Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
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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 8661 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 8661 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 204977 34 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 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 204977 34 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 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 2968 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 2968 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 2968 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 2968 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 109471 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 109471 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 9248 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 9248 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 110102 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 110102 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 702 40 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
997 702 40 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 702 40 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 702 40 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 210757 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 111815 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 111815 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 167329 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 167329 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 162815 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 162815 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 211262 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 112068 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 112068 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 9227 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 9227 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 75853 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 75853 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 75854 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 75854 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 106711 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 106711 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 206113 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 206113 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 98191 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 98191 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 4218 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 4218 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 206084 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 206084 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 205758 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 205758 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 206120 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 206120 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 210633 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 210800 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 210828 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 210993 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 122033 7 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 122033 7 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 75855 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 75855 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 206100 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 206100 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 205805 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 205805 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 5343 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 5343 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 123562 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 123562 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 111060 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 111060 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 214056 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 5073 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 5073 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 5073 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 5073 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 112180 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 112180 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 97669 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 97669 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 4482 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 4482 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 206108 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 206108 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 206057 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 206057 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 205782 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 205782 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 105707 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 105707 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 112155 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 112155 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 123561 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 123561 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 214138 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 209578 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 209578 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 9254 1 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 9254 1 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 4683 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 4683 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 210811 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 5343 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 5343 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 205803 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 205803 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 205783 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 205783 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 205463 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 205463 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 209105 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 106923 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 106923 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 208880 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
10166981 205349 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 205349 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 206045 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 206045 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 206050 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 206050 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 206089 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 206089 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 105709 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 105709 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 9034 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 9034 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 141245 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 141245 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 206077 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 206077 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 206155 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 206155 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 210965 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 9307 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 9307 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 209463 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 211029 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 205777 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 205777 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 8155 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 8155 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 111857 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 111857 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 205342 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 205342 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 106951 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 106951 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 205815 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 205815 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 208810 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 7742 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 7742 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 4623 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 4623 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 208617 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 388 82 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 388 82 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 388 82 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 388 82 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 388 82 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 209442 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 214133 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 168591 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 168591 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 75847 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 75847 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 112172 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 112172 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 7742 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 7742 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 96596 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 96596 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 205691 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 205691 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 206188 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 206188 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 205816 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 205816 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 109321 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 109321 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 208807 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 98305 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 98305 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 106743 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 106743 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 206079 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 206079 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 205844 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 205844 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 206046 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 206046 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 205606 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 205606 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 211882 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 4624 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 4624 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 108062 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 108062 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 205806 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 205806 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 209464 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 211077 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 211209 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 106680 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 106680 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 206190 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 206190 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 161315 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 161315 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 206158 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 206158 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 205643 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 205643 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 206054 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 206054 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 214129 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 167357 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 167357 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 167302 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 167302 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 9034 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 9034 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 9307 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 9307 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 99328 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 99328 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 214137 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 100076 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 100076 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 111898 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 111898 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
11362537 107022 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 107022 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 206090 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 206090 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 172146 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 172146 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 75846 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 75846 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 111007 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 111007 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 207135 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 209133 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 211090 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 106750 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 106750 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 99589 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 99589 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 96099 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 96099 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 98024 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 98024 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 214127 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 96596 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 96596 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 208064 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 211879 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 208063 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 111799 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 111799 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 112156 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 112156 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 209453 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 205764 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 205764 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 112172 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 112172 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 97669 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 97669 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 208857 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 210640 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 205712 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 205712 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 111039 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 111039 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 106426 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 106426 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 210967 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 4658 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 4658 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 97770 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 97770 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 4658 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 4658 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 211200 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 206142 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 206142 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 98024 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 98024 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 4235 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 4235 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 96637 23 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 96637 23 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 8528 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 8528 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 78239 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 78239 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 108062 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 108062 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 106381 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 106381 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 208616 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 211887 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 214059 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 106945 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 106945 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 8155 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 8155 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 106832 