc31)OCO2	10.1016/j.bmcl.2010.08.074
	CHEMBL1271863	25206	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer	ChEMBL	559	10	3	8	3.8	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC(=O)O)ccc31)OCO2	10.1016/j.bmcl.2010.08.074
	10760657	66797	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	355	7	1	6	4.0	N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1ccoc1	10.1021/jm990378b
	CHEMBL173565	66797	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	355	7	1	6	4.0	N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1ccoc1	10.1021/jm990378b
	10717279	103822	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	425	9	1	5	4.8	CCCCCCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL266996	103822	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	425	9	1	5	4.8	CCCCCCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	18948954	174685	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	360	4	2	5	3.5	Cc1noc(NS(=O)(=O)c2cccc3c(C(C)(C)O)cccc23)c1C	10.1021/jm00008a013
	CHEMBL431300	174685	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	360	4	2	5	3.5	Cc1noc(NS(=O)(=O)c2cccc3c(C(C)(C)O)cccc23)c1C	10.1021/jm00008a013
	11783885	107664	0	None	-	0	Rat	7.5	pIC50	=	7.5	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	382	7	1	5	4.6	CCCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21	10.1021/jm031041j
	CHEMBL293702	107664	0	None	-	0	Rat	7.5	pIC50	=	7.5	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	382	7	1	5	4.6	CCCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21	10.1021/jm031041j
	18617340	112180	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	422	4	1	4	3.9	CCc1ccc(Br)c(S(=O)(=O)Nc2onc(C)c2Br)c1	10.1016/0960-894X(96)00441-6
	CHEMBL311742	112180	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	422	4	1	4	3.9	CCc1ccc(Br)c(S(=O)(=O)Nc2onc(C)c2Br)c1	10.1016/0960-894X(96)00441-6
	11783885	107664	0	None	-	0	Rat	7.5	pIC50	=	7.5	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	382	7	1	5	4.6	CCCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21	10.1021/jm010382z
	CHEMBL293702	107664	0	None	-	0	Rat	7.5	pIC50	=	7.5	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	382	7	1	5	4.6	CCCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21	10.1021/jm010382z
	155511294	176348	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	469	6	1	8	2.5	Cc1ccc(=O)n([C@@H](C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)n1	10.1016/j.bmcl.2016.06.014
	CHEMBL4435789	176348	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	469	6	1	8	2.5	Cc1ccc(=O)n([C@@H](C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)n1	10.1016/j.bmcl.2016.06.014
	44293805	107891	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	545	10	2	10	3.5	CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCc1nn[nH]n1)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	CHEMBL295140	107891	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	545	10	2	10	3.5	CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCc1nn[nH]n1)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	10693679	214152	0	None	-	0	Rat	7.5	pIC50	=	7.5	Binding	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	ChEMBL	425	10	2	5	4.7	Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1C(N)=O	10.1021/jm9707131
	CHEMBL93749	214152	0	None	-	0	Rat	7.5	pIC50	=	7.5	Binding	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	ChEMBL	425	10	2	5	4.7	Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1C(N)=O	10.1021/jm9707131
	9848132	214356	0	None	1	2	Rat	7.5	pIC50	=	7.5	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	483	6	1	8	2.8	Cc1cc(C)c(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)n1	10.1016/S0960-894X(96)00617-8
	CHEMBL94918	214356	0	None	1	2	Rat	7.5	pIC50	=	7.5	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	483	6	1	8	2.8	Cc1cc(C)c(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)n1	10.1016/S0960-894X(96)00617-8
	44387111	172961	0	None	-	0	Rat	7.5	pIC50	=	7.5	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	548	10	5	5	4.2	Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CC3CCC2C3)nc1C(=O)O	10.1021/jm950592+
	CHEMBL426413	172961	0	None	-	0	Rat	7.5	pIC50	=	7.5	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	548	10	5	5	4.2	Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CC3CCC2C3)nc1C(=O)O	10.1021/jm950592+
	10506505	135447	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor	ChEMBL	535	11	4	5	4.8	Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@@H](CC(=O)NC2CCCCC2)CC(C)C)nc1C(=O)O	10.1021/jm9505932
	CHEMBL366805	135447	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor	ChEMBL	535	11	4	5	4.8	Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@@H](CC(=O)NC2CCCCC2)CC(C)C)nc1C(=O)O	10.1021/jm9505932
	CHEMBL137716	215527	0	None	-	0	Pig	7.5	pIC50	=	7.5	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		COC(=O)n1cc(C[C@@H]2NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](C(C)C)NC(=O)[C@H]3CCCN3C(=O)[C@H](CC(=O)O)NC2=O)c2ccccc21	10.1021/jm00021a021
	137655525	165770	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	525	7	3	9	3.5	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(O)ccc31)OCO2	10.1016/j.bmcl.2017.04.049
	CHEMBL4096346	165770	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	525	7	3	9	3.5	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(O)ccc31)OCO2	10.1016/j.bmcl.2017.04.049
	10383850	106545	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	359	5	1	5	3.6	CCc1c(C)noc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12	10.1021/jm00008a013
	CHEMBL285122	106545	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	359	5	1	5	3.6	CCc1c(C)noc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12	10.1021/jm00008a013
	10882352	209762	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	340	4	1	5	3.4	CCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21	10.1021/jm010382z
	CHEMBL63099	209762	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	340	4	1	5	3.4	CCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21	10.1021/jm010382z
	44279383	106770	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor	ChEMBL	398	3	2	3	4.2	O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(-c3ccccc3)cc21	10.1016/0960-894X(95)00230-Q
	CHEMBL286687	106770	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor	ChEMBL	398	3	2	3	4.2	O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(-c3ccccc3)cc21	10.1016/0960-894X(95)00230-Q
	23445221	209874	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	470	5	1	7	4.4	Cc1ccc(OC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1	10.1016/S0960-894X(97)00367-3
	CHEMBL63937	209874	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	470	5	1	7	4.4	Cc1ccc(OC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1	10.1016/S0960-894X(97)00367-3
	44327237	214708	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	511	8	1	8	3.5	CCCc1cc(C)c(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)n1	10.1016/S0960-894X(96)00617-8
	CHEMBL96847	214708	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	511	8	1	8	3.5	CCCc1cc(C)c(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)n1	10.1016/S0960-894X(96)00617-8
	15453172	211764	4	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	392	4	1	4	4.2	Cc1noc(NS(=O)(=O)c2ccc(-c3ccccc3)cc2)c1Br	10.1016/0960-894X(96)00441-6
	CHEMBL76623	211764	4	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	392	4	1	4	4.2	Cc1noc(NS(=O)(=O)c2ccc(-c3ccccc3)cc2)c1Br	10.1016/0960-894X(96)00441-6
	44213923	115058	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	563	8	1	8	4.1	COc1ccc(C2=NN(C(C(=O)NS(=O)(=O)c3ccc(C(C)C)cc3)c3ccc4c(c3)OCO4)C(=O)CC2)cc1	10.1016/S0960-894X(96)00617-8
	CHEMBL319743	115058	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	563	8	1	8	4.1	COc1ccc(C2=NN(C(C(=O)NS(=O)(=O)c3ccc(C(C)C)cc3)c3ccc4c(c3)OCO4)C(=O)CC2)cc1	10.1016/S0960-894X(96)00617-8
	10530457	68886	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	538	9	5	6	4.0	Cc1oc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)NO	10.1021/jm950592+
	CHEMBL177602	68886	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	538	9	5	6	4.0	Cc1oc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)NO	10.1021/jm950592+
	10168939	138146	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	695	11	2	12	5.9	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCC#CCOC(=O)Nc1ccccn1	10.1016/s0960-894x(02)01084-3
	CHEMBL368860	138146	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	695	11	2	12	5.9	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCC#CCOC(=O)Nc1ccccn1	10.1016/s0960-894x(02)01084-3
	CHEMBL170600	215624	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1cn(C)c2ccccc12)C(=O)N[C@H](CC(=O)O)C(=O)O	10.1016/0960-894X(95)00144-I
	CHEMBL1201469	21279	0	None	-1	4	Human	5.5	pIC50	=	5.5	Binding	DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)	ChEMBL		None	None	None		None	nan
	23445227	127603	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor	ChEMBL	472	6	1	8	3.9	Cc1noc(NS(=O)(=O)c2ccsc2COc2ccc3c(c2)OCO3)c1Br	10.1016/S0960-894X(97)00132-7
	CHEMBL355800	127603	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor	ChEMBL	472	6	1	8	3.9	Cc1noc(NS(=O)(=O)c2ccsc2COc2ccc3c(c2)OCO3)c1Br	10.1016/S0960-894X(97)00132-7
	10789525	68544	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	446	8	1	6	4.4	COc1ccc(C(=O)/C(Cc2cccc(OC)c2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1	10.1021/jm031041j
	CHEMBL177221	68544	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	446	8	1	6	4.4	COc1ccc(C(=O)/C(Cc2cccc(OC)c2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1	10.1021/jm031041j
	10789524	11964	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	446	6	1	7	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OC)c2)cc1	10.1021/jm9606507
	CHEMBL10607	11964	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	446	6	1	7	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OC)c2)cc1	10.1021/jm9606507
	10896413	107383	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	504	9	1	7	5.4	COc1ccc(CCOC2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1	10.1021/jm010382z
	CHEMBL291841	107383	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	504	9	1	7	5.4	COc1ccc(CCOC2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1	10.1021/jm010382z
	11762291	107412	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	460	6	1	6	5.2	COc1ccccc1C1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	CHEMBL292041	107412	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	460	6	1	6	5.2	COc1ccccc1C1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	11059249	109395	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	440	10	1	6	5.3	CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OCCCC)cc21	10.1021/jm010382z
	CHEMBL304202	109395	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	440	10	1	6	5.3	CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OCCCC)cc21	10.1021/jm010382z
	11144468	210240	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	430	5	1	5	5.2	CC(C)Oc1ccc2c(c1)C(c1ccccc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	CHEMBL65925	210240	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	430	5	1	5	5.2	CC(C)Oc1ccc2c(c1)C(c1ccccc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	10184817	16346	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	488	14	1	5	5.1	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)CCC	10.1021/jm980217s
	CHEMBL112417	16346	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	488	14	1	5	5.1	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)CCC	10.1021/jm980217s
	44314904	109924	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Binding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranesBinding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranes	ChEMBL	585	12	5	5	3.6	CSCCC(NC(=O)[C@@H](Cc1c(C)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O	10.1021/jm9600914
	CHEMBL307936	109924	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Binding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranesBinding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranes	ChEMBL	585	12	5	5	3.6	CSCCC(NC(=O)[C@@H](Cc1c(C)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O	10.1021/jm9600914
	155564169	182112	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	545	11	1	12	2.0	COc1ccc(Cl)c(Oc2c(NS(C)(=O)=O)ncnc2OCCOc2ncc(S(C)(=O)=O)cn2)c1	10.1016/j.bmcl.2016.06.014
	CHEMBL4574034	182112	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	545	11	1	12	2.0	COc1ccc(Cl)c(Oc2c(NS(C)(=O)=O)ncnc2OCCOc2ncc(S(C)(=O)=O)cn2)c1	10.1016/j.bmcl.2016.06.014
	71455062	88454	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	669	14	1	12	5.0	COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(C(F)(F)F)cn1	10.1021/jm3009103
	CHEMBL2163705	88454	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	669	14	1	12	5.0	COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(C(F)(F)F)cn1	10.1021/jm3009103
	44295005	16992	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	538	10	1	9	4.8	COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)c(F)c1	10.1016/s0960-894x(98)00301-1
	CHEMBL1160205	16992	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	538	10	1	9	4.8	COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)c(F)c1	10.1016/s0960-894x(98)00301-1
	10226215	108209	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	455	5	2	8	3.8	Cc1cc2c(cc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2	10.1021/jm9608366
	CHEMBL297473	108209	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	455	5	2	8	3.8	Cc1cc2c(cc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2	10.1021/jm9608366
	44291255	180238	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	455	5	2	8	3.8	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc3c(c2C)OCO3)c1Cl	10.1021/jm9700068
	CHEMBL45296	180238	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	455	5	2	8	3.8	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc3c(c2C)OCO3)c1Cl	10.1021/jm9700068
	CHEMBL414165	219894	0	None	-	0	Pig	8.5	pIC50	=	8.5	Binding	Inhibitory effect against porcine ET-A receptorInhibitory effect against porcine ET-A receptor	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](c2cccs2)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	44311345	210996	0	None	-	1	Human	8.5	pIC50	=	8.5	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	663	13	3	12	5.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CCNCC2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	CHEMBL70895	210996	0	None	-	1	Human	8.5	pIC50	=	8.5	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	663	13	3	12	5.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CCNCC2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	CHEMBL414165	219894	0	None	-	0	Pig	8.5	pIC50	=	8.5	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](c2cccs2)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	8260	7319	54	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Antagonist activity at ETA receptor (unknown origin) in presence of ET1Antagonist activity at ETA receptor (unknown origin) in presence of ET1	ChEMBL	479	8	1	9	3.9	COc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cn1)C)c1ccncc1	10.1016/j.bmcl.2016.06.014
	9912992	7319	54	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Antagonist activity at ETA receptor (unknown origin) in presence of ET1Antagonist activity at ETA receptor (unknown origin) in presence of ET1	ChEMBL	479	8	1	9	3.9	COc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cn1)C)c1ccncc1	10.1016/j.bmcl.2016.06.014
	CHEMBL3989834	7319	54	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Antagonist activity at ETA receptor (unknown origin) in presence of ET1Antagonist activity at ETA receptor (unknown origin) in presence of ET1	ChEMBL	479	8	1	9	3.9	COc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cn1)C)c1ccncc1	10.1016/j.bmcl.2016.06.014
	44458597	105567	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	535	7	3	8	2.3	Cn1cc(C(C(=O)NS(=O)(=O)c2ccccc2C(=O)O)c2ccc3c(c2)OCO3)c2ccc(C(N)=O)cc21	10.1016/s0960-894x(01)00660-6
	CHEMBL278349	105567	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	535	7	3	8	2.3	Cn1cc(C(C(=O)NS(=O)(=O)c2ccccc2C(=O)O)c2ccc3c(c2)OCO3)c2ccc(C(N)=O)cc21	10.1016/s0960-894x(01)00660-6
	11017071	16727	0	None	-	0	Pig	8.5	pIC50	=	8.5	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	547	9	1	9	4.3	Cc1ccc(-c2c(NS(=O)(=O)c3cccs3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm0102304
	CHEMBL114683	16727	0	None	-	0	Pig	8.5	pIC50	=	8.5	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	547	9	1	9	4.3	Cc1ccc(-c2c(NS(=O)(=O)c3cccs3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm0102304
	10994373	169233	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	474	5	1	7	5.0	CC(C)Oc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	CHEMBL416675	169233	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	474	5	1	7	5.0	CC(C)Oc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	10122033	88452	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	631	15	1	13	4.0	COc1cnc(OCCOc2nc(-c3ncccn3)nc(NS(=O)(=O)CCc3ccccc3)c2Oc2ccccc2OC)nc1	10.1021/jm3009103
	CHEMBL2163703	88452	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	631	15	1	13	4.0	COc1cnc(OCCOc2nc(-c3ncccn3)nc(NS(=O)(=O)CCc3ccccc3)c2Oc2ccccc2OC)nc1	10.1021/jm3009103
	44334145	11424	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	460	6	1	6	4.6	COc1ccc([C@@H]2c3nc(N(C)C(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1	10.1016/s0960-894x(02)00663-7
	CHEMBL103090	11424	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	460	6	1	6	4.6	COc1ccc([C@@H]2c3nc(N(C)C(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1	10.1016/s0960-894x(02)00663-7
	44352026	124263	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	548	11	1	5	5.7	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(C(F)(F)F)cc1	10.1021/jm010237l
	CHEMBL339969	124263	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	548	11	1	5	5.7	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(C(F)(F)F)cc1	10.1021/jm010237l
	44339840	16060	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	486	13	1	5	5.1	C/C=C(\C)CC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC	10.1021/jm980217s
	CHEMBL110904	16060	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	486	13	1	5	5.1	C/C=C(\C)CC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC	10.1021/jm980217s
	10577829	16439	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	518	13	1	7	3.9	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1OCCCO1	10.1021/jm980217s
	CHEMBL112877	16439	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	518	13	1	7	3.9	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1OCCCO1	10.1021/jm980217s
	73669821	124405	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	Displacement of PD156707 from rat ETA receptor after 1 hr by Lowry methodDisplacement of PD156707 from rat ETA receptor after 1 hr by Lowry method	ChEMBL	448	10	1	6	5.2	CC(=O)c1ccc(OCc2ccc3c(c2)OCO3)cc1OC(CCC(=O)O)c1ccccc1	10.1016/j.bmc.2015.01.003
	CHEMBL3400988	124405	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	Displacement of PD156707 from rat ETA receptor after 1 hr by Lowry methodDisplacement of PD156707 from rat ETA receptor after 1 hr by Lowry method	ChEMBL	448	10	1	6	5.2	CC(=O)c1ccc(OCc2ccc3c(c2)OCO3)cc1OC(CCC(=O)O)c1ccccc1	10.1016/j.bmc.2015.01.003
	21041307	181748	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	482	10	2	9	2.6	CNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Cl)cc1	10.1016/j.bmcl.2016.06.014
	CHEMBL4566095	181748	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	482	10	2	9	2.6	CNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Cl)cc1	10.1016/j.bmcl.2016.06.014
	10274552	80288	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	434	6	1	8	3.6	Cc1cc2c(cc1CC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1C)OCO2	10.1021/jm9700068
	CHEMBL20168	80288	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	434	6	1	8	3.6	Cc1cc2c(cc1CC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1C)OCO2	10.1021/jm9700068
	10274552	80288	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor	ChEMBL	434	6	1	8	3.6	Cc1cc2c(cc1CC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1C)OCO2	10.1021/jm000349x
	CHEMBL20168	80288	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor	ChEMBL	434	6	1	8	3.6	Cc1cc2c(cc1CC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1C)OCO2	10.1021/jm000349x
	16004692	9232	91	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Antagonist activity at human ETA receptor expressed in CHO cells in presence of ET1Antagonist activity at human ETA receptor expressed in CHO cells in presence of ET1	ChEMBL	586	11	2	8	3.6	CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br	10.1016/j.bmcl.2016.06.014
	4809	9232	91	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Antagonist activity at human ETA receptor expressed in CHO cells in presence of ET1Antagonist activity at human ETA receptor expressed in CHO cells in presence of ET1	ChEMBL	586	11	2	8	3.6	CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br	10.1016/j.bmcl.2016.06.014
	7352	9232	91	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Antagonist activity at human ETA receptor expressed in CHO cells in presence of ET1Antagonist activity at human ETA receptor expressed in CHO cells in presence of ET1	ChEMBL	586	11	2	8	3.6	CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br	10.1016/j.bmcl.2016.06.014
	CHEMBL2103873	9232	91	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Antagonist activity at human ETA receptor expressed in CHO cells in presence of ET1Antagonist activity at human ETA receptor expressed in CHO cells in presence of ET1	ChEMBL	586	11	2	8	3.6	CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br	10.1016/j.bmcl.2016.06.014
	DB08932	9232	91	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Antagonist activity at human ETA receptor expressed in CHO cells in presence of ET1Antagonist activity at human ETA receptor expressed in CHO cells in presence of ET1	ChEMBL	586	11	2	8	3.6	CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br	10.1016/j.bmcl.2016.06.014
	10070	7237	47	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	544	8	2	8	2.5	Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N	10.1016/j.bmcl.2016.06.014
	25099191	7237	47	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	544	8	2	8	2.5	Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N	10.1016/j.bmcl.2016.06.014
	CHEMBL2165326	7237	47	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	544	8	2	8	2.5	Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N	10.1016/j.bmcl.2016.06.014
	DB15059	7237	47	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	544	8	2	8	2.5	Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N	10.1016/j.bmcl.2016.06.014
	10070	7237	47	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	544	8	2	8	2.5	Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N	10.1021/jm3009103
	25099191	7237	47	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	544	8	2	8	2.5	Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N	10.1021/jm3009103
	CHEMBL2165326	7237	47	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	544	8	2	8	2.5	Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N	10.1021/jm3009103
	DB15059	7237	47	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	544	8	2	8	2.5	Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N	10.1021/jm3009103
	71455065	88474	1	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	679	14	2	11	4.8	COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(-c2ccncc2)nc1OCCOc1ncc(Br)cn1	10.1021/jm3009103
	CHEMBL2163724	88474	1	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	679	14	2	11	4.8	COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(-c2ccncc2)nc1OCCOc1ncc(Br)cn1	10.1021/jm3009103
	17869373	21406	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	460	8	1	7	4.7	COc1ccc(C(=O)/C(Cc2cccc(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1	10.1016/s0960-894x(98)00301-1
	CHEMBL1205094	21406	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	460	8	1	7	4.7	COc1ccc(C(=O)/C(Cc2cccc(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1	10.1016/s0960-894x(98)00301-1
	CHEMBL51890	21406	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	460	8	1	7	4.7	COc1ccc(C(=O)/C(Cc2cccc(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1	10.1016/s0960-894x(98)00301-1
	44295106	21514	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	472	7	1	7	4.6	COc1ccc(C(=O)/C(Cc2ccc3c(c2)CCO3)=C(\C(=O)O)c2ccc3nsnc3c2)cc1	10.1016/s0960-894x(98)00301-1
	CHEMBL1206319	21514	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	472	7	1	7	4.6	COc1ccc(C(=O)/C(Cc2ccc3c(c2)CCO3)=C(\C(=O)O)c2ccc3nsnc3c2)cc1	10.1016/s0960-894x(98)00301-1
	CHEMBL262000	21514	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	472	7	1	7	4.6	COc1ccc(C(=O)/C(Cc2ccc3c(c2)CCO3)=C(\C(=O)O)c2ccc3nsnc3c2)cc1	10.1016/s0960-894x(98)00301-1
	17869279	21651	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	460	8	1	7	4.7	COc1ccc(C(=O)/C(Cc2ccccc2OC)=C(\C(=O)O)c2ccc3nsnc3c2)cc1	10.1016/s0960-894x(98)00301-1
	CHEMBL1207701	21651	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	460	8	1	7	4.7	COc1ccc(C(=O)/C(Cc2ccccc2OC)=C(\C(=O)O)c2ccc3nsnc3c2)cc1	10.1016/s0960-894x(98)00301-1
	CHEMBL431160	21651	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	460	8	1	7	4.7	COc1ccc(C(=O)/C(Cc2ccccc2OC)=C(\C(=O)O)c2ccc3nsnc3c2)cc1	10.1016/s0960-894x(98)00301-1
	44320171	113734	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	504	6	1	5	6.4	O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1CC12CC3CC(CC(C3)C1)C2	10.1016/s0960-894x(00)00513-8
	CHEMBL314974	113734	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	504	6	1	5	6.4	O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1CC12CC3CC(CC(C3)C1)C2	10.1016/s0960-894x(00)00513-8
	11135910	16983	0	None	-	0	Pig	8.5	pIC50	=	8.5	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	624	10	1	10	5.4	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(-c4ccccn4)s3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm0102304
	CHEMBL116002	16983	0	None	-	0	Pig	8.5	pIC50	=	8.5	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	624	10	1	10	5.4	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(-c4ccccn4)s3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm0102304
	10205245	78984	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	466	5	2	9	3.4	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2C#N)OCO3)c1Cl	10.1021/jm9608366
	CHEMBL19808	78984	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	466	5	2	9	3.4	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2C#N)OCO3)c1Cl	10.1021/jm9608366
	44291575	186214	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	466	5	2	9	3.4	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc3c(c2C#N)OCO3)c1Cl	10.1021/jm9700068
	CHEMBL47404	186214	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	466	5	2	9	3.4	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc3c(c2C#N)OCO3)c1Cl	10.1021/jm9700068
	10205245	78984	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor	ChEMBL	466	5	2	9	3.4	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2C#N)OCO3)c1Cl	10.1021/jm000349x
	CHEMBL19808	78984	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor	ChEMBL	466	5	2	9	3.4	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2C#N)OCO3)c1Cl	10.1021/jm000349x
	CHEMBL133257	215494	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Inhibitory effect against Human ET-A receptorInhibitory effect against Human ET-A receptor	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C2CCCC2)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	11634755	69081	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	480	7	1	7	4.9	COc1cc(/C(C(=O)O)=C(\CC2CCCCC2)C(=O)c2ccc3c(c2)OCCO3)cc2c1OCO2	10.1021/jm031041j
	CHEMBL177886	69081	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	480	7	1	7	4.9	COc1cc(/C(C(=O)O)=C(\CC2CCCCC2)C(=O)c2ccc3c(c2)OCCO3)cc2c1OCO2	10.1021/jm031041j
	44304492	103335	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL	949	23	9	8	4.3	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	CHEMBL262993	103335	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL	949	23	9	8	4.3	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	18738878	201611	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	547	8	2	7	4.2	CCn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c2ccc(C(N)=O)cc21	10.1016/s0960-894x(01)00660-6
	CHEMBL539420	201611	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	547	8	2	7	4.2	CCn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c2ccc(C(N)=O)cc21	10.1016/s0960-894x(01)00660-6
	9958846	176956	0	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	Displacement of 125I-ET1 from ETA receptor in rat A7R5 cellsDisplacement of 125I-ET1 from ETA receptor in rat A7R5 cells	ChEMBL	537	13	1	10	3.7	COCCOc1nc(-c2ncccn2)nc(NS(=O)(=O)CCc2ccccc2)c1Oc1ccccc1OC	10.1016/j.bmcl.2016.06.014
	CHEMBL4444693	176956	0	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	Displacement of 125I-ET1 from ETA receptor in rat A7R5 cellsDisplacement of 125I-ET1 from ETA receptor in rat A7R5 cells	ChEMBL	537	13	1	10	3.7	COCCOc1nc(-c2ncccn2)nc(NS(=O)(=O)CCc2ccccc2)c1Oc1ccccc1OC	10.1016/j.bmcl.2016.06.014
	71455140	88783	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	598	12	2	8	4.7	CC(C)c1ccc(-c2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm3009103
	CHEMBL2165336	88783	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	598	12	2	8	4.7	CC(C)c1ccc(-c2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm3009103
	11123269	213079	0	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	452	6	1	5	5.8	O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1CC1CCCCC1	10.1016/s0960-894x(00)00513-8
	CHEMBL87070	213079	0	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	452	6	1	5	5.8	O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1CC1CCCCC1	10.1016/s0960-894x(00)00513-8
	10697520	18889	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	530	10	2	6	4.9	CCCC(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1	10.1021/jm990171i
	CHEMBL1184086	18889	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	530	10	2	6	4.9	CCCC(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1	10.1021/jm990171i
	CHEMBL331936	18889	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	530	10	2	6	4.9	CCCC(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1	10.1021/jm990171i
	10530156	16329	0	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	526	14	1	6	5.0	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc(OC)cc2OC)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	CHEMBL112347	16329	0	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	526	14	1	6	5.0	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc(OC)cc2OC)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	44295206	21565	0	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	580	12	1	11	4.7	COc1cc(C/C(C(=O)c2cc(OC)c(OC)c(OC)c2)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC	10.1016/s0960-894x(98)00301-1
	CHEMBL1206728	21565	0	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	580	12	1	11	4.7	COc1cc(C/C(C(=O)c2cc(OC)c(OC)c(OC)c2)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC	10.1016/s0960-894x(98)00301-1
	CHEMBL301577	21565	0	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	580	12	1	11	4.7	COc1cc(C/C(C(=O)c2cc(OC)c(OC)c(OC)c2)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC	10.1016/s0960-894x(98)00301-1
	11059349	210288	0	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	446	6	1	6	4.8	CCOc1ccc2c(c1)C(c1ccc(OC)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm031041j
	CHEMBL66264	210288	0	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	446	6	1	6	4.8	CCOc1ccc2c(c1)C(c1ccc(OC)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm031041j
	15453178	111530	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	348	4	1	4	4.1	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2)c1Cl	10.1016/0960-894X(96)00441-6
	CHEMBL310739	111530	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	348	4	1	4	4.1	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2)c1Cl	10.1016/0960-894X(96)00441-6
	11059349	210288	0	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	446	6	1	6	4.8	CCOc1ccc2c(c1)C(c1ccc(OC)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	CHEMBL66264	210288	0	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	446	6	1	6	4.8	CCOc1ccc2c(c1)C(c1ccc(OC)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	44314610	109633	0	None	-	0	Pig	8.4	pIC50	=	8.4	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	671	12	6	5	3.9	CC(C)CC(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)N[C@H](Cc1c(Br)[nH]c2ccccc12)C(=O)NC(Cc1c[nH]cn1)C(=O)O	10.1021/jm9600914
	CHEMBL305650	109633	0	None	-	0	Pig	8.4	pIC50	=	8.4	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	671	12	6	5	3.9	CC(C)CC(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)N[C@H](Cc1c(Br)[nH]c2ccccc12)C(=O)NC(Cc1c[nH]cn1)C(=O)O	10.1021/jm9600914
	44314619	211465	0	None	-	0	Pig	8.4	pIC50	=	8.4	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	631	12	5	4	4.5	CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O	10.1021/jm9600914
	CHEMBL73925	211465	0	None	-	0	Pig	8.4	pIC50	=	8.4	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	631	12	5	4	4.5	CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O	10.1021/jm9600914
	71451529	88468	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	632	14	2	12	3.4	CCCNS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC	10.1021/jm3009103
	CHEMBL2163719	88468	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	632	14	2	12	3.4	CCCNS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC	10.1021/jm3009103
	10504920	169889	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	480	6	2	9	3.5	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2CC#N)OCO3)c1Cl	10.1021/jm9608366
	CHEMBL417719	169889	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	480	6	2	9	3.5	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2CC#N)OCO3)c1Cl	10.1021/jm9608366
	CHEMBL284250	217639	0	None	-	0	Pig	8.4	pIC50	=	8.4	Binding	Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)[C@@H](NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O	10.1016/0960-894X(95)00237-N
	10579100	173120	0	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	578	10	2	6	5.4	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(Cc2ccccc2)c2ccccc2)cc1	10.1021/jm031041j
	CHEMBL122614	173120	0	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	578	10	2	6	5.4	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(Cc2ccccc2)c2ccccc2)cc1	10.1021/jm031041j
	CHEMBL427303	173120	0	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	578	10	2	6	5.4	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(Cc2ccccc2)c2ccccc2)cc1	10.1021/jm031041j
	10579100	173120	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	578	10	2	6	5.4	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(Cc2ccccc2)c2ccccc2)cc1	10.1021/jm990171i
	CHEMBL122614	173120	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	578	10	2	6	5.4	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(Cc2ccccc2)c2ccccc2)cc1	10.1021/jm990171i
	CHEMBL427303	173120	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	578	10	2	6	5.4	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(Cc2ccccc2)c2ccccc2)cc1	10.1021/jm990171i
	10695363	12026	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	462	6	1	7	4.5	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(SC)cc2)cc1	10.1021/jm9606507
	CHEMBL10636	12026	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	462	6	1	7	4.5	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(SC)cc2)cc1	10.1021/jm9606507
	73669820	124406	0	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	Displacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry method	ChEMBL	462	10	1	7	5.5	CC(=O)c1ccc(OCc2ccc3nsnc3c2)cc1OC(CCC(=O)O)c1ccccc1	10.1016/j.bmc.2015.01.003
	CHEMBL3400989	124406	0	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	Displacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry method	ChEMBL	462	10	1	7	5.5	CC(=O)c1ccc(OCc2ccc3nsnc3c2)cc1OC(CCC(=O)O)c1ccccc1	10.1016/j.bmc.2015.01.003
	44380952	34261	0	None	-	0	Pig	8.4	pIC50	=	8.4	Binding	In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.	ChEMBL	679	10	1	9	7.3	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)nc(-c3cccs3)nc2OCCOc2ncc(Br)cn2)cc1	10.1016/s0960-894x(01)00682-5
	CHEMBL136871	34261	0	None	-	0	Pig	8.4	pIC50	=	8.4	Binding	In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.	ChEMBL	679	10	1	9	7.3	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)nc(-c3cccs3)nc2OCCOc2ncc(Br)cn2)cc1	10.1016/s0960-894x(01)00682-5
	44291897	108070	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	482	7	2	9	3.6	COc1cc(C#N)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(OC)c1	10.1021/jm9608366
	CHEMBL296456	108070	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	482	7	2	9	3.6	COc1cc(C#N)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(OC)c1	10.1021/jm9608366
	9956918	177662	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	482	7	2	9	3.6	COc1cc(C#N)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)cc1OC	10.1021/jm9700068
	CHEMBL44544	177662	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	482	7	2	9	3.6	COc1cc(C#N)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)cc1OC	10.1021/jm9700068
	44279172	115429	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors	ChEMBL	532	10	2	6	4.6	CCCCCNC(=O)c1cccc(S(=O)(=O)Nc2ncc(Br)nc2OC)c1-c1ccccc1	10.1016/S0960-894X(97)00228-X
	CHEMBL32075	115429	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors	ChEMBL	532	10	2	6	4.6	CCCCCNC(=O)c1cccc(S(=O)(=O)Nc2ncc(Br)nc2OC)c1-c1ccccc1	10.1016/S0960-894X(97)00228-X
	10022121	108606	0	None	-	0	Rat	7.5	pIC50	=	7.5	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	371	4	1	5	3.8	Cc1noc(NS(=O)(=O)c2cccc3c(N4CCCC4)cccc23)c1C	10.1021/jm00008a013
	CHEMBL30032	108606	0	None	-	0	Rat	7.5	pIC50	=	7.5	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	371	4	1	5	3.8	Cc1noc(NS(=O)(=O)c2cccc3c(N4CCCC4)cccc23)c1C	10.1021/jm00008a013
	9957225	12037	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	490	8	0	8	4.7	COc1ccc(C2OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1	10.1021/jm9606507
	CHEMBL10644	12037	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	490	8	0	8	4.7	COc1ccc(C2OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1	10.1021/jm9606507
	18738880	174953	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	561	8	2	7	4.5	CCn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c2ccc(C(=O)NC)cc21	10.1016/s0960-894x(01)00660-6
	CHEMBL433221	174953	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	561	8	2	7	4.5	CCn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c2ccc(C(=O)NC)cc21	10.1016/s0960-894x(01)00660-6
	10738157	66026	0	None	-	0	Rat	7.5	pIC50	=	7.5	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	374	7	1	5	4.0	Cc1ccccc1C(Oc1cc(OCc2cccnc2)ccc1C#N)C(=O)O	10.1021/jm990378b
	CHEMBL170348	66026	0	None	-	0	Rat	7.5	pIC50	=	7.5	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	374	7	1	5	4.0	Cc1ccccc1C(Oc1cc(OCc2cccnc2)ccc1C#N)C(=O)O	10.1021/jm990378b
	10714797	127495	0	None	-	0	Rat	7.5	pIC50	=	7.5	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	380	7	1	6	4.1	Cc1ccccc1C(Oc1cc(OCc2cncs2)ccc1C#N)C(=O)O	10.1021/jm990378b
	CHEMBL354740	127495	0	None	-	0	Rat	7.5	pIC50	=	7.5	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	380	7	1	6	4.1	Cc1ccccc1C(Oc1cc(OCc2cncs2)ccc1C#N)C(=O)O	10.1021/jm990378b
	10622380	108232	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	426	7	1	7	3.9	COc1cccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c1	10.1021/jm9700068
	CHEMBL297679	108232	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	426	7	1	7	3.9	COc1cccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c1	10.1021/jm9700068
	CHEMBL2369736	216443	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N(C)[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm970161m
	CHEMBL65559	222640	0	None	-	0	Pig	7.5	pIC50	=	7.5	Binding	Inhibition of endothelin (ET-A) binding to porcine heart membranes Inhibition of endothelin (ET-A) binding to porcine heart membranes	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/0960-894X(95)00349-X
	9850566	10966	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	551	8	1	8	6.1	COc1cc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OCc1ccccc1	10.1016/0960-894X(96)00170-9
	CHEMBL10016	10966	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	551	8	1	8	6.1	COc1cc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OCc1ccccc1	10.1016/0960-894X(96)00170-9
	CHEMBL342615	218454	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Inhibitory effect against Human Endothelin A receptorInhibitory effect against Human Endothelin A receptor	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CS(=O)(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	44311527	210902	0	None	-	1	Human	7.5	pIC50	=	7.5	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	675	12	2	11	7.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2cccs2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	CHEMBL70365	210902	0	None	-	1	Human	7.5	pIC50	=	7.5	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	675	12	2	11	7.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2cccs2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	CHEMBL148751	215563	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	The inhibitory constant was evaluated against Endothelin A receptorThe inhibitory constant was evaluated against Endothelin A receptor	ChEMBL		None	None	None		CC[C@@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)CN(Cc1ccccc1)C(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@H](C)CC	10.1016/S0960-894X(01)81219-1
	10836474	68554	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	432	9	1	5	4.7	COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc(OC)cc2OC)cc1	10.1021/jm031041j
	CHEMBL177287	68554	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	432	9	1	5	4.7	COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc(OC)cc2OC)cc1	10.1021/jm031041j
	10788853	12882	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	432	7	1	6	4.1	COc1ccc(C2(O)OC(=O)C(c3ccc(OC)cc3OC)=C2Cc2ccccc2)cc1	10.1021/jm9606507
	CHEMBL10808	12882	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	432	7	1	6	4.1	COc1ccc(C2(O)OC(=O)C(c3ccc(OC)cc3OC)=C2Cc2ccccc2)cc1	10.1021/jm9606507
	10717504	105289	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	430	6	0	6	4.5	COc1ccc(C2(OC)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1	10.1021/jm9606507
	CHEMBL276173	105289	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	430	6	0	6	4.5	COc1ccc(C2(OC)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1	10.1021/jm9606507
	10717504	105289	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells	ChEMBL	430	6	0	6	4.5	COc1ccc(C2(OC)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1	10.1016/S0960-894X(97)00002-4
	CHEMBL276173	105289	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells	ChEMBL	430	6	0	6	4.5	COc1ccc(C2(OC)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1	10.1016/S0960-894X(97)00002-4
	10522605	213557	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	361	6	1	4	5.0	Cc1ccccc1/C(=C\c1cc(OCc2ccsc2)ccc1C#N)CO	10.1021/jm970847e
	CHEMBL90191	213557	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	361	6	1	4	5.0	Cc1ccccc1/C(=C\c1cc(OCc2ccsc2)ccc1C#N)CO	10.1021/jm970847e
	10595639	213850	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	375	6	1	4	5.1	Cc1ccccc1/C(=C\c1cc(OCc2ccsc2)ccc1C#N)C(=O)O	10.1021/jm970847e
	CHEMBL91810	213850	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	375	6	1	4	5.1	Cc1ccccc1/C(=C\c1cc(OCc2ccsc2)ccc1C#N)C(=O)O	10.1021/jm970847e
	10697377	67861	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	523	10	4	6	4.2	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCC2)nc1C(=O)O	10.1021/jm950592+
	CHEMBL176513	67861	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	523	10	4	6	4.2	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCC2)nc1C(=O)O	10.1021/jm950592+
	CHEMBL3349461	218188	0	None	-	0	Pig	5.5	pIC50	=	5.5	Binding	Binding activity against Endothelin A receptor of Porcine aortic smooth muscle membranesBinding activity against Endothelin A receptor of Porcine aortic smooth muscle membranes	ChEMBL		None	None	None		CC(C)C[C@@H]1NC(=O)[C@@H](C(C)C)NC(=O)[C@H](C)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00089a028
	18617366	174615	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	394	3	1	4	3.3	Cc1noc(NS(=O)(=O)c2ccc(Br)cc2)c1Br	10.1016/0960-894X(96)00441-6
	CHEMBL430822	174615	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	394	3	1	4	3.3	Cc1noc(NS(=O)(=O)c2ccc(Br)cc2)c1Br	10.1016/0960-894X(96)00441-6
	44314864	109813	0	None	-	0	Pig	5.5	pIC50	=	5.5	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	566	11	5	5	3.4	CCCC(NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C)C(=O)O	10.1021/jm9600914
	CHEMBL307077	109813	0	None	-	0	Pig	5.5	pIC50	=	5.5	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	566	11	5	5	3.4	CCCC(NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C)C(=O)O	10.1021/jm9600914
	10788691	213542	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	428	6	1	3	6.0	Cc1ccccc1/C(=C\c1cc(OCc2ccsc2)ccc1Br)C(=O)O	10.1021/jm970847e
	CHEMBL90094	213542	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	428	6	1	3	6.0	Cc1ccccc1/C(=C\c1cc(OCc2ccsc2)ccc1Br)C(=O)O	10.1021/jm970847e
	127035544	143138	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	721	14	2	9	7.4	CCCc1nc2c(C)cc(C(=O)NCCc3cc(OC)ccc3OC)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	CHEMBL3734870	143138	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	721	14	2	9	7.4	CCCc1nc2c(C)cc(C(=O)NCCc3cc(OC)ccc3OC)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	10549875	66574	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	417	7	1	6	4.4	Cc1ccccc1C(Oc1cc(OCc2cccc3c2OCO3)ccc1C#N)C(=O)O	10.1021/jm990378b
	CHEMBL172691	66574	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	417	7	1	6	4.4	Cc1ccccc1C(Oc1cc(OCc2cccc3c2OCO3)ccc1C#N)C(=O)O	10.1021/jm990378b
	CHEMBL2367550	216363	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N(C)[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm970161m
	10506524	67954	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	536	9	4	5	4.2	CNC(=O)c1nc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)oc1C	10.1021/jm950592+
	CHEMBL176565	67954	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	536	9	4	5	4.2	CNC(=O)c1nc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)oc1C	10.1021/jm950592+
	10743900	134585	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	497	11	4	5	4.0	CCN(CC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(C)o1	10.1021/jm950592+
	CHEMBL366387	134585	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	497	11	4	5	4.0	CCN(CC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(C)o1	10.1021/jm950592+
	CHEMBL432683	220413	0	None	-	0	Pig	5.5	pIC50	=	5.5	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	44368396	51366	0	None	-	0	Pig	4.5	pIC50	=	4.5	Binding	Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.	ChEMBL	506	8	2	5	4.9	COc1ccc(C(=O)N(Cc2cc3c(cc2Cl)OCO3)C(Cc2c[nH]c3ccccc23)C(=O)O)cc1	10.1016/s0960-894x(01)00009-9
	CHEMBL152017	51366	0	None	-	0	Pig	4.5	pIC50	=	4.5	Binding	Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.	ChEMBL	506	8	2	5	4.9	COc1ccc(C(=O)N(Cc2cc3c(cc2Cl)OCO3)C(Cc2c[nH]c3ccccc23)C(=O)O)cc1	10.1016/s0960-894x(01)00009-9
	95285	104048	37	None	-	0	Rat	4.5	pIC50	=	4.5	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	256	3	2	5	1.7	O=S(=O)(Nc1nccs1)c1ccc(O)cc1	10.1021/jm00008a013
	CHEMBL26894	104048	37	None	-	0	Rat	4.5	pIC50	=	4.5	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	256	3	2	5	1.7	O=S(=O)(Nc1nccs1)c1ccc(O)cc1	10.1021/jm00008a013
	CHEMBL1791272	215696	0	None	-	0	Human	4.5	pIC50	=	4.5	Binding	Inhibition of [125I]endothelin-1 [ET-1] binding to endothelin A receptor (ETA) of rabbit renal artery vascular smooth muscle cellsInhibition of [125I]endothelin-1 [ET-1] binding to endothelin A receptor (ETA) of rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(C)=O)[C@H](C)CC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/0960-894X(95)00152-J
	10027408	103920	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	463	10	2	5	6.1	Cc1noc(NS(=O)(=O)c2cccc3c(NCCCCCc4ccccc4)cccc23)c1C	10.1021/jm00008a013
	CHEMBL26786	103920	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	463	10	2	5	6.1	Cc1noc(NS(=O)(=O)c2cccc3c(NCCCCCc4ccccc4)cccc23)c1C	10.1021/jm00008a013
	23445410	112921	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	412	4	1	5	4.6	Cc1ccccc1-c1ccsc1S(=O)(=O)Nc1onc(C)c1Br	10.1016/S0960-894X(96)00496-9
	CHEMBL313551	112921	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	412	4	1	5	4.6	Cc1ccccc1-c1ccsc1S(=O)(=O)Nc1onc(C)c1Br	10.1016/S0960-894X(96)00496-9
	23445379	136877	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor	ChEMBL	456	6	1	6	4.8	Cc1ccc(OCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1	10.1016/S0960-894X(97)00132-7
	CHEMBL367776	136877	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor	ChEMBL	456	6	1	6	4.8	Cc1ccc(OCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1	10.1016/S0960-894X(97)00132-7
	44459299	96382	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	520	7	3	6	4.4	CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2c[nH]c3cc(C(=O)O)ccc23)cc1	10.1016/s0960-894x(01)00660-6
	CHEMBL23752	96382	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	520	7	3	6	4.4	CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2c[nH]c3cc(C(=O)O)ccc23)cc1	10.1016/s0960-894x(01)00660-6
	44293754	108742	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	531	9	2	10	3.5	CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCC(=O)O)N(c1nn[nH]n1)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	CHEMBL301371	108742	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	531	9	2	10	3.5	CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCC(=O)O)N(c1nn[nH]n1)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	10552051	107948	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	463	6	2	9	3.3	CC(=O)c1cc2c(cc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1C)OCO2	10.1021/jm9608366
	CHEMBL295583	107948	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	463	6	2	9	3.3	CC(=O)c1cc2c(cc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1C)OCO2	10.1021/jm9608366
	18704821	106597	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors	ChEMBL	419	5	1	5	3.7	COc1nc(Br)cnc1NS(=O)(=O)c1ccccc1-c1ccccc1	10.1016/S0960-894X(97)00228-X
	CHEMBL285512	106597	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors	ChEMBL	419	5	1	5	3.7	COc1nc(Br)cnc1NS(=O)(=O)c1ccccc1-c1ccccc1	10.1016/S0960-894X(97)00228-X
	44279367	106530	0	None	-	0	Pig	6.5	pIC50	=	6.5	Binding	Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	485	11	5	4	2.0	CC(C)C[C@H](NC(=O)N1CCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	CHEMBL285031	106530	0	None	-	0	Pig	6.5	pIC50	=	6.5	Binding	Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	485	11	5	4	2.0	CC(C)C[C@H](NC(=O)N1CCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	10575356	16481	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	446	8	1	4	3.7	CCCN(C)C(=O)CN1C[C@H](c2ccc(F)c(F)c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	CHEMBL113184	16481	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	446	8	1	4	3.7	CCCN(C)C(=O)CN1C[C@H](c2ccc(F)c(F)c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	10551532	117361	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	450	8	1	4	3.9	CCCN(C)C(=O)CN1C[C@H](c2ccc3c(c2)CCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	CHEMBL325444	117361	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	450	8	1	4	3.9	CCCN(C)C(=O)CN1C[C@H](c2ccc3c(c2)CCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	127035219	143136	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	677	12	2	8	7.4	CCCc1nc2c(C)cc(C(=O)NCc3ccccc3OC)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	CHEMBL3734849	143136	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	677	12	2	8	7.4	CCCc1nc2c(C)cc(C(=O)NCc3ccccc3OC)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	44293719	103431	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	581	12	2	10	3.9	CCOc1ccc2c(c1)[C@@H](c1cc(OC)c(OC)c(OC)c1OCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	CHEMBL263723	103431	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	581	12	2	10	3.9	CCOc1ccc2c(c1)[C@@H](c1cc(OC)c(OC)c(OC)c1OCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	11800505	69009	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor	ChEMBL	536	11	3	6	5.1	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@@H](CC(=O)NC2CCCCC2)CC(C)C)nc1C(=O)O	10.1021/jm9505932
	CHEMBL177839	69009	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor	ChEMBL	536	11	3	6	5.1	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@@H](CC(=O)NC2CCCCC2)CC(C)C)nc1C(=O)O	10.1021/jm9505932
	10570511	213888	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	360	6	1	4	4.2	N#Cc1ccc(OCc2ccsc2)cc1/C=C(/C(N)=O)c1ccccc1	10.1021/jm970847e
	CHEMBL92092	213888	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	360	6	1	4	4.2	N#Cc1ccc(OCc2ccsc2)cc1/C=C(/C(N)=O)c1ccccc1	10.1021/jm970847e
	44276577	113634	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	459	7	1	7	4.1	COc1cccc(Cn2[nH]c(-c3ccc([N+](=O)[O-])cc3)c(Cc3ccc4c(c3)OCO4)c2=O)c1	10.1016/s0960-894x(00)00232-8
	CHEMBL3144850	113634	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	459	7	1	7	4.1	COc1cccc(Cn2[nH]c(-c3ccc([N+](=O)[O-])cc3)c(Cc3ccc4c(c3)OCO4)c2=O)c1	10.1016/s0960-894x(00)00232-8
	10357554	104340	1	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	302	3	1	4	3.2	Cc1noc(NS(=O)(=O)c2cccc3ccccc23)c1C	10.1021/jm00004a012
	CHEMBL27065	104340	1	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	302	3	1	4	3.2	Cc1noc(NS(=O)(=O)c2cccc3ccccc23)c1C	10.1021/jm00004a012
	44368539	51948	0	None	-	0	Pig	4.5	pIC50	=	4.5	Binding	Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.	ChEMBL	475	9	2	6	3.9	COc1cccc(CN(C(=O)/C=C/c2ccc3c(c2)OCO3)C(Cc2ccc(O)cc2)C(=O)O)c1	10.1016/s0960-894x(01)00009-9
	CHEMBL152552	51948	0	None	-	0	Pig	4.5	pIC50	=	4.5	Binding	Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.	ChEMBL	475	9	2	6	3.9	COc1cccc(CN(C(=O)/C=C/c2ccc3c(c2)OCO3)C(Cc2ccc(O)cc2)C(=O)O)c1	10.1016/s0960-894x(01)00009-9
	10476286	103203	0	None	-	0	Rat	4.5	pIC50	=	4.5	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	403	6	1	7	3.2	CCOC(=O)c1c(C)noc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12	10.1021/jm00008a013
	CHEMBL26206	103203	0	None	-	0	Rat	4.5	pIC50	=	4.5	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	403	6	1	7	3.2	CCOC(=O)c1c(C)noc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12	10.1021/jm00008a013
	127037496	143181	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	613	12	2	7	6.9	CCCCNC(=O)c1cc(C)c2nc(CCC)n(Cc3ccc(-c4ccccc4S(=O)(=O)Nc4onc(C)c4C)cc3)c2c1	10.1039/C4MD00499J
	CHEMBL3735311	143181	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	613	12	2	7	6.9	CCCCNC(=O)c1cc(C)c2nc(CCC)n(Cc3ccc(-c4ccccc4S(=O)(=O)Nc4onc(C)c4C)cc3)c2c1	10.1039/C4MD00499J
	22998508	213711	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	412	4	1	5	4.6	Cc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1	10.1016/S0960-894X(96)00496-9
	CHEMBL91073	213711	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	412	4	1	5	4.6	Cc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1	10.1016/S0960-894X(96)00496-9
	10020445	108145	0	None	-	0	Rat	4.5	pIC50	=	4.5	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2ccc3cccc(N(C)C)c3c2)c1C	10.1021/jm00008a013
	CHEMBL29705	108145	0	None	-	0	Rat	4.5	pIC50	=	4.5	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2ccc3cccc(N(C)C)c3c2)c1C	10.1021/jm00008a013
	10020445	108145	0	None	-	0	Rat	4.5	pIC50	=	4.5	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2ccc3cccc(N(C)C)c3c2)c1C	10.1021/jm00004a012
	CHEMBL29705	108145	0	None	-	0	Rat	4.5	pIC50	=	4.5	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2ccc3cccc(N(C)C)c3c2)c1C	10.1021/jm00004a012
	10645779	103944	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	419	4	1	4	4.2	Cc1cc(Br)cnc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12	10.1021/jm9604585
	CHEMBL268116	103944	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	419	4	1	4	4.2	Cc1cc(Br)cnc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12	10.1021/jm9604585
	10832243	210282	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	358	5	1	6	2.5	COc1ccc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)nn1	10.1021/jm9604585
	CHEMBL6624	210282	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	358	5	1	6	2.5	COc1ccc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)nn1	10.1021/jm9604585
	10692649	209885	1	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	404	4	1	3	4.5	CN(C)c1cccc2c(S(=O)(=O)Nc3ccc(Br)cc3)cccc12	10.1021/jm9604585
	CHEMBL6400	209885	1	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	404	4	1	3	4.5	CN(C)c1cccc2c(S(=O)(=O)Nc3ccc(Br)cc3)cccc12	10.1021/jm9604585
	CHEMBL293874	217671	0	None	-	0	Pig	7.5	pIC50	=	7.5	Binding	Binding activity against Endothelin A receptor of Porcine aortic smooth muscle membranesBinding activity against Endothelin A receptor of Porcine aortic smooth muscle membranes	ChEMBL		None	None	None		CC(C)C[C@@H]1NC(=O)[C@H](C(C)C)NC(=O)CN(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00089a028
	18738879	97008	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	548	8	2	7	4.8	CCn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c2ccc(C(=O)O)cc21	10.1016/s0960-894x(01)00660-6
	CHEMBL23833	97008	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	548	8	2	7	4.8	CCn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c2ccc(C(=O)O)cc21	10.1016/s0960-894x(01)00660-6
	18738879	97008	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells	ChEMBL	548	8	2	7	4.8	CCn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c2ccc(C(=O)O)cc21	10.1007/s00044-004-0021-y
	CHEMBL23833	97008	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells	ChEMBL	548	8	2	7	4.8	CCn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c2ccc(C(=O)O)cc21	10.1007/s00044-004-0021-y
	10548486	180895	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	391	5	2	6	3.7	Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1021/jm9608366
	CHEMBL45456	180895	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	391	5	2	6	3.7	Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1021/jm9608366
	44327661	171369	0	None	-	0	Rat	7.5	pIC50	=	7.5	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	483	5	1	8	2.7	Cc1ccc(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c2ccc3c(c2)OCO3)n1	10.1016/S0960-894X(96)00617-8
	CHEMBL421563	171369	0	None	-	0	Rat	7.5	pIC50	=	7.5	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	483	5	1	8	2.7	Cc1ccc(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c2ccc3c(c2)OCO3)n1	10.1016/S0960-894X(96)00617-8
	44327226	214694	0	None	-	0	Rat	7.5	pIC50	=	7.5	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	497	7	1	8	3.1	CCc1cc(C)nn(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c1=O	10.1016/S0960-894X(96)00617-8
	CHEMBL96762	214694	0	None	-	0	Rat	7.5	pIC50	=	7.5	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	497	7	1	8	3.1	CCc1cc(C)nn(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c1=O	10.1016/S0960-894X(96)00617-8
	CHEMBL132542	215482	0	None	-	0	Pig	7.5	pIC50	=	7.5	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)CN(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	10647372	213896	0	None	-	0	Rat	7.5	pIC50	=	7.5	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	454	8	1	6	3.1	CCN(CC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL9212	213896	0	None	-	0	Rat	7.5	pIC50	=	7.5	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	454	8	1	6	3.1	CCN(CC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL329609	218097	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)[C@@H](C)CC	10.1021/jm00015a003
	10665805	104954	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	354	4	1	6	3.0	CCC1=C(c2ccc3c(c2)OCO3)C(=O)OC1(O)c1ccc(OC)cc1	10.1021/jm9606507
	CHEMBL273951	104954	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	354	4	1	6	3.0	CCC1=C(c2ccc3c(c2)OCO3)C(=O)OC1(O)c1ccc(OC)cc1	10.1021/jm9606507
	44298381	202683	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	476	9	2	7	4.9	COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCO)c1	10.1016/s0960-894x(00)00366-8
	CHEMBL55909	202683	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	476	9	2	7	4.9	COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCO)c1	10.1016/s0960-894x(00)00366-8
	44279408	111438	0	None	-	0	Pig	5.5	pIC50	=	5.5	Binding	Binding affinity against ETA receptor in porcine aortic smooth muscle membraneBinding affinity against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	521	13	6	4	2.7	CC(C)C[C@H](NC(=O)NCc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	CHEMBL31051	111438	0	None	-	0	Pig	5.5	pIC50	=	5.5	Binding	Binding affinity against ETA receptor in porcine aortic smooth muscle membraneBinding affinity against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	521	13	6	4	2.7	CC(C)C[C@H](NC(=O)NCc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	44327868	118221	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL	906	24	9	8	3.9	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC12CC3CC(CC(C3)C1)C2)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	CHEMBL327523	118221	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL	906	24	9	8	3.9	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC12CC3CC(CC(C3)C1)C2)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	CHEMBL2369713	216434	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Inhibition of [125I]endothelin-1 [ET-1] binding to endothelin A receptor (ETA) of rabbit renal artery vascular smooth muscle cellsInhibition of [125I]endothelin-1 [ET-1] binding to endothelin A receptor (ETA) of rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/0960-894X(95)00152-J
	CHEMBL1793934	215711	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)N(C)C(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)[C@@H](C)CC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1021/jm970161m
	44327399	168322	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	539	7	1	8	4.2	CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)N2N=C(c3cccs3)CCC2=O)cc1	10.1016/S0960-894X(96)00617-8
	CHEMBL412865	168322	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	539	7	1	8	4.2	CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)N2N=C(c3cccs3)CCC2=O)cc1	10.1016/S0960-894X(96)00617-8
	44327734	214879	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	561	8	1	9	3.9	COc1ccc(-c2ccc(=O)n(C(C(=O)NS(=O)(=O)c3ccc(C(C)C)cc3)c3ccc4c(c3)OCO4)n2)cc1	10.1016/S0960-894X(96)00617-8
	CHEMBL97851	214879	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	561	8	1	9	3.9	COc1ccc(-c2ccc(=O)n(C(C(=O)NS(=O)(=O)c3ccc(C(C)C)cc3)c3ccc4c(c3)OCO4)n2)cc1	10.1016/S0960-894X(96)00617-8
	CHEMBL282340	217630	0	None	-	0	Pig	4.5	pIC50	=	4.5	Binding	Binding affinity against ETA receptor in porcine aortic smooth muscle membrane was determinedBinding affinity against ETA receptor in porcine aortic smooth muscle membrane was determined	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)[C@H](N)C(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CC(=O)O)C(=O)O	10.1016/0960-894X(95)00221-E
	44284506	174738	0	None	-	0	Pig	4.5	pIC50	=	4.5	Binding	Compound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranesCompound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranes	ChEMBL	596	14	4	4	4.6	CC(C)C[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)N(C)C(=O)[C@@H](CC(C)C)NC(=O)Cc1ccccc1Cl)C(=O)O	10.1021/jm00087a001
	CHEMBL431699	174738	0	None	-	0	Pig	4.5	pIC50	=	4.5	Binding	Compound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranesCompound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranes	ChEMBL	596	14	4	4	4.6	CC(C)C[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)N(C)C(=O)[C@@H](CC(C)C)NC(=O)Cc1ccccc1Cl)C(=O)O	10.1021/jm00087a001
	10555806	18894	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	616	12	2	7	6.0	CC(C)OCCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)(C)C)cc1	10.1021/jm990171i
	CHEMBL1184095	18894	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	616	12	2	7	6.0	CC(C)OCCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)(C)C)cc1	10.1021/jm990171i
	CHEMBL332289	18894	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	616	12	2	7	6.0	CC(C)OCCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)(C)C)cc1	10.1021/jm990171i
	23445505	210336	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	412	5	1	7	4.0	Cc1ccc(OC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)cc1	10.1016/S0960-894X(97)00367-3
	CHEMBL66641	210336	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	412	5	1	7	4.0	Cc1ccc(OC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)cc1	10.1016/S0960-894X(97)00367-3
	44314676	109701	0	None	-	0	Pig	7.5	pIC50	=	7.5	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	589	12	5	4	4.6	CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C)C(=O)O	10.1021/jm9600914
	CHEMBL306171	109701	0	None	-	0	Pig	7.5	pIC50	=	7.5	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	589	12	5	4	4.6	CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C)C(=O)O	10.1021/jm9600914
	10577388	22351	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	502	7	2	6	4.5	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2cc(C)ccc2C)cc1	10.1021/jm990170q
	CHEMBL122111	22351	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	502	7	2	6	4.5	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2cc(C)ccc2C)cc1	10.1021/jm990170q
	10625270	120152	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	502	7	2	6	4.5	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(C)cccc2C)cc1	10.1021/jm990170q
	CHEMBL331767	120152	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	502	7	2	6	4.5	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(C)cccc2C)cc1	10.1021/jm990170q
	70240112	178382	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	626	10	2	11	5.0	CC#CCOc1nc(-c2ccnc(-c3nnn[nH]3)c2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/j.bmcl.2016.06.014
	CHEMBL4465332	178382	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	626	10	2	11	5.0	CC#CCOc1nc(-c2ccnc(-c3nnn[nH]3)c2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/j.bmcl.2016.06.014
	44310016	210618	0	None	-	0	Rat	7.5	pIC50	=	7.5	Binding	Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor	ChEMBL	489	6	1	9	4.8	COc1cc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4nsnc4c3)c2cc1OC	10.1016/s0960-894x(97)10151-2
	CHEMBL68557	210618	0	None	-	0	Rat	7.5	pIC50	=	7.5	Binding	Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor	ChEMBL	489	6	1	9	4.8	COc1cc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4nsnc4c3)c2cc1OC	10.1016/s0960-894x(97)10151-2
	44386143	137470	0	None	-	0	Rat	7.5	pIC50	=	7.5	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	571	9	3	6	5.2	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCc3ccccc32)nc1C(=O)O	10.1021/jm950592+
	CHEMBL368360	137470	0	None	-	0	Rat	7.5	pIC50	=	7.5	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	571	9	3	6	5.2	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCc3ccccc32)nc1C(=O)O	10.1021/jm950592+
	44310016	210618	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Potency at Endothelin A receptor was determinedPotency at Endothelin A receptor was determined	ChEMBL	489	6	1	9	4.8	COc1cc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4nsnc4c3)c2cc1OC	10.1021/jm0300429
	CHEMBL68557	210618	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Potency at Endothelin A receptor was determinedPotency at Endothelin A receptor was determined	ChEMBL	489	6	1	9	4.8	COc1cc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4nsnc4c3)c2cc1OC	10.1021/jm0300429
	CHEMBL422285	220064	0	None	-	0	Pig	7.5	pIC50	=	7.5	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CCC[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	44279312	114102	0	None	-	0	Pig	6.5	pIC50	=	6.5	Binding	Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	565	12	6	4	3.5	CC(C)C[C@H](NC(=O)NC12CC3CC(CC(C3)C1)C2)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	CHEMBL31746	114102	0	None	-	0	Pig	6.5	pIC50	=	6.5	Binding	Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	565	12	6	4	3.5	CC(C)C[C@H](NC(=O)NC12CC3CC(CC(C3)C1)C2)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	44305079	108868	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	354	4	1	5	3.8	CC(C)Oc1ccc2c(c1)C=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	CHEMBL302189	108868	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	354	4	1	5	3.8	CC(C)Oc1ccc2c(c1)C=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	44293813	190888	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	581	12	2	10	3.9	CCOc1ccc2c(c1)[C@H](c1cc(OC)c(OC)c(OC)c1OCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	CHEMBL48261	190888	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	581	12	2	10	3.9	CCOc1ccc2c(c1)[C@H](c1cc(OC)c(OC)c(OC)c1OCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	44270523	55390	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells	ChEMBL	724	14	1	9	8.0	CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2	10.1016/0960-894X(95)00186-W
	CHEMBL15573	55390	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells	ChEMBL	724	14	1	9	8.0	CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2	10.1016/0960-894X(95)00186-W
	CHEMBL404763	219311	0	None	-	0	Pig	6.5	pIC50	=	6.5	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)C(C)(C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	44293716	108193	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	433	6	1	6	4.0	COc1ccc([C@@H]2c3cc(OC)ccc3[C@@H](c3ccc4c(c3)OCO4)N2CC(=O)O)cc1	10.1016/s0960-894x(01)00273-6
	CHEMBL297353	108193	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	433	6	1	6	4.0	COc1ccc([C@@H]2c3cc(OC)ccc3[C@@H](c3ccc4c(c3)OCO4)N2CC(=O)O)cc1	10.1016/s0960-894x(01)00273-6
	18936171	203285	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)	ChEMBL	489	7	1	8	4.2	COc1ccccc1Cn1c(=O)c(C(=O)O)c(-c2ccc3c(c2)OCO3)c2c(OC)c(OC)ccc21	10.1016/S0960-894X(97)00319-3
	CHEMBL56348	203285	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)	ChEMBL	489	7	1	8	4.2	COc1ccccc1Cn1c(=O)c(C(=O)O)c(-c2ccc3c(c2)OCO3)c2c(OC)c(OC)ccc21	10.1016/S0960-894X(97)00319-3
	44332546	113990	0	None	-	0	Human	4.5	pIC50	=	4.5	Binding	Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells	ChEMBL	491	5	0	7	5.7	O=C(OCc1ccc2c(c1)OCO2)C(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12	10.1016/S0960-894X(96)00551-3
	CHEMBL316648	113990	0	None	-	0	Human	4.5	pIC50	=	4.5	Binding	Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells	ChEMBL	491	5	0	7	5.7	O=C(OCc1ccc2c(c1)OCO2)C(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12	10.1016/S0960-894X(96)00551-3
	44322947	213480	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	428	5	1	6	4.3	COc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1	10.1016/S0960-894X(96)00496-9
	CHEMBL89689	213480	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	428	5	1	6	4.3	COc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1	10.1016/S0960-894X(96)00496-9
	10067069	106262	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	360	4	1	6	3.0	COC(=O)c1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12	10.1021/jm00008a013
	CHEMBL283195	106262	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	360	4	1	6	3.0	COC(=O)c1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12	10.1021/jm00008a013
	44385805	68070	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	532	10	1	10	4.1	C#CCOc1nc(-c2cnccn2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	CHEMBL176698	68070	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	532	10	1	10	4.1	C#CCOc1nc(-c2cnccn2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	10230375	136427	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	534	9	2	11	2.6	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2ncccn2)nc1OCC#CCO	10.1016/s0960-894x(02)01084-3
	CHEMBL367317	136427	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	534	9	2	11	2.6	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2ncccn2)nc1OCC#CCO	10.1016/s0960-894x(02)01084-3
	44384557	138168	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	504	9	1	10	3.3	C#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	CHEMBL369003	138168	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	504	9	1	10	3.3	C#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	23445547	119119	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	398	4	1	5	4.3	Cc1noc(NS(=O)(=O)c2cc(-c3ccccc3)cs2)c1Br	10.1016/S0960-894X(96)00496-9
	CHEMBL329375	119119	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	398	4	1	5	4.3	Cc1noc(NS(=O)(=O)c2cc(-c3ccccc3)cs2)c1Br	10.1016/S0960-894X(96)00496-9
	CHEMBL303204	217697	0	None	-	0	Pig	7.5	pIC50	=	7.5	Binding	Binding activity against Endothelin A receptor of Porcine aortic smooth muscle membranesBinding activity against Endothelin A receptor of Porcine aortic smooth muscle membranes	ChEMBL		None	None	None		CC(C)C[C@@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H](C)N(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00089a028
	22467219	92123	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells	ChEMBL	492	6	2	7	3.3	Cc1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(CO)ccc23)cc1	10.1007/s00044-004-0021-y
	CHEMBL2261362	92123	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells	ChEMBL	492	6	2	7	3.3	Cc1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(CO)ccc23)cc1	10.1007/s00044-004-0021-y
	44320461	113126	0	None	-	0	Rat	7.5	pIC50	=	7.5	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	514	6	1	5	6.6	O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1Cc1ccc(Cl)c(Cl)c1	10.1016/s0960-894x(00)00513-8
	CHEMBL313920	113126	0	None	-	0	Rat	7.5	pIC50	=	7.5	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	514	6	1	5	6.6	O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1Cc1ccc(Cl)c(Cl)c1	10.1016/s0960-894x(00)00513-8
	10457385	119465	0	None	-	1	Rat	7.5	pIC50	=	7.5	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	469	6	1	8	2.5	Cc1ccc(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)n1	10.1016/S0960-894X(96)00617-8
	CHEMBL330424	119465	0	None	-	1	Rat	7.5	pIC50	=	7.5	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	469	6	1	8	2.5	Cc1ccc(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)n1	10.1016/S0960-894X(96)00617-8
	CHEMBL263537	217352	0	None	-	0	Pig	7.5	pIC50	=	7.5	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H](C)N(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	10670664	214096	0	None	-	0	Rat	7.5	pIC50	=	7.5	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	438	8	2	6	2.6	C=CCNC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL9342	214096	0	None	-	0	Rat	7.5	pIC50	=	7.5	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	438	8	2	6	2.6	C=CCNC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	10792636	175294	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	544	10	2	6	5.4	CCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(CC)cccc2CC)cc1	10.1021/jm990170q
	CHEMBL435385	175294	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	544	10	2	6	5.4	CCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(CC)cccc2CC)cc1	10.1021/jm990170q
	44327423	214320	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	483	6	1	8	2.8	Cc1cc(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)nc1C	10.1016/S0960-894X(96)00617-8
	CHEMBL94720	214320	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	483	6	1	8	2.8	Cc1cc(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)nc1C	10.1016/S0960-894X(96)00617-8
	9998563	103620	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	359	4	2	5	3.2	CC(=O)Nc1ccc(S(=O)(=O)Nc2onc(C)c2C)c2ccccc12	10.1021/jm00008a013
	CHEMBL26527	103620	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	359	4	2	5	3.2	CC(=O)Nc1ccc(S(=O)(=O)Nc2onc(C)c2C)c2ccccc12	10.1021/jm00008a013
	10895198	107731	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	426	9	1	6	5.0	CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2cccc(OCCC)c21	10.1021/jm010382z
	CHEMBL294123	107731	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	426	9	1	6	5.0	CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2cccc(OCCC)c21	10.1021/jm010382z
	44298612	202304	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	281	4	2	5	1.9	CCc1c(NS(=O)(=O)c2ccc(N)cc2)noc1C	10.1016/s0960-894x(00)00366-8
	CHEMBL55405	202304	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	281	4	2	5	1.9	CCc1c(NS(=O)(=O)c2ccc(N)cc2)noc1C	10.1016/s0960-894x(00)00366-8
	9998563	103620	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	359	4	2	5	3.2	CC(=O)Nc1ccc(S(=O)(=O)Nc2onc(C)c2C)c2ccccc12	10.1021/jm00004a012
	CHEMBL26527	103620	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	359	4	2	5	3.2	CC(=O)Nc1ccc(S(=O)(=O)Nc2onc(C)c2C)c2ccccc12	10.1021/jm00004a012
	44332638	11148	0	None	-	0	Human	4.5	pIC50	=	4.5	Binding	Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells	ChEMBL	477	6	0	6	6.0	COc1ccc(COC(=O)C(c2ccc3c(c2)OCO3)c2c3ccccc3nc3ccccc23)cc1	10.1016/S0960-894X(96)00551-3
	CHEMBL101239	11148	0	None	-	0	Human	4.5	pIC50	=	4.5	Binding	Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells	ChEMBL	477	6	0	6	6.0	COc1ccc(COC(=O)C(c2ccc3c(c2)OCO3)c2c3ccccc3nc3ccccc23)cc1	10.1016/S0960-894X(96)00551-3
	137643691	165037	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	569	10	2	7	5.5	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC4CCC4)ccc31)OCO2	10.1016/j.bmcl.2017.04.049
	CHEMBL4088634	165037	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	569	10	2	7	5.5	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC4CCC4)ccc31)OCO2	10.1016/j.bmcl.2017.04.049
	23445538	66845	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor	ChEMBL	456	6	1	6	4.8	Cc1ccc(OCc2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1	10.1016/S0960-894X(97)00132-7
	CHEMBL173805	66845	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor	ChEMBL	456	6	1	6	4.8	Cc1ccc(OCc2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1	10.1016/S0960-894X(97)00132-7
	23445272	134528	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	440	6	1	5	4.7	Cc1ccc(CCc2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1	10.1016/S0960-894X(97)00133-9
	CHEMBL366364	134528	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	440	6	1	5	4.7	Cc1ccc(CCc2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1	10.1016/S0960-894X(97)00133-9
	10615322	210197	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	316	4	1	7	1.9	COC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1C	10.1016/S0960-894X(97)00367-3
	CHEMBL65639	210197	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	316	4	1	7	1.9	COC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1C	10.1016/S0960-894X(97)00367-3
	11762081	210098	0	None	-	0	Rat	7.5	pIC50	=	7.5	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	446	7	1	5	5.5	COc1ccc(C2=C(C(=O)O)C(c3ccc(OC)cc3)Oc3ccc(OC(C)C)cc32)cc1	10.1021/jm031041j
	CHEMBL64851	210098	0	None	-	0	Rat	7.5	pIC50	=	7.5	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	446	7	1	5	5.5	COc1ccc(C2=C(C(=O)O)C(c3ccc(OC)cc3)Oc3ccc(OC(C)C)cc32)cc1	10.1021/jm031041j
	CHEMBL307324	217758	0	None	-	0	Pig	7.5	pIC50	=	7.5	Binding	Binding activity against Endothelin A receptor of Porcine aortic smooth muscle membranesBinding activity against Endothelin A receptor of Porcine aortic smooth muscle membranes	ChEMBL		None	None	None		CC(C)C[C@H]1C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CC(=O)O)C(=O)N2CCC[C@H]2C(=O)N[C@@H](C(C)C)C(=O)N1C	10.1021/jm00089a028
	CHEMBL319719	218000	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	10503067	14942	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	436	5	1	6	4.9	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2CC2CCCCCC2)cc1	10.1021/jm9606507
	CHEMBL10919	14942	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	436	5	1	6	4.9	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2CC2CCCCCC2)cc1	10.1021/jm9606507
	11762081	210098	0	None	-	0	Rat	7.5	pIC50	=	7.5	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	446	7	1	5	5.5	COc1ccc(C2=C(C(=O)O)C(c3ccc(OC)cc3)Oc3ccc(OC(C)C)cc32)cc1	10.1021/jm010382z
	CHEMBL64851	210098	0	None	-	0	Rat	7.5	pIC50	=	7.5	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	446	7	1	5	5.5	COc1ccc(C2=C(C(=O)O)C(c3ccc(OC)cc3)Oc3ccc(OC(C)C)cc32)cc1	10.1021/jm010382z
	155519245	177123	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Displacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cellsDisplacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cells	ChEMBL	592	10	2	10	4.2	COc1ccc(Cl)c(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)nc(N3CCOCC3)nc2OCCO)c1	10.1016/j.bmcl.2016.06.014
	CHEMBL4447261	177123	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Displacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cellsDisplacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cells	ChEMBL	592	10	2	10	4.2	COc1ccc(Cl)c(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)nc(N3CCOCC3)nc2OCCO)c1	10.1016/j.bmcl.2016.06.014
	22467240	105963	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	558	7	2	9	3.8	CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(-c4nn[nH]n4)ccc23)cc1	10.1016/s0960-894x(01)00660-6
	CHEMBL281378	105963	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	558	7	2	9	3.8	CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(-c4nn[nH]n4)ccc23)cc1	10.1016/s0960-894x(01)00660-6
	10305334	135825	0	None	-	1	Human	7.5	pIC50	=	7.5	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	680	12	2	11	6.3	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccncc2)nc1OCC#CCOC(=O)Nc1ccccc1	10.1016/s0960-894x(02)01084-3
	CHEMBL367036	135825	0	None	-	1	Human	7.5	pIC50	=	7.5	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	680	12	2	11	6.3	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccncc2)nc1OCC#CCOC(=O)Nc1ccccc1	10.1016/s0960-894x(02)01084-3
	CHEMBL138120	215530	0	None	-	0	Pig	7.5	pIC50	=	7.5	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@@H]1C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CC(=O)O)C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C(C)C)C(=O)N1C	10.1021/jm00021a021
	11133491	108946	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	416	3	1	6	4.2	O=C(O)C1=C(c2ccc3c(c2)OCO3)c2ccccc2OC1c1ccc2c(c1)OCO2	10.1021/jm010382z
	CHEMBL302659	108946	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	416	3	1	6	4.2	O=C(O)C1=C(c2ccc3c(c2)OCO3)c2ccccc2OC1c1ccc2c(c1)OCO2	10.1021/jm010382z
	10950843	209731	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	474	8	1	6	5.6	CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1cccc(OC)c1)O2	10.1021/jm010382z
	CHEMBL62951	209731	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	474	8	1	6	5.6	CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1cccc(OC)c1)O2	10.1021/jm010382z
	44279370	113983	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor	ChEMBL	426	4	2	3	4.7	CCc1ccc(-c2ccc3c(c2)C(=O)c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@H]32)cc1	10.1016/0960-894X(95)00230-Q
	CHEMBL31662	113983	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor	ChEMBL	426	4	2	3	4.7	CCc1ccc(-c2ccc3c(c2)C(=O)c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@H]32)cc1	10.1016/0960-894X(95)00230-Q
	CHEMBL1790451	215668	0	None	-	0	Pig	6.5	pIC50	=	6.5	Binding	Inhibition of endothelin (ET-A) binding to porcine heart membranes Inhibition of endothelin (ET-A) binding to porcine heart membranes	ChEMBL		None	None	None		CC(=O)N[C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)C(C)C)[C@H](C)O)C1c2ccccc2CCc2ccccc21	10.1016/0960-894X(95)00349-X
	10790376	173688	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	466	6	1	6	3.3	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N2CCCCC2)cc1	10.1021/jm9505369
	CHEMBL428644	173688	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	466	6	1	6	3.3	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N2CCCCC2)cc1	10.1021/jm9505369
	44266655	11815	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	445	5	1	7	4.5	COc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2c(c1)OCO2	10.1016/0960-894X(96)00170-9
	CHEMBL10523	11815	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	445	5	1	7	4.5	COc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2c(c1)OCO2	10.1016/0960-894X(96)00170-9
	44371420	57684	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes	ChEMBL	485	7	1	7	5.2	COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3cccc(OC)c3OC)c3c2oc2ccccc23)cc1	10.1016/s0960-894x(99)00040-2
	CHEMBL157763	57684	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes	ChEMBL	485	7	1	7	5.2	COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3cccc(OC)c3OC)c3c2oc2ccccc23)cc1	10.1016/s0960-894x(99)00040-2
	10425958	106729	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	317	3	2	5	2.8	Cc1noc(NS(=O)(=O)c2ccc(N)c3ccccc23)c1C	10.1021/jm00008a013
	CHEMBL286406	106729	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	317	3	2	5	2.8	Cc1noc(NS(=O)(=O)c2ccc(N)c3ccccc23)c1C	10.1021/jm00008a013
	CHEMBL438194	220532	14	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00070a001
	44327881	168454	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL	1044	26	9	8	6.4	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	CHEMBL413179	168454	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL	1044	26	9	8	6.4	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	44298613	202306	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	287	3	2	5	2.0	Cc1onc(NS(=O)(=O)c2ccc(N)cc2)c1Cl	10.1016/s0960-894x(00)00366-8
	CHEMBL55406	202306	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	287	3	2	5	2.0	Cc1onc(NS(=O)(=O)c2ccc(N)cc2)c1Cl	10.1016/s0960-894x(00)00366-8
	CHEMBL438768	220575	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	In vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricleIn vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricle	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)80156-6
	44277387	113627	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	450	7	2	6	3.0	O=C(O)COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2=O)c1	10.1016/s0960-894x(00)00232-8
	CHEMBL3144800	113627	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	450	7	2	6	3.0	O=C(O)COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2=O)c1	10.1016/s0960-894x(00)00232-8
	10425958	106729	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	317	3	2	5	2.8	Cc1noc(NS(=O)(=O)c2ccc(N)c3ccccc23)c1C	10.1021/jm00004a012
	CHEMBL286406	106729	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	317	3	2	5	2.8	Cc1noc(NS(=O)(=O)c2ccc(N)c3ccccc23)c1C	10.1021/jm00004a012
	44266645	214536	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	417	5	1	6	4.7	COc1ccc(-n2c(C(=O)O)c(-c3ccc4c(c3)OCO4)c3cc(OC)ccc32)cc1	10.1016/0960-894X(96)00170-9
	CHEMBL9588	214536	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	417	5	1	6	4.7	COc1ccc(-n2c(C(=O)O)c(-c3ccc4c(c3)OCO4)c3cc(OC)ccc32)cc1	10.1016/0960-894X(96)00170-9
	127034918	143236	0	None	-	0	Human	4.5	pIC50	=	4.5	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	599	11	2	7	6.6	CCCNC(=O)c1cc(C)c2nc(CCC)n(Cc3ccc(-c4ccccc4S(=O)(=O)Nc4onc(C)c4C)cc3)c2c1	10.1039/C4MD00499J
	CHEMBL3735797	143236	0	None	-	0	Human	4.5	pIC50	=	4.5	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	599	11	2	7	6.6	CCCNC(=O)c1cc(C)c2nc(CCC)n(Cc3ccc(-c4ccccc4S(=O)(=O)Nc4onc(C)c4C)cc3)c2c1	10.1039/C4MD00499J
	CHEMBL263025	217337	0	None	-	0	Pig	4.5	pIC50	=	4.5	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)CNC(=O)[C@@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	44386523	139360	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	621	10	4	6	5.5	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2c(F)c(F)c(F)c(F)c2F)nc1C(=O)O	10.1021/jm950592+
	CHEMBL369874	139360	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	621	10	4	6	5.5	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2c(F)c(F)c(F)c(F)c2F)nc1C(=O)O	10.1021/jm950592+
	CHEMBL421190	220048	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	CHEMBL2304009	216244	0	None	-	0	Pig	7.4	pIC50	=	7.4	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc2c(Br)[nH]c3ccccc23)NC(=O)[C@@H](C(C)C)NC1=O	10.1021/jm9600914
	CHEMBL87243	222672	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1021/jm00070a001
	44327347	103538	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL	1102	26	9	8	7.1	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C1c2ccccc2CCc2ccccc21)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	CHEMBL264579	103538	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL	1102	26	9	8	7.1	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C1c2ccccc2CCc2ccccc21)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	44368516	51585	0	None	-	0	Pig	4.4	pIC50	=	4.4	Binding	Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.	ChEMBL	451	11	2	6	4.1	COc1ccc(CN(Cc2cc(OC)cc(OC)c2)C(Cc2ccc(O)cc2)C(=O)O)cc1	10.1016/s0960-894x(01)00009-9
	CHEMBL152203	51585	0	None	-	0	Pig	4.4	pIC50	=	4.4	Binding	Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.	ChEMBL	451	11	2	6	4.1	COc1ccc(CN(Cc2cc(OC)cc(OC)c2)C(Cc2ccc(O)cc2)C(=O)O)cc1	10.1016/s0960-894x(01)00009-9
	10816835	68159	0	None	-	0	Rat	4.4	pIC50	=	4.4	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	567	11	4	5	5.7	CCCc1sc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O	10.1021/jm950591h
	CHEMBL176992	68159	0	None	-	0	Rat	4.4	pIC50	=	4.4	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	567	11	4	5	5.7	CCCc1sc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O	10.1021/jm950591h
	137652304	164005	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	544	10	3	8	3.7	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCCN)ccc31)OCO2	10.1016/j.bmcl.2017.04.049
	CHEMBL4076290	164005	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	544	10	3	8	3.7	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCCN)ccc31)OCO2	10.1016/j.bmcl.2017.04.049
	22998446	113409	0	None	-	0	Human	4.4	pIC50	=	4.4	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	398	4	1	5	4.3	Cc1noc(NS(=O)(=O)c2ccc(-c3ccccc3)s2)c1Br	10.1016/S0960-894X(96)00496-9
	CHEMBL314320	113409	0	None	-	0	Human	4.4	pIC50	=	4.4	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	398	4	1	5	4.3	Cc1noc(NS(=O)(=O)c2ccc(-c3ccccc3)s2)c1Br	10.1016/S0960-894X(96)00496-9
	443289	7498	47	None	2	3	Human	7.4	pIC50	=	7.4	Binding	Antagonist activity at Homo sapiens (human) ETA receptorAntagonist activity at Homo sapiens (human) ETA receptor	ChEMBL		None	None	None		None	10.1007/s00044-013-0542-3
	997	7498	47	None	2	3	Human	7.4	pIC50	=	7.4	Binding	Antagonist activity at Homo sapiens (human) ETA receptorAntagonist activity at Homo sapiens (human) ETA receptor	ChEMBL		None	None	None		None	10.1007/s00044-013-0542-3
	CHEMBL314691	7498	47	None	2	3	Human	7.4	pIC50	=	7.4	Binding	Antagonist activity at Homo sapiens (human) ETA receptorAntagonist activity at Homo sapiens (human) ETA receptor	ChEMBL		None	None	None		None	10.1007/s00044-013-0542-3
	DB12054	7498	47	None	2	3	Human	7.4	pIC50	=	7.4	Binding	Antagonist activity at Homo sapiens (human) ETA receptorAntagonist activity at Homo sapiens (human) ETA receptor	ChEMBL		None	None	None		None	10.1007/s00044-013-0542-3
	11798762	213402	0	None	-	0	Rat	7.4	pIC50	=	7.4	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	475	9	1	7	3.1	CCCS(=O)(=O)CCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL8911	213402	0	None	-	0	Rat	7.4	pIC50	=	7.4	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	475	9	1	7	3.1	CCCS(=O)(=O)CCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	10768346	138321	0	None	-	0	Rat	7.4	pIC50	=	7.4	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	522	10	5	5	4.0	Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCC2)nc1C(=O)O	10.1021/jm950592+
	CHEMBL369202	138321	0	None	-	0	Rat	7.4	pIC50	=	7.4	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	522	10	5	5	4.0	Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCC2)nc1C(=O)O	10.1021/jm950592+
	24997097	25245	3	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	501	7	3	7	4.0	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(O)ccc31)OCO2	10.1016/j.bmcl.2017.04.049
	CHEMBL1272137	25245	3	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	501	7	3	7	4.0	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(O)ccc31)OCO2	10.1016/j.bmcl.2017.04.049
	44309445	109476	4	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor	ChEMBL	370	4	1	5	3.4	CN(C)c1cccc2c(S(=O)(=O)Nc3ccc4c(c3)OCO4)cccc12	10.1016/s0960-894x(97)10151-2
	CHEMBL304761	109476	4	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor	ChEMBL	370	4	1	5	3.4	CN(C)c1cccc2c(S(=O)(=O)Nc3ccc4c(c3)OCO4)cccc12	10.1016/s0960-894x(97)10151-2
	10816963	120106	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	574	12	2	7	5.0	CCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC)cc1	10.1021/jm990170q
	CHEMBL331625	120106	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	574	12	2	7	5.0	CCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC)cc1	10.1021/jm990170q
	CHEMBL289687	217654	0	None	-	0	Rat	5.4	pIC50	=	5.4	Binding	Compound was evaluated for the binding affinity to endothelin receptor in the rat heart ventricle.Compound was evaluated for the binding affinity to endothelin receptor in the rat heart ventricle.	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]cn1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00087a001
	10602726	172565	0	None	-	0	Rat	5.4	pIC50	=	5.4	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	549	10	4	5	5.1	CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(C2CC2)o1	10.1021/jm950591h
	CHEMBL424764	172565	0	None	-	0	Rat	5.4	pIC50	=	5.4	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	549	10	4	5	5.1	CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(C2CC2)o1	10.1021/jm950591h
	44332623	11538	1	None	-	0	Human	4.4	pIC50	=	4.4	Binding	Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells	ChEMBL	320	3	1	4	2.9	Cc1cc(C(C(N)=O)c2ccc3c(c2)OCO3)c2ccccc2n1	10.1016/S0960-894X(96)00551-3
	CHEMBL103886	11538	1	None	-	0	Human	4.4	pIC50	=	4.4	Binding	Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells	ChEMBL	320	3	1	4	2.9	Cc1cc(C(C(N)=O)c2ccc3c(c2)OCO3)c2ccccc2n1	10.1016/S0960-894X(96)00551-3
	137655285	165756	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	568	10	3	10	3.1	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(OCCN)ccc31)OCO2	10.1016/j.bmcl.2017.04.049
	CHEMBL4096211	165756	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	568	10	3	10	3.1	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(OCCN)ccc31)OCO2	10.1016/j.bmcl.2017.04.049
	44177614	136429	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	547	10	1	9	5.4	C=CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	CHEMBL367339	136429	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	547	10	1	9	5.4	C=CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	22467229	105733	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	519	7	2	7	4.1	CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(CN)ccc23)cc1	10.1016/s0960-894x(01)00660-6
	CHEMBL279703	105733	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	519	7	2	7	4.1	CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(CN)ccc23)cc1	10.1016/s0960-894x(01)00660-6
	44385008	138139	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	574	10	2	9	4.9	C#CCOc1nc(-c2ccnc(CO)c2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	CHEMBL368829	138139	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	574	10	2	9	4.9	C#CCOc1nc(-c2ccnc(CO)c2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	19010493	105132	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells	ChEMBL	543	11	1	7	6.5	CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)O)c1ccc2c(c1)OCO2	10.1016/0960-894X(95)00186-W
	CHEMBL275179	105132	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells	ChEMBL	543	11	1	7	6.5	CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)O)c1ccc2c(c1)OCO2	10.1016/0960-894X(95)00186-W
	42630532	25171	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	541	10	2	7	4.9	C=CCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2	10.1016/j.bmcl.2017.04.049
	CHEMBL1271479	25171	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	541	10	2	7	4.9	C=CCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2	10.1016/j.bmcl.2017.04.049
	42630532	25171	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer	ChEMBL	541	10	2	7	4.9	C=CCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2	10.1016/j.bmcl.2010.08.074
	CHEMBL1271479	25171	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer	ChEMBL	541	10	2	7	4.9	C=CCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2	10.1016/j.bmcl.2010.08.074
	24997097	25245	3	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer	ChEMBL	501	7	3	7	4.0	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(O)ccc31)OCO2	10.1016/j.bmcl.2010.08.074
	CHEMBL1272137	25245	3	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer	ChEMBL	501	7	3	7	4.0	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(O)ccc31)OCO2	10.1016/j.bmcl.2010.08.074
	10173807	57656	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes	ChEMBL	455	6	1	6	5.2	COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2ccccc23)cc1	10.1016/s0960-894x(99)00040-2
	CHEMBL157742	57656	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes	ChEMBL	455	6	1	6	5.2	COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2ccccc23)cc1	10.1016/s0960-894x(99)00040-2
	18995990	106132	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.	ChEMBL	507	7	1	9	5.0	COc1cccc(Sc2c(C(=O)O)n(Cc3cc(OC)c4c(c3)OCO4)c3cc4c(cc23)OCO4)c1	10.1016/0960-894X(96)00232-6
	CHEMBL282426	106132	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.	ChEMBL	507	7	1	9	5.0	COc1cccc(Sc2c(C(=O)O)n(Cc3cc(OC)c4c(c3)OCO4)c3cc4c(cc23)OCO4)c1	10.1016/0960-894X(96)00232-6
	10160887	106924	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.	ChEMBL	447	5	1	7	5.0	O=C(O)c1c(Sc2ccc3c(c2)OCO3)c2ccccc2n1Cc1ccc2c(c1)OCO2	10.1016/0960-894X(96)00232-6
	CHEMBL28779	106924	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.	ChEMBL	447	5	1	7	5.0	O=C(O)c1c(Sc2ccc3c(c2)OCO3)c2ccccc2n1Cc1ccc2c(c1)OCO2	10.1016/0960-894X(96)00232-6
	CHEMBL411797	219736	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	44298277	201778	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	474	9	1	7	5.1	COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCC=O)c1	10.1016/s0960-894x(00)00366-8
	CHEMBL54773	201778	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	474	9	1	7	5.1	COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCC=O)c1	10.1016/s0960-894x(00)00366-8
	10288713	108820	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)	ChEMBL	473	7	1	7	4.6	CCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)c(=O)n2Cc1ccccc1OC	10.1016/S0960-894X(97)00319-3
	CHEMBL301840	108820	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)	ChEMBL	473	7	1	7	4.6	CCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)c(=O)n2Cc1ccccc1OC	10.1016/S0960-894X(97)00319-3
	CHEMBL62514	222623	0	None	-	0	Pig	6.4	pIC50	=	6.4	Binding	Inhibition of endothelin (ET-A) binding to porcine heart membranes Inhibition of endothelin (ET-A) binding to porcine heart membranes	ChEMBL		None	None	None		CC(=O)N[C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)C(C)C)C1c2ccccc2CCc2ccccc21	10.1016/0960-894X(95)00349-X
	10383832	174958	0	None	-	0	Rat	5.4	pIC50	=	5.4	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	359	4	2	5	3.2	CC(=O)Nc1ccc2cc(S(=O)(=O)Nc3onc(C)c3C)ccc2c1	10.1021/jm00008a013
	CHEMBL433234	174958	0	None	-	0	Rat	5.4	pIC50	=	5.4	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	359	4	2	5	3.2	CC(=O)Nc1ccc2cc(S(=O)(=O)Nc3onc(C)c3C)ccc2c1	10.1021/jm00008a013
	10540843	92614	9	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)	ChEMBL	282	4	1	3	4.0	Cc1c(C(=O)O)oc2cccc(OCc3ccccc3)c12	10.1007/s00044-013-0542-3
	CHEMBL2296889	92614	9	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)	ChEMBL	282	4	1	3	4.0	Cc1c(C(=O)O)oc2cccc(OCc3ccccc3)c12	10.1007/s00044-013-0542-3
	CHEMBL408141	219482	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)80156-6
	18617407	211759	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	320	3	1	4	3.4	Cc1noc(NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1C	10.1016/0960-894X(96)00441-6
	CHEMBL76576	211759	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	320	3	1	4	3.4	Cc1noc(NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1C	10.1016/0960-894X(96)00441-6
	44276886	113610	0	None	-	0	Rat	5.4	pIC50	=	5.4	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	410	4	1	4	4.2	O=c1c(Cc2ccc3c(c2)OCO3)c(C(F)(F)F)[nH]n1Cc1ccccc1Cl	10.1016/s0960-894x(00)00232-8
	CHEMBL3144600	113610	0	None	-	0	Rat	5.4	pIC50	=	5.4	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	410	4	1	4	4.2	O=c1c(Cc2ccc3c(c2)OCO3)c(C(F)(F)F)[nH]n1Cc1ccccc1Cl	10.1016/s0960-894x(00)00232-8
	44277368	113622	0	None	-	0	Rat	5.4	pIC50	=	5.4	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	480	8	2	7	3.0	COc1ccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2=O)c(OCC(=O)O)c1	10.1016/s0960-894x(00)00232-8
	CHEMBL3144733	113622	0	None	-	0	Rat	5.4	pIC50	=	5.4	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	480	8	2	7	3.0	COc1ccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2=O)c(OCC(=O)O)c1	10.1016/s0960-894x(00)00232-8
	10070783	103831	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells	ChEMBL	420	4	1	5	4.5	O=C1OC(O)(c2ccc(Cl)cc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2	10.1021/jm9606507
	CHEMBL267094	103831	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells	ChEMBL	420	4	1	5	4.5	O=C1OC(O)(c2ccc(Cl)cc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2	10.1021/jm9606507
	10383832	174958	0	None	-	0	Rat	5.4	pIC50	=	5.4	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	359	4	2	5	3.2	CC(=O)Nc1ccc2cc(S(=O)(=O)Nc3onc(C)c3C)ccc2c1	10.1021/jm00004a012
	CHEMBL433234	174958	0	None	-	0	Rat	5.4	pIC50	=	5.4	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	359	4	2	5	3.2	CC(=O)Nc1ccc2cc(S(=O)(=O)Nc3onc(C)c3C)ccc2c1	10.1021/jm00004a012
	44368482	51458	0	None	-	0	Pig	4.4	pIC50	=	4.4	Binding	Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.	ChEMBL	523	8	2	7	4.2	O=C(O)C(Cc1ccc(O)cc1)N(Cc1cc2c(cc1Cl)OCO2)C(=O)/C=C/c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00009-9
	CHEMBL152091	51458	0	None	-	0	Pig	4.4	pIC50	=	4.4	Binding	Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.	ChEMBL	523	8	2	7	4.2	O=C(O)C(Cc1ccc(O)cc1)N(Cc1cc2c(cc1Cl)OCO2)C(=O)/C=C/c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00009-9
	4550514	103980	6	None	-	0	Rat	4.4	pIC50	=	4.4	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	386	5	3	5	3.7	Cc1noc(NS(=O)(=O)c2ccc(NC(=O)Nc3ccccc3)cc2)c1C	10.1021/jm00008a013
	CHEMBL26842	103980	6	None	-	0	Rat	4.4	pIC50	=	4.4	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	386	5	3	5	3.7	Cc1noc(NS(=O)(=O)c2ccc(NC(=O)Nc3ccccc3)cc2)c1C	10.1021/jm00008a013
	127035083	143134	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	677	12	2	8	7.4	CCCc1nc2c(C)cc(C(=O)NCc3ccc(OC)cc3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	CHEMBL3734835	143134	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	677	12	2	8	7.4	CCCc1nc2c(C)cc(C(=O)NCc3ccc(OC)cc3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	76320429	92616	0	None	-	0	Rat	7.4	pIC50	=	7.4	Binding	Displacement of [125I]ET-1 from ETA receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hrDisplacement of [125I]ET-1 from ETA receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hr	ChEMBL	324	4	1	6	3.6	Cc1c(C(=O)O)oc2cccc(OCc3ccc4nonc4c3)c12	10.1007/s00044-013-0542-3
	CHEMBL2296900	92616	0	None	-	0	Rat	7.4	pIC50	=	7.4	Binding	Displacement of [125I]ET-1 from ETA receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hrDisplacement of [125I]ET-1 from ETA receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hr	ChEMBL	324	4	1	6	3.6	Cc1c(C(=O)O)oc2cccc(OCc3ccc4nonc4c3)c12	10.1007/s00044-013-0542-3
	10875450	16596	0	None	-	0	Pig	7.4	pIC50	=	7.4	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	565	11	1	10	4.9	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2nccc(C)n2)c1	10.1021/jm0102304
	CHEMBL113927	16596	0	None	-	0	Pig	7.4	pIC50	=	7.4	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	565	11	1	10	4.9	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2nccc(C)n2)c1	10.1021/jm0102304
	18704814	106898	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors	ChEMBL	475	7	1	5	4.9	COc1nc(Br)cnc1NS(=O)(=O)c1ccccc1-c1ccc(CC(C)C)cc1	10.1016/S0960-894X(97)00228-X
	CHEMBL287581	106898	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors	ChEMBL	475	7	1	5	4.9	COc1nc(Br)cnc1NS(=O)(=O)c1ccccc1-c1ccc(CC(C)C)cc1	10.1016/S0960-894X(97)00228-X
	44279173	114040	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors	ChEMBL	476	6	2	6	3.1	CNC(=O)c1cccc(S(=O)(=O)Nc2ncc(Br)nc2OC)c1-c1ccccc1	10.1016/S0960-894X(97)00228-X
	CHEMBL31696	114040	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors	ChEMBL	476	6	2	6	3.1	CNC(=O)c1cccc(S(=O)(=O)Nc2ncc(Br)nc2OC)c1-c1ccccc1	10.1016/S0960-894X(97)00228-X
	44279237	117309	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors	ChEMBL	462	6	2	6	2.8	COc1nc(Br)cnc1NS(=O)(=O)c1cccc(C(N)=O)c1-c1ccccc1	10.1016/S0960-894X(97)00228-X
	CHEMBL32512	117309	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors	ChEMBL	462	6	2	6	2.8	COc1nc(Br)cnc1NS(=O)(=O)c1cccc(C(N)=O)c1-c1ccccc1	10.1016/S0960-894X(97)00228-X
	44309996	210538	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor	ChEMBL	483	5	1	8	5.2	COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccc4nsnc4c3)c3c2oc2ccccc23)cc1	10.1016/s0960-894x(97)10151-2
	CHEMBL67971	210538	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor	ChEMBL	483	5	1	8	5.2	COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccc4nsnc4c3)c3c2oc2ccccc23)cc1	10.1016/s0960-894x(97)10151-2
	CHEMBL342913	218474	0	None	-	0	Pig	6.4	pIC50	=	6.4	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		COC(=O)C[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm00021a021
	44279300	113310	0	None	-	0	Pig	5.4	pIC50	=	5.4	Binding	Binding affinity against ETA receptor in porcine aortic smooth muscle membrane was determinedBinding affinity against ETA receptor in porcine aortic smooth muscle membrane was determined	ChEMBL	472	13	5	4	2.4	CC(C)CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	CHEMBL31405	113310	0	None	-	0	Pig	5.4	pIC50	=	5.4	Binding	Binding affinity against ETA receptor in porcine aortic smooth muscle membrane was determinedBinding affinity against ETA receptor in porcine aortic smooth muscle membrane was determined	ChEMBL	472	13	5	4	2.4	CC(C)CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	44279350	174955	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor	ChEMBL	428	4	2	4	4.2	COc1cccc(-c2ccc3c(c2)C(=O)c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@H]32)c1	10.1016/0960-894X(95)00230-Q
	CHEMBL433229	174955	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor	ChEMBL	428	4	2	4	4.2	COc1cccc(-c2ccc3c(c2)C(=O)c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@H]32)c1	10.1016/0960-894X(95)00230-Q
	10390467	103903	0	None	-	0	Rat	4.4	pIC50	=	4.4	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	481	6	1	5	6.4	Cc1noc(NS(=O)(=O)c2cccc3c(N=C(c4ccccc4)c4ccccc4)cccc23)c1C	10.1021/jm00008a013
	CHEMBL26776	103903	0	None	-	0	Rat	4.4	pIC50	=	4.4	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	481	6	1	5	6.4	Cc1noc(NS(=O)(=O)c2cccc3c(N=C(c4ccccc4)c4ccccc4)cccc23)c1C	10.1021/jm00008a013
	10373814	21671	0	None	-	0	Pig	4.4	pIC50	=	4.4	Binding	Displacement of [125]ET1 from ETA receptor in pig thoracic aortaDisplacement of [125]ET1 from ETA receptor in pig thoracic aorta	ChEMBL	1016	2	6	12	7.0	O=C1NCCc2ccc(c(Br)c2)Oc2cc(ccc2O)CCNC(=O)/C(=N/O)Cc2cc(Br)c(OS(=O)(=O)O)c(c2)Oc2c(Br)cc(cc2Br)C/C1=N\O	10.1021/np50099a026
	CHEMBL1207961	21671	0	None	-	0	Pig	4.4	pIC50	=	4.4	Binding	Displacement of [125]ET1 from ETA receptor in pig thoracic aortaDisplacement of [125]ET1 from ETA receptor in pig thoracic aorta	ChEMBL	1016	2	6	12	7.0	O=C1NCCc2ccc(c(Br)c2)Oc2cc(ccc2O)CCNC(=O)/C(=N/O)Cc2cc(Br)c(OS(=O)(=O)O)c(c2)Oc2c(Br)cc(cc2Br)C/C1=N\O	10.1021/np50099a026
	CHEMBL465400	21671	0	None	-	0	Pig	4.4	pIC50	=	4.4	Binding	Displacement of [125]ET1 from ETA receptor in pig thoracic aortaDisplacement of [125]ET1 from ETA receptor in pig thoracic aorta	ChEMBL	1016	2	6	12	7.0	O=C1NCCc2ccc(c(Br)c2)Oc2cc(ccc2O)CCNC(=O)/C(=N/O)Cc2cc(Br)c(OS(=O)(=O)O)c(c2)Oc2c(Br)cc(cc2Br)C/C1=N\O	10.1021/np50099a026
	10793886	66592	0	None	-	0	Rat	4.4	pIC50	=	4.4	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	615	11	4	5	6.3	CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(Cc2ccccc2)s1	10.1021/jm950591h
	CHEMBL172760	66592	0	None	-	0	Rat	4.4	pIC50	=	4.4	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	615	11	4	5	6.3	CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(Cc2ccccc2)s1	10.1021/jm950591h
	10625083	213425	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	496	10	1	5	5.3	CCCCN(CCCC)C(=O)N1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL8925	213425	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	496	10	1	5	5.3	CCCCN(CCCC)C(=O)N1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	10833400	168673	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	376	4	1	5	3.5	Cc1cc(Cl)nnc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12	10.1021/jm9604585
	CHEMBL415106	168673	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	376	4	1	5	3.5	Cc1cc(Cl)nnc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12	10.1021/jm9604585
	11793650	104099	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	372	6	1	6	2.9	CCOc1ccc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)nn1	10.1021/jm9604585
	CHEMBL269237	104099	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	372	6	1	6	2.9	CCOc1ccc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)nn1	10.1021/jm9604585
	25211074	25257	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in membranes by radioligand assayAntagonist activity at ETA receptor (unknown origin) expressed in membranes by radioligand assay	ChEMBL	543	10	2	7	5.1	CCCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2	10.1016/j.bmcl.2017.04.049
	CHEMBL1272244	25257	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in membranes by radioligand assayAntagonist activity at ETA receptor (unknown origin) expressed in membranes by radioligand assay	ChEMBL	543	10	2	7	5.1	CCCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2	10.1016/j.bmcl.2017.04.049
	CHEMBL405599	219347	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	10767505	12072	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	494	6	1	8	3.2	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(S(C)(=O)=O)cc2)cc1	10.1021/jm9606507
	CHEMBL10661	12072	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	494	6	1	8	3.2	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(S(C)(=O)=O)cc2)cc1	10.1021/jm9606507
	10673715	16323	0	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	528	14	1	5	5.4	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCCCC(F)(F)F	10.1021/jm980217s
	CHEMBL112314	16323	0	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	528	14	1	5	5.4	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCCCC(F)(F)F	10.1021/jm980217s
	10650210	109563	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	545	9	1	9	3.5	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OCCN3CCOCC3)c2)cc1	10.1021/jm980504w
	CHEMBL305267	109563	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	545	9	1	9	3.5	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OCCN3CCOCC3)c2)cc1	10.1021/jm980504w
	10361993	106342	0	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	373	5	1	5	4.1	Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C(C)C)cccc23)c1C	10.1021/jm00004a012
	CHEMBL283652	106342	0	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	373	5	1	5	4.1	Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C(C)C)cccc23)c1C	10.1021/jm00004a012
	44304492	103335	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells	ChEMBL	949	23	9	8	4.3	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm970161m
	CHEMBL262993	103335	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells	ChEMBL	949	23	9	8	4.3	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm970161m
	CHEMBL133257	215494	0	None	-	0	Pig	8.4	pIC50	=	8.4	Binding	Inhibitory effect against porcine ET-A receptorInhibitory effect against porcine ET-A receptor	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C2CCCC2)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	44311232	210886	0	None	-	1	Human	8.4	pIC50	=	8.4	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	658	13	2	13	5.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ncccn2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	CHEMBL70293	210886	0	None	-	1	Human	8.4	pIC50	=	8.4	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	658	13	2	13	5.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ncccn2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	44311233	210888	0	None	-	1	Human	8.4	pIC50	=	8.4	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	630	12	2	13	4.3	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2ncccn2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	CHEMBL70303	210888	0	None	-	1	Human	8.4	pIC50	=	8.4	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	630	12	2	13	4.3	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2ncccn2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	CHEMBL133257	215494	0	None	-	0	Pig	8.4	pIC50	=	8.4	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C2CCCC2)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	10961277	107794	0	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	446	5	2	6	4.9	CC(C)Oc1ccc2c(c1)C(c1ccc(O)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	CHEMBL294496	107794	0	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	446	5	2	6	4.9	CC(C)Oc1ccc2c(c1)C(c1ccc(O)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	10391968	195213	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	521	10	2	8	3.9	CCOc1ccc2c(c1)[C@H](c1ccc(OC)cc1OCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	CHEMBL50232	195213	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	521	10	2	8	3.9	CCOc1ccc2c(c1)[C@H](c1ccc(OC)cc1OCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	25211074	25257	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	543	10	2	7	5.1	CCCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2	10.1016/j.bmcl.2017.04.049
	CHEMBL1272244	25257	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	543	10	2	7	5.1	CCCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2	10.1016/j.bmcl.2017.04.049
	11058717	209595	0	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	412	8	1	6	4.6	CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OCC)cc21	10.1021/jm010382z
	CHEMBL62348	209595	0	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	412	8	1	6	4.6	CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OCC)cc21	10.1021/jm010382z
	9807200	92120	0	None	346	2	Human	8.4	pIC50	=	8.4	Binding	Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells	ChEMBL	536	7	2	8	3.6	COc1cc(C)ccc1S(=O)(=O)NC(=O)[C@@H](c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(=O)O)ccc12	10.1007/s00044-004-0021-y
	CHEMBL2261359	92120	0	None	346	2	Human	8.4	pIC50	=	8.4	Binding	Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells	ChEMBL	536	7	2	8	3.6	COc1cc(C)ccc1S(=O)(=O)NC(=O)[C@@H](c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(=O)O)ccc12	10.1007/s00044-004-0021-y
	71451528	88464	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)	ChEMBL	631	14	1	12	4.3	CCCCS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC	10.1016/j.bmcl.2016.06.014
	CHEMBL2163715	88464	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)	ChEMBL	631	14	1	12	4.3	CCCCS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC	10.1016/j.bmcl.2016.06.014
	21041249	88437	1	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	648	11	1	8	4.7	CN(Cc1ccccc1)S(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1	10.1021/jm3009103
	CHEMBL2163688	88437	1	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	648	11	1	8	4.7	CN(Cc1ccccc1)S(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1	10.1021/jm3009103
	71451525	88446	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	629	12	1	12	5.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCOc1ncccn1	10.1021/jm3009103
	CHEMBL2163697	88446	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	629	12	1	12	5.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCOc1ncccn1	10.1021/jm3009103
	71451528	88464	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	631	14	1	12	4.3	CCCCS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC	10.1021/jm3009103
	CHEMBL2163715	88464	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	631	14	1	12	4.3	CCCCS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC	10.1021/jm3009103
	11059576	210072	0	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	460	7	1	6	5.2	CCCOc1ccc2c(c1)C(c1ccc(OC)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	CHEMBL64726	210072	0	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	460	7	1	6	5.2	CCCOc1ccc2c(c1)C(c1ccc(OC)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	21041266	88787	1	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	584	10	2	8	3.3	O=S(=O)(Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1)NC1CC1	10.1021/jm3009103
	CHEMBL2165340	88787	1	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	584	10	2	8	3.3	O=S(=O)(Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1)NC1CC1	10.1021/jm3009103
	10625633	213918	0	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	514	12	1	8	2.4	COCCN(CCOC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL9223	213918	0	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	514	12	1	8	2.4	COCCN(CCOC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	10697636	174599	0	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	536	13	1	7	4.9	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1SCCS1	10.1021/jm980217s
	CHEMBL430683	174599	0	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	536	13	1	7	4.9	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1SCCS1	10.1021/jm980217s
	10279940	108128	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	527	8	2	10	3.6	CC(=O)OCCc1cc2c(cc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2	10.1021/jm9608366
	CHEMBL296927	108128	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	527	8	2	10	3.6	CC(=O)OCCc1cc2c(cc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2	10.1021/jm9608366
	44333578	11377	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	417	5	1	5	4.4	CCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(02)00663-7
	CHEMBL102773	11377	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	417	5	1	5	4.4	CCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(02)00663-7
	44439111	103951	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Displacement of [125I]ET1 from human ETA receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETA receptor expressed in CHO cells	ChEMBL	979	31	2	15	7.0	CC(=O)CC(=O)CCc1ccc(NC(=O)CCOCCOCCOCCOCCOc2ccc(CC(=O)N(C)Cc3cc(-c4ncco4)ccc3-c3ccccc3S(=O)(=O)Nc3ccno3)cc2)cc1	10.1016/j.bmcl.2006.10.009
	CHEMBL268201	103951	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Displacement of [125I]ET1 from human ETA receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETA receptor expressed in CHO cells	ChEMBL	979	31	2	15	7.0	CC(=O)CC(=O)CCc1ccc(NC(=O)CCOCCOCCOCCOCCOc2ccc(CC(=O)N(C)Cc3cc(-c4ncco4)ccc3-c3ccccc3S(=O)(=O)Nc3ccno3)cc2)cc1	10.1016/j.bmcl.2006.10.009
	44295032	21562	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	520	10	1	9	4.7	COc1cccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)c1	10.1016/s0960-894x(98)00301-1
	CHEMBL1206717	21562	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	520	10	1	9	4.7	COc1cccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)c1	10.1016/s0960-894x(98)00301-1
	CHEMBL299572	21562	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	520	10	1	9	4.7	COc1cccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)c1	10.1016/s0960-894x(98)00301-1
	9959298	67289	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor	ChEMBL	552	10	2	7	5.4	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)OC(=O)N(C)C2CCCCC2)nc1C(=O)O	10.1021/jm9505932
	CHEMBL175698	67289	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor	ChEMBL	552	10	2	7	5.4	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)OC(=O)N(C)C2CCCCC2)nc1C(=O)O	10.1021/jm9505932
	10625530	213819	3	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	510	12	1	6	4.7	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm031041j
	CHEMBL9162	213819	3	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	510	12	1	6	4.7	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm031041j
	10625530	213819	3	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	510	12	1	6	4.7	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL9162	213819	3	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	510	12	1	6	4.7	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	10917653	210156	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	468	11	1	6	6.1	CCCCCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	CHEMBL65292	210156	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	468	11	1	6	6.1	CCCCCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	104865	7493	99	None	1	4	Human	8.3	pIC50	=	8.3	Binding	Binding affinity to human ETA receptorBinding affinity to human ETA receptor	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/j.ejmech.2016.06.006
	3494	7493	99	None	1	4	Human	8.3	pIC50	=	8.3	Binding	Binding affinity to human ETA receptorBinding affinity to human ETA receptor	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/j.ejmech.2016.06.006
	392	7493	99	None	1	4	Human	8.3	pIC50	=	8.3	Binding	Binding affinity to human ETA receptorBinding affinity to human ETA receptor	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/j.ejmech.2016.06.006
	CHEMBL957	7493	99	None	1	4	Human	8.3	pIC50	=	8.3	Binding	Binding affinity to human ETA receptorBinding affinity to human ETA receptor	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/j.ejmech.2016.06.006
	DB00559	7493	99	None	1	4	Human	8.3	pIC50	=	8.3	Binding	Binding affinity to human ETA receptorBinding affinity to human ETA receptor	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/j.ejmech.2016.06.006
	104865	7493	99	None	-1	4	Rat	8.3	pIC50	=	8.3	Binding	Displacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry method	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/j.bmc.2015.01.003
	3494	7493	99	None	-1	4	Rat	8.3	pIC50	=	8.3	Binding	Displacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry method	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/j.bmc.2015.01.003
	392	7493	99	None	-1	4	Rat	8.3	pIC50	=	8.3	Binding	Displacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry method	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/j.bmc.2015.01.003
	CHEMBL957	7493	99	None	-1	4	Rat	8.3	pIC50	=	8.3	Binding	Displacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry method	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/j.bmc.2015.01.003
	DB00559	7493	99	None	-1	4	Rat	8.3	pIC50	=	8.3	Binding	Displacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry method	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/j.bmc.2015.01.003
	17885921	113578	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	453	6	1	6	5.2	O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccn2)nn1CC1CCCCC1	10.1016/s0960-894x(00)00513-8
	CHEMBL314454	113578	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	453	6	1	6	5.2	O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccn2)nn1CC1CCCCC1	10.1016/s0960-894x(00)00513-8
	11798504	103898	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	468	9	1	6	3.5	CCCCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL267695	103898	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	468	9	1	6	3.5	CCCCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	10648135	16114	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	472	13	1	5	4.7	C/C=C/CC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC	10.1021/jm980217s
	CHEMBL111218	16114	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	472	13	1	5	4.7	C/C=C/CC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC	10.1021/jm980217s
	44314581	111654	0	None	-	0	Pig	8.3	pIC50	=	8.3	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	591	11	6	5	2.8	Cc1[nH]c2ccccc2c1C[C@@H](NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)NC(Cc1c[nH]cn1)C(=O)O	10.1021/jm9600914
	CHEMBL311134	111654	0	None	-	0	Pig	8.3	pIC50	=	8.3	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	591	11	6	5	2.8	Cc1[nH]c2ccccc2c1C[C@@H](NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)NC(Cc1c[nH]cn1)C(=O)O	10.1021/jm9600914
	11798504	103898	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Radioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cells	ChEMBL	468	9	1	6	3.5	CCCCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL267695	103898	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Radioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cells	ChEMBL	468	9	1	6	3.5	CCCCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	11113473	210148	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	472	6	1	5	6.3	CC(C)Oc1ccc2c(c1)C(c1ccc(C(C)C)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	CHEMBL65201	210148	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	472	6	1	5	6.3	CC(C)Oc1ccc2c(c1)C(c1ccc(C(C)C)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	CHEMBL2304006	216241	0	None	-	0	Pig	8.3	pIC50	=	8.3	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		O=C(O)C[C@H]1NC(=O)[C@H](Cc2c(Br)[nH]c3ccccc23)NC(=O)[C@@H](C2CC2)NC(=O)[C@H](C2CCCC2)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm9600914
	44320419	113851	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	496	7	2	6	5.1	O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1CC1CCC(C(=O)O)CC1	10.1016/s0960-894x(00)00513-8
	CHEMBL315805	113851	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	496	7	2	6	5.1	O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1CC1CCC(C(=O)O)CC1	10.1016/s0960-894x(00)00513-8
	10576428	21359	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells	ChEMBL	473	8	2	6	4.3	COc1ccc(C(=O)/C(Cc2ccc(NC(C)=O)cc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1	10.1021/jm9606507
	CHEMBL10905	21359	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells	ChEMBL	473	8	2	6	4.3	COc1ccc(C(=O)/C(Cc2ccc(NC(C)=O)cc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1	10.1021/jm9606507
	CHEMBL1204673	21359	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells	ChEMBL	473	8	2	6	4.3	COc1ccc(C(=O)/C(Cc2ccc(NC(C)=O)cc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1	10.1021/jm9606507
	CHEMBL328942	218095	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	18617318	112390	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	394	3	1	4	3.3	Cc1noc(NS(=O)(=O)c2ccccc2Br)c1Br	10.1016/0960-894X(96)00441-6
	CHEMBL312266	112390	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	394	3	1	4	3.3	Cc1noc(NS(=O)(=O)c2ccccc2Br)c1Br	10.1016/0960-894X(96)00441-6
	10526002	14823	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	417	5	1	7	3.2	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccnc2)cc1	10.1021/jm9606507
	CHEMBL10910	14823	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	417	5	1	7	3.2	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccnc2)cc1	10.1021/jm9606507
	CHEMBL2304018	216253	0	None	-	0	Pig	7.4	pIC50	=	7.4	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc2c(Cl)[nH]c3ccccc23)NC(=O)[C@@H](C(C)C)NC1=O	10.1021/jm9600914
	18004820	23225	0	None	-	1	Human	7.4	pIC50	=	7.4	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	527	9	2	7	4.7	CCCc1nc(Cl)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	CHEMBL12333	23225	0	None	-	1	Human	7.4	pIC50	=	7.4	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	527	9	2	7	4.7	CCCc1nc(Cl)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	71456865	88477	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	632	14	2	11	3.7	COc1nc(NS(=O)(=O)NCc2ccccc2)c(Oc2ccccc2OC)c(OCCOc2ncc(Br)cn2)n1	10.1021/jm3009103
	CHEMBL2163727	88477	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	632	14	2	11	3.7	COc1nc(NS(=O)(=O)NCc2ccccc2)c(Oc2ccccc2OC)c(OCCOc2ncc(Br)cn2)n1	10.1021/jm3009103
	10504148	214038	0	None	-	0	Rat	7.4	pIC50	=	7.4	Binding	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	ChEMBL	459	10	1	5	6.7	Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1-c1ccccn1	10.1021/jm9707131
	CHEMBL92965	214038	0	None	-	0	Rat	7.4	pIC50	=	7.4	Binding	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	ChEMBL	459	10	1	5	6.7	Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1-c1ccccn1	10.1021/jm9707131
	104865	7493	99	None	1	4	Human	7.4	pIC50	=	7.4	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/s0960-894x(02)01084-3
	3494	7493	99	None	1	4	Human	7.4	pIC50	=	7.4	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/s0960-894x(02)01084-3
	392	7493	99	None	1	4	Human	7.4	pIC50	=	7.4	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/s0960-894x(02)01084-3
	CHEMBL957	7493	99	None	1	4	Human	7.4	pIC50	=	7.4	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/s0960-894x(02)01084-3
	DB00559	7493	99	None	1	4	Human	7.4	pIC50	=	7.4	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/s0960-894x(02)01084-3
	CHEMBL2369709	216431	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Inhibition of [125I]endothelin-1 [ET-1] binding to endothelin A receptor (ETA) of rabbit renal artery vascular smooth muscle cellsInhibition of [125I]endothelin-1 [ET-1] binding to endothelin A receptor (ETA) of rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/0960-894X(95)00152-J
	CHEMBL405100	219322	0	None	-	0	Pig	7.4	pIC50	=	7.4	Binding	Inhibition of endothelin (ET-A) binding to porcine heart membranes Inhibition of endothelin (ET-A) binding to porcine heart membranes	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/0960-894X(95)00349-X
	CHEMBL438820	220579	0	None	-	0	Pig	7.4	pIC50	=	7.4	Binding	Inhibition of endothelin (ET-A) binding to porcine heart membranes Inhibition of endothelin (ET-A) binding to porcine heart membranes	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/0960-894X(95)00349-X
	10002033	107789	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	417	7	2	7	3.6	CCOC(=O)C(C)Nc1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12	10.1021/jm00008a013
	CHEMBL29448	107789	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	417	7	2	7	3.6	CCOC(=O)C(C)Nc1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12	10.1021/jm00008a013
	10718141	11995	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	444	5	1	7	3.6	COC(=O)c1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1	10.1021/jm9606507
	CHEMBL10622	11995	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	444	5	1	7	3.6	COC(=O)c1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1	10.1021/jm9606507
	10027018	105265	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	454	4	1	5	5.1	O=C1OC(O)(c2ccc(Cl)c(Cl)c2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2	10.1021/jm9606507
	CHEMBL275991	105265	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	454	4	1	5	5.1	O=C1OC(O)(c2ccc(Cl)c(Cl)c2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2	10.1021/jm9606507
	44279413	106728	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor	ChEMBL	400	2	2	3	3.3	O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(Br)cc21	10.1016/0960-894X(95)00230-Q
	CHEMBL286395	106728	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor	ChEMBL	400	2	2	3	3.3	O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(Br)cc21	10.1016/0960-894X(95)00230-Q
	10716071	214095	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	401	7	1	5	5.4	O=[N+]([O-])c1ccc(OCc2ccsc2)cc1/C=C(/CO)c1ccccc1Cl	10.1021/jm970847e
	CHEMBL93411	214095	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	401	7	1	5	5.4	O=[N+]([O-])c1ccc(OCc2ccsc2)cc1/C=C(/CO)c1ccccc1Cl	10.1021/jm970847e
	44298330	108325	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	518	10	1	8	5.4	COC(=O)CCCc1onc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Sc1cccc(OC)c1	10.1016/s0960-894x(00)00366-8
	CHEMBL298340	108325	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	518	10	1	8	5.4	COC(=O)CCCc1onc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Sc1cccc(OC)c1	10.1016/s0960-894x(00)00366-8
	CHEMBL85341	222667	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Inhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cellsInhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00095a029
	10792782	138142	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	551	10	4	6	5.0	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCCC2)nc1C(=O)O	10.1021/jm950592+
	CHEMBL368847	138142	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	551	10	4	6	5.0	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCCC2)nc1C(=O)O	10.1021/jm950592+
	CHEMBL147510	215557	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	The inhibitory constant was evaluated against Endothelin A receptorThe inhibitory constant was evaluated against Endothelin A receptor	ChEMBL		None	None	None		CC[C@@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCN)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@H](C)CC	10.1016/S0960-894X(01)81219-1
	10087191	108614	1	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells	ChEMBL	317	3	2	5	2.8	Cc1noc(NS(=O)(=O)c2cccc3c(N)cccc23)c1C	10.1021/jm00029a001
	CHEMBL30039	108614	1	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells	ChEMBL	317	3	2	5	2.8	Cc1noc(NS(=O)(=O)c2cccc3c(N)cccc23)c1C	10.1021/jm00029a001
	10087191	108614	1	None	-	0	Rat	5.4	pIC50	=	5.4	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	317	3	2	5	2.8	Cc1noc(NS(=O)(=O)c2cccc3c(N)cccc23)c1C	10.1021/jm00008a013
	CHEMBL30039	108614	1	None	-	0	Rat	5.4	pIC50	=	5.4	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	317	3	2	5	2.8	Cc1noc(NS(=O)(=O)c2cccc3c(N)cccc23)c1C	10.1021/jm00008a013
	5329	176255	119	None	-	0	Rat	5.4	pIC50	=	5.4	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	253	3	2	5	1.4	Cc1cc(NS(=O)(=O)c2ccc(N)cc2)no1	10.1021/jm00008a013
	CHEMBL443	176255	119	None	-	0	Rat	5.4	pIC50	=	5.4	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	253	3	2	5	1.4	Cc1cc(NS(=O)(=O)c2ccc(N)cc2)no1	10.1021/jm00008a013
	CHEMBL405709	219355	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1021/jm00015a003
	5329	176255	119	None	-	0	Rat	5.4	pIC50	=	5.4	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	253	3	2	5	1.4	Cc1cc(NS(=O)(=O)c2ccc(N)cc2)no1	10.1021/jm00004a012
	CHEMBL443	176255	119	None	-	0	Rat	5.4	pIC50	=	5.4	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	253	3	2	5	1.4	Cc1cc(NS(=O)(=O)c2ccc(N)cc2)no1	10.1021/jm00004a012
	44327619	214217	0	None	-	0	Rat	5.4	pIC50	=	5.4	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	511	6	1	8	3.5	CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)n2nc(C(C)(C)C)ccc2=O)cc1	10.1016/S0960-894X(96)00617-8
	CHEMBL94102	214217	0	None	-	0	Rat	5.4	pIC50	=	5.4	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	511	6	1	8	3.5	CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)n2nc(C(C)(C)C)ccc2=O)cc1	10.1016/S0960-894X(96)00617-8
	44327714	214718	0	None	-	0	Rat	5.4	pIC50	=	5.4	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	575	8	1	9	4.2	COc1ccc(-c2cc(C)c(=O)n(C(C(=O)NS(=O)(=O)c3ccc(C(C)C)cc3)c3ccc4c(c3)OCO4)n2)cc1	10.1016/S0960-894X(96)00617-8
	CHEMBL96935	214718	0	None	-	0	Rat	5.4	pIC50	=	5.4	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	575	8	1	9	4.2	COc1ccc(-c2cc(C)c(=O)n(C(C(=O)NS(=O)(=O)c3ccc(C(C)C)cc3)c3ccc4c(c3)OCO4)n2)cc1	10.1016/S0960-894X(96)00617-8
	182140	195876	32	None	-	0	Human	4.4	pIC50	=	4.4	Binding	Displacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cellsDisplacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cells	ChEMBL	430	8	0	7	3.7	COC[C@@H]1Cc2cc(OC)c3c(c2[C@H](c2ccc(OC)c(OC)c2)[C@H]1COC)OCO3	10.1021/np50124a006
	CHEMBL510130	195876	32	None	-	0	Human	4.4	pIC50	=	4.4	Binding	Displacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cellsDisplacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cells	ChEMBL	430	8	0	7	3.7	COC[C@@H]1Cc2cc(OC)c3c(c2[C@H](c2ccc(OC)c(OC)c2)[C@H]1COC)OCO3	10.1021/np50124a006
	44277130	106230	0	None	-	0	Rat	4.4	pIC50	=	4.4	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	450	8	1	7	3.6	COc1cccc(Cn2nc(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2OCCO)c1	10.1016/s0960-894x(00)00232-8
	CHEMBL283037	106230	0	None	-	0	Rat	4.4	pIC50	=	4.4	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	450	8	1	7	3.6	COc1cccc(Cn2nc(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2OCCO)c1	10.1016/s0960-894x(00)00232-8
	44277131	113612	0	None	-	0	Rat	4.4	pIC50	=	4.4	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	380	5	1	3	4.0	COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc(F)cc3)c2=O)c1	10.1016/s0960-894x(00)00232-8
	CHEMBL3144603	113612	0	None	-	0	Rat	4.4	pIC50	=	4.4	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	380	5	1	3	4.0	COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc(F)cc3)c2=O)c1	10.1016/s0960-894x(00)00232-8
	44357135	123025	0	None	-	0	Pig	4.4	pIC50	=	4.4	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL	642	10	6	8	-0.1	CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)c2ccccc2NC=O)NC1=O	10.1021/jm00021a021
	CHEMBL335863	123025	0	None	-	0	Pig	4.4	pIC50	=	4.4	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL	642	10	6	8	-0.1	CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)c2ccccc2NC=O)NC1=O	10.1021/jm00021a021
	10814222	16324	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	470	10	1	6	3.4	CCCN(C)C(=O)CN1C[C@H](c2ccc(OC)cc2OC)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	CHEMBL112325	16324	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	470	10	1	6	3.4	CCCN(C)C(=O)CN1C[C@H](c2ccc(OC)cc2OC)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	18995992	106614	0	None	-	1	Human	7.4	pIC50	=	7.4	Binding	Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.	ChEMBL	507	7	1	9	5.0	COc1ccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc4c(cc23)OCO4)cc1OC	10.1016/0960-894X(96)00232-6
	CHEMBL28563	106614	0	None	-	1	Human	7.4	pIC50	=	7.4	Binding	Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.	ChEMBL	507	7	1	9	5.0	COc1ccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc4c(cc23)OCO4)cc1OC	10.1016/0960-894X(96)00232-6
	44339755	16551	0	None	-	0	Rat	7.4	pIC50	=	7.4	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	551	12	1	7	2.7	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CN1CCCCS1(=O)=O	10.1021/jm980217s
	CHEMBL113589	16551	0	None	-	0	Rat	7.4	pIC50	=	7.4	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	551	12	1	7	2.7	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CN1CCCCS1(=O)=O	10.1021/jm980217s
	10763680	127560	0	None	-	0	Rat	7.4	pIC50	=	7.4	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	403	7	1	6	4.1	N#Cc1ccc(OCc2ccc3c(c2)OCO3)cc1OC(C(=O)O)c1ccccc1	10.1021/jm990378b
	CHEMBL355413	127560	0	None	-	0	Rat	7.4	pIC50	=	7.4	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	403	7	1	6	4.1	N#Cc1ccc(OCc2ccc3c(c2)OCO3)cc1OC(C(=O)O)c1ccccc1	10.1021/jm990378b
	9894460	213488	9	None	-24	3	Rat	7.4	pIC50	=	7.4	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	539	10	2	7	4.8	CCCc1cc(C(=O)O)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2	10.1016/S0960-894X(96)00617-8
	CHEMBL313871	213488	9	None	-24	3	Rat	7.4	pIC50	=	7.4	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	539	10	2	7	4.8	CCCc1cc(C(=O)O)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2	10.1016/S0960-894X(96)00617-8
	CHEMBL8978	213488	9	None	-24	3	Rat	7.4	pIC50	=	7.4	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	539	10	2	7	4.8	CCCc1cc(C(=O)O)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2	10.1016/S0960-894X(96)00617-8
	10554410	127160	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor	ChEMBL	538	10	3	7	5.0	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)OC2CCCCC2)nc1C(=O)O	10.1021/jm9505932
	CHEMBL353320	127160	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor	ChEMBL	538	10	3	7	5.0	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)OC2CCCCC2)nc1C(=O)O	10.1021/jm9505932
	10916597	210094	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	410	7	1	5	5.4	CCCCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm031041j
	CHEMBL64832	210094	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	410	7	1	5	5.4	CCCCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm031041j
	CHEMBL304756	217754	0	None	-	0	Pig	6.4	pIC50	=	6.4	Binding	Binding activity against Endothelin A receptor of Porcine aortic smooth muscle membranesBinding activity against Endothelin A receptor of Porcine aortic smooth muscle membranes	ChEMBL		None	None	None		CC(C)C[C@@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00089a028
	11058658	210027	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	409	7	1	5	4.8	CCCCC1=C(C(N)=O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	CHEMBL64558	210027	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	409	7	1	5	4.8	CCCCC1=C(C(N)=O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	CHEMBL337897	218379	0	None	-	0	Pig	6.4	pIC50	=	6.4	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	4642915	104713	1	None	-	0	Rat	5.4	pIC50	=	5.4	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	402	5	3	5	4.1	Cc1noc(NS(=O)(=O)c2ccc(N/C(S)=N/c3ccccc3)cc2)c1C	10.1021/jm00008a013
	CHEMBL27256	104713	1	None	-	0	Rat	5.4	pIC50	=	5.4	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	402	5	3	5	4.1	Cc1noc(NS(=O)(=O)c2ccc(N/C(S)=N/c3ccccc3)cc2)c1C	10.1021/jm00008a013
	44213925	118481	0	None	-	0	Rat	5.4	pIC50	=	5.4	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	593	9	1	9	4.1	COc1ccc(C2=NN(C(C(=O)NS(=O)(=O)c3ccc(C(C)C)cc3)c3ccc4c(c3)OCO4)C(=O)CC2)cc1OC	10.1016/S0960-894X(96)00617-8
	CHEMBL328683	118481	0	None	-	0	Rat	5.4	pIC50	=	5.4	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	593	9	1	9	4.1	COc1ccc(C2=NN(C(C(=O)NS(=O)(=O)c3ccc(C(C)C)cc3)c3ccc4c(c3)OCO4)C(=O)CC2)cc1OC	10.1016/S0960-894X(96)00617-8
	44266532	11273	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	401	3	1	6	4.5	O=C(O)c1c(-c2ccc3c(c2)OCO3)c2ccccc2n1-c1ccc2c(c1)OCO2	10.1016/0960-894X(96)00170-9
	CHEMBL10211	11273	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	401	3	1	6	4.5	O=C(O)c1c(-c2ccc3c(c2)OCO3)c2ccccc2n1-c1ccc2c(c1)OCO2	10.1016/0960-894X(96)00170-9
	10816264	66703	0	None	-	0	Rat	4.4	pIC50	=	4.4	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	539	9	4	5	5.0	Cc1sc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O	10.1021/jm950591h
	CHEMBL173181	66703	0	None	-	0	Rat	4.4	pIC50	=	4.4	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	539	9	4	5	5.0	Cc1sc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O	10.1021/jm950591h
	10840476	138619	0	None	-	0	Rat	4.4	pIC50	=	4.4	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	553	10	4	5	5.3	CCc1sc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O	10.1021/jm950591h
	CHEMBL369420	138619	0	None	-	0	Rat	4.4	pIC50	=	4.4	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	553	10	4	5	5.3	CCc1sc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O	10.1021/jm950591h
	23445345	209839	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	378	5	1	7	3.4	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Oc2ccccc2)c1C	10.1016/S0960-894X(97)00367-3
	CHEMBL63611	209839	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	378	5	1	7	3.4	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Oc2ccccc2)c1C	10.1016/S0960-894X(97)00367-3
	10280531	169710	0	None	-	1	Human	6.4	pIC50	=	6.4	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	541	10	2	7	5.1	CCCCc1nc(Cl)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	CHEMBL417429	169710	0	None	-	1	Human	6.4	pIC50	=	6.4	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	541	10	2	7	5.1	CCCCc1nc(Cl)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	10366742	113885	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	454	6	1	5	5.5	CCCc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1	10.1016/S0960-894X(96)00496-9
	CHEMBL316012	113885	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	454	6	1	5	5.5	CCCc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1	10.1016/S0960-894X(96)00496-9
	44371410	56195	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes	ChEMBL	439	5	1	5	5.5	COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3C)c3c2oc2ccccc23)cc1	10.1016/s0960-894x(99)00040-2
	CHEMBL156453	56195	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes	ChEMBL	439	5	1	5	5.5	COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3C)c3c2oc2ccccc23)cc1	10.1016/s0960-894x(99)00040-2
	CHEMBL406279	219381	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00070a001
	44383187	66939	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.	ChEMBL	617	13	4	5	4.5	CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1cn(C)c2ccccc12)C(=O)NCc1cccc(CCC(=O)O)c1	10.1016/0960-894X(95)00144-I
	CHEMBL173974	66939	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.	ChEMBL	617	13	4	5	4.5	CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1cn(C)c2ccccc12)C(=O)NCc1cccc(CCC(=O)O)c1	10.1016/0960-894X(95)00144-I
	15296635	106331	0	None	-	0	Pig	6.4	pIC50	=	6.4	Binding	Binding affinity against ETA receptor in porcine aortic smooth muscle membraneBinding affinity against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	488	11	5	5	2.7	CC(C)C[C@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	CHEMBL283591	106331	0	None	-	0	Pig	6.4	pIC50	=	6.4	Binding	Binding affinity against ETA receptor in porcine aortic smooth muscle membraneBinding affinity against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	488	11	5	5	2.7	CC(C)C[C@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	44279516	106627	0	None	-	0	Pig	6.4	pIC50	=	6.4	Binding	Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	512	13	5	5	2.6	CC(C)C[C@H](NC(=O)Cc1cccs1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	CHEMBL285729	106627	0	None	-	0	Pig	6.4	pIC50	=	6.4	Binding	Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	512	13	5	5	2.6	CC(C)C[C@H](NC(=O)Cc1cccs1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	15340613	113621	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	414	6	1	5	4.2	COc1cccc(Cn2[nH]c(-c3ccccc3)c(Cc3ccc4c(c3)OCO4)c2=O)c1	10.1016/s0960-894x(00)00232-8
	CHEMBL3144732	113621	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	414	6	1	5	4.2	COc1cccc(Cn2[nH]c(-c3ccccc3)c(Cc3ccc4c(c3)OCO4)c2=O)c1	10.1016/s0960-894x(00)00232-8
	44317215	212042	2	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	266	3	1	4	2.4	Cc1ccc(S(=O)(=O)Nc2onc(C)c2C)cc1	10.1016/0960-894X(96)00441-6
	CHEMBL78952	212042	2	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	266	3	1	4	2.4	Cc1ccc(S(=O)(=O)Nc2onc(C)c2C)cc1	10.1016/0960-894X(96)00441-6
	10816963	120106	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	574	12	2	7	5.0	CCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC)cc1	10.1021/jm990170q
	CHEMBL331625	120106	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	574	12	2	7	5.0	CCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC)cc1	10.1021/jm990170q
	CHEMBL1791015	215694	0	None	-	0	Pig	5.4	pIC50	=	5.4	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	44368417	51423	0	None	-	0	Pig	4.4	pIC50	=	4.4	Binding	Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.	ChEMBL	504	12	2	6	4.9	COc1ccc(CN(Cc2cc(OC)c(OC)c(OC)c2)C(Cc2c[nH]c3ccccc23)C(=O)O)cc1	10.1016/s0960-894x(01)00009-9
	CHEMBL152065	51423	0	None	-	0	Pig	4.4	pIC50	=	4.4	Binding	Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.	ChEMBL	504	12	2	6	4.9	COc1ccc(CN(Cc2cc(OC)c(OC)c(OC)c2)C(Cc2c[nH]c3ccccc23)C(=O)O)cc1	10.1016/s0960-894x(01)00009-9
	10383833	106884	0	None	-	0	Rat	4.4	pIC50	=	4.4	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	359	4	2	5	3.2	CC(=O)Nc1ccc2ccc(S(=O)(=O)Nc3onc(C)c3C)cc2c1	10.1021/jm00008a013
	CHEMBL28751	106884	0	None	-	0	Rat	4.4	pIC50	=	4.4	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	359	4	2	5	3.2	CC(=O)Nc1ccc2ccc(S(=O)(=O)Nc3onc(C)c3C)cc2c1	10.1021/jm00008a013
	10383833	106884	0	None	-	0	Rat	4.4	pIC50	=	4.4	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	359	4	2	5	3.2	CC(=O)Nc1ccc2ccc(S(=O)(=O)Nc3onc(C)c3C)cc2c1	10.1021/jm00004a012
	CHEMBL28751	106884	0	None	-	0	Rat	4.4	pIC50	=	4.4	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	359	4	2	5	3.2	CC(=O)Nc1ccc2ccc(S(=O)(=O)Nc3onc(C)c3C)cc2c1	10.1021/jm00004a012
	CHEMBL265066	103590	0	None	-	0	Pig	6.4	pIC50	=	6.4	Binding	Tested for its inhibitory activity against Endothelin A receptorTested for its inhibitory activity against Endothelin A receptor	ChEMBL	646	8	2	13	5.8	COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC(=O)C2=C(C)N=C(C)/C(=C(/O)OC)[C@@H]2c2cccc([N+](=O)[O-])c2)[C@H]1c1cccc([N+](=O)[O-])c1	10.1016/S0960-894X(01)81025-8
	9913198	12092	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	484	5	1	6	4.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(C(F)(F)F)c2)cc1	10.1021/jm9606507
	CHEMBL10676	12092	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	484	5	1	6	4.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(C(F)(F)F)c2)cc1	10.1021/jm9606507
	11733450	210199	0	None	-	0	Rat	7.4	pIC50	=	7.4	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	474	6	1	7	5.0	CCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	CHEMBL65658	210199	0	None	-	0	Rat	7.4	pIC50	=	7.4	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	474	6	1	7	5.0	CCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	10502577	19176	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	426	7	1	7	3.9	COc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)cc1	10.1021/jm9700068
	CHEMBL1185771	19176	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	426	7	1	7	3.9	COc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)cc1	10.1021/jm9700068
	CHEMBL432109	19176	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	426	7	1	7	3.9	COc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)cc1	10.1021/jm9700068
	10599829	103904	0	None	-	0	Rat	7.4	pIC50	=	7.4	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	454	9	2	6	3.2	CCCCNC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL267761	103904	0	None	-	0	Rat	7.4	pIC50	=	7.4	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	454	9	2	6	3.2	CCCCNC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	44266575	11415	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	459	6	1	7	5.2	CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2-c1ccc2c(c1)OCO2	10.1016/0960-894X(96)00170-9
	CHEMBL10302	11415	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	459	6	1	7	5.2	CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2-c1ccc2c(c1)OCO2	10.1016/0960-894X(96)00170-9
	44317005	211805	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	320	3	1	4	3.4	Cc1noc(NS(=O)(=O)c2cc(Cl)cc(Cl)c2)c1C	10.1016/0960-894X(96)00441-6
	CHEMBL76949	211805	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	320	3	1	4	3.4	Cc1noc(NS(=O)(=O)c2cc(Cl)cc(Cl)c2)c1C	10.1016/0960-894X(96)00441-6
	10070783	103831	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	420	4	1	5	4.5	O=C1OC(O)(c2ccc(Cl)cc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2	10.1021/jm9606507
	CHEMBL267094	103831	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	420	4	1	5	4.5	O=C1OC(O)(c2ccc(Cl)cc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2	10.1021/jm9606507
	44298305	201367	0	None	-	0	Rat	5.4	pIC50	=	5.4	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	504	10	2	7	5.3	COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCC(=O)O)c1	10.1016/s0960-894x(00)00366-8
	CHEMBL53097	201367	0	None	-	0	Rat	5.4	pIC50	=	5.4	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	504	10	2	7	5.3	COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCC(=O)O)c1	10.1016/s0960-894x(00)00366-8
	44276948	113613	0	None	-	0	Rat	5.4	pIC50	=	5.4	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	396	5	1	3	4.5	COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc(Cl)cc3)c2=O)c1	10.1016/s0960-894x(00)00232-8
	CHEMBL3144604	113613	0	None	-	0	Rat	5.4	pIC50	=	5.4	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	396	5	1	3	4.5	COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc(Cl)cc3)c2=O)c1	10.1016/s0960-894x(00)00232-8
	9820754	115339	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells	ChEMBL	371	3	0	5	4.4	COC(=O)C(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12	10.1016/S0960-894X(96)00551-3
	CHEMBL320236	115339	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells	ChEMBL	371	3	0	5	4.4	COC(=O)C(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12	10.1016/S0960-894X(96)00551-3
	10604167	19189	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	640	10	2	6	6.4	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)(c2ccccc2)c2ccccc2)cc1	10.1021/jm990171i
	CHEMBL1185826	19189	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	640	10	2	6	6.4	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)(c2ccccc2)c2ccccc2)cc1	10.1021/jm990171i
	CHEMBL434986	19189	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	640	10	2	6	6.4	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)(c2ccccc2)c2ccccc2)cc1	10.1021/jm990171i
	10647172	213545	0	None	-	0	Rat	5.4	pIC50	=	5.4	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	449	6	1	5	4.6	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2Cc2ccc(F)cc2)cc1	10.1021/jm9505369
	CHEMBL9012	213545	0	None	-	0	Rat	5.4	pIC50	=	5.4	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	449	6	1	5	4.6	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2Cc2ccc(F)cc2)cc1	10.1021/jm9505369
	44265906	104044	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	441	9	1	6	3.9	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CCOCC(C)C)cc1	10.1021/jm9505369
	CHEMBL268902	104044	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	441	9	1	6	3.9	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CCOCC(C)C)cc1	10.1021/jm9505369
	18617377	212253	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	344	3	1	4	3.2	Cc1ccc(C)c(S(=O)(=O)Nc2onc(C)c2Br)c1	10.1016/0960-894X(96)00441-6
	CHEMBL80484	212253	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	344	3	1	4	3.2	Cc1ccc(C)c(S(=O)(=O)Nc2onc(C)c2Br)c1	10.1016/0960-894X(96)00441-6
	10668427	172123	0	None	-	0	Rat	7.4	pIC50	=	7.4	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	395	7	1	6	3.8	N#Cc1ccc(OCc2ccnnc2)cc1OC(C(=O)O)c1ccccc1Cl	10.1021/jm990378b
	CHEMBL423608	172123	0	None	-	0	Rat	7.4	pIC50	=	7.4	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	395	7	1	6	3.8	N#Cc1ccc(OCc2ccnnc2)cc1OC(C(=O)O)c1ccccc1Cl	10.1021/jm990378b
	10765750	169938	0	None	-	0	Rat	7.4	pIC50	=	7.4	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	445	8	1	6	3.0	CC[S+]([O-])CCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL417972	169938	0	None	-	0	Rat	7.4	pIC50	=	7.4	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	445	8	1	6	3.0	CC[S+]([O-])CCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	44383753	66840	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	466	5	1	5	5.7	Cc1cc(C)c(/C=C/c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1	10.1016/S0960-894X(97)00133-9