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 106832 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 106844 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 106844 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 205854 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 205854 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 163093 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 163093 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 205530 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 205530 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 205845 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 205845 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 162780 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 162780 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 205756 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 205756 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 206166 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 206166 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 155757 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 155757 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 111501 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 111501 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 9254 1 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 9254 1 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 209562 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 112059 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 112059 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 112286 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 112286 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 167307 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 167307 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 99823 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 99823 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 99364 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 99364 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 96304 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 96304 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 206179 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 206179 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 162886 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 162886 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 205840 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 205840 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 206082 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 206082 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 106665 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 106665 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 97770 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 97770 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 167593 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 167593 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 112074 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 112074 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 107799 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 107799 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 164316 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 164316 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 205855 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 205855 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 209465 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 209560 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 5183 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 5183 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 4482 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 4482 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 75845 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 75845 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 142050 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 142050 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 8528 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 8528 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 106738 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 106738 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 4102 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 4102 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 101625 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 101625 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 208901 13 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 209027 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 697 94 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 697 94 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
392 697 94 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 697 94 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 697 94 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 75850 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 75850 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 106452 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 106452 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 4295 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 4295 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 112043 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 112043 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 207562 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 4102 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 4102 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 106716 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 106716 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 9227 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 9227 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 107133 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 107133 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 205867 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 205867 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 75849 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 75849 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 75851 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 75851 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 75848 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 75848 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 75852 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 75852 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 4218 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 4218 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 206086 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 206086 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 206123 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 206123 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 5183 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 5183 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 206094 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 206094 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 75844 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 75844 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 202399 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 202399 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 202419 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 202419 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 202694 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 202694 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 202385 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 202385 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 202400 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 202400 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 202409 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 202409 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 202414 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 202414 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 61865 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 61865 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 60135 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 60135 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 101816 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 101816 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 129204 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 129204 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 96784 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 96784 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 205833 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 205833 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 129137 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 129137 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 202534 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 202534 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 102675 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 102675 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 207157 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 208619 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 202432 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 202432 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 98007 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 98007 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 205810 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 205810 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 96235 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 96235 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 56214 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 56214 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 61759 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 61759 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 130805 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 130805 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 204977 34 None -1 4 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 204977 34 None -1 4 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 101850 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 101850 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 2968 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 2968 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 2968 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 2968 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 130854 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 130854 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 130163 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 130163 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 129206 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 129206 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 59281 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 59281 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 204972 6 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 204972 6 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 204972 6 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 14446 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 14446 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 14446 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 130614 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 130614 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 129203 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 129203 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 101905 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 101905 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 61042 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 61042 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 59307 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 59307 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 208620 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 193937 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 193937 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 130162 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 130162 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 130027 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 130027 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 202507 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 202507 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 697 94 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 697 94 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
392 697 94 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 697 94 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 697 94 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 119300 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 119300 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 60993 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 60993 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 211110 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 128150 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 128150 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 128512 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 128512 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 106777 3 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 106777 3 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 112178 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 112178 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 198316 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 198316 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 59370 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 59370 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 60078 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 60078 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 60028 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 60028 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 697 94 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 697 94 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
392 697 94 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 697 94 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 697 94 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 59300 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 59300 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 131622 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 131622 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 129691 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 129691 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 176436 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 176436 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 445 41 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 445 41 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 445 41 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 445 41 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 388 82 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 388 82 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 388 82 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 388 82 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 388 82 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 702 40 None 1 4 Human 7.2 pA2 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7647976
997 702 40 None 1 4 Human 7.2 pA2 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7647976
CHEMBL314691 702 40 None 1 4 Human 7.2 pA2 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7647976
DB12054 702 40 None 1 4 Human 7.2 pA2 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7647976
104865 697 94 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 697 94 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
392 697 94 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 697 94 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 697 94 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 3540 46 None 20 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 3540 46 None 20 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 3540 46 None 20 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 3540 46 None 20 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 3540 46 None 20 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 3540 46 None 20 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 3668 0 None -1 2 Rat 8.4 pA2 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7780649
5311469 3668 0 None -1 2 Rat 8.4 pA2 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7780649
23670447 2968 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 2968 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 2968 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 2968 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 2968 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 2968 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 2968 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 2968 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 518 38 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 518 38 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 518 38 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 518 38 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 933 30 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 933 30 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 933 30 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 933 30 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 168154 104 None 1 2 Human 8.4 pIC50 = 8.4 Functional
NoneNone
Drug Central 255 3 2 5 1.5 Nc1ccc(S(=O)(=O)Nc2nccs2)cc1 None
CHEMBL437 168154 104 None 1 2 Human 8.4 pIC50 = 8.4 Functional
NoneNone
Drug Central 255 3 2 5 1.5 Nc1ccc(S(=O)(=O)Nc2nccs2)cc1 None
5344 172891 98 None -100 5 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 172891 98 None -100 5 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 216009 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 527 46 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 527 46 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 527 46 None 141