	CHEMBL173761	66840	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	466	5	1	5	5.7	Cc1cc(C)c(/C=C/c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1	10.1016/S0960-894X(97)00133-9
	44439105	175489	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]ET1 from human ETA receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETA receptor expressed in CHO cells	ChEMBL	848	26	2	12	6.5	CC(=O)CC(=O)CCc1ccc(NC(=O)CCOCCOCCOCCOc2ccc(-c3ccccc3S(=O)(=O)Nc3ccno3)c(CN(C)C(=O)CC(C)(C)C)c2)cc1	10.1016/j.bmcl.2006.10.009
	CHEMBL436821	175489	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]ET1 from human ETA receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETA receptor expressed in CHO cells	ChEMBL	848	26	2	12	6.5	CC(=O)CC(=O)CCc1ccc(NC(=O)CCOCCOCCOCCOc2ccc(-c3ccccc3S(=O)(=O)Nc3ccno3)c(CN(C)C(=O)CC(C)(C)C)c2)cc1	10.1016/j.bmcl.2006.10.009
	10357554	104340	1	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	302	3	1	4	3.2	Cc1noc(NS(=O)(=O)c2cccc3ccccc23)c1C	10.1016/0960-894X(96)00441-6
	CHEMBL27065	104340	1	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	302	3	1	4	3.2	Cc1noc(NS(=O)(=O)c2cccc3ccccc23)c1C	10.1016/0960-894X(96)00441-6
	10972369	174847	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	448	6	3	6	4.9	COc1ccc(C2=C(C(=O)O)C(c3ccc(O)c(O)c3)Oc3ccc(OC(C)C)cc32)cc1	10.1021/jm010382z
	CHEMBL432489	174847	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	448	6	3	6	4.9	COc1ccc(C2=C(C(=O)O)C(c3ccc(O)c(O)c3)Oc3ccc(OC(C)C)cc32)cc1	10.1021/jm010382z
	11801544	68551	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	589	10	4	6	5.1	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2C3CC4CC(C3)CC2C4)nc1C(=O)O	10.1021/jm950592+
	CHEMBL177261	68551	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	589	10	4	6	5.1	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2C3CC4CC(C3)CC2C4)nc1C(=O)O	10.1021/jm950592+
	CHEMBL135907	215514	0	None	-	0	Pig	6.4	pIC50	=	6.4	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@@H]1NC(=O)[C@@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC1=O	10.1021/jm00021a021
	23445562	107392	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	398	5	1	7	3.7	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Oc2ccccc2)c1Cl	10.1016/S0960-894X(97)00367-3
	CHEMBL291891	107392	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	398	5	1	7	3.7	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Oc2ccccc2)c1Cl	10.1016/S0960-894X(97)00367-3
	CHEMBL438194	220532	14	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Inhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cellsInhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00095a029
	CHEMBL34540	218487	14	None	-	0	Rat	4.4	pIC50	=	4.4	Binding	Compound was evaluated for the binding affinity to endothelin receptor in the rat heart ventricle.Compound was evaluated for the binding affinity to endothelin receptor in the rat heart ventricle.	ChEMBL		None	None	None		None	10.1021/jm00087a001
	104865	7493	99	None	1	4	Human	7.4	pIC50	=	7.4	Binding	Antagonist activity at ET-A receptor (unknown origin)Antagonist activity at ET-A receptor (unknown origin)	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/acs.jmedchem.5b01781
	3494	7493	99	None	1	4	Human	7.4	pIC50	=	7.4	Binding	Antagonist activity at ET-A receptor (unknown origin)Antagonist activity at ET-A receptor (unknown origin)	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/acs.jmedchem.5b01781
	392	7493	99	None	1	4	Human	7.4	pIC50	=	7.4	Binding	Antagonist activity at ET-A receptor (unknown origin)Antagonist activity at ET-A receptor (unknown origin)	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/acs.jmedchem.5b01781
	CHEMBL957	7493	99	None	1	4	Human	7.4	pIC50	=	7.4	Binding	Antagonist activity at ET-A receptor (unknown origin)Antagonist activity at ET-A receptor (unknown origin)	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/acs.jmedchem.5b01781
	DB00559	7493	99	None	1	4	Human	7.4	pIC50	=	7.4	Binding	Antagonist activity at ET-A receptor (unknown origin)Antagonist activity at ET-A receptor (unknown origin)	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/acs.jmedchem.5b01781
	10839947	124080	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	530	9	2	6	5.0	CCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm990170q
	CHEMBL339657	124080	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	530	9	2	6	5.0	CCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm990170q
	104865	7493	99	None	1	4	Human	7.4	pIC50	=	7.4	Binding	Displacement of 125I-ET1 from human smooth muscle ETA receptorDisplacement of 125I-ET1 from human smooth muscle ETA receptor	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/j.bmcl.2016.06.014
	3494	7493	99	None	1	4	Human	7.4	pIC50	=	7.4	Binding	Displacement of 125I-ET1 from human smooth muscle ETA receptorDisplacement of 125I-ET1 from human smooth muscle ETA receptor	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/j.bmcl.2016.06.014
	392	7493	99	None	1	4	Human	7.4	pIC50	=	7.4	Binding	Displacement of 125I-ET1 from human smooth muscle ETA receptorDisplacement of 125I-ET1 from human smooth muscle ETA receptor	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/j.bmcl.2016.06.014
	CHEMBL957	7493	99	None	1	4	Human	7.4	pIC50	=	7.4	Binding	Displacement of 125I-ET1 from human smooth muscle ETA receptorDisplacement of 125I-ET1 from human smooth muscle ETA receptor	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/j.bmcl.2016.06.014
	DB00559	7493	99	None	1	4	Human	7.4	pIC50	=	7.4	Binding	Displacement of 125I-ET1 from human smooth muscle ETA receptorDisplacement of 125I-ET1 from human smooth muscle ETA receptor	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/j.bmcl.2016.06.014
	104865	7493	99	None	1	4	Human	7.4	pIC50	=	7.4	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm3009103
	3494	7493	99	None	1	4	Human	7.4	pIC50	=	7.4	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm3009103
	392	7493	99	None	1	4	Human	7.4	pIC50	=	7.4	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm3009103
	CHEMBL957	7493	99	None	1	4	Human	7.4	pIC50	=	7.4	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm3009103
	DB00559	7493	99	None	1	4	Human	7.4	pIC50	=	7.4	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm3009103
	10741025	188460	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	424	6	1	6	4.5	Cc1cc(C)cc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c1	10.1021/jm9700068
	CHEMBL47765	188460	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	424	6	1	6	4.5	Cc1cc(C)cc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c1	10.1021/jm9700068
	CHEMBL347948	218493	0	None	-	0	Mouse	7.4	pIC50	=	7.4	Binding	Inhibition of [125I]ET1 binding to Endothelin A receptor of murine 3T3 cellsInhibition of [125I]ET1 binding to Endothelin A receptor of murine 3T3 cells	ChEMBL		None	None	None		CC[C@H](C)[C@@H](NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)81219-1
	18184234	68983	0	None	-	2	Human	7.4	pIC50	=	7.4	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	605	15	2	10	4.2	CCS(=O)(=O)NCCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	CHEMBL177802	68983	0	None	-	2	Human	7.4	pIC50	=	7.4	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	605	15	2	10	4.2	CCS(=O)(=O)NCCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	10599230	213774	0	None	-	0	Rat	7.3	pIC50	=	7.3	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	440	8	2	6	2.8	CCCNC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm031041j
	CHEMBL9141	213774	0	None	-	0	Rat	7.3	pIC50	=	7.3	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	440	8	2	6	2.8	CCCNC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm031041j
	10599230	213774	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Radioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cells	ChEMBL	440	8	2	6	2.8	CCCNC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL9141	213774	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Radioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cells	ChEMBL	440	8	2	6	2.8	CCCNC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	11767189	16730	0	None	-	0	Pig	7.3	pIC50	=	7.3	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	601	11	1	10	5.8	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2cnc3ccccc3n2)c1	10.1021/jm0102304
	CHEMBL114704	16730	0	None	-	0	Pig	7.3	pIC50	=	7.3	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	601	11	1	10	5.8	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2cnc3ccccc3n2)c1	10.1021/jm0102304
	10793053	18230	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	564	9	2	6	5.2	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)c2ccccc2)cc1	10.1021/jm990171i
	CHEMBL1180363	18230	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	564	9	2	6	5.2	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)c2ccccc2)cc1	10.1021/jm990171i
	CHEMBL123994	18230	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	564	9	2	6	5.2	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)c2ccccc2)cc1	10.1021/jm990171i
	15340617	106013	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	464	8	1	7	3.7	COc1cccc(Cn2nc(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2OCC(=O)O)c1	10.1016/s0960-894x(00)00232-8
	CHEMBL281677	106013	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	464	8	1	7	3.7	COc1cccc(Cn2nc(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2OCC(=O)O)c1	10.1016/s0960-894x(00)00232-8
	44386621	68051	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	549	10	4	6	4.5	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CC3CCC2C3)nc1C(=O)O	10.1021/jm950592+
	CHEMBL176653	68051	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	549	10	4	6	4.5	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CC3CCC2C3)nc1C(=O)O	10.1021/jm950592+
	10650331	139350	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor	ChEMBL	551	10	3	6	5.0	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)N(C)C(=O)NC2CCCCC2)nc1C(=O)O	10.1021/jm9505932
	CHEMBL369821	139350	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor	ChEMBL	551	10	3	6	5.0	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)N(C)C(=O)NC2CCCCC2)nc1C(=O)O	10.1021/jm9505932
	56678451	70100	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells	ChEMBL	937	25	8	8	4.5	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C(c1ccccc1)c1ccccc1)N(C)C(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm970161m
	CHEMBL1793927	70100	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells	ChEMBL	937	25	8	8	4.5	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C(c1ccccc1)c1ccccc1)N(C)C(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm970161m
	10205429	68380	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	470	8	2	9	2.5	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(C)nc1OCC#CCO	10.1016/s0960-894x(02)01084-3
	CHEMBL177111	68380	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	470	8	2	9	2.5	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(C)nc1OCC#CCO	10.1016/s0960-894x(02)01084-3
	71458717	88445	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	433	9	2	10	1.5	COc1ccccc1Oc1c(NS(C)(=O)=O)nc(-c2ncccn2)nc1OCCO	10.1021/jm3009103
	CHEMBL2163696	88445	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	433	9	2	10	1.5	COc1ccccc1Oc1c(NS(C)(=O)=O)nc(-c2ncccn2)nc1OCCO	10.1021/jm3009103
	10598840	67268	0	None	-	0	Rat	7.3	pIC50	=	7.3	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	432	9	1	5	4.7	COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2cc(OC)cc(OC)c2)cc1	10.1021/jm031041j
	CHEMBL175545	67268	0	None	-	0	Rat	7.3	pIC50	=	7.3	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	432	9	1	5	4.7	COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2cc(OC)cc(OC)c2)cc1	10.1021/jm031041j
	10670372	104022	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	432	7	1	6	4.1	COc1ccc(C2(O)OC(=O)C(c3cc(OC)cc(OC)c3)=C2Cc2ccccc2)cc1	10.1021/jm9606507
	CHEMBL268754	104022	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	432	7	1	6	4.1	COc1ccc(C2(O)OC(=O)C(c3cc(OC)cc(OC)c3)=C2Cc2ccccc2)cc1	10.1021/jm9606507
	44314664	211475	0	None	-	0	Pig	7.3	pIC50	=	7.3	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	615	12	5	4	5.1	CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CCCC1)C(=O)O	10.1021/jm9600914
	CHEMBL74000	211475	0	None	-	0	Pig	7.3	pIC50	=	7.3	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	615	12	5	4	5.1	CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CCCC1)C(=O)O	10.1021/jm9600914
	76330201	92124	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells	ChEMBL	526	6	1	7	4.5	COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(Cl)ccc12	10.1007/s00044-004-0021-y
	CHEMBL2261363	92124	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells	ChEMBL	526	6	1	7	4.5	COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(Cl)ccc12	10.1007/s00044-004-0021-y
	10479787	66389	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	468	6	1	5	5.3	Cc1cc(C)c(CCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1	10.1016/S0960-894X(97)00133-9
	CHEMBL171972	66389	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	468	6	1	5	5.3	Cc1cc(C)c(CCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1	10.1016/S0960-894X(97)00133-9
	18995988	107113	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.	ChEMBL	389	6	1	4	5.5	COc1cccc(Sc2c(C(=O)O)n(Cc3ccccc3)c3ccccc23)c1	10.1016/0960-894X(96)00232-6
	CHEMBL28948	107113	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.	ChEMBL	389	6	1	4	5.5	COc1cccc(Sc2c(C(=O)O)n(Cc3ccccc3)c3ccccc23)c1	10.1016/0960-894X(96)00232-6
	10029811	104732	0	None	-	0	Rat	4.3	pIC50	=	4.3	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	525	8	2	5	6.4	Cc1noc(NS(=O)(=O)c2cccc3c(NC(=O)CC(c4ccccc4)c4ccccc4)cccc23)c1C	10.1021/jm00008a013
	CHEMBL27262	104732	0	None	-	0	Rat	4.3	pIC50	=	4.3	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	525	8	2	5	6.4	Cc1noc(NS(=O)(=O)c2cccc3c(NC(=O)CC(c4ccccc4)c4ccccc4)cccc23)c1C	10.1021/jm00008a013
	44279127	106264	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor	ChEMBL	432	3	2	3	4.8	O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(-c3ccc(Cl)cc3)cc21	10.1016/0960-894X(95)00230-Q
	CHEMBL283200	106264	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor	ChEMBL	432	3	2	3	4.8	O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(-c3ccc(Cl)cc3)cc21	10.1016/0960-894X(95)00230-Q
	10815168	174930	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	497	5	2	6	5.2	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc(C(C)(C)C)cc2)c1Br	10.1021/jm9608366
	CHEMBL433074	174930	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	497	5	2	6	5.2	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc(C(C)(C)C)cc2)c1Br	10.1021/jm9608366
	9869444	104021	0	None	-	1	Human	7.3	pIC50	=	7.3	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	473	7	1	7	5.3	CCCOc1ccc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2c1	10.1016/0960-894X(96)00170-9
	CHEMBL268751	104021	0	None	-	1	Human	7.3	pIC50	=	7.3	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	473	7	1	7	5.3	CCCOc1ccc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2c1	10.1016/0960-894X(96)00170-9
	CHEMBL342440	218453	0	None	-	0	Pig	7.3	pIC50	=	7.3	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CCC[C@@H]1NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC1=O	10.1021/jm00021a021
	23445250	174885	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	468	6	1	5	5.8	Cc1cc(CC(C)C)ccc1-c1ccsc1S(=O)(=O)Nc1onc(C)c1Br	10.1016/S0960-894X(96)00496-9
	CHEMBL432815	174885	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	468	6	1	5	5.8	Cc1cc(CC(C)C)ccc1-c1ccsc1S(=O)(=O)Nc1onc(C)c1Br	10.1016/S0960-894X(96)00496-9
	44316515	211783	2	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	360	4	1	5	2.9	COc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1C	10.1016/0960-894X(96)00441-6
	CHEMBL76779	211783	2	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	360	4	1	5	2.9	COc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1C	10.1016/0960-894X(96)00441-6
	44314472	110575	0	None	-	0	Pig	6.3	pIC50	=	6.3	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	594	13	5	5	4.2	CCCCC(NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1021/jm9600914
	CHEMBL309003	110575	0	None	-	0	Pig	6.3	pIC50	=	6.3	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	594	13	5	5	4.2	CCCCC(NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1021/jm9600914
	10626177	67165	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor	ChEMBL	535	11	4	5	4.8	Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)CC2CCCCC2)nc1C(=O)O	10.1021/jm9505932
	CHEMBL174871	67165	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor	ChEMBL	535	11	4	5	4.8	Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)CC2CCCCC2)nc1C(=O)O	10.1021/jm9505932
	44283420	168571	0	None	-	0	Pig	6.3	pIC50	=	6.3	Binding	Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	594	13	5	5	4.2	CCCC[C@H](NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1016/0960-894X(95)00237-N
	CHEMBL414175	168571	0	None	-	0	Pig	6.3	pIC50	=	6.3	Binding	Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	594	13	5	5	4.2	CCCC[C@H](NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1016/0960-894X(95)00237-N
	23548251	88456	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	661	16	1	14	4.0	COc1cc(OC)nc(OCCOc2nc(-c3ncccn3)nc(NS(=O)(=O)CCc3ccccc3)c2Oc2ccccc2OC)n1	10.1021/jm3009103
	CHEMBL2163707	88456	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	661	16	1	14	4.0	COc1cc(OC)nc(OCCOc2nc(-c3ncccn3)nc(NS(=O)(=O)CCc3ccccc3)c2Oc2ccccc2OC)n1	10.1021/jm3009103
	11801523	15028	0	None	-	0	Rat	7.3	pIC50	=	7.3	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	588	16	1	7	5.3	CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCC)cc1	10.1021/jm970101g
	CHEMBL109242	15028	0	None	-	0	Rat	7.3	pIC50	=	7.3	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	588	16	1	7	5.3	CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCC)cc1	10.1021/jm970101g
	10961960	209655	0	None	-	0	Rat	7.3	pIC50	=	7.3	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	487	8	1	7	4.4	CCCCC1=C(C(=O)NS(C)(=O)=O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	CHEMBL62633	209655	0	None	-	0	Rat	7.3	pIC50	=	7.3	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	487	8	1	7	4.4	CCCCC1=C(C(=O)NS(C)(=O)=O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	CHEMBL304260	217752	0	None	-	0	Pig	7.3	pIC50	=	7.3	Binding	Inhibition of endothelin (ET-A) binding to porcine heart membranes Inhibition of endothelin (ET-A) binding to porcine heart membranes	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/0960-894X(95)00349-X
	9830495	137927	0	None	-	1	Human	7.3	pIC50	=	7.3	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	618	14	2	9	5.0	CCS(=O)(=O)NCCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	CHEMBL368617	137927	0	None	-	1	Human	7.3	pIC50	=	7.3	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	618	14	2	9	5.0	CCS(=O)(=O)NCCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	137661460	166154	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	565	10	2	9	4.4	C=CCOc1ccc2c(c1)c(=O)c(Cc1cccc(-c3nnn[nH]3)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2	10.1016/j.bmcl.2017.04.049
	CHEMBL4100579	166154	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	565	10	2	9	4.4	C=CCOc1ccc2c(c1)c(=O)c(Cc1cccc(-c3nnn[nH]3)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2	10.1016/j.bmcl.2017.04.049
	CHEMBL2370255	216598	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	10645550	104127	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	416	5	1	6	3.8	COc1ccccc1C1(O)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1ccccc1	10.1021/jm9606507
	CHEMBL269461	104127	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	416	5	1	6	3.8	COc1ccccc1C1(O)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1ccccc1	10.1021/jm9606507
	11145841	107732	0	None	-	0	Rat	5.3	pIC50	=	5.3	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	528	9	1	6	6.9	CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc(OC3CCCC3)cc1)O2	10.1021/jm010382z
	CHEMBL294127	107732	0	None	-	0	Rat	5.3	pIC50	=	5.3	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	528	9	1	6	6.9	CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc(OC3CCCC3)cc1)O2	10.1021/jm010382z
	44279129	113772	0	None	-	0	Human	4.3	pIC50	=	4.3	Binding	Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor	ChEMBL	428	4	2	4	4.2	COc1ccccc1-c1ccc2c(c1)C(=O)c1ccccc1[C@@H]1[C@H](C(=O)O)[C@H](C(=O)O)[C@H]21	10.1016/0960-894X(95)00230-Q
	CHEMBL31524	113772	0	None	-	0	Human	4.3	pIC50	=	4.3	Binding	Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor	ChEMBL	428	4	2	4	4.2	COc1ccccc1-c1ccc2c(c1)C(=O)c1ccccc1[C@@H]1[C@H](C(=O)O)[C@H](C(=O)O)[C@H]21	10.1016/0960-894X(95)00230-Q
	44277245	113624	0	None	-	0	Rat	4.3	pIC50	=	4.3	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	392	6	1	4	3.9	COc1ccc(Cc2c(C(F)(F)F)[nH]n(Cc3cccc(OC)c3)c2=O)cc1	10.1016/s0960-894x(00)00232-8
	CHEMBL3144736	113624	0	None	-	0	Rat	4.3	pIC50	=	4.3	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	392	6	1	4	3.9	COc1ccc(Cc2c(C(F)(F)F)[nH]n(Cc3cccc(OC)c3)c2=O)cc1	10.1016/s0960-894x(00)00232-8
	44385522	66400	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	642	13	2	11	4.2	CCS(=O)(=O)NCCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	CHEMBL172029	66400	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	642	13	2	11	4.2	CCS(=O)(=O)NCCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	9808545	18224	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	588	11	2	7	5.2	COCCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)(C)C)cc1	10.1021/jm990171i
	CHEMBL1180353	18224	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	588	11	2	7	5.2	COCCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)(C)C)cc1	10.1021/jm990171i
	CHEMBL123408	18224	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	588	11	2	7	5.2	COCCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)(C)C)cc1	10.1021/jm990171i
	10571380	66850	0	None	-	0	Rat	7.3	pIC50	=	7.3	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	373	7	1	4	4.7	Cc1ccccc1C(Oc1cc(OCc2ccccc2)ccc1C#N)C(=O)O	10.1021/jm990378b
	CHEMBL173838	66850	0	None	-	0	Rat	7.3	pIC50	=	7.3	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	373	7	1	4	4.7	Cc1ccccc1C(Oc1cc(OCc2ccccc2)ccc1C#N)C(=O)O	10.1021/jm990378b
	9845967	17865	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells	ChEMBL	416	7	1	5	4.4	COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1	10.1021/jm9606507
	CHEMBL10801	17865	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells	ChEMBL	416	7	1	5	4.4	COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1	10.1021/jm9606507
	CHEMBL1178000	17865	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells	ChEMBL	416	7	1	5	4.4	COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1	10.1021/jm9606507
	CHEMBL51530	17865	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells	ChEMBL	416	7	1	5	4.4	COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1	10.1021/jm9606507
	CHEMBL433853	220426	0	None	-	0	Pig	7.3	pIC50	=	7.3	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C(C)(C)S)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	44371450	55638	0	None	-	0	Rat	6.3	pIC50	=	6.3	Binding	Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes	ChEMBL	485	7	1	7	5.2	COc1ccc(OC)c(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2ccccc23)c1	10.1016/s0960-894x(99)00040-2
	CHEMBL155937	55638	0	None	-	0	Rat	6.3	pIC50	=	6.3	Binding	Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes	ChEMBL	485	7	1	7	5.2	COc1ccc(OC)c(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2ccccc23)c1	10.1016/s0960-894x(99)00040-2
	15453210	212025	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	376	5	1	6	2.6	COc1ccc(S(=O)(=O)Nc2onc(C)c2Br)cc1OC	10.1016/0960-894X(96)00441-6
	CHEMBL78853	212025	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	376	5	1	6	2.6	COc1ccc(S(=O)(=O)Nc2onc(C)c2Br)cc1OC	10.1016/0960-894X(96)00441-6
	44316458	212220	2	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	408	3	1	4	3.6	Cc1noc(NS(=O)(=O)c2cc(Br)ccc2Br)c1C	10.1016/0960-894X(96)00441-6
	CHEMBL80317	212220	2	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	408	3	1	4	3.6	Cc1noc(NS(=O)(=O)c2cc(Br)ccc2Br)c1C	10.1016/0960-894X(96)00441-6
	10404449	106280	0	None	-	0	Rat	5.3	pIC50	=	5.3	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	331	4	1	5	3.0	Cc1cnoc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12	10.1021/jm00008a013
	CHEMBL283300	106280	0	None	-	0	Rat	5.3	pIC50	=	5.3	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	331	4	1	5	3.0	Cc1cnoc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12	10.1021/jm00008a013
	9865706	104910	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	400	4	1	5	4.1	Cc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1	10.1021/jm9606507
	CHEMBL273613	104910	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	400	4	1	5	4.1	Cc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1	10.1021/jm9606507
	44385523	67838	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	666	13	2	9	5.9	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C2CC2)nc1OCCNS(=O)(=O)c1ccc(C)cc1	10.1016/s0960-894x(02)01083-1
	CHEMBL176418	67838	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	666	13	2	9	5.9	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C2CC2)nc1OCCNS(=O)(=O)c1ccc(C)cc1	10.1016/s0960-894x(02)01083-1
	CHEMBL409777	219563	0	None	-	0	Rat	4.3	pIC50	=	4.3	Binding	In vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricleIn vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricle	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)80156-6
	9957883	105433	0	None	-	1	Human	8.3	pIC50	=	8.3	Binding	Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.	ChEMBL	507	7	1	9	5.0	COc1cc2c(Sc3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC	10.1016/0960-894X(96)00232-6
	CHEMBL27732	105433	0	None	-	1	Human	8.3	pIC50	=	8.3	Binding	Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.	ChEMBL	507	7	1	9	5.0	COc1cc2c(Sc3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC	10.1016/0960-894X(96)00232-6
	10626031	116475	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	529	13	1	7	2.9	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCN1C(=O)CCC1=O	10.1021/jm980217s
	CHEMBL322799	116475	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	529	13	1	7	2.9	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCN1C(=O)CCC1=O	10.1021/jm980217s
	10767210	118092	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	484	12	1	4	5.1	CCCCN(CCCC)C(=O)CN1C[C@H](c2cccc(F)c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	CHEMBL326719	118092	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	484	12	1	4	5.1	CCCCN(CCCC)C(=O)CN1C[C@H](c2cccc(F)c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	9871837	21975	0	None	-	1	Human	8.3	pIC50	=	8.3	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	535	10	2	7	4.9	CCCc1nc(CC)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(C)c1	10.1039/C4MD00499J
	CHEMBL12106	21975	0	None	-	1	Human	8.3	pIC50	=	8.3	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	535	10	2	7	4.9	CCCc1nc(CC)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(C)c1	10.1039/C4MD00499J
	44458650	91678	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	521	7	2	8	2.7	COc1ccccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12	10.1016/s0960-894x(01)00660-6
	CHEMBL22367	91678	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	521	7	2	8	2.7	COc1ccccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12	10.1016/s0960-894x(01)00660-6
	10619391	67012	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	374	7	1	5	4.0	Cc1ccccc1C(Oc1cc(OCc2ccncc2)ccc1C#N)C(=O)O	10.1021/jm990378b
	CHEMBL173251	67012	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	374	7	1	5	4.0	Cc1ccccc1C(Oc1cc(OCc2ccncc2)ccc1C#N)C(=O)O	10.1021/jm990378b
	CHEMBL174092	67012	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	374	7	1	5	4.0	Cc1ccccc1C(Oc1cc(OCc2ccncc2)ccc1C#N)C(=O)O	10.1021/jm990378b
	10547407	85140	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	374	7	1	5	4.0	Cc1ccccc1[C@H](Oc1cc(OCc2ccncc2)ccc1C#N)C(=O)O	10.1021/jm990378b
	CHEMBL2110232	85140	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	374	7	1	5	4.0	Cc1ccccc1[C@H](Oc1cc(OCc2ccncc2)ccc1C#N)C(=O)O	10.1021/jm990378b
	10453733	119088	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	ChEMBL	402	9	1	5	4.8	Cc1ccccc1[C@@H](CCC(=O)O)Oc1cc(OCc2cccnc2)ccc1C#N	10.1021/jm9707131
	CHEMBL329181	119088	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	ChEMBL	402	9	1	5	4.8	Cc1ccccc1[C@@H](CCC(=O)O)Oc1cc(OCc2cccnc2)ccc1C#N	10.1021/jm9707131
	9953204	214211	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	ChEMBL	407	9	1	5	5.5	Cc1ccccc1[C@@H](CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1C#N	10.1021/jm9707131
	CHEMBL94071	214211	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	ChEMBL	407	9	1	5	5.5	Cc1ccccc1[C@@H](CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1C#N	10.1021/jm9707131
	10210086	68055	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	571	10	2	12	3.0	C#CCOc1nc(-c2ccnc(-c3nn[nH]n3)c2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	CHEMBL176664	68055	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	571	10	2	12	3.0	C#CCOc1nc(-c2ccnc(-c3nn[nH]n3)c2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	10361107	168827	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	359	5	2	5	4.1	Cc1noc(NS(=O)(=O)c2cccc3c(NC(C)C)cccc23)c1C	10.1021/jm00004a012
	CHEMBL416026	168827	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	359	5	2	5	4.1	Cc1noc(NS(=O)(=O)c2cccc3c(NC(C)C)cccc23)c1C	10.1021/jm00004a012
	CHEMBL64271	222632	0	None	-	0	Pig	8.3	pIC50	=	8.3	Binding	Inhibition of endothelin (ET-A) binding to porcine heart membranes Inhibition of endothelin (ET-A) binding to porcine heart membranes	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/0960-894X(95)00349-X
	10281929	16165	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	588	16	1	7	5.3	CCCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm970101g
	CHEMBL111517	16165	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	588	16	1	7	5.3	CCCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm970101g
	10553490	187895	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	501	8	3	10	2.9	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2OCCO)OCO3)c1Cl	10.1021/jm9608366
	CHEMBL47604	187895	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	501	8	3	10	2.9	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2OCCO)OCO3)c1Cl	10.1021/jm9608366
	44386921	68054	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	384	5	1	6	3.8	COC1=C(C(=O)O)[C@H](c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm031041j
	CHEMBL176661	68054	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	384	5	1	6	3.8	COC1=C(C(=O)O)[C@H](c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm031041j
	10721344	14312	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	548	13	1	8	3.0	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CCOC	10.1021/jm970101g
	CHEMBL108748	14312	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	548	13	1	8	3.0	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CCOC	10.1021/jm970101g
	10918390	26093	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	522	12	1	5	5.3	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CC)cc1	10.1021/jm010237l
	CHEMBL129060	26093	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	522	12	1	5	5.3	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CC)cc1	10.1021/jm010237l
	9807178	209770	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	384	5	1	6	3.8	COC1=C(C(=O)O)[C@@H](c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	CHEMBL63121	209770	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	384	5	1	6	3.8	COC1=C(C(=O)O)[C@@H](c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	10767280	115445	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	486	14	1	5	5.1	C=C(C)CCC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC	10.1021/jm980217s
	CHEMBL320763	115445	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	486	14	1	5	5.1	C=C(C)CCC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC	10.1021/jm980217s
	44458669	91448	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	505	6	2	7	3.0	Cc1ccccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12	10.1016/s0960-894x(01)00660-6
	CHEMBL22249	91448	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	505	6	2	7	3.0	Cc1ccccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12	10.1016/s0960-894x(01)00660-6
	107810	8465	30	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.	ChEMBL	604	12	4	6	3.4	CC(C[C@@H](C(=O)N[C@@H](C(=O)N[C@@H](C(=O)O)Cc1ccccn1)Cc1cn(c2c1cccc2)C)NC(=O)N1CCCCCC1)C	10.1016/0960-894X(95)00144-I
	998	8465	30	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.	ChEMBL	604	12	4	6	3.4	CC(C[C@@H](C(=O)N[C@@H](C(=O)N[C@@H](C(=O)O)Cc1ccccn1)Cc1cn(c2c1cccc2)C)NC(=O)N1CCCCCC1)C	10.1016/0960-894X(95)00144-I
	CHEMBL352396	8465	30	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.	ChEMBL	604	12	4	6	3.4	CC(C[C@@H](C(=O)N[C@@H](C(=O)N[C@@H](C(=O)O)Cc1ccccn1)Cc1cn(c2c1cccc2)C)NC(=O)N1CCCCCC1)C	10.1016/0960-894X(95)00144-I
	22009947	92119	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells	ChEMBL	536	7	2	8	3.6	COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(=O)O)ccc12	10.1007/s00044-004-0021-y
	CHEMBL2261358	92119	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells	ChEMBL	536	7	2	8	3.6	COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(=O)O)ccc12	10.1007/s00044-004-0021-y
	9984193	107934	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	521	10	2	8	3.9	CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1021/jm031041j
	CHEMBL295440	107934	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	521	10	2	8	3.9	CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1021/jm031041j
	9984193	107934	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	521	10	2	8	3.9	CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	CHEMBL295440	107934	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	521	10	2	8	3.9	CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	10649119	18210	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	502	8	2	6	4.1	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(C)c2ccccc2)cc1	10.1021/jm990171i
	CHEMBL1180318	18210	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	502	8	2	6	4.1	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(C)c2ccccc2)cc1	10.1021/jm990171i
	CHEMBL121761	18210	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	502	8	2	6	4.1	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(C)c2ccccc2)cc1	10.1021/jm990171i
	73669994	124408	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Displacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry method	ChEMBL	429	9	1	7	4.7	N#Cc1ccc(OCc2ccc3nonc3c2)cc1OC(CCC(=O)O)c1ccccc1	10.1016/j.bmc.2015.01.003
	CHEMBL3400996	124408	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Displacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry method	ChEMBL	429	9	1	7	4.7	N#Cc1ccc(OCc2ccc3nonc3c2)cc1OC(CCC(=O)O)c1ccccc1	10.1016/j.bmc.2015.01.003
	44314750	172431	0	None	-	0	Pig	8.3	pIC50	=	8.3	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	647	13	5	4	5.1	CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1021/jm9600914
	CHEMBL424422	172431	0	None	-	0	Pig	8.3	pIC50	=	8.3	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	647	13	5	4	5.1	CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1021/jm9600914
	10140965	107949	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	485	7	3	9	3.0	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2CCO)OCO3)c1Cl	10.1021/jm9608366
	CHEMBL295588	107949	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	485	7	3	9	3.0	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2CCO)OCO3)c1Cl	10.1021/jm9608366
	44283419	107093	0	None	-	0	Pig	8.3	pIC50	=	8.3	Binding	Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	647	13	5	4	5.1	CCCC[C@H](NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1016/0960-894X(95)00237-N
	CHEMBL289349	107093	0	None	-	0	Pig	8.3	pIC50	=	8.3	Binding	Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	647	13	5	4	5.1	CCCC[C@H](NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1016/0960-894X(95)00237-N
	44314905	211826	0	None	-	0	Pig	8.2	pIC50	=	8.2	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	567	12	5	4	4.0	CCCCC(NC(=O)[C@@H](Cc1c(C)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O	10.1021/jm9600914
	CHEMBL77083	211826	0	None	-	0	Pig	8.2	pIC50	=	8.2	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	567	12	5	4	4.0	CCCCC(NC(=O)[C@@H](Cc1c(C)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O	10.1021/jm9600914
	44333867	11414	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	403	4	1	5	4.1	COc1ccc([C@@H]2c3nc(C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1	10.1016/s0960-894x(02)00663-7
	CHEMBL103001	11414	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	403	4	1	5	4.1	COc1ccc([C@@H]2c3nc(C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1	10.1016/s0960-894x(02)00663-7
	10415822	136597	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	579	9	3	7	4.7	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCOC23CCCCC3)nc1C(=O)O	10.1021/jm950592+
	CHEMBL367551	136597	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	579	9	3	7	4.7	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCOC23CCCCC3)nc1C(=O)O	10.1021/jm950592+
	11798998	213614	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	482	10	1	6	3.9	CCCCCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL9050	213614	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	482	10	1	6	3.9	CCCCCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	122272	103872	31	None	1	2	Human	8.2	pIC50	=	8.2	Binding	Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C	10.1016/0960-894X(96)00441-6
	CHEMBL267458	103872	31	None	1	2	Human	8.2	pIC50	=	8.2	Binding	Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C	10.1016/0960-894X(96)00441-6
	10415348	67862	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	557	9	3	6	4.8	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCc3ccccc32)nc1C(=O)O	10.1021/jm950592+
	CHEMBL176514	67862	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	557	9	3	6	4.8	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCc3ccccc32)nc1C(=O)O	10.1021/jm950592+
	CHEMBL438733	220570	0	None	-	0	Pig	8.2	pIC50	=	8.2	Binding	Tested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptorTested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptor	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC(=O)[C@H]2CSSC[C@@H](N)C(=O)N[C@@H](CO)C(=O)N2)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00077a013
	10647642	14872	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	460	6	2	7	3.5	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(C(=O)O)c2)cc1	10.1021/jm9606507
	CHEMBL10915	14872	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	460	6	2	7	3.5	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(C(=O)O)c2)cc1	10.1021/jm9606507
	11799625	120575	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	502	7	2	6	4.5	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2ccc(C)c(C)c2)cc1	10.1021/jm990170q
	CHEMBL332431	120575	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	502	7	2	6	4.5	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2ccc(C)c(C)c2)cc1	10.1021/jm990170q
	9871561	181579	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cellsDisplacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cells	ChEMBL	527	10	2	8	4.6	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cc2)nc(C(F)(F)F)nc1OCCO	10.1016/j.bmcl.2016.06.014
	CHEMBL4562189	181579	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cellsDisplacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cells	ChEMBL	527	10	2	8	4.6	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cc2)nc(C(F)(F)F)nc1OCCO	10.1016/j.bmcl.2016.06.014
	9873255	66408	0	None	-	2	Human	7.3	pIC50	=	7.3	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	591	14	2	10	3.8	CCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	CHEMBL172071	66408	0	None	-	2	Human	7.3	pIC50	=	7.3	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	591	14	2	10	3.8	CCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	122272	103872	31	None	1	2	Human	7.3	pIC50	=	7.3	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C	10.1021/jm9604585
	CHEMBL267458	103872	31	None	1	2	Human	7.3	pIC50	=	7.3	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C	10.1021/jm9604585
	10553017	104883	0	None	-	0	Rat	7.3	pIC50	=	7.3	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	488	7	1	6	3.9	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(C)c2ccccc2)cc1	10.1021/jm9505369
	CHEMBL273476	104883	0	None	-	0	Rat	7.3	pIC50	=	7.3	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	488	7	1	6	3.9	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(C)c2ccccc2)cc1	10.1021/jm9505369
	10502023	129170	0	None	-	0	Rat	6.3	pIC50	=	6.3	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	416	7	1	5	4.4	COc1cccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)c1	10.1021/jm031041j
	CHEMBL360066	129170	0	None	-	0	Rat	6.3	pIC50	=	6.3	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	416	7	1	5	4.4	COc1cccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)c1	10.1021/jm031041j
	CHEMBL384728	219113	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	3370402	112568	5	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	252	3	1	4	2.1	Cc1noc(NS(=O)(=O)c2ccccc2)c1C	10.1016/0960-894X(96)00441-6
	CHEMBL312670	112568	5	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	252	3	1	4	2.1	Cc1noc(NS(=O)(=O)c2ccccc2)c1C	10.1016/0960-894X(96)00441-6
	10740614	105084	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	416	5	1	6	3.8	COc1cccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)c1	10.1021/jm9606507
	CHEMBL274857	105084	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	416	5	1	6	3.8	COc1cccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)c1	10.1021/jm9606507
	10714851	118702	0	None	-	0	Rat	6.3	pIC50	=	6.3	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	381	7	1	5	4.9	O=C(O)/C(=C/c1cc(OCc2ccsc2)ccc1[N+](=O)[O-])c1ccccc1	10.1021/jm970847e
	CHEMBL328786	118702	0	None	-	0	Rat	6.3	pIC50	=	6.3	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	381	7	1	5	4.9	O=C(O)/C(=C/c1cc(OCc2ccsc2)ccc1[N+](=O)[O-])c1ccccc1	10.1021/jm970847e
	44211959	62210	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells	ChEMBL	620	12	1	9	5.5	CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)NS(C)(=O)=O)c1ccc2c(c1)OCO2	10.1016/0960-894X(95)00186-W
	CHEMBL16197	62210	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells	ChEMBL	620	12	1	9	5.5	CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)NS(C)(=O)=O)c1ccc2c(c1)OCO2	10.1016/0960-894X(95)00186-W
	44368480	51382	0	None	-	0	Pig	5.3	pIC50	=	5.3	Binding	Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.	ChEMBL	495	13	1	7	4.4	COc1ccc(CC(C(=O)O)N(Cc2ccc(OC)cc2)Cc2cc(OC)c(OC)c(OC)c2)cc1	10.1016/s0960-894x(01)00009-9
	CHEMBL152034	51382	0	None	-	0	Pig	5.3	pIC50	=	5.3	Binding	Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.	ChEMBL	495	13	1	7	4.4	COc1ccc(CC(C(=O)O)N(Cc2ccc(OC)cc2)Cc2cc(OC)c(OC)c(OC)c2)cc1	10.1016/s0960-894x(01)00009-9
	10017402	108669	2	None	-	0	Rat	5.3	pIC50	=	5.3	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	295	5	2	5	2.5	CCNc1ccc(S(=O)(=O)Nc2onc(C)c2C)cc1	10.1021/jm00008a013
	CHEMBL30078	108669	2	None	-	0	Rat	5.3	pIC50	=	5.3	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	295	5	2	5	2.5	CCNc1ccc(S(=O)(=O)Nc2onc(C)c2C)cc1	10.1021/jm00008a013
	44328057	103669	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL	986	26	9	9	4.9	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)c1cccnc1)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	CHEMBL265734	103669	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL	986	26	9	9	4.9	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)c1cccnc1)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	CHEMBL2370253	216596	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	44279351	106720	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor	ChEMBL	412	3	2	3	4.5	Cc1ccccc1-c1ccc2c(c1)C(=O)c1ccccc1[C@@H]1[C@H](C(=O)O)[C@H](C(=O)O)[C@H]21	10.1016/0960-894X(95)00230-Q
	CHEMBL286333	106720	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor	ChEMBL	412	3	2	3	4.5	Cc1ccccc1-c1ccc2c(c1)C(=O)c1ccccc1[C@@H]1[C@H](C(=O)O)[C@H](C(=O)O)[C@H]21	10.1016/0960-894X(95)00230-Q
	31771	103741	37	None	-	0	Rat	5.3	pIC50	=	5.3	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	267	3	2	5	1.7	Cc1onc(NS(=O)(=O)c2ccc(N)cc2)c1C	10.1016/s0960-894x(00)00366-8
	CHEMBL26630	103741	37	None	-	0	Rat	5.3	pIC50	=	5.3	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	267	3	2	5	1.7	Cc1onc(NS(=O)(=O)c2ccc(N)cc2)c1C	10.1016/s0960-894x(00)00366-8
	10017402	108669	2	None	-	0	Rat	5.3	pIC50	=	5.3	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	295	5	2	5	2.5	CCNc1ccc(S(=O)(=O)Nc2onc(C)c2C)cc1	10.1021/jm00004a012
	CHEMBL30078	108669	2	None	-	0	Rat	5.3	pIC50	=	5.3	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	295	5	2	5	2.5	CCNc1ccc(S(=O)(=O)Nc2onc(C)c2C)cc1	10.1021/jm00004a012
	10454873	103197	0	None	-	0	Rat	4.3	pIC50	=	4.3	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	421	6	1	5	4.6	Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1Cc1ccccc1	10.1021/jm00008a013
	CHEMBL26203	103197	0	None	-	0	Rat	4.3	pIC50	=	4.3	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	421	6	1	5	4.6	Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1Cc1ccccc1	10.1021/jm00008a013
	44383536	127175	0	None	-	0	Human	4.3	pIC50	=	4.3	Binding	Tested for binding affinity towards rabbit Endothelin A receptorTested for binding affinity towards rabbit Endothelin A receptor	ChEMBL	362	3	2	5	2.9	C/C=C/C=C/C(=O)O[C@@H]1C=C2COC(O)[C@]2(O)[C@@]2(C)CCCC(C)(C)C12	10.1016/s0960-894x(00)00136-0
	CHEMBL353502	127175	0	None	-	0	Human	4.3	pIC50	=	4.3	Binding	Tested for binding affinity towards rabbit Endothelin A receptorTested for binding affinity towards rabbit Endothelin A receptor	ChEMBL	362	3	2	5	2.9	C/C=C/C=C/C(=O)O[C@@H]1C=C2COC(O)[C@]2(O)[C@@]2(C)CCCC(C)(C)C12	10.1016/s0960-894x(00)00136-0
	10671298	210231	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	450	6	1	6	3.7	CCOc1nc(Br)cnc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12	10.1021/jm9604585
	CHEMBL6588	210231	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	450	6	1	6	3.7	CCOc1nc(Br)cnc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12	10.1021/jm9604585
	10789830	103793	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	453	4	1	4	3.7	CN(C)c1cccc2c(S(=O)(=O)Nc3ccc(I)cn3)cccc12	10.1021/jm9604585
	CHEMBL266684	103793	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	453	4	1	4	3.7	CN(C)c1cccc2c(S(=O)(=O)Nc3ccc(I)cn3)cccc12	10.1021/jm9604585
	10740942	210320	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	422	4	2	6	3.0	CN(C)c1cccc2c(S(=O)(=O)Nc3ncc(Br)nc3O)cccc12	10.1021/jm9604585
	CHEMBL6647	210320	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	422	4	2	6	3.0	CN(C)c1cccc2c(S(=O)(=O)Nc3ncc(Br)nc3O)cccc12	10.1021/jm9604585
	10595728	210329	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	376	4	1	5	3.5	Cc1cc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)nnc1Cl	10.1021/jm9604585
	CHEMBL6660	210329	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	376	4	1	5	3.5	Cc1cc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)nnc1Cl	10.1021/jm9604585
	10644647	127278	0	None	-	0	Rat	6.3	pIC50	=	6.3	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	399	7	1	5	5.1	N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1ccc(Cl)cc1	10.1021/jm990378b
	CHEMBL354428	127278	0	None	-	0	Rat	6.3	pIC50	=	6.3	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	399	7	1	5	5.1	N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1ccc(Cl)cc1	10.1021/jm990378b
	9845562	11513	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	430	5	1	6	4.1	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(C)cc2)cc1	10.1021/jm9606507
	CHEMBL10374	11513	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	430	5	1	6	4.1	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(C)cc2)cc1	10.1021/jm9606507
	44279535	110913	0	None	-	0	Pig	7.3	pIC50	=	7.3	Binding	Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	527	11	5	4	3.2	CC(C)C[C@H](NC(=O)N1C(C)CCCC1C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	CHEMBL30944	110913	0	None	-	0	Pig	7.3	pIC50	=	7.3	Binding	Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	527	11	5	4	3.2	CC(C)C[C@H](NC(=O)N1C(C)CCCC1C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	44314675	104904	0	None	-	0	Pig	7.3	pIC50	=	7.3	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	603	13	5	4	5.0	CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)CC)C(=O)O	10.1021/jm9600914
	CHEMBL273583	104904	0	None	-	0	Pig	7.3	pIC50	=	7.3	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	603	13	5	4	5.0	CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)CC)C(=O)O	10.1021/jm9600914
	CHEMBL2304005	216240	0	None	-	0	Pig	7.3	pIC50	=	7.3	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		Cc1[nH]c2ccccc2c1C[C@@H]1NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](C(C)C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC1=O	10.1021/jm9600914
	9955093	173075	0	None	-	0	Rat	7.3	pIC50	=	7.3	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	443	7	1	5	5.2	N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1ccccc1Br	10.1021/jm990378b
	CHEMBL427117	173075	0	None	-	0	Rat	7.3	pIC50	=	7.3	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	443	7	1	5	5.2	N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1ccccc1Br	10.1021/jm990378b
	10281606	136450	0	None	-	1	Human	7.3	pIC50	=	7.3	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	575	9	2	10	4.2	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCC#CCO	10.1016/s0960-894x(02)01084-3
	CHEMBL367382	136450	0	None	-	1	Human	7.3	pIC50	=	7.3	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	575	9	2	10	4.2	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCC#CCO	10.1016/s0960-894x(02)01084-3
	9809270	138118	0	None	-	2	Human	7.3	pIC50	=	7.3	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	622	14	2	12	2.3	CCCS(=O)(=O)NCCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	CHEMBL368738	138118	0	None	-	2	Human	7.3	pIC50	=	7.3	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	622	14	2	12	2.3	CCCS(=O)(=O)NCCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	10896930	16594	0	None	-	0	Pig	7.3	pIC50	=	7.3	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	551	11	1	10	4.6	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2cccnn2)c1	10.1021/jm0102304
	CHEMBL113888	16594	0	None	-	0	Pig	7.3	pIC50	=	7.3	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	551	11	1	10	4.6	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2cccnn2)c1	10.1021/jm0102304
	44373550	126628	0	None	-	0	Rat	6.3	pIC50	=	6.3	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	331	3	2	5	2.1	Cc1onc(NS(=O)(=O)c2ccc(N)cc2)c1Br	10.1021/jm00004a012
	CHEMBL348641	126628	0	None	-	0	Rat	6.3	pIC50	=	6.3	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	331	3	2	5	2.1	Cc1onc(NS(=O)(=O)c2ccc(N)cc2)c1Br	10.1021/jm00004a012
	10647182	116499	0	None	-	0	Rat	5.3	pIC50	=	5.3	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	449	8	2	4	3.9	CCCN(C)C(=O)CN1C[C@H](c2ccc3cc[nH]c3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	CHEMBL322935	116499	0	None	-	0	Rat	5.3	pIC50	=	5.3	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	449	8	2	4	3.9	CCCN(C)C(=O)CN1C[C@H](c2ccc3cc[nH]c3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	10579195	138117	0	None	-	0	Rat	4.3	pIC50	=	4.3	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	584	10	5	4	5.7	CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(-c2ccccc2)[nH]1	10.1021/jm950591h
	CHEMBL368711	138117	0	None	-	0	Rat	4.3	pIC50	=	4.3	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	584	10	5	4	5.7	CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(-c2ccccc2)[nH]1	10.1021/jm950591h
	10531664	175321	0	None	-	0	Rat	4.3	pIC50	=	4.3	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	601	10	4	5	6.4	CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(-c2ccccc2)s1	10.1021/jm950591h
	CHEMBL435537	175321	0	None	-	0	Rat	4.3	pIC50	=	4.3	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	601	10	4	5	6.4	CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(-c2ccccc2)s1	10.1021/jm950591h
	9897092	66710	0	None	-	1	Human	5.3	pIC50	=	5.3	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	779	17	2	13	6.0	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2cc(OC)c(OC)c(OC)c2)nc1OCCNS(=O)(=O)c1ccc(C)cc1	10.1016/s0960-894x(02)01083-1
	CHEMBL173201	66710	0	None	-	1	Human	5.3	pIC50	=	5.3	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	779	17	2	13	6.0	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2cc(OC)c(OC)c(OC)c2)nc1OCCNS(=O)(=O)c1ccc(C)cc1	10.1016/s0960-894x(02)01083-1
	23445523	66795	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor	ChEMBL	472	6	1	8	3.9	Cc1noc(NS(=O)(=O)c2sccc2COc2ccc3c(c2)OCO3)c1Br	10.1016/S0960-894X(97)00132-7
	CHEMBL173557	66795	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor	ChEMBL	472	6	1	8	3.9	Cc1noc(NS(=O)(=O)c2sccc2COc2ccc3c(c2)OCO3)c1Br	10.1016/S0960-894X(97)00132-7
	9961347	18734	1	None	-	0	Human	4.3	pIC50	=	4.3	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	664	13	2	7	6.6	Cc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC(C)C)cc1)c1ccccc1C	10.1021/jm990171i
	CHEMBL1182945	18734	1	None	-	0	Human	4.3	pIC50	=	4.3	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	664	13	2	7	6.6	Cc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC(C)C)cc1)c1ccccc1C	10.1021/jm990171i
	CHEMBL273642	18734	1	None	-	0	Human	4.3	pIC50	=	4.3	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	664	13	2	7	6.6	Cc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC(C)C)cc1)c1ccccc1C	10.1021/jm990171i
	10764220	213863	0	None	-	0	Rat	6.3	pIC50	=	6.3	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	413	8	1	6	3.3	CCOCCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL9189	213863	0	None	-	0	Rat	6.3	pIC50	=	6.3	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	413	8	1	6	3.3	CCOCCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	10907399	209735	0	None	-	0	Rat	5.3	pIC50	=	5.3	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	516	11	1	6	6.8	CCCCOc1ccc(C2Oc3ccc(OCCCC)cc3C(c3ccc4c(c3)OCO4)=C2C(=O)O)cc1	10.1021/jm010382z
	CHEMBL62976	209735	0	None	-	0	Rat	5.3	pIC50	=	5.3	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	516	11	1	6	6.8	CCCCOc1ccc(C2Oc3ccc(OCCCC)cc3C(c3ccc4c(c3)OCO4)=C2C(=O)O)cc1	10.1021/jm010382z
	10745212	138325	0	None	-	0	Rat	5.3	pIC50	=	5.3	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	548	10	5	4	4.9	CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(C2CC2)[nH]1	10.1021/jm950591h
	CHEMBL369257	138325	0	None	-	0	Rat	5.3	pIC50	=	5.3	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	548	10	5	4	4.9	CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(C2CC2)[nH]1	10.1021/jm950591h
	10550844	104084	0	None	-	0	Rat	5.3	pIC50	=	5.3	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	435	5	1	6	3.7	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2C(=O)c2ccco2)cc1	10.1021/jm9505369
	CHEMBL269140	104084	0	None	-	0	Rat	5.3	pIC50	=	5.3	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	435	5	1	6	3.7	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2C(=O)c2ccco2)cc1	10.1021/jm9505369
	10548721	66432	0	None	-	0	Rat	6.3	pIC50	=	6.3	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	395	8	1	6	4.4	COc1ccccc1C(Oc1cc(OCc2ccsc2)ccc1C#N)C(=O)O	10.1021/jm990378b
	CHEMBL172164	66432	0	None	-	0	Rat	6.3	pIC50	=	6.3	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	395	8	1	6	4.4	COc1ccccc1C(Oc1cc(OCc2ccsc2)ccc1C#N)C(=O)O	10.1021/jm990378b
	44316768	212022	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	358	4	1	4	3.4	CCc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1C	10.1016/0960-894X(96)00441-6
	CHEMBL78830	212022	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	358	4	1	4	3.4	CCc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1C	10.1016/0960-894X(96)00441-6
	44279458	106494	0	None	-	0	Pig	7.3	pIC50	=	7.3	Binding	Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	531	13	6	5	2.0	CC(C)C[C@H](NC(=O)N(CCO)C(C)(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	CHEMBL284785	106494	0	None	-	0	Pig	7.3	pIC50	=	7.3	Binding	Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	531	13	6	5	2.0	CC(C)C[C@H](NC(=O)N(CCO)C(C)(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	9910709	66122	0	None	-	0	Rat	7.3	pIC50	=	7.3	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	433	7	1	5	5.4	N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1ccccc1C(F)(F)F	10.1021/jm990378b
	CHEMBL170715	66122	0	None	-	0	Rat	7.3	pIC50	=	7.3	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	433	7	1	5	5.4	N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1ccccc1C(F)(F)F	10.1021/jm990378b
	10144372	172833	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	562	10	2	11	3.4	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ncccn2)nc1OCC#CCO	10.1016/s0960-894x(02)01084-3
	CHEMBL425682	172833	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	562	10	2	11	3.4	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ncccn2)nc1OCC#CCO	10.1016/s0960-894x(02)01084-3
	10344511	66457	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	466	5	1	5	5.7	Cc1cc(C)c(/C=C/c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1	10.1016/S0960-894X(97)00133-9
	CHEMBL172248	66457	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	466	5	1	5	5.7	Cc1cc(C)c(/C=C/c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1	10.1016/S0960-894X(97)00133-9
	44279290	113805	0	None	-	0	Pig	6.3	pIC50	=	6.3	Binding	Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	547	11	5	4	3.0	CC(C)C[C@H](NC(=O)N1CCc2ccccc2C1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	CHEMBL31546	113805	0	None	-	0	Pig	6.3	pIC50	=	6.3	Binding	Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	547	11	5	4	3.0	CC(C)C[C@H](NC(=O)N1CCc2ccccc2C1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	10971076	209642	0	None	-	0	Rat	6.3	pIC50	=	6.3	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	386	3	1	4	4.7	Cc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccccc32)cc1	10.1021/jm010382z
	CHEMBL62585	209642	0	None	-	0	Rat	6.3	pIC50	=	6.3	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	386	3	1	4	4.7	Cc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccccc32)cc1	10.1021/jm010382z
	44279128	113689	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor	ChEMBL	428	4	2	4	4.2	COc1ccc(-c2ccc3c(c2)C(=O)c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@H]32)cc1	10.1016/0960-894X(95)00230-Q
	CHEMBL31469	113689	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor	ChEMBL	428	4	2	4	4.2	COc1ccc(-c2ccc3c(c2)C(=O)c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@H]32)cc1	10.1016/0960-894X(95)00230-Q
	44298393	206610	0	None	-	0	Rat	6.3	pIC50	=	6.3	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	432	6	1	6	5.2	COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2C)c1	10.1016/s0960-894x(00)00366-8
	CHEMBL59425	206610	0	None	-	0	Rat	6.3	pIC50	=	6.3	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	432	6	1	6	5.2	COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2C)c1	10.1016/s0960-894x(00)00366-8
	CHEMBL136583	215518	0	None	-	0	Pig	6.3	pIC50	=	6.3	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H](C(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	10546317	213945	0	None	-	0	Rat	5.3	pIC50	=	5.3	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	358	8	1	2	5.7	O=C(O)CC/C(=C/c1cccc(OCc2ccccc2)c1)c1ccccc1	10.1021/jm970847e
	CHEMBL92402	213945	0	None	-	0	Rat	5.3	pIC50	=	5.3	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	358	8	1	2	5.7	O=C(O)CC/C(=C/c1cccc(OCc2ccccc2)c1)c1ccccc1	10.1021/jm970847e
	10106336	104682	8	None	-	0	Rat	4.3	pIC50	=	4.3	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	254	3	2	5	1.5	Cc1cc(NS(=O)(=O)c2ccc(O)cc2)no1	10.1021/jm00008a013
	CHEMBL27248	104682	8	None	-	0	Rat	4.3	pIC50	=	4.3	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	254	3	2	5	1.5	Cc1cc(NS(=O)(=O)c2ccc(O)cc2)no1	10.1021/jm00008a013
	18617394	112406	0	None	-	0	Human	4.3	pIC50	=	4.3	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	294	3	1	4	3.0	Cc1cc(C)c(S(=O)(=O)Nc2onc(C)c2C)c(C)c1	10.1016/0960-894X(96)00441-6
	CHEMBL312372	112406	0	None	-	0	Human	4.3	pIC50	=	4.3	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	294	3	1	4	3.0	Cc1cc(C)c(S(=O)(=O)Nc2onc(C)c2C)c(C)c1	10.1016/0960-894X(96)00441-6
	10106336	104682	8	None	-	0	Rat	4.3	pIC50	=	4.3	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	254	3	2	5	1.5	Cc1cc(NS(=O)(=O)c2ccc(O)cc2)no1	10.1021/jm00004a012
	CHEMBL27248	104682	8	None	-	0	Rat	4.3	pIC50	=	4.3	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	254	3	2	5	1.5	Cc1cc(NS(=O)(=O)c2ccc(O)cc2)no1	10.1021/jm00004a012
	10815167	107970	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	497	7	2	6	5.4	CCC(C)c1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1	10.1021/jm9608366
	CHEMBL295697	107970	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	497	7	2	6	5.4	CCC(C)c1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1	10.1021/jm9608366
	23445313	172416	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor	ChEMBL	470	6	1	6	5.1	Cc1cc(C)c(OCc2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1	10.1016/S0960-894X(97)00132-7
	CHEMBL424371	172416	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor	ChEMBL	470	6	1	6	5.1	Cc1cc(C)c(OCc2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1	10.1016/S0960-894X(97)00132-7
	44279516	106627	0	None	-	0	Pig	6.3	pIC50	=	6.3	Binding	Binding affinity against ETA receptor in porcine aortic smooth muscle membraneBinding affinity against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	512	13	5	5	2.6	CC(C)C[C@H](NC(=O)Cc1cccs1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	CHEMBL285729	106627	0	None	-	0	Pig	6.3	pIC50	=	6.3	Binding	Binding affinity against ETA receptor in porcine aortic smooth muscle membraneBinding affinity against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	512	13	5	5	2.6	CC(C)C[C@H](NC(=O)Cc1cccs1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	CHEMBL96822	222699	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NS(C)(=O)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	10426645	169854	0	None	-	0	Rat	5.3	pIC50	=	5.3	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	328	4	1	4	3.8	Cc1noc(NS(=O)(=O)c2cccc(-c3ccccc3)c2)c1C	10.1021/jm00008a013
	CHEMBL417651	169854	0	None	-	0	Rat	5.3	pIC50	=	5.3	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	328	4	1	4	3.8	Cc1noc(NS(=O)(=O)c2cccc(-c3ccccc3)c2)c1C	10.1021/jm00008a013
	44291602	107957	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	515	8	2	10	3.6	COC(=O)c1cc(OC)cc(OC)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl	10.1021/jm9608366
	CHEMBL295632	107957	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	515	8	2	10	3.6	COC(=O)c1cc(OC)cc(OC)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl	10.1021/jm9608366
	44279409	106635	0	None	-	0	Pig	7.3	pIC50	=	7.3	Binding	Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	555	11	5	4	4.0	CC(C)C[C@H](NC(=O)N1CCCCCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	CHEMBL285782	106635	0	None	-	0	Pig	7.3	pIC50	=	7.3	Binding	Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	555	11	5	4	4.0	CC(C)C[C@H](NC(=O)N1CCCCCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	23445533	67186	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	454	6	1	5	5.0	Cc1ccc(CCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1	10.1016/S0960-894X(97)00133-9
	CHEMBL175045	67186	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	454	6	1	5	5.0	Cc1ccc(CCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1	10.1016/S0960-894X(97)00133-9
	18617354	212256	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	384	3	1	4	3.9	Cc1noc(NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1Br	10.1016/0960-894X(96)00441-6
	CHEMBL80507	212256	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	384	3	1	4	3.9	Cc1noc(NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1Br	10.1016/0960-894X(96)00441-6
	23445445	109437	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	377	5	2	6	3.4	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccccc2)c1C	10.1016/S0960-894X(97)00367-3
	CHEMBL304481	109437	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	377	5	2	6	3.4	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccccc2)c1C	10.1016/S0960-894X(97)00367-3
	127034917	143313	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	654	12	2	8	6.2	CCCc1nc2c(C)cc(C(=O)NCCN3CCCC3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	CHEMBL3736507	143313	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	654	12	2	8	6.2	CCCc1nc2c(C)cc(C(=O)NCCN3CCCC3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	44266628	11537	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	417	5	1	6	4.7	COc1cccc(-c2c(C(=O)O)n(-c3ccc4c(c3)OCO4)c3ccc(OC)cc23)c1	10.1016/0960-894X(96)00170-9
	CHEMBL10388	11537	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	417	5	1	6	4.7	COc1cccc(-c2c(C(=O)O)n(-c3ccc4c(c3)OCO4)c3ccc(OC)cc23)c1	10.1016/0960-894X(96)00170-9
	127035545	143147	0	None	-	0	Human	4.3	pIC50	=	4.3	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	721	14	2	9	7.4	CCCc1nc2c(C)cc(C(=O)NCCc3ccc(OC)c(OC)c3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	CHEMBL3734955	143147	0	None	-	0	Human	4.3	pIC50	=	4.3	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	721	14	2	9	7.4	CCCc1nc2c(C)cc(C(=O)NCCc3ccc(OC)c(OC)c3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	11797486	18815	1	None	-	0	Human	7.3	pIC50	=	7.3	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	442	6	2	8	3.5	Cc1noc(NS(=O)(=O)c2ccsc2C(O)Cc2ccc3c(c2)OCO3)c1Cl	10.1021/jm9700068
	CHEMBL1183448	18815	1	None	-	0	Human	7.3	pIC50	=	7.3	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	442	6	2	8	3.5	Cc1noc(NS(=O)(=O)c2ccsc2C(O)Cc2ccc3c(c2)OCO3)c1Cl	10.1021/jm9700068
	CHEMBL297557	18815	1	None	-	0	Human	7.3	pIC50	=	7.3	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	442	6	2	8	3.5	Cc1noc(NS(=O)(=O)c2ccsc2C(O)Cc2ccc3c(c2)OCO3)c1Cl	10.1021/jm9700068
	44279325	118402	0	None	-	0	Pig	6.3	pIC50	=	6.3	Binding	Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	501	12	6	4	2.5	CC(C)C[C@H](NC(=O)NCC(C)(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	CHEMBL32845	118402	0	None	-	0	Pig	6.3	pIC50	=	6.3	Binding	Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	501	12	6	4	2.5	CC(C)C[C@H](NC(=O)NCC(C)(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	76326542	92117	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells	ChEMBL	504	7	1	6	5.2	CCn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c2ccccc21	10.1007/s00044-004-0021-y
	CHEMBL2261356	92117	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells	ChEMBL	504	7	1	6	5.2	CCn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c2ccccc21	10.1007/s00044-004-0021-y
	10337624	106874	0	None	-	0	Rat	5.3	pIC50	=	5.3	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2cccc3ccc(N(C)C)cc23)c1C	10.1021/jm00008a013
	CHEMBL287451	106874	0	None	-	0	Rat	5.3	pIC50	=	5.3	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2cccc3ccc(N(C)C)cc23)c1C	10.1021/jm00008a013
	15340616	113611	0	None	-	0	Rat	5.3	pIC50	=	5.3	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	420	4	1	6	3.3	O=c1c(Cc2ccc3c(c2)OCO3)c(C(F)(F)F)[nH]n1Cc1ccc2c(c1)OCO2	10.1016/s0960-894x(00)00232-8
	CHEMBL3144602	113611	0	None	-	0	Rat	5.3	pIC50	=	5.3	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	420	4	1	6	3.3	O=c1c(Cc2ccc3c(c2)OCO3)c(C(F)(F)F)[nH]n1Cc1ccc2c(c1)OCO2	10.1016/s0960-894x(00)00232-8
	10337624	106874	0	None	-	0	Rat	5.3	pIC50	=	5.3	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2cccc3ccc(N(C)C)cc23)c1C	10.1021/jm00004a012
	CHEMBL287451	106874	0	None	-	0	Rat	5.3	pIC50	=	5.3	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2cccc3ccc(N(C)C)cc23)c1C	10.1021/jm00004a012
	CHEMBL137011	215522	0	None	-	0	Pig	5.3	pIC50	=	5.3	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)[C@@H]1NC(=O)[C@@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC1=O	10.1021/jm00021a021
	127034757	143173	0	None	-	0	Human	4.3	pIC50	=	4.3	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	679	12	2	7	7.5	CCCc1nc2c(C)cc(C(=O)NCCc3ccc(F)cc3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	CHEMBL3735265	143173	0	None	-	0	Human	4.3	pIC50	=	4.3	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	679	12	2	7	7.5	CCCc1nc2c(C)cc(C(=O)NCCc3ccc(F)cc3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	10185233	66836	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	497	8	2	8	3.8	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)ncnc1OCC#CCO	10.1016/s0960-894x(02)01084-3
	CHEMBL173721	66836	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	497	8	2	8	3.8	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)ncnc1OCC#CCO	10.1016/s0960-894x(02)01084-3
	44279145	117321	0	None	-	0	Pig	7.2	pIC50	=	7.2	Binding	Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	515	13	5	4	3.0	CC(C)C[C@H](NC(=O)N(C(C)C)C(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	CHEMBL32518	117321	0	None	-	0	Pig	7.2	pIC50	=	7.2	Binding	Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	515	13	5	4	3.0	CC(C)C[C@H](NC(=O)N(C(C)C)C(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	44295097	21535	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	604	13	1	9	7.0	COc1ccc(C(=O)/C(Cc2cc(OC(C)C)c(OC(C)C)c(OC(C)C)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1	10.1016/s0960-894x(98)00301-1
	CHEMBL1206461	21535	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	604	13	1	9	7.0	COc1ccc(C(=O)/C(Cc2cc(OC(C)C)c(OC(C)C)c(OC(C)C)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1	10.1016/s0960-894x(98)00301-1
	CHEMBL276362	21535	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	604	13	1	9	7.0	COc1ccc(C(=O)/C(Cc2cc(OC(C)C)c(OC(C)C)c(OC(C)C)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1	10.1016/s0960-894x(98)00301-1
	10621170	18012	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	402	5	2	8	3.0	Cc1cc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)no1	10.1021/jm9608366
	CHEMBL1178890	18012	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	402	5	2	8	3.0	Cc1cc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)no1	10.1021/jm9608366
	CHEMBL48120	18012	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	402	5	2	8	3.0	Cc1cc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)no1	10.1021/jm9608366
	CHEMBL149091	215565	0	None	-	0	Mouse	7.2	pIC50	=	7.2	Binding	Inhibition of [125I]ET1 binding to Endothelin A receptor of murine 3T3 cellsInhibition of [125I]ET1 binding to Endothelin A receptor of murine 3T3 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@H](C)CC	10.1016/S0960-894X(01)81219-1
	10549815	68388	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	416	8	1	4	5.0	COc1ccc(C/C(C(=O)c2ccc(OC)cc2)=C(/C(=O)O)c2ccc(C)cc2)cc1	10.1021/jm031041j
	CHEMBL177123	68388	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	416	8	1	4	5.0	COc1ccc(C/C(C(=O)c2ccc(OC)cc2)=C(/C(=O)O)c2ccc(C)cc2)cc1	10.1021/jm031041j
	10047521	15402	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	416	6	1	5	4.4	COc1ccc(CC2=C(c3ccc(C)cc3)C(=O)OC2(O)c2ccc(OC)cc2)cc1	10.1021/jm9606507
	CHEMBL10951	15402	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	416	6	1	5	4.4	COc1ccc(CC2=C(c3ccc(C)cc3)C(=O)OC2(O)c2ccc(OC)cc2)cc1	10.1021/jm9606507
	10815883	66358	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	522	9	5	4	4.3	Cc1[nH]c([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O	10.1021/jm950591h
	CHEMBL171855	66358	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	522	9	5	4	4.3	Cc1[nH]c([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O	10.1021/jm950591h
	10815883	66358	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	522	9	5	4	4.3	Cc1[nH]c([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O	10.1021/jm950592+
	CHEMBL171855	66358	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	522	9	5	4	4.3	Cc1[nH]c([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O	10.1021/jm950592+
	10043017	106057	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells	ChEMBL	342	4	1	4	4.3	C=C(C)c1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12	10.1021/jm00029a001
	CHEMBL281942	106057	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells	ChEMBL	342	4	1	4	4.3	C=C(C)c1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12	10.1021/jm00029a001
	10043017	106057	0	None	-	0	Rat	5.2	pIC50	=	5.2	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	342	4	1	4	4.3	C=C(C)c1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12	10.1021/jm00008a013
	CHEMBL281942	106057	0	None	-	0	Rat	5.2	pIC50	=	5.2	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	342	4	1	4	4.3	C=C(C)c1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12	10.1021/jm00008a013
	234762	106779	31	None	-	0	Rat	4.2	pIC50	=	4.2	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	256	3	2	6	0.9	Nc1ccc(S(=O)(=O)Nc2nncs2)cc1	10.1021/jm00008a013
	CHEMBL286737	106779	31	None	-	0	Rat	4.2	pIC50	=	4.2	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	256	3	2	6	0.9	Nc1ccc(S(=O)(=O)Nc2nncs2)cc1	10.1021/jm00008a013
	44332807	114012	0	None	-	0	Human	4.2	pIC50	=	4.2	Binding	Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells	ChEMBL	447	5	0	5	6.0	O=C(OCc1ccccc1)C(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12	10.1016/S0960-894X(96)00551-3
	CHEMBL316792	114012	0	None	-	0	Human	4.2	pIC50	=	4.2	Binding	Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells	ChEMBL	447	5	0	5	6.0	O=C(OCc1ccccc1)C(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12	10.1016/S0960-894X(96)00551-3
	10649086	182032	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	500	5	3	8	4.0	Cc1noc(NS(=O)(=O)c2ccsc2NC(=O)Nc2ccc3c(c2)OCO3)c1Br	10.1021/jm9700068
	CHEMBL45723	182032	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	500	5	3	8	4.0	Cc1noc(NS(=O)(=O)c2ccsc2NC(=O)Nc2ccc3c(c2)OCO3)c1Br	10.1021/jm9700068
	18995998	169170	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.	ChEMBL	523	9	1	9	5.3	COc1cccc(Sc2c(C(=O)O)n(Cc3cc(OC)c4c(c3)OCO4)c3cc(OC)c(OC)cc23)c1	10.1016/0960-894X(96)00232-6
	CHEMBL416570	169170	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.	ChEMBL	523	9	1	9	5.3	COc1cccc(Sc2c(C(=O)O)n(Cc3cc(OC)c4c(c3)OCO4)c3cc(OC)c(OC)cc23)c1	10.1016/0960-894X(96)00232-6
	44293631	174582	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	463	7	2	7	4.1	CCOc1ccc2c(c1)[C@H](c1ccc(OC)cc1O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	CHEMBL430572	174582	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	463	7	2	7	4.1	CCOc1ccc2c(c1)[C@H](c1ccc(OC)cc1O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	CHEMBL328942	218095	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm970161m
	44265858	174371	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	509	12	1	6	4.1	CCCCN(CCCC)C(=O)CN1CC(c2ccc3c(c2)OCO3)C(C(N)=O)C1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL430084	174371	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	509	12	1	6	4.1	CCCCN(CCCC)C(=O)CN1CC(c2ccc3c(c2)OCO3)C(C(N)=O)C1c1ccc(OC)cc1	10.1021/jm9505369
	44386144	68758	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	555	9	3	7	5.2	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)n2ccc3ccccc32)nc1C(=O)O	10.1021/jm950592+
	CHEMBL177431	68758	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	555	9	3	7	5.2	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)n2ccc3ccccc32)nc1C(=O)O	10.1021/jm950592+
	23445336	66950	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	468	6	1	5	5.3	Cc1cc(C)c(CCc2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1	10.1016/S0960-894X(97)00133-9
	CHEMBL173977	66950	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	468	6	1	5	5.3	Cc1cc(C)c(CCc2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1	10.1016/S0960-894X(97)00133-9
	CHEMBL2370070	216558	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCN)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00070a001
	CHEMBL216082	216096	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	10426645	169854	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	328	4	1	4	3.8	Cc1noc(NS(=O)(=O)c2cccc(-c3ccccc3)c2)c1C	10.1016/0960-894X(96)00441-6
	CHEMBL417651	169854	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	328	4	1	4	3.8	Cc1noc(NS(=O)(=O)c2cccc(-c3ccccc3)c2)c1C	10.1016/0960-894X(96)00441-6
	44279333	112997	0	None	-	0	Pig	6.2	pIC50	=	6.2	Binding	Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	513	11	5	4	2.6	CC(C)C[C@H](NC(=O)N1CCC(C)CC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	CHEMBL31388	112997	0	None	-	0	Pig	6.2	pIC50	=	6.2	Binding	Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	513	11	5	4	2.6	CC(C)C[C@H](NC(=O)N1CCC(C)CC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	44294580	21407	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	502	8	1	7	5.8	COc1ccc(C(=O)/C(Cc2ccc(OC(C)(C)C)cc2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1	10.1016/s0960-894x(98)00301-1
	CHEMBL1205104	21407	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	502	8	1	7	5.8	COc1ccc(C(=O)/C(Cc2ccc(OC(C)(C)C)cc2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1	10.1016/s0960-894x(98)00301-1
	CHEMBL52338	21407	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	502	8	1	7	5.8	COc1ccc(C(=O)/C(Cc2ccc(OC(C)(C)C)cc2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1	10.1016/s0960-894x(98)00301-1
	127034916	143178	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	668	12	2	8	6.6	CCCc1nc2c(C)cc(C(=O)NCCN3CCCCC3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	CHEMBL3735302	143178	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	668	12	2	8	6.6	CCCc1nc2c(C)cc(C(=O)NCCN3CCCCC3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	CHEMBL432091	220411	0	None	-	0	Rat	4.2	pIC50	=	4.2	Binding	Compound was evaluated for the binding affinity to endothelin receptor in the rat heart ventricle.Compound was evaluated for the binding affinity to endothelin receptor in the rat heart ventricle.	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00087a001
	44384723	137665	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	563	13	2	10	3.0	CCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	CHEMBL368528	137665	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	563	13	2	10	3.0	CCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	9853025	66591	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	690	14	2	13	3.9	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCNS(=O)(=O)c1cccs1	10.1016/s0960-894x(02)01083-1
	CHEMBL172759	66591	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	690	14	2	13	3.9	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCNS(=O)(=O)c1cccs1	10.1016/s0960-894x(02)01083-1
	44320212	113777	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	520	9	2	7	4.7	O=C(O)COc1ccccc1Cn1nc(-c2ccccc2)c(Cc2cc3c(cc2Cl)OCO3)c1C(=O)O	10.1016/s0960-894x(00)00513-8
	CHEMBL315280	113777	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	520	9	2	7	4.7	O=C(O)COc1ccccc1Cn1nc(-c2ccccc2)c(Cc2cc3c(cc2Cl)OCO3)c1C(=O)O	10.1016/s0960-894x(00)00513-8
	44386161	68050	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	573	9	1	9	5.6	CCC#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	CHEMBL176650	68050	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	573	9	1	9	5.6	CCC#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	18996000	106128	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.	ChEMBL	491	9	1	7	6.1	CCCOc1ccc2c(Sc3cccc(OC)c3)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2c1	10.1016/0960-894X(96)00232-6
	CHEMBL282398	106128	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.	ChEMBL	491	9	1	7	6.1	CCCOc1ccc2c(Sc3cccc(OC)c3)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2c1	10.1016/0960-894X(96)00232-6
	10476492	175971	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	407	6	2	5	4.9	Cc1noc(NS(=O)(=O)c2cccc3c(NCc4ccccc4)cccc23)c1C	10.1021/jm00008a013
	CHEMBL440653	175971	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	407	6	2	5	4.9	Cc1noc(NS(=O)(=O)c2cccc3c(NCc4ccccc4)cccc23)c1C	10.1021/jm00008a013
	CHEMBL343379	218478	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Inhibitory effect against Human Endothelin A receptorInhibitory effect against Human Endothelin A receptor	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC1=O	10.1021/jm00021a021
	15453209	211910	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	358	3	1	4	3.5	Cc1cc(C)c(S(=O)(=O)Nc2onc(C)c2Br)c(C)c1	10.1016/0960-894X(96)00441-6
	CHEMBL77962	211910	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	358	3	1	4	3.5	Cc1cc(C)c(S(=O)(=O)Nc2onc(C)c2Br)c(C)c1	10.1016/0960-894X(96)00441-6
	19347988	105660	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Compound was evaluated for the receptor binding activity in rabbit artery vascular smooth muscle cells expressing Endothelin A receptorCompound was evaluated for the receptor binding activity in rabbit artery vascular smooth muscle cells expressing Endothelin A receptor	ChEMBL	316	4	1	4	4.8	COc1cccc(Sc2c(C(=O)O)sc3ccccc23)c1	10.1016/0960-894X(96)00232-6
	CHEMBL27911	105660	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Compound was evaluated for the receptor binding activity in rabbit artery vascular smooth muscle cells expressing Endothelin A receptorCompound was evaluated for the receptor binding activity in rabbit artery vascular smooth muscle cells expressing Endothelin A receptor	ChEMBL	316	4	1	4	4.8	COc1cccc(Sc2c(C(=O)O)sc3ccccc23)c1	10.1016/0960-894X(96)00232-6
	10289348	16085	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	516	16	1	5	5.9	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(CCC)CCC	10.1021/jm980217s
	CHEMBL111023	16085	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	516	16	1	5	5.9	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(CCC)CCC	10.1021/jm980217s
	44215416	181859	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	649	11	2	13	5.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2ccnc(-c3noc(=S)[nH]3)c2)nc1OCC1CCCO1	10.1016/j.bmcl.2016.06.014
	CHEMBL4568468	181859	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	649	11	2	13	5.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2ccnc(-c3noc(=S)[nH]3)c2)nc1OCC1CCCO1	10.1016/j.bmcl.2016.06.014
	44212539	210872	0	None	-	1	Human	8.2	pIC50	=	8.2	Binding	Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes	ChEMBL	671	12	2	12	5.9	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCOC(=O)Nc1ccccn1	10.1016/j.bmcl.2016.06.014
	CHEMBL70203	210872	0	None	-	1	Human	8.2	pIC50	=	8.2	Binding	Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes	ChEMBL	671	12	2	12	5.9	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCOC(=O)Nc1ccccn1	10.1016/j.bmcl.2016.06.014
	10739431	66354	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	394	7	1	5	4.4	N#Cc1ccc(OCc2ccncc2)cc1OC(C(=O)O)c1ccccc1Cl	10.1021/jm990378b
	CHEMBL171844	66354	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	394	7	1	5	4.4	N#Cc1ccc(OCc2ccncc2)cc1OC(C(=O)O)c1ccccc1Cl	10.1021/jm990378b
	10740501	67056	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	414	7	1	6	4.8	Cc1ccccc1C(Oc1cc(OCc2ccc3ncoc3c2)ccc1C#N)C(=O)O	10.1021/jm990378b
	CHEMBL174235	67056	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	414	7	1	6	4.8	Cc1ccccc1C(Oc1cc(OCc2ccc3ncoc3c2)ccc1C#N)C(=O)O	10.1021/jm990378b
	11799541	188048	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	499	8	3	9	3.4	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2CCCO)OCO3)c1Cl	10.1021/jm9608366
	CHEMBL47620	188048	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	499	8	3	9	3.4	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2CCCO)OCO3)c1Cl	10.1021/jm9608366
	44212539	210872	0	None	-	1	Human	8.2	pIC50	=	8.2	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	671	12	2	12	5.9	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	CHEMBL70203	210872	0	None	-	1	Human	8.2	pIC50	=	8.2	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	671	12	2	12	5.9	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	44311135	210969	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	607	11	2	10	5.7	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	CHEMBL70800	210969	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	607	11	2	10	5.7	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	44293720	189265	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	551	11	2	9	3.9	CCOc1ccc2c(c1)[C@@H](c1ccc(OC)c(OC)c1OCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	CHEMBL47868	189265	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	551	11	2	9	3.9	CCOc1ccc2c(c1)[C@@H](c1ccc(OC)c(OC)c1OCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	10554539	108020	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	543	9	2	11	3.4	CC(=O)OCCOc1cc2c(cc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2	10.1021/jm9608366
	CHEMBL296129	108020	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	543	9	2	11	3.4	CC(=O)OCCOc1cc2c(cc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2	10.1021/jm9608366
	137647152	164429	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	581	10	2	9	4.8	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(OCC(C)C)ccc31)OCO2	10.1016/j.bmcl.2017.04.049
	CHEMBL4081426	164429	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	581	10	2	9	4.8	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(OCC(C)C)ccc31)OCO2	10.1016/j.bmcl.2017.04.049
	10429404	111655	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	372	5	1	4	3.7	CCc1ccc(CC)c(S(=O)(=O)Nc2onc(C)c2Br)c1	10.1016/0960-894X(96)00441-6
	CHEMBL311138	111655	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	372	5	1	4	3.7	CCc1ccc(CC)c(S(=O)(=O)Nc2onc(C)c2Br)c1	10.1016/0960-894X(96)00441-6
	44320315	113834	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	496	7	2	7	5.0	O=C(O)c1cccc(Cn2nc(-c3cccs3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)c1	10.1016/s0960-894x(00)00513-8
	CHEMBL315638	113834	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	496	7	2	7	5.0	O=C(O)c1cccc(Cn2nc(-c3cccs3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)c1	10.1016/s0960-894x(00)00513-8
	11006147	19200	0	None	-	0	Pig	8.2	pIC50	=	8.2	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	550	11	2	10	4.7	COc1cccc(Oc2c(NCCOc3ncccn3)ncnc2NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1	10.1021/jm0102304
	CHEMBL1185931	19200	0	None	-	0	Pig	8.2	pIC50	=	8.2	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	550	11	2	10	4.7	COc1cccc(Oc2c(NCCOc3ncccn3)ncnc2NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1	10.1021/jm0102304
	CHEMBL442031	19200	0	None	-	0	Pig	8.2	pIC50	=	8.2	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	550	11	2	10	4.7	COc1cccc(Oc2c(NCCOc3ncccn3)ncnc2NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1	10.1021/jm0102304
	2809510	136084	5	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Inhibition of [125]ET-1 binding to human Endothelin A receptor expressed in vero cellsInhibition of [125]ET-1 binding to human Endothelin A receptor expressed in vero cells	ChEMBL	362	5	1	7	2.8	COC(=O)c1cc(S(=O)(=O)Nc2cccc(-c3cnco3)c2)oc1C	10.1021/jm031041j
	CHEMBL367093	136084	5	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Inhibition of [125]ET-1 binding to human Endothelin A receptor expressed in vero cellsInhibition of [125]ET-1 binding to human Endothelin A receptor expressed in vero cells	ChEMBL	362	5	1	7	2.8	COC(=O)c1cc(S(=O)(=O)Nc2cccc(-c3cnco3)c2)oc1C	10.1021/jm031041j
	10531650	175040	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	600	11	1	7	5.0	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)c1ccc(Cl)cc1	10.1021/jm970101g
	CHEMBL433842	175040	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	600	11	1	7	5.0	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)c1ccc(Cl)cc1	10.1021/jm970101g
	10918533	109620	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	536	8	1	6	6.8	CC(C)Oc1ccc2c(c1)C(c1ccc(OCc3ccccc3)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	CHEMBL305577	109620	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	536	8	1	6	6.8	CC(C)Oc1ccc2c(c1)C(c1ccc(OCc3ccccc3)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	52949155	25183	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer	ChEMBL	557	10	2	7	5.4	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC(C)C)ccc31)OCO2	10.1016/j.bmcl.2010.08.074
	CHEMBL1271640	25183	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer	ChEMBL	557	10	2	7	5.4	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC(C)C)ccc31)OCO2	10.1016/j.bmcl.2010.08.074
	44315008	109608	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Binding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranesBinding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranes	ChEMBL	665	13	5	5	4.7	CCSCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1021/jm9600914
	CHEMBL305524	109608	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Binding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranesBinding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranes	ChEMBL	665	13	5	5	4.7	CCSCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1021/jm9600914
	44458604	105389	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	559	6	2	7	3.7	Cn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(F)(F)F)cc2)c2ccc3c(c2)OCO3)c2ccc(C(N)=O)cc21	10.1016/s0960-894x(01)00660-6
	CHEMBL276982	105389	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	559	6	2	7	3.7	Cn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(F)(F)F)cc2)c2ccc3c(c2)OCO3)c2ccc(C(N)=O)cc21	10.1016/s0960-894x(01)00660-6
	10239569	21560	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	534	9	1	10	4.4	COc1cc(C/C(C(=O)c2ccc3c(c2)OCO3)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC	10.1016/s0960-894x(98)00301-1
	CHEMBL1206715	21560	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	534	9	1	10	4.4	COc1cc(C/C(C(=O)c2ccc3c(c2)OCO3)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC	10.1016/s0960-894x(98)00301-1
	CHEMBL299328	21560	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	534	9	1	10	4.4	COc1cc(C/C(C(=O)c2ccc3c(c2)OCO3)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC	10.1016/s0960-894x(98)00301-1
	52943105	25251	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	529	9	2	7	4.7	CCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2	10.1016/j.bmcl.2017.04.049
	CHEMBL1272190	25251	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	529	9	2	7	4.7	CCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2	10.1016/j.bmcl.2017.04.049
	52943105	25251	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer	ChEMBL	529	9	2	7	4.7	CCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2	10.1016/j.bmcl.2010.08.074
	CHEMBL1272190	25251	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer	ChEMBL	529	9	2	7	4.7	CCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2	10.1016/j.bmcl.2010.08.074
	10137382	188963	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	427	5	3	7	3.8	Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(O)c1	10.1021/jm9608366
	CHEMBL47827	188963	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	427	5	3	7	3.8	Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(O)c1	10.1021/jm9608366
	10527706	103776	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	454	8	1	6	3.1	CCCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL266594	103776	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	454	8	1	6	3.1	CCCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	10671037	138222	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	446	8	1	6	4.4	COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1	10.1021/jm031041j
	CHEMBL273660	138222	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	446	8	1	6	4.4	COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1	10.1021/jm031041j
	CHEMBL369085	138222	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	446	8	1	6	4.4	COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1	10.1021/jm031041j
	10503525	12639	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	446	6	1	7	3.8	COc1ccc(C2(O)OC(=O)C(c3cc(OC)c4c(c3)OCO4)=C2Cc2ccccc2)cc1	10.1021/jm9606507
	CHEMBL10794	12639	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	446	6	1	7	3.8	COc1ccc(C2(O)OC(=O)C(c3cc(OC)c4c(c3)OCO4)=C2Cc2ccccc2)cc1	10.1021/jm9606507
	44314609	211527	0	None	-	0	Pig	8.2	pIC50	=	8.2	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	720	12	6	4	5.6	CC(C)CC(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)N[C@H](Cc1c(Br)[nH]c2ccccc12)C(=O)NC(Cc1c[nH]c2ccccc12)C(=O)O	10.1021/jm9600914
	CHEMBL74471	211527	0	None	-	0	Pig	8.2	pIC50	=	8.2	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	720	12	6	4	5.6	CC(C)CC(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)N[C@H](Cc1c(Br)[nH]c2ccccc12)C(=O)NC(Cc1c[nH]c2ccccc12)C(=O)O	10.1021/jm9600914
	71460535	88460	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	693	15	1	12	5.1	COc1ccccc1Oc1c(NS(=O)(=O)CCCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1	10.1021/jm3009103
	CHEMBL2163711	88460	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	693	15	1	12	5.1	COc1ccccc1Oc1c(NS(=O)(=O)CCCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1	10.1021/jm3009103
	11826259	209684	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	437	8	1	7	4.5	CC(C)Oc1ccc2c(c1)C(OCCCC#N)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	CHEMBL62759	209684	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	437	8	1	7	4.5	CC(C)Oc1ccc2c(c1)C(OCCCC#N)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	71455139	88778	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	556	11	2	8	3.6	O=S(=O)(NCc1ccccc1)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccccc1	10.1021/jm3009103
	CHEMBL2165331	88778	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	556	11	2	8	3.6	O=S(=O)(NCc1ccccc1)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccccc1	10.1021/jm3009103
	10697883	18011	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	548	8	3	10	2.5	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2CNS(C)(=O)=O)OCO3)c1Cl	10.1021/jm9608366
	CHEMBL1178885	18011	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	548	8	3	10	2.5	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2CNS(C)(=O)=O)OCO3)c1Cl	10.1021/jm9608366
	CHEMBL47828	18011	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	548	8	3	10	2.5	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2CNS(C)(=O)=O)OCO3)c1Cl	10.1021/jm9608366
	21979601	88775	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)	ChEMBL	602	13	2	10	3.7	COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)ncnc1OCCOc1ncc(Br)cn1	10.1016/j.bmcl.2016.06.014
	CHEMBL2165328	88775	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)	ChEMBL	602	13	2	10	3.7	COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)ncnc1OCCOc1ncc(Br)cn1	10.1016/j.bmcl.2016.06.014
	71462248	88478	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	676	17	2	12	3.8	COCCOc1nc(NS(=O)(=O)NCc2ccccc2)c(Oc2ccccc2OC)c(OCCOc2ncc(Br)cn2)n1	10.1021/jm3009103
	CHEMBL2163728	88478	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	676	17	2	12	3.8	COCCOc1nc(NS(=O)(=O)NCc2ccccc2)c(Oc2ccccc2OC)c(OCCOc2ncc(Br)cn2)n1	10.1021/jm3009103
	21979601	88775	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	602	13	2	10	3.7	COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)ncnc1OCCOc1ncc(Br)cn1	10.1021/jm3009103
	CHEMBL2165328	88775	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	602	13	2	10	3.7	COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)ncnc1OCCOc1ncc(Br)cn1	10.1021/jm3009103
	10360201	102461	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	345	4	1	5	3.3	Cc1onc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C	10.1021/jm00008a013
	CHEMBL25816	102461	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	345	4	1	5	3.3	Cc1onc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C	10.1021/jm00008a013
	9974857	104169	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	345	5	2	5	3.7	CCNc1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12	10.1021/jm00008a013
	CHEMBL26978	104169	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	345	5	2	5	3.7	CCNc1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12	10.1021/jm00008a013
	CHEMBL1788127	217895	8	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00070a001
	CHEMBL313760	217895	8	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00070a001
	10506868	70031	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	550	10	5	5	4.7	Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCCC2)nc1C(=O)O	10.1021/jm950592+
	CHEMBL179138	70031	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	550	10	5	5	4.7	Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCCC2)nc1C(=O)O	10.1021/jm950592+
	44266594	10973	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	491	8	1	8	4.8	COc1ccc(-c2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc(OC)c(OC)cc23)cc1OC	10.1016/0960-894X(96)00170-9
	CHEMBL10019	10973	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	491	8	1	8	4.8	COc1ccc(-c2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc(OC)c(OC)cc23)cc1OC	10.1016/0960-894X(96)00170-9
	44266646	105341	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	475	6	1	8	4.5	COc1cc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC	10.1016/0960-894X(96)00170-9
	CHEMBL276638	105341	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	475	6	1	8	4.5	COc1cc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC	10.1016/0960-894X(96)00170-9
	10577879	16041	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	520	9	0	9	4.5	COc1ccc(C2(OC)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1	10.1021/jm9606507
	CHEMBL11082	16041	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	520	9	0	9	4.5	COc1ccc(C2(OC)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1	10.1021/jm9606507
	345351	16131	4	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	386	4	1	5	3.8	O=C1OC(O)(c2ccccc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2	10.1021/jm9606507
	CHEMBL11131	16131	4	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	386	4	1	5	3.8	O=C1OC(O)(c2ccccc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2	10.1021/jm9606507
	10763444	118424	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	399	7	1	5	5.0	O=C(O)/C(=C/c1cc(OCc2ccsc2)ccc1[N+](=O)[O-])c1ccccc1F	10.1021/jm970847e
	CHEMBL328580	118424	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	399	7	1	5	5.0	O=C(O)/C(=C/c1cc(OCc2ccsc2)ccc1[N+](=O)[O-])c1ccccc1F	10.1021/jm970847e
	10597928	119542	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	414	6	1	3	5.9	Cc1ccccc1/C(=C\c1cc(OCc2ccsc2)ccc1Br)CO	10.1021/jm970847e
	CHEMBL330543	119542	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	414	6	1	3	5.9	Cc1ccccc1/C(=C\c1cc(OCc2ccsc2)ccc1Br)CO	10.1021/jm970847e
	10690863	213642	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	375	7	1	4	4.8	O=C(O)/C(=C/c1cc(OCc2ccccc2)ccc1[N+](=O)[O-])c1ccccc1	10.1021/jm970847e
	CHEMBL90666	213642	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	375	7	1	4	4.8	O=C(O)/C(=C/c1cc(OCc2ccccc2)ccc1[N+](=O)[O-])c1ccccc1	10.1021/jm970847e
	44277263	113614	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	440	5	1	5	4.2	COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3cc4c(cc3Cl)OCO4)c2=O)c1	10.1016/s0960-894x(00)00232-8
	CHEMBL3144605	113614	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	440	5	1	5	4.2	COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3cc4c(cc3Cl)OCO4)c2=O)c1	10.1016/s0960-894x(00)00232-8
	10403526	108662	1	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	317	3	2	5	2.8	Cc1noc(NS(=O)(=O)c2ccc3cc(N)ccc3c2)c1C	10.1021/jm00004a012
	CHEMBL30075	108662	1	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	317	3	2	5	2.8	Cc1noc(NS(=O)(=O)c2ccc3cc(N)ccc3c2)c1C	10.1021/jm00004a012
	44270522	52580	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells	ChEMBL	744	15	1	10	8.2	CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)NS(=O)(=O)c1ccc(CC(C)C)s1)c1ccc2c(c1)OCO2	10.1016/0960-894X(95)00186-W
	CHEMBL15310	52580	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells	ChEMBL	744	15	1	10	8.2	CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)NS(=O)(=O)c1ccc(CC(C)C)s1)c1ccc2c(c1)OCO2	10.1016/0960-894X(95)00186-W
	44368390	52080	0	None	-	0	Pig	5.2	pIC50	=	5.2	Binding	Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.	ChEMBL	475	9	2	6	3.9	COc1ccc(CN(C(=O)/C=C/c2ccc3c(c2)OCO3)C(Cc2ccc(O)cc2)C(=O)O)cc1	10.1016/s0960-894x(01)00009-9
	CHEMBL152654	52080	0	None	-	0	Pig	5.2	pIC50	=	5.2	Binding	Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.	ChEMBL	475	9	2	6	3.9	COc1ccc(CN(C(=O)/C=C/c2ccc3c(c2)OCO3)C(Cc2ccc(O)cc2)C(=O)O)cc1	10.1016/s0960-894x(01)00009-9
	14673588	11179	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Compound was evaluated for binding affinity against rabbit Endothelin A receptorCompound was evaluated for binding affinity against rabbit Endothelin A receptor	ChEMBL	342	6	1	4	5.0	CC(C)Oc1c(C(=O)O)sc2ccc(OCc3ccccc3)cc12	10.1016/0960-894X(96)00170-9
	CHEMBL10143	11179	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Compound was evaluated for binding affinity against rabbit Endothelin A receptorCompound was evaluated for binding affinity against rabbit Endothelin A receptor	ChEMBL	342	6	1	4	5.0	CC(C)Oc1c(C(=O)O)sc2ccc(OCc3ccccc3)cc12	10.1016/0960-894X(96)00170-9
	14673588	11179	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Compound was evaluated for the receptor binding activity in rabbit artery vascular smooth muscle cells expressing Endothelin A receptorCompound was evaluated for the receptor binding activity in rabbit artery vascular smooth muscle cells expressing Endothelin A receptor	ChEMBL	342	6	1	4	5.0	CC(C)Oc1c(C(=O)O)sc2ccc(OCc3ccccc3)cc12	10.1016/0960-894X(96)00232-6
	CHEMBL10143	11179	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Compound was evaluated for the receptor binding activity in rabbit artery vascular smooth muscle cells expressing Endothelin A receptorCompound was evaluated for the receptor binding activity in rabbit artery vascular smooth muscle cells expressing Endothelin A receptor	ChEMBL	342	6	1	4	5.0	CC(C)Oc1c(C(=O)O)sc2ccc(OCc3ccccc3)cc12	10.1016/0960-894X(96)00232-6
	10735178	213980	0	None	-	0	Rat	5.2	pIC50	=	5.2	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	330	6	1	2	4.9	O=C(O)/C(=C/c1cccc(OCc2ccccc2)c1)c1ccccc1	10.1021/jm970847e
	CHEMBL92607	213980	0	None	-	0	Rat	5.2	pIC50	=	5.2	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	330	6	1	2	4.9	O=C(O)/C(=C/c1cccc(OCc2ccccc2)c1)c1ccccc1	10.1021/jm970847e
	22998396	107591	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	398	4	1	5	4.3	Cc1noc(NS(=O)(=O)c2ccsc2-c2ccccc2)c1Br	10.1016/S0960-894X(96)00496-9
	CHEMBL293232	107591	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	398	4	1	5	4.3	Cc1noc(NS(=O)(=O)c2ccsc2-c2ccccc2)c1Br	10.1016/S0960-894X(96)00496-9
	22998396	107591	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	398	4	1	5	4.3	Cc1noc(NS(=O)(=O)c2ccsc2-c2ccccc2)c1Br	10.1016/S0960-894X(97)00367-3
	CHEMBL293232	107591	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	398	4	1	5	4.3	Cc1noc(NS(=O)(=O)c2ccsc2-c2ccccc2)c1Br	10.1016/S0960-894X(97)00367-3
	10685758	209889	2	None	-	0	Human	5.2	pIC50	=	5.2	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	302	4	2	6	1.9	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)O)c1C	10.1016/S0960-894X(97)00367-3
	CHEMBL64006	209889	2	None	-	0	Human	5.2	pIC50	=	5.2	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	302	4	2	6	1.9	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)O)c1C	10.1016/S0960-894X(97)00367-3
	192311	114051	4	None	-	1	Pig	7.2	pIC50	=	7.2	Binding	Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	513	11	5	4	2.8	CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	CHEMBL31702	114051	4	None	-	1	Pig	7.2	pIC50	=	7.2	Binding	Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	513	11	5	4	2.8	CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	10627805	23351	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	630	7	2	6	5.4	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(Br)cccc2Br)cc1	10.1021/jm990170q
	CHEMBL123926	23351	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	630	7	2	6	5.4	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(Br)cccc2Br)cc1	10.1021/jm990170q
	22467231	105067	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	515	6	1	7	4.5	CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(C#N)ccc23)cc1	10.1016/s0960-894x(01)00660-6
	CHEMBL274758	105067	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	515	6	1	7	4.5	CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(C#N)ccc23)cc1	10.1016/s0960-894x(01)00660-6
	52943235	24889	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer	ChEMBL	571	12	2	7	5.9	CCCCCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2	10.1016/j.bmcl.2010.08.074
	CHEMBL1269101	24889	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer	ChEMBL	571	12	2	7	5.9	CCCCCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2	10.1016/j.bmcl.2010.08.074
	44332803	11479	0	None	-	0	Human	4.2	pIC50	=	4.2	Binding	Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells	ChEMBL	335	3	0	5	3.6	COC(=O)C(c1ccc2c(c1)OCO2)c1cc(C)nc2ccccc12	10.1016/S0960-894X(96)00551-3
	CHEMBL103497	11479	0	None	-	0	Human	4.2	pIC50	=	4.2	Binding	Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells	ChEMBL	335	3	0	5	3.6	COC(=O)C(c1ccc2c(c1)OCO2)c1cc(C)nc2ccccc12	10.1016/S0960-894X(96)00551-3
	22998414	209795	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	422	5	1	9	3.1	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Oc2ccc3c(c2)OCO3)c1C	10.1016/S0960-894X(97)00367-3
	CHEMBL63290	209795	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	422	5	1	9	3.1	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Oc2ccc3c(c2)OCO3)c1C	10.1016/S0960-894X(97)00367-3
	9984393	66846	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.	ChEMBL	527	11	4	5	2.8	CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1cn(C)c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00144-I
	CHEMBL173808	66846	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.	ChEMBL	527	11	4	5	2.8	CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1cn(C)c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00144-I
	18617345	111981	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	384	3	1	4	3.9	Cc1noc(NS(=O)(=O)c2cc(Cl)cc(Cl)c2)c1Br	10.1016/0960-894X(96)00441-6
	CHEMBL311461	111981	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	384	3	1	4	3.9	Cc1noc(NS(=O)(=O)c2cc(Cl)cc(Cl)c2)c1Br	10.1016/0960-894X(96)00441-6
	10918216	209621	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	508	7	1	6	6.0	COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OCc4ccccc4)cc32)cc1	10.1021/jm010382z
	CHEMBL62450	209621	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	508	7	1	6	6.0	COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OCc4ccccc4)cc32)cc1	10.1021/jm010382z
	10576889	18008	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	485	6	3	7	3.6	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cccc(C(=O)O)c2)c1Br	10.1021/jm9608366
	CHEMBL1178864	18008	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	485	6	3	7	3.6	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cccc(C(=O)O)c2)c1Br	10.1021/jm9608366
	CHEMBL47008	18008	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	485	6	3	7	3.6	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cccc(C(=O)O)c2)c1Br	10.1021/jm9608366
	23445457	135802	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor	ChEMBL	470	6	1	6	5.1	Cc1cc(C)c(OCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1	10.1016/S0960-894X(97)00132-7
	CHEMBL367024	135802	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor	ChEMBL	470	6	1	6	5.1	Cc1cc(C)c(OCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1	10.1016/S0960-894X(97)00132-7
	23445304	138124	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	484	6	1	7	4.4	Cc1cc2c(cc1CCc1sccc1S(=O)(=O)Nc1onc(C)c1Br)OCO2	10.1016/S0960-894X(97)00133-9
	CHEMBL368780	138124	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	484	6	1	7	4.4	Cc1cc2c(cc1CCc1sccc1S(=O)(=O)Nc1onc(C)c1Br)OCO2	10.1016/S0960-894X(97)00133-9
	CHEMBL407771	219461	0	None	-	0	Pig	7.2	pIC50	=	7.2	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CCCC[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	18995989	107331	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.	ChEMBL	583	9	1	9	6.6	COc1cc2c(Sc3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OCc1ccccc1	10.1016/0960-894X(96)00232-6
	CHEMBL29147	107331	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.	ChEMBL	583	9	1	9	6.6	COc1cc2c(Sc3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OCc1ccccc1	10.1016/0960-894X(96)00232-6
	10711546	212255	7	None	-	1	Human	6.2	pIC50	=	6.2	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	330	3	1	4	2.9	Cc1noc(NS(=O)(=O)c2ccccc2Br)c1C	10.1016/0960-894X(96)00441-6
	CHEMBL80506	212255	7	None	-	1	Human	6.2	pIC50	=	6.2	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	330	3	1	4	2.9	Cc1noc(NS(=O)(=O)c2ccccc2Br)c1C	10.1016/0960-894X(96)00441-6
	44279360	113367	0	None	-	0	Pig	6.2	pIC50	=	6.2	Binding	Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	498	13	5	4	2.9	CC(C)C[C@H](NC(=O)CC1CCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	CHEMBL31426	113367	0	None	-	0	Pig	6.2	pIC50	=	6.2	Binding	Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	498	13	5	4	2.9	CC(C)C[C@H](NC(=O)CC1CCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	10602475	67144	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	537	9	3	6	4.6	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O	10.1021/jm950592+
	CHEMBL174658	67144	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	537	9	3	6	4.6	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O	10.1021/jm950592+
	44327585	168562	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL	992	26	9	8	5.7	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C1CCCCC1)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	CHEMBL414082	168562	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL	992	26	9	8	5.7	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C1CCCCC1)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	CHEMBL2304017	216252	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Binding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranesBinding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranes	ChEMBL		None	None	None		CSC(C)(C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc2c(C#N)[nH]c3ccccc23)NC(=O)[C@@H](C(C)C)NC1=O	10.1021/jm9600914
	44298324	202648	0	None	-	0	Rat	5.2	pIC50	=	5.2	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	448	7	2	7	4.4	COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CO)c1	10.1016/s0960-894x(00)00366-8
	CHEMBL55876	202648	0	None	-	0	Rat	5.2	pIC50	=	5.2	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	448	7	2	7	4.4	COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CO)c1	10.1016/s0960-894x(00)00366-8
	23445457	135802	0	None	-	0	Human	4.2	pIC50	=	4.2	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	470	6	1	6	5.1	Cc1cc(C)c(OCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1	10.1016/S0960-894X(97)00133-9
	CHEMBL367024	135802	0	None	-	0	Human	4.2	pIC50	=	4.2	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	470	6	1	6	5.1	Cc1cc(C)c(OCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1	10.1016/S0960-894X(97)00133-9
	44383537	66023	0	None	-	0	Human	4.2	pIC50	=	4.2	Binding	Tested for binding affinity towards human Endothelin A receptorTested for binding affinity towards human Endothelin A receptor	ChEMBL	388	4	2	5	3.4	C/C=C/C=C/C=C/C(=O)O[C@@H]1C=C2COC(O)[C@]2(O)[C@@]2(C)CCCC(C)(C)C12	10.1016/s0960-894x(00)00136-0
	CHEMBL170335	66023	0	None	-	0	Human	4.2	pIC50	=	4.2	Binding	Tested for binding affinity towards human Endothelin A receptorTested for binding affinity towards human Endothelin A receptor	ChEMBL	388	4	2	5	3.4	C/C=C/C=C/C=C/C(=O)O[C@@H]1C=C2COC(O)[C@]2(O)[C@@]2(C)CCCC(C)(C)C12	10.1016/s0960-894x(00)00136-0
	127036867	144160	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes	ChEMBL	614	11	3	8	5.7	CCCc1nc2c(C)cc(C(=O)NCc3cccc(OC)c3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1	10.1039/C5MD00169B
	CHEMBL3753134	144160	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes	ChEMBL	614	11	3	8	5.7	CCCc1nc2c(C)cc(C(=O)NCc3cccc(OC)c3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1	10.1039/C5MD00169B
	9896468	177448	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	Displacement of 125I-ET1 from ETA receptor in rat A7R5 cellsDisplacement of 125I-ET1 from ETA receptor in rat A7R5 cells	ChEMBL	703	13	2	10	6.7	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(N2CCOCC2)nc1OCCC(=O)Nc1ccccc1C(C)C	10.1016/j.bmcl.2016.06.014
	CHEMBL4451582	177448	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	Displacement of 125I-ET1 from ETA receptor in rat A7R5 cellsDisplacement of 125I-ET1 from ETA receptor in rat A7R5 cells	ChEMBL	703	13	2	10	6.7	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(N2CCOCC2)nc1OCCC(=O)Nc1ccccc1C(C)C	10.1016/j.bmcl.2016.06.014
	10646616	210545	3	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	436	5	1	6	3.3	COc1nc(Br)cnc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12	10.1021/jm9604585
	CHEMBL6800	210545	3	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	436	5	1	6	3.3	COc1nc(Br)cnc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12	10.1021/jm9604585
	10555208	19177	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	578	9	2	6	5.5	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)c2ccccc2C)cc1	10.1021/jm990171i
	CHEMBL1185774	19177	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	578	9	2	6	5.5	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)c2ccccc2C)cc1	10.1021/jm990171i
	CHEMBL432227	19177	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	578	9	2	6	5.5	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)c2ccccc2C)cc1	10.1021/jm990171i
	10740507	135822	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	414	7	1	4	4.9	CCc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1	10.1021/jm031041j
	CHEMBL367032	135822	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	414	7	1	4	4.9	CCc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1	10.1021/jm031041j
	10693110	105074	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	414	5	1	5	4.4	CCc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1	10.1021/jm9606507
	CHEMBL274805	105074	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	414	5	1	5	4.4	CCc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1	10.1021/jm9606507
	11733215	209915	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	459	6	1	6	4.6	COc1ccc(C2=C(C(N)=O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1	10.1021/jm010382z
	CHEMBL64127	209915	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	459	6	1	6	4.6	COc1ccc(C2=C(C(N)=O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1	10.1021/jm010382z
	44298409	201777	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	490	10	2	7	5.2	COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCCO)c1	10.1016/s0960-894x(00)00366-8
	CHEMBL54770	201777	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	490	10	2	7	5.2	COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCCO)c1	10.1016/s0960-894x(00)00366-8
	44383771	66622	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	371	7	1	6	4.5	N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1ccsc1	10.1021/jm990378b
	CHEMBL172879	66622	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	371	7	1	6	4.5	N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1ccsc1	10.1021/jm990378b
	10717923	105469	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	439	5	2	6	4.7	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1	10.1016/S0960-894X(97)00133-9
	CHEMBL277595	105469	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	439	5	2	6	4.7	Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1	10.1016/S0960-894X(97)00133-9
	10550094	209860	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	420	4	1	5	3.6	Cc1nc(Br)cnc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12	10.1021/jm9604585
	CHEMBL6382	209860	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	420	4	1	5	3.6	Cc1nc(Br)cnc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12	10.1021/jm9604585
	10740138	210869	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	406	4	1	5	3.3	CN(C)c1cccc2c(S(=O)(=O)Nc3cnc(Br)nc3)cccc12	10.1021/jm9604585
	CHEMBL7019	210869	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	406	4	1	5	3.3	CN(C)c1cccc2c(S(=O)(=O)Nc3cnc(Br)nc3)cccc12	10.1021/jm9604585
	44327890	148190	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL	985	26	9	8	5.5	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)c1ccccc1)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	CHEMBL384052	148190	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL	985	26	9	8	5.5	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)c1ccccc1)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	44298304	108332	0	None	-	0	Rat	5.2	pIC50	=	5.2	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	503	10	2	7	4.7	COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCC(N)=O)c1	10.1016/s0960-894x(00)00366-8
	CHEMBL298395	108332	0	None	-	0	Rat	5.2	pIC50	=	5.2	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	503	10	2	7	4.7	COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCC(N)=O)c1	10.1016/s0960-894x(00)00366-8
	10496523	210060	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	328	4	1	5	2.5	CN(C)c1cccc2c(S(=O)(=O)Nc3ncccn3)cccc12	10.1021/jm9604585
	CHEMBL6468	210060	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	328	4	1	5	2.5	CN(C)c1cccc2c(S(=O)(=O)Nc3ncccn3)cccc12	10.1021/jm9604585
	17869231	21398	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	548	11	1	9	5.5	COc1cc(C/C(C(=O)c2ccc(OC(C)C)cc2)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC	10.1016/s0960-894x(98)00301-1
	CHEMBL1205061	21398	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	548	11	1	9	5.5	COc1cc(C/C(C(=O)c2ccc(OC(C)C)cc2)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC	10.1016/s0960-894x(98)00301-1
	CHEMBL48315	21398	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	548	11	1	9	5.5	COc1cc(C/C(C(=O)c2ccc(OC(C)C)cc2)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC	10.1016/s0960-894x(98)00301-1
	9853077	66401	0	None	-	2	Human	7.2	pIC50	=	7.2	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	696	13	2	12	5.3	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCNS(=O)(=O)c1cccs1	10.1016/s0960-894x(02)01083-1
	CHEMBL172030	66401	0	None	-	2	Human	7.2	pIC50	=	7.2	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	696	13	2	12	5.3	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCNS(=O)(=O)c1cccs1	10.1016/s0960-894x(02)01083-1
	CHEMBL1791008	215693	0	None	-	0	Pig	7.2	pIC50	=	7.2	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC[C@@H](C)[C@@H]1NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC1=O	10.1021/jm00021a021
	44327238	114184	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	497	8	1	8	3.1	CCCc1ccc(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)n1	10.1016/S0960-894X(96)00617-8
	CHEMBL318017	114184	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes	ChEMBL	497	8	1	8	3.1	CCCc1ccc(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)n1	10.1016/S0960-894X(96)00617-8
	44277036	176996	0	None	-	0	Rat	4.2	pIC50	=	4.2	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	492	10	1	7	4.5	COc1cccc(Cn2nc(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2OCCCC(=O)O)c1	10.1016/s0960-894x(00)00232-8
	CHEMBL444545	176996	0	None	-	0	Rat	4.2	pIC50	=	4.2	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	492	10	1	7	4.5	COc1cccc(Cn2nc(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2OCCCC(=O)O)c1	10.1016/s0960-894x(00)00232-8
	44294712	21564	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	566	11	1	9	5.6	COc1cc(C/C(C(=O)c2ccc(OC(C)C)c(F)c2)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC	10.1016/s0960-894x(98)00301-1
	CHEMBL1206722	21564	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	566	11	1	9	5.6	COc1cc(C/C(C(=O)c2ccc(OC(C)C)c(F)c2)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC	10.1016/s0960-894x(98)00301-1
	CHEMBL300201	21564	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	566	11	1	9	5.6	COc1cc(C/C(C(=O)c2ccc(OC(C)C)c(F)c2)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC	10.1016/s0960-894x(98)00301-1
	11071689	16233	0	None	-	0	Pig	7.2	pIC50	=	7.2	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	549	11	1	8	5.8	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ccccc2)c1	10.1021/jm0102304
	CHEMBL111876	16233	0	None	-	0	Pig	7.2	pIC50	=	7.2	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	549	11	1	8	5.8	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ccccc2)c1	10.1021/jm0102304
	23445468	18004	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	459	5	3	9	2.4	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc(O)nn2)c1Br	10.1021/jm9608366
	CHEMBL1178818	18004	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	459	5	3	9	2.4	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc(O)nn2)c1Br	10.1021/jm9608366
	CHEMBL44615	18004	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	459	5	3	9	2.4	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc(O)nn2)c1Br	10.1021/jm9608366
	CHEMBL263295	217344	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1021/jm00015a003
	44279677	109003	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor	ChEMBL	478	2	2	3	4.0	O=C1c2cc(Br)ccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(Br)cc21	10.1016/0960-894X(95)00230-Q
	CHEMBL30297	109003	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor	ChEMBL	478	2	2	3	4.0	O=C1c2cc(Br)ccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(Br)cc21	10.1016/0960-894X(95)00230-Q
	CHEMBL147908	215560	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cellsDisplacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)81215-4
	23445412	109039	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	426	5	1	7	4.3	Cc1ccc(OC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1	10.1016/S0960-894X(97)00367-3
	CHEMBL303203	109039	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	426	5	1	7	4.3	Cc1ccc(OC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1	10.1016/S0960-894X(97)00367-3
	44385942	68150	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	551	10	4	6	4.9	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2C)nc1C(=O)O	10.1021/jm950592+
	CHEMBL176913	68150	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	551	10	4	6	4.9	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2C)nc1C(=O)O	10.1021/jm950592+
	10449431	106810	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells	ChEMBL	332	4	1	5	3.3	COc1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12	10.1021/jm00029a001
	CHEMBL28692	106810	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells	ChEMBL	332	4	1	5	3.3	COc1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12	10.1021/jm00029a001
	44276828	103547	0	None	-	0	Rat	5.2	pIC50	=	5.2	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	324	5	3	6	1.0	Cc1noc(NS(=O)(=O)c2ccc(NC(=O)CN)cc2)c1C	10.1021/jm00008a013
	CHEMBL26470	103547	0	None	-	0	Rat	5.2	pIC50	=	5.2	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	324	5	3	6	1.0	Cc1noc(NS(=O)(=O)c2ccc(NC(=O)CN)cc2)c1C	10.1021/jm00008a013
	10449431	106810	0	None	-	0	Rat	5.2	pIC50	=	5.2	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	332	4	1	5	3.3	COc1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12	10.1021/jm00008a013
	CHEMBL28692	106810	0	None	-	0	Rat	5.2	pIC50	=	5.2	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	332	4	1	5	3.3	COc1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12	10.1021/jm00008a013
	CHEMBL436884	220469	0	None	-	0	Rat	5.2	pIC50	=	5.2	Binding	In vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricleIn vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricle	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)80156-6
	44383537	66023	0	None	-	0	Human	4.2	pIC50	=	4.2	Binding	Tested for binding affinity towards rabbit Endothelin A receptorTested for binding affinity towards rabbit Endothelin A receptor	ChEMBL	388	4	2	5	3.4	C/C=C/C=C/C=C/C(=O)O[C@@H]1C=C2COC(O)[C@]2(O)[C@@]2(C)CCCC(C)(C)C12	10.1016/s0960-894x(00)00136-0
	CHEMBL170335	66023	0	None	-	0	Human	4.2	pIC50	=	4.2	Binding	Tested for binding affinity towards rabbit Endothelin A receptorTested for binding affinity towards rabbit Endothelin A receptor	ChEMBL	388	4	2	5	3.4	C/C=C/C=C/C=C/C(=O)O[C@@H]1C=C2COC(O)[C@]2(O)[C@@]2(C)CCCC(C)(C)C12	10.1016/s0960-894x(00)00136-0
	6450144	129339	8	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	Antagonist activity at endothelin A receptor in Wistar rat thoracic aorta strips assessed as inhibition of ET1-induced vasoconstriction preincubated for 5 mins followed by ET1 additionAntagonist activity at endothelin A receptor in Wistar rat thoracic aorta strips assessed as inhibition of ET1-induced vasoconstriction preincubated for 5 mins followed by ET1 addition	ChEMBL	632	5	3	6	8.1	CC1(C)CC[C@]2(C(=O)O)CC[C@]3(COC(=O)/C=C/c4ccc(O)c(O)c4)C(=CC[C@@H]4[C@@]5(C)CCC(=O)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]2C1	10.1016/j.bmc.2015.06.055
	CHEMBL3601500	129339	8	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	Antagonist activity at endothelin A receptor in Wistar rat thoracic aorta strips assessed as inhibition of ET1-induced vasoconstriction preincubated for 5 mins followed by ET1 additionAntagonist activity at endothelin A receptor in Wistar rat thoracic aorta strips assessed as inhibition of ET1-induced vasoconstriction preincubated for 5 mins followed by ET1 addition	ChEMBL	632	5	3	6	8.1	CC1(C)CC[C@]2(C(=O)O)CC[C@]3(COC(=O)/C=C/c4ccc(O)c(O)c4)C(=CC[C@@H]4[C@@]5(C)CCC(=O)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]2C1	10.1016/j.bmc.2015.06.055
	11728313	170054	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	368	6	1	5	4.2	CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21	10.1021/jm010382z
	CHEMBL418667	170054	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	368	6	1	5	4.2	CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21	10.1021/jm010382z
	CHEMBL2304008	216243	0	None	-	0	Pig	7.2	pIC50	=	7.2	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CSC(C)(C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc2c(Br)[nH]c3ccccc23)NC(=O)[C@@H](C(C)C)NC1=O	10.1021/jm9600914
	19363918	21408	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	474	7	1	8	4.4	COc1ccc(C(=O)/C(Cc2ccc3c(c2)OCO3)=C(\C(=O)O)c2ccc3nsnc3c2)cc1	10.1016/s0960-894x(98)00301-1
	CHEMBL1205106	21408	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	474	7	1	8	4.4	COc1ccc(C(=O)/C(Cc2ccc3c(c2)OCO3)=C(\C(=O)O)c2ccc3nsnc3c2)cc1	10.1016/s0960-894x(98)00301-1
	CHEMBL52535	21408	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	474	7	1	8	4.4	COc1ccc(C(=O)/C(Cc2ccc3c(c2)OCO3)=C(\C(=O)O)c2ccc3nsnc3c2)cc1	10.1016/s0960-894x(98)00301-1
	44293927	108795	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	507	9	1	8	4.4	CCOc1ccc2c(c1)[C@@H](c1cc(OC)c(OC)c(OC)c1)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	CHEMBL301723	108795	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	507	9	1	8	4.4	CCOc1ccc2c(c1)[C@@H](c1cc(OC)c(OC)c(OC)c1)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	135884434	137343	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	628	10	2	12	5.2	C#CCOc1nc(-c2ccnc(-c3noc(O)n3)c2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	CHEMBL368117	137343	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	628	10	2	12	5.2	C#CCOc1nc(-c2ccnc(-c3noc(O)n3)c2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	44386535	138143	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	549	10	4	6	4.9	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2cccc(F)c2)nc1C(=O)O	10.1021/jm950592+
	CHEMBL368853	138143	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	549	10	4	6	4.9	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2cccc(F)c2)nc1C(=O)O	10.1021/jm950592+
	10403526	108662	1	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	317	3	2	5	2.8	Cc1noc(NS(=O)(=O)c2ccc3cc(N)ccc3c2)c1C	10.1021/jm00008a013
	CHEMBL30075	108662	1	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	317	3	2	5	2.8	Cc1noc(NS(=O)(=O)c2ccc3cc(N)ccc3c2)c1C	10.1021/jm00008a013
	10815902	172990	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	523	10	5	5	4.6	Cc1oc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)nc1C(=O)O	10.1021/jm950592+
	CHEMBL426589	172990	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	523	10	5	5	4.6	Cc1oc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)nc1C(=O)O	10.1021/jm950592+
	44332578	11087	0	None	-	0	Human	4.2	pIC50	=	4.2	Binding	Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells	ChEMBL	413	3	0	5	5.6	CC(C)(C)OC(=O)C(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12	10.1016/S0960-894X(96)00551-3
	CHEMBL100874	11087	0	None	-	0	Human	4.2	pIC50	=	4.2	Binding	Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells	ChEMBL	413	3	0	5	5.6	CC(C)(C)OC(=O)C(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12	10.1016/S0960-894X(96)00551-3
	CHEMBL431874	220407	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1021/jm00070a001
	44279251	106837	0	None	-	0	Pig	5.2	pIC50	=	5.2	Binding	Binding affinity against ETA receptor in porcine aortic smooth muscle membraneBinding affinity against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	486	12	5	4	2.8	CC(C)C[C@H](NC(=O)CC(C)(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	CHEMBL287141	106837	0	None	-	0	Pig	5.2	pIC50	=	5.2	Binding	Binding affinity against ETA receptor in porcine aortic smooth muscle membraneBinding affinity against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	486	12	5	4	2.8	CC(C)C[C@H](NC(=O)CC(C)(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	10265127	103611	2	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	270	3	1	4	2.2	Cc1noc(NS(=O)(=O)c2ccc(F)cc2)c1C	10.1016/0960-894X(96)00441-6
	CHEMBL26522	103611	2	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	270	3	1	4	2.2	Cc1noc(NS(=O)(=O)c2ccc(F)cc2)c1C	10.1016/0960-894X(96)00441-6
	CHEMBL3301647	218108	0	None	-	0	Pig	5.2	pIC50	=	5.2	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)C[C@@H]1NC(=O)[C@@H](C(C)C)NC(=O)[C@@H]2CCCN2C(=O)[C@H](C(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	10880982	109543	0	None	-	0	Rat	4.2	pIC50	=	4.2	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	296	2	1	4	3.0	O=C(O)C1=Cc2ccccc2OC1c1ccc2c(c1)OCO2	10.1021/jm031041j
	CHEMBL305149	109543	0	None	-	0	Rat	4.2	pIC50	=	4.2	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	296	2	1	4	3.0	O=C(O)C1=Cc2ccccc2OC1c1ccc2c(c1)OCO2	10.1021/jm031041j
	10880982	109543	0	None	-	0	Rat	4.2	pIC50	=	4.2	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	296	2	1	4	3.0	O=C(O)C1=Cc2ccccc2OC1c1ccc2c(c1)OCO2	10.1021/jm010382z
	CHEMBL305149	109543	0	None	-	0	Rat	4.2	pIC50	=	4.2	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	296	2	1	4	3.0	O=C(O)C1=Cc2ccccc2OC1c1ccc2c(c1)OCO2	10.1021/jm010382z
	CHEMBL385492	219131	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1021/jm00015a003
	10737416	66498	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	363	7	1	5	4.2	Cc1ccccc1C(Oc1cc(OCc2ccoc2)ccc1C#N)C(=O)O	10.1021/jm990378b
	CHEMBL172412	66498	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	363	7	1	5	4.2	Cc1ccccc1C(Oc1cc(OCc2ccoc2)ccc1C#N)C(=O)O	10.1021/jm990378b
	44293526	108134	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	563	11	2	8	4.9	CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCC(C)(C)C(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	CHEMBL296974	108134	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	563	11	2	8	4.9	CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCC(C)(C)C(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	10336018	108885	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	318	3	2	5	3.0	Cc1noc(NS(=O)(=O)c2cccc3c(O)cccc23)c1C	10.1021/jm00004a012
	CHEMBL30228	108885	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	318	3	2	5	3.0	Cc1noc(NS(=O)(=O)c2cccc3c(O)cccc23)c1C	10.1021/jm00004a012
	22998438	209858	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	456	5	1	7	4.1	Cc1ccccc1OC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Br	10.1016/S0960-894X(97)00367-3
	CHEMBL63805	209858	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	456	5	1	7	4.1	Cc1ccccc1OC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Br	10.1016/S0960-894X(97)00367-3
	10602451	68527	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor	ChEMBL	536	11	3	6	5.1	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)CC2CCCCC2)nc1C(=O)O	10.1021/jm9505932
	CHEMBL177179	68527	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor	ChEMBL	536	11	3	6	5.1	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)CC2CCCCC2)nc1C(=O)O	10.1021/jm9505932
	1011	10125	29	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes	ChEMBL	609	12	3	10	4.8	OC[C@H](COc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ccc(cc1)OC)O	10.1016/j.bmcl.2016.06.014
	5312146	10125	29	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes	ChEMBL	609	12	3	10	4.8	OC[C@H](COc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ccc(cc1)OC)O	10.1016/j.bmcl.2016.06.014
	CHEMBL1628620	10125	29	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes	ChEMBL	609	12	3	10	4.8	OC[C@H](COc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ccc(cc1)OC)O	10.1016/j.bmcl.2016.06.014
	10531851	66526	0	None	-	0	Rat	4.2	pIC50	=	4.2	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	614	11	3	7	5.3	CC(C)C[C@H](NC(=O)N1CCCCCC1)c1nc(C(=O)N[C@H](Cc2ccccn2)C(=O)O)c(Cc2cn(C)c3ccccc23)o1	10.1021/jm950591h
	CHEMBL172506	66526	0	None	-	0	Rat	4.2	pIC50	=	4.2	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	614	11	3	7	5.3	CC(C)C[C@H](NC(=O)N1CCCCCC1)c1nc(C(=O)N[C@H](Cc2ccccn2)C(=O)O)c(Cc2cn(C)c3ccccc23)o1	10.1021/jm950591h
	10529715	213929	0	None	-	0	Rat	5.2	pIC50	=	5.2	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	510	12	1	6	4.7	CCCCN(CCCC)CC(=O)N1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL9228	213929	0	None	-	0	Rat	5.2	pIC50	=	5.2	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	510	12	1	6	4.7	CCCCN(CCCC)CC(=O)N1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	10694547	213854	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	443	10	1	7	2.9	COCCOCCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL9183	213854	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	443	10	1	7	2.9	COCCOCCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	10836835	103876	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	440	7	2	5	3.8	CCCCNC(=O)N1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL267483	103876	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	440	7	2	5	3.8	CCCCNC(=O)N1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	10599453	214051	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	ChEMBL	445	9	1	6	5.2	Cc1ccccc1[C@@H](CCC(=O)O)Oc1cc(OCc2ccc3c(c2)OCO3)ccc1C#N	10.1021/jm9707131
	CHEMBL93097	214051	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	ChEMBL	445	9	1	6	5.2	Cc1ccccc1[C@@H](CCC(=O)O)Oc1cc(OCc2ccc3c(c2)OCO3)ccc1C#N	10.1021/jm9707131
	5340	175509	106	None	-	0	Rat	4.2	pIC50	=	4.2	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	255	3	2	5	1.5	Nc1ccc(S(=O)(=O)Nc2nccs2)cc1	10.1021/jm00008a013
	CHEMBL437	175509	106	None	-	0	Rat	4.2	pIC50	=	4.2	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	255	3	2	5	1.5	Nc1ccc(S(=O)(=O)Nc2nccs2)cc1	10.1021/jm00008a013
	5340	175509	106	None	-	0	Human	4.2	pIC50	=	4.2	Binding	Inhibitory concentration against Endothelin A receptorInhibitory concentration against Endothelin A receptor	ChEMBL	255	3	2	5	1.5	Nc1ccc(S(=O)(=O)Nc2nccs2)cc1	10.1021/jm030480f
	CHEMBL437	175509	106	None	-	0	Human	4.2	pIC50	=	4.2	Binding	Inhibitory concentration against Endothelin A receptorInhibitory concentration against Endothelin A receptor	ChEMBL	255	3	2	5	1.5	Nc1ccc(S(=O)(=O)Nc2nccs2)cc1	10.1021/jm030480f
	18995991	107076	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.	ChEMBL	537	8	1	10	5.0	COc1cc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc4c(cc23)OCO4)cc(OC)c1OC	10.1016/0960-894X(96)00232-6
	CHEMBL28920	107076	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.	ChEMBL	537	8	1	10	5.0	COc1cc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc4c(cc23)OCO4)cc(OC)c1OC	10.1016/0960-894X(96)00232-6
	10649585	116550	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	518	14	1	7	3.9	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCCC1OCCO1	10.1021/jm980217s
	CHEMBL323175	116550	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	518	14	1	7	3.9	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCCC1OCCO1	10.1021/jm980217s
	22574723	22710	0	None	-	1	Human	8.2	pIC50	=	8.2	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	549	11	2	7	5.2	CCCc1nc(CC)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(CC)c1	10.1039/C4MD00499J
	CHEMBL12233	22710	0	None	-	1	Human	8.2	pIC50	=	8.2	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	549	11	2	7	5.2	CCCc1nc(CC)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(CC)c1	10.1039/C4MD00499J
	20747575	105200	0	None	-	1	Human	8.2	pIC50	=	8.2	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	579	12	2	8	5.0	CCCc1nc(CC)c(C(=O)NC)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(COC)c1	10.1039/C4MD00499J
	CHEMBL275545	105200	0	None	-	1	Human	8.2	pIC50	=	8.2	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	579	12	2	8	5.0	CCCc1nc(CC)c(C(=O)NC)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(COC)c1	10.1039/C4MD00499J
	71455064	88471	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	694	14	1	12	4.5	COc1ccccc1Oc1c(NS(=O)(=O)N(C)Cc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1	10.1021/jm3009103
	CHEMBL2163721	88471	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	694	14	1	12	4.5	COc1ccccc1Oc1c(NS(=O)(=O)N(C)Cc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1	10.1021/jm3009103
	10693270	66843	1	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	417	7	1	6	4.4	Cc1ccccc1C(Oc1cc(OCc2ccc3c(c2)OCO3)ccc1C#N)C(=O)O	10.1021/jm990378b
	CHEMBL172144	66843	1	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	417	7	1	6	4.4	Cc1ccccc1C(Oc1cc(OCc2ccc3c(c2)OCO3)ccc1C#N)C(=O)O	10.1021/jm990378b
	CHEMBL173792	66843	1	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	417	7	1	6	4.4	Cc1ccccc1C(Oc1cc(OCc2ccc3c(c2)OCO3)ccc1C#N)C(=O)O	10.1021/jm990378b
	10601191	119581	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	ChEMBL	492	11	3	6	5.7	Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1-c1cc(C(=O)O)[nH]n1	10.1021/jm9707131
	CHEMBL330679	119581	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	ChEMBL	492	11	3	6	5.7	Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1-c1cc(C(=O)O)[nH]n1	10.1021/jm9707131
	22010244	213580	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	ChEMBL	407	9	1	5	5.5	Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1C#N	10.1021/jm9707131
	CHEMBL90320	213580	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	ChEMBL	407	9	1	5	5.5	Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1C#N	10.1021/jm9707131
	10740214	214083	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	ChEMBL	408	9	1	6	4.9	Cc1ccccc1[C@@H](CCC(=O)O)Oc1cc(OCc2cnsc2)ccc1C#N	10.1021/jm9707131
	CHEMBL93331	214083	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	ChEMBL	408	9	1	6	4.9	Cc1ccccc1[C@@H](CCC(=O)O)Oc1cc(OCc2cnsc2)ccc1C#N	10.1021/jm9707131
	10190108	137476	0	None	-	1	Human	8.2	pIC50	=	8.2	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	681	12	2	12	5.7	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccncc2)nc1OCC#CCOC(=O)Nc1ccccn1	10.1016/s0960-894x(02)01084-3
	CHEMBL368386	137476	0	None	-	1	Human	8.2	pIC50	=	8.2	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	681	12	2	12	5.7	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccncc2)nc1OCC#CCOC(=O)Nc1ccccn1	10.1016/s0960-894x(02)01084-3
	44333887	115402	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	446	7	2	6	3.9	CCNCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(02)00663-7
	CHEMBL320631	115402	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	446	7	2	6	3.9	CCNCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(02)00663-7
	44311528	210921	0	None	-	1	Human	8.2	pIC50	=	8.2	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	633	12	2	10	6.3	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C2CC2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	CHEMBL70487	210921	0	None	-	1	Human	8.2	pIC50	=	8.2	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	633	12	2	10	6.3	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C2CC2)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	44311284	211024	0	None	-	1	Human	8.2	pIC50	=	8.2	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	635	12	2	10	6.5	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C(C)C)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	CHEMBL71070	211024	0	None	-	1	Human	8.2	pIC50	=	8.2	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	635	12	2	10	6.5	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C(C)C)nc1OCCOC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	137642741	165018	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	553	9	2	9	4.2	CCOc1ccc2c(c1)c(=O)c(Cc1cccc(-c3nnn[nH]3)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2	10.1016/j.bmcl.2017.04.049
	CHEMBL4088349	165018	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	553	9	2	9	4.2	CCOc1ccc2c(c1)c(=O)c(Cc1cccc(-c3nnn[nH]3)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2	10.1016/j.bmcl.2017.04.049
	10224228	186391	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	424	6	1	6	4.5	Cc1ccc(C)c(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c1	10.1021/jm9700068
	CHEMBL47424	186391	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	424	6	1	6	4.5	Cc1ccc(C)c(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c1	10.1021/jm9700068
	101039204	165706	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	610	7	6	6	0.8	CC(C)C[C@@H]1NC(=O)[C@@H](C(C)C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2017.04.049
	CHEMBL4095638	165706	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	610	7	6	6	0.8	CC(C)C[C@@H]1NC(=O)[C@@H](C(C)C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2017.04.049
	11742628	105011	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	416	5	1	6	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1	10.1021/jm9606507
	CHEMBL274383	105011	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	416	5	1	6	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1	10.1021/jm9606507
	9845967	17865	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells	ChEMBL	416	7	1	5	4.4	COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1	10.1016/S0960-894X(97)00002-4
	CHEMBL10801	17865	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells	ChEMBL	416	7	1	5	4.4	COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1	10.1016/S0960-894X(97)00002-4
	CHEMBL1178000	17865	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells	ChEMBL	416	7	1	5	4.4	COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1	10.1016/S0960-894X(97)00002-4
	CHEMBL51530	17865	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells	ChEMBL	416	7	1	5	4.4	COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1	10.1016/S0960-894X(97)00002-4
	52944276	25201	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer	ChEMBL	559	11	3	8	4.1	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCCCO)ccc31)OCO2	10.1016/j.bmcl.2010.08.074
	CHEMBL1271807	25201	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer	ChEMBL	559	11	3	8	4.1	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCCCO)ccc31)OCO2	10.1016/j.bmcl.2010.08.074
	9845967	17865	0	None	-	0	Rat	8.1	pIC50	=	8.1	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	416	7	1	5	4.4	COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1	10.1016/s0960-894x(98)00301-1
	CHEMBL10801	17865	0	None	-	0	Rat	8.1	pIC50	=	8.1	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	416	7	1	5	4.4	COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1	10.1016/s0960-894x(98)00301-1
	CHEMBL1178000	17865	0	None	-	0	Rat	8.1	pIC50	=	8.1	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	416	7	1	5	4.4	COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1	10.1016/s0960-894x(98)00301-1
	CHEMBL51530	17865	0	None	-	0	Rat	8.1	pIC50	=	8.1	Binding	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	ChEMBL	416	7	1	5	4.4	COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1	10.1016/s0960-894x(98)00301-1
	104865	7493	99	None	-	4	Pig	8.1	pIC50	=	8.1	Binding	Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm000538f
	3494	7493	99	None	-	4	Pig	8.1	pIC50	=	8.1	Binding	Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm000538f
	392	7493	99	None	-	4	Pig	8.1	pIC50	=	8.1	Binding	Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm000538f
	CHEMBL957	7493	99	None	-	4	Pig	8.1	pIC50	=	8.1	Binding	Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm000538f
	DB00559	7493	99	None	-	4	Pig	8.1	pIC50	=	8.1	Binding	Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm000538f
	10790686	12022	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	474	5	1	8	3.6	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc3c(c2)OCCO3)cc1	10.1021/jm9606507
	CHEMBL10635	12022	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	474	5	1	8	3.6	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc3c(c2)OCCO3)cc1	10.1021/jm9606507
	44458999	175007	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	525	6	2	7	3.3	Cn1cc(C(C(=O)NS(=O)(=O)c2ccc(Cl)cc2)c2ccc3c(c2)OCO3)c2ccc(C(N)=O)cc21	10.1016/s0960-894x(01)00660-6
	CHEMBL433619	175007	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	525	6	2	7	3.3	Cn1cc(C(C(=O)NS(=O)(=O)c2ccc(Cl)cc2)c2ccc3c(c2)OCO3)c2ccc(C(N)=O)cc21	10.1016/s0960-894x(01)00660-6
	104865	7493	99	None	-	4	Pig	8.1	pIC50	=	8.1	Binding	In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/s0960-894x(01)00682-5
	3494	7493	99	None	-	4	Pig	8.1	pIC50	=	8.1	Binding	In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/s0960-894x(01)00682-5
	392	7493	99	None	-	4	Pig	8.1	pIC50	=	8.1	Binding	In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/s0960-894x(01)00682-5
	CHEMBL957	7493	99	None	-	4	Pig	8.1	pIC50	=	8.1	Binding	In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/s0960-894x(01)00682-5
	DB00559	7493	99	None	-	4	Pig	8.1	pIC50	=	8.1	Binding	In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/s0960-894x(01)00682-5
	104865	7493	99	None	-	4	Pig	8.1	pIC50	=	8.1	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm0102304
	3494	7493	99	None	-	4	Pig	8.1	pIC50	=	8.1	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm0102304
	392	7493	99	None	-	4	Pig	8.1	pIC50	=	8.1	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm0102304
	CHEMBL957	7493	99	None	-	4	Pig	8.1	pIC50	=	8.1	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm0102304
	DB00559	7493	99	None	-	4	Pig	8.1	pIC50	=	8.1	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm0102304
	44385593	136252	0	None	-	0	Rat	8.1	pIC50	=	8.1	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	530	10	5	5	4.5	Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2ccccc2)nc1C(=O)O	10.1021/jm950592+
	CHEMBL367208	136252	0	None	-	0	Rat	8.1	pIC50	=	8.1	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	530	10	5	5	4.5	Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2ccccc2)nc1C(=O)O	10.1021/jm950592+
	10553316	103851	0	None	-	0	Rat	8.1	pIC50	=	8.1	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	496	11	1	6	4.3	CCCCCCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL267279	103851	0	None	-	0	Rat	8.1	pIC50	=	8.1	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	496	11	1	6	4.3	CCCCCCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	44439108	173893	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]ET1 from human ETA receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETA receptor expressed in CHO cells	ChEMBL	1267	53	3	22	5.7	CC(=O)CC(=O)CCc1ccc(NC(=O)CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCCC(=O)N(C)Cc2cc(-c3ncco3)ccc2-c2ccccc2S(=O)(=O)Nc2ccno2)cc1	10.1016/j.bmcl.2006.10.009
	CHEMBL429019	173893	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]ET1 from human ETA receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETA receptor expressed in CHO cells	ChEMBL	1267	53	3	22	5.7	CC(=O)CC(=O)CCc1ccc(NC(=O)CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCCC(=O)N(C)Cc2cc(-c3ncco3)ccc2-c2ccccc2S(=O)(=O)Nc2ccno2)cc1	10.1016/j.bmcl.2006.10.009
	71451527	88455	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	641	15	1	12	4.8	COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(C2CC2)cn1	10.1021/jm3009103
	CHEMBL2163706	88455	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	641	15	1	12	4.8	COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(C2CC2)cn1	10.1021/jm3009103
	71462246	88466	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	604	12	2	12	2.6	CNS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC	10.1021/jm3009103
	CHEMBL2163717	88466	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	604	12	2	12	2.6	CNS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC	10.1021/jm3009103
	10667000	103947	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	372	5	1	6	2.8	COc1nc(C)cnc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12	10.1021/jm9604585
	CHEMBL268174	103947	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	372	5	1	6	2.8	COc1nc(C)cnc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12	10.1021/jm9604585
	10765171	14667	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	432	7	1	6	4.1	COc1ccc(C2(O)OC(=O)C(c3ccc(OC)c(OC)c3)=C2Cc2ccccc2)cc1	10.1021/jm9606507
	CHEMBL10901	14667	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	432	7	1	6	4.1	COc1ccc(C2(O)OC(=O)C(c3ccc(OC)c(OC)c3)=C2Cc2ccccc2)cc1	10.1021/jm9606507
	11798228	105272	2	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	461	6	1	8	3.7	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc([N+](=O)[O-])c2)cc1	10.1021/jm9606507
	CHEMBL276018	105272	2	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	461	6	1	8	3.7	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc([N+](=O)[O-])c2)cc1	10.1021/jm9606507
	9863916	67055	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	365	7	1	5	4.4	N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1ccccc1	10.1021/jm990378b
	CHEMBL174229	67055	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	365	7	1	5	4.4	N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1ccccc1	10.1021/jm990378b
	44320432	213034	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	442	6	1	7	3.6	O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1CC1OCCO1	10.1016/s0960-894x(00)00513-8
	CHEMBL86821	213034	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	442	6	1	7	3.6	O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1CC1OCCO1	10.1016/s0960-894x(00)00513-8
	CHEMBL433893	220427	0	None	-	0	Mouse	7.2	pIC50	=	7.2	Binding	Inhibition of [125I]ET1 binding to Endothelin A receptor of murine 3T3 cellsInhibition of [125I]ET1 binding to Endothelin A receptor of murine 3T3 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCc1ccccc1)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@H](C)CC	10.1016/S0960-894X(01)81219-1
	9980487	12042	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	436	6	1	5	4.8	COc1ccc(CC2=C(c3ccc(Cl)cc3)C(=O)OC2(O)c2ccc(OC)cc2)cc1	10.1021/jm9606507
	CHEMBL10648	12042	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	436	6	1	5	4.8	COc1ccc(CC2=C(c3ccc(Cl)cc3)C(=O)OC2(O)c2ccc(OC)cc2)cc1	10.1021/jm9606507
	10692351	16166	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	400	5	0	5	4.7	COc1ccc(C2OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1	10.1021/jm9606507
	CHEMBL11152	16166	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	400	5	0	5	4.7	COc1ccc(C2OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1	10.1021/jm9606507
	10894688	210285	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	402	4	1	5	4.4	COc1cccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccccc32)c1	10.1021/jm010382z
	CHEMBL66246	210285	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	402	4	1	5	4.4	COc1cccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccccc32)c1	10.1021/jm010382z
	10835638	118333	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	414	6	1	3	5.7	O=C(O)/C(=C/c1cc(OCc2ccsc2)ccc1Br)c1ccccc1	10.1021/jm970847e
	CHEMBL328057	118333	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	414	6	1	3	5.7	O=C(O)/C(=C/c1cc(OCc2ccsc2)ccc1Br)c1ccccc1	10.1021/jm970847e
	10739089	118405	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	389	8	1	4	5.6	N#Cc1ccc(OCc2ccsc2)cc1/C=C(/CCC(=O)O)c1ccccc1	10.1021/jm970847e
	CHEMBL328464	118405	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	389	8	1	4	5.6	N#Cc1ccc(OCc2ccsc2)cc1/C=C(/CCC(=O)O)c1ccccc1	10.1021/jm970847e
	CHEMBL1793933	215710	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H]([C@@H](C)CC)N(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1021/jm970161m
	19010490	60309	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells	ChEMBL	648	13	1	9	6.3	CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)NS(=O)(=O)C(C)C)c1ccc2c(c1)OCO2	10.1016/0960-894X(95)00186-W
	CHEMBL16018	60309	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells	ChEMBL	648	13	1	9	6.3	CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)NS(=O)(=O)C(C)C)c1ccc2c(c1)OCO2	10.1016/0960-894X(95)00186-W
	CHEMBL85341	222667	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00070a001
	127029203	144205	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes	ChEMBL	628	12	3	8	5.8	CCCc1nc2c(C)cc(C(=O)NCCc3ccccc3OC)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1	10.1039/C5MD00169B
	CHEMBL3753458	144205	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes	ChEMBL	628	12	3	8	5.8	CCCc1nc2c(C)cc(C(=O)NCCc3ccccc3OC)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1	10.1039/C5MD00169B
	18617322	212239	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	350	3	1	4	3.2	Cc1noc(NS(=O)(=O)c2ccccc2Cl)c1Br	10.1016/0960-894X(96)00441-6
	CHEMBL80438	212239	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	350	3	1	4	3.2	Cc1noc(NS(=O)(=O)c2ccccc2Cl)c1Br	10.1016/0960-894X(96)00441-6
	44371531	171644	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes	ChEMBL	467	6	1	5	6.3	COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3C(C)C)c3c2oc2ccccc23)cc1	10.1016/s0960-894x(99)00040-2
	CHEMBL422002	171644	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes	ChEMBL	467	6	1	5	6.3	COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3C(C)C)c3c2oc2ccccc23)cc1	10.1016/s0960-894x(99)00040-2
	CHEMBL438768	220575	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)80156-6
	CHEMBL2370247	216592	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](C(c2ccccc2)c2ccccc2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]([C@@H](C)CC)NC1=O	10.1021/jm00015a003
	127026040	144257	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes	ChEMBL	591	11	3	8	4.6	CCCc1nc2c(C)cc(C(=O)NCCN3CCCC3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1	10.1039/C5MD00169B
	CHEMBL3753888	144257	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes	ChEMBL	591	11	3	8	4.6	CCCc1nc2c(C)cc(C(=O)NCCN3CCCC3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1	10.1039/C5MD00169B
	44298597	107614	0	None	-	0	Rat	4.2	pIC50	=	4.2	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	343	5	2	5	3.0	Cc1onc(NS(=O)(=O)c2ccc(N)cc2)c1Cc1ccccc1	10.1016/s0960-894x(00)00366-8
	CHEMBL293376	107614	0	None	-	0	Rat	4.2	pIC50	=	4.2	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	343	5	2	5	3.0	Cc1onc(NS(=O)(=O)c2ccc(N)cc2)c1Cc1ccccc1	10.1016/s0960-894x(00)00366-8
	18617333	112304	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	424	4	1	5	3.3	COc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1Br	10.1016/0960-894X(96)00441-6
	CHEMBL312187	112304	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	424	4	1	5	3.3	COc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1Br	10.1016/0960-894X(96)00441-6
	44459247	94798	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	575	8	1	7	4.9	CCn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c2ccc(C(=O)N(C)C)cc21	10.1016/s0960-894x(01)00660-6
	CHEMBL23444	94798	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor	ChEMBL	575	8	1	7	4.9	CCn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c2ccc(C(=O)N(C)C)cc21	10.1016/s0960-894x(01)00660-6
	44385127	68142	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Tested for the inhibitory activity of cloned human ETA receptor by using I-ET-1 as radioligand in a competitive radioligand assayTested for the inhibitory activity of cloned human ETA receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	482	5	1	7	4.8	Cc1cc2c(cc1/C=C/c1ccsc1S(=O)(=O)Nc1onc(C)c1Br)OCO2	10.1016/S0960-894X(97)00133-9
	CHEMBL176854	68142	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Tested for the inhibitory activity of cloned human ETA receptor by using I-ET-1 as radioligand in a competitive radioligand assayTested for the inhibitory activity of cloned human ETA receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	482	5	1	7	4.8	Cc1cc2c(cc1/C=C/c1ccsc1S(=O)(=O)Nc1onc(C)c1Br)OCO2	10.1016/S0960-894X(97)00133-9
	44316994	211729	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	266	3	1	4	2.4	Cc1cccc(S(=O)(=O)Nc2onc(C)c2C)c1	10.1016/0960-894X(96)00441-6
	CHEMBL76420	211729	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	266	3	1	4	2.4	Cc1cccc(S(=O)(=O)Nc2onc(C)c2C)c1	10.1016/0960-894X(96)00441-6
	127036866	144047	0	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes	ChEMBL	614	11	3	8	5.7	CCCc1nc2c(C)cc(C(=O)NCc3ccccc3OC)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1	10.1039/C5MD00169B
	CHEMBL3752117	144047	0	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes	ChEMBL	614	11	3	8	5.7	CCCc1nc2c(C)cc(C(=O)NCc3ccccc3OC)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1	10.1039/C5MD00169B
	18184256	136261	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	662	13	2	13	3.0	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCCNS(=O)(=O)c1cccs1	10.1016/s0960-894x(02)01083-1
	CHEMBL367275	136261	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	662	13	2	13	3.0	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCCNS(=O)(=O)c1cccs1	10.1016/s0960-894x(02)01083-1
	71458720	88459	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	665	13	1	12	4.7	COc1ccccc1Oc1c(NS(=O)(=O)Cc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1	10.1021/jm3009103
	CHEMBL2163710	88459	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	665	13	1	12	4.7	COc1ccccc1Oc1c(NS(=O)(=O)Cc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1	10.1021/jm3009103
	44384652	68059	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	582	8	1	9	5.2	Cc1noc(NS(=O)(=O)c2sccc2/C=C/c2cc3c(cc2COC2CCOCC2)OCO3)c1Br	10.1016/S0960-894X(97)00133-9
	CHEMBL176675	68059	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	582	8	1	9	5.2	Cc1noc(NS(=O)(=O)c2sccc2/C=C/c2cc3c(cc2COC2CCOCC2)OCO3)c1Br	10.1016/S0960-894X(97)00133-9
	CHEMBL353605	218506	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1cn(C)c2ccccc12)C(=O)NC(C)(C)C(=O)O	10.1016/0960-894X(95)00144-I
	10672060	16032	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	470	10	1	6	3.4	CCCN(C)C(=O)CN1C[C@H](c2ccc(OC)c(OC)c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	CHEMBL110794	16032	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	470	10	1	6	3.4	CCCN(C)C(=O)CN1C[C@H](c2ccc(OC)c(OC)c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	10626501	135301	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	550	10	5	4	5.1	CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(C(C)C)[nH]1	10.1021/jm950591h
	CHEMBL366745	135301	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	550	10	5	4	5.1	CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(C(C)C)[nH]1	10.1021/jm950591h
	10721386	67149	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	550	11	5	5	4.8	CCn1cc(C[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)c2nc(C(=O)O)c(C)[nH]2)c2ccccc21	10.1021/jm950592+
	CHEMBL174686	67149	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	550	11	5	5	4.8	CCn1cc(C[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)c2nc(C(=O)O)c(C)[nH]2)c2ccccc21	10.1021/jm950592+
	10603414	67839	0	None	-	0	Rat	5.1	pIC50	=	5.1	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	585	10	4	5	5.9	CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(-c2ccccc2)o1	10.1021/jm950591h
	CHEMBL176420	67839	0	None	-	0	Rat	5.1	pIC50	=	5.1	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	585	10	4	5	5.9	CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(-c2ccccc2)o1	10.1021/jm950591h
	71455061	88448	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	511	11	1	12	2.4	COc1ccccc1Oc1c(NS(C)(=O)=O)nc(-c2ncccn2)nc1OCCOc1ncccn1	10.1021/jm3009103
	CHEMBL2163699	88448	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	511	11	1	12	2.4	COc1ccccc1Oc1c(NS(C)(=O)=O)nc(-c2ncccn2)nc1OCCOc1ncccn1	10.1021/jm3009103
	11826173	209599	1	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	432	5	1	6	4.5	COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC)cc32)cc1	10.1021/jm031041j
	CHEMBL62363	209599	1	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	432	5	1	6	4.5	COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC)cc32)cc1	10.1021/jm031041j
	11826173	209599	1	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	432	5	1	6	4.5	COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC)cc32)cc1	10.1021/jm010382z
	CHEMBL62363	209599	1	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	432	5	1	6	4.5	COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC)cc32)cc1	10.1021/jm010382z
	44385490	138586	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	532	10	4	7	4.2	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2ccccn2)nc1C(=O)O	10.1021/jm950592+
	CHEMBL369386	138586	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	532	10	4	7	4.2	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2ccccn2)nc1C(=O)O	10.1021/jm950592+
	10833686	210184	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	380	4	1	7	2.4	COC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Br	10.1016/S0960-894X(97)00367-3
	CHEMBL65531	210184	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	380	4	1	7	2.4	COC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Br	10.1016/S0960-894X(97)00367-3
	44266621	105338	0	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	387	4	1	5	4.7	COc1ccc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(-c3ccccc3)c2c1	10.1016/0960-894X(96)00170-9
	CHEMBL276615	105338	0	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	387	4	1	5	4.7	COc1ccc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(-c3ccccc3)c2c1	10.1016/0960-894X(96)00170-9
	10722389	18897	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	606	10	2	6	6.0	CCc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1C	10.1021/jm990171i
	CHEMBL1184099	18897	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	606	10	2	6	6.0	CCc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1C	10.1021/jm990171i
	CHEMBL332424	18897	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	606	10	2	6	6.0	CCc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1C	10.1021/jm990171i
	10621704	66767	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	414	7	1	6	4.8	Cc1ccccc1C(Oc1cc(OCc2ccc3ocnc3c2)ccc1C#N)C(=O)O	10.1021/jm990378b
	CHEMBL173444	66767	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	414	7	1	6	4.8	Cc1ccccc1C(Oc1cc(OCc2ccc3ocnc3c2)ccc1C#N)C(=O)O	10.1021/jm990378b
	CHEMBL151361	215572	0	None	-	0	Mouse	7.1	pIC50	=	7.1	Binding	Inhibition of [125I]ET1 binding to Endothelin A receptor of murine 3T3 cellsInhibition of [125I]ET1 binding to Endothelin A receptor of murine 3T3 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@H](C)CC	10.1016/S0960-894X(01)81219-1
	44270498	105700	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells	ChEMBL	702	13	1	10	7.2	CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)NS(=O)(=O)c1ccc(CC(C)C)s1)c1ccc2c(c1)OCO2	10.1016/0960-894X(95)00186-W
	CHEMBL279419	105700	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells	ChEMBL	702	13	1	10	7.2	CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)NS(=O)(=O)c1ccc(CC(C)C)s1)c1ccc2c(c1)OCO2	10.1016/0960-894X(95)00186-W
	10577941	68132	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	522	10	6	4	4.3	Cc1[nH]c([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)nc1C(=O)O	10.1021/jm950592+
	CHEMBL176794	68132	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	522	10	6	4	4.3	Cc1[nH]c([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)nc1C(=O)O	10.1021/jm950592+
	CHEMBL2370070	216558	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cellsDisplacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCN)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)81215-4
	44276596	113619	0	None	-	0	Rat	5.1	pIC50	=	5.1	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	458	8	1	6	4.2	COc1ccc(Cc2[nH]n(Cc3cccc(OC)c3)c(=O)c2Cc2ccc3c(c2)OCO3)cc1	10.1016/s0960-894x(00)00232-8
	CHEMBL3144728	113619	0	None	-	0	Rat	5.1	pIC50	=	5.1	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	458	8	1	6	4.2	COc1ccc(Cc2[nH]n(Cc3cccc(OC)c3)c(=O)c2Cc2ccc3c(c2)OCO3)cc1	10.1016/s0960-894x(00)00232-8
	10477792	180583	2	None	-	0	Human	4.1	pIC50	=	4.1	Binding	Displacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cellsDisplacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cells	ChEMBL	430	8	0	7	3.7	COC[C@@H]1Cc2cc3c(c(OC)c2[C@H](c2ccc(OC)c(OC)c2)[C@H]1COC)OCO3	10.1021/np50124a006
	CHEMBL453822	180583	2	None	-	0	Human	4.1	pIC50	=	4.1	Binding	Displacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cellsDisplacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cells	ChEMBL	430	8	0	7	3.7	COC[C@@H]1Cc2cc3c(c(OC)c2[C@H](c2ccc(OC)c(OC)c2)[C@H]1COC)OCO3	10.1021/np50124a006
	10305181	67223	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	666	11	2	12	4.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)NC1CCCCC1	10.1016/s0960-894x(02)01084-3
	CHEMBL175278	67223	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	666	11	2	12	4.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)NC1CCCCC1	10.1016/s0960-894x(02)01084-3
	10578300	136768	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor	ChEMBL	537	10	4	6	4.8	Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)OC2CCCCC2)nc1C(=O)O	10.1021/jm9505932
	CHEMBL367645	136768	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor	ChEMBL	537	10	4	6	4.8	Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)OC2CCCCC2)nc1C(=O)O	10.1021/jm9505932
	44279126	107503	0	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor	ChEMBL	466	3	2	3	5.5	O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(-c3ccc(Cl)cc3Cl)cc21	10.1016/0960-894X(95)00230-Q
	CHEMBL29265	107503	0	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor	ChEMBL	466	3	2	3	5.5	O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(-c3ccc(Cl)cc3Cl)cc21	10.1016/0960-894X(95)00230-Q
	44284490	107002	0	None	-	0	Pig	5.1	pIC50	=	5.1	Binding	Compound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranesCompound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranes	ChEMBL	616	13	3	5	3.9	CNC(=O)[C@H](Cc1ccccn1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)N(C)C(=O)[C@@H](CC(=O)N1CCCCCC1)CC(C)C	10.1021/jm00087a001
	CHEMBL288514	107002	0	None	-	0	Pig	5.1	pIC50	=	5.1	Binding	Compound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranesCompound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranes	ChEMBL	616	13	3	5	3.9	CNC(=O)[C@H](Cc1ccccn1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)N(C)C(=O)[C@@H](CC(=O)N1CCCCCC1)CC(C)C	10.1021/jm00087a001
	CHEMBL1206620	215386	0	None	-	0	Pig	5.1	pIC50	=	5.1	Binding	Compound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranesCompound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranes	ChEMBL		None	None	None		CC(C)C[C@@H](NC(=O)N1CCCCCC1)C(=O)N(C)[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccn1)C(=O)N(C)CC(=O)O	10.1021/jm00087a001
	CHEMBL287980	215386	0	None	-	0	Pig	5.1	pIC50	=	5.1	Binding	Compound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranesCompound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranes	ChEMBL		None	None	None		CC(C)C[C@@H](NC(=O)N1CCCCCC1)C(=O)N(C)[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccn1)C(=O)N(C)CC(=O)O	10.1021/jm00087a001
	44332641	11512	0	None	-	0	Human	4.1	pIC50	=	4.1	Binding	Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells	ChEMBL	384	4	0	4	5.2	COC(=O)C(Cc1c2ccccc2cc2ccccc12)c1ccc2c(c1)OCO2	10.1016/S0960-894X(96)00551-3
	CHEMBL103731	11512	0	None	-	0	Human	4.1	pIC50	=	4.1	Binding	Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells	ChEMBL	384	4	0	4	5.2	COC(=O)C(Cc1c2ccccc2cc2ccccc12)c1ccc2c(c1)OCO2	10.1016/S0960-894X(96)00551-3
	10598270	103719	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	421	6	1	5	4.1	CCCC#CCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL266144	103719	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	421	6	1	5	4.1	CCCC#CCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	10744041	104077	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	502	8	1	6	3.9	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(C)Cc2ccccc2)cc1	10.1021/jm9505369
	CHEMBL269108	104077	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	502	8	1	6	3.9	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(C)Cc2ccccc2)cc1	10.1021/jm9505369
	11101703	174697	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	412	7	1	5	5.3	CCCC[C@@H]1c2cc(OC(C)C)ccc2O[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O	10.1021/jm031041j
	CHEMBL431372	174697	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	412	7	1	5	5.3	CCCC[C@@H]1c2cc(OC(C)C)ccc2O[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O	10.1021/jm031041j
	11101703	174697	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	412	7	1	5	5.3	CCCC[C@@H]1c2cc(OC(C)C)ccc2O[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O	10.1021/jm010382z
	CHEMBL431372	174697	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	412	7	1	5	5.3	CCCC[C@@H]1c2cc(OC(C)C)ccc2O[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O	10.1021/jm010382z
	44293736	194930	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	463	7	2	7	4.1	CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	CHEMBL49850	194930	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	463	7	2	7	4.1	CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	CHEMBL147058	215556	0	None	-	0	Mouse	7.1	pIC50	=	7.1	Binding	Inhibition of [125I]ET1 binding to Endothelin A receptor of murine 3T3 cellsInhibition of [125I]ET1 binding to Endothelin A receptor of murine 3T3 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@H](C)CC	10.1016/S0960-894X(01)81219-1
	9874557	136516	0	None	-	2	Human	7.1	pIC50	=	7.1	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	667	15	2	10	5.5	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CC2)nc1OCCCNS(=O)(=O)c1ccc(C)cc1	10.1016/s0960-894x(02)01083-1
	CHEMBL367443	136516	0	None	-	2	Human	7.1	pIC50	=	7.1	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	667	15	2	10	5.5	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CC2)nc1OCCCNS(=O)(=O)c1ccc(C)cc1	10.1016/s0960-894x(02)01083-1
	10516176	211979	3	None	-	1	Human	6.1	pIC50	=	6.1	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	270	3	1	4	2.2	Cc1noc(NS(=O)(=O)c2ccccc2F)c1C	10.1016/0960-894X(96)00441-6
	CHEMBL78499	211979	3	None	-	1	Human	6.1	pIC50	=	6.1	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	270	3	1	4	2.2	Cc1noc(NS(=O)(=O)c2ccccc2F)c1C	10.1016/0960-894X(96)00441-6
	44298278	201446	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	462	8	2	7	4.5	COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCO)c1	10.1016/s0960-894x(00)00366-8
	CHEMBL53168	201446	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	462	8	2	7	4.5	COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCO)c1	10.1016/s0960-894x(00)00366-8
	10626522	137061	0	None	-	0	Rat	5.1	pIC50	=	5.1	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	551	11	4	5	5.2	CCCc1oc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O	10.1021/jm950591h
	CHEMBL367989	137061	0	None	-	0	Rat	5.1	pIC50	=	5.1	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	551	11	4	5	5.2	CCCc1oc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O	10.1021/jm950591h
	9961347	18734	1	None	-	0	Human	4.1	pIC50	=	4.1	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	664	13	2	7	6.6	Cc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC(C)C)cc1)c1ccccc1C	10.1021/jm990171i
	CHEMBL1182945	18734	1	None	-	0	Human	4.1	pIC50	=	4.1	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	664	13	2	7	6.6	Cc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC(C)C)cc1)c1ccccc1C	10.1021/jm990171i
	CHEMBL273642	18734	1	None	-	0	Human	4.1	pIC50	=	4.1	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	664	13	2	7	6.6	Cc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC(C)C)cc1)c1ccccc1C	10.1021/jm990171i
	137638953	163626	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	579	10	2	9	4.6	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(OCC4CC4)ccc31)OCO2	10.1016/j.bmcl.2017.04.049
	CHEMBL4071505	163626	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	579	10	2	9	4.6	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(OCC4CC4)ccc31)OCO2	10.1016/j.bmcl.2017.04.049
	11728411	209660	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	372	3	1	4	4.4	O=C(O)C1=C(c2ccccc2)c2ccccc2OC1c1ccc2c(c1)OCO2	10.1021/jm031041j
	CHEMBL62659	209660	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	372	3	1	4	4.4	O=C(O)C1=C(c2ccccc2)c2ccccc2OC1c1ccc2c(c1)OCO2	10.1021/jm031041j
	5344	180252	101	None	-	1	Human	6.1	pIC50	=	6.1	Binding	Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells	ChEMBL	267	3	2	5	1.7	Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C	10.1021/jm00029a001
	CHEMBL453	180252	101	None	-	1	Human	6.1	pIC50	=	6.1	Binding	Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells	ChEMBL	267	3	2	5	1.7	Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C	10.1021/jm00029a001
	5344	180252	101	None	-	1	Rat	6.1	pIC50	=	6.1	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	267	3	2	5	1.7	Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C	10.1021/jm00008a013
	CHEMBL453	180252	101	None	-	1	Rat	6.1	pIC50	=	6.1	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	267	3	2	5	1.7	Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C	10.1021/jm00008a013
	11728411	209660	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	372	3	1	4	4.4	O=C(O)C1=C(c2ccccc2)c2ccccc2OC1c1ccc2c(c1)OCO2	10.1021/jm010382z
	CHEMBL62659	209660	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	372	3	1	4	4.4	O=C(O)C1=C(c2ccccc2)c2ccccc2OC1c1ccc2c(c1)OCO2	10.1021/jm010382z
	5344	180252	101	None	-	1	Human	6.1	pIC50	=	6.1	Binding	Inhibitory concentration against Endothelin A receptorInhibitory concentration against Endothelin A receptor	ChEMBL	267	3	2	5	1.7	Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C	10.1021/jm030480f
	CHEMBL453	180252	101	None	-	1	Human	6.1	pIC50	=	6.1	Binding	Inhibitory concentration against Endothelin A receptorInhibitory concentration against Endothelin A receptor	ChEMBL	267	3	2	5	1.7	Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C	10.1021/jm030480f
	10334781	102785	0	None	-	0	Rat	5.1	pIC50	=	5.1	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	297	4	1	6	2.0	Cc1noc(NS(=O)(=O)c2cccc([N+](=O)[O-])c2)c1C	10.1021/jm00008a013
	CHEMBL25970	102785	0	None	-	0	Rat	5.1	pIC50	=	5.1	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	297	4	1	6	2.0	Cc1noc(NS(=O)(=O)c2cccc([N+](=O)[O-])c2)c1C	10.1021/jm00008a013
	9983872	108500	0	None	-	0	Rat	5.1	pIC50	=	5.1	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	511	9	2	5	6.9	Cc1noc(NS(=O)(=O)c2cccc3c(NCCC(c4ccccc4)c4ccccc4)cccc23)c1C	10.1021/jm00008a013
	CHEMBL29954	108500	0	None	-	0	Rat	5.1	pIC50	=	5.1	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	511	9	2	5	6.9	Cc1noc(NS(=O)(=O)c2cccc3c(NCCC(c4ccccc4)c4ccccc4)cccc23)c1C	10.1021/jm00008a013
	10336018	108885	0	None	-	0	Rat	5.1	pIC50	=	5.1	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	318	3	2	5	3.0	Cc1noc(NS(=O)(=O)c2cccc3c(O)cccc23)c1C	10.1021/jm00008a013
	CHEMBL30228	108885	0	None	-	0	Rat	5.1	pIC50	=	5.1	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	318	3	2	5	3.0	Cc1noc(NS(=O)(=O)c2cccc3c(O)cccc23)c1C	10.1021/jm00008a013
	CHEMBL413825	219866	0	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Binding affinity in LtK cells stably transfected with human endothelin A (ETA) receptorBinding affinity in LtK cells stably transfected with human endothelin A (ETA) receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(N)=O)NC(=O)CNC(=O)[C@H](CC(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]2CCCN2C1=O	10.1016/0960-894X(95)00084-7
	10840422	138144	0	None	-	0	Rat	5.1	pIC50	=	5.1	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	550	11	5	4	4.9	CCCc1[nH]c([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O	10.1021/jm950591h
	CHEMBL368854	138144	0	None	-	0	Rat	5.1	pIC50	=	5.1	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	550	11	5	4	4.9	CCCc1[nH]c([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O	10.1021/jm950591h
	10624915	213012	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	490	6	2	6	4.5	COc1ccc(NC(=O)N2C[C@@H](c3ccc4c(c3)OCO4)[C@H](C(=O)O)[C@H]2c2ccc(OC)cc2)cc1	10.1021/jm9505369
	CHEMBL8671	213012	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	490	6	2	6	4.5	COc1ccc(NC(=O)N2C[C@@H](c3ccc4c(c3)OCO4)[C@H](C(=O)O)[C@H]2c2ccc(OC)cc2)cc1	10.1021/jm9505369
	18617288	211925	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	316	3	1	4	2.5	Cc1noc(NS(=O)(=O)c2ccccc2)c1Br	10.1016/0960-894X(96)00441-6
	CHEMBL78080	211925	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	316	3	1	4	2.5	Cc1noc(NS(=O)(=O)c2ccccc2)c1Br	10.1016/0960-894X(96)00441-6
	44320444	213222	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	481	7	2	8	4.0	O=C(O)c1cc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)on1	10.1016/s0960-894x(00)00513-8
	CHEMBL88019	213222	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	481	7	2	8	4.0	O=C(O)c1cc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)on1	10.1016/s0960-894x(00)00513-8
	CHEMBL146866	215555	0	None	-	0	Mouse	7.1	pIC50	=	7.1	Binding	Inhibition of [125I]ET1 binding to Endothelin A receptor of murine 3T3 cellsInhibition of [125I]ET1 binding to Endothelin A receptor of murine 3T3 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@H](C)CC	10.1016/S0960-894X(01)81219-1
	44384651	135277	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	498	6	2	8	4.0	Cc1noc(NS(=O)(=O)c2sccc2/C=C/c2cc3c(cc2CO)OCO3)c1Br	10.1016/S0960-894X(97)00133-9
	CHEMBL366680	135277	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	498	6	2	8	4.0	Cc1noc(NS(=O)(=O)c2sccc2/C=C/c2cc3c(cc2CO)OCO3)c1Br	10.1016/S0960-894X(97)00133-9
	44332624	10953	0	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells	ChEMBL	356	3	1	4	3.7	NC(=O)C(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12	10.1016/S0960-894X(96)00551-3
	CHEMBL100120	10953	0	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells	ChEMBL	356	3	1	4	3.7	NC(=O)C(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12	10.1016/S0960-894X(96)00551-3
	10743872	103982	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	496	13	1	6	5.2	CCCCN(CCCC)CCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL268432	103982	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	496	13	1	6	5.2	CCCCN(CCCC)CCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	3847484	210512	3	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	360	4	1	3	4.4	CN(C)c1cccc2c(S(=O)(=O)Nc3ccc(Cl)cc3)cccc12	10.1021/jm9604585
	CHEMBL6778	210512	3	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor	ChEMBL	360	4	1	3	4.4	CN(C)c1cccc2c(S(=O)(=O)Nc3ccc(Cl)cc3)cccc12	10.1021/jm9604585
	10145418	88447	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)	ChEMBL	601	14	1	12	4.0	COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncccn1	10.1016/j.bmcl.2016.06.014
	CHEMBL2163698	88447	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)	ChEMBL	601	14	1	12	4.0	COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncccn1	10.1016/j.bmcl.2016.06.014
	CHEMBL354082	218508	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1cn(C)c2ccccc12)C(=O)N[C@H](CO)C(=O)O	10.1016/0960-894X(95)00144-I
	CHEMBL354152	218509	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1cn(C)c2ccccc12)C(=O)N[C@H](Cc1cn(C)c2ccccc12)C(=O)O	10.1016/0960-894X(95)00144-I
	10646372	12224	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	432	5	2	7	3.5	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(O)cc2)cc1	10.1021/jm9606507
	CHEMBL10744	12224	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	432	5	2	7	3.5	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(O)cc2)cc1	10.1021/jm9606507
	10950392	209733	0	None	-	0	Rat	8.1	pIC50	=	8.1	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	448	5	1	5	5.4	CC(C)Oc1ccc2c(c1)C(c1ccc(F)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	CHEMBL62966	209733	0	None	-	0	Rat	8.1	pIC50	=	8.1	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	448	5	1	5	5.4	CC(C)Oc1ccc2c(c1)C(c1ccc(F)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2	10.1021/jm010382z
	11113542	209989	0	None	-	0	Rat	8.1	pIC50	=	8.1	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	476	8	1	6	5.5	COc1ccc(C2=C(C(=O)O)C(c3ccc(OC)cc3OC)Oc3ccc(OC(C)C)cc32)cc1	10.1021/jm010382z
	CHEMBL64398	209989	0	None	-	0	Rat	8.1	pIC50	=	8.1	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	476	8	1	6	5.5	COc1ccc(C2=C(C(=O)O)C(c3ccc(OC)cc3OC)Oc3ccc(OC(C)C)cc32)cc1	10.1021/jm010382z
	44314575	110349	0	None	-	0	Pig	8.1	pIC50	=	8.1	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	601	13	5	5	4.2	CSCCC(NC(=O)[C@@H](Cc1c(C)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1021/jm9600914
	CHEMBL308584	110349	0	None	-	0	Pig	8.1	pIC50	=	8.1	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	601	13	5	5	4.2	CSCCC(NC(=O)[C@@H](Cc1c(C)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1021/jm9600914
	22010244	213580	0	None	-	0	Rat	8.1	pIC50	=	8.1	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	407	9	1	5	5.5	Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1C#N	10.1021/jm970847e
	CHEMBL90320	213580	0	None	-	0	Rat	8.1	pIC50	=	8.1	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	407	9	1	5	5.5	Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1C#N	10.1021/jm970847e
	44439106	160386	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]ET1 from human ETA receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETA receptor expressed in CHO cells	ChEMBL	1005	37	2	17	5.8	CC(=O)CC(=O)CCc1ccc(NC(=O)CCOCCOCCOCCOCCOCCOCCOCCC(=O)N(C)Cc2cc(-c3ncco3)ccc2-c2ccccc2S(=O)(=O)Nc2ccno2)cc1	10.1016/j.bmcl.2006.10.009
	CHEMBL398070	160386	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]ET1 from human ETA receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETA receptor expressed in CHO cells	ChEMBL	1005	37	2	17	5.8	CC(=O)CC(=O)CCc1ccc(NC(=O)CCOCCOCCOCCOCCOCCOCCOCCC(=O)N(C)Cc2cc(-c3ncco3)ccc2-c2ccccc2S(=O)(=O)Nc2ccno2)cc1	10.1016/j.bmcl.2006.10.009
	10145418	88447	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	601	14	1	12	4.0	COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncccn1	10.1021/jm3009103
	CHEMBL2163698	88447	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	601	14	1	12	4.0	COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncccn1	10.1021/jm3009103
	44304492	103335	0	None	-	0	Pig	8.1	pIC50	=	8.1	Binding	Inhibition of endothelin (ET-A) binding to porcine heart membranes Inhibition of endothelin (ET-A) binding to porcine heart membranes	ChEMBL	949	23	9	8	4.3	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(95)00349-X
	CHEMBL262993	103335	0	None	-	0	Pig	8.1	pIC50	=	8.1	Binding	Inhibition of endothelin (ET-A) binding to porcine heart membranes Inhibition of endothelin (ET-A) binding to porcine heart membranes	ChEMBL	949	23	9	8	4.3	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(95)00349-X
	CHEMBL265614	217435	19	None	-	0	Pig	8.1	pIC50	=	8.1	Binding	Inhibition of endothelin (ET-A) binding to porcine heart membranes Inhibition of endothelin (ET-A) binding to porcine heart membranes	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(95)00349-X
	104865	7493	99	None	1	4	Human	8.1	pIC50	=	8.1	Binding	Receptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cellsReceptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cells	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/S0960-894X(97)00400-9
	3494	7493	99	None	1	4	Human	8.1	pIC50	=	8.1	Binding	Receptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cellsReceptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cells	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/S0960-894X(97)00400-9
	392	7493	99	None	1	4	Human	8.1	pIC50	=	8.1	Binding	Receptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cellsReceptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cells	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/S0960-894X(97)00400-9
	CHEMBL957	7493	99	None	1	4	Human	8.1	pIC50	=	8.1	Binding	Receptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cellsReceptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cells	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/S0960-894X(97)00400-9
	DB00559	7493	99	None	1	4	Human	8.1	pIC50	=	8.1	Binding	Receptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cellsReceptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cells	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/S0960-894X(97)00400-9
	10230835	117010	0	None	-	0	Rat	8.1	pIC50	=	8.1	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	546	12	1	7	4.0	CCCS(=O)(=O)N(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)CC(C)C	10.1021/jm970101g
	CHEMBL323789	117010	0	None	-	0	Rat	8.1	pIC50	=	8.1	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	546	12	1	7	4.0	CCCS(=O)(=O)N(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)CC(C)C	10.1021/jm970101g
	10383884	211988	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	359	4	2	5	2.9	CNc1ccc(C)cc1S(=O)(=O)Nc1onc(C)c1Br	10.1016/0960-894X(96)00441-6
	CHEMBL78563	211988	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	359	4	2	5	2.9	CNc1ccc(C)cc1S(=O)(=O)Nc1onc(C)c1Br	10.1016/0960-894X(96)00441-6
	44314660	111142	0	None	-	0	Pig	8.1	pIC50	=	8.1	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	633	13	5	4	4.7	CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1CCCCC1C)C(=O)O	10.1021/jm9600914
	CHEMBL310111	111142	0	None	-	0	Pig	8.1	pIC50	=	8.1	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	633	13	5	4	4.7	CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1CCCCC1C)C(=O)O	10.1021/jm9600914
	CHEMBL2304011	216246	0	None	-	0	Pig	8.1	pIC50	=	8.1	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		Cc1[nH]c2ccccc2c1C[C@@H]1NC(=O)[C@@H](C2CC2)NC(=O)[C@H](C(C)C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC1=O	10.1021/jm9600914
	10766385	105204	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	460	6	1	7	4.1	COc1ccc(C2(O)OC(=O)C(c3cc(OC)c4c(c3)OCO4)=C2Cc2ccccc2)cc1C	10.1021/jm9606507
	CHEMBL275559	105204	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	460	6	1	7	4.1	COc1ccc(C2(O)OC(=O)C(c3cc(OC)c4c(c3)OCO4)=C2Cc2ccccc2)cc1C	10.1021/jm9606507
	44333889	11855	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	463	7	1	6	5.3	CCCSc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(02)00663-7
	CHEMBL105494	11855	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor	ChEMBL	463	7	1	6	5.3	CCCSc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(02)00663-7
	10647373	103746	0	None	-	0	Rat	8.1	pIC50	=	8.1	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	454	8	2	6	3.0	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)NCC(C)C)cc1	10.1021/jm9505369
	CHEMBL266337	103746	0	None	-	0	Rat	8.1	pIC50	=	8.1	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	454	8	2	6	3.0	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)NCC(C)C)cc1	10.1021/jm9505369
	10817057	16466	0	None	-	0	Rat	8.1	pIC50	=	8.1	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	580	11	1	7	4.7	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)c1ccc(C)cc1	10.1021/jm970101g
	CHEMBL113087	16466	0	None	-	0	Rat	8.1	pIC50	=	8.1	Binding	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	ChEMBL	580	11	1	7	4.7	CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)c1ccc(C)cc1	10.1021/jm970101g
	9840391	111316	6	None	-	1	Human	8.1	pIC50	=	8.1	Binding	Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	328	4	1	4	3.8	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2)c1C	10.1016/0960-894X(96)00441-6
	CHEMBL310427	111316	6	None	-	1	Human	8.1	pIC50	=	8.1	Binding	Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	328	4	1	4	3.8	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2)c1C	10.1016/0960-894X(96)00441-6
	9803428	108981	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	442	5	1	9	3.4	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Oc2ccc3c(c2)OCO3)c1Cl	10.1016/S0960-894X(97)00367-3
	CHEMBL302872	108981	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	442	5	1	9	3.4	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Oc2ccc3c(c2)OCO3)c1Cl	10.1016/S0960-894X(97)00367-3
	CHEMBL336033	218353	1	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Inhibitory effect against Human Endothelin A receptorInhibitory effect against Human Endothelin A receptor	ChEMBL		None	None	None		CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm00021a021
	104865	7493	99	None	1	4	Human	8.1	pIC50	=	8.1	Binding	Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1039/C5MD00169B
	3494	7493	99	None	1	4	Human	8.1	pIC50	=	8.1	Binding	Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1039/C5MD00169B
	392	7493	99	None	1	4	Human	8.1	pIC50	=	8.1	Binding	Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1039/C5MD00169B
	CHEMBL957	7493	99	None	1	4	Human	8.1	pIC50	=	8.1	Binding	Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1039/C5MD00169B
	DB00559	7493	99	None	1	4	Human	8.1	pIC50	=	8.1	Binding	Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1039/C5MD00169B
	10504689	16213	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	474	6	1	8	3.6	COC(=O)c1cccc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)c1	10.1021/jm9606507
	CHEMBL11176	16213	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	474	6	1	8	3.6	COC(=O)c1cccc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)c1	10.1021/jm9606507
	10840410	210839	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	550	10	2	10	3.3	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCC(=O)O)c2)cc1	10.1021/jm980504w
	CHEMBL70017	210839	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.	ChEMBL	550	10	2	10	3.3	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCC(=O)O)c2)cc1	10.1021/jm980504w
	CHEMBL2304006	216241	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Binding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranesBinding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranes	ChEMBL		None	None	None		O=C(O)C[C@H]1NC(=O)[C@H](Cc2c(Br)[nH]c3ccccc23)NC(=O)[C@@H](C2CC2)NC(=O)[C@H](C2CCCC2)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm9600914
	CHEMBL411171	219646	0	None	-	1	Pig	8.1	pIC50	=	8.1	Binding	Tested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptorTested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptor	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00077a013
	22467266	92121	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells	ChEMBL	522	7	2	8	3.4	COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(CO)ccc12	10.1007/s00044-004-0021-y
	CHEMBL2261360	92121	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells	ChEMBL	522	7	2	8	3.4	COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(CO)ccc12	10.1007/s00044-004-0021-y
	10626362	18223	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	544	8	2	6	5.2	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)(C)C)cc1	10.1021/jm990171i
	CHEMBL1180351	18223	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	544	8	2	6	5.2	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)(C)C)cc1	10.1021/jm990171i
	CHEMBL123316	18223	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	ChEMBL	544	8	2	6	5.2	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)(C)C)cc1	10.1021/jm990171i
	22467230	92130	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells	ChEMBL	536	8	1	8	4.0	COCc1ccc2c(C(C(=O)NS(=O)(=O)c3ccc(C)cc3OC)c3ccc4c(c3)OCO4)cn(C)c2c1	10.1007/s00044-004-0021-y
	CHEMBL2261601	92130	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells	ChEMBL	536	8	1	8	4.0	COCc1ccc2c(C(C(=O)NS(=O)(=O)c3ccc(C)cc3OC)c3ccc4c(c3)OCO4)cn(C)c2c1	10.1007/s00044-004-0021-y
	11038925	16630	0	None	-	0	Pig	8.1	pIC50	=	8.1	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	550	11	1	9	5.2	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ccccn2)c1	10.1021/jm0102304
	CHEMBL114105	16630	0	None	-	0	Pig	8.1	pIC50	=	8.1	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	550	11	1	9	5.2	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ccccn2)c1	10.1021/jm0102304
	9826741	107534	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	486	5	1	9	3.6	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Oc2ccc3c(c2)OCO3)c1Br	10.1016/S0960-894X(97)00367-3
	CHEMBL292802	107534	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	486	5	1	9	3.6	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Oc2ccc3c(c2)OCO3)c1Br	10.1016/S0960-894X(97)00367-3
	9826741	107534	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor	ChEMBL	486	5	1	9	3.6	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Oc2ccc3c(c2)OCO3)c1Br	10.1016/S0960-894X(97)00132-7
	CHEMBL292802	107534	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor	ChEMBL	486	5	1	9	3.6	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Oc2ccc3c(c2)OCO3)c1Br	10.1016/S0960-894X(97)00132-7
	10068813	104804	8	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	387	8	2	5	4.8	CCCCCNc1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12	10.1021/jm00008a013
	CHEMBL27299	104804	8	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	387	8	2	5	4.8	CCCCCNc1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12	10.1021/jm00008a013
	104865	7493	99	None	1	4	Human	7.1	pIC50	=	7.1	Binding	Binding affinity to recombinant human ETABinding affinity to recombinant human ETA	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/acs.jmedchem.0c01093
	3494	7493	99	None	1	4	Human	7.1	pIC50	=	7.1	Binding	Binding affinity to recombinant human ETABinding affinity to recombinant human ETA	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/acs.jmedchem.0c01093
	392	7493	99	None	1	4	Human	7.1	pIC50	=	7.1	Binding	Binding affinity to recombinant human ETABinding affinity to recombinant human ETA	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/acs.jmedchem.0c01093
	CHEMBL957	7493	99	None	1	4	Human	7.1	pIC50	=	7.1	Binding	Binding affinity to recombinant human ETABinding affinity to recombinant human ETA	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/acs.jmedchem.0c01093
	DB00559	7493	99	None	1	4	Human	7.1	pIC50	=	7.1	Binding	Binding affinity to recombinant human ETABinding affinity to recombinant human ETA	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/acs.jmedchem.0c01093
	10406285	118429	1	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	361	6	1	4	4.8	N#Cc1ccc(OCc2ccsc2)cc1/C=C(/C(=O)O)c1ccccc1	10.1021/jm970847e
	CHEMBL328600	118429	1	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	361	6	1	4	4.8	N#Cc1ccc(OCc2ccsc2)cc1/C=C(/C(=O)O)c1ccccc1	10.1021/jm970847e
	104865	7493	99	None	1	4	Human	7.1	pIC50	=	7.1	Binding	Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/j.bmcl.2016.06.014
	3494	7493	99	None	1	4	Human	7.1	pIC50	=	7.1	Binding	Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/j.bmcl.2016.06.014
	392	7493	99	None	1	4	Human	7.1	pIC50	=	7.1	Binding	Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/j.bmcl.2016.06.014
	CHEMBL957	7493	99	None	1	4	Human	7.1	pIC50	=	7.1	Binding	Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/j.bmcl.2016.06.014
	DB00559	7493	99	None	1	4	Human	7.1	pIC50	=	7.1	Binding	Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/j.bmcl.2016.06.014
	18184229	66382	0	None	-	2	Human	7.1	pIC50	=	7.1	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	605	15	2	10	4.2	CCCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	CHEMBL171950	66382	0	None	-	2	Human	7.1	pIC50	=	7.1	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	605	15	2	10	4.2	CCCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	44266552	11285	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	473	7	1	7	5.3	CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2c(c1)OCO2	10.1016/0960-894X(96)00170-9
	CHEMBL10218	11285	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	473	7	1	7	5.3	CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2c(c1)OCO2	10.1016/0960-894X(96)00170-9
	44266567	105009	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	461	5	1	8	4.5	COc1cc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(-c3ccc4c(c3)OCO4)c2cc1OC	10.1016/0960-894X(96)00170-9
	CHEMBL274368	105009	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	461	5	1	8	4.5	COc1cc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(-c3ccc4c(c3)OCO4)c2cc1OC	10.1016/0960-894X(96)00170-9
	104865	7493	99	None	1	4	Human	7.1	pIC50	=	7.1	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/S0960-894X(97)00400-9
	3494	7493	99	None	1	4	Human	7.1	pIC50	=	7.1	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/S0960-894X(97)00400-9
	392	7493	99	None	1	4	Human	7.1	pIC50	=	7.1	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/S0960-894X(97)00400-9
	CHEMBL957	7493	99	None	1	4	Human	7.1	pIC50	=	7.1	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/S0960-894X(97)00400-9
	DB00559	7493	99	None	1	4	Human	7.1	pIC50	=	7.1	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/S0960-894X(97)00400-9
	19432672	211000	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	606	11	3	9	5.3	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCNC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	CHEMBL70924	211000	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	606	11	3	9	5.3	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCNC(=O)Nc1ccccn1	10.1016/S0960-894X(97)00400-9
	10623877	15260	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	461	6	1	8	3.7	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc([N+](=O)[O-])cc2)cc1	10.1021/jm9606507
	CHEMBL10940	15260	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	461	6	1	8	3.7	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc([N+](=O)[O-])cc2)cc1	10.1021/jm9606507
	11015023	109497	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	406	3	1	4	5.1	O=C(O)C1=C(c2ccc(Cl)cc2)c2ccccc2OC1c1ccc2c(c1)OCO2	10.1021/jm010382z
	CHEMBL304875	109497	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	406	3	1	4	5.1	O=C(O)C1=C(c2ccc(Cl)cc2)c2ccccc2OC1c1ccc2c(c1)OCO2	10.1021/jm010382z
	19095644	176491	0	None	-	1	Human	6.1	pIC50	=	6.1	Binding	Binding affinity to recombinant human ETABinding affinity to recombinant human ETA	ChEMBL	549	10	2	8	5.4	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ccccc2)nc1OCCO	10.1021/acs.jmedchem.0c01093
	CHEMBL4438132	176491	0	None	-	1	Human	6.1	pIC50	=	6.1	Binding	Binding affinity to recombinant human ETABinding affinity to recombinant human ETA	ChEMBL	549	10	2	8	5.4	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ccccc2)nc1OCCO	10.1021/acs.jmedchem.0c01093
	14041110	106790	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor	ChEMBL	322	2	2	3	2.5	O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccccc21	10.1016/0960-894X(95)00230-Q
	CHEMBL286808	106790	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor	ChEMBL	322	2	2	3	2.5	O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccccc21	10.1016/0960-894X(95)00230-Q
	10497859	170205	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	347	6	1	4	4.7	N#Cc1ccc(OCc2ccsc2)cc1/C=C(/CO)c1ccccc1	10.1021/jm970847e
	CHEMBL419694	170205	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	347	6	1	4	4.7	N#Cc1ccc(OCc2ccsc2)cc1/C=C(/CO)c1ccccc1	10.1021/jm970847e
	44298325	202456	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	446	7	1	6	5.5	CCc1onc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Sc1cccc(OC)c1	10.1016/s0960-894x(00)00366-8
	CHEMBL55664	202456	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	446	7	1	6	5.5	CCc1onc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Sc1cccc(OC)c1	10.1016/s0960-894x(00)00366-8
	19095644	176491	0	None	-	1	Human	6.1	pIC50	=	6.1	Binding	Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes	ChEMBL	549	10	2	8	5.4	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ccccc2)nc1OCCO	10.1016/j.bmcl.2016.06.014
	CHEMBL4438132	176491	0	None	-	1	Human	6.1	pIC50	=	6.1	Binding	Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes	ChEMBL	549	10	2	8	5.4	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ccccc2)nc1OCCO	10.1016/j.bmcl.2016.06.014
	5344	180252	101	None	-	1	Rat	6.1	pIC50	=	6.1	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	267	3	2	5	1.7	Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C	10.1021/jm00004a012
	CHEMBL453	180252	101	None	-	1	Rat	6.1	pIC50	=	6.1	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	267	3	2	5	1.7	Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C	10.1021/jm00004a012
	44386621	68051	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	549	10	4	6	4.5	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CC3CCC2C3)nc1C(=O)O	10.1021/jm950592+
	CHEMBL176653	68051	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	549	10	4	6	4.5	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CC3CCC2C3)nc1C(=O)O	10.1021/jm950592+
	44266542	169589	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	521	7	1	7	6.1	O=C(O)c1c(-c2ccc3c(c2)OCO3)c2cc(OCc3ccccc3)ccc2n1Cc1ccc2c(c1)OCO2	10.1016/0960-894X(96)00170-9
	CHEMBL417246	169589	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells	ChEMBL	521	7	1	7	6.1	O=C(O)c1c(-c2ccc3c(c2)OCO3)c2cc(OCc3ccccc3)ccc2n1Cc1ccc2c(c1)OCO2	10.1016/0960-894X(96)00170-9
	44368428	51350	0	None	-	0	Pig	5.1	pIC50	=	5.1	Binding	Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.	ChEMBL	521	9	2	5	5.5	O=C(O)C(Cc1ccc(O)cc1)N(Cc1ccccc1-c1ccccc1)C(=O)/C=C/c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00009-9
	CHEMBL152001	51350	0	None	-	0	Pig	5.1	pIC50	=	5.1	Binding	Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.	ChEMBL	521	9	2	5	5.5	O=C(O)C(Cc1ccc(O)cc1)N(Cc1ccccc1-c1ccccc1)C(=O)/C=C/c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00009-9
	CHEMBL330489	218111	0	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1021/jm00070a001
	CHEMBL86737	222669	0	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1021/jm00070a001
	CHEMBL330489	218111	0	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Displacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cellsDisplacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/S0960-894X(01)81215-4
	10627378	67197	0	None	-	0	Rat	5.1	pIC50	=	5.1	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	598	11	5	4	5.6	CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(Cc2ccccc2)[nH]1	10.1021/jm950591h
	CHEMBL175103	67197	0	None	-	0	Rat	5.1	pIC50	=	5.1	Binding	Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes	ChEMBL	598	11	5	4	5.6	CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(Cc2ccccc2)[nH]1	10.1021/jm950591h
	18995996	105978	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.	ChEMBL	569	10	1	8	6.9	COc1cccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc(OC)c(OCc4ccccc4)cc23)c1	10.1016/0960-894X(96)00232-6
	CHEMBL281451	105978	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.	ChEMBL	569	10	1	8	6.9	COc1cccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc(OC)c(OCc4ccccc4)cc23)c1	10.1016/0960-894X(96)00232-6
	44279366	106437	0	None	-	0	Pig	7.1	pIC50	=	7.1	Binding	Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	499	11	5	4	2.4	CC(C)C[C@H](NC(=O)N1CCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	CHEMBL284392	106437	0	None	-	0	Pig	7.1	pIC50	=	7.1	Binding	Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	499	11	5	4	2.4	CC(C)C[C@H](NC(=O)N1CCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	44384757	172927	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	482	5	1	7	4.8	Cc1cc2c(cc1/C=C/c1sccc1S(=O)(=O)Nc1onc(C)c1Br)OCO2	10.1016/S0960-894X(97)00133-9
	CHEMBL426218	172927	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	482	5	1	7	4.8	Cc1cc2c(cc1/C=C/c1sccc1S(=O)(=O)Nc1onc(C)c1Br)OCO2	10.1016/S0960-894X(97)00133-9
	11103152	170019	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	504	9	1	7	5.6	CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc(OC)c(OC)c1)O2	10.1021/jm010382z
	CHEMBL418473	170019	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	504	9	1	7	5.6	CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc(OC)c(OC)c1)O2	10.1021/jm010382z
	44314580	211916	0	None	-	0	Pig	6.1	pIC50	=	6.1	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	608	13	5	5	4.5	CCCCC(NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C(C)C)C(=O)O	10.1021/jm9600914
	CHEMBL78023	211916	0	None	-	0	Pig	6.1	pIC50	=	6.1	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	608	13	5	5	4.5	CCCCC(NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C(C)C)C(=O)O	10.1021/jm9600914
	CHEMBL441006	220654	0	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Binding affinity in LtK cells stably transfected with human endothelin A (ETA) receptorBinding affinity in LtK cells stably transfected with human endothelin A (ETA) receptor	ChEMBL		None	None	None		CC(=O)[C@H](Cc1c[nH]c2ccccc12)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/0960-894X(95)00084-7
	23445388	213303	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	398	4	1	5	4.3	Cc1noc(NS(=O)(=O)c2sccc2-c2ccccc2)c1Br	10.1016/S0960-894X(96)00496-9
	CHEMBL88506	213303	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	398	4	1	5	4.3	Cc1noc(NS(=O)(=O)c2sccc2-c2ccccc2)c1Br	10.1016/S0960-894X(96)00496-9
	9917072	68877	0	None	-	2	Human	7.1	pIC50	=	7.1	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	619	16	2	10	4.6	CCCS(=O)(=O)NCCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	CHEMBL177538	68877	0	None	-	2	Human	7.1	pIC50	=	7.1	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	619	16	2	10	4.6	CCCS(=O)(=O)NCCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01083-1
	23445408	118412	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	454	6	1	5	5.5	Cc1noc(NS(=O)(=O)c2sccc2-c2ccc(CC(C)C)cc2)c1Br	10.1016/S0960-894X(96)00496-9
	CHEMBL328517	118412	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	454	6	1	5	5.5	Cc1noc(NS(=O)(=O)c2sccc2-c2ccc(CC(C)C)cc2)c1Br	10.1016/S0960-894X(96)00496-9
	44270602	105634	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells	ChEMBL	688	13	1	10	7.0	CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)NS(=O)(=O)c1cccs1)c1ccc2c(c1)OCO2	10.1016/0960-894X(95)00186-W
	CHEMBL278930	105634	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells	ChEMBL	688	13	1	10	7.0	CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)NS(=O)(=O)c1cccs1)c1ccc2c(c1)OCO2	10.1016/0960-894X(95)00186-W
	1009	6982	25	None	-	1	Human	5.1	pIC50	=	5.1	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	558	11	2	6	5.8	CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2	10.1021/jm990170q
	5310991	6982	25	None	-	1	Human	5.1	pIC50	=	5.1	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	558	11	2	6	5.8	CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2	10.1021/jm990170q
	CHEMBL332794	6982	25	None	-	1	Human	5.1	pIC50	=	5.1	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	558	11	2	6	5.8	CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2	10.1021/jm990170q
	44383535	66054	0	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Tested for binding affinity towards human Endothelin A receptorTested for binding affinity towards human Endothelin A receptor	ChEMBL	280	4	1	5	1.5	C/C=C/C=C/C(=O)O[C@@H]1C=C2COC(OC)[C@]2(O)CC1	10.1016/s0960-894x(00)00136-0
	CHEMBL170446	66054	0	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Tested for binding affinity towards human Endothelin A receptorTested for binding affinity towards human Endothelin A receptor	ChEMBL	280	4	1	5	1.5	C/C=C/C=C/C(=O)O[C@@H]1C=C2COC(OC)[C@]2(O)CC1	10.1016/s0960-894x(00)00136-0
	10960638	107845	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	414	4	1	4	5.6	CC(C)c1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccccc32)cc1	10.1021/jm010382z
	CHEMBL294793	107845	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	414	4	1	4	5.6	CC(C)c1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccccc32)cc1	10.1021/jm010382z
	23445358	118340	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	412	4	1	5	4.6	Cc1cccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c1	10.1016/S0960-894X(96)00496-9
	CHEMBL328089	118340	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	412	4	1	5	4.6	Cc1cccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c1	10.1016/S0960-894X(96)00496-9
	10546830	108152	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	365	4	2	6	1.7	Cc1noc(NS(=O)(=O)c2ccsc2C(N)=O)c1Br	10.1021/jm9608366
	CHEMBL297107	108152	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	365	4	2	6	1.7	Cc1noc(NS(=O)(=O)c2ccsc2C(N)=O)c1Br	10.1021/jm9608366
	44386069	66509	0	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	704	13	2	11	5.5	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCNS(=O)(=O)c1ccc(C)cc1	10.1016/s0960-894x(02)01083-1
	CHEMBL172441	66509	0	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	704	13	2	11	5.5	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCNS(=O)(=O)c1ccc(C)cc1	10.1016/s0960-894x(02)01083-1
	18995999	105288	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.	ChEMBL	477	6	1	8	5.0	COc1cccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc4c(cc23)OCO4)c1	10.1016/0960-894X(96)00232-6
	CHEMBL27617	105288	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.	ChEMBL	477	6	1	8	5.0	COc1cccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc4c(cc23)OCO4)c1	10.1016/0960-894X(96)00232-6
	44384611	135432	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	644	10	2	12	5.8	C#CCOc1nc(-c2ccnc(-c3noc(S)n3)c2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	CHEMBL366797	135432	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	644	10	2	12	5.8	C#CCOc1nc(-c2ccnc(-c3noc(S)n3)c2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	10405292	104352	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2cccc3cc(N(C)C)ccc23)c1C	10.1021/jm00008a013
	CHEMBL27073	104352	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2cccc3cc(N(C)C)ccc23)c1C	10.1021/jm00008a013
	44316526	212200	2	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	344	3	1	4	3.2	Cc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1C	10.1016/0960-894X(96)00441-6
	CHEMBL80180	212200	2	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	344	3	1	4	3.2	Cc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1C	10.1016/0960-894X(96)00441-6
	10674642	120147	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	574	10	3	7	4.7	CCc1cc(C(=O)O)cc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm990170q
	CHEMBL331758	120147	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	574	10	3	7	4.7	CCc1cc(C(=O)O)cc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm990170q
	10405292	104352	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2cccc3cc(N(C)C)ccc23)c1C	10.1021/jm00004a012
	CHEMBL27073	104352	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2cccc3cc(N(C)C)ccc23)c1C	10.1021/jm00004a012
	19010508	63119	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells	ChEMBL	501	9	1	7	5.5	CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)O)c1ccc2c(c1)OCO2	10.1016/0960-894X(95)00186-W
	CHEMBL16306	63119	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells	ChEMBL	501	9	1	7	5.5	CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)O)c1ccc2c(c1)OCO2	10.1016/0960-894X(95)00186-W
	14973488	120584	0	None	-	0	Human	4.1	pIC50	=	4.1	Binding	Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells	ChEMBL	295	4	1	5	2.2	Cc1noc(NS(=O)(=O)c2ccc(N(C)C)cc2)c1C	10.1021/jm00029a001
	CHEMBL332471	120584	0	None	-	0	Human	4.1	pIC50	=	4.1	Binding	Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells	ChEMBL	295	4	1	5	2.2	Cc1noc(NS(=O)(=O)c2ccc(N(C)C)cc2)c1C	10.1021/jm00029a001
	14973488	120584	0	None	-	0	Rat	4.1	pIC50	=	4.1	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	295	4	1	5	2.2	Cc1noc(NS(=O)(=O)c2ccc(N(C)C)cc2)c1C	10.1021/jm00004a012
	CHEMBL332471	120584	0	None	-	0	Rat	4.1	pIC50	=	4.1	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	295	4	1	5	2.2	Cc1noc(NS(=O)(=O)c2ccc(N(C)C)cc2)c1C	10.1021/jm00004a012
	44293685	108557	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	521	10	2	8	3.9	CCOc1ccc2c(c1)[C@@H](c1cccc(OC)c1OCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	CHEMBL300000	108557	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	521	10	2	8	3.9	CCOc1ccc2c(c1)[C@@H](c1cccc(OC)c1OCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	10576377	18779	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	471	6	2	7	3.9	COc1cccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c1	10.1021/jm9608366
	CHEMBL1183291	18779	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	471	6	2	7	3.9	COc1cccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c1	10.1021/jm9608366
	CHEMBL288967	18779	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	471	6	2	7	3.9	COc1cccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c1	10.1021/jm9608366
	44384715	67136	0	None	-	1	Human	7.1	pIC50	=	7.1	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	559	9	1	9	5.2	CC#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	CHEMBL174607	67136	0	None	-	1	Human	7.1	pIC50	=	7.1	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	559	9	1	9	5.2	CC#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	44265861	103983	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	481	11	1	6	5.1	CCCC(CCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL268433	103983	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	481	11	1	6	5.1	CCCC(CCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL433406	220419	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)NC)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	5344	180252	101	None	-	1	Human	6.1	pIC50	=	6.1	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	267	3	2	5	1.7	Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C	10.1016/0960-894X(96)00441-6
	CHEMBL453	180252	101	None	-	1	Human	6.1	pIC50	=	6.1	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	267	3	2	5	1.7	Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C	10.1016/0960-894X(96)00441-6
	CHEMBL308208	217762	0	None	-	0	Pig	5.1	pIC50	=	5.1	Binding	Binding activity against Endothelin A receptor of Porcine aortic smooth muscle membranesBinding activity against Endothelin A receptor of Porcine aortic smooth muscle membranes	ChEMBL		None	None	None		CC(C)[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm00089a028
	CHEMBL341751	218439	0	None	-	0	Pig	5.1	pIC50	=	5.1	Binding	The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.	ChEMBL		None	None	None		CC(C)[C@@H]1NC(=O)[C@@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm00021a021
	10763577	66673	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	401	7	1	4	5.3	Cc1ccccc1C(Oc1cc(OCc2c(C)cccc2C)ccc1C#N)C(=O)O	10.1021/jm990378b
	CHEMBL173054	66673	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	401	7	1	4	5.3	Cc1ccccc1C(Oc1cc(OCc2c(C)cccc2C)ccc1C#N)C(=O)O	10.1021/jm990378b
	10916428	169474	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	402	4	1	5	4.4	COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccccc32)cc1	10.1021/jm031041j
	CHEMBL417050	169474	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	402	4	1	5	4.4	COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccccc32)cc1	10.1021/jm031041j
	15289331	106340	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.	ChEMBL	433	6	1	6	5.3	COc1cccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3ccccc23)c1	10.1016/0960-894X(96)00232-6
	CHEMBL283648	106340	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.	ChEMBL	433	6	1	6	5.3	COc1cccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3ccccc23)c1	10.1016/0960-894X(96)00232-6
	10916428	169474	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	402	4	1	5	4.4	COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccccc32)cc1	10.1021/jm010382z
	CHEMBL417050	169474	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	402	4	1	5	4.4	COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccccc32)cc1	10.1021/jm010382z
	9810400	105383	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	710	14	2	12	5.6	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCCNS(=O)(=O)c1cccs1	10.1016/s0960-894x(02)01083-1
	CHEMBL276949	105383	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	710	14	2	12	5.6	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCCNS(=O)(=O)c1cccs1	10.1016/s0960-894x(02)01083-1
	10338501	108832	1	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	359	4	2	5	3.2	CC(=O)Nc1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12	10.1021/jm00004a012
	CHEMBL30199	108832	1	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	359	4	2	5	3.2	CC(=O)Nc1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12	10.1021/jm00004a012
	10275056	119286	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	440	6	1	5	5.2	CCCc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1	10.1016/S0960-894X(96)00496-9
	CHEMBL329890	119286	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor	ChEMBL	440	6	1	5	5.2	CCCc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1	10.1016/S0960-894X(96)00496-9
	9998564	106257	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	359	4	2	5	3.2	CC(=O)Nc1ccc2cccc(S(=O)(=O)Nc3onc(C)c3C)c2c1	10.1021/jm00008a013
	CHEMBL283175	106257	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	359	4	2	5	3.2	CC(=O)Nc1ccc2cccc(S(=O)(=O)Nc3onc(C)c3C)c2c1	10.1021/jm00008a013
	9998564	106257	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	359	4	2	5	3.2	CC(=O)Nc1ccc2cccc(S(=O)(=O)Nc3onc(C)c3C)c2c1	10.1021/jm00004a012
	CHEMBL283175	106257	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	359	4	2	5	3.2	CC(=O)Nc1ccc2cccc(S(=O)(=O)Nc3onc(C)c3C)c2c1	10.1021/jm00004a012
	10602312	66437	0	None	-	0	Rat	5.1	pIC50	=	5.1	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	531	11	5	5	4.5	Cc1oc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NCc2ccccc2)nc1C(=O)O	10.1021/jm950592+
	CHEMBL172178	66437	0	None	-	0	Rat	5.1	pIC50	=	5.1	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	531	11	5	5	4.5	Cc1oc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NCc2ccccc2)nc1C(=O)O	10.1021/jm950592+
	10571971	174951	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	ChEMBL	382	9	1	4	5.6	Cc1ccccc1C(CCC(=O)O)Oc1cccc(OCc2ccsc2)c1	10.1021/jm9707131
	CHEMBL433209	174951	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	ChEMBL	382	9	1	4	5.6	Cc1ccccc1C(CCC(=O)O)Oc1cccc(OCc2ccsc2)c1	10.1021/jm9707131
	137639474	163676	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	607	10	2	9	5.4	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(OCC4CCCC4)ccc31)OCO2	10.1016/j.bmcl.2017.04.049
	CHEMBL4072165	163676	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	607	10	2	9	5.4	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(OCC4CCCC4)ccc31)OCO2	10.1016/j.bmcl.2017.04.049
	10696788	182694	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	In vitro inhibitory activity against human Endothelin A receptor using radioligand binding assay.In vitro inhibitory activity against human Endothelin A receptor using radioligand binding assay.	ChEMBL	501	5	2	9	3.9	Cc1noc(NS(=O)(=O)c2ccsc2NC(=O)Oc2ccc3c(c2)OCO3)c1Br	10.1021/jm9700068
	CHEMBL45872	182694	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	In vitro inhibitory activity against human Endothelin A receptor using radioligand binding assay.In vitro inhibitory activity against human Endothelin A receptor using radioligand binding assay.	ChEMBL	501	5	2	9	3.9	Cc1noc(NS(=O)(=O)c2ccsc2NC(=O)Oc2ccc3c(c2)OCO3)c1Br	10.1021/jm9700068
	10338501	108832	1	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells	ChEMBL	359	4	2	5	3.2	CC(=O)Nc1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12	10.1021/jm00029a001
	CHEMBL30199	108832	1	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells	ChEMBL	359	4	2	5	3.2	CC(=O)Nc1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12	10.1021/jm00029a001
	10475320	103273	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	387	5	2	5	3.8	Cc1noc(NS(=O)(=O)c2cccc3c(NC(=O)C(C)C)cccc23)c1C	10.1021/jm00008a013
	CHEMBL26252	103273	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	387	5	2	5	3.8	Cc1noc(NS(=O)(=O)c2cccc3c(NC(=O)C(C)C)cccc23)c1C	10.1021/jm00008a013
	10338501	108832	1	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	359	4	2	5	3.2	CC(=O)Nc1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12	10.1021/jm00008a013
	CHEMBL30199	108832	1	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	359	4	2	5	3.2	CC(=O)Nc1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12	10.1021/jm00008a013
	56678452	70101	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells	ChEMBL	937	26	9	9	3.6	CC[C@H](C)[C@H](NC(=O)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)[C@H](C)CC)C(=O)CNC(=O)[C@H](N)Cc1c[nH]c2ccccc12	10.1021/jm970161m
	CHEMBL1793928	70101	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells	ChEMBL	937	26	9	9	3.6	CC[C@H](C)[C@H](NC(=O)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)[C@H](C)CC)C(=O)CNC(=O)[C@H](N)Cc1c[nH]c2ccccc12	10.1021/jm970161m
	44311288	210963	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	592	11	1	10	5.3	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCOC(=O)c1cccnc1	10.1016/S0960-894X(97)00400-9
	CHEMBL70781	210963	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	592	11	1	10	5.3	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCOC(=O)c1cccnc1	10.1016/S0960-894X(97)00400-9
	14673588	11179	0	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.	ChEMBL	342	6	1	4	5.0	CC(C)Oc1c(C(=O)O)sc2ccc(OCc3ccccc3)cc12	10.1016/0960-894X(96)00232-6
	CHEMBL10143	11179	0	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.	ChEMBL	342	6	1	4	5.0	CC(C)Oc1c(C(=O)O)sc2ccc(OCc3ccccc3)cc12	10.1016/0960-894X(96)00232-6
	14673588	11179	0	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Compound was evaluated for binding affinity against human Endothelin A receptorCompound was evaluated for binding affinity against human Endothelin A receptor	ChEMBL	342	6	1	4	5.0	CC(C)Oc1c(C(=O)O)sc2ccc(OCc3ccccc3)cc12	10.1016/0960-894X(96)00170-9
	CHEMBL10143	11179	0	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Compound was evaluated for binding affinity against human Endothelin A receptorCompound was evaluated for binding affinity against human Endothelin A receptor	ChEMBL	342	6	1	4	5.0	CC(C)Oc1c(C(=O)O)sc2ccc(OCc3ccccc3)cc12	10.1016/0960-894X(96)00170-9
	10790183	213024	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	461	8	1	6	4.3	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CCOc2ccccc2)cc1	10.1021/jm9505369
	CHEMBL8677	213024	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	461	8	1	6	4.3	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CCOc2ccccc2)cc1	10.1021/jm9505369
	127026058	144024	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes	ChEMBL	600	10	3	8	6.0	CCCc1nc2c(C)cc(C(=O)Nc3ccccc3OC)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1	10.1039/C5MD00169B
	CHEMBL3751899	144024	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes	ChEMBL	600	10	3	8	6.0	CCCc1nc2c(C)cc(C(=O)Nc3ccccc3OC)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1	10.1039/C5MD00169B
	10839533	108222	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	513	5	2	9	2.9	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)NC(=O)c2ccc3c(c2)OCO3)c1Br	10.1021/jm9700068
	CHEMBL297599	108222	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	513	5	2	9	2.9	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)NC(=O)c2ccc3c(c2)OCO3)c1Br	10.1021/jm9700068
	10839947	124080	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	530	9	2	6	5.0	CCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm990170q
	CHEMBL339657	124080	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	530	9	2	6	5.0	CCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm990170q
	44320777	212984	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	550	10	2	8	4.7	COc1ccc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)c(OCC(=O)O)c1	10.1016/s0960-894x(00)00513-8
	CHEMBL86505	212984	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles	ChEMBL	550	10	2	8	4.7	COc1ccc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)c(OCC(=O)O)c1	10.1016/s0960-894x(00)00513-8
	10415067	52139	0	None	-	0	Pig	5.1	pIC50	=	5.1	Binding	Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.	ChEMBL	546	8	2	6	5.0	O=C(O)C(Cc1c[nH]c2ccccc12)N(Cc1cc2c(cc1Cl)OCO2)C(=O)/C=C/c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00009-9
	CHEMBL152713	52139	0	None	-	0	Pig	5.1	pIC50	=	5.1	Binding	Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.	ChEMBL	546	8	2	6	5.0	O=C(O)C(Cc1c[nH]c2ccccc12)N(Cc1cc2c(cc1Cl)OCO2)C(=O)/C=C/c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00009-9
	10449375	102544	0	None	-	0	Rat	5.1	pIC50	=	5.1	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	331	4	1	5	3.0	Cc1cc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)on1	10.1021/jm00008a013
	CHEMBL25854	102544	0	None	-	0	Rat	5.1	pIC50	=	5.1	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	331	4	1	5	3.0	Cc1cc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)on1	10.1021/jm00008a013
	CHEMBL289687	217654	0	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]cn1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00070a001
	3811690	212189	3	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	330	3	1	4	2.9	Cc1noc(NS(=O)(=O)c2ccc(Br)cc2)c1C	10.1016/0960-894X(96)00441-6
	CHEMBL80129	212189	3	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	330	3	1	4	2.9	Cc1noc(NS(=O)(=O)c2ccc(Br)cc2)c1C	10.1016/0960-894X(96)00441-6
	CHEMBL289687	217654	0	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Inhibition of [125I]endothelin-1 [ET-1] binding to endothelin A receptor (ETA) of rabbit renal artery vascular smooth muscle cellsInhibition of [125I]endothelin-1 [ET-1] binding to endothelin A receptor (ETA) of rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]cn1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(95)00152-J
	127035082	143289	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	677	12	2	8	7.4	CCCc1nc2c(C)cc(C(=O)NCc3cccc(OC)c3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	CHEMBL3736262	143289	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	677	12	2	8	7.4	CCCc1nc2c(C)cc(C(=O)NCc3cccc(OC)c3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	15411002	115329	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells	ChEMBL	563	9	1	10	4.2	CNC(=O)OC1(c2ccc(OC)cc2)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1cc(OC)c(OC)c(OC)c1	10.1016/S0960-894X(97)00002-4
	CHEMBL320183	115329	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells	ChEMBL	563	9	1	10	4.2	CNC(=O)OC1(c2ccc(OC)cc2)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1cc(OC)c(OC)c(OC)c1	10.1016/S0960-894X(97)00002-4
	44314661	109802	0	None	-	0	Pig	8.1	pIC50	=	8.1	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	603	14	5	4	5.1	CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(CCCC)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1021/jm9600914
	CHEMBL306977	109802	0	None	-	0	Pig	8.1	pIC50	=	8.1	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	603	14	5	4	5.1	CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(CCCC)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1021/jm9600914
	10646514	66113	0	None	-	0	Rat	8.1	pIC50	=	8.1	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	434	7	1	6	5.1	N#Cc1ccc(OCc2ccc3ncoc3c2)cc1OC(C(=O)O)c1ccccc1Cl	10.1021/jm990378b
	CHEMBL170681	66113	0	None	-	0	Rat	8.1	pIC50	=	8.1	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	434	7	1	6	5.1	N#Cc1ccc(OCc2ccc3ncoc3c2)cc1OC(C(=O)O)c1ccccc1Cl	10.1021/jm990378b
	10619391	67012	0	None	-	0	Rat	8.1	pIC50	=	8.1	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	374	7	1	5	4.0	Cc1ccccc1C(Oc1cc(OCc2ccncc2)ccc1C#N)C(=O)O	10.1021/jm990378b
	CHEMBL173251	67012	0	None	-	0	Rat	8.1	pIC50	=	8.1	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	374	7	1	5	4.0	Cc1ccccc1C(Oc1cc(OCc2ccncc2)ccc1C#N)C(=O)O	10.1021/jm990378b
	CHEMBL174092	67012	0	None	-	0	Rat	8.1	pIC50	=	8.1	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	374	7	1	5	4.0	Cc1ccccc1C(Oc1cc(OCc2ccncc2)ccc1C#N)C(=O)O	10.1021/jm990378b
	9931773	85139	0	None	-	0	Rat	8.1	pIC50	=	8.1	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	417	7	1	6	4.4	Cc1ccccc1[C@H](Oc1cc(OCc2ccc3c(c2)OCO3)ccc1C#N)C(=O)O	10.1021/jm990378b
	CHEMBL2110231	85139	0	None	-	0	Rat	8.1	pIC50	=	8.1	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	417	7	1	6	4.4	Cc1ccccc1[C@H](Oc1cc(OCc2ccc3c(c2)OCO3)ccc1C#N)C(=O)O	10.1021/jm990378b
	44311285	109076	0	None	-	1	Human	8.1	pIC50	=	8.1	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	635	13	2	10	6.4	CCCc1nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c(Oc2ccccc2OC)c(OCCOC(=O)Nc2ccccn2)n1	10.1016/S0960-894X(97)00400-9
	CHEMBL303428	109076	0	None	-	1	Human	8.1	pIC50	=	8.1	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	635	13	2	10	6.4	CCCc1nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c(Oc2ccccc2OC)c(OCCOC(=O)Nc2ccccn2)n1	10.1016/S0960-894X(97)00400-9
	10992620	210129	0	None	-	0	Rat	8.0	pIC50	=	8.0	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	384	5	1	6	3.8	COC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	CHEMBL65070	210129	0	None	-	0	Rat	8.0	pIC50	=	8.0	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	384	5	1	6	3.8	COC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21	10.1021/jm010382z
	44314646	211818	0	None	-	0	Pig	8.0	pIC50	=	8.0	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	633	13	5	4	4.7	CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1CCCCCC1)C(=O)O	10.1021/jm9600914
	CHEMBL77033	211818	0	None	-	0	Pig	8.0	pIC50	=	8.0	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	633	13	5	4	4.7	CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1CCCCCC1)C(=O)O	10.1021/jm9600914
	44314889	110519	0	None	-	0	Pig	8.0	pIC50	=	8.0	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	633	12	5	4	4.7	CCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1021/jm9600914
	CHEMBL308815	110519	0	None	-	0	Pig	8.0	pIC50	=	8.0	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	633	12	5	4	4.7	CCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1021/jm9600914
	44314620	109922	0	None	-	0	Pig	8.0	pIC50	=	8.0	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	587	12	5	4	4.4	CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O	10.1021/jm9600914
	CHEMBL307903	109922	0	None	-	0	Pig	8.0	pIC50	=	8.0	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	587	12	5	4	4.4	CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O	10.1021/jm9600914
	23445404	107688	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	456	5	1	7	4.1	Cc1ccc(OC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1	10.1016/S0960-894X(97)00367-3
	CHEMBL293877	107688	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor	ChEMBL	456	5	1	7	4.1	Cc1ccc(OC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1	10.1016/S0960-894X(97)00367-3
	10119105	108224	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	526	7	2	9	3.1	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2CC(=O)N(C)C)OCO3)c1Cl	10.1021/jm9608366
	CHEMBL297618	108224	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	526	7	2	9	3.1	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2CC(=O)N(C)C)OCO3)c1Cl	10.1021/jm9608366
	10650062	67218	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor	ChEMBL	537	10	4	6	4.8	Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)OC(=O)NC2CCCCC2)nc1C(=O)O	10.1021/jm9505932
	CHEMBL175228	67218	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor	ChEMBL	537	10	4	6	4.8	Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)OC(=O)NC2CCCCC2)nc1C(=O)O	10.1021/jm9505932
	155517241	176937	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	522	14	2	11	2.9	CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1Oc1ccccc1OC	10.1016/j.bmcl.2016.06.014
	CHEMBL4444355	176937	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	522	14	2	11	2.9	CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1Oc1ccccc1OC	10.1016/j.bmcl.2016.06.014
	10129267	88463	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	617	13	1	12	3.9	CCCS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC	10.1021/jm3009103
	CHEMBL2163714	88463	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	617	13	1	12	3.9	CCCS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC	10.1021/jm3009103
	44314723	211777	0	None	-	0	Pig	8.0	pIC50	=	8.0	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	583	13	5	4	4.7	CCCCC(NC(=O)[C@@H](Cc1c(C)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1021/jm9600914
	CHEMBL76735	211777	0	None	-	0	Pig	8.0	pIC50	=	8.0	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	583	13	5	4	4.7	CCCCC(NC(=O)[C@@H](Cc1c(C)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1021/jm9600914
	44314659	211899	0	None	-	0	Pig	8.0	pIC50	=	8.0	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	631	12	5	4	4.5	C=CCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1021/jm9600914
	CHEMBL77853	211899	0	None	-	0	Pig	8.0	pIC50	=	8.0	Binding	Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.	ChEMBL	631	12	5	4	4.5	C=CCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O	10.1021/jm9600914
	52949155	25183	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	557	10	2	7	5.4	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC(C)C)ccc31)OCO2	10.1016/j.bmcl.2017.04.049
	CHEMBL1271640	25183	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay	ChEMBL	557	10	2	7	5.4	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC(C)C)ccc31)OCO2	10.1016/j.bmcl.2017.04.049
	10814318	15924	0	None	-	0	Rat	8.0	pIC50	=	8	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	472	14	1	5	4.7	C=CCCC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC	10.1021/jm980217s
	CHEMBL110064	15924	0	None	-	0	Rat	8.0	pIC50	=	8	Binding	Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)	ChEMBL	472	14	1	5	4.7	C=CCCC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC	10.1021/jm980217s
	52944083	25190	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer	ChEMBL	557	10	2	7	5.5	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OC(C)CC)ccc31)OCO2	10.1016/j.bmcl.2010.08.074
	CHEMBL1271691	25190	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer	ChEMBL	557	10	2	7	5.5	CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OC(C)CC)ccc31)OCO2	10.1016/j.bmcl.2010.08.074
	71456864	88467	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	618	13	2	12	3.0	CCNS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC	10.1021/jm3009103
	CHEMBL2163718	88467	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	ChEMBL	618	13	2	12	3.0	CCNS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC	10.1021/jm3009103
	11734340	170490	0	None	-	0	Pig	8.0	pIC50	=	8	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	552	10	1	10	4.6	CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccncc2)nc1	10.1021/jm0102304
	CHEMBL420501	170490	0	None	-	0	Pig	8.0	pIC50	=	8	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	552	10	1	10	4.6	CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccncc2)nc1	10.1021/jm0102304
	10501279	104994	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	402	6	1	5	4.1	COc1ccc(C2(O)OC(=O)C(c3cccc(OC)c3)=C2Cc2ccccc2)cc1	10.1021/jm9606507
	CHEMBL274307	104994	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	402	6	1	5	4.1	COc1ccc(C2(O)OC(=O)C(c3cccc(OC)c3)=C2Cc2ccccc2)cc1	10.1021/jm9606507
	44371516	57759	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes	ChEMBL	469	7	1	6	5.6	CCOc1ccccc1Cn1c(=O)c(C(=O)O)c(-c2ccc(OC)cc2)c2oc3ccccc3c21	10.1016/s0960-894x(99)00040-2
	CHEMBL157827	57759	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes	ChEMBL	469	7	1	6	5.6	CCOc1ccccc1Cn1c(=O)c(C(=O)O)c(-c2ccc(OC)cc2)c2oc3ccccc3c21	10.1016/s0960-894x(99)00040-2
	CHEMBL279259	217618	0	None	-	0	Mouse	6.1	pIC50	=	6.1	Binding	Binding affinity for Endothelin A receptor was determined in murine 3T3 cellsBinding affinity for Endothelin A receptor was determined in murine 3T3 cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](N)CCCNC(=O)[C@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(00)80326-1
	11794876	213955	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	393	7	1	4	4.9	O=C(O)/C(=C/c1cc(OCc2ccccc2)ccc1[N+](=O)[O-])c1ccccc1F	10.1021/jm970847e
	CHEMBL92446	213955	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.	ChEMBL	393	7	1	4	4.9	O=C(O)/C(=C/c1cc(OCc2ccccc2)ccc1[N+](=O)[O-])c1ccccc1F	10.1021/jm970847e
	44213651	11070	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells	ChEMBL	343	3	1	4	4.2	OCC(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12	10.1016/S0960-894X(96)00551-3
	CHEMBL100795	11070	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells	ChEMBL	343	3	1	4	4.2	OCC(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12	10.1016/S0960-894X(96)00551-3
	10742024	103718	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	446	7	1	6	3.9	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CCc2ccccn2)cc1	10.1021/jm9505369
	CHEMBL266143	103718	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells	ChEMBL	446	7	1	6	3.9	COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CCc2ccccn2)cc1	10.1021/jm9505369
	10841134	67222	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	589	10	4	6	5.3	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC23CC4CC(CC(C4)C2)C3)nc1C(=O)O	10.1021/jm950592+
	CHEMBL175277	67222	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	589	10	4	6	5.3	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC23CC4CC(CC(C4)C2)C3)nc1C(=O)O	10.1021/jm950592+
	44311321	210964	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	607	11	2	10	5.7	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCOC(=O)Nc1cccnc1	10.1016/S0960-894X(97)00400-9
	CHEMBL70788	210964	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	ChEMBL	607	11	2	10	5.7	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCOC(=O)Nc1cccnc1	10.1016/S0960-894X(97)00400-9
	5344	180252	101	None	-	1	Rat	5.1	pIC50	=	5.1	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	267	3	2	5	1.7	Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C	10.1016/s0960-894x(00)00366-8
	CHEMBL453	180252	101	None	-	1	Rat	5.1	pIC50	=	5.1	Binding	Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor	ChEMBL	267	3	2	5	1.7	Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C	10.1016/s0960-894x(00)00366-8
	10015852	106217	2	None	-	0	Rat	5.1	pIC50	=	5.1	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	268	3	2	5	1.8	Cc1noc(NS(=O)(=O)c2ccc(O)cc2)c1C	10.1021/jm00004a012
	CHEMBL282961	106217	2	None	-	0	Rat	5.1	pIC50	=	5.1	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	268	3	2	5	1.8	Cc1noc(NS(=O)(=O)c2ccc(O)cc2)c1C	10.1021/jm00004a012
	22616255	212312	11	None	-	0	Human	4.1	pIC50	=	4.1	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	297	4	1	6	2.0	Cc1noc(NS(=O)(=O)c2ccc([N+](=O)[O-])cc2)c1C	10.1016/0960-894X(96)00441-6
	CHEMBL80945	212312	11	None	-	0	Human	4.1	pIC50	=	4.1	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	297	4	1	6	2.0	Cc1noc(NS(=O)(=O)c2ccc([N+](=O)[O-])cc2)c1C	10.1016/0960-894X(96)00441-6
	23445333	134584	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	484	6	1	7	4.4	Cc1cc2c(cc1CCc1ccsc1S(=O)(=O)Nc1onc(C)c1Br)OCO2	10.1016/S0960-894X(97)00133-9
	CHEMBL366378	134584	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	484	6	1	7	4.4	Cc1cc2c(cc1CCc1ccsc1S(=O)(=O)Nc1onc(C)c1Br)OCO2	10.1016/S0960-894X(97)00133-9
	CHEMBL313984	217902	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00070a001
	CHEMBL317099	217977	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00015a003
	10792636	175294	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	544	10	2	6	5.4	CCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(CC)cccc2CC)cc1	10.1021/jm990170q
	CHEMBL435385	175294	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	544	10	2	6	5.4	CCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(CC)cccc2CC)cc1	10.1021/jm990170q
	CHEMBL315658	217970	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00070a001
	127026042	144035	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes	ChEMBL	620	11	3	9	3.8	CCCc1nc2c(C)cc(C(=O)NCCN3CCN(C)CC3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1	10.1039/C5MD00169B
	CHEMBL3751986	144035	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes	ChEMBL	620	11	3	9	3.8	CCCc1nc2c(C)cc(C(=O)NCCN3CCN(C)CC3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1	10.1039/C5MD00169B
	CHEMBL315658	217970	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Displacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cellsDisplacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)81215-4
	11145367	16789	0	None	-	0	Pig	7.0	pIC50	=	7.0	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	487	10	1	8	4.4	COCCOc1ncnc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1cccc(OC)c1	10.1021/jm0102304
	CHEMBL114985	16789	0	None	-	0	Pig	7.0	pIC50	=	7.0	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	487	10	1	8	4.4	COCCOc1ncnc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1cccc(OC)c1	10.1021/jm0102304
	10745418	120769	1	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	558	9	2	6	6.2	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(C(C)C)cccc2C(C)C)cc1	10.1021/jm990170q
	CHEMBL332627	120769	1	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	558	9	2	6	6.2	COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(C(C)C)cccc2C(C)C)cc1	10.1021/jm990170q
	10015852	106217	2	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells	ChEMBL	268	3	2	5	1.8	Cc1noc(NS(=O)(=O)c2ccc(O)cc2)c1C	10.1021/jm00029a001
	CHEMBL282961	106217	2	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells	ChEMBL	268	3	2	5	1.8	Cc1noc(NS(=O)(=O)c2ccc(O)cc2)c1C	10.1021/jm00029a001
	10015852	106217	2	None	-	0	Rat	5.0	pIC50	=	5.0	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	268	3	2	5	1.8	Cc1noc(NS(=O)(=O)c2ccc(O)cc2)c1C	10.1021/jm00008a013
	CHEMBL282961	106217	2	None	-	0	Rat	5.0	pIC50	=	5.0	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	268	3	2	5	1.8	Cc1noc(NS(=O)(=O)c2ccc(O)cc2)c1C	10.1021/jm00008a013
	11813885	174573	0	None	-	0	Pig	7.0	pIC50	=	7.0	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	579	12	1	10	5.3	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCCOc2ncc(C)cn2)c1	10.1021/jm0102304
	CHEMBL430515	174573	0	None	-	0	Pig	7.0	pIC50	=	7.0	Binding	In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells	ChEMBL	579	12	1	10	5.3	COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCCOc2ncc(C)cn2)c1	10.1021/jm0102304
	CHEMBL313056	217890	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1021/jm00070a001
	10576217	16533	0	None	-	0	Rat	6.0	pIC50	=	6.0	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	467	12	1	5	4.4	CCCCN(CCCC)C(=O)CN1C[C@H](c2cccnc2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	CHEMBL113494	16533	0	None	-	0	Rat	6.0	pIC50	=	6.0	Binding	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	ChEMBL	467	12	1	5	4.4	CCCCN(CCCC)C(=O)CN1C[C@H](c2cccnc2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1	10.1021/jm960077r
	CHEMBL146155	215554	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Displacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cellsDisplacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)81215-4
	11798109	19131	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	457	7	2	7	4.2	COc1cccc(NCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)c1	10.1021/jm9608366
	CHEMBL1185459	19131	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	457	7	2	7	4.2	COc1cccc(NCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)c1	10.1021/jm9608366
	CHEMBL416086	19131	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	457	7	2	7	4.2	COc1cccc(NCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)c1	10.1021/jm9608366
	23445544	68149	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Tested for its activity in cloned human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayTested for its activity in cloned human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	438	5	1	5	5.1	Cc1ccc(/C=C/c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1	10.1016/S0960-894X(97)00133-9
	CHEMBL176912	68149	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Tested for its activity in cloned human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayTested for its activity in cloned human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay	ChEMBL	438	5	1	5	5.1	Cc1ccc(/C=C/c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1	10.1016/S0960-894X(97)00133-9
	3887	8853	45	None	-436	4	Human	7.0	pIC50	=	7.0	Binding	Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane incubated for 2 hrsDisplacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane incubated for 2 hrs	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01781
	5311192	8853	45	None	-436	4	Human	7.0	pIC50	=	7.0	Binding	Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane incubated for 2 hrsDisplacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane incubated for 2 hrs	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01781
	CHEMBL72410	8853	45	None	-436	4	Human	7.0	pIC50	=	7.0	Binding	Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane incubated for 2 hrsDisplacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane incubated for 2 hrs	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01781
	44386002	67070	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	503	9	1	9	3.9	C#CCOc1nc(-c2ccncc2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	CHEMBL174326	67070	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	503	9	1	9	3.9	C#CCOc1nc(-c2ccncc2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	11005242	209674	0	None	-	0	Rat	7.0	pIC50	=	7.0	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	474	8	1	6	5.6	CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc(OC)cc1)O2	10.1021/jm010382z
	CHEMBL62719	209674	0	None	-	0	Rat	7.0	pIC50	=	7.0	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	474	8	1	6	5.6	CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc(OC)cc1)O2	10.1021/jm010382z
	44293682	192465	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	447	7	1	6	4.4	CCOc1ccc2c(c1)[C@H](c1ccc(OC)cc1)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	CHEMBL48652	192465	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	447	7	1	6	4.4	CCOc1ccc2c(c1)[C@H](c1ccc(OC)cc1)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	10553165	16512	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	492	7	1	6	5.4	O=C1OC(O)(c2ccc(OCc3ccccc3)cc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2	10.1021/jm9606507
	CHEMBL11341	16512	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells	ChEMBL	492	7	1	6	5.4	O=C1OC(O)(c2ccc(OCc3ccccc3)cc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2	10.1021/jm9606507
	CHEMBL414917	219939	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Binding affinity in LtK cells stably transfected with human endothelin A (ETA) receptorBinding affinity in LtK cells stably transfected with human endothelin A (ETA) receptor	ChEMBL		None	None	None		NC(=O)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)C1c2ccccc2CCc2ccccc21)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/0960-894X(95)00084-7
	CHEMBL289687	217654	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Displacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cellsDisplacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]cn1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)81215-4
	CHEMBL289687	217654	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Inhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cellsInhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cells	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]cn1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00095a029
	127035085	143210	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	661	12	2	7	7.4	CCCc1nc2c(C)cc(C(=O)NCCc3ccccc3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	CHEMBL3735574	143210	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	ChEMBL	661	12	2	7	7.4	CCCc1nc2c(C)cc(C(=O)NCCc3ccccc3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1039/C4MD00499J
	44293741	193740	0	None	-	0	Rat	7.0	pIC50	=	7.0	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	447	7	1	6	4.4	CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1021/jm031041j
	CHEMBL49040	193740	0	None	-	0	Rat	7.0	pIC50	=	7.0	Binding	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	ChEMBL	447	7	1	6	4.4	CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1021/jm031041j
	44293868	108367	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	551	11	2	9	3.9	CCOc1ccc2c(c1)[C@H](c1ccc(OC)c(OC)c1OCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	CHEMBL298664	108367	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	551	11	2	9	3.9	CCOc1ccc2c(c1)[C@H](c1ccc(OC)c(OC)c1OCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	44293741	193740	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	447	7	1	6	4.4	CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	CHEMBL49040	193740	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor	ChEMBL	447	7	1	6	4.4	CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	44384766	66439	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	532	10	1	10	4.1	C#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	CHEMBL172184	66439	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	532	10	1	10	4.1	C#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	44385940	137450	0	None	-	0	Rat	6.0	pIC50	=	6.0	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	551	10	4	6	4.9	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCC(C)C2)nc1C(=O)O	10.1021/jm950592+
	CHEMBL368255	137450	0	None	-	0	Rat	6.0	pIC50	=	6.0	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	551	10	4	6	4.9	Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCC(C)C2)nc1C(=O)O	10.1021/jm950592+
	44386421	67511	0	None	-	0	Rat	5.0	pIC50	=	5.0	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	537	10	4	5	4.5	Cc1oc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1CC(=O)O	10.1021/jm950592+
	CHEMBL176093	67511	0	None	-	0	Rat	5.0	pIC50	=	5.0	Binding	Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates	ChEMBL	537	10	4	5	4.5	Cc1oc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1CC(=O)O	10.1021/jm950592+
	9807456	67247	0	None	-	1	Human	7.0	pIC50	=	7.0	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	545	9	1	9	4.8	C#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	CHEMBL175435	67247	0	None	-	1	Human	7.0	pIC50	=	7.0	Binding	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	ChEMBL	545	9	1	9	4.8	C#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC	10.1016/s0960-894x(02)01084-3
	10195727	210706	0	None	-	0	Rat	7.0	pIC50	=	7.0	Binding	Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor	ChEMBL	487	7	1	8	5.6	CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2nsnc2c1	10.1016/s0960-894x(97)10151-2
	CHEMBL69150	210706	0	None	-	0	Rat	7.0	pIC50	=	7.0	Binding	Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor	ChEMBL	487	7	1	8	5.6	CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2nsnc2c1	10.1016/s0960-894x(97)10151-2
	10195727	210706	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Potency at Endothelin A receptor was determinedPotency at Endothelin A receptor was determined	ChEMBL	487	7	1	8	5.6	CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2nsnc2c1	10.1021/jm0300429
	CHEMBL69150	210706	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Potency at Endothelin A receptor was determinedPotency at Endothelin A receptor was determined	ChEMBL	487	7	1	8	5.6	CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2nsnc2c1	10.1021/jm0300429
	44279360	113367	0	None	-	0	Pig	6.0	pIC50	=	6.0	Binding	Binding affinity against ETA receptor in porcine aortic smooth muscle membraneBinding affinity against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	498	13	5	4	2.9	CC(C)C[C@H](NC(=O)CC1CCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	CHEMBL31426	113367	0	None	-	0	Pig	6.0	pIC50	=	6.0	Binding	Binding affinity against ETA receptor in porcine aortic smooth muscle membraneBinding affinity against ETA receptor in porcine aortic smooth muscle membrane	ChEMBL	498	13	5	4	2.9	CC(C)C[C@H](NC(=O)CC1CCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O	10.1016/0960-894X(95)00221-E
	11048815	109092	0	None	-	0	Rat	6.0	pIC50	=	6.0	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	460	7	1	6	5.2	CCCOc1ccc2c(c1)OC(c1ccc3c(c1)OCO3)C(C(=O)O)=C2c1ccc(OC)cc1	10.1021/jm010382z
	CHEMBL303531	109092	0	None	-	0	Rat	6.0	pIC50	=	6.0	Binding	Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells	ChEMBL	460	7	1	6	5.2	CCCOc1ccc2c(c1)OC(c1ccc3c(c1)OCO3)C(C(=O)O)=C2c1ccc(OC)cc1	10.1021/jm010382z
	10625738	176272	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	517	6	2	6	5.5	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc(-c3ccccc3)cc2)c1Br	10.1021/jm9608366
	CHEMBL44321	176272	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay	ChEMBL	517	6	2	6	5.5	Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc(-c3ccccc3)cc2)c1Br	10.1021/jm9608366
	9801094	66265	0	None	-	0	Rat	7.0	pIC50	=	7.0	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	399	7	1	5	5.1	N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1cccc(Cl)c1	10.1021/jm990378b
	CHEMBL171446	66265	0	None	-	0	Rat	7.0	pIC50	=	7.0	Binding	In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.	ChEMBL	399	7	1	5	5.1	N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1cccc(Cl)c1	10.1021/jm990378b
	CHEMBL359235	218584	0	None	-	0	Mouse	7.0	pIC50	=	7.0	Binding	Inhibition of [125I]ET1 binding to Endothelin A receptor of murine 3T3 cellsInhibition of [125I]ET1 binding to Endothelin A receptor of murine 3T3 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@H](C)CC	10.1016/S0960-894X(01)81219-1
	44316686	110294	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	286	3	1	4	2.7	Cc1noc(NS(=O)(=O)c2ccccc2Cl)c1C	10.1016/0960-894X(96)00441-6
	CHEMBL308521	110294	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	286	3	1	4	2.7	Cc1noc(NS(=O)(=O)c2ccccc2Cl)c1C	10.1016/0960-894X(96)00441-6
	10021240	102270	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells	ChEMBL	357	6	2	5	3.7	Cc1noc(NS(=O)(=O)c2ccc(NCc3ccccc3)cc2)c1C	10.1021/jm00029a001
	CHEMBL25730	102270	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells	ChEMBL	357	6	2	5	3.7	Cc1noc(NS(=O)(=O)c2ccc(NCc3ccccc3)cc2)c1C	10.1021/jm00029a001
	10021240	102270	0	None	-	0	Rat	5.0	pIC50	=	5.0	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	357	6	2	5	3.7	Cc1noc(NS(=O)(=O)c2ccc(NCc3ccccc3)cc2)c1C	10.1021/jm00008a013
	CHEMBL25730	102270	0	None	-	0	Rat	5.0	pIC50	=	5.0	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	357	6	2	5	3.7	Cc1noc(NS(=O)(=O)c2ccc(NCc3ccccc3)cc2)c1C	10.1021/jm00008a013
	10087192	106359	1	None	-	0	Rat	5.0	pIC50	=	5.0	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	317	3	2	5	2.8	Cc1noc(NS(=O)(=O)c2ccc3cccc(N)c3c2)c1C	10.1021/jm00008a013
	CHEMBL283879	106359	1	None	-	0	Rat	5.0	pIC50	=	5.0	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	ChEMBL	317	3	2	5	2.8	Cc1noc(NS(=O)(=O)c2ccc3cccc(N)c3c2)c1C	10.1021/jm00008a013
	10087192	106359	1	None	-	0	Rat	5.0	pIC50	=	5.0	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	317	3	2	5	2.8	Cc1noc(NS(=O)(=O)c2ccc3cccc(N)c3c2)c1C	10.1021/jm00004a012
	CHEMBL283879	106359	1	None	-	0	Rat	5.0	pIC50	=	5.0	Binding	Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells	ChEMBL	317	3	2	5	2.8	Cc1noc(NS(=O)(=O)c2ccc3cccc(N)c3c2)c1C	10.1021/jm00004a012
	44276993	113631	0	None	-	0	Rat	4.0	pIC50	=	4.0	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	362	5	1	3	3.8	COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccccc3)c2=O)c1	10.1016/s0960-894x(00)00232-8
	CHEMBL3144831	113631	0	None	-	0	Rat	4.0	pIC50	=	4.0	Binding	In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay	ChEMBL	362	5	1	3	3.8	COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccccc3)c2=O)c1	10.1016/s0960-894x(00)00232-8
	5472495	193412	47	None	-	1	Human	5.0	pIC50	=	5.0	Binding	DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)	ChEMBL	372	4	1	3	4.0	CC1=C(CC(=O)O)c2cc(F)ccc2/C1=C\c1ccc(S(C)(=O)=O)cc1	nan
	CHEMBL488025	193412	47	None	-	1	Human	5.0	pIC50	=	5.0	Binding	DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)	ChEMBL	372	4	1	3	4.0	CC1=C(CC(=O)O)c2cc(F)ccc2/C1=C\c1ccc(S(C)(=O)=O)cc1	nan
	18617381	112458	0	None	-	0	Human	6.0	pIC50	=	6	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	300	3	1	4	3.1	Cc1noc(NS(=O)(=O)c2cccc(Cl)c2C)c1C	10.1016/0960-894X(96)00441-6
	CHEMBL312551	112458	0	None	-	0	Human	6.0	pIC50	=	6	Binding	Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	300	3	1	4	3.1	Cc1noc(NS(=O)(=O)c2cccc(Cl)c2C)c1C	10.1016/0960-894X(96)00441-6
	15453170	111678	4	None	-	0	Human	5.0	pIC50	=	5	Binding	Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	328	4	1	4	3.8	Cc1noc(NS(=O)(=O)c2ccc(-c3ccccc3)cc2)c1C	10.1016/0960-894X(96)00441-6
	CHEMBL311258	111678	4	None	-	0	Human	5.0	pIC50	=	5	Binding	Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation	ChEMBL	328	4	1	4	3.8	Cc1noc(NS(=O)(=O)c2ccc(-c3ccccc3)cc2)c1C	10.1016/0960-894X(96)00441-6
	1009	6982	25	None	-	1	Human	5.0	pIC50	=	5	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	558	11	2	6	5.8	CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2	10.1021/jm990170q
	5310991	6982	25	None	-	1	Human	5.0	pIC50	=	5	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	558	11	2	6	5.8	CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2	10.1021/jm990170q
	CHEMBL332794	6982	25	None	-	1	Human	5.0	pIC50	=	5	Binding	Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)	ChEMBL	558	11	2	6	5.8	CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2	10.1021/jm990170q
	44284481	220504	0	None	-6	5	Rat	9.8	pKd	=	9.8	Binding	Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligandBinding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)81085-4
	CHEMBL437472	220504	0	None	-6	5	Rat	9.8	pKd	=	9.8	Binding	Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligandBinding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)81085-4
	CHEMBL409577	219548	0	None	-	1	Rat	9.5	pKd	=	9.5	Binding	Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 1)Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 1)	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC(=O)[C@H](C)NC(=O)[C@@H](CO)NC(=O)[C@H](N)CSSC[C@H](C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)[C@@H](C)CC)[C@@H](C)CC)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](C(C)C)NC(=O)[C@H](C)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC1=O	10.1016/S0960-894X(01)81085-4
	CHEMBL442316	220690	0	None	-	1	Rat	9.2	pKd	=	9.2	Binding	Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 1)Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 1)	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)81085-4
	19095644	176491	0	None	-	1	Rat	6.9	pKd	=	6.9	Binding	Antagonist activity at rat aortic ring ETA receptor in presence of ET1Antagonist activity at rat aortic ring ETA receptor in presence of ET1	ChEMBL	549	10	2	8	5.4	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ccccc2)nc1OCCO	10.1016/j.bmcl.2016.06.014
	CHEMBL4438132	176491	0	None	-	1	Rat	6.9	pKd	=	6.9	Binding	Antagonist activity at rat aortic ring ETA receptor in presence of ET1Antagonist activity at rat aortic ring ETA receptor in presence of ET1	ChEMBL	549	10	2	8	5.4	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ccccc2)nc1OCCO	10.1016/j.bmcl.2016.06.014
	CHEMBL438470	220551	0	None	-	1	Rat	6.9	pKd	=	6.9	Binding	Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligandBinding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@@H](C)NC2=O)C(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)81085-4
	CHEMBL412467	219772	0	None	-	1	Rat	5.9	pKd	=	5.9	Binding	Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 2)Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 2)	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@H](C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)81085-4
	19735343	182830	0	None	-	1	Rat	5.8	pKd	=	5.8	Binding	Antagonist activity at rat aortic ring ETA receptor in presence of ET1Antagonist activity at rat aortic ring ETA receptor in presence of ET1	ChEMBL	473	7	2	6	4.0	O=S(=O)(Nc1ncnc(OCCO)c1-c1ccc(Cl)cc1)c1ccc(C(F)(F)F)cc1	10.1016/j.bmcl.2016.06.014
	CHEMBL4590568	182830	0	None	-	1	Rat	5.8	pKd	=	5.8	Binding	Antagonist activity at rat aortic ring ETA receptor in presence of ET1Antagonist activity at rat aortic ring ETA receptor in presence of ET1	ChEMBL	473	7	2	6	4.0	O=S(=O)(Nc1ncnc(OCCO)c1-c1ccc(Cl)cc1)c1ccc(C(F)(F)F)cc1	10.1016/j.bmcl.2016.06.014
	CHEMBL409577	219548	0	None	-	1	Rat	7.8	pKd	=	7.8	Binding	Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 2)Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 2)	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC(=O)[C@H](C)NC(=O)[C@@H](CO)NC(=O)[C@H](N)CSSC[C@H](C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)[C@@H](C)CC)[C@@H](C)CC)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](C(C)C)NC(=O)[C@H](C)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC1=O	10.1016/S0960-894X(01)81085-4
	CHEMBL386629	219164	0	None	-	1	Rat	6.7	pKd	=	6.7	Binding	Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligandBinding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@@H](C)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)81085-4
	155519384	177197	0	None	-	1	Rat	7.7	pKd	=	7.7	Binding	Antagonist activity at rat aortic ring ETA receptor in presence of ET1Antagonist activity at rat aortic ring ETA receptor in presence of ET1	ChEMBL	674	12	1	13	4.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)c1ccccn1	10.1016/j.bmcl.2016.06.014
	CHEMBL4448273	177197	0	None	-	1	Rat	7.7	pKd	=	7.7	Binding	Antagonist activity at rat aortic ring ETA receptor in presence of ET1Antagonist activity at rat aortic ring ETA receptor in presence of ET1	ChEMBL	674	12	1	13	4.1	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)c1ccccn1	10.1016/j.bmcl.2016.06.014
	CHEMBL438027	220522	0	None	-	1	Rat	5.7	pKd	=	5.7	Binding	Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 2)Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 2)	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)81085-4
	CHEMBL263581	217355	0	None	-	1	Rat	8.7	pKd	=	8.7	Binding	Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligandBinding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/S0960-894X(01)81085-4
	CHEMBL410001	219573	0	None	-	1	Rat	5.5	pKd	=	5.5	Binding	Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligandBinding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)81085-4
	CHEMBL412467	219772	0	None	-	1	Rat	7.5	pKd	=	7.5	Binding	Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 1)Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 1)	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@H](C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)81085-4
	CHEMBL409171	219528	0	None	-	1	Rat	5.5	pKd	=	5.5	Binding	Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 2)Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 2)	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/S0960-894X(01)81085-4
	104865	7493	99	None	-1	4	Rat	7.4	pKd	=	7.4	Binding	Antagonist activity at rat aortic ring ETA receptor in presence of ET1Antagonist activity at rat aortic ring ETA receptor in presence of ET1	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/j.bmcl.2016.06.014
	3494	7493	99	None	-1	4	Rat	7.4	pKd	=	7.4	Binding	Antagonist activity at rat aortic ring ETA receptor in presence of ET1Antagonist activity at rat aortic ring ETA receptor in presence of ET1	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/j.bmcl.2016.06.014
	392	7493	99	None	-1	4	Rat	7.4	pKd	=	7.4	Binding	Antagonist activity at rat aortic ring ETA receptor in presence of ET1Antagonist activity at rat aortic ring ETA receptor in presence of ET1	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/j.bmcl.2016.06.014
	CHEMBL957	7493	99	None	-1	4	Rat	7.4	pKd	=	7.4	Binding	Antagonist activity at rat aortic ring ETA receptor in presence of ET1Antagonist activity at rat aortic ring ETA receptor in presence of ET1	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/j.bmcl.2016.06.014
	DB00559	7493	99	None	-1	4	Rat	7.4	pKd	=	7.4	Binding	Antagonist activity at rat aortic ring ETA receptor in presence of ET1Antagonist activity at rat aortic ring ETA receptor in presence of ET1	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1016/j.bmcl.2016.06.014
	10395582	23740	0	None	-	1	Rat	5.4	pKd	=	5.4	Binding	Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligandBinding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand	ChEMBL	806	8	6	13	3.2	CC(=O)O[C@@]12CO[C@@H]1C[C@H](O)[C@@]1(C)C(=O)[C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)Nc4ccccc4)C(C)(C)C)C[C@@](O)([C@@H](OC(=O)c4ccccc4)[C@@H]12)C3(C)C	10.1016/S0960-894X(01)81085-4
	CHEMBL125377	23740	0	None	-	1	Rat	5.4	pKd	=	5.4	Binding	Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligandBinding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand	ChEMBL	806	8	6	13	3.2	CC(=O)O[C@@]12CO[C@@H]1C[C@H](O)[C@@]1(C)C(=O)[C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)Nc4ccccc4)C(C)(C)C)C[C@@](O)([C@@H](OC(=O)c4ccccc4)[C@@H]12)C3(C)C	10.1016/S0960-894X(01)81085-4
	CHEMBL414286	219899	0	None	-	1	Rat	6.4	pKd	=	6.4	Binding	Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 2)Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 2)	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@@H](N)C(=O)N[C@H](C)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)81085-4
	CHEMBL409578	219549	0	None	-	1	Rat	5.3	pKd	=	5.3	Binding	Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligandBinding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@@H](NC(C)=O)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)81085-4
	CHEMBL412346	219763	0	None	-	1	Rat	7.3	pKd	=	7.3	Binding	Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligandBinding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)81085-4
	CHEMBL438027	220522	0	None	-	1	Rat	8.2	pKd	=	8.2	Binding	Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 1)Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 1)	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)81085-4
	CHEMBL268318	217523	0	None	-	1	Rat	6.2	pKd	=	6.2	Binding	Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligandBinding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](C)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)81085-4
	CHEMBL442316	220690	0	None	-	1	Rat	7.1	pKd	=	7.1	Binding	Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 2)Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 2)	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)81085-4
	CHEMBL414286	219899	0	None	-	1	Rat	8.0	pKd	=	8.0	Binding	Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 1)Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 1)	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@@H](N)C(=O)N[C@H](C)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/S0960-894X(01)81085-4
	CHEMBL407887	219471	0	None	-	1	Rat	6.0	pKd	=	6.0	Binding	Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligandBinding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand	ChEMBL		None	None	None		CSCC[C@@H]1NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC1=O)C(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)O)CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N2	10.1016/S0960-894X(01)81085-4
	10983585	180053	0	None	-	1	Rat	6.0	pKd	=	6.0	Binding	Antagonist activity at rat aortic ring ETA receptor in presence of ET1Antagonist activity at rat aortic ring ETA receptor in presence of ET1	ChEMBL	473	9	2	8	3.7	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)ncnc1OCCO	10.1016/j.bmcl.2016.06.014
	CHEMBL4525321	180053	0	None	-	1	Rat	6.0	pKd	=	6.0	Binding	Antagonist activity at rat aortic ring ETA receptor in presence of ET1Antagonist activity at rat aortic ring ETA receptor in presence of ET1	ChEMBL	473	9	2	8	3.7	COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)ncnc1OCCO	10.1016/j.bmcl.2016.06.014
	CHEMBL409171	219528	0	None	-	1	Rat	7.0	pKd	=	7.0	Binding	Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 1)Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 1)	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/S0960-894X(01)81085-4
	44277840	105030	0	None	81283	2	Human	11.0	pKi	=	11	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	522	7	1	7	5.8	Cc1onc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2N(C)C(=O)CC(C)(C)C)c1C	10.1021/jm020289q
	CHEMBL274489	105030	0	None	81283	2	Human	11.0	pKi	=	11	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	522	7	1	7	5.8	Cc1onc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2N(C)C(=O)CC(C)(C)C)c1C	10.1021/jm020289q
	11071765	175986	0	None	8709	2	Human	11.0	pKi	=	11	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	556	9	1	7	5.6	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)Cc2ccccc2)c1C	10.1021/jm020289q
	CHEMBL440780	175986	0	None	8709	2	Human	11.0	pKi	=	11	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	556	9	1	7	5.6	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)Cc2ccccc2)c1C	10.1021/jm020289q
	44275660	105452	0	None	-	1	Human	11.0	pKi	=	11	Binding	Inhibitory concentration against Endothelin A receptorInhibitory concentration against Endothelin A receptor	ChEMBL	522	8	2	7	5.5	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CNC(=O)CC(C)(C)C)c1C	10.1021/jm030480f
	CHEMBL277447	105452	0	None	-	1	Human	11.0	pKi	=	11	Binding	Inhibitory concentration against Endothelin A receptorInhibitory concentration against Endothelin A receptor	ChEMBL	522	8	2	7	5.5	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CNC(=O)CC(C)(C)C)c1C	10.1021/jm030480f
	9852318	16386	8	None	2691	2	Human	10.8	pKi	=	10.8	Binding	Ability to inhibit [125I]ET1 binding to human cloned endothelin A receptor expressed on CHO cellsAbility to inhibit [125I]ET1 binding to human cloned endothelin A receptor expressed on CHO cells	ChEMBL	613	11	2	9	4.5	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm000538f
	CHEMBL112624	16386	8	None	2691	2	Human	10.8	pKi	=	10.8	Binding	Ability to inhibit [125I]ET1 binding to human cloned endothelin A receptor expressed on CHO cellsAbility to inhibit [125I]ET1 binding to human cloned endothelin A receptor expressed on CHO cells	ChEMBL	613	11	2	9	4.5	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm000538f
	CHEMBL1627022	16386	8	None	2691	2	Human	10.8	pKi	=	10.8	Binding	Ability to inhibit [125I]ET1 binding to human cloned endothelin A receptor expressed on CHO cellsAbility to inhibit [125I]ET1 binding to human cloned endothelin A receptor expressed on CHO cells	ChEMBL	613	11	2	9	4.5	Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1	10.1021/jm000538f
	10119517	106010	0	None	169824	2	Human	10.7	pKi	=	10.7	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	536	8	1	7	5.8	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)CC(C)(C)C)c1C	10.1021/jm020289q
	CHEMBL281659	106010	0	None	169824	2	Human	10.7	pKi	=	10.7	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	536	8	1	7	5.8	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)CC(C)(C)C)c1C	10.1021/jm020289q
	11124425	106640	0	None	75857	2	Human	10.7	pKi	=	10.7	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	543	7	1	8	5.7	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2Cn2ccc(C(F)(F)F)n2)c1C	10.1021/jm020289q
	CHEMBL285832	106640	0	None	75857	2	Human	10.7	pKi	=	10.7	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	543	7	1	8	5.7	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2Cn2ccc(C(F)(F)F)n2)c1C	10.1021/jm020289q
	10918301	108273	0	None	7585	2	Human	10.7	pKi	=	10.7	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	514	8	1	7	6.1	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)c2ccccc2)c1C	10.1021/jm020289q
	CHEMBL29793	108273	0	None	7585	2	Human	10.7	pKi	=	10.7	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	514	8	1	7	6.1	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)c2ccccc2)c1C	10.1021/jm020289q
	44284481	220504	0	None	-4	5	Human	10.6	pKi	=	10.6	Binding	Binding affinity to human ETA receptor by radioligand displacement assayBinding affinity to human ETA receptor by radioligand displacement assay	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/j.ejmech.2013.01.044
	CHEMBL437472	220504	0	None	-4	5	Human	10.6	pKi	=	10.6	Binding	Binding affinity to human ETA receptor by radioligand displacement assayBinding affinity to human ETA receptor by radioligand displacement assay	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/j.ejmech.2013.01.044
	11731054	105587	0	None	21379	2	Human	10.5	pKi	=	10.5	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	522	7	1	7	5.4	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)C(C)(C)C)c1C	10.1021/jm020289q
	CHEMBL27855	105587	0	None	21379	2	Human	10.5	pKi	=	10.5	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	522	7	1	7	5.4	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)C(C)(C)C)c1C	10.1021/jm020289q
	159594	7310	45	None	-1	3	Rat	10.5	pKi	=	10.5	Binding	Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm030528p
	3487	7310	45	None	-1	3	Rat	10.5	pKi	=	10.5	Binding	Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm030528p
	CHEMBL9194	7310	45	None	-1	3	Rat	10.5	pKi	=	10.5	Binding	Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm030528p
	DB06199	7310	45	None	-1	3	Rat	10.5	pKi	=	10.5	Binding	Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm030528p
	186002	109619	23	None	-1	3	Rat	10.5	pKi	=	10.5	Binding	Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor	ChEMBL	531	10	2	6	5.4	CCCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1C[C@H](C)C(=O)O)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2	10.1021/jm030528p
	CHEMBL305576	109619	23	None	-1	3	Rat	10.5	pKi	=	10.5	Binding	Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor	ChEMBL	531	10	2	6	5.4	CCCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1C[C@H](C)C(=O)O)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2	10.1021/jm030528p
	44284481	220504	0	None	-6	5	Rat	10.5	pKi	=	10.5	Binding	Compound was evaluated for the binding affinity to Endothelin A receptor in the rat atriumCompound was evaluated for the binding affinity to Endothelin A receptor in the rat atrium	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00087a001
	CHEMBL437472	220504	0	None	-6	5	Rat	10.5	pKi	=	10.5	Binding	Compound was evaluated for the binding affinity to Endothelin A receptor in the rat atriumCompound was evaluated for the binding affinity to Endothelin A receptor in the rat atrium	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00087a001
	159594	7310	45	None	1	3	Human	10.5	pKi	=	10.5	Binding	Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membraneDisplacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/acs.jmedchem.5b01781
	3487	7310	45	None	1	3	Human	10.5	pKi	=	10.5	Binding	Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membraneDisplacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/acs.jmedchem.5b01781
	CHEMBL9194	7310	45	None	1	3	Human	10.5	pKi	=	10.5	Binding	Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membraneDisplacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/acs.jmedchem.5b01781
	DB06199	7310	45	None	1	3	Human	10.5	pKi	=	10.5	Binding	Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membraneDisplacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/acs.jmedchem.5b01781
	159594	7310	45	None	1	3	Human	10.5	pKi	=	10.5	Binding	Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm9505369
	3487	7310	45	None	1	3	Human	10.5	pKi	=	10.5	Binding	Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm9505369
	CHEMBL9194	7310	45	None	1	3	Human	10.5	pKi	=	10.5	Binding	Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm9505369
	DB06199	7310	45	None	1	3	Human	10.5	pKi	=	10.5	Binding	Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm9505369
	9936145	25799	2	None	-	1	Human	10.4	pKi	=	10.4	Binding	Binding affinity against human Endothelin A receptorBinding affinity against human Endothelin A receptor	ChEMBL	510	11	1	4	5.3	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(C)c(F)c1	10.1021/jm010237l
	CHEMBL128818	25799	2	None	-	1	Human	10.4	pKi	=	10.4	Binding	Binding affinity against human Endothelin A receptorBinding affinity against human Endothelin A receptor	ChEMBL	510	11	1	4	5.3	CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(C)c(F)c1	10.1021/jm010237l
	44284481	220504	0	None	-3	5	Pig	10.4	pKi	=	10.4	Binding	Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(96)00421-0
	CHEMBL437472	220504	0	None	-3	5	Pig	10.4	pKi	=	10.4	Binding	Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(96)00421-0
	9958321	85926	0	None	19498	2	Human	10.4	pKi	=	10.4	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	520	7	1	7	5.2	Cc1onc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN2CCC(C)(C)C2=O)c1C	10.1021/jm020289q
	CHEMBL2113316	85926	0	None	19498	2	Human	10.4	pKi	=	10.4	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	520	7	1	7	5.2	Cc1onc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN2CCC(C)(C)C2=O)c1C	10.1021/jm020289q
	11813553	106122	0	None	14454	2	Human	10.4	pKi	=	10.4	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	542	8	1	7	5.7	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)c2ccccc2)c1C	10.1021/jm020289q
	CHEMBL282359	106122	0	None	14454	2	Human	10.4	pKi	=	10.4	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	542	8	1	7	5.7	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)c2ccccc2)c1C	10.1021/jm020289q
	11027595	107017	0	None	19952	2	Human	10.4	pKi	=	10.4	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	508	8	1	7	5.0	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)C(C)C)c1C	10.1021/jm020289q
	CHEMBL28863	107017	0	None	19952	2	Human	10.4	pKi	=	10.4	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	508	8	1	7	5.0	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)C(C)C)c1C	10.1021/jm020289q
	10918368	109300	0	None	21379	2	Human	10.4	pKi	=	10.4	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	520	7	1	7	5.2	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN2CC(C)(C)CC2=O)c1C	10.1021/jm020289q
	CHEMBL30405	109300	0	None	21379	2	Human	10.4	pKi	=	10.4	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	520	7	1	7	5.2	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN2CC(C)(C)CC2=O)c1C	10.1021/jm020289q
	159594	7310	45	None	-1	3	Rat	10.3	pKi	=	10.3	Binding	binding affinity against human Endothelin A receptorbinding affinity against human Endothelin A receptor	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm010237l
	3487	7310	45	None	-1	3	Rat	10.3	pKi	=	10.3	Binding	binding affinity against human Endothelin A receptorbinding affinity against human Endothelin A receptor	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm010237l
	CHEMBL9194	7310	45	None	-1	3	Rat	10.3	pKi	=	10.3	Binding	binding affinity against human Endothelin A receptorbinding affinity against human Endothelin A receptor	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm010237l
	DB06199	7310	45	None	-1	3	Rat	10.3	pKi	=	10.3	Binding	binding affinity against human Endothelin A receptorbinding affinity against human Endothelin A receptor	ChEMBL	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	10.1021/jm010237l
	11082168	105991	0	None	7585	2	Human	10.3	pKi	=	10.3	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	548	8	1	7	5.3	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)CC(F)(F)F)c1C	10.1021/jm020289q
	CHEMBL281549	105991	0	None	7585	2	Human	10.3	pKi	=	10.3	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	548	8	1	7	5.3	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)CC(F)(F)F)c1C	10.1021/jm020289q
	10929533	107131	0	None	10964	2	Human	10.3	pKi	=	10.3	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	534	9	1	7	5.6	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C(=O)C(C)C)C2CC2)c1C	10.1021/jm020289q
	CHEMBL28963	107131	0	None	10964	2	Human	10.3	pKi	=	10.3	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	534	9	1	7	5.6	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C(=O)C(C)C)C2CC2)c1C	10.1021/jm020289q
	9914310	213422	8	None	1995	2	Human	10.2	pKi	=	10.2	Binding	Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells	ChEMBL	510	12	1	6	4.7	CCCCN(CCCC)C(=O)CN1CC(c2ccc3c(c2)OCO3)C(C(=O)O)C1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL8923	213422	8	None	1995	2	Human	10.2	pKi	=	10.2	Binding	Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells	ChEMBL	510	12	1	6	4.7	CCCCN(CCCC)C(=O)CN1CC(c2ccc3c(c2)OCO3)C(C(=O)O)C1c1ccc(OC)cc1	10.1021/jm9505369
	11762890	107439	0	None	14791	2	Human	10.2	pKi	=	10.2	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	505	8	2	9	5.3	Cc1cc(NCc2cc(-c3ncco3)ccc2-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)no1	10.1021/jm020289q
	CHEMBL29223	107439	0	None	14791	2	Human	10.2	pKi	=	10.2	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	505	8	2	9	5.3	Cc1cc(NCc2cc(-c3ncco3)ccc2-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)no1	10.1021/jm020289q
	131845706	10245	6	None	-11	2	Rat	10.1	pKi	=	10.1	Binding	Compound was evaluated for the binding affinity to Endothelin A receptor in the rat atriumCompound was evaluated for the binding affinity to Endothelin A receptor in the rat atrium	ChEMBL		None	None	None		None	10.1021/jm00087a001
	71308726	10245	6	None	-11	2	Rat	10.1	pKi	=	10.1	Binding	Compound was evaluated for the binding affinity to Endothelin A receptor in the rat atriumCompound was evaluated for the binding affinity to Endothelin A receptor in the rat atrium	ChEMBL		None	None	None		None	10.1021/jm00087a001
	995	10245	6	None	-11	2	Rat	10.1	pKi	=	10.1	Binding	Compound was evaluated for the binding affinity to Endothelin A receptor in the rat atriumCompound was evaluated for the binding affinity to Endothelin A receptor in the rat atrium	ChEMBL		None	None	None		None	10.1021/jm00087a001
	CHEMBL1222310	10245	6	None	-11	2	Rat	10.1	pKi	=	10.1	Binding	Compound was evaluated for the binding affinity to Endothelin A receptor in the rat atriumCompound was evaluated for the binding affinity to Endothelin A receptor in the rat atrium	ChEMBL		None	None	None		None	10.1021/jm00087a001
	CHEMBL4524099	10245	6	None	-11	2	Rat	10.1	pKi	=	10.1	Binding	Compound was evaluated for the binding affinity to Endothelin A receptor in the rat atriumCompound was evaluated for the binding affinity to Endothelin A receptor in the rat atrium	ChEMBL		None	None	None		None	10.1021/jm00087a001
	44284481	220504	0	None	-6	5	Rat	10.0	pKi	=	10.0	Binding	Compound was evaluated for the binding affinity to Endothelin A receptor in the rat aortaCompound was evaluated for the binding affinity to Endothelin A receptor in the rat aorta	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00087a001
	CHEMBL437472	220504	0	None	-6	5	Rat	10.0	pKi	=	10.0	Binding	Compound was evaluated for the binding affinity to Endothelin A receptor in the rat aortaCompound was evaluated for the binding affinity to Endothelin A receptor in the rat aorta	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00087a001
	9937336	181458	1	None	229	2	Human	10.0	pKi	=	10.0	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	510	9	1	7	4.8	CCCc1nc(C)ccc1O[C@@H](C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2	10.1016/j.bmcl.2016.06.014
	CHEMBL4559129	181458	1	None	229	2	Human	10.0	pKi	=	10.0	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	510	9	1	7	4.8	CCCc1nc(C)ccc1O[C@@H](C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2	10.1016/j.bmcl.2016.06.014
	9865409	109106	0	None	199	2	Human	9.9	pKi	=	9.9	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	394	8	1	6	3.2	COc1cc(C)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1	10.1021/jm960274q
	CHEMBL303631	109106	0	None	199	2	Human	9.9	pKi	=	9.9	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	394	8	1	6	3.2	COc1cc(C)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1	10.1021/jm960274q
	9894460	213488	9	None	24	3	Human	9.9	pKi	=	9.9	Binding	Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells	ChEMBL	539	10	2	7	4.8	CCCc1cc(C(=O)O)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2	10.1021/jm9505369
	CHEMBL313871	213488	9	None	24	3	Human	9.9	pKi	=	9.9	Binding	Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells	ChEMBL	539	10	2	7	4.8	CCCc1cc(C(=O)O)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2	10.1021/jm9505369
	CHEMBL8978	213488	9	None	24	3	Human	9.9	pKi	=	9.9	Binding	Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells	ChEMBL	539	10	2	7	4.8	CCCc1cc(C(=O)O)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2	10.1021/jm9505369
	12286	7735	36	None	1348	2	Human	9.9	pKi	=	9.9	Binding	Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)	ChEMBL	577	11	3	13	2.4	Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC	10.1021/jm980217s
	6433095	7735	36	None	1348	2	Human	9.9	pKi	=	9.9	Binding	Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)	ChEMBL	577	11	3	13	2.4	Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC	10.1021/jm980217s
	CHEMBL109648	7735	36	None	1348	2	Human	9.9	pKi	=	9.9	Binding	Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)	ChEMBL	577	11	3	13	2.4	Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC	10.1021/jm980217s
	DB06677	7735	36	None	1348	2	Human	9.9	pKi	=	9.9	Binding	Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)	ChEMBL	577	11	3	13	2.4	Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC	10.1021/jm980217s
	44284481	220504	0	None	-4	5	Human	9.9	pKi	=	9.9	Binding	Displacement of [125I]Endothelin-1 from human recombinant ETA receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Endothelin-1 from human recombinant ETA receptor expressed in CHOK1 cells after 2 hrs	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/j.bmcl.2013.01.025
	CHEMBL437472	220504	0	None	-4	5	Human	9.9	pKi	=	9.9	Binding	Displacement of [125I]Endothelin-1 from human recombinant ETA receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Endothelin-1 from human recombinant ETA receptor expressed in CHOK1 cells after 2 hrs	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/j.bmcl.2013.01.025
	44284481	220504	0	None	-4	5	Human	9.9	pKi	=	9.9	Binding	Displacement of radiolabeled endothelin-1 from human endothelin ETA receptorDisplacement of radiolabeled endothelin-1 from human endothelin ETA receptor	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm8007618
	CHEMBL437472	220504	0	None	-4	5	Human	9.9	pKi	=	9.9	Binding	Displacement of radiolabeled endothelin-1 from human endothelin ETA receptorDisplacement of radiolabeled endothelin-1 from human endothelin ETA receptor	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm8007618
	10973161	107821	0	None	6456	2	Human	9.8	pKi	=	9.8	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	502	8	2	9	4.8	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CNc2ccncn2)c1C	10.1021/jm020289q
	CHEMBL29464	107821	0	None	6456	2	Human	9.8	pKi	=	9.8	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	502	8	2	9	4.8	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CNc2ccncn2)c1C	10.1021/jm020289q
	11103326	174684	0	None	12589	2	Human	9.8	pKi	=	9.8	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	520	8	1	7	5.4	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)CC(F)(F)F)c1C	10.1021/jm020289q
	CHEMBL431296	174684	0	None	12589	2	Human	9.8	pKi	=	9.8	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	520	8	1	7	5.4	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)CC(F)(F)F)c1C	10.1021/jm020289q
	9870830	213493	38	None	66	2	Human	9.8	pKi	=	9.8	Binding	Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells	ChEMBL	506	8	1	9	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1	10.1021/jm9505369
	CHEMBL8981	213493	38	None	66	2	Human	9.8	pKi	=	9.8	Binding	Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells	ChEMBL	506	8	1	9	3.8	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1	10.1021/jm9505369
	23670447	9803	2	None	114	2	Human	9.8	pKi	=	9.8	Binding	Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)	ChEMBL	528	10	0	9	0.1	COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+]	10.1021/jm980217s
	999	9803	2	None	114	2	Human	9.8	pKi	=	9.8	Binding	Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)	ChEMBL	528	10	0	9	0.1	COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+]	10.1021/jm980217s
	CHEMBL1204799	9803	2	None	114	2	Human	9.8	pKi	=	9.8	Binding	Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)	ChEMBL	528	10	0	9	0.1	COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+]	10.1021/jm980217s
	CHEMBL25438	9803	2	None	114	2	Human	9.8	pKi	=	9.8	Binding	Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)	ChEMBL	528	10	0	9	0.1	COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+]	10.1021/jm980217s
	108002	10267	23	None	56	2	Human	9.7	pKi	=	9.7	Binding	Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor	ChEMBL	520	10	2	7	4.7	CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC	10.1021/jm970101g
	3528	10267	23	None	56	2	Human	9.7	pKi	=	9.7	Binding	Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor	ChEMBL	520	10	2	7	4.7	CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC	10.1021/jm970101g
	CHEMBL8823	10267	23	None	56	2	Human	9.7	pKi	=	9.7	Binding	Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor	ChEMBL	520	10	2	7	4.7	CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC	10.1021/jm970101g
	11754273	107750	0	None	21877	2	Human	9.7	pKi	=	9.7	Binding	Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.	ChEMBL	466	7	2	7	4.1	CC(=O)NCc1cc(-c2ncco2)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C	10.1021/jm000105c
	CHEMBL29422	107750	0	None	21877	2	Human	9.7	pKi	=	9.7	Binding	Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.	ChEMBL	466	7	2	7	4.1	CC(=O)NCc1cc(-c2ncco2)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C	10.1021/jm000105c
	11059912	106116	0	None	23988	2	Human	9.7	pKi	=	9.7	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	481	9	1	7	5.6	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2COCC(C)C)c1C	10.1021/jm020289q
	CHEMBL282303	106116	0	None	23988	2	Human	9.7	pKi	=	9.7	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	481	9	1	7	5.6	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2COCC(C)C)c1C	10.1021/jm020289q
	10972867	106479	0	None	19952	2	Human	9.7	pKi	=	9.7	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	480	7	1	7	4.4	CC(=O)N(C)Cc1cc(-c2ncco2)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C	10.1021/jm020289q
	CHEMBL284656	106479	0	None	19952	2	Human	9.7	pKi	=	9.7	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	480	7	1	7	4.4	CC(=O)N(C)Cc1cc(-c2ncco2)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C	10.1021/jm020289q
	11754273	107750	0	None	21877	2	Human	9.7	pKi	=	9.7	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	466	7	2	7	4.1	CC(=O)NCc1cc(-c2ncco2)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C	10.1021/jm020289q
	CHEMBL29422	107750	0	None	21877	2	Human	9.7	pKi	=	9.7	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	466	7	2	7	4.1	CC(=O)NCc1cc(-c2ncco2)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C	10.1021/jm020289q
	131845706	10245	6	None	-11	2	Rat	9.6	pKi	=	9.6	Binding	Compound was evaluated for the binding affinity to Endothelin A receptor in the rat aortaCompound was evaluated for the binding affinity to Endothelin A receptor in the rat aorta	ChEMBL		None	None	None		None	10.1021/jm00087a001
	71308726	10245	6	None	-11	2	Rat	9.6	pKi	=	9.6	Binding	Compound was evaluated for the binding affinity to Endothelin A receptor in the rat aortaCompound was evaluated for the binding affinity to Endothelin A receptor in the rat aorta	ChEMBL		None	None	None		None	10.1021/jm00087a001
	995	10245	6	None	-11	2	Rat	9.6	pKi	=	9.6	Binding	Compound was evaluated for the binding affinity to Endothelin A receptor in the rat aortaCompound was evaluated for the binding affinity to Endothelin A receptor in the rat aorta	ChEMBL		None	None	None		None	10.1021/jm00087a001
	CHEMBL1222310	10245	6	None	-11	2	Rat	9.6	pKi	=	9.6	Binding	Compound was evaluated for the binding affinity to Endothelin A receptor in the rat aortaCompound was evaluated for the binding affinity to Endothelin A receptor in the rat aorta	ChEMBL		None	None	None		None	10.1021/jm00087a001
	CHEMBL4524099	10245	6	None	-11	2	Rat	9.6	pKi	=	9.6	Binding	Compound was evaluated for the binding affinity to Endothelin A receptor in the rat aortaCompound was evaluated for the binding affinity to Endothelin A receptor in the rat aorta	ChEMBL		None	None	None		None	10.1021/jm00087a001
	46228086	206613	0	None	707	2	Mouse	9.6	pKi	=	9.6	Binding	Displacement of [125I]ET1 from endothelin A receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin A receptor in DBA mouse microsomes	ChEMBL	598	10	1	9	4.6	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCBr)c2)cc1	10.1016/j.bmc.2009.08.058
	CHEMBL594265	206613	0	None	707	2	Mouse	9.6	pKi	=	9.6	Binding	Displacement of [125I]ET1 from endothelin A receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin A receptor in DBA mouse microsomes	ChEMBL	598	10	1	9	4.6	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCBr)c2)cc1	10.1016/j.bmc.2009.08.058
	11123603	108573	0	None	14125	2	Human	9.5	pKi	=	9.5	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	475	7	1	8	4.7	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2Cn2ccnc2)c1C	10.1021/jm020289q
	CHEMBL30009	108573	0	None	14125	2	Human	9.5	pKi	=	9.5	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	475	7	1	8	4.7	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2Cn2ccnc2)c1C	10.1021/jm020289q
	11730445	108685	0	None	4677	2	Human	9.5	pKi	=	9.5	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	475	7	1	8	4.7	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2Cn2cccn2)c1C	10.1021/jm020289q
	CHEMBL30092	108685	0	None	4677	2	Human	9.5	pKi	=	9.5	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	475	7	1	8	4.7	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2Cn2cccn2)c1C	10.1021/jm020289q
	46228118	209321	0	None	263	2	Mouse	9.4	pKi	=	9.4	Binding	Displacement of [125I]ET1 from endothelin A receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin A receptor in DBA mouse microsomes	ChEMBL	690	13	1	12	4.7	COc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OCCOc3ccc(S(C)(=O)=O)cc3)cc2)cc(OC)c1OC	10.1016/j.bmc.2009.08.058
	CHEMBL611626	209321	0	None	263	2	Mouse	9.4	pKi	=	9.4	Binding	Displacement of [125I]ET1 from endothelin A receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin A receptor in DBA mouse microsomes	ChEMBL	690	13	1	12	4.7	COc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OCCOc3ccc(S(C)(=O)=O)cc3)cc2)cc(OC)c1OC	10.1016/j.bmc.2009.08.058
	11082049	106336	0	None	933	2	Human	9.4	pKi	=	9.4	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	534	7	1	7	5.6	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN2CCCC(C)(C)C2=O)c1C	10.1021/jm020289q
	CHEMBL283610	106336	0	None	933	2	Human	9.4	pKi	=	9.4	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	534	7	1	7	5.6	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN2CCCC(C)(C)C2=O)c1C	10.1021/jm020289q
	10432263	108929	0	None	85	2	Human	9.4	pKi	=	9.4	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	420	8	1	6	3.4	COc1nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)nc2c1CCC2	10.1021/jm960274q
	CHEMBL302564	108929	0	None	85	2	Human	9.4	pKi	=	9.4	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	420	8	1	6	3.4	COc1nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)nc2c1CCC2	10.1021/jm960274q
	10864118	108245	0	None	4265	2	Human	9.4	pKi	=	9.4	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	508	8	1	7	5.2	CC(=O)N(Cc1cc(-c2ncco2)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C)C(C)C	10.1021/jm020289q
	CHEMBL29775	108245	0	None	4265	2	Human	9.4	pKi	=	9.4	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	508	8	1	7	5.2	CC(=O)N(Cc1cc(-c2ncco2)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C)C(C)C	10.1021/jm020289q
	11477084	10382	53	None	1	2	Human	9.4	pKi	=	9.4	Binding	Binding affinity against human Endothelin A receptorBinding affinity against human Endothelin A receptor	ChEMBL	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	10.1021/jm9700068
	216235	10382	53	None	1	2	Human	9.4	pKi	=	9.4	Binding	Binding affinity against human Endothelin A receptorBinding affinity against human Endothelin A receptor	ChEMBL	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	10.1021/jm9700068
	3548	10382	53	None	1	2	Human	9.4	pKi	=	9.4	Binding	Binding affinity against human Endothelin A receptorBinding affinity against human Endothelin A receptor	ChEMBL	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	10.1021/jm9700068
	3950	10382	53	None	1	2	Human	9.4	pKi	=	9.4	Binding	Binding affinity against human Endothelin A receptorBinding affinity against human Endothelin A receptor	ChEMBL	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	10.1021/jm9700068
	CHEMBL282724	10382	53	None	1	2	Human	9.4	pKi	=	9.4	Binding	Binding affinity against human Endothelin A receptorBinding affinity against human Endothelin A receptor	ChEMBL	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	10.1021/jm9700068
	DB06268	10382	53	None	1	2	Human	9.4	pKi	=	9.4	Binding	Binding affinity against human Endothelin A receptorBinding affinity against human Endothelin A receptor	ChEMBL	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	10.1021/jm9700068
	11477084	10382	53	None	-1	2	Rat	9.4	pKi	=	9.4	Binding	Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor	ChEMBL	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	10.1021/jm030528p
	216235	10382	53	None	-1	2	Rat	9.4	pKi	=	9.4	Binding	Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor	ChEMBL	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	10.1021/jm030528p
	3548	10382	53	None	-1	2	Rat	9.4	pKi	=	9.4	Binding	Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor	ChEMBL	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	10.1021/jm030528p
	3950	10382	53	None	-1	2	Rat	9.4	pKi	=	9.4	Binding	Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor	ChEMBL	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	10.1021/jm030528p
	CHEMBL282724	10382	53	None	-1	2	Rat	9.4	pKi	=	9.4	Binding	Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor	ChEMBL	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	10.1021/jm030528p
	DB06268	10382	53	None	-1	2	Rat	9.4	pKi	=	9.4	Binding	Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor	ChEMBL	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	10.1021/jm030528p
	108002	10267	23	None	56	2	Human	9.4	pKi	=	9.4	Binding	Inhibition of [125I]ET1 binding to cloned human ET-A receptorInhibition of [125I]ET1 binding to cloned human ET-A receptor	ChEMBL	520	10	2	7	4.7	CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC	10.1021/jm00037a003
	3528	10267	23	None	56	2	Human	9.4	pKi	=	9.4	Binding	Inhibition of [125I]ET1 binding to cloned human ET-A receptorInhibition of [125I]ET1 binding to cloned human ET-A receptor	ChEMBL	520	10	2	7	4.7	CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC	10.1021/jm00037a003
	CHEMBL8823	10267	23	None	56	2	Human	9.4	pKi	=	9.4	Binding	Inhibition of [125I]ET1 binding to cloned human ET-A receptorInhibition of [125I]ET1 binding to cloned human ET-A receptor	ChEMBL	520	10	2	7	4.7	CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC	10.1021/jm00037a003
	108002	10267	23	None	56	2	Human	9.4	pKi	=	9.4	Binding	Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells	ChEMBL	520	10	2	7	4.7	CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC	10.1021/jm9505369
	3528	10267	23	None	56	2	Human	9.4	pKi	=	9.4	Binding	Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells	ChEMBL	520	10	2	7	4.7	CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC	10.1021/jm9505369
	CHEMBL8823	10267	23	None	56	2	Human	9.4	pKi	=	9.4	Binding	Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells	ChEMBL	520	10	2	7	4.7	CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC	10.1021/jm9505369
	44339756	117549	0	None	-	1	Human	9.4	pKi	=	9.4	Binding	Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)	ChEMBL	454	6	1	8	4.0	Cc1cc2c(cc1CC(=O)c1ccsc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2	10.1021/jm980217s
	CHEMBL326059	117549	0	None	-	1	Human	9.4	pKi	=	9.4	Binding	Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)	ChEMBL	454	6	1	8	4.0	Cc1cc2c(cc1CC(=O)c1ccsc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2	10.1021/jm980217s
	9849547	190785	0	None	34	2	Human	9.4	pKi	=	9.4	Binding	Tested for in vitro inhibition of [125I]ET1 binding to CHO cells expressing human Endothelin A receptorTested for in vitro inhibition of [125I]ET1 binding to CHO cells expressing human Endothelin A receptor	ChEMBL	520	10	2	7	4.7	CCCOc1ccc2c(c1)[C@H](c1ccc(OC)cc1OCC(=O)O)[C@@H](C(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	CHEMBL48196	190785	0	None	34	2	Human	9.4	pKi	=	9.4	Binding	Tested for in vitro inhibition of [125I]ET1 binding to CHO cells expressing human Endothelin A receptorTested for in vitro inhibition of [125I]ET1 binding to CHO cells expressing human Endothelin A receptor	ChEMBL	520	10	2	7	4.7	CCCOc1ccc2c(c1)[C@H](c1ccc(OC)cc1OCC(=O)O)[C@@H](C(=O)O)[C@@H]2c1ccc2c(c1)OCO2	10.1016/s0960-894x(01)00273-6
	11734435	108079	0	None	6456	2	Human	9.4	pKi	=	9.4	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	562	9	1	7	6.3	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)CC2CCCCC2)c1C	10.1021/jm020289q
	CHEMBL29652	108079	0	None	6456	2	Human	9.4	pKi	=	9.4	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	562	9	1	7	6.3	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)CC2CCCCC2)c1C	10.1021/jm020289q
	9915028	16183	18	None	28183	2	Human	9.3	pKi	=	9.3	Binding	Affinity Biochemical interaction ([125I]-endothelin-1 saturation binding assay) EUB0000348aPTSA EDNRAAffinity Biochemical interaction ([125I]-endothelin-1 saturation binding assay) EUB0000348aPTSA EDNRA	ChEMBL	532	15	1	6	5.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC	10.6019/CHEMBL5210307
	CHEMBL111612	16183	18	None	28183	2	Human	9.3	pKi	=	9.3	Binding	Affinity Biochemical interaction ([125I]-endothelin-1 saturation binding assay) EUB0000348aPTSA EDNRAAffinity Biochemical interaction ([125I]-endothelin-1 saturation binding assay) EUB0000348aPTSA EDNRA	ChEMBL	532	15	1	6	5.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC	10.6019/CHEMBL5210307
	CHEMBL4761843	16183	18	None	28183	2	Human	9.3	pKi	=	9.3	Binding	Affinity Biochemical interaction ([125I]-endothelin-1 saturation binding assay) EUB0000348aPTSA EDNRAAffinity Biochemical interaction ([125I]-endothelin-1 saturation binding assay) EUB0000348aPTSA EDNRA	ChEMBL	532	15	1	6	5.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC	10.6019/CHEMBL5210307
	9915028	16183	18	None	28183	2	Human	9.3	pKi	=	9.3	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	532	15	1	6	5.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC	10.1021/jm010237l
	CHEMBL111612	16183	18	None	28183	2	Human	9.3	pKi	=	9.3	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	532	15	1	6	5.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC	10.1021/jm010237l
	CHEMBL4761843	16183	18	None	28183	2	Human	9.3	pKi	=	9.3	Binding	Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat	ChEMBL	532	15	1	6	5.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC	10.1021/jm010237l
	9915028	16183	18	None	28183	2	Human	9.3	pKi	=	9.3	Binding	Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)	ChEMBL	532	15	1	6	5.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC	10.1021/jm980217s
	CHEMBL111612	16183	18	None	28183	2	Human	9.3	pKi	=	9.3	Binding	Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)	ChEMBL	532	15	1	6	5.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC	10.1021/jm980217s
	CHEMBL4761843	16183	18	None	28183	2	Human	9.3	pKi	=	9.3	Binding	Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)	ChEMBL	532	15	1	6	5.5	CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC	10.1021/jm980217s
	10815239	115335	0	None	125	2	Human	9.3	pKi	=	9.3	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	500	10	1	7	5.0	COc1ccc(OC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1OC	10.1021/jm9910425
	CHEMBL320224	115335	0	None	125	2	Human	9.3	pKi	=	9.3	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	500	10	1	7	5.0	COc1ccc(OC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1OC	10.1021/jm9910425
	11794992	11744	0	None	39810	2	Human	9.3	pKi	=	9.3	Binding	Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.	ChEMBL	395	5	1	6	4.4	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3cocn3)cc2)c1C	10.1021/jm000105c
	CHEMBL104848	11744	0	None	39810	2	Human	9.3	pKi	=	9.3	Binding	Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.	ChEMBL	395	5	1	6	4.4	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3cocn3)cc2)c1C	10.1021/jm000105c
	11812665	106544	0	None	18197	2	Human	9.2	pKi	=	9.2	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	467	8	1	7	5.3	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2COC(C)C)c1C	10.1021/jm020289q
	CHEMBL285118	106544	0	None	18197	2	Human	9.2	pKi	=	9.2	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	467	8	1	7	5.3	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2COC(C)C)c1C	10.1021/jm020289q
	11124545	108150	0	None	4168	2	Human	9.2	pKi	=	9.2	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	557	9	1	8	5.0	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)Cc2ccccn2)c1C	10.1021/jm020289q
	CHEMBL29710	108150	0	None	4168	2	Human	9.2	pKi	=	9.2	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	557	9	1	8	5.0	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)Cc2ccccn2)c1C	10.1021/jm020289q
	10907333	108859	0	None	1819	2	Human	9.2	pKi	=	9.2	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	508	7	2	7	4.9	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CC(=O)NC(C)(C)C)c1C	10.1021/jm020289q
	CHEMBL30215	108859	0	None	1819	2	Human	9.2	pKi	=	9.2	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	508	7	2	7	4.9	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CC(=O)NC(C)(C)C)c1C	10.1021/jm020289q
	10786696	109564	0	None	223	2	Human	9.2	pKi	=	9.2	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	392	8	1	5	3.8	CCc1cc(C)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1	10.1021/jm960274q
	CHEMBL305270	109564	0	None	223	2	Human	9.2	pKi	=	9.2	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	392	8	1	5	3.8	CCc1cc(C)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1	10.1021/jm960274q
	11081276	108000	0	None	2238	2	Human	9.1	pKi	=	9.1	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	476	7	1	8	5.0	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2Cc2ncco2)c1C	10.1021/jm020289q
	CHEMBL29598	108000	0	None	2238	2	Human	9.1	pKi	=	9.1	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	476	7	1	8	5.0	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2Cc2ncco2)c1C	10.1021/jm020289q
	10973218	107746	0	None	3388	2	Human	9.1	pKi	=	9.1	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	506	8	2	7	5.1	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CNCC(F)(F)F)c1C	10.1021/jm020289q
	CHEMBL29420	107746	0	None	3388	2	Human	9.1	pKi	=	9.1	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	506	8	2	7	5.1	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CNCC(F)(F)F)c1C	10.1021/jm020289q
	44311692	109943	0	None	-3	2	Human	9.1	pKi	=	9.1	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	667	13	3	7	4.5	C=CCS(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1	10.1016/s0960-894x(98)00387-4
	CHEMBL308102	109943	0	None	-3	2	Human	9.1	pKi	=	9.1	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	667	13	3	7	4.5	C=CCS(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1	10.1016/s0960-894x(98)00387-4
	9822616	128770	0	None	17782	2	Human	9.1	pKi	=	9.1	Binding	Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.	ChEMBL	406	5	1	6	4.2	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncccn3)cc2)c1C	10.1016/s0960-894x(01)00791-0
	CHEMBL359273	128770	0	None	17782	2	Human	9.1	pKi	=	9.1	Binding	Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.	ChEMBL	406	5	1	6	4.2	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncccn3)cc2)c1C	10.1016/s0960-894x(01)00791-0
	9979632	109678	0	None	41	2	Human	9.1	pKi	=	9.1	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	422	8	1	7	2.8	COc1nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)nc2c1CCO2	10.1021/jm960274q
	CHEMBL305980	109678	0	None	41	2	Human	9.1	pKi	=	9.1	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	422	8	1	7	2.8	COc1nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)nc2c1CCO2	10.1021/jm960274q
	17979744	25026	0	None	-	1	Human	9.0	pKi	=	9	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	657	10	1	8	6.6	CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(CN3CCC(C)(C)C3=O)c1)C(=O)CCCC2	10.1016/s0960-894x(03)00018-0
	CHEMBL12703	25026	0	None	-	1	Human	9.0	pKi	=	9	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	657	10	1	8	6.6	CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(CN3CCC(C)(C)C3=O)c1)C(=O)CCCC2	10.1016/s0960-894x(03)00018-0
	197712	108957	57	None	194	2	Human	9.0	pKi	=	9	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	378	7	1	5	3.5	COC(c1ccccc1)(c1ccccc1)C(Oc1nc(C)cc(C)n1)C(=O)O	10.1021/jm960274q
	CHEMBL302753	108957	57	None	194	2	Human	9.0	pKi	=	9	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	378	7	1	5	3.5	COC(c1ccccc1)(c1ccccc1)C(Oc1nc(C)cc(C)n1)C(=O)O	10.1021/jm960274q
	10763862	169996	0	None	1096	2	Human	9.0	pKi	=	9	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	406	9	1	5	4.0	CCc1cc(CC)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1	10.1021/jm960274q
	CHEMBL418326	169996	0	None	1096	2	Human	9.0	pKi	=	9	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	406	9	1	5	4.0	CCc1cc(CC)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1	10.1021/jm960274q
	11733544	106011	0	None	7244	2	Human	9.0	pKi	=	9	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	480	7	1	7	4.0	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CC(=O)N(C)C)c1C	10.1021/jm020289q
	CHEMBL281668	106011	0	None	7244	2	Human	9.0	pKi	=	9	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	480	7	1	7	4.0	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CC(=O)N(C)C)c1C	10.1021/jm020289q
	11103112	106644	0	None	4570	2	Human	9.0	pKi	=	9	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	501	8	1	7	6.0	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2COc2ccccc2)c1C	10.1021/jm020289q
	CHEMBL28586	106644	0	None	4570	2	Human	9.0	pKi	=	9	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	501	8	1	7	6.0	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2COc2ccccc2)c1C	10.1021/jm020289q
	45257114	206642	0	None	218	2	Mouse	9.0	pKi	=	9.0	Binding	Displacement of [125I]ET1 from endothelin A receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin A receptor in DBA mouse microsomes	ChEMBL	538	10	1	9	4.2	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCF)c2)cc1	10.1016/j.bmc.2009.08.058
	CHEMBL594482	206642	0	None	218	2	Mouse	9.0	pKi	=	9.0	Binding	Displacement of [125I]ET1 from endothelin A receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin A receptor in DBA mouse microsomes	ChEMBL	538	10	1	9	4.2	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCF)c2)cc1	10.1016/j.bmc.2009.08.058
	178103	174730	14	None	100	2	Human	9.0	pKi	=	9.0	Binding	Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor	ChEMBL	506	10	2	7	4.6	CCCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCCO)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2	10.1021/jm970101g
	CHEMBL431651	174730	14	None	100	2	Human	9.0	pKi	=	9.0	Binding	Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor	ChEMBL	506	10	2	7	4.6	CCCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCCO)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2	10.1021/jm970101g
	45257114	206642	0	None	218	2	Mouse	9.0	pKi	=	9.0	Binding	Displacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting	ChEMBL	538	10	1	9	4.2	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCF)c2)cc1	10.1021/jm101110w
	CHEMBL594482	206642	0	None	218	2	Mouse	9.0	pKi	=	9.0	Binding	Displacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting	ChEMBL	538	10	1	9	4.2	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCF)c2)cc1	10.1021/jm101110w
	178103	174730	14	None	100	2	Human	9.0	pKi	=	9.0	Binding	Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)	ChEMBL	506	10	2	7	4.6	CCCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCCO)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2	10.1021/jm980217s
	CHEMBL431651	174730	14	None	100	2	Human	9.0	pKi	=	9.0	Binding	Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)	ChEMBL	506	10	2	7	4.6	CCCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCCO)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2	10.1021/jm980217s
	46228117	206563	0	None	1	2	Mouse	8.9	pKi	=	8.9	Binding	Displacement of [125I]ET1 from endothelin A receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin A receptor in DBA mouse microsomes	ChEMBL	690	13	1	12	4.7	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOc3ccc(S(C)(=O)=O)cc3)c2)cc1	10.1016/j.bmc.2009.08.058
	CHEMBL593928	206563	0	None	1	2	Mouse	8.9	pKi	=	8.9	Binding	Displacement of [125I]ET1 from endothelin A receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin A receptor in DBA mouse microsomes	ChEMBL	690	13	1	12	4.7	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOc3ccc(S(C)(=O)=O)cc3)c2)cc1	10.1016/j.bmc.2009.08.058
	10840560	11439	0	None	2	2	Human	8.9	pKi	=	8.9	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	558	13	1	8	5.2	COc1cc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc(OC)c1OC	10.1021/jm9910425
	CHEMBL103201	11439	0	None	2	2	Human	8.9	pKi	=	8.9	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	558	13	1	8	5.2	COc1cc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc(OC)c1OC	10.1021/jm9910425
	13016	7457	13	None	1	4	Human	8.9	pKi	=	8.9	Binding	Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.	ChEMBL	395	5	1	6	4.4	CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4	10.1016/s0960-894x(01)00791-0
	9843631	7457	13	None	1	4	Human	8.9	pKi	=	8.9	Binding	Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.	ChEMBL	395	5	1	6	4.4	CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4	10.1016/s0960-894x(01)00791-0
	CHEMBL24461	7457	13	None	1	4	Human	8.9	pKi	=	8.9	Binding	Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.	ChEMBL	395	5	1	6	4.4	CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4	10.1016/s0960-894x(01)00791-0
	13016	7457	13	None	1	4	Human	8.9	pKi	=	8.9	Binding	Binding affinity to ETA receptorBinding affinity to ETA receptor	ChEMBL	395	5	1	6	4.4	CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4	10.1021/jm300682j
	9843631	7457	13	None	1	4	Human	8.9	pKi	=	8.9	Binding	Binding affinity to ETA receptorBinding affinity to ETA receptor	ChEMBL	395	5	1	6	4.4	CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4	10.1021/jm300682j
	CHEMBL24461	7457	13	None	1	4	Human	8.9	pKi	=	8.9	Binding	Binding affinity to ETA receptorBinding affinity to ETA receptor	ChEMBL	395	5	1	6	4.4	CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4	10.1021/jm300682j
	13016	7457	13	None	-1	4	Rat	8.9	pKi	=	8.9	Binding	Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor	ChEMBL	395	5	1	6	4.4	CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4	10.1021/jm030528p
	9843631	7457	13	None	-1	4	Rat	8.9	pKi	=	8.9	Binding	Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor	ChEMBL	395	5	1	6	4.4	CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4	10.1021/jm030528p
	CHEMBL24461	7457	13	None	-1	4	Rat	8.9	pKi	=	8.9	Binding	Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor	ChEMBL	395	5	1	6	4.4	CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4	10.1021/jm030528p
	13016	7457	13	None	1	4	Human	8.9	pKi	=	8.9	Binding	Compound was evaluated for its binding affinity towards human Endothelin A receptorCompound was evaluated for its binding affinity towards human Endothelin A receptor	ChEMBL	395	5	1	6	4.4	CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4	10.1021/jm020138n
	9843631	7457	13	None	1	4	Human	8.9	pKi	=	8.9	Binding	Compound was evaluated for its binding affinity towards human Endothelin A receptorCompound was evaluated for its binding affinity towards human Endothelin A receptor	ChEMBL	395	5	1	6	4.4	CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4	10.1021/jm020138n
	CHEMBL24461	7457	13	None	1	4	Human	8.9	pKi	=	8.9	Binding	Compound was evaluated for its binding affinity towards human Endothelin A receptorCompound was evaluated for its binding affinity towards human Endothelin A receptor	ChEMBL	395	5	1	6	4.4	CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4	10.1021/jm020138n
	13016	7457	13	None	-1	4	Rat	8.9	pKi	=	8.9	Binding	Displacement of [125I]-ET1 from ETA receptor in A10 rat thoracic aorta smooth muscle after 3 hrs by scintillation counting methodDisplacement of [125I]-ET1 from ETA receptor in A10 rat thoracic aorta smooth muscle after 3 hrs by scintillation counting method	ChEMBL	395	5	1	6	4.4	CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4	10.1016/j.bmcl.2016.06.014
	9843631	7457	13	None	-1	4	Rat	8.9	pKi	=	8.9	Binding	Displacement of [125I]-ET1 from ETA receptor in A10 rat thoracic aorta smooth muscle after 3 hrs by scintillation counting methodDisplacement of [125I]-ET1 from ETA receptor in A10 rat thoracic aorta smooth muscle after 3 hrs by scintillation counting method	ChEMBL	395	5	1	6	4.4	CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4	10.1016/j.bmcl.2016.06.014
	CHEMBL24461	7457	13	None	-1	4	Rat	8.9	pKi	=	8.9	Binding	Displacement of [125I]-ET1 from ETA receptor in A10 rat thoracic aorta smooth muscle after 3 hrs by scintillation counting methodDisplacement of [125I]-ET1 from ETA receptor in A10 rat thoracic aorta smooth muscle after 3 hrs by scintillation counting method	ChEMBL	395	5	1	6	4.4	CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4	10.1016/j.bmcl.2016.06.014
	51003306	64837	0	None	295	2	Mouse	8.9	pKi	=	8.9	Binding	Displacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting	ChEMBL	670	19	1	12	4.2	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOCCOCCOCCF)c2)cc1	10.1021/jm101110w
	CHEMBL1672880	64837	0	None	295	2	Mouse	8.9	pKi	=	8.9	Binding	Displacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting	ChEMBL	670	19	1	12	4.2	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOCCOCCOCCF)c2)cc1	10.1021/jm101110w
	13016	7457	13	None	1	4	Human	8.9	pKi	=	8.9	Binding	Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.	ChEMBL	395	5	1	6	4.4	CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4	10.1021/jm000105c
	9843631	7457	13	None	1	4	Human	8.9	pKi	=	8.9	Binding	Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.	ChEMBL	395	5	1	6	4.4	CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4	10.1021/jm000105c
	CHEMBL24461	7457	13	None	1	4	Human	8.9	pKi	=	8.9	Binding	Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.	ChEMBL	395	5	1	6	4.4	CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4	10.1021/jm000105c
	13016	7457	13	None	1	4	Human	8.9	pKi	=	8.9	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	395	5	1	6	4.4	CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4	10.1021/jm020289q
	9843631	7457	13	None	1	4	Human	8.9	pKi	=	8.9	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	395	5	1	6	4.4	CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4	10.1021/jm020289q
	CHEMBL24461	7457	13	None	1	4	Human	8.9	pKi	=	8.9	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	395	5	1	6	4.4	CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4	10.1021/jm020289q
	13016	7457	13	None	1	4	Human	8.9	pKi	=	8.9	Binding	Inhibitory concentration against Endothelin A receptorInhibitory concentration against Endothelin A receptor	ChEMBL	395	5	1	6	4.4	CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4	10.1021/jm030480f
	9843631	7457	13	None	1	4	Human	8.9	pKi	=	8.9	Binding	Inhibitory concentration against Endothelin A receptorInhibitory concentration against Endothelin A receptor	ChEMBL	395	5	1	6	4.4	CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4	10.1021/jm030480f
	CHEMBL24461	7457	13	None	1	4	Human	8.9	pKi	=	8.9	Binding	Inhibitory concentration against Endothelin A receptorInhibitory concentration against Endothelin A receptor	ChEMBL	395	5	1	6	4.4	CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4	10.1021/jm030480f
	9938533	112190	4	None	-1	2	Human	8.8	pKi	=	8.8	Binding	Compound was tested for the binding affinity against Endothelin A receptorCompound was tested for the binding affinity against Endothelin A receptor	ChEMBL	596	13	2	7	4.0	CCCCS(=O)(=O)NC(=O)[C@@H](NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)C	10.1016/s0960-894x(98)00388-6
	CHEMBL311854	112190	4	None	-1	2	Human	8.8	pKi	=	8.8	Binding	Compound was tested for the binding affinity against Endothelin A receptorCompound was tested for the binding affinity against Endothelin A receptor	ChEMBL	596	13	2	7	4.0	CCCCS(=O)(=O)NC(=O)[C@@H](NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)C	10.1016/s0960-894x(98)00388-6
	10553793	11233	0	None	75	2	Human	8.8	pKi	=	8.8	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	512	11	2	6	4.8	Cc1cc(C)nc(OC(C(=O)O)C(OCCc2ccc(C(=O)O)cc2)(c2ccccc2)c2ccccc2)n1	10.1021/jm9910425
	CHEMBL101742	11233	0	None	75	2	Human	8.8	pKi	=	8.8	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	512	11	2	6	4.8	Cc1cc(C)nc(OC(C(=O)O)C(OCCc2ccc(C(=O)O)cc2)(c2ccccc2)c2ccccc2)n1	10.1021/jm9910425
	11113812	107573	0	None	1258	2	Human	8.8	pKi	=	8.8	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	497	7	1	6	6.6	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2/C=C\c2ccccc2)c1C	10.1021/jm020289q
	CHEMBL29313	107573	0	None	1258	2	Human	8.8	pKi	=	8.8	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	497	7	1	6	6.6	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2/C=C\c2ccccc2)c1C	10.1021/jm020289q
	CHEMBL1790180	215662	0	None	-72	3	Rat	8.8	pKi	=	8.8	Binding	Compound was evaluated for the binding affinity to Endothelin A receptor in the rat atriumCompound was evaluated for the binding affinity to Endothelin A receptor in the rat atrium	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CCc3ccc(O)cc3)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H](Cc3ccccc3)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00087a001
	9938533	112190	4	None	-1	2	Human	8.7	pKi	=	8.7	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	596	13	2	7	4.0	CCCCS(=O)(=O)NC(=O)[C@@H](NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)C	10.1016/s0960-894x(98)00387-4
	CHEMBL311854	112190	4	None	-1	2	Human	8.7	pKi	=	8.7	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	596	13	2	7	4.0	CCCCS(=O)(=O)NC(=O)[C@@H](NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)C	10.1016/s0960-894x(98)00387-4
	9895957	17445	18	None	3	3	Human	8.7	pKi	=	8.7	Binding	Binding affinity at endothelin receptor subtype ABinding affinity at endothelin receptor subtype A	ChEMBL	659	11	1	7	6.8	CCCCC1=NC2(CCCC2)C(=O)N1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(CN2CCC(C)(C)C2=O)c1	10.1016/j.bmc.2012.06.011
	CHEMBL11706	17445	18	None	3	3	Human	8.7	pKi	=	8.7	Binding	Binding affinity at endothelin receptor subtype ABinding affinity at endothelin receptor subtype A	ChEMBL	659	11	1	7	6.8	CCCCC1=NC2(CCCC2)C(=O)N1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(CN2CCC(C)(C)C2=O)c1	10.1016/j.bmc.2012.06.011
	44311728	111130	0	None	-13	2	Human	8.7	pKi	=	8.7	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	653	12	3	7	4.4	C=CS(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1	10.1016/s0960-894x(98)00387-4
	CHEMBL310039	111130	0	None	-13	2	Human	8.7	pKi	=	8.7	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	653	12	3	7	4.4	C=CS(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1	10.1016/s0960-894x(98)00387-4
	9895957	17445	18	None	3	3	Human	8.7	pKi	=	8.7	Binding	Compound was evaluated for its binding affinity towards human Endothelin A receptorCompound was evaluated for its binding affinity towards human Endothelin A receptor	ChEMBL	659	11	1	7	6.8	CCCCC1=NC2(CCCC2)C(=O)N1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(CN2CCC(C)(C)C2=O)c1	10.1021/jm020138n
	CHEMBL11706	17445	18	None	3	3	Human	8.7	pKi	=	8.7	Binding	Compound was evaluated for its binding affinity towards human Endothelin A receptorCompound was evaluated for its binding affinity towards human Endothelin A receptor	ChEMBL	659	11	1	7	6.8	CCCCC1=NC2(CCCC2)C(=O)N1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(CN2CCC(C)(C)C2=O)c1	10.1021/jm020138n
	9895957	17445	18	None	3	3	Human	8.7	pKi	=	8.7	Binding	Inhibitory concentration against endothelin receptor type AInhibitory concentration against endothelin receptor type A	ChEMBL	659	11	1	7	6.8	CCCCC1=NC2(CCCC2)C(=O)N1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(CN2CCC(C)(C)C2=O)c1	10.1021/jm058225d
	CHEMBL11706	17445	18	None	3	3	Human	8.7	pKi	=	8.7	Binding	Inhibitory concentration against endothelin receptor type AInhibitory concentration against endothelin receptor type A	ChEMBL	659	11	1	7	6.8	CCCCC1=NC2(CCCC2)C(=O)N1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(CN2CCC(C)(C)C2=O)c1	10.1021/jm058225d
	10555112	11509	0	None	12	2	Human	8.7	pKi	=	8.7	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	572	14	2	8	4.6	COc1cc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)ccc1OCC(=O)O	10.1021/jm9910425
	CHEMBL103695	11509	0	None	12	2	Human	8.7	pKi	=	8.7	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	572	14	2	8	4.6	COc1cc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)ccc1OCC(=O)O	10.1021/jm9910425
	11799974	11303	0	None	12	2	Human	8.7	pKi	=	8.7	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	514	12	1	7	4.8	COc1ccc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(OC)n2)C(=O)O)cc1	10.1021/jm9910425
	CHEMBL102307	11303	0	None	12	2	Human	8.7	pKi	=	8.7	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	514	12	1	7	4.8	COc1ccc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(OC)n2)C(=O)O)cc1	10.1021/jm9910425
	44311805	211345	0	None	-26	2	Human	8.0	pKi	=	8	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	669	12	3	7	4.7	Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccno3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NS(=O)(=O)C(C)C)c1	10.1016/s0960-894x(98)00387-4
	CHEMBL73000	211345	0	None	-26	2	Human	8.0	pKi	=	8	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	669	12	3	7	4.7	Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccno3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NS(=O)(=O)C(C)C)c1	10.1016/s0960-894x(98)00387-4
	13015	8312	30	None	-	1	Human	8.0	pKi	=	8	Binding	Inhibitory concentration against endothelin receptor type AInhibitory concentration against endothelin receptor type A	ChEMBL	536	8	1	7	5.8	CC1=C(ON=C1NS(=O)(=O)C2=CC=CC=C2C3=C(C=C(C=C3)C4=NC=CO4)CN(C)C(=O)CC(C)(C)C)C	10.1021/jm058225d
	156690	8312	30	None	-	1	Human	8.0	pKi	=	8	Binding	Inhibitory concentration against endothelin receptor type AInhibitory concentration against endothelin receptor type A	ChEMBL	536	8	1	7	5.8	CC1=C(ON=C1NS(=O)(=O)C2=CC=CC=C2C3=C(C=C(C=C3)C4=NC=CO4)CN(C)C(=O)CC(C)(C)C)C	10.1021/jm058225d
	CHEMBL383581	8312	30	None	-	1	Human	8.0	pKi	=	8	Binding	Inhibitory concentration against endothelin receptor type AInhibitory concentration against endothelin receptor type A	ChEMBL	536	8	1	7	5.8	CC1=C(ON=C1NS(=O)(=O)C2=CC=CC=C2C3=C(C=C(C=C3)C4=NC=CO4)CN(C)C(=O)CC(C)(C)C)C	10.1021/jm058225d
	10812403	45874	0	None	120	2	Rat	7.0	pKi	=	7	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	427	7	2	5	4.1	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2C(N)=O)c1C	10.1021/jm970872k
	CHEMBL146904	45874	0	None	120	2	Rat	7.0	pKi	=	7	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	427	7	2	5	4.1	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2C(N)=O)c1C	10.1021/jm970872k
	10573784	172116	0	None	95	2	Rat	7.0	pKi	=	7	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	413	7	2	5	4.4	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2CN)c1C	10.1021/jm970872k
	CHEMBL423583	172116	0	None	95	2	Rat	7.0	pKi	=	7	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	413	7	2	5	4.4	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2CN)c1C	10.1021/jm970872k
	1481	8847	116	None	-112	3	Human	5.0	pKi	=	5	Binding	Binding affinity to ETA receptorBinding affinity to ETA receptor	ChEMBL	428	7	1	5	4.8	CCCCC1=NC2(C(=O)N1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)CCCC2	10.1021/jm300682j
	3749	8847	116	None	-112	3	Human	5.0	pKi	=	5	Binding	Binding affinity to ETA receptorBinding affinity to ETA receptor	ChEMBL	428	7	1	5	4.8	CCCCC1=NC2(C(=O)N1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)CCCC2	10.1021/jm300682j
	589	8847	116	None	-112	3	Human	5.0	pKi	=	5	Binding	Binding affinity to ETA receptorBinding affinity to ETA receptor	ChEMBL	428	7	1	5	4.8	CCCCC1=NC2(C(=O)N1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)CCCC2	10.1021/jm300682j
	6908	8847	116	None	-112	3	Human	5.0	pKi	=	5	Binding	Binding affinity to ETA receptorBinding affinity to ETA receptor	ChEMBL	428	7	1	5	4.8	CCCCC1=NC2(C(=O)N1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)CCCC2	10.1021/jm300682j
	CHEMBL1513	8847	116	None	-112	3	Human	5.0	pKi	=	5	Binding	Binding affinity to ETA receptorBinding affinity to ETA receptor	ChEMBL	428	7	1	5	4.8	CCCCC1=NC2(C(=O)N1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)CCCC2	10.1021/jm300682j
	DB01029	8847	116	None	-112	3	Human	5.0	pKi	=	5	Binding	Binding affinity to ETA receptorBinding affinity to ETA receptor	ChEMBL	428	7	1	5	4.8	CCCCC1=NC2(C(=O)N1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)CCCC2	10.1021/jm300682j
	10619232	128773	0	None	-	1	Rat	7.0	pKi	=	7.0	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	371	5	1	5	3.8	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2N(C)C)c1C	10.1021/jm970872k
	CHEMBL359332	128773	0	None	-	1	Rat	7.0	pKi	=	7.0	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	371	5	1	5	3.8	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2N(C)C)c1C	10.1021/jm970872k
	44267891	25531	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	532	8	1	7	5.9	CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)cc1)C(=O)CCCC2	10.1016/s0960-894x(03)00018-0
	CHEMBL12779	25531	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	532	8	1	7	5.9	CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)cc1)C(=O)CCCC2	10.1016/s0960-894x(03)00018-0
	44333366	114203	0	None	-1	2	Human	7.0	pKi	=	7.0	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	570	12	1	8	5.2	COc1ccc(CCOC(c2ccc(C)cc2)(c2ccc(C)cc2)C(Oc2nc3c(c(OC)n2)COC3)C(=O)O)cc1	10.1021/jm9910425
	CHEMBL318146	114203	0	None	-1	2	Human	7.0	pKi	=	7.0	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	570	12	1	8	5.2	COc1ccc(CCOC(c2ccc(C)cc2)(c2ccc(C)cc2)C(Oc2nc3c(c(OC)n2)COC3)C(=O)O)cc1	10.1021/jm9910425
	10742005	210476	0	None	162	2	Human	8.0	pKi	=	8.0	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	446	9	1	7	3.2	COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2cccc(F)c2)c2cccc(F)c2)n1	10.1021/jm960274q
	CHEMBL67536	210476	0	None	162	2	Human	8.0	pKi	=	8.0	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	446	9	1	7	3.2	COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2cccc(F)c2)c2cccc(F)c2)n1	10.1021/jm960274q
	10740258	116455	0	None	1096	2	Human	8.0	pKi	=	8.0	Binding	Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.	ChEMBL	409	5	1	6	4.7	Cc1cnc(-c2ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)cc2)o1	10.1021/jm000105c
	CHEMBL322674	116455	0	None	1096	2	Human	8.0	pKi	=	8.0	Binding	Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.	ChEMBL	409	5	1	6	4.7	Cc1cnc(-c2ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)cc2)o1	10.1021/jm000105c
	10321341	152214	0	None	93	2	Human	8.0	pKi	=	8.0	Binding	Inhibition of [125I]ET1 binding to cloned human ET-A receptorInhibition of [125I]ET1 binding to cloned human ET-A receptor	ChEMBL	446	7	1	5	5.2	CCCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2	10.1021/jm00037a003
	CHEMBL39142	152214	0	None	93	2	Human	8.0	pKi	=	8.0	Binding	Inhibition of [125I]ET1 binding to cloned human ET-A receptorInhibition of [125I]ET1 binding to cloned human ET-A receptor	ChEMBL	446	7	1	5	5.2	CCCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2	10.1021/jm00037a003
	10598958	48208	0	None	-	1	Rat	7.0	pKi	=	7.0	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	434	6	1	6	3.9	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(S(=O)(=O)C(C)C)cc2)c1C	10.1021/jm970872k
	CHEMBL149050	48208	0	None	-	1	Rat	7.0	pKi	=	7.0	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	434	6	1	6	3.9	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(S(=O)(=O)C(C)C)cc2)c1C	10.1021/jm970872k
	10715881	128319	0	None	37	2	Rat	7.0	pKi	=	7.0	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	398	5	1	4	5.3	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)(C)C)cc2)c1C	10.1021/jm970872k
	CHEMBL358545	128319	0	None	37	2	Rat	7.0	pKi	=	7.0	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	398	5	1	4	5.3	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)(C)C)cc2)c1C	10.1021/jm970872k
	9848710	175859	4	None	-301	4	Pig	5.0	pKi	=	5.0	Binding	Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated	ChEMBL	497	9	3	3	4.3	Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1	10.1016/0960-894X(96)00421-0
	CHEMBL439759	175859	4	None	-301	4	Pig	5.0	pKi	=	5.0	Binding	Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated	ChEMBL	497	9	3	3	4.3	Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1	10.1016/0960-894X(96)00421-0
	9848710	175859	4	None	-301	4	Human	5.0	pKi	=	5.0	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	497	9	3	3	4.3	Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1	10.1016/s0960-894x(98)00387-4
	CHEMBL439759	175859	4	None	-301	4	Human	5.0	pKi	=	5.0	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	497	9	3	3	4.3	Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1	10.1016/s0960-894x(98)00387-4
	10761748	127804	0	None	-	1	Rat	7.0	pKi	=	7.0	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	371	5	1	5	3.8	Cc1noc(NS(=O)(=O)c2ccccc2-c2cccc(N(C)C)c2)c1C	10.1021/jm970872k
	CHEMBL356591	127804	0	None	-	1	Rat	7.0	pKi	=	7.0	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	371	5	1	5	3.8	Cc1noc(NS(=O)(=O)c2ccccc2-c2cccc(N(C)C)c2)c1C	10.1021/jm970872k
	44286764	152599	0	None	-	1	Human	5.0	pKi	=	5.0	Binding	Inhibition of [125I]ET1 binding to cloned human ET-A receptorInhibition of [125I]ET1 binding to cloned human ET-A receptor	ChEMBL	314	3	1	1	4.7	O=C(O)[C@@H]1[C@@H](c2ccccc2)c2ccccc2[C@H]1c1ccccc1	10.1021/jm00037a003
	CHEMBL39171	152599	0	None	-	1	Human	5.0	pKi	=	5.0	Binding	Inhibition of [125I]ET1 binding to cloned human ET-A receptorInhibition of [125I]ET1 binding to cloned human ET-A receptor	ChEMBL	314	3	1	1	4.7	O=C(O)[C@@H]1[C@@H](c2ccccc2)c2ccccc2[C@H]1c1ccccc1	10.1021/jm00037a003
	10503999	48088	0	None	6	2	Rat	5.9	pKi	=	5.9	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	456	8	3	6	3.9	Cc1noc(NS(=O)(=O)c2ccc(NC(=O)CN)cc2-c2ccc(CC(C)C)cc2)c1C	10.1021/jm970872k
	CHEMBL148953	48088	0	None	6	2	Rat	5.9	pKi	=	5.9	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	456	8	3	6	3.9	Cc1noc(NS(=O)(=O)c2ccc(NC(=O)CN)cc2-c2ccc(CC(C)C)cc2)c1C	10.1021/jm970872k
	10762600	175081	0	None	154	2	Rat	7.9	pKi	=	7.9	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	384	6	1	4	5.0	Cc1onc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2)c1C	10.1021/jm970872k
	CHEMBL434082	175081	0	None	154	2	Rat	7.9	pKi	=	7.9	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	384	6	1	4	5.0	Cc1onc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2)c1C	10.1021/jm970872k
	10209324	21262	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	546	8	1	7	6.2	CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(C)c1)C(=O)CCCC2	10.1016/s0960-894x(03)00018-0
	CHEMBL12013	21262	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	546	8	1	7	6.2	CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(C)c1)C(=O)CCCC2	10.1016/s0960-894x(03)00018-0
	44311851	211442	0	None	-162	2	Human	6.9	pKi	=	6.9	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	564	10	3	5	4.9	Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccon3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1	10.1016/s0960-894x(98)00387-4
	CHEMBL73697	211442	0	None	-162	2	Human	6.9	pKi	=	6.9	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	564	10	3	5	4.9	Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccon3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1	10.1016/s0960-894x(98)00387-4
	10692125	209842	0	None	26	2	Human	6.9	pKi	=	6.9	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	396	8	2	7	2.3	COc1cc(OC)nc(OC(C(=O)O)C(O)(c2ccccc2)c2ccccc2)n1	10.1021/jm960274q
	CHEMBL63648	209842	0	None	26	2	Human	6.9	pKi	=	6.9	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	396	8	2	7	2.3	COc1cc(OC)nc(OC(C(=O)O)C(O)(c2ccccc2)c2ccccc2)n1	10.1021/jm960274q
	44314607	168040	0	None	-1412	2	Pig	5.9	pKi	=	5.9	Binding	Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated	ChEMBL	1534	46	19	18	-0.2	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(96)00421-0
	77282208	168040	0	None	-1412	2	Pig	5.9	pKi	=	5.9	Binding	Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated	ChEMBL	1534	46	19	18	-0.2	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(96)00421-0
	CHEMBL412003	168040	0	None	-1412	2	Pig	5.9	pKi	=	5.9	Binding	Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated	ChEMBL	1534	46	19	18	-0.2	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(96)00421-0
	10620897	48390	0	None	14	2	Rat	5.9	pKi	=	5.9	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	398	6	1	4	5.3	Cc1cccc(-c2ccc(CC(C)C)cc2)c1S(=O)(=O)Nc1onc(C)c1C	10.1021/jm970872k
	CHEMBL149171	48390	0	None	14	2	Rat	5.9	pKi	=	5.9	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	398	6	1	4	5.3	Cc1cccc(-c2ccc(CC(C)C)cc2)c1S(=O)(=O)Nc1onc(C)c1C	10.1021/jm970872k
	CHEMBL4513786	220746	7	None	-2344	8	Human	4.9	pKi	=	4.9	Binding	Affinity Biochemical interaction ([125I]-endothelin-1 saturation binding assay) EUB0000289bCl EDNRAAffinity Biochemical interaction ([125I]-endothelin-1 saturation binding assay) EUB0000289bCl EDNRA	ChEMBL		None	None	None		CCCCN(CCCC)C(=O)CN1C[C@@H](c2cc(OC)c3c(c2)OCO3)[C@H](C(=O)O)[C@H]1CC(C)(C)CCC	10.6019/CHEMBL5210307
	CHEMBL4796803	220746	7	None	-2344	8	Human	4.9	pKi	=	4.9	Binding	Affinity Biochemical interaction ([125I]-endothelin-1 saturation binding assay) EUB0000289bCl EDNRAAffinity Biochemical interaction ([125I]-endothelin-1 saturation binding assay) EUB0000289bCl EDNRA	ChEMBL		None	None	None		CCCCN(CCCC)C(=O)CN1C[C@@H](c2cc(OC)c3c(c2)OCO3)[C@H](C(=O)O)[C@H]1CC(C)(C)CCC	10.6019/CHEMBL5210307
	5344	180252	101	None	-	1	Human	4.9	pKi	=	4.9	Binding	DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)	ChEMBL	267	3	2	5	1.7	Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C	nan
	CHEMBL453	180252	101	None	-	1	Human	4.9	pKi	=	4.9	Binding	DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)	ChEMBL	267	3	2	5	1.7	Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C	nan
	10740469	46079	0	None	154	2	Rat	7.9	pKi	=	7.9	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	413	7	2	5	5.0	CNc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C	10.1021/jm970872k
	CHEMBL147081	46079	0	None	154	2	Rat	7.9	pKi	=	7.9	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	413	7	2	5	5.0	CNc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C	10.1021/jm970872k
	10668636	128750	0	None	147	2	Rat	7.9	pKi	=	7.9	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	399	6	2	5	4.5	Cc1noc(NS(=O)(=O)c2ccc(N)cc2-c2ccc(CC(C)C)cc2)c1C	10.1021/jm970872k
	CHEMBL359167	128750	0	None	147	2	Rat	7.9	pKi	=	7.9	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	399	6	2	5	4.5	Cc1noc(NS(=O)(=O)c2ccc(N)cc2-c2ccc(CC(C)C)cc2)c1C	10.1021/jm970872k
	10166561	16836	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	562	9	2	8	5.4	CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(CO)c1)C(=O)CCCC2	10.1016/s0960-894x(03)00018-0
	CHEMBL11528	16836	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	562	9	2	8	5.4	CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(CO)c1)C(=O)CCCC2	10.1016/s0960-894x(03)00018-0
	10809354	127913	1	None	-	1	Rat	6.9	pKi	=	6.9	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	373	5	1	6	3.7	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2[N+](=O)[O-])c1C	10.1021/jm970872k
	CHEMBL357580	127913	1	None	-	1	Rat	6.9	pKi	=	6.9	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	373	5	1	6	3.7	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2[N+](=O)[O-])c1C	10.1021/jm970872k
	19934544	212979	0	None	-2	2	Human	4.9	pKi	=	4.9	Binding	Affinity against ET A receptorAffinity against ET A receptor	ChEMBL	482	7	3	4	4.9	CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(NC(=O)Cc3c[nH]c4ccccc34)ccc21	10.1016/0960-894X(95)00019-P
	CHEMBL86489	212979	0	None	-2	2	Human	4.9	pKi	=	4.9	Binding	Affinity against ET A receptorAffinity against ET A receptor	ChEMBL	482	7	3	4	4.9	CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(NC(=O)Cc3c[nH]c4ccccc34)ccc21	10.1016/0960-894X(95)00019-P
	44267862	22134	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	571	9	1	8	5.9	CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(CC#N)c1)C(=O)CCCC2	10.1016/s0960-894x(03)00018-0
	CHEMBL12144	22134	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	571	9	1	8	5.9	CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(CC#N)c1)C(=O)CCCC2	10.1016/s0960-894x(03)00018-0
	10453858	166881	0	None	31	2	Human	7.8	pKi	=	7.8	Binding	Inhibition of [125I]ET1 binding to cloned human ET-A receptorInhibition of [125I]ET1 binding to cloned human ET-A receptor	ChEMBL	404	4	2	5	4.1	COc1ccc([C@@H]2c3cc(O)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1	10.1021/jm00037a003
	CHEMBL41087	166881	0	None	31	2	Human	7.8	pKi	=	7.8	Binding	Inhibition of [125I]ET1 binding to cloned human ET-A receptorInhibition of [125I]ET1 binding to cloned human ET-A receptor	ChEMBL	404	4	2	5	4.1	COc1ccc([C@@H]2c3cc(O)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1	10.1021/jm00037a003
	10837085	109086	0	None	39	2	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	446	9	1	7	3.2	COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccccc2F)c2ccccc2F)n1	10.1021/jm960274q
	CHEMBL303501	109086	0	None	39	2	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	446	9	1	7	3.2	COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccccc2F)c2ccccc2F)n1	10.1021/jm960274q
	10670204	48308	0	None	17	2	Rat	5.8	pKi	=	5.8	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	428	7	2	5	4.7	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2C(=O)O)c1C	10.1021/jm970872k
	CHEMBL149111	48308	0	None	17	2	Rat	5.8	pKi	=	5.8	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	428	7	2	5	4.7	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2C(=O)O)c1C	10.1021/jm970872k
	10603135	116521	0	None	1	2	Human	6.8	pKi	=	6.8	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	570	14	1	7	6.0	CCc1ccc(C(OCCc2ccc(OC)cc2)(c2ccc(CC)cc2)C(Oc2nc(C)cc(OC)n2)C(=O)O)cc1	10.1021/jm9910425
	CHEMBL322996	116521	0	None	1	2	Human	6.8	pKi	=	6.8	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	570	14	1	7	6.0	CCc1ccc(C(OCCc2ccc(OC)cc2)(c2ccc(CC)cc2)C(Oc2nc(C)cc(OC)n2)C(=O)O)cc1	10.1021/jm9910425
	10521320	126543	0	None	-	1	Rat	7.8	pKi	=	7.8	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	343	4	2	5	3.3	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2N)c1C	10.1021/jm970872k
	CHEMBL347958	126543	0	None	-	1	Rat	7.8	pKi	=	7.8	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	343	4	2	5	3.3	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2N)c1C	10.1021/jm970872k
	10549727	171666	0	None	125	2	Rat	7.8	pKi	=	7.8	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	414	7	1	5	5.0	COc1cccc(S(=O)(=O)Nc2onc(C)c2C)c1-c1ccc(CC(C)C)cc1	10.1021/jm970872k
	CHEMBL422128	171666	0	None	125	2	Rat	7.8	pKi	=	7.8	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	414	7	1	5	5.0	COc1cccc(S(=O)(=O)Nc2onc(C)c2C)c1-c1ccc(CC(C)C)cc1	10.1021/jm970872k
	44267893	105193	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	535	10	2	7	4.9	CCCc1nc(CC)c(C(=O)NC)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1016/s0960-894x(03)00018-0
	CHEMBL275523	105193	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	535	10	2	7	4.9	CCCc1nc(CC)c(C(=O)NC)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1016/s0960-894x(03)00018-0
	10740953	12088	0	None	758	2	Human	7.8	pKi	=	7.8	Binding	Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.	ChEMBL	423	5	1	6	5.0	Cc1nc(-c2ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)cc2)oc1C	10.1021/jm000105c
	CHEMBL106749	12088	0	None	758	2	Human	7.8	pKi	=	7.8	Binding	Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.	ChEMBL	423	5	1	6	5.0	Cc1nc(-c2ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)cc2)oc1C	10.1021/jm000105c
	44274885	100861	0	None	29	2	Human	6.8	pKi	=	6.8	Binding	Binding affinity against human Endothelin A receptorBinding affinity against human Endothelin A receptor	ChEMBL	454	10	1	7	4.5	COc1cc(OC)nc(CC(C(=O)O)C(C)(Oc2ccc(SC)cc2)c2ccccc2)n1	10.1021/jm030480f
	CHEMBL24906	100861	0	None	29	2	Human	6.8	pKi	=	6.8	Binding	Binding affinity against human Endothelin A receptorBinding affinity against human Endothelin A receptor	ChEMBL	454	10	1	7	4.5	COc1cc(OC)nc(CC(C(=O)O)C(C)(Oc2ccc(SC)cc2)c2ccccc2)n1	10.1021/jm030480f
	44307287	210537	0	None	29	2	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	470	10	0	9	4.1	COC(=O)C(Oc1nc(OC)cc(OC)n1)C(C)(Oc1ccc(SC)cc1)c1ccccc1	10.1021/jm960274q
	CHEMBL67957	210537	0	None	29	2	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	470	10	0	9	4.1	COC(=O)C(Oc1nc(OC)cc(OC)n1)C(C)(Oc1ccc(SC)cc1)c1ccccc1	10.1021/jm960274q
	176	7186	66	None	-7	31	Human	4.8	pKi	=	4.8	Binding	DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
	2157	7186	66	None	-7	31	Human	4.8	pKi	=	4.8	Binding	DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
	2566	7186	66	None	-7	31	Human	4.8	pKi	=	4.8	Binding	DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
	CHEMBL633	7186	66	None	-7	31	Human	4.8	pKi	=	4.8	Binding	DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
	DB01118	7186	66	None	-7	31	Human	4.8	pKi	=	4.8	Binding	DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
	10620185	126429	0	None	89	2	Rat	7.8	pKi	=	7.8	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	386	6	1	5	4.5	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(OC(C)C)cc2)c1C	10.1021/jm970872k
	CHEMBL346853	126429	0	None	89	2	Rat	7.8	pKi	=	7.8	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	386	6	1	5	4.5	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(OC(C)C)cc2)c1C	10.1021/jm970872k
	10741144	126547	0	None	407	2	Rat	7.8	pKi	=	7.8	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	427	8	2	5	4.5	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2NC=O)c1C	10.1021/jm970872k
	CHEMBL347982	126547	0	None	407	2	Rat	7.8	pKi	=	7.8	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	427	8	2	5	4.5	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2NC=O)c1C	10.1021/jm970872k
	17979733	104018	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	576	10	1	8	6.0	CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(COC)c1)C(=O)CCCC2	10.1016/s0960-894x(03)00018-0
	CHEMBL268706	104018	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	576	10	1	8	6.0	CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(COC)c1)C(=O)CCCC2	10.1016/s0960-894x(03)00018-0
	44303033	209997	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	472	6	1	5	5.4	COc1ccc(CC2C(c3ccc(Cl)c(Cl)c3)C(=O)O[C@@]2(O)c2ccc(OC)cc2)cc1	10.1021/jm990504b
	CHEMBL64424	209997	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	472	6	1	5	5.4	COc1ccc(CC2C(c3ccc(Cl)c(Cl)c3)C(=O)O[C@@]2(O)c2ccc(OC)cc2)cc1	10.1021/jm990504b
	9934204	113722	0	None	-1	2	Human	4.8	pKi	=	4.8	Binding	Affinity against ET A receptorAffinity against ET A receptor	ChEMBL	465	7	2	4	6.0	CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(NCc3cccc4ccccc34)ccc21	10.1016/0960-894X(95)00019-P
	CHEMBL314915	113722	0	None	-1	2	Human	4.8	pKi	=	4.8	Binding	Affinity against ET A receptorAffinity against ET A receptor	ChEMBL	465	7	2	4	6.0	CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(NCc3cccc4ccccc34)ccc21	10.1016/0960-894X(95)00019-P
	10836754	210369	0	None	14	2	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	438	11	1	7	3.7	CCOc1cc(OCC)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1	10.1021/jm960274q
	CHEMBL66893	210369	0	None	14	2	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	438	11	1	7	3.7	CCOc1cc(OCC)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1	10.1021/jm960274q
	10691437	11854	0	None	-1	4	Rat	7.8	pKi	=	7.8	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	384	6	1	4	5.0	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2)c1C	10.1021/jm970872k
	CHEMBL105490	11854	0	None	-1	4	Rat	7.8	pKi	=	7.8	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	384	6	1	4	5.0	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2)c1C	10.1021/jm970872k
	443289	7498	47	None	2	3	Human	7.8	pKi	=	7.8	Binding	Affinity against ET A receptorAffinity against ET A receptor	ChEMBL		None	None	None		None	10.1016/0960-894X(95)00019-P
	997	7498	47	None	2	3	Human	7.8	pKi	=	7.8	Binding	Affinity against ET A receptorAffinity against ET A receptor	ChEMBL		None	None	None		None	10.1016/0960-894X(95)00019-P
	CHEMBL314691	7498	47	None	2	3	Human	7.8	pKi	=	7.8	Binding	Affinity against ET A receptorAffinity against ET A receptor	ChEMBL		None	None	None		None	10.1016/0960-894X(95)00019-P
	DB12054	7498	47	None	2	3	Human	7.8	pKi	=	7.8	Binding	Affinity against ET A receptorAffinity against ET A receptor	ChEMBL		None	None	None		None	10.1016/0960-894X(95)00019-P
	10691437	11854	0	None	1	4	Human	7.8	pKi	=	7.8	Binding	Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.	ChEMBL	384	6	1	4	5.0	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2)c1C	10.1021/jm000105c
	CHEMBL105490	11854	0	None	1	4	Human	7.8	pKi	=	7.8	Binding	Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.	ChEMBL	384	6	1	4	5.0	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2)c1C	10.1021/jm000105c
	CHEMBL1201469	21279	0	None	-1	4	Human	5.7	pKi	=	5.7	Binding	DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)	ChEMBL		None	None	None		None	nan
	22103797	48152	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.	ChEMBL	408	5	1	6	4.2	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3nccn3C)cc2)c1C	10.1016/s0960-894x(01)00791-0
	CHEMBL149010	48152	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.	ChEMBL	408	5	1	6	4.2	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3nccn3C)cc2)c1C	10.1016/s0960-894x(01)00791-0
	5122650	109708	5	None	100	2	Human	7.7	pKi	=	7.7	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	364	7	1	5	3.2	COC(c1ccccc1)(c1ccccc1)C(Oc1nccc(C)n1)C(=O)O	10.1021/jm960274q
	CHEMBL306218	109708	5	None	100	2	Human	7.7	pKi	=	7.7	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	364	7	1	5	3.2	COC(c1ccccc1)(c1ccccc1)C(Oc1nccc(C)n1)C(=O)O	10.1021/jm960274q
	11797288	210395	0	None	89	2	Human	7.7	pKi	=	7.7	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	438	11	1	7	3.7	CCCOC(c1ccccc1)(c1ccccc1)C(Oc1nc(OC)cc(OC)n1)C(=O)O	10.1021/jm960274q
	CHEMBL67084	210395	0	None	89	2	Human	7.7	pKi	=	7.7	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	438	11	1	7	3.7	CCCOC(c1ccccc1)(c1ccccc1)C(Oc1nc(OC)cc(OC)n1)C(=O)O	10.1021/jm960274q
	10669224	115243	0	None	1778	2	Human	7.7	pKi	=	7.7	Binding	Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.	ChEMBL	409	6	1	6	4.3	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(Cc3ncco3)cc2)c1C	10.1021/jm000105c
	CHEMBL319924	115243	0	None	1778	2	Human	7.7	pKi	=	7.7	Binding	Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.	ChEMBL	409	6	1	6	4.3	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(Cc3ncco3)cc2)c1C	10.1021/jm000105c
	10673091	170104	0	None	4	2	Human	7.7	pKi	=	7.7	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	502	10	1	5	5.8	Cc1cc(C)nc(OC(C(=O)O)C(OCCc2ccc(Cl)cc2)(c2ccccc2)c2ccccc2)n1	10.1021/jm9910425
	CHEMBL418992	170104	0	None	4	2	Human	7.7	pKi	=	7.7	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	502	10	1	5	5.8	Cc1cc(C)nc(OC(C(=O)O)C(OCCc2ccc(Cl)cc2)(c2ccccc2)c2ccccc2)n1	10.1021/jm9910425
	10836583	46467	0	None	43	2	Rat	6.7	pKi	=	6.7	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	434	7	1	5	5.3	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(OCc3ccccc3)cc2)c1C	10.1021/jm970872k
	CHEMBL147521	46467	0	None	43	2	Rat	6.7	pKi	=	6.7	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	434	7	1	5	5.3	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(OCc3ccccc3)cc2)c1C	10.1021/jm970872k
	10643748	128215	0	None	29	2	Rat	6.7	pKi	=	6.7	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	384	6	1	4	5.0	Cc1noc(NS(=O)(=O)c2ccccc2-c2cccc(CC(C)C)c2)c1C	10.1021/jm970872k
	CHEMBL358226	128215	0	None	29	2	Rat	6.7	pKi	=	6.7	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	384	6	1	4	5.0	Cc1noc(NS(=O)(=O)c2ccccc2-c2cccc(CC(C)C)c2)c1C	10.1021/jm970872k
	10813050	50827	0	None	602	2	Rat	8.7	pKi	=	8.7	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	441	9	2	5	4.2	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2CNC=O)c1C	10.1021/jm970872k
	CHEMBL151440	50827	0	None	602	2	Rat	8.7	pKi	=	8.7	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	441	9	2	5	4.2	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2CNC=O)c1C	10.1021/jm970872k
	9895957	17445	18	None	3	3	Human	8.7	pKi	=	8.7	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	659	11	1	7	6.8	CCCCC1=NC2(CCCC2)C(=O)N1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(CN2CCC(C)(C)C2=O)c1	10.1016/s0960-894x(03)00018-0
	CHEMBL11706	17445	18	None	3	3	Human	8.7	pKi	=	8.7	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	659	11	1	7	6.8	CCCCC1=NC2(CCCC2)C(=O)N1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(CN2CCC(C)(C)C2=O)c1	10.1016/s0960-894x(03)00018-0
	10835335	11609	0	None	50118	2	Human	8.7	pKi	=	8.7	Binding	Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.	ChEMBL	409	5	1	6	4.7	Cc1coc(-c2ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)cc2)n1	10.1021/jm000105c
	CHEMBL104223	11609	0	None	50118	2	Human	8.7	pKi	=	8.7	Binding	Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.	ChEMBL	409	5	1	6	4.7	Cc1coc(-c2ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)cc2)n1	10.1021/jm000105c
	11799973	11204	0	None	31	2	Human	8.7	pKi	=	8.7	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	514	11	1	7	5.1	COc1ccc(COC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1OC	10.1021/jm9910425
	CHEMBL101587	11204	0	None	31	2	Human	8.7	pKi	=	8.7	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	514	11	1	7	5.1	COc1ccc(COC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1OC	10.1021/jm9910425
	9893800	114007	12	None	2	2	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting methodDisplacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting method	ChEMBL	528	12	1	7	5.1	COc1ccc(CCOC(c2ccccc2)(c2ccccc2)[C@H](Oc2nc(C)cc(C)n2)C(=O)O)cc1OC	10.1021/acs.jmedchem.5b01781
	CHEMBL316735	114007	12	None	2	2	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting methodDisplacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting method	ChEMBL	528	12	1	7	5.1	COc1ccc(CCOC(c2ccccc2)(c2ccccc2)[C@H](Oc2nc(C)cc(C)n2)C(=O)O)cc1OC	10.1021/acs.jmedchem.5b01781
	9893800	114007	12	None	2	2	Human	8.7	pKi	=	8.7	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	528	12	1	7	5.1	COc1ccc(CCOC(c2ccccc2)(c2ccccc2)[C@H](Oc2nc(C)cc(C)n2)C(=O)O)cc1OC	10.1021/jm9910425
	CHEMBL316735	114007	12	None	2	2	Human	8.7	pKi	=	8.7	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	528	12	1	7	5.1	COc1ccc(CCOC(c2ccccc2)(c2ccccc2)[C@H](Oc2nc(C)cc(C)n2)C(=O)O)cc1OC	10.1021/jm9910425
	44311727	211248	0	None	-9	2	Human	8.7	pKi	=	8.7	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	669	13	3	7	4.7	CCCS(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1	10.1016/s0960-894x(98)00387-4
	CHEMBL72348	211248	0	None	-9	2	Human	8.7	pKi	=	8.7	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	669	13	3	7	4.7	CCCS(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1	10.1016/s0960-894x(98)00387-4
	76312118	92122	0	None	691	2	Human	8.7	pKi	=	8.7	Binding	Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells	ChEMBL	522	7	2	8	3.4	COc1cc(C)ccc1S(=O)(=O)NC(=O)[C@@H](c1ccc2c(c1)OCO2)c1cn(C)c2cc(CO)ccc12	10.1007/s00044-004-0021-y
	CHEMBL2261361	92122	0	None	691	2	Human	8.7	pKi	=	8.7	Binding	Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells	ChEMBL	522	7	2	8	3.4	COc1cc(C)ccc1S(=O)(=O)NC(=O)[C@@H](c1ccc2c(c1)OCO2)c1cn(C)c2cc(CO)ccc12	10.1007/s00044-004-0021-y
	18660521	48471	0	None	2754	2	Human	8.6	pKi	=	8.6	Binding	Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.	ChEMBL	405	5	1	5	4.8	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ccccn3)cc2)c1C	10.1016/s0960-894x(01)00791-0
	CHEMBL149232	48471	0	None	2754	2	Human	8.6	pKi	=	8.6	Binding	Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.	ChEMBL	405	5	1	5	4.8	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ccccn3)cc2)c1C	10.1016/s0960-894x(01)00791-0
	44311915	111568	0	None	-6	2	Human	8.6	pKi	=	8.6	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	703	12	3	7	5.4	Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccno3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NS(=O)(=O)c2ccccc2)c1	10.1016/s0960-894x(98)00387-4
	CHEMBL310920	111568	0	None	-6	2	Human	8.6	pKi	=	8.6	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	703	12	3	7	5.4	Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccno3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NS(=O)(=O)c2ccccc2)c1	10.1016/s0960-894x(98)00387-4
	10768897	114434	1	None	6	2	Human	8.6	pKi	=	8.6	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	544	13	1	8	4.8	COc1cc(C)nc(OC(C(=O)O)C(OCCc2ccc(OC)c(OC)c2)(c2ccccc2)c2ccccc2)n1	10.1021/jm9910425
	CHEMBL319031	114434	1	None	6	2	Human	8.6	pKi	=	8.6	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	544	13	1	8	4.8	COc1cc(C)nc(OC(C(=O)O)C(OCCc2ccc(OC)c(OC)c2)(c2ccccc2)c2ccccc2)n1	10.1021/jm9910425
	51003307	64838	0	None	3548	2	Mouse	8.6	pKi	=	8.6	Binding	Displacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting	ChEMBL	751	21	1	15	4.0	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCc3cn(CCOCCOCCOCCF)nn3)c2)cc1	10.1021/jm101110w
	CHEMBL1672881	64838	0	None	3548	2	Mouse	8.6	pKi	=	8.6	Binding	Displacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting	ChEMBL	751	21	1	15	4.0	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCc3cn(CCOCCOCCOCCF)nn3)c2)cc1	10.1021/jm101110w
	45257115	208111	0	None	39	2	Mouse	8.6	pKi	=	8.6	Binding	Displacement of [125I]ET1 from endothelin A receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin A receptor in DBA mouse microsomes	ChEMBL	538	10	1	9	4.2	COc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OCCF)cc2)cc(OC)c1OC	10.1016/j.bmc.2009.08.058
	CHEMBL604286	208111	0	None	39	2	Mouse	8.6	pKi	=	8.6	Binding	Displacement of [125I]ET1 from endothelin A receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin A receptor in DBA mouse microsomes	ChEMBL	538	10	1	9	4.2	COc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OCCF)cc2)cc(OC)c1OC	10.1016/j.bmc.2009.08.058
	CHEMBL1790180	215662	0	None	-72	3	Rat	8.6	pKi	=	8.6	Binding	Compound was evaluated for the binding affinity to Endothelin A receptor in the rat aortaCompound was evaluated for the binding affinity to Endothelin A receptor in the rat aorta	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CCc3ccc(O)cc3)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H](Cc3ccccc3)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1021/jm00087a001
	11049336	106716	0	None	3630	2	Human	8.6	pKi	=	8.6	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	497	7	1	6	6.6	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2/C=C/c2ccccc2)c1C	10.1021/jm020289q
	CHEMBL286279	106716	0	None	3630	2	Human	8.6	pKi	=	8.6	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	497	7	1	6	6.6	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2/C=C/c2ccccc2)c1C	10.1021/jm020289q
	10670965	49100	0	None	851	2	Rat	8.6	pKi	=	8.6	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	444	9	2	6	4.3	Cc1noc(NS(=O)(=O)c2cccc(OCCO)c2-c2ccc(CC(C)C)cc2)c1C	10.1021/jm970872k
	CHEMBL149819	49100	0	None	851	2	Rat	8.6	pKi	=	8.6	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	444	9	2	6	4.3	Cc1noc(NS(=O)(=O)c2cccc(OCCO)c2-c2ccc(CC(C)C)cc2)c1C	10.1021/jm970872k
	44311804	109795	0	None	-12	2	Human	8.5	pKi	=	8.5	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	683	14	3	7	5.1	CCCCS(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1	10.1016/s0960-894x(98)00387-4
	CHEMBL306950	109795	0	None	-12	2	Human	8.5	pKi	=	8.5	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	683	14	3	7	5.1	CCCCS(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1	10.1016/s0960-894x(98)00387-4
	10501931	50647	0	None	64	2	Rat	7.7	pKi	=	7.7	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	414	7	2	5	4.5	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2CO)c1C	10.1021/jm970872k
	CHEMBL151160	50647	0	None	64	2	Rat	7.7	pKi	=	7.7	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	414	7	2	5	4.5	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2CO)c1C	10.1021/jm970872k
	10668819	127892	0	None	602	2	Rat	7.7	pKi	=	7.7	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	402	6	1	4	5.1	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2F)c1C	10.1021/jm970872k
	CHEMBL357395	127892	0	None	602	2	Rat	7.7	pKi	=	7.7	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	402	6	1	4	5.1	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2F)c1C	10.1021/jm970872k
	22574798	22292	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	579	13	2	8	5.2	CCCc1nc(CC)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(COCC)c1	10.1016/s0960-894x(03)00018-0
	CHEMBL12175	22292	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	579	13	2	8	5.2	CCCc1nc(CC)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(COCC)c1	10.1016/s0960-894x(03)00018-0
	17979749	24619	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	550	8	1	7	6.0	CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(F)c1)C(=O)CCCC2	10.1016/s0960-894x(03)00018-0
	CHEMBL12590	24619	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	550	8	1	7	6.0	CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(F)c1)C(=O)CCCC2	10.1016/s0960-894x(03)00018-0
	44267860	173904	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	590	11	1	8	6.4	CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(COCC)c1)C(=O)CCCC2	10.1016/s0960-894x(03)00018-0
	CHEMBL429037	173904	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	590	11	1	8	6.4	CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(COCC)c1)C(=O)CCCC2	10.1016/s0960-894x(03)00018-0
	10599129	109013	0	None	5	2	Human	6.7	pKi	=	6.7	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	438	9	1	7	3.5	COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccc(C)cc2)c2ccc(C)cc2)n1	10.1021/jm960274q
	CHEMBL303034	109013	0	None	5	2	Human	6.7	pKi	=	6.7	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	438	9	1	7	3.5	COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccc(C)cc2)c2ccc(C)cc2)n1	10.1021/jm960274q
	44314882	163955	0	None	-380	2	Pig	5.7	pKi	=	5.7	Binding	Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated	ChEMBL	1562	47	19	18	0.4	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(96)00421-0
	77282212	163955	0	None	-380	2	Pig	5.7	pKi	=	5.7	Binding	Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated	ChEMBL	1562	47	19	18	0.4	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(96)00421-0
	CHEMBL407559	163955	0	None	-380	2	Pig	5.7	pKi	=	5.7	Binding	Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated	ChEMBL	1562	47	19	18	0.4	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(96)00421-0
	10813228	114437	0	None	46	2	Human	5.7	pKi	=	5.7	Binding	Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.	ChEMBL	445	5	1	6	5.6	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3nc4ccccc4o3)cc2)c1C	10.1021/jm000105c
	CHEMBL319036	114437	0	None	46	2	Human	5.7	pKi	=	5.7	Binding	Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.	ChEMBL	445	5	1	6	5.6	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3nc4ccccc4o3)cc2)c1C	10.1021/jm000105c
	10545378	45990	0	None	-	1	Rat	5.7	pKi	=	5.7	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	344	5	1	5	3.9	Cc1noc(NS(=O)(=O)c2ccccc2Oc2ccccc2)c1C	10.1021/jm970872k
	CHEMBL147007	45990	0	None	-	1	Rat	5.7	pKi	=	5.7	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	344	5	1	5	3.9	Cc1noc(NS(=O)(=O)c2ccccc2Oc2ccccc2)c1C	10.1021/jm970872k
	20747573	23922	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	593	13	2	8	5.4	CCCc1nc(CC)c(C(=O)NC)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(COCC)c1	10.1016/s0960-894x(03)00018-0
	CHEMBL12557	23922	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	593	13	2	8	5.4	CCCc1nc(CC)c(C(=O)NC)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(COCC)c1	10.1016/s0960-894x(03)00018-0
	10719157	109072	0	None	58	2	Human	7.7	pKi	=	7.7	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	470	11	1	9	2.9	COc1cccc(C(OC)(c2cccc(OC)c2)C(Oc2nc(OC)cc(OC)n2)C(=O)O)c1	10.1021/jm960274q
	CHEMBL303390	109072	0	None	58	2	Human	7.7	pKi	=	7.7	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	470	11	1	9	2.9	COc1cccc(C(OC)(c2cccc(OC)c2)C(Oc2nc(OC)cc(OC)n2)C(=O)O)c1	10.1021/jm960274q
	19085508	46360	0	None	218	2	Human	6.7	pKi	=	6.7	Binding	Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.	ChEMBL	466	7	1	8	4.2	COc1cc(OC)nc(-c2ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)cc2)n1	10.1016/s0960-894x(01)00791-0
	CHEMBL147365	46360	0	None	218	2	Human	6.7	pKi	=	6.7	Binding	Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.	ChEMBL	466	7	1	8	4.2	COc1cc(OC)nc(-c2ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)cc2)n1	10.1016/s0960-894x(01)00791-0
	CHEMBL315927	217973	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Affinity against ET A receptorAffinity against ET A receptor	ChEMBL		None	None	None		CC(C)C[C@@H]1NC(=O)[C@@H](C(C)C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](Cc2cccc3ccccc23)NC1=O	10.1016/0960-894X(95)00019-P
	10505434	11438	0	None	7	2	Human	7.6	pKi	=	7.6	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	496	11	1	5	5.8	Cc1ccc(CCCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1	10.1021/jm9910425
	CHEMBL103190	11438	0	None	7	2	Human	7.6	pKi	=	7.6	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	496	11	1	5	5.8	Cc1ccc(CCCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1	10.1021/jm9910425
	11801906	105304	0	None	-1	2	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	612	13	1	8	6.2	COc1cc(C)nc(OC(C(=O)O)C(OCCc2ccc(OC)c(OC)c2)(c2ccc(Cl)cc2)c2ccc(Cl)cc2)n1	10.1021/jm9910425
	CHEMBL276288	105304	0	None	-1	2	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	612	13	1	8	6.2	COc1cc(C)nc(OC(C(=O)O)C(OCCc2ccc(OC)c(OC)c2)(c2ccc(Cl)cc2)c2ccc(Cl)cc2)n1	10.1021/jm9910425
	44311698	210889	0	None	-524	2	Human	5.6	pKi	=	5.6	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	574	10	3	4	5.3	Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccccn3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1	10.1016/s0960-894x(98)00387-4
	CHEMBL70310	210889	0	None	-524	2	Human	5.6	pKi	=	5.6	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	574	10	3	4	5.3	Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccccn3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1	10.1016/s0960-894x(98)00387-4
	10670662	210227	0	None	53	2	Human	7.6	pKi	=	7.6	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	438	9	1	7	3.5	COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2cccc(C)c2)c2cccc(C)c2)n1	10.1021/jm960274q
	CHEMBL65833	210227	0	None	53	2	Human	7.6	pKi	=	7.6	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	438	9	1	7	3.5	COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2cccc(C)c2)c2cccc(C)c2)n1	10.1021/jm960274q
	CHEMBL87296	222674	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Affinity against ET A receptorAffinity against ET A receptor	ChEMBL		None	None	None		CC(C)C[C@@H]1NC(=O)[C@@H](C(C)C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC1=O	10.1016/0960-894X(95)00019-P
	10645256	47814	0	None	-	1	Rat	4.6	pKi	=	4.6	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	410	6	1	4	5.2	CC(C)Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc3c2CCCC3)cc1	10.1021/jm970872k
	CHEMBL148757	47814	0	None	-	1	Rat	4.6	pKi	=	4.6	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	410	6	1	4	5.2	CC(C)Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc3c2CCCC3)cc1	10.1021/jm970872k
	10552683	209890	0	None	5	2	Human	6.6	pKi	=	6.6	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	478	9	1	7	4.2	COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccc(Cl)cc2)c2ccc(Cl)cc2)n1	10.1021/jm960274q
	CHEMBL64009	209890	0	None	5	2	Human	6.6	pKi	=	6.6	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	478	9	1	7	4.2	COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccc(Cl)cc2)c2ccc(Cl)cc2)n1	10.1021/jm960274q
	18660522	126430	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.	ChEMBL	406	5	1	6	4.2	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ccncn3)cc2)c1C	10.1016/s0960-894x(01)00791-0
	CHEMBL346862	126430	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.	ChEMBL	406	5	1	6	4.2	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ccncn3)cc2)c1C	10.1016/s0960-894x(01)00791-0
	46228116	208001	0	None	2	2	Mouse	7.6	pKi	=	7.6	Binding	Displacement of [125I]ET1 from endothelin A receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin A receptor in DBA mouse microsomes	ChEMBL	598	10	1	9	4.6	COc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OCCBr)cc2)cc(OC)c1OC	10.1016/j.bmc.2009.08.058
	CHEMBL603635	208001	0	None	2	2	Mouse	7.6	pKi	=	7.6	Binding	Displacement of [125I]ET1 from endothelin A receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin A receptor in DBA mouse microsomes	ChEMBL	598	10	1	9	4.6	COc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OCCBr)cc2)cc(OC)c1OC	10.1016/j.bmc.2009.08.058
	3921421	114076	8	None	9	2	Human	7.6	pKi	=	7.6	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	468	10	1	5	5.1	Cc1cc(C)nc(OC(C(=O)O)C(OCCc2ccccc2)(c2ccccc2)c2ccccc2)n1	10.1021/jm9910425
	CHEMBL317233	114076	8	None	9	2	Human	7.6	pKi	=	7.6	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	468	10	1	5	5.1	Cc1cc(C)nc(OC(C(=O)O)C(OCCc2ccccc2)(c2ccccc2)c2ccccc2)n1	10.1021/jm9910425
	44314832	168052	0	None	-251	2	Pig	6.6	pKi	=	6.6	Binding	Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated	ChEMBL	1496	45	18	17	0.5	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(96)00421-0
	CHEMBL412065	168052	0	None	-251	2	Pig	6.6	pKi	=	6.6	Binding	Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated	ChEMBL	1496	45	18	17	0.5	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(96)00421-0
	44274960	106339	0	None	12	2	Human	6.6	pKi	=	6.6	Binding	Binding affinity against human Endothelin A receptorBinding affinity against human Endothelin A receptor	ChEMBL	450	10	1	6	4.9	COc1cc(OC)nc(CC(C(=O)O)C(C)(Oc2ccc(C(C)C)cc2)c2ccccc2)n1	10.1021/jm030480f
	CHEMBL283637	106339	0	None	12	2	Human	6.6	pKi	=	6.6	Binding	Binding affinity against human Endothelin A receptorBinding affinity against human Endothelin A receptor	ChEMBL	450	10	1	6	4.9	COc1cc(OC)nc(CC(C(=O)O)C(C)(Oc2ccc(C(C)C)cc2)c2ccccc2)n1	10.1021/jm030480f
	44311699	210948	0	None	-331	2	Human	6.6	pKi	=	6.6	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	563	10	3	4	5.5	Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccco3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1	10.1016/s0960-894x(98)00387-4
	CHEMBL70686	210948	0	None	-331	2	Human	6.6	pKi	=	6.6	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	563	10	3	4	5.5	Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccco3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1	10.1016/s0960-894x(98)00387-4
	44307412	210437	0	None	12	2	Human	6.6	pKi	=	6.6	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	466	10	0	8	4.5	COC(=O)C(Oc1nc(OC)cc(OC)n1)C(C)(Oc1ccc(C(C)C)cc1)c1ccccc1	10.1021/jm960274q
	CHEMBL67325	210437	0	None	12	2	Human	6.6	pKi	=	6.6	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	466	10	0	8	4.5	COC(=O)C(Oc1nc(OC)cc(OC)n1)C(C)(Oc1ccc(C(C)C)cc1)c1ccccc1	10.1021/jm960274q
	10721484	114138	0	None	-1	2	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	554	13	1	6	6.3	CCc1ccc(C(OCCc2ccc(OC)cc2)(c2ccc(CC)cc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1	10.1021/jm9910425
	CHEMBL317716	114138	0	None	-1	2	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	554	13	1	6	6.3	CCc1ccc(C(OCCc2ccc(OC)cc2)(c2ccc(CC)cc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1	10.1021/jm9910425
	10621777	49848	0	None	12	2	Rat	5.6	pKi	=	5.6	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	415	7	1	6	4.6	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2)c1[N+](=O)[O-]	10.1021/jm970872k
	CHEMBL150481	49848	0	None	12	2	Rat	5.6	pKi	=	5.6	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	415	7	1	6	4.6	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2)c1[N+](=O)[O-]	10.1021/jm970872k
	9797546	47666	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.	ChEMBL	329	4	1	5	3.2	Cc1noc(NS(=O)(=O)c2ccccc2-c2cccnc2)c1C	10.1021/jm970872k
	CHEMBL148637	47666	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.	ChEMBL	329	4	1	5	3.2	Cc1noc(NS(=O)(=O)c2ccccc2-c2cccnc2)c1C	10.1021/jm970872k
	22103537	48846	0	None	144	2	Human	6.6	pKi	=	6.6	Binding	Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.	ChEMBL	395	5	1	6	4.4	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ccno3)cc2)c1C	10.1016/s0960-894x(01)00791-0
	CHEMBL149592	48846	0	None	144	2	Human	6.6	pKi	=	6.6	Binding	Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.	ChEMBL	395	5	1	6	4.4	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ccno3)cc2)c1C	10.1016/s0960-894x(01)00791-0
	44312023	211243	0	None	-22	2	Human	4.6	pKi	=	4.6	Binding	Compound was tested for the binding affinity against Endothelin A receptorCompound was tested for the binding affinity against Endothelin A receptor	ChEMBL	596	13	2	7	4.0	CCCCS(=O)(=O)NC(=O)[C@H](NC(=O)[C@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)C	10.1016/s0960-894x(98)00388-6
	CHEMBL72295	211243	0	None	-22	2	Human	4.6	pKi	=	4.6	Binding	Compound was tested for the binding affinity against Endothelin A receptorCompound was tested for the binding affinity against Endothelin A receptor	ChEMBL	596	13	2	7	4.0	CCCCS(=O)(=O)NC(=O)[C@H](NC(=O)[C@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)C	10.1016/s0960-894x(98)00388-6
	10595347	49255	0	None	537	2	Rat	7.6	pKi	=	7.6	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	370	6	1	4	4.7	CCCc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1021/jm970872k
	CHEMBL149953	49255	0	None	537	2	Rat	7.6	pKi	=	7.6	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	370	6	1	4	4.7	CCCc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1021/jm970872k
	10741830	49617	0	None	3	2	Rat	5.6	pKi	=	5.6	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	441	7	2	5	4.9	CC(=O)Nc1ccc(S(=O)(=O)Nc2onc(C)c2C)c(-c2ccc(CC(C)C)cc2)c1	10.1021/jm970872k
	CHEMBL150269	49617	0	None	3	2	Rat	5.6	pKi	=	5.6	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	441	7	2	5	4.9	CC(=O)Nc1ccc(S(=O)(=O)Nc2onc(C)c2C)c(-c2ccc(CC(C)C)cc2)c1	10.1021/jm970872k
	15297287	171191	0	None	-3	2	Human	4.6	pKi	=	4.6	Binding	Affinity against ET A receptorAffinity against ET A receptor	ChEMBL	424	5	2	4	5.2	O=C(O)CN1C(=O)c2ccccc2Nc2ccc(OCc3cccc4ccccc34)cc21	10.1016/0960-894X(95)00019-P
	CHEMBL421349	171191	0	None	-3	2	Human	4.6	pKi	=	4.6	Binding	Affinity against ET A receptorAffinity against ET A receptor	ChEMBL	424	5	2	4	5.2	O=C(O)CN1C(=O)c2ccccc2Nc2ccc(OCc3cccc4ccccc34)cc21	10.1016/0960-894X(95)00019-P
	10599293	45799	0	None	128	2	Rat	7.5	pKi	=	7.5	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	441	9	2	5	5.8	CCCNc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C	10.1021/jm970872k
	CHEMBL146845	45799	0	None	128	2	Rat	7.5	pKi	=	7.5	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	441	9	2	5	5.8	CCCNc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C	10.1021/jm970872k
	10508342	11502	0	None	-1	2	Human	6.5	pKi	=	6.5	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	638	13	1	8	6.3	COc1ccc(CCOC(c2ccc(Cl)cc2)(c2ccc(Cl)cc2)C(Oc2nc3c(c(OC)n2)CCC3)C(=O)O)cc1OC	10.1021/jm9910425
	CHEMBL103605	11502	0	None	-1	2	Human	6.5	pKi	=	6.5	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	638	13	1	8	6.3	COc1ccc(CCOC(c2ccc(Cl)cc2)(c2ccc(Cl)cc2)C(Oc2nc3c(c(OC)n2)CCC3)C(=O)O)cc1OC	10.1021/jm9910425
	44311849	109850	0	None	-5	2	Human	8.5	pKi	=	8.5	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	694	14	2	7	5.8	CCCCS(=O)(=O)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1	10.1016/s0960-894x(98)00387-4
	CHEMBL307384	109850	0	None	-5	2	Human	8.5	pKi	=	8.5	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	694	14	2	7	5.8	CCCCS(=O)(=O)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1	10.1016/s0960-894x(98)00387-4
	11800649	11381	0	None	7	2	Human	8.5	pKi	=	8.5	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	542	13	1	7	5.5	CCOc1ccc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1OC	10.1021/jm9910425
	CHEMBL102797	11381	0	None	7	2	Human	8.5	pKi	=	8.5	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	542	13	1	7	5.5	CCOc1ccc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1OC	10.1021/jm9910425
	19085510	126333	0	None	6025	2	Human	8.5	pKi	=	8.5	Binding	Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.	ChEMBL	405	5	1	5	4.8	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3cccnc3)cc2)c1C	10.1016/s0960-894x(01)00791-0
	CHEMBL345951	126333	0	None	6025	2	Human	8.5	pKi	=	8.5	Binding	Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.	ChEMBL	405	5	1	5	4.8	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3cccnc3)cc2)c1C	10.1016/s0960-894x(01)00791-0
	10528863	11392	0	None	4	2	Human	8.5	pKi	=	8.5	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	484	10	2	6	4.8	Cc1cc(C)nc(OC(C(=O)O)C(OCCc2ccc(O)cc2)(c2ccccc2)c2ccccc2)n1	10.1021/jm9910425
	CHEMBL102868	11392	0	None	4	2	Human	8.5	pKi	=	8.5	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	484	10	2	6	4.8	Cc1cc(C)nc(OC(C(=O)O)C(OCCc2ccc(O)cc2)(c2ccccc2)c2ccccc2)n1	10.1021/jm9910425
	6433100	11321	7	None	2	2	Human	8.5	pKi	=	8.5	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	528	12	1	7	5.1	COc1ccc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1OC	10.1021/jm9910425
	CHEMBL102405	11321	7	None	2	2	Human	8.5	pKi	=	8.5	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	528	12	1	7	5.1	COc1ccc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1OC	10.1021/jm9910425
	51003353	64840	0	None	10	2	Mouse	8.5	pKi	=	8.5	Binding	Displacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting	ChEMBL	886	26	1	17	5.5	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOCCOCCOCCn3cc(CCCCOc4cccnc4F)nn3)c2)cc1	10.1021/jm101110w
	CHEMBL1672883	64840	0	None	10	2	Mouse	8.5	pKi	=	8.5	Binding	Displacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting	ChEMBL	886	26	1	17	5.5	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOCCOCCOCCn3cc(CCCCOc4cccnc4F)nn3)c2)cc1	10.1021/jm101110w
	10548722	12252	0	None	20892	2	Human	8.4	pKi	=	8.4	Binding	Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.	ChEMBL	395	5	1	6	4.4	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3cnco3)cc2)c1C	10.1021/jm000105c
	CHEMBL107574	12252	0	None	20892	2	Human	8.4	pKi	=	8.4	Binding	Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.	ChEMBL	395	5	1	6	4.4	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3cnco3)cc2)c1C	10.1021/jm000105c
	44311726	109862	0	None	-10	2	Human	8.4	pKi	=	8.4	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	667	12	3	7	4.8	C/C=C/S(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1	10.1016/s0960-894x(98)00387-4
	CHEMBL307471	109862	0	None	-10	2	Human	8.4	pKi	=	8.4	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	667	12	3	7	4.8	C/C=C/S(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1	10.1016/s0960-894x(98)00387-4
	51003354	64841	0	None	74	2	Mouse	8.4	pKi	=	8.4	Binding	Displacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting	ChEMBL	920	24	1	17	4.5	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOCCOCCOCCn3cc(CN(C)S(=O)(=O)c4ccc(F)cc4)nn3)c2)cc1	10.1021/jm101110w
	CHEMBL1672884	64841	0	None	74	2	Mouse	8.4	pKi	=	8.4	Binding	Displacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting	ChEMBL	920	24	1	17	4.5	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOCCOCCOCCn3cc(CN(C)S(=O)(=O)c4ccc(F)cc4)nn3)c2)cc1	10.1021/jm101110w
	18660523	48600	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.	ChEMBL	406	5	1	6	4.2	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3cncnc3)cc2)c1C	10.1016/s0960-894x(01)00791-0
	CHEMBL149340	48600	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.	ChEMBL	406	5	1	6	4.2	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3cncnc3)cc2)c1C	10.1016/s0960-894x(01)00791-0
	10525034	126452	0	None	89	2	Rat	7.5	pKi	=	7.5	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	400	7	1	5	4.8	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(OCC(C)C)cc2)c1C	10.1021/jm970872k
	CHEMBL347125	126452	0	None	89	2	Rat	7.5	pKi	=	7.5	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	400	7	1	5	4.8	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(OCC(C)C)cc2)c1C	10.1021/jm970872k
	10505357	116180	0	None	10	2	Human	7.5	pKi	=	7.5	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	494	10	1	5	5.9	Cc1ccc(/C=C/COC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1	10.1021/jm9910425
	CHEMBL321984	116180	0	None	10	2	Human	7.5	pKi	=	7.5	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	494	10	1	5	5.9	Cc1ccc(/C=C/COC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1	10.1021/jm9910425
	10624645	11105	0	None	1	2	Human	7.5	pKi	=	7.5	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	482	10	1	5	5.4	Cc1ccc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1	10.1021/jm9910425
	CHEMBL100954	11105	0	None	1	2	Human	7.5	pKi	=	7.5	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	482	10	1	5	5.4	Cc1ccc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1	10.1021/jm9910425
	10713411	171724	0	None	-	1	Rat	7.5	pKi	=	7.5	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	358	5	1	5	3.8	COc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1021/jm970872k
	CHEMBL422496	171724	0	None	-	1	Rat	7.5	pKi	=	7.5	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	358	5	1	5	3.8	COc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1021/jm970872k
	10671031	109471	0	None	29	2	Human	7.5	pKi	=	7.5	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	446	9	1	7	3.2	COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccc(F)cc2)c2ccc(F)cc2)n1	10.1021/jm960274q
	CHEMBL304721	109471	0	None	29	2	Human	7.5	pKi	=	7.5	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	446	9	1	7	3.2	COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccc(F)cc2)c2ccc(F)cc2)n1	10.1021/jm960274q
	10622410	50803	0	None	-	1	Rat	6.5	pKi	=	6.5	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	427	7	1	5	5.0	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2N(C)C)c1C	10.1021/jm970872k
	CHEMBL151395	50803	0	None	-	1	Rat	6.5	pKi	=	6.5	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	427	7	1	5	5.0	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2N(C)C)c1C	10.1021/jm970872k
	19934534	113472	0	None	-5	2	Human	4.5	pKi	=	4.5	Binding	Affinity against ET A receptorAffinity against ET A receptor	ChEMBL	468	6	3	4	5.0	CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(NC(=O)c3cc4ccccc4[nH]3)ccc21	10.1016/0960-894X(95)00019-P
	CHEMBL314364	113472	0	None	-5	2	Human	4.5	pKi	=	4.5	Binding	Affinity against ET A receptorAffinity against ET A receptor	ChEMBL	468	6	3	4	5.0	CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(NC(=O)c3cc4ccccc4[nH]3)ccc21	10.1016/0960-894X(95)00019-P
	10741834	50817	0	None	85	2	Rat	7.5	pKi	=	7.5	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	441	8	2	5	5.8	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2NC(C)C)c1C	10.1021/jm970872k
	CHEMBL151422	50817	0	None	85	2	Rat	7.5	pKi	=	7.5	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	441	8	2	5	5.8	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2NC(C)C)c1C	10.1021/jm970872k
	9864017	48102	0	None	194	2	Human	6.5	pKi	=	6.5	Binding	Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.	ChEMBL	367	4	2	4	4.2	Cc1noc(NS(=O)(=O)c2ccccc2-c2cc3ccccc3[nH]2)c1C	10.1021/jm970872k
	CHEMBL148967	48102	0	None	194	2	Human	6.5	pKi	=	6.5	Binding	Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.	ChEMBL	367	4	2	4	4.2	Cc1noc(NS(=O)(=O)c2ccccc2-c2cc3ccccc3[nH]2)c1C	10.1021/jm970872k
	10743346	109388	0	None	4	2	Human	6.5	pKi	=	6.5	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	480	11	1	7	4.7	COc1cc(OC)nc(OC(C(=O)O)C(OCCC(C)(C)C)(c2ccccc2)c2ccccc2)n1	10.1021/jm960274q
	CHEMBL304173	109388	0	None	4	2	Human	6.5	pKi	=	6.5	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	480	11	1	7	4.7	COc1cc(OC)nc(OC(C(=O)O)C(OCCC(C)(C)C)(c2ccccc2)c2ccccc2)n1	10.1021/jm960274q
	10709109	50904	0	None	-	1	Rat	5.5	pKi	=	5.5	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	297	4	1	6	2.0	Cc1noc(NS(=O)(=O)c2ccccc2[N+](=O)[O-])c1C	10.1021/jm970872k
	CHEMBL151545	50904	0	None	-	1	Rat	5.5	pKi	=	5.5	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	297	4	1	6	2.0	Cc1noc(NS(=O)(=O)c2ccccc2[N+](=O)[O-])c1C	10.1021/jm970872k
	10691438	51266	0	None	51	2	Rat	7.4	pKi	=	7.4	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	384	7	1	4	5.1	CCCCc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1021/jm970872k
	CHEMBL151926	51266	0	None	51	2	Rat	7.4	pKi	=	7.4	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	384	7	1	4	5.1	CCCCc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1021/jm970872k
	44213540	46255	0	None	831	2	Human	7.4	pKi	=	7.4	Binding	Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.	ChEMBL	421	5	1	5	4.1	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3cccc[n+]3[O-])cc2)c1C	10.1016/s0960-894x(01)00791-0
	CHEMBL147238	46255	0	None	831	2	Human	7.4	pKi	=	7.4	Binding	Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.	ChEMBL	421	5	1	5	4.1	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3cccc[n+]3[O-])cc2)c1C	10.1016/s0960-894x(01)00791-0
	10693130	128747	0	None	16	2	Rat	6.4	pKi	=	6.4	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	414	7	1	5	5.0	COc1ccc(S(=O)(=O)Nc2onc(C)c2C)c(-c2ccc(CC(C)C)cc2)c1	10.1021/jm970872k
	CHEMBL359152	128747	0	None	16	2	Rat	6.4	pKi	=	6.4	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	414	7	1	5	5.0	COc1ccc(S(=O)(=O)Nc2onc(C)c2C)c(-c2ccc(CC(C)C)cc2)c1	10.1021/jm970872k
	44365561	49044	0	None	524	2	Human	7.4	pKi	=	7.4	Binding	Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.	ChEMBL	404	5	1	4	5.4	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ccccc3)cc2)c1C	10.1016/s0960-894x(01)00791-0
	CHEMBL149763	49044	0	None	524	2	Human	7.4	pKi	=	7.4	Binding	Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.	ChEMBL	404	5	1	4	5.4	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ccccc3)cc2)c1C	10.1016/s0960-894x(01)00791-0
	44365878	49060	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.	ChEMBL	396	5	2	7	2.9	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3nn[nH]n3)cc2)c1C	10.1016/s0960-894x(01)00791-0
	CHEMBL149778	49060	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.	ChEMBL	396	5	2	7	2.9	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3nn[nH]n3)cc2)c1C	10.1016/s0960-894x(01)00791-0
	10501299	126632	0	None	147	2	Rat	7.4	pKi	=	7.4	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	402	6	1	5	5.3	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(SC(C)C)cc2)c1C	10.1021/jm970872k
	CHEMBL348685	126632	0	None	147	2	Rat	7.4	pKi	=	7.4	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	402	6	1	5	5.3	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(SC(C)C)cc2)c1C	10.1021/jm970872k
	11813485	24861	0	None	-8	2	Human	7.4	pKi	=	7.4	Binding	Compound was evaluated for its binding affinity towards human Endothelin A receptorCompound was evaluated for its binding affinity towards human Endothelin A receptor	ChEMBL	534	9	1	6	6.0	CCCCC1=NC2(CCCC2)C(=O)N1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1021/jm020138n
	CHEMBL126755	24861	0	None	-8	2	Human	7.4	pKi	=	7.4	Binding	Compound was evaluated for its binding affinity towards human Endothelin A receptorCompound was evaluated for its binding affinity towards human Endothelin A receptor	ChEMBL	534	9	1	6	6.0	CCCCC1=NC2(CCCC2)C(=O)N1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1021/jm020138n
	10769887	114269	0	None	1	2	Human	7.4	pKi	=	7.4	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	600	15	1	8	6.0	CCc1ccc(C(OCCc2ccc(OC)c(OC)c2)(c2ccc(CC)cc2)C(Oc2nc(C)cc(OC)n2)C(=O)O)cc1	10.1021/jm9910425
	CHEMBL318535	114269	0	None	1	2	Human	7.4	pKi	=	7.4	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	600	15	1	8	6.0	CCc1ccc(C(OCCc2ccc(OC)c(OC)c2)(c2ccc(CC)cc2)C(Oc2nc(C)cc(OC)n2)C(=O)O)cc1	10.1021/jm9910425
	10526510	127846	0	None	12	2	Rat	5.4	pKi	=	5.4	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	427	8	1	6	4.2	COc1cc(OC)nc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2)n1	10.1021/jm970872k
	CHEMBL356972	127846	0	None	12	2	Rat	5.4	pKi	=	5.4	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	427	8	1	6	4.2	COc1cc(OC)nc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2)n1	10.1021/jm970872k
	22103385	127863	0	None	19054	2	Human	8.4	pKi	=	8.4	Binding	Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.	ChEMBL	396	5	1	7	3.8	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3nnco3)cc2)c1C	10.1016/s0960-894x(01)00791-0
	CHEMBL357077	127863	0	None	19054	2	Human	8.4	pKi	=	8.4	Binding	Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.	ChEMBL	396	5	1	7	3.8	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3nnco3)cc2)c1C	10.1016/s0960-894x(01)00791-0
	20747574	18879	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	565	12	2	8	4.8	CCCc1nc(CC)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(COC)c1	10.1016/s0960-894x(03)00018-0
	CHEMBL11840	18879	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	565	12	2	8	4.8	CCCc1nc(CC)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(COC)c1	10.1016/s0960-894x(03)00018-0
	9807200	92120	0	None	346	2	Human	8.4	pKi	=	8.4	Binding	Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells	ChEMBL	536	7	2	8	3.6	COc1cc(C)ccc1S(=O)(=O)NC(=O)[C@@H](c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(=O)O)ccc12	10.1007/s00044-004-0021-y
	CHEMBL2261359	92120	0	None	346	2	Human	8.4	pKi	=	8.4	Binding	Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells	ChEMBL	536	7	2	8	3.6	COc1cc(C)ccc1S(=O)(=O)NC(=O)[C@@H](c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(=O)O)ccc12	10.1007/s00044-004-0021-y
	51003352	64839	0	None	1230	2	Mouse	8.4	pKi	=	8.4	Binding	Displacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting	ChEMBL	1020	35	1	21	4.7	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOCCOCCOCCOCc3cn(CCOCCOCCOCCOc4cccnc4F)nn3)c2)cc1	10.1021/jm101110w
	CHEMBL1672882	64839	0	None	1230	2	Mouse	8.4	pKi	=	8.4	Binding	Displacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting	ChEMBL	1020	35	1	21	4.7	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOCCOCCOCCOCc3cn(CCOCCOCCOCCOc4cccnc4F)nn3)c2)cc1	10.1021/jm101110w
	9908909	12081	11	None	-1	3	Rat	8.3	pKi	=	8.3	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	399	6	2	5	4.5	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2N)c1C	10.1021/jm970872k
	CHEMBL106684	12081	11	None	-1	3	Rat	8.3	pKi	=	8.3	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	399	6	2	5	4.5	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2N)c1C	10.1021/jm970872k
	10811477	11590	0	None	19952	2	Human	8.3	pKi	=	8.3	Binding	Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.	ChEMBL	409	5	1	6	4.7	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncoc3C)cc2)c1C	10.1021/jm000105c
	CHEMBL104172	11590	0	None	19952	2	Human	8.3	pKi	=	8.3	Binding	Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.	ChEMBL	409	5	1	6	4.7	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncoc3C)cc2)c1C	10.1021/jm000105c
	9908909	12081	11	None	1	3	Human	8.3	pKi	=	8.3	Binding	Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.	ChEMBL	399	6	2	5	4.5	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2N)c1C	10.1021/jm000105c
	CHEMBL106684	12081	11	None	1	3	Human	8.3	pKi	=	8.3	Binding	Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.	ChEMBL	399	6	2	5	4.5	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2N)c1C	10.1021/jm000105c
	443289	7498	47	None	-2	3	Rat	7.4	pKi	=	7.4	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL		None	None	None		None	10.1021/jm970872k
	997	7498	47	None	-2	3	Rat	7.4	pKi	=	7.4	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL		None	None	None		None	10.1021/jm970872k
	CHEMBL314691	7498	47	None	-2	3	Rat	7.4	pKi	=	7.4	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL		None	None	None		None	10.1021/jm970872k
	DB12054	7498	47	None	-2	3	Rat	7.4	pKi	=	7.4	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL		None	None	None		None	10.1021/jm970872k
	9950670	50330	0	None	-	1	Rat	7.4	pKi	=	7.4	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	358	5	2	5	3.3	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2CO)c1C	10.1021/jm970872k
	CHEMBL150891	50330	0	None	-	1	Rat	7.4	pKi	=	7.4	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	358	5	2	5	3.3	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2CO)c1C	10.1021/jm970872k
	18004820	23225	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	527	9	2	7	4.7	CCCc1nc(Cl)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1016/s0960-894x(03)00018-0
	CHEMBL12333	23225	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	527	9	2	7	4.7	CCCc1nc(Cl)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1016/s0960-894x(03)00018-0
	10208527	104972	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	526	9	1	7	5.8	CCCc1nc(Cl)c(C(C)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1016/s0960-894x(03)00018-0
	CHEMBL274154	104972	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	526	9	1	7	5.8	CCCc1nc(Cl)c(C(C)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1016/s0960-894x(03)00018-0
	11795351	49623	0	None	109	2	Rat	6.4	pKi	=	6.4	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	401	6	1	4	4.8	CC(C)Cc1ccc(-c2ccccc2S(=O)(=O)Nc2ccc(Cl)nn2)cc1	10.1021/jm970872k
	CHEMBL150273	49623	0	None	109	2	Rat	6.4	pKi	=	6.4	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	401	6	1	4	4.8	CC(C)Cc1ccc(-c2ccccc2S(=O)(=O)Nc2ccc(Cl)nn2)cc1	10.1021/jm970872k
	44303148	209936	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	456	4	1	5	5.1	O=C1O[C@@](O)(c2ccc(Cl)c(Cl)c2)C(Cc2ccccc2)C1c1ccc2c(c1)OCO2	10.1021/jm990504b
	CHEMBL64200	209936	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	456	4	1	5	5.1	O=C1O[C@@](O)(c2ccc(Cl)c(Cl)c2)C(Cc2ccccc2)C1c1ccc2c(c1)OCO2	10.1021/jm990504b
	19934549	112770	0	None	-3	2	Human	4.4	pKi	=	4.4	Binding	Affinity against ET A receptorAffinity against ET A receptor	ChEMBL	439	6	2	3	5.4	CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(Cc3c[nH]c4ccccc34)ccc21	10.1016/0960-894X(95)00019-P
	CHEMBL313184	112770	0	None	-3	2	Human	4.4	pKi	=	4.4	Binding	Affinity against ET A receptorAffinity against ET A receptor	ChEMBL	439	6	2	3	5.4	CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(Cc3c[nH]c4ccccc34)ccc21	10.1016/0960-894X(95)00019-P
	10280531	169710	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	541	10	2	7	5.1	CCCCc1nc(Cl)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1016/s0960-894x(03)00018-0
	CHEMBL417429	169710	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	541	10	2	7	5.1	CCCCc1nc(Cl)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1016/s0960-894x(03)00018-0
	10528341	21349	0	None	95	2	Rat	7.4	pKi	=	7.4	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	458	9	2	6	4.4	Cc1noc(NS(=O)(=O)c2cccc(OCC(=O)O)c2-c2ccc(CC(C)C)cc2)c1C	10.1021/jm970872k
	CHEMBL1204523	21349	0	None	95	2	Rat	7.4	pKi	=	7.4	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	458	9	2	6	4.4	Cc1noc(NS(=O)(=O)c2cccc(OCC(=O)O)c2-c2ccc(CC(C)C)cc2)c1C	10.1021/jm970872k
	CHEMBL149152	21349	0	None	95	2	Rat	7.4	pKi	=	7.4	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	458	9	2	6	4.4	Cc1noc(NS(=O)(=O)c2cccc(OCC(=O)O)c2-c2ccc(CC(C)C)cc2)c1C	10.1021/jm970872k
	155543936	180014	0	None	-218776	2	Rat	5.4	pKi	=	5.4	Binding	Compound was evaluated for the binding affinity to Endothelin A receptor in the rat atriumCompound was evaluated for the binding affinity to Endothelin A receptor in the rat atrium	ChEMBL	2514	48	34	38	-9.8	CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CC(N)=O)NC2=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1021/jm00087a001
	CHEMBL4524100	180014	0	None	-218776	2	Rat	5.4	pKi	=	5.4	Binding	Compound was evaluated for the binding affinity to Endothelin A receptor in the rat atriumCompound was evaluated for the binding affinity to Endothelin A receptor in the rat atrium	ChEMBL	2514	48	34	38	-9.8	CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CC(N)=O)NC2=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1021/jm00087a001
	10407051	107169	0	None	5	2	Human	6.4	pKi	=	6.4	Binding	Inhibition of [125I]ET1 binding to cloned human ET-A receptorInhibition of [125I]ET1 binding to cloned human ET-A receptor	ChEMBL	374	5	1	3	4.7	COc1ccc([C@H]2c3ccccc3[C@@H](c3ccc(OC)cc3)[C@@H]2C(=O)O)cc1	10.1021/jm00037a003
	CHEMBL290026	107169	0	None	5	2	Human	6.4	pKi	=	6.4	Binding	Inhibition of [125I]ET1 binding to cloned human ET-A receptorInhibition of [125I]ET1 binding to cloned human ET-A receptor	ChEMBL	374	5	1	3	4.7	COc1ccc([C@H]2c3ccccc3[C@@H](c3ccc(OC)cc3)[C@@H]2C(=O)O)cc1	10.1021/jm00037a003
	10647471	49099	0	None	125	2	Rat	7.4	pKi	=	7.4	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	456	7	3	5	4.7	CNC(=O)Nc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C	10.1021/jm970872k
	CHEMBL149818	49099	0	None	125	2	Rat	7.4	pKi	=	7.4	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	456	7	3	5	4.7	CNC(=O)Nc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C	10.1021/jm970872k
	10045790	148430	0	None	17	2	Human	7.4	pKi	=	7.4	Binding	Inhibition of [125I]ET1 binding to cloned human ET-A receptorInhibition of [125I]ET1 binding to cloned human ET-A receptor	ChEMBL	388	4	1	4	4.4	COc1ccc([C@H]2c3ccccc3[C@@H](c3ccc4c(c3)OCO4)[C@@H]2C(=O)O)cc1	10.1021/jm00037a003
	CHEMBL38537	148430	0	None	17	2	Human	7.4	pKi	=	7.4	Binding	Inhibition of [125I]ET1 binding to cloned human ET-A receptorInhibition of [125I]ET1 binding to cloned human ET-A receptor	ChEMBL	388	4	1	4	4.4	COc1ccc([C@H]2c3ccccc3[C@@H](c3ccc4c(c3)OCO4)[C@@H]2C(=O)O)cc1	10.1021/jm00037a003
	22103589	47950	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.	ChEMBL	394	5	2	5	4.1	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncc[nH]3)cc2)c1C	10.1016/s0960-894x(01)00791-0
	CHEMBL148855	47950	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.	ChEMBL	394	5	2	5	4.1	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncc[nH]3)cc2)c1C	10.1016/s0960-894x(01)00791-0
	3887	8853	45	None	-436	4	Pig	6.4	pKi	=	6.4	Binding	Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated	ChEMBL		None	None	None		None	10.1016/0960-894X(96)00421-0
	5311192	8853	45	None	-436	4	Pig	6.4	pKi	=	6.4	Binding	Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated	ChEMBL		None	None	None		None	10.1016/0960-894X(96)00421-0
	CHEMBL72410	8853	45	None	-436	4	Pig	6.4	pKi	=	6.4	Binding	Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated	ChEMBL		None	None	None		None	10.1016/0960-894X(96)00421-0
	3887	8853	45	None	-436	4	Human	6.4	pKi	=	6.4	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL		None	None	None		None	10.1016/s0960-894x(98)00387-4
	5311192	8853	45	None	-436	4	Human	6.4	pKi	=	6.4	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL		None	None	None		None	10.1016/s0960-894x(98)00387-4
	CHEMBL72410	8853	45	None	-436	4	Human	6.4	pKi	=	6.4	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL		None	None	None		None	10.1016/s0960-894x(98)00387-4
	10499516	127756	0	None	-	1	Rat	5.4	pKi	=	5.4	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	372	5	2	5	3.5	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(C(=O)O)cc2)c1C	10.1021/jm970872k
	CHEMBL356220	127756	0	None	-	1	Rat	5.4	pKi	=	5.4	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	372	5	2	5	3.5	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(C(=O)O)cc2)c1C	10.1021/jm970872k
	44311701	174935	1	None	-213	2	Human	7.4	pKi	=	7.4	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	564	10	3	5	4.9	Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccno3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1	10.1016/s0960-894x(98)00387-4
	CHEMBL433106	174935	1	None	-213	2	Human	7.4	pKi	=	7.4	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	564	10	3	5	4.9	Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccno3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1	10.1016/s0960-894x(98)00387-4
	10280562	22287	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	542	9	1	8	5.4	CCCc1nc(Cl)c(C(=O)OC)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1016/s0960-894x(03)00018-0
	CHEMBL12172	22287	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	542	9	1	8	5.4	CCCc1nc(Cl)c(C(=O)OC)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1016/s0960-894x(03)00018-0
	10516176	211979	3	None	-	1	Rat	5.3	pKi	=	5.3	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	270	3	1	4	2.2	Cc1noc(NS(=O)(=O)c2ccccc2F)c1C	10.1021/jm970872k
	CHEMBL78499	211979	3	None	-	1	Rat	5.3	pKi	=	5.3	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	270	3	1	4	2.2	Cc1noc(NS(=O)(=O)c2ccccc2F)c1C	10.1021/jm970872k
	10793160	105182	0	None	-2	2	Human	7.3	pKi	=	7.3	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	570	13	1	8	5.6	COc1cc(/C=C/COC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc(OC)c1OC	10.1021/jm9910425
	CHEMBL275471	105182	0	None	-2	2	Human	7.3	pKi	=	7.3	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	570	13	1	8	5.6	COc1cc(/C=C/COC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc(OC)c1OC	10.1021/jm9910425
	122272	103872	31	None	1	2	Human	7.3	pKi	=	7.3	Binding	Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C	10.1021/jm9505369
	CHEMBL267458	103872	31	None	1	2	Human	7.3	pKi	=	7.3	Binding	Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C	10.1021/jm9505369
	122272	103872	31	None	1	2	Human	7.3	pKi	=	7.3	Binding	Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C	10.1021/jm980217s
	CHEMBL267458	103872	31	None	1	2	Human	7.3	pKi	=	7.3	Binding	Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C	10.1021/jm980217s
	10810897	128271	0	None	3801	2	Rat	8.3	pKi	=	8.3	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	398	6	1	4	5.3	Cc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C	10.1021/jm970872k
	CHEMBL358254	128271	0	None	3801	2	Rat	8.3	pKi	=	8.3	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	398	6	1	4	5.3	Cc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C	10.1021/jm970872k
	10621010	171641	0	None	186	2	Rat	8.3	pKi	=	8.3	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	400	6	2	5	4.7	Cc1noc(NS(=O)(=O)c2cccc(O)c2-c2ccc(CC(C)C)cc2)c1C	10.1021/jm970872k
	CHEMBL421955	171641	0	None	186	2	Rat	8.3	pKi	=	8.3	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	400	6	2	5	4.7	Cc1noc(NS(=O)(=O)c2cccc(O)c2-c2ccc(CC(C)C)cc2)c1C	10.1021/jm970872k
	9871837	21975	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	535	10	2	7	4.9	CCCc1nc(CC)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(C)c1	10.1016/s0960-894x(03)00018-0
	CHEMBL12106	21975	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	535	10	2	7	4.9	CCCc1nc(CC)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(C)c1	10.1016/s0960-894x(03)00018-0
	9985001	103784	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	549	10	2	7	5.2	CCCc1nc(CC)c(C(=O)NC)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(C)c1	10.1016/s0960-894x(03)00018-0
	CHEMBL266628	103784	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	549	10	2	7	5.2	CCCc1nc(CC)c(C(=O)NC)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(C)c1	10.1016/s0960-894x(03)00018-0
	44311772	109810	0	None	-10	2	Human	8.3	pKi	=	8.3	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	628	15	2	8	4.1	CCCCS(=O)(=O)NC(=O)C(CCSC)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1	10.1016/s0960-894x(98)00387-4
	CHEMBL307045	109810	0	None	-10	2	Human	8.3	pKi	=	8.3	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	628	15	2	8	4.1	CCCCS(=O)(=O)NC(=O)C(CCSC)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1	10.1016/s0960-894x(98)00387-4
	44311838	211397	0	None	-13	2	Human	8.3	pKi	=	8.3	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	655	12	3	7	4.3	CCS(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1	10.1016/s0960-894x(98)00387-4
	CHEMBL73373	211397	0	None	-13	2	Human	8.3	pKi	=	8.3	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	655	12	3	7	4.3	CCS(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1	10.1016/s0960-894x(98)00387-4
	44311850	109968	0	None	-10	2	Human	8.3	pKi	=	8.3	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	717	13	3	7	5.5	Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccno3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NS(=O)(=O)Cc2ccccc2)c1	10.1016/s0960-894x(98)00387-4
	CHEMBL308269	109968	0	None	-10	2	Human	8.3	pKi	=	8.3	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	717	13	3	7	5.5	Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccno3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NS(=O)(=O)Cc2ccccc2)c1	10.1016/s0960-894x(98)00387-4
	44311773	211457	0	None	-7	2	Human	8.3	pKi	=	8.3	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	582	13	2	7	3.8	CCCCS(=O)(=O)NC(=O)C(CC)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1	10.1016/s0960-894x(98)00387-4
	CHEMBL73835	211457	0	None	-7	2	Human	8.3	pKi	=	8.3	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	582	13	2	7	3.8	CCCCS(=O)(=O)NC(=O)C(CC)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1	10.1016/s0960-894x(98)00387-4
	22103743	49610	0	None	9332	2	Human	8.3	pKi	=	8.3	Binding	Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.	ChEMBL	411	5	1	6	4.9	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3nccs3)cc2)c1C	10.1016/s0960-894x(01)00791-0
	CHEMBL150260	49610	0	None	9332	2	Human	8.3	pKi	=	8.3	Binding	Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.	ChEMBL	411	5	1	6	4.9	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3nccs3)cc2)c1C	10.1016/s0960-894x(01)00791-0
	10667808	126069	0	None	338	2	Rat	7.3	pKi	=	7.3	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	385	6	2	5	4.6	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(NC(C)C)cc2)c1C	10.1021/jm970872k
	CHEMBL343867	126069	0	None	338	2	Rat	7.3	pKi	=	7.3	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	385	6	2	5	4.6	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(NC(C)C)cc2)c1C	10.1021/jm970872k
	10761688	126633	0	None	380	2	Rat	7.3	pKi	=	7.3	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	370	5	1	4	4.9	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(C(C)C)cc2)c1C	10.1021/jm970872k
	CHEMBL348700	126633	0	None	380	2	Rat	7.3	pKi	=	7.3	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	370	5	1	4	4.9	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(C(C)C)cc2)c1C	10.1021/jm970872k
	10501166	48652	0	None	47	2	Rat	6.3	pKi	=	6.3	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	400	6	2	5	4.7	Cc1noc(NS(=O)(=O)c2cc(O)ccc2-c2ccc(CC(C)C)cc2)c1C	10.1021/jm970872k
	CHEMBL149391	48652	0	None	47	2	Rat	6.3	pKi	=	6.3	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	400	6	2	5	4.7	Cc1noc(NS(=O)(=O)c2cc(O)ccc2-c2ccc(CC(C)C)cc2)c1C	10.1021/jm970872k
	44314444	168501	0	None	-457	2	Pig	5.3	pKi	=	5.3	Binding	Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated	ChEMBL	1470	45	18	17	-0.5	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(96)00421-0
	CHEMBL413604	168501	0	None	-457	2	Pig	5.3	pKi	=	5.3	Binding	Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated	ChEMBL	1470	45	18	17	-0.5	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(96)00421-0
	9799352	127885	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.	ChEMBL	367	4	2	4	4.2	Cc1noc(NS(=O)(=O)c2ccccc2-c2c[nH]c3ccccc23)c1C	10.1021/jm970872k
	CHEMBL357331	127885	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.	ChEMBL	367	4	2	4	4.2	Cc1noc(NS(=O)(=O)c2ccccc2-c2c[nH]c3ccccc23)c1C	10.1021/jm970872k
	10690608	127837	0	None	112	2	Rat	7.3	pKi	=	7.3	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	371	5	1	5	3.8	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(N(C)C)cc2)c1C	10.1021/jm970872k
	CHEMBL356901	127837	0	None	112	2	Rat	7.3	pKi	=	7.3	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	371	5	1	5	3.8	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(N(C)C)cc2)c1C	10.1021/jm970872k
	44311700	109599	0	None	-234	2	Human	7.3	pKi	=	7.3	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	579	10	3	4	6.0	Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccsc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1	10.1016/s0960-894x(98)00387-4
	CHEMBL305462	109599	0	None	-234	2	Human	7.3	pKi	=	7.3	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	579	10	3	4	6.0	Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccsc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1	10.1016/s0960-894x(98)00387-4
	122272	103872	31	None	-1	2	Rat	7.3	pKi	=	7.3	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C	10.1021/jm970872k
	CHEMBL267458	103872	31	None	-1	2	Rat	7.3	pKi	=	7.3	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C	10.1021/jm970872k
	10521258	128074	0	None	416	2	Rat	7.3	pKi	=	7.3	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	342	4	1	4	4.1	Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1021/jm970872k
	CHEMBL358020	128074	0	None	416	2	Rat	7.3	pKi	=	7.3	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	342	4	1	4	4.1	Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1021/jm970872k
	122272	103872	31	None	1	2	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards ET1 receptor was determined in A10 cellsBinding affinity towards ET1 receptor was determined in A10 cells	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C	10.1021/jm00029a001
	CHEMBL267458	103872	31	None	1	2	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards ET1 receptor was determined in A10 cellsBinding affinity towards ET1 receptor was determined in A10 cells	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C	10.1021/jm00029a001
	10166104	21949	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	549	10	1	7	5.2	CCCc1nc(CC)c(C(=O)N(C)C)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1016/s0960-894x(03)00018-0
	CHEMBL12102	21949	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	549	10	1	7	5.2	CCCc1nc(CC)c(C(=O)N(C)C)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1016/s0960-894x(03)00018-0
	17979745	24691	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	521	10	2	7	4.6	CCCc1nc(CC)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1016/s0960-894x(03)00018-0
	CHEMBL12592	24691	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	521	10	2	7	4.6	CCCc1nc(CC)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1	10.1016/s0960-894x(03)00018-0
	122272	103872	31	None	1	2	Human	7.3	pKi	=	7.3	Binding	Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C	10.1021/jm000105c
	CHEMBL267458	103872	31	None	1	2	Human	7.3	pKi	=	7.3	Binding	Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.	ChEMBL	345	4	1	5	3.3	Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C	10.1021/jm000105c
	10718666	128299	0	None	3	2	Rat	6.3	pKi	=	6.3	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	457	9	3	6	4.5	Cc1noc(NS(=O)(=O)c2ccc(NCC(=O)O)cc2-c2ccc(CC(C)C)cc2)c1C	10.1021/jm970872k
	CHEMBL358461	128299	0	None	3	2	Rat	6.3	pKi	=	6.3	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	457	9	3	6	4.5	Cc1noc(NS(=O)(=O)c2ccc(NCC(=O)O)cc2-c2ccc(CC(C)C)cc2)c1C	10.1021/jm970872k
	10670536	127865	0	None	-	1	Rat	6.3	pKi	=	6.3	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	435	6	1	6	3.0	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(S(=O)(=O)N(C)C)cc2)c1C	10.1021/jm970872k
	CHEMBL357099	127865	0	None	-	1	Rat	6.3	pKi	=	6.3	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	435	6	1	6	3.0	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(S(=O)(=O)N(C)C)cc2)c1C	10.1021/jm970872k
	10088869	151134	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Inhibition of [125I]ET1 binding to cloned human Endothelin A receptorInhibition of [125I]ET1 binding to cloned human Endothelin A receptor	ChEMBL	344	4	1	2	4.7	COc1ccc([C@H]2c3ccccc3[C@@H](c3ccccc3)[C@@H]2C(=O)O)cc1	10.1021/jm00037a003
	CHEMBL39057	151134	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Inhibition of [125I]ET1 binding to cloned human Endothelin A receptorInhibition of [125I]ET1 binding to cloned human Endothelin A receptor	ChEMBL	344	4	1	2	4.7	COc1ccc([C@H]2c3ccccc3[C@@H](c3ccccc3)[C@@H]2C(=O)O)cc1	10.1021/jm00037a003
	10839202	126014	0	None	6	2	Rat	5.2	pKi	=	5.2	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	503	8	2	5	6.2	Cc1noc(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3)cc2-c2ccc(CC(C)C)cc2)c1C	10.1021/jm970872k
	CHEMBL343477	126014	0	None	6	2	Rat	5.2	pKi	=	5.2	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	503	8	2	5	6.2	Cc1noc(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3)cc2-c2ccc(CC(C)C)cc2)c1C	10.1021/jm970872k
	10563752	47742	2	None	-	1	Rat	5.2	pKi	=	5.2	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	267	3	2	5	1.7	Cc1noc(NS(=O)(=O)c2ccccc2N)c1C	10.1021/jm970872k
	CHEMBL148702	47742	2	None	-	1	Rat	5.2	pKi	=	5.2	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	267	3	2	5	1.7	Cc1noc(NS(=O)(=O)c2ccccc2N)c1C	10.1021/jm970872k
	9953358	101575	13	None	102	2	Human	8.2	pKi	=	8.2	Binding	Binding affinity against human Endothelin A receptor; orally active in vivo at 30 mg/kg, poBinding affinity against human Endothelin A receptor; orally active in vivo at 30 mg/kg, po	ChEMBL	410	9	1	7	2.9	COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1	10.1021/jm030480f
	CHEMBL25344	101575	13	None	102	2	Human	8.2	pKi	=	8.2	Binding	Binding affinity against human Endothelin A receptor; orally active in vivo at 30 mg/kg, poBinding affinity against human Endothelin A receptor; orally active in vivo at 30 mg/kg, po	ChEMBL	410	9	1	7	2.9	COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1	10.1021/jm030480f
	44311803	211333	0	None	-26	2	Human	8.2	pKi	=	8.2	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	699	15	3	8	4.3	CCOCCS(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1	10.1016/s0960-894x(98)00387-4
	CHEMBL72924	211333	0	None	-26	2	Human	8.2	pKi	=	8.2	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	699	15	3	8	4.3	CCOCCS(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1	10.1016/s0960-894x(98)00387-4
	177236	8107	45	None	-2	3	Rat	8.2	pKi	=	8.2	Binding	Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor	ChEMBL	410	9	1	7	2.9	COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1	10.1021/jm030528p
	3508	8107	45	None	-2	3	Rat	8.2	pKi	=	8.2	Binding	Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor	ChEMBL	410	9	1	7	2.9	COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1	10.1021/jm030528p
	CHEMBL23261	8107	45	None	-2	3	Rat	8.2	pKi	=	8.2	Binding	Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor	ChEMBL	410	9	1	7	2.9	COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1	10.1021/jm030528p
	DB04883	8107	45	None	-2	3	Rat	8.2	pKi	=	8.2	Binding	Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor	ChEMBL	410	9	1	7	2.9	COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1	10.1021/jm030528p
	9953358	101575	13	None	102	2	Human	8.2	pKi	=	8.2	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	410	9	1	7	2.9	COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1	10.1021/jm960274q
	CHEMBL25344	101575	13	None	102	2	Human	8.2	pKi	=	8.2	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	410	9	1	7	2.9	COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1	10.1021/jm960274q
	177236	8107	45	None	2	3	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	410	9	1	7	2.9	COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1	10.1016/j.bmcl.2016.06.014
	3508	8107	45	None	2	3	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	410	9	1	7	2.9	COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1	10.1016/j.bmcl.2016.06.014
	CHEMBL23261	8107	45	None	2	3	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	410	9	1	7	2.9	COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1	10.1016/j.bmcl.2016.06.014
	DB04883	8107	45	None	2	3	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	ChEMBL	410	9	1	7	2.9	COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1	10.1016/j.bmcl.2016.06.014
	11006149	107875	0	None	380	2	Human	8.2	pKi	=	8.2	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	550	8	1	7	6.2	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C(=O)C(C)(C)C)C(C)C)c1C	10.1021/jm020289q
	CHEMBL29502	107875	0	None	380	2	Human	8.2	pKi	=	8.2	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	550	8	1	7	6.2	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C(=O)C(C)(C)C)C(C)C)c1C	10.1021/jm020289q
	10648996	11126	0	None	3	2	Human	8.2	pKi	=	8.2	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	498	11	1	6	5.1	COc1ccc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1	10.1021/jm9910425
	CHEMBL101069	11126	0	None	3	2	Human	8.2	pKi	=	8.2	Binding	Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells	ChEMBL	498	11	1	6	5.1	COc1ccc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1	10.1021/jm9910425
	18660520	46338	0	None	3548	2	Human	8.2	pKi	=	8.2	Binding	Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.	ChEMBL	406	5	1	6	4.2	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3cnccn3)cc2)c1C	10.1016/s0960-894x(01)00791-0
	CHEMBL147340	46338	0	None	3548	2	Human	8.2	pKi	=	8.2	Binding	Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.	ChEMBL	406	5	1	6	4.2	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3cnccn3)cc2)c1C	10.1016/s0960-894x(01)00791-0
	10741151	49841	0	None	223	2	Rat	8.2	pKi	=	8.2	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	427	8	2	5	5.4	CCNc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C	10.1021/jm970872k
	CHEMBL150474	49841	0	None	223	2	Rat	8.2	pKi	=	8.2	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	427	8	2	5	5.4	CCNc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C	10.1021/jm970872k
	10503421	126287	0	None	245	2	Rat	8.2	pKi	=	8.2	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	443	9	3	6	4.4	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2NCCO)c1C	10.1021/jm970872k
	CHEMBL345542	126287	0	None	245	2	Rat	8.2	pKi	=	8.2	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	443	9	3	6	4.4	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2NCCO)c1C	10.1021/jm970872k
	104865	7493	99	None	1	4	Human	8.2	pKi	=	8.2	Binding	Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm970101g
	3494	7493	99	None	1	4	Human	8.2	pKi	=	8.2	Binding	Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm970101g
	392	7493	99	None	1	4	Human	8.2	pKi	=	8.2	Binding	Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm970101g
	CHEMBL957	7493	99	None	1	4	Human	8.2	pKi	=	8.2	Binding	Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm970101g
	DB00559	7493	99	None	1	4	Human	8.2	pKi	=	8.2	Binding	Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm970101g
	104865	7493	99	None	-1	4	Rat	8.2	pKi	=	8.2	Binding	Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm030528p
	3494	7493	99	None	-1	4	Rat	8.2	pKi	=	8.2	Binding	Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm030528p
	392	7493	99	None	-1	4	Rat	8.2	pKi	=	8.2	Binding	Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm030528p
	CHEMBL957	7493	99	None	-1	4	Rat	8.2	pKi	=	8.2	Binding	Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm030528p
	DB00559	7493	99	None	-1	4	Rat	8.2	pKi	=	8.2	Binding	Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm030528p
	44265871	173697	0	None	53	2	Human	8.2	pKi	=	8.2	Binding	Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells	ChEMBL	547	10	2	8	4.6	COc1ccccc1Cc1c(CCCO)nc(-c2ncccn2)nc1NS(=O)(=O)c1ccc(C(C)(C)C)cc1	10.1021/jm9505369
	CHEMBL428661	173697	0	None	53	2	Human	8.2	pKi	=	8.2	Binding	Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells	ChEMBL	547	10	2	8	4.6	COc1ccccc1Cc1c(CCCO)nc(-c2ncccn2)nc1NS(=O)(=O)c1ccc(C(C)(C)C)cc1	10.1021/jm9505369
	22103787	47766	0	None	1380	2	Human	8.2	pKi	=	8.2	Binding	Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.	ChEMBL	394	5	1	6	3.9	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-n3cccn3)cc2)c1C	10.1016/s0960-894x(01)00791-0
	CHEMBL148719	47766	0	None	1380	2	Human	8.2	pKi	=	8.2	Binding	Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.	ChEMBL	394	5	1	6	3.9	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-n3cccn3)cc2)c1C	10.1016/s0960-894x(01)00791-0
	44311989	211350	0	None	-1	2	Human	8.2	pKi	=	8.2	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	610	14	2	7	4.4	CCCCS(=O)(=O)NC(=O)C(NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)CC	10.1016/s0960-894x(98)00387-4
	CHEMBL73042	211350	0	None	-1	2	Human	8.2	pKi	=	8.2	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	610	14	2	7	4.4	CCCCS(=O)(=O)NC(=O)C(NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)CC	10.1016/s0960-894x(98)00387-4
	10620958	48483	0	None	331	2	Rat	7.2	pKi	=	7.2	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	399	6	1	5	4.6	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(N(C)C(C)C)cc2)c1C	10.1021/jm970872k
	CHEMBL149241	48483	0	None	331	2	Rat	7.2	pKi	=	7.2	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	399	6	1	5	4.6	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(N(C)C(C)C)cc2)c1C	10.1021/jm970872k
	10803738	125766	0	None	-	1	Rat	6.2	pKi	=	6.2	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	294	4	1	4	3.2	Cc1noc(NS(=O)(=O)c2ccccc2C(C)C)c1C	10.1021/jm970872k
	CHEMBL342498	125766	0	None	-	1	Rat	6.2	pKi	=	6.2	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	294	4	1	4	3.2	Cc1noc(NS(=O)(=O)c2ccccc2C(C)C)c1C	10.1021/jm970872k
	5472495	193412	47	None	-	1	Human	5.2	pKi	=	5.2	Binding	DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)	ChEMBL	372	4	1	3	4.0	CC1=C(CC(=O)O)c2cc(F)ccc2/C1=C\c1ccc(S(C)(=O)=O)cc1	nan
	CHEMBL488025	193412	47	None	-	1	Human	5.2	pKi	=	5.2	Binding	DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)	ChEMBL	372	4	1	3	4.0	CC1=C(CC(=O)O)c2cc(F)ccc2/C1=C\c1ccc(S(C)(=O)=O)cc1	nan
	10691439	51317	0	None	245	2	Rat	7.2	pKi	=	7.2	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	384	4	1	4	5.1	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(C(C)(C)C)cc2)c1C	10.1021/jm970872k
	CHEMBL151971	51317	0	None	245	2	Rat	7.2	pKi	=	7.2	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	384	4	1	4	5.1	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(C(C)(C)C)cc2)c1C	10.1021/jm970872k
	10783588	172461	0	None	-	1	Rat	7.2	pKi	=	7.2	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	343	4	2	5	3.3	Cc1noc(NS(=O)(=O)c2ccccc2-c2cccc(N)c2)c1C	10.1021/jm970872k
	CHEMBL424504	172461	0	None	-	1	Rat	7.2	pKi	=	7.2	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	343	4	2	5	3.3	Cc1noc(NS(=O)(=O)c2ccccc2-c2cccc(N)c2)c1C	10.1021/jm970872k
	44314783	173228	0	None	-7943	2	Pig	6.2	pKi	=	6.2	Binding	Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated	ChEMBL	1576	47	19	18	0.8	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(96)00421-0
	77282213	173228	0	None	-7943	2	Pig	6.2	pKi	=	6.2	Binding	Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated	ChEMBL	1576	47	19	18	0.8	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(96)00421-0
	CHEMBL427778	173228	0	None	-7943	2	Pig	6.2	pKi	=	6.2	Binding	Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated	ChEMBL	1576	47	19	18	0.8	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(96)00421-0
	5310990	173609	11	None	-	1	Human	7.2	pKi	=	7.2	Binding	Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells	ChEMBL	510	12	1	6	4.7	CCCCN(CCCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	CHEMBL428504	173609	11	None	-	1	Human	7.2	pKi	=	7.2	Binding	Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells	ChEMBL	510	12	1	6	4.7	CCCCN(CCCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1	10.1021/jm9505369
	10600059	51293	0	None	-	1	Rat	5.2	pKi	=	5.2	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	460	8	1	4	6.2	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2)c1Cc1ccccc1	10.1021/jm970872k
	CHEMBL151954	51293	0	None	-	1	Rat	5.2	pKi	=	5.2	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	460	8	1	4	6.2	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2)c1Cc1ccccc1	10.1021/jm970872k
	9830098	109807	0	None	-5	2	Human	5.2	pKi	=	5.2	Binding	Compound was tested for the binding affinity against Endothelin A receptorCompound was tested for the binding affinity against Endothelin A receptor	ChEMBL	596	13	2	7	4.0	CCCCS(=O)(=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)C	10.1016/s0960-894x(98)00388-6
	CHEMBL307033	109807	0	None	-5	2	Human	5.2	pKi	=	5.2	Binding	Compound was tested for the binding affinity against Endothelin A receptorCompound was tested for the binding affinity against Endothelin A receptor	ChEMBL	596	13	2	7	4.0	CCCCS(=O)(=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)C	10.1016/s0960-894x(98)00388-6
	22574723	22710	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	549	11	2	7	5.2	CCCc1nc(CC)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(CC)c1	10.1016/s0960-894x(03)00018-0
	CHEMBL12233	22710	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	549	11	2	7	5.2	CCCc1nc(CC)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(CC)c1	10.1016/s0960-894x(03)00018-0
	20747575	105200	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	579	12	2	8	5.0	CCCc1nc(CC)c(C(=O)NC)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(COC)c1	10.1016/s0960-894x(03)00018-0
	CHEMBL275545	105200	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	579	12	2	8	5.0	CCCc1nc(CC)c(C(=O)NC)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(COC)c1	10.1016/s0960-894x(03)00018-0
	10693607	109483	0	None	354	2	Human	8.2	pKi	=	8.2	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	424	10	1	7	3.3	CCOC(c1ccccc1)(c1ccccc1)C(Oc1nc(OC)cc(OC)n1)C(=O)O	10.1021/jm960274q
	CHEMBL304778	109483	0	None	354	2	Human	8.2	pKi	=	8.2	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	424	10	1	7	3.3	CCOC(c1ccccc1)(c1ccccc1)C(Oc1nc(OC)cc(OC)n1)C(=O)O	10.1021/jm960274q
	51002601	64842	0	None	123	2	Mouse	8.1	pKi	=	8.1	Binding	Displacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting	ChEMBL	906	24	2	17	4.2	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOCCOCCOCCn3cc(CNS(=O)(=O)c4ccc(F)cc4)nn3)c2)cc1	10.1021/jm101110w
	CHEMBL1672885	64842	0	None	123	2	Mouse	8.1	pKi	=	8.1	Binding	Displacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting	ChEMBL	906	24	2	17	4.2	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOCCOCCOCCn3cc(CNS(=O)(=O)c4ccc(F)cc4)nn3)c2)cc1	10.1021/jm101110w
	51002602	64843	0	None	812	2	Mouse	8.1	pKi	=	8.1	Binding	Displacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting	ChEMBL	751	21	1	15	4.0	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOCCOCCOCCn3cc(CF)nn3)c2)cc1	10.1021/jm101110w
	CHEMBL1672886	64843	0	None	812	2	Mouse	8.1	pKi	=	8.1	Binding	Displacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETA receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting	ChEMBL	751	21	1	15	4.0	COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOCCOCCOCCn3cc(CF)nn3)c2)cc1	10.1021/jm101110w
	10549472	12109	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.	ChEMBL	409	5	1	6	4.7	Cc1nc(-c2ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)cc2)co1	10.1021/jm000105c
	CHEMBL106846	12109	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.	ChEMBL	409	5	1	6	4.7	Cc1nc(-c2ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)cc2)co1	10.1021/jm000105c
	10734431	50105	0	None	-	1	Rat	6.2	pKi	=	6.2	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	320	3	1	4	3.1	Cc1noc(NS(=O)(=O)c2ccccc2C(F)(F)F)c1C	10.1021/jm970872k
	CHEMBL150697	50105	0	None	-	1	Rat	6.2	pKi	=	6.2	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	320	3	1	4	3.1	Cc1noc(NS(=O)(=O)c2ccccc2C(F)(F)F)c1C	10.1021/jm970872k
	20747572	23249	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	555	10	2	7	5.3	CCCc1nc(CC)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(Cl)c1	10.1016/s0960-894x(03)00018-0
	CHEMBL12348	23249	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	555	10	2	7	5.3	CCCc1nc(CC)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(Cl)c1	10.1016/s0960-894x(03)00018-0
	19934546	212993	0	None	8	2	Human	5.2	pKi	=	5.2	Binding	Affinity against ET A receptorAffinity against ET A receptor	ChEMBL	466	7	1	4	6.0	CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(OCc3cccc4ccccc34)ccc21	10.1016/0960-894X(95)00019-P
	CHEMBL86581	212993	0	None	8	2	Human	5.2	pKi	=	5.2	Binding	Affinity against ET A receptorAffinity against ET A receptor	ChEMBL	466	7	1	4	6.0	CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(OCc3cccc4ccccc34)ccc21	10.1016/0960-894X(95)00019-P
	10718053	50887	0	None	5	2	Rat	5.1	pKi	=	5.1	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	442	8	1	6	4.8	CCOC(=O)c1c(C)noc1NS(=O)(=O)c1ccccc1-c1ccc(CC(C)C)cc1	10.1021/jm970872k
	CHEMBL151525	50887	0	None	5	2	Rat	5.1	pKi	=	5.1	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	442	8	1	6	4.8	CCOC(=O)c1c(C)noc1NS(=O)(=O)c1ccccc1-c1ccc(CC(C)C)cc1	10.1021/jm970872k
	10597897	47949	0	None	724	2	Rat	7.1	pKi	=	7.1	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	414	7	1	5	5.0	COc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C	10.1021/jm970872k
	CHEMBL148853	47949	0	None	724	2	Rat	7.1	pKi	=	7.1	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	414	7	1	5	5.0	COc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C	10.1021/jm970872k
	10668703	171962	0	None	1230	2	Rat	8.1	pKi	=	8.1	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	400	6	2	5	4.7	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2O)c1C	10.1021/jm970872k
	CHEMBL422851	171962	0	None	1230	2	Rat	8.1	pKi	=	8.1	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	400	6	2	5	4.7	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2O)c1C	10.1021/jm970872k
	44311763	211228	0	None	-6	2	Human	8.1	pKi	=	8.1	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	610	14	2	7	4.4	CCCCS(=O)(=O)NC(=O)C(CC(C)C)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1	10.1016/s0960-894x(98)00387-4
	CHEMBL72217	211228	0	None	-6	2	Human	8.1	pKi	=	8.1	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	610	14	2	7	4.4	CCCCS(=O)(=O)NC(=O)C(CC(C)C)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1	10.1016/s0960-894x(98)00387-4
	22574645	24565	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	597	14	2	8	5.1	CCCc1nc(CC)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(COCCF)c1	10.1016/s0960-894x(03)00018-0
	CHEMBL12588	24565	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	ChEMBL	597	14	2	8	5.1	CCCc1nc(CC)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(COCCF)c1	10.1016/s0960-894x(03)00018-0
	104865	7493	99	None	1	4	Human	8.1	pKi	=	8.1	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm020289q
	3494	7493	99	None	1	4	Human	8.1	pKi	=	8.1	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm020289q
	392	7493	99	None	1	4	Human	8.1	pKi	=	8.1	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm020289q
	CHEMBL957	7493	99	None	1	4	Human	8.1	pKi	=	8.1	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm020289q
	DB00559	7493	99	None	1	4	Human	8.1	pKi	=	8.1	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm020289q
	11071062	106043	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	494	9	1	7	5.5	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)CC(C)C)c1C	10.1021/jm020289q
	CHEMBL281869	106043	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells	ChEMBL	494	9	1	7	5.5	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)CC(C)C)c1C	10.1021/jm020289q
	44311873	211249	0	None	-2	2	Human	8.1	pKi	=	8.1	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	636	13	2	7	5.0	CCCCS(=O)(=O)NC(=O)C(NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C1CCCCC1	10.1016/s0960-894x(98)00387-4
	CHEMBL72358	211249	0	None	-2	2	Human	8.1	pKi	=	8.1	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	636	13	2	7	5.0	CCCCS(=O)(=O)NC(=O)C(NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C1CCCCC1	10.1016/s0960-894x(98)00387-4
	10548904	126288	0	None	380	2	Rat	7.1	pKi	=	7.1	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	398	7	1	4	5.3	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CCC(C)C)cc2)c1C	10.1021/jm970872k
	CHEMBL345551	126288	0	None	380	2	Rat	7.1	pKi	=	7.1	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	398	7	1	4	5.3	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CCC(C)C)cc2)c1C	10.1021/jm970872k
	10711546	212255	7	None	-	1	Rat	5.1	pKi	=	5.1	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle (Endothelin A receptor) was determined by radioligand binding assayAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle (Endothelin A receptor) was determined by radioligand binding assay	ChEMBL	330	3	1	4	2.9	Cc1noc(NS(=O)(=O)c2ccccc2Br)c1C	10.1021/jm970872k
	CHEMBL80506	212255	7	None	-	1	Rat	5.1	pKi	=	5.1	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle (Endothelin A receptor) was determined by radioligand binding assayAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle (Endothelin A receptor) was determined by radioligand binding assay	ChEMBL	330	3	1	4	2.9	Cc1noc(NS(=O)(=O)c2ccccc2Br)c1C	10.1021/jm970872k
	19934535	113752	0	None	-7	2	Human	4.1	pKi	=	4.1	Binding	Affinity against ET A receptorAffinity against ET A receptor	ChEMBL	468	6	3	4	5.0	CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(NC(=O)c3c[nH]c4ccccc34)ccc21	10.1016/0960-894X(95)00019-P
	CHEMBL315096	113752	0	None	-7	2	Human	4.1	pKi	=	4.1	Binding	Affinity against ET A receptorAffinity against ET A receptor	ChEMBL	468	6	3	4	5.0	CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(NC(=O)c3c[nH]c4ccccc34)ccc21	10.1016/0960-894X(95)00019-P
	104865	7493	99	None	1	4	Human	7.1	pKi	=	7.1	Binding	Ability to inhibit [125I]ET1 binding to human cloned endothelin A receptor expressed on CHO cellsAbility to inhibit [125I]ET1 binding to human cloned endothelin A receptor expressed on CHO cells	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm000538f
	3494	7493	99	None	1	4	Human	7.1	pKi	=	7.1	Binding	Ability to inhibit [125I]ET1 binding to human cloned endothelin A receptor expressed on CHO cellsAbility to inhibit [125I]ET1 binding to human cloned endothelin A receptor expressed on CHO cells	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm000538f
	392	7493	99	None	1	4	Human	7.1	pKi	=	7.1	Binding	Ability to inhibit [125I]ET1 binding to human cloned endothelin A receptor expressed on CHO cellsAbility to inhibit [125I]ET1 binding to human cloned endothelin A receptor expressed on CHO cells	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm000538f
	CHEMBL957	7493	99	None	1	4	Human	7.1	pKi	=	7.1	Binding	Ability to inhibit [125I]ET1 binding to human cloned endothelin A receptor expressed on CHO cellsAbility to inhibit [125I]ET1 binding to human cloned endothelin A receptor expressed on CHO cells	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm000538f
	DB00559	7493	99	None	1	4	Human	7.1	pKi	=	7.1	Binding	Ability to inhibit [125I]ET1 binding to human cloned endothelin A receptor expressed on CHO cellsAbility to inhibit [125I]ET1 binding to human cloned endothelin A receptor expressed on CHO cells	ChEMBL	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	10.1021/jm000538f
	9949368	48160	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.	ChEMBL	329	4	1	5	3.2	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccn2)c1C	10.1021/jm970872k
	CHEMBL149018	48160	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.	ChEMBL	329	4	1	5	3.2	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccn2)c1C	10.1021/jm970872k
	44320537	113928	0	None	-	1	Human	4.1	pKi	=	4.1	Binding	Affinity against ET A receptorAffinity against ET A receptor	ChEMBL	479	6	2	4	5.7	CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(NC(=O)c3cccc4ccccc34)ccc21	10.1016/0960-894X(95)00019-P
	CHEMBL316247	113928	0	None	-	1	Human	4.1	pKi	=	4.1	Binding	Affinity against ET A receptorAffinity against ET A receptor	ChEMBL	479	6	2	4	5.7	CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(NC(=O)c3cccc4ccccc34)ccc21	10.1016/0960-894X(95)00019-P
	44311810	111567	0	None	-35	2	Human	6.1	pKi	=	6.1	Binding	Compound was tested for the binding affinity against Endothelin A receptorCompound was tested for the binding affinity against Endothelin A receptor	ChEMBL	596	13	2	7	4.0	CCCCS(=O)(=O)NC(=O)[C@H](NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)C	10.1016/s0960-894x(98)00388-6
	CHEMBL310919	111567	0	None	-35	2	Human	6.1	pKi	=	6.1	Binding	Compound was tested for the binding affinity against Endothelin A receptorCompound was tested for the binding affinity against Endothelin A receptor	ChEMBL	596	13	2	7	4.0	CCCCS(=O)(=O)NC(=O)[C@H](NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)C	10.1016/s0960-894x(98)00388-6
	10814297	210308	0	None	17	2	Human	7.1	pKi	=	7.1	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	472	10	1	7	4.3	COc1cc(OC)nc(OC(C(=O)O)C(Oc2ccccc2)(c2ccccc2)c2ccccc2)n1	10.1021/jm960274q
	CHEMBL66402	210308	0	None	17	2	Human	7.1	pKi	=	7.1	Binding	Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells	ChEMBL	472	10	1	7	4.3	COc1cc(OC)nc(OC(C(=O)O)C(Oc2ccccc2)(c2ccccc2)c2ccccc2)n1	10.1021/jm960274q
	44311852	109861	0	None	-144	2	Human	7.1	pKi	=	7.1	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	579	10	3	4	6.0	Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3cccs3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1	10.1016/s0960-894x(98)00387-4
	CHEMBL307470	109861	0	None	-144	2	Human	7.1	pKi	=	7.1	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	579	10	3	4	6.0	Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3cccs3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1	10.1016/s0960-894x(98)00387-4
	9818889	127922	0	None	-	1	Human	5.1	pKi	=	5.1	Binding	Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.	ChEMBL	330	4	1	6	2.5	Cc1noc(NS(=O)(=O)c2ccccc2-c2ncccn2)c1C	10.1021/jm970872k
	CHEMBL357678	127922	0	None	-	1	Human	5.1	pKi	=	5.1	Binding	Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.	ChEMBL	330	4	1	6	2.5	Cc1noc(NS(=O)(=O)c2ccccc2-c2ncccn2)c1C	10.1021/jm970872k
	10742502	128045	0	None	134	2	Rat	7.1	pKi	=	7.1	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	457	9	3	6	4.5	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2NCC(=O)O)c1C	10.1021/jm970872k
	CHEMBL357823	128045	0	None	134	2	Rat	7.1	pKi	=	7.1	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	457	9	3	6	4.5	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2NCC(=O)O)c1C	10.1021/jm970872k
	44311858	103378	0	None	-2	2	Human	8.0	pKi	=	8.0	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	598	13	3	8	2.8	CCCCS(=O)(=O)NC(=O)C(NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)O	10.1016/s0960-894x(98)00387-4
	CHEMBL263301	103378	0	None	-2	2	Human	8.0	pKi	=	8.0	Binding	Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor	ChEMBL	598	13	3	8	2.8	CCCCS(=O)(=O)NC(=O)C(NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)O	10.1016/s0960-894x(98)00387-4
	10257882	10418	43	None	-11	2	Human	8.0	pKi	=	8.0	Binding	Binding affinity to ETA receptorBinding affinity to ETA receptor	ChEMBL	592	12	1	7	6.5	CCCCC1=NC2(C(=O)N1Cc1ccc(c(c1)COCC)c1ccccc1S(=O)(=O)Nc1noc(c1C)C)CCCC2	10.1021/jm300682j
	8448	10418	43	None	-11	2	Human	8.0	pKi	=	8.0	Binding	Binding affinity to ETA receptorBinding affinity to ETA receptor	ChEMBL	592	12	1	7	6.5	CCCCC1=NC2(C(=O)N1Cc1ccc(c(c1)COCC)c1ccccc1S(=O)(=O)Nc1noc(c1C)C)CCCC2	10.1021/jm300682j
	CHEMBL539423	10418	43	None	-11	2	Human	8.0	pKi	=	8.0	Binding	Binding affinity to ETA receptorBinding affinity to ETA receptor	ChEMBL	592	12	1	7	6.5	CCCCC1=NC2(C(=O)N1Cc1ccc(c(c1)COCC)c1ccccc1S(=O)(=O)Nc1noc(c1C)C)CCCC2	10.1021/jm300682j
	DB12548	10418	43	None	-11	2	Human	8.0	pKi	=	8.0	Binding	Binding affinity to ETA receptorBinding affinity to ETA receptor	ChEMBL	592	12	1	7	6.5	CCCCC1=NC2(C(=O)N1Cc1ccc(c(c1)COCC)c1ccccc1S(=O)(=O)Nc1noc(c1C)C)CCCC2	10.1021/jm300682j
	10257882	10418	43	None	-11	2	Human	8.0	pKi	=	8.0	Binding	Inhibitory concentration against endothelin receptor type AInhibitory concentration against endothelin receptor type A	ChEMBL	592	12	1	7	6.5	CCCCC1=NC2(C(=O)N1Cc1ccc(c(c1)COCC)c1ccccc1S(=O)(=O)Nc1noc(c1C)C)CCCC2	10.1021/jm058225d
	8448	10418	43	None	-11	2	Human	8.0	pKi	=	8.0	Binding	Inhibitory concentration against endothelin receptor type AInhibitory concentration against endothelin receptor type A	ChEMBL	592	12	1	7	6.5	CCCCC1=NC2(C(=O)N1Cc1ccc(c(c1)COCC)c1ccccc1S(=O)(=O)Nc1noc(c1C)C)CCCC2	10.1021/jm058225d
	CHEMBL539423	10418	43	None	-11	2	Human	8.0	pKi	=	8.0	Binding	Inhibitory concentration against endothelin receptor type AInhibitory concentration against endothelin receptor type A	ChEMBL	592	12	1	7	6.5	CCCCC1=NC2(C(=O)N1Cc1ccc(c(c1)COCC)c1ccccc1S(=O)(=O)Nc1noc(c1C)C)CCCC2	10.1021/jm058225d
	DB12548	10418	43	None	-11	2	Human	8.0	pKi	=	8.0	Binding	Inhibitory concentration against endothelin receptor type AInhibitory concentration against endothelin receptor type A	ChEMBL	592	12	1	7	6.5	CCCCC1=NC2(C(=O)N1Cc1ccc(c(c1)COCC)c1ccccc1S(=O)(=O)Nc1noc(c1C)C)CCCC2	10.1021/jm058225d
	9840391	111316	6	None	-	1	Rat	7.1	pKi	=	7.1	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	328	4	1	4	3.8	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2)c1C	10.1021/jm970872k
	CHEMBL310427	111316	6	None	-	1	Rat	7.1	pKi	=	7.1	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	328	4	1	4	3.8	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2)c1C	10.1021/jm970872k
	9840650	51144	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.	ChEMBL	334	4	1	5	3.8	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccsc2)c1C	10.1021/jm970872k
	CHEMBL151819	51144	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.	ChEMBL	334	4	1	5	3.8	Cc1noc(NS(=O)(=O)c2ccccc2-c2ccsc2)c1C	10.1021/jm970872k
	9927658	127997	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.	ChEMBL	334	4	1	5	3.8	Cc1noc(NS(=O)(=O)c2ccccc2-c2cccs2)c1C	10.1021/jm970872k
	CHEMBL357789	127997	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.	ChEMBL	334	4	1	5	3.8	Cc1noc(NS(=O)(=O)c2ccccc2-c2cccs2)c1C	10.1021/jm970872k
	44314820	162500	0	None	-380	2	Pig	7.0	pKi	=	7.0	Binding	Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated	ChEMBL	1518	45	18	17	1.0	CC[C@H](C)[C@H](NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(96)00421-0
	77282210	162500	0	None	-380	2	Pig	7.0	pKi	=	7.0	Binding	Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated	ChEMBL	1518	45	18	17	1.0	CC[C@H](C)[C@H](NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(96)00421-0
	CHEMBL405377	162500	0	None	-380	2	Pig	7.0	pKi	=	7.0	Binding	Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated	ChEMBL	1518	45	18	17	1.0	CC[C@H](C)[C@H](NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC	10.1016/0960-894X(96)00421-0
	10737908	48225	0	None	102	2	Rat	6.0	pKi	=	6.0	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	370	6	1	4	4.6	Cc1cnoc1NS(=O)(=O)c1ccccc1-c1ccc(CC(C)C)cc1	10.1021/jm970872k
	CHEMBL149060	48225	0	None	102	2	Rat	6.0	pKi	=	6.0	Binding	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	ChEMBL	370	6	1	4	4.6	Cc1cnoc1NS(=O)(=O)c1ccccc1-c1ccc(CC(C)C)cc1	10.1021/jm970872k
	5340	175509	106	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	Drug Central	255	3	2	5	1.5	Nc1ccc(S(=O)(=O)Nc2nccs2)cc1	None
	CHEMBL437	175509	106	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	Drug Central	255	3	2	5	1.5	Nc1ccc(S(=O)(=O)Nc2nccs2)cc1	None
	5329	176255	119	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	Drug Central	253	3	2	5	1.4	Cc1cc(NS(=O)(=O)c2ccc(N)cc2)no1	None
	CHEMBL443	176255	119	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	Drug Central	253	3	2	5	1.4	Cc1cc(NS(=O)(=O)c2ccc(N)cc2)no1	None
	5344	180252	101	None	-	1	Rat	8.2	pIC50	=	8.2	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	Drug Central	267	3	2	5	1.7	Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C	None
	CHEMBL453	180252	101	None	-	1	Rat	8.2	pIC50	=	8.2	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	Drug Central	267	3	2	5	1.7	Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C	None
	6662	224518	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.	Drug Central	309	3	1	6	1.6	CC(=O)N(C1=C(C)C(C)=NO1)S(=O)(=O)C1=CC=C(N)C=C1	None
	104865	7493	99	None	-	4	Pig	8.1	pIC50	=	8.1	Binding	In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.	Drug Central	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	None
	3494	7493	99	None	-	4	Pig	8.1	pIC50	=	8.1	Binding	In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.	Drug Central	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	None
	392	7493	99	None	-	4	Pig	8.1	pIC50	=	8.1	Binding	In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.	Drug Central	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	None
	CHEMBL957	7493	99	None	-	4	Pig	8.1	pIC50	=	8.1	Binding	In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.	Drug Central	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	None
	DB00559	7493	99	None	-	4	Pig	8.1	pIC50	=	8.1	Binding	In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.	Drug Central	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	None
	16004692	9232	91	None	-	0	Human	8.0	pIC50	=	8.0	Binding	IC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETAIC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETA	Drug Central	586	11	2	8	3.6	CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br	None
	4809	9232	91	None	-	0	Human	8.0	pIC50	=	8.0	Binding	IC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETAIC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETA	Drug Central	586	11	2	8	3.6	CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br	None
	7352	9232	91	None	-	0	Human	8.0	pIC50	=	8.0	Binding	IC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETAIC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETA	Drug Central	586	11	2	8	3.6	CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br	None
	CHEMBL2103873	9232	91	None	-	0	Human	8.0	pIC50	=	8.0	Binding	IC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETAIC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETA	Drug Central	586	11	2	8	3.6	CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br	None
	DB08932	9232	91	None	-	0	Human	8.0	pIC50	=	8.0	Binding	IC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETAIC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETA	Drug Central	586	11	2	8	3.6	CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br	None
	10605470	9806	0	None	-	1	Human	9.0	pKd	=	9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	823	17	3	10	6.2	COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)O)/Cc1cc(OCCCC(=O)NCCc2ccc(c(c2)I)O)c(c(c1)OC)OC	9489609
	3519	9806	0	None	-	1	Human	9.0	pKd	=	9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	823	17	3	10	6.2	COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)O)/Cc1cc(OCCCC(=O)NCCc2ccc(c(c2)I)O)c(c(c1)OC)OC	9489609
	CHEMBL2068816	9806	0	None	-	1	Human	9.0	pKd	=	9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	823	17	3	10	6.2	COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)O)/Cc1cc(OCCCC(=O)NCCc2ccc(c(c2)I)O)c(c(c1)OC)OC	9489609
	23670447	9803	2	None	114	2	Human	9.4	pKd	=	9.4	Binding	UnclassifiedUnclassified	Guide to Pharmacology	528	10	0	9	0.1	COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+]	9023329
	999	9803	2	None	114	2	Human	9.4	pKd	=	9.4	Binding	UnclassifiedUnclassified	Guide to Pharmacology	528	10	0	9	0.1	COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+]	9023329
	CHEMBL1204799	9803	2	None	114	2	Human	9.4	pKd	=	9.4	Binding	UnclassifiedUnclassified	Guide to Pharmacology	528	10	0	9	0.1	COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+]	9023329
	CHEMBL25438	9803	2	None	114	2	Human	9.4	pKd	=	9.4	Binding	UnclassifiedUnclassified	Guide to Pharmacology	528	10	0	9	0.1	COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+]	9023329
	186002	109619	23	125I-ENDOTHELIN	1	3	Human	10.5	pKi	=	10.5	Binding	NoneNone	PDSP KiDatabase	531	10	2	6	5.4	CCCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1C[C@H](C)C(=O)O)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2	None
	CHEMBL305576	109619	23	125I-ENDOTHELIN	1	3	Human	10.5	pKi	=	10.5	Binding	NoneNone	PDSP KiDatabase	531	10	2	6	5.4	CCCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1C[C@H](C)C(=O)O)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2	None
	None	222855	0	125I-ENDOTHELIN	52	2	Human	9.4	pKi	=	9.4	Binding	NoneNone	PDSP KiDatabase	520	10	2	7	4.7	CCCOC1=CC2=C(C=C1)C(C(C2C3=C(C=C(C=C3)OC)OCC(=O)O)C(=O)O)C4=CC5=C(C=C4)OCO5	None
	3075702	224111	0	125I-Endothelin 1	-2	37	Human	6.0	pKi	=	6	Binding	NoneNone	PDSP KiDatabase	198	3	1	3	1.5	C1CNC1COC2=CN=C(C=C2)Cl	None
	44208932	147485	7	UNDEFINED	-89125	37	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	475	5	1	3	6.8	Cc1ccc(Cn2nc(C(=O)NC3C4(C)CCC(C4)C3(C)C)cc2-c2ccc(Cl)c(C)c2)cc1	None
	CHEMBL381689	147485	7	UNDEFINED	-89125	37	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	475	5	1	3	6.8	Cc1ccc(Cn2nc(C(=O)NC3C4(C)CCC(C4)C3(C)C)cc2-c2ccc(Cl)c(C)c2)cc1	None
	1973	210262	15	125I-ENDOTHELIN	-3	36	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	462	3	1	7	3.9	Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12	None
	CHEMBL1394464	210262	15	125I-ENDOTHELIN	-3	36	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	462	3	1	7	3.9	Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12	None
	CHEMBL66089	210262	15	125I-ENDOTHELIN	-3	36	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	462	3	1	7	3.9	Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12	None
	None	223272	0	125I-ENDOTHELIN	-10471285	17	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	372	2	1	3	4.4	CC(C)(C)C1=CC=C(C=C1)NC(=O)N2CCN(CC2)C3=C(C=CC=N3)Cl	None
	104865	7493	99	125I-ENDOTHELIN	1	4	Human	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	None
	3494	7493	99	125I-ENDOTHELIN	1	4	Human	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	None
	392	7493	99	125I-ENDOTHELIN	1	4	Human	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	None
	CHEMBL957	7493	99	125I-ENDOTHELIN	1	4	Human	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	None
	DB00559	7493	99	125I-ENDOTHELIN	1	4	Human	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	None
	176	7186	66	None	-7	31	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)	Drug Central	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	None
	2157	7186	66	None	-7	31	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)	Drug Central	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	None
	2566	7186	66	None	-7	31	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)	Drug Central	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	None
	CHEMBL633	7186	66	None	-7	31	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)	Drug Central	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	None
	DB01118	7186	66	None	-7	31	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)	Drug Central	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	None
	1481	8847	116	None	-112	3	Human	8.3	pKi	=	8.3	Binding	Binding affinity to ETA receptorBinding affinity to ETA receptor	Drug Central	428	7	1	5	4.8	CCCCC1=NC2(C(=O)N1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)CCCC2	None
	3749	8847	116	None	-112	3	Human	8.3	pKi	=	8.3	Binding	Binding affinity to ETA receptorBinding affinity to ETA receptor	Drug Central	428	7	1	5	4.8	CCCCC1=NC2(C(=O)N1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)CCCC2	None
	589	8847	116	None	-112	3	Human	8.3	pKi	=	8.3	Binding	Binding affinity to ETA receptorBinding affinity to ETA receptor	Drug Central	428	7	1	5	4.8	CCCCC1=NC2(C(=O)N1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)CCCC2	None
	6908	8847	116	None	-112	3	Human	8.3	pKi	=	8.3	Binding	Binding affinity to ETA receptorBinding affinity to ETA receptor	Drug Central	428	7	1	5	4.8	CCCCC1=NC2(C(=O)N1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)CCCC2	None
	CHEMBL1513	8847	116	None	-112	3	Human	8.3	pKi	=	8.3	Binding	Binding affinity to ETA receptorBinding affinity to ETA receptor	Drug Central	428	7	1	5	4.8	CCCCC1=NC2(C(=O)N1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)CCCC2	None
	DB01029	8847	116	None	-112	3	Human	8.3	pKi	=	8.3	Binding	Binding affinity to ETA receptorBinding affinity to ETA receptor	Drug Central	428	7	1	5	4.8	CCCCC1=NC2(C(=O)N1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)CCCC2	None
	5472495	193412	47	None	-	1	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)	Drug Central	372	4	1	3	4.0	CC1=C(CC(=O)O)c2cc(F)ccc2/C1=C\c1ccc(S(C)(=O)=O)cc1	None
	CHEMBL488025	193412	47	None	-	1	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)	Drug Central	372	4	1	3	4.0	CC1=C(CC(=O)O)c2cc(F)ccc2/C1=C\c1ccc(S(C)(=O)=O)cc1	None
	104865	7493	99	None	1	4	Human	8.1	pKi	=	8.1	Binding	Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor	Drug Central	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	None
	3494	7493	99	None	1	4	Human	8.1	pKi	=	8.1	Binding	Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor	Drug Central	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	None
	392	7493	99	None	1	4	Human	8.1	pKi	=	8.1	Binding	Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor	Drug Central	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	None
	CHEMBL957	7493	99	None	1	4	Human	8.1	pKi	=	8.1	Binding	Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor	Drug Central	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	None
	DB00559	7493	99	None	1	4	Human	8.1	pKi	=	8.1	Binding	Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor	Drug Central	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	None
	104865	7493	99	None	-1	4	Rat	8.1	pKi	=	8.1	Binding	Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor	Drug Central	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	None
	3494	7493	99	None	-1	4	Rat	8.1	pKi	=	8.1	Binding	Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor	Drug Central	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	None
	392	7493	99	None	-1	4	Rat	8.1	pKi	=	8.1	Binding	Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor	Drug Central	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	None
	CHEMBL957	7493	99	None	-1	4	Rat	8.1	pKi	=	8.1	Binding	Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor	Drug Central	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	None
	DB00559	7493	99	None	-1	4	Rat	8.1	pKi	=	8.1	Binding	Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor	Drug Central	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	None
	104865	7493	99	125I-ENDOTHELIN	1	4	Human	8.1	pKi	=	8.1	Binding	NoneNone	PDSP KiDatabase	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	None
	3494	7493	99	125I-ENDOTHELIN	1	4	Human	8.1	pKi	=	8.1	Binding	NoneNone	PDSP KiDatabase	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	None
	392	7493	99	125I-ENDOTHELIN	1	4	Human	8.1	pKi	=	8.1	Binding	NoneNone	PDSP KiDatabase	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	None
	CHEMBL957	7493	99	125I-ENDOTHELIN	1	4	Human	8.1	pKi	=	8.1	Binding	NoneNone	PDSP KiDatabase	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	None
	DB00559	7493	99	125I-ENDOTHELIN	1	4	Human	8.1	pKi	=	8.1	Binding	NoneNone	PDSP KiDatabase	551	10	2	10	4.2	OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1	None
	11477084	10382	53	None	1	2	Human	8.0	pKi	=	8.0	Binding	Binding affinity against human Endothelin A receptorBinding affinity against human Endothelin A receptor	Drug Central	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	None
	216235	10382	53	None	1	2	Human	8.0	pKi	=	8.0	Binding	Binding affinity against human Endothelin A receptorBinding affinity against human Endothelin A receptor	Drug Central	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	None
	3548	10382	53	None	1	2	Human	8.0	pKi	=	8.0	Binding	Binding affinity against human Endothelin A receptorBinding affinity against human Endothelin A receptor	Drug Central	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	None
	3950	10382	53	None	1	2	Human	8.0	pKi	=	8.0	Binding	Binding affinity against human Endothelin A receptorBinding affinity against human Endothelin A receptor	Drug Central	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	None
	CHEMBL282724	10382	53	None	1	2	Human	8.0	pKi	=	8.0	Binding	Binding affinity against human Endothelin A receptorBinding affinity against human Endothelin A receptor	Drug Central	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	None
	DB06268	10382	53	None	1	2	Human	8.0	pKi	=	8.0	Binding	Binding affinity against human Endothelin A receptorBinding affinity against human Endothelin A receptor	Drug Central	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	None
	11477084	10382	53	None	-1	2	Rat	8.0	pKi	=	8.0	Binding	Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor	Drug Central	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	None
	216235	10382	53	None	-1	2	Rat	8.0	pKi	=	8.0	Binding	Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor	Drug Central	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	None
	3548	10382	53	None	-1	2	Rat	8.0	pKi	=	8.0	Binding	Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor	Drug Central	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	None
	3950	10382	53	None	-1	2	Rat	8.0	pKi	=	8.0	Binding	Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor	Drug Central	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	None
	CHEMBL282724	10382	53	None	-1	2	Rat	8.0	pKi	=	8.0	Binding	Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor	Drug Central	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	None
	DB06268	10382	53	None	-1	2	Rat	8.0	pKi	=	8.0	Binding	Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor	Drug Central	454	6	1	8	4.0	O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C	None
	3951	7179	86	None	-1	2	Human	8.0	pKi	=	8.0	Binding	NoneNone	Drug Central	378	7	1	5	3.5	COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1	None
	4337	7179	86	None	-1	2	Human	8.0	pKi	=	8.0	Binding	NoneNone	Drug Central	378	7	1	5	3.5	COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1	None
	6918493	7179	86	None	-1	2	Human	8.0	pKi	=	8.0	Binding	NoneNone	Drug Central	378	7	1	5	3.5	COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1	None
	CHEMBL1111	7179	86	None	-1	2	Human	8.0	pKi	=	8.0	Binding	NoneNone	Drug Central	378	7	1	5	3.5	COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1	None
	DB06403	7179	86	None	-1	2	Human	8.0	pKi	=	8.0	Binding	NoneNone	Drug Central	378	7	1	5	3.5	COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1	None
	12286	7735	36	None	1348	2	Human	9.9	pKi	=	9.9	Binding	Binding affinity measured as displacement of ET-1 from CHO cells expressing hET<sub>A</sub>Binding affinity measured as displacement of ET-1 from CHO cells expressing hET<sub>A</sub>	Guide to Pharmacology	577	11	3	13	2.4	Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC	9703472
	6433095	7735	36	None	1348	2	Human	9.9	pKi	=	9.9	Binding	Binding affinity measured as displacement of ET-1 from CHO cells expressing hET<sub>A</sub>Binding affinity measured as displacement of ET-1 from CHO cells expressing hET<sub>A</sub>	Guide to Pharmacology	577	11	3	13	2.4	Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC	9703472
	CHEMBL109648	7735	36	None	1348	2	Human	9.9	pKi	=	9.9	Binding	Binding affinity measured as displacement of ET-1 from CHO cells expressing hET<sub>A</sub>Binding affinity measured as displacement of ET-1 from CHO cells expressing hET<sub>A</sub>	Guide to Pharmacology	577	11	3	13	2.4	Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC	9703472
	DB06677	7735	36	None	1348	2	Human	9.9	pKi	=	9.9	Binding	Binding affinity measured as displacement of ET-1 from CHO cells expressing hET<sub>A</sub>Binding affinity measured as displacement of ET-1 from CHO cells expressing hET<sub>A</sub>	Guide to Pharmacology	577	11	3	13	2.4	Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC	9703472
	159594	7310	45	None	1	3	Human	10.5	pKi	=	10.5	Binding	CHO cells expressing human ET<sub>A</sub> receptor.CHO cells expressing human ET<sub>A</sub> receptor.	Guide to Pharmacology	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	8632312
	159594	7310	45	None	1	3	Human	10.5	pKi	=	10.5	Binding	CHO cells expressing human ET<sub>A</sub> receptor.CHO cells expressing human ET<sub>A</sub> receptor.	Guide to Pharmacology	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	8676339
	3487	7310	45	None	1	3	Human	10.5	pKi	=	10.5	Binding	CHO cells expressing human ET<sub>A</sub> receptor.CHO cells expressing human ET<sub>A</sub> receptor.	Guide to Pharmacology	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	8632312
	3487	7310	45	None	1	3	Human	10.5	pKi	=	10.5	Binding	CHO cells expressing human ET<sub>A</sub> receptor.CHO cells expressing human ET<sub>A</sub> receptor.	Guide to Pharmacology	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	8676339
	CHEMBL9194	7310	45	None	1	3	Human	10.5	pKi	=	10.5	Binding	CHO cells expressing human ET<sub>A</sub> receptor.CHO cells expressing human ET<sub>A</sub> receptor.	Guide to Pharmacology	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	8632312
	CHEMBL9194	7310	45	None	1	3	Human	10.5	pKi	=	10.5	Binding	CHO cells expressing human ET<sub>A</sub> receptor.CHO cells expressing human ET<sub>A</sub> receptor.	Guide to Pharmacology	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	8676339
	DB06199	7310	45	None	1	3	Human	10.5	pKi	=	10.5	Binding	CHO cells expressing human ET<sub>A</sub> receptor.CHO cells expressing human ET<sub>A</sub> receptor.	Guide to Pharmacology	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	8632312
	DB06199	7310	45	None	1	3	Human	10.5	pKi	=	10.5	Binding	CHO cells expressing human ET<sub>A</sub> receptor.CHO cells expressing human ET<sub>A</sub> receptor.	Guide to Pharmacology	510	12	1	6	4.7	CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC	8676339
	13015	8312	30	None	-	1	Human	11.0	pKi	=	11	Binding	UnclassifiedUnclassified	Guide to Pharmacology	536	8	1	7	5.8	CC1=C(ON=C1NS(=O)(=O)C2=CC=CC=C2C3=C(C=C(C=C3)C4=NC=CO4)CN(C)C(=O)CC(C)(C)C)C	12502366
	156690	8312	30	None	-	1	Human	11.0	pKi	=	11	Binding	UnclassifiedUnclassified	Guide to Pharmacology	536	8	1	7	5.8	CC1=C(ON=C1NS(=O)(=O)C2=CC=CC=C2C3=C(C=C(C=C3)C4=NC=CO4)CN(C)C(=O)CC(C)(C)C)C	12502366
	CHEMBL383581	8312	30	None	-	1	Human	11.0	pKi	=	11	Binding	UnclassifiedUnclassified	Guide to Pharmacology	536	8	1	7	5.8	CC1=C(ON=C1NS(=O)(=O)C2=CC=CC=C2C3=C(C=C(C=C3)C4=NC=CO4)CN(C)C(=O)CC(C)(C)C)C	12502366
	10257882	10418	43	None	-11	2	Human	8.0	pKi	=	8.0	Binding	UnclassifiedUnclassified	Guide to Pharmacology	592	12	1	7	6.5	CCCCC1=NC2(C(=O)N1Cc1ccc(c(c1)COCC)c1ccccc1S(=O)(=O)Nc1noc(c1C)C)CCCC2	16220969
	8448	10418	43	None	-11	2	Human	8.0	pKi	=	8.0	Binding	UnclassifiedUnclassified	Guide to Pharmacology	592	12	1	7	6.5	CCCCC1=NC2(C(=O)N1Cc1ccc(c(c1)COCC)c1ccccc1S(=O)(=O)Nc1noc(c1C)C)CCCC2	16220969
	CHEMBL539423	10418	43	None	-11	2	Human	8.0	pKi	=	8.0	Binding	UnclassifiedUnclassified	Guide to Pharmacology	592	12	1	7	6.5	CCCCC1=NC2(C(=O)N1Cc1ccc(c(c1)COCC)c1ccccc1S(=O)(=O)Nc1noc(c1C)C)CCCC2	16220969
	DB12548	10418	43	None	-11	2	Human	8.0	pKi	=	8.0	Binding	UnclassifiedUnclassified	Guide to Pharmacology	592	12	1	7	6.5	CCCCC1=NC2(C(=O)N1Cc1ccc(c(c1)COCC)c1ccccc1S(=O)(=O)Nc1noc(c1C)C)CCCC2	16220969
	13016	7457	13	None	1	4	Human	8.9	pKi	=	8.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	395	5	1	6	4.4	CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4	10956219
	9843631	7457	13	None	1	4	Human	8.9	pKi	=	8.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	395	5	1	6	4.4	CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4	10956219
	CHEMBL24461	7457	13	None	1	4	Human	8.9	pKi	=	8.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	395	5	1	6	4.4	CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4	10956219
	177236	8107	45	None	2	3	Human	8.9	pKi	=	8.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	410	9	1	7	2.9	COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1	8667356
	3508	8107	45	None	2	3	Human	8.9	pKi	=	8.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	410	9	1	7	2.9	COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1	8667356
	CHEMBL23261	8107	45	None	2	3	Human	8.9	pKi	=	8.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	410	9	1	7	2.9	COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1	8667356
	DB04883	8107	45	None	2	3	Human	8.9	pKi	=	8.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	410	9	1	7	2.9	COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1	8667356

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Ligand source activities (1 row/activity